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Tcipatent Report 2016 - Weeks 33 to 36

Reports comprise records taken from the Online Database. Report Types:- 4-Weekly Reports published every 4 weeks showing the latest records added to the database – text-searchable PDFs, published since 1 January 2014. Back issues available. Bespoke Reports from the Database using selected criteria, e.g. by Drug, Patentee etc. (contact us for prices) Sample report contents: Alectinib, Alogliptin, Apixaban, Bisoprolol, Canagliflozin, Canagliflozin ( Dapagliflozin Empagliflozin Ipragliflozin ) , Ceftaroline fosamil, Ceritinib, Cobicistat, Dabigatran etexilate, Efavirenz, Eluxadoline, Eslicarbazepine acetate, Esomeprazole, Ibrutinib, Ibrutinib, Methionine, Perampanel, Pimavanserin, Praziquantel, Sacubitril, Sacubitril, Silodosin, Tofacitinib, Topiroxostat, Vilazodone, Vorapaxar, Vortioxetine

Reports comprise records taken from the Online Database. Report Types:-

4-Weekly Reports published every 4 weeks showing the latest records added to the database – text-searchable PDFs, published since 1 January 2014. Back issues available.
Bespoke Reports from the Database using selected criteria, e.g. by Drug, Patentee etc. (contact us for prices)

Sample report contents:

Alectinib, Alogliptin, Apixaban, Bisoprolol, Canagliflozin, Canagliflozin ( Dapagliflozin Empagliflozin Ipragliflozin ) , Ceftaroline fosamil, Ceritinib, Cobicistat, Dabigatran etexilate, Efavirenz, Eluxadoline, Eslicarbazepine acetate, Esomeprazole, Ibrutinib, Ibrutinib, Methionine, Perampanel, Pimavanserin, Praziquantel, Sacubitril, Sacubitril, Silodosin, Tofacitinib, Topiroxostat, Vilazodone, Vorapaxar, Vortioxetine

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Marketed Drug Process Patent <strong>Report</strong><br />

[Extracted from the Claimed Intermediate Structure Searchable Database]<br />

Second Quarter, April <strong>to</strong> June 2017<br />

© The Claimed Intermediate • www.tcipatent.com


This Marketed Drug Process Patent <strong>Report</strong> has been extracted from the<br />

Claimed Intermediate Structure Searchable Database<br />

The Database contains some <strong>36</strong>00+ Text/Structure Searchable Syntheses since January 2010.<br />

The <strong>Report</strong>s cover new DE, FR, GB, US and WO patent specifications.<br />

Equivalent specifications are not included but may be obtained from free and commercial databases.<br />

Due <strong>to</strong> the vagaries of Patent Classification systems some relevant specifications may be missed.<br />

However, these and other omissions will be included as noted or pointed out.<br />

The Database provides details of 17600+ exemplary Intermediates used in Process Patents.<br />

Bespoke <strong>Report</strong>s can be supplied by Drug, Patentee or Period.<br />

For more information or a subscription contact info@tcipatent.com<br />

www.tcipatent.com<br />

Tel:+44(0)1273 7<strong>36</strong>080<br />

© <strong>Tcipatent</strong> Ltd • www.tcipatent.com


Contents: Quarter 2, April <strong>to</strong> June 2017<br />

Page<br />

1<br />

2<br />

3<br />

4<br />

5<br />

6<br />

7<br />

8<br />

9<br />

10<br />

11<br />

12<br />

13<br />

14<br />

15<br />

16<br />

17<br />

18<br />

19<br />

20<br />

21<br />

22<br />

Drug Name<br />

Apremilast<br />

Apremilast<br />

Apremilast<br />

Apremilast<br />

Armodafinil<br />

Baricitinib<br />

Barnidipine<br />

Brexpiprazole<br />

Brexpiprazole<br />

Brivaracetam<br />

Brivaracetam<br />

Buprenorphine<br />

Canagliflozin<br />

Canagliflozin<br />

Canagliflozin<br />

Canagliflozin<br />

Canagliflozin<br />

Canagliflozin<br />

Cangrelor<br />

Carboprost<br />

Carfilzomib<br />

Cariprazine<br />

Patentee<br />

Alembic Pharmaceuticals Limited<br />

Pliva Hrvatska D.O.O. and Teva Pharmaceuticals USA, Inc.<br />

Sun Pharmaceutical Industries Limited<br />

Zaklady Farmaceutyczne Polpharma SA<br />

Natco Pharma Ltd<br />

Egis Gyogyszergyar ZRT.<br />

USV Private Limited<br />

Crystal Pharma S.A.U<br />

Scinopharm Taiwan, Ltd.<br />

UCB Biopharma SPRL<br />

UCB Biopharma SPRL<br />

Noramco, Inc.<br />

Dr. Reddy's Labora<strong>to</strong>ries Limited<br />

Harman Finochem Limited<br />

Lupin Limited<br />

Zaklady Farmaceutyczne Polpharma SA<br />

Zentiva, K.S.<br />

Zentiva, K.S.<br />

Jiangsu Hengrui Medicine Co., Ltd. and Suncadia Pharmaceuticals Co., Ltd<br />

Chinoin Gyogyszer es Vegyeszeti Termekek Gyara ZRT.<br />

Mylan Labora<strong>to</strong>ries Limited<br />

Suzhou Miracpharma Technology Co., Ltd


Contents: Quarter 2, April <strong>to</strong> June 2017<br />

Page<br />

23<br />

24<br />

25<br />

26<br />

27<br />

28<br />

29<br />

30<br />

31<br />

32<br />

<strong>33</strong><br />

34<br />

35<br />

<strong>36</strong><br />

37<br />

38<br />

39<br />

40<br />

41<br />

42<br />

43<br />

44<br />

Drug Name<br />

Cobimetinib<br />

Dapagliflozin<br />

Dapagliflozin<br />

Dasatinib<br />

Dolutegravir<br />

Droxidopa<br />

Efinaconazole<br />

Eliglustat<br />

Eltrombopag<br />

Enzalutamide<br />

Epirubicin<br />

Fexofenadine<br />

Flibanserin<br />

Flurbiprofen<br />

Flutemetamol<br />

Fosaprepitant<br />

Fulvestrant<br />

Gadoteric acid<br />

Hydrocodone<br />

Ibrutinib<br />

Idelalisib<br />

Indacaterol<br />

Patentee<br />

Suzhou Miracpharma Technology Co., Ltd<br />

Harman Finochem Limited<br />

Zentiva, K.S.<br />

Shilpa Medicare Limited<br />

Lupin Limited<br />

Quimica Sintetica, S.A.<br />

Virupaksha Organics Limited<br />

Dr. Reddy's Labora<strong>to</strong>ries Limited<br />

Amneal Pharmaceuticals Company GmbH<br />

Sun Pharmaceutical Industries Limited<br />

Zhejiang Hisun Pharmaceutical Co., Ltd. and Shanghai Institute of Pharmaceutical Industry<br />

Sanofi-Aventis Deutschland GmbH<br />

Vigonvita Life Sciences Suzhou Co., Ltd. and Shanghai Institute of Materia Medica, Chines Academy of Sci<br />

Taisho Pharmaceutical Co., Ltd.<br />

GE Healthcare Limited and Nihon Medi-Physics Co., Ltd<br />

Piramal Enterprises Limited<br />

Natco Pharma Ltd<br />

GE Healthcare AS<br />

Noramco Inc.<br />

Scinopharm Taiwan, Ltd.<br />

Egis Gyogyszergyar ZRT.<br />

Labora<strong>to</strong>rios Lesvi, S.L.


Contents: Quarter 2, April <strong>to</strong> June 2017<br />

Page<br />

45<br />

46<br />

47<br />

48<br />

49<br />

50<br />

51<br />

52<br />

53<br />

54<br />

55<br />

56<br />

57<br />

58<br />

59<br />

60<br />

61<br />

62<br />

63<br />

64<br />

65<br />

66<br />

Drug Name<br />

Indacaterol<br />

Indocyanine green<br />

Ivacaf<strong>to</strong>r<br />

Labetalol<br />

Lacosamide<br />

Ledipasvir<br />

Lisdexamfetamine<br />

Lisinopril<br />

Lomitapide<br />

Luliconazole<br />

Luliconazole<br />

Lumacaf<strong>to</strong>r<br />

Macitentan<br />

Nintedanib<br />

Obeticholic acid<br />

Obeticholic acid<br />

Olmutinib<br />

Omarigliptin<br />

Omarigliptin<br />

Pimavanserin<br />

Pimecrolimus<br />

Pirfenidone<br />

Patentee<br />

Olon S.P.A.<br />

Dishman Pharmaceuticals and Chemicals Limited<br />

Optimus Drugs Private Limited<br />

Davaluri Ramamohan Rao<br />

API Corporation<br />

Optimus Drugs (P) Ltd<br />

Sun Pharmaceutical Industries Limited<br />

Zhejiang Huahai Pharmaceuticals Co., Ltd.<br />

MSN Labor<strong>to</strong>ries Private Limited<br />

Labora<strong>to</strong>rios Lesvi, S.L.<br />

Pola Pharma Inc. and Nihon Nohyaku Co., Ltd.<br />

Glenmark Pharmaceuticals Limited<br />

Laurus Labs Private Limited<br />

Mylan Labora<strong>to</strong>ries Limited<br />

Intercept Pharmaceuticals Inc.<br />

Intercept Pharmaceuticals, Inc<br />

Hanmi Pharm. Co., Ltd.<br />

F.I.S. - Fabbrica Italiana Sintetici S.P.A.<br />

Sun Pharmaceutical Industries Limited<br />

Zentiva, K.S.<br />

Medichem, S.A. and BrightGene Bio-Medical Technology Co., Ltd.<br />

Procos S.p.A.


Contents: Quarter 2, April <strong>to</strong> June 2017<br />

Page<br />

67<br />

68<br />

69<br />

70<br />

71<br />

72<br />

73<br />

74<br />

75<br />

76<br />

77<br />

78<br />

79<br />

80<br />

81<br />

82<br />

83<br />

84<br />

85<br />

86<br />

87<br />

88<br />

Drug Name<br />

Riociguat<br />

Rivaroxaban<br />

Romidepsin<br />

Sacubitril<br />

Sacubitril<br />

Sacubitril<br />

Saroglitazar<br />

Selexipag<br />

Silodosin<br />

Silodosin<br />

Simeprevir<br />

Sitagliptin<br />

Sofosbuvir<br />

Sofosbuvir<br />

Sonidegib<br />

Tedizolid<br />

Tedizolid<br />

Teriflunomide<br />

Tes<strong>to</strong>sterone<br />

Thalidomide<br />

Ticagrelor<br />

Valbenazine<br />

Patentee<br />

Alembic Pharmaceuticals Limited<br />

Lonza Ltd<br />

MSN Labora<strong>to</strong>ries Private Limited and Venkat Reddy, Ghojala<br />

Chiral Quest (Suzhou) Co., Ltd. and Jiangxi Long Life Bio-Pharmaceutical Co., Ltd.<br />

Novartis AG<br />

Zentiva, K.S.<br />

Cadila Healthcare Limited<br />

Lupin Limited<br />

Huang, Huan<br />

Urquima, S.A.<br />

Lupin Limited<br />

F.I.S. - Fabbrica Italiana Sintetici S.p.A.<br />

Mylan Labora<strong>to</strong>ries Limited<br />

Sun Pharmaceutical Industries Limited<br />

Suzhou Miracpharma Technology Co., Ltd<br />

St Pharm Co., Ltd.<br />

Zheijiang Huahai Pharmaceutical Co., Ltd. and Shanghai Syncores Technologies Inc. Ltd.<br />

Natco Pharma Ltd<br />

Lupin Limited<br />

Natco Pharma Ltd<br />

Avra labora<strong>to</strong>ries Pvt. Ltd.<br />

Neurocrine Biosciences, Inc.


Contents: Quarter 2, April <strong>to</strong> June 2017<br />

Page<br />

89<br />

90<br />

Drug Name<br />

Velpatasvir<br />

Voriconazole<br />

Patentee<br />

Mylan Labora<strong>to</strong>ries Limited<br />

Zhejiang Huahai Pharmaceutical Co., Ltd


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Apremilast<br />

Patent Specification<br />

Number: WO 2017/085568<br />

Publication Date:<br />

2017-05-26<br />

First Filing<br />

Priority Details: 20151119IN4347/MUM<br />

Patentee: Alembic Pharmaceuticals Limited<br />

Patent Description: Apremilast is obtained via the preparation of claimed intermediates 3 and 4. X-ray defined crystalline form Al-1 apremilast benzyl alcohol solvate is claimed.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 1


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Apremilast<br />

Patent Specification<br />

Number: WO 2017/059040<br />

Publication Date:<br />

2017-04-06<br />

First Filing<br />

Priority Details: 20150929US62/234094<br />

Patentee: Pliva Hrvatska D.O.O. and Teva Pharmaceuticals USA, Inc.<br />

Patent Description: Apremilast is obtained via prepared claimed intermediates IV, V, VI and VIII. Other process intermediates are claimed.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 2


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Apremilast<br />

Patent Specification<br />

Number: WO 2017/094031<br />

Publication Date:<br />

2017-06-08<br />

First Filing<br />

Priority Details: 20151204IN4599/MUM<br />

Patentee: Sun Pharmaceutical Industries Limited<br />

Patent Description: Apremilast is obtained via the preparation of claimed intermediate II and enantiomers thereof.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 3


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Apremilast<br />

Patent Specification<br />

Number: EP 3181549<br />

Publication Date:<br />

2017-06-21<br />

First Filing<br />

Priority Details: 20151217EP460122<br />

Patentee: Zaklady Farmaceutyczne Polpharma SA<br />

Patent Description: Apremilast is obtained via the reaction shown in the absence of acetic or formic acid.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 4


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Armodafinil<br />

Patent Specification<br />

Number: WO 2017/064723<br />

Publication Date:<br />

2017-04-20<br />

First Filing<br />

Priority Details: 20151012IN5455/CHE<br />

Patentee: Natco Pharma Ltd<br />

Patent Description: Armodafinil is obtained via resolution with (S)-(-)-alpha-methylbenzylamine. Armodafinil polymorphic form 1 of defined particle size is claimed.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 5


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Baricitinib<br />

Patent Specification<br />

Number: WO 2017/109524<br />

Publication Date:<br />

2017-06-29<br />

First Filing<br />

Priority Details: 20151223HU647<br />

Patentee: Egis Gyogyszergyar ZRT.<br />

Patent Description: Baricitinib is obtained via prepared claimed intermediates I and II and salts as defined.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 6


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Barnidipine<br />

Patent Specification<br />

Number: EP 3168215<br />

Publication Date:<br />

2017-05-17<br />

First Filing<br />

Priority Details: 20151110IN4298/MU<br />

Patentee: USV Private Limited<br />

Patent Description: Barnidipine is obtained via the preparation of claimed intermediate IIIa and analogues as defined.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 7


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Brexpiprazole<br />

Patent Specification<br />

Number: EP 3150591<br />

Publication Date:<br />

2017-04-05<br />

First Filing<br />

Priority Details: 20151002EP382479<br />

Patentee: Crystal Pharma S.A.U<br />

Patent Description: Brexpiprazole is obtained via prepared claimed intermediates IV and III and analogues as defined. Other process intermediates are claimed.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 8


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Brexpiprazole<br />

Patent Specification<br />

Number: WO 2017/078621<br />

Publication Date:<br />

2017-05-11<br />

First Filing<br />

Priority Details: 20151103US62/250248<br />

Patentee: Scinopharm Taiwan, Ltd.<br />

Patent Description: Brexpiprazole is obtained via the reaction of prepared intermediate XIV and intermediate XV in the presence of a reducing agent and an organic solvent.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 9


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Brivaracetam<br />

Patent Specification<br />

Number: WO 2017/076737<br />

Publication Date:<br />

2017-05-11<br />

First Filing<br />

Priority Details: 20151103EP192758<br />

Patentee: UCB Biopharma SPRL<br />

Patent Description: Brivaracetam is obtained in three steps in an integrated continuous flow system.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 10


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Brivaracetam<br />

Patent Specification<br />

Number: WO 2017/076738<br />

Publication Date:<br />

2017-05-11<br />

First Filing<br />

Priority Details: 20151103EP192760<br />

Patentee: UCB Biopharma SPRL<br />

Patent Description: Brivaracetam is obtained via an asymmetric catalytic hydrogenation step.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 11


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Buprenorphine<br />

Patent Specification<br />

Number: US 2017/0101415<br />

Publication Date:<br />

2017-04-13<br />

First Filing<br />

Priority Details: 20151012US62/240329<br />

Patentee: Noramco, Inc.<br />

Patent Description: Buprenorphine is obtained from thebaine via the preparation of intermediate I.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 12


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Canagliflozin<br />

Patent Specification<br />

Number: WO 2017/093949<br />

Publication Date:<br />

2017-06-08<br />

First Filing<br />

Priority Details: 20151204IN6500/CHE<br />

Patentee: Dr. Reddy's Labora<strong>to</strong>ries Limited<br />

Patent Description: Canagliflozin is obtained via prepared substantially purified intermediate 18a'.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 13


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Canagliflozin<br />

Patent Specification<br />

Number: WO 2017/060924<br />

Publication Date:<br />

2017-04-13<br />

First Filing<br />

Priority Details: 20151009IN3838/MUM<br />

Patentee: Harman Finochem Limited<br />

Patent Description: Canagliflozin is obtained via the prepared and isolated claimed intermediate A and the prop-2-ynyl analogue as defined.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 14


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Canagliflozin<br />

Patent Specification<br />

Number: WO 2017/064679<br />

Publication Date:<br />

2017-04-20<br />

First Filing<br />

Priority Details: 20151015IN3921/MUM<br />

Patentee: Lupin Limited<br />

Patent Description: Canagliflozin is obtained and purified via conversion <strong>to</strong> L-proline co-crystal.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 15


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Canagliflozin<br />

Patent Specification<br />

Number: WO 2017/071813<br />

Publication Date:<br />

2017-05-04<br />

First Filing<br />

Priority Details: 20151030EP460103<br />

Patentee: Zaklady Farmaceutyczne Polpharma SA<br />

Patent Description: Canagliflozin is obtained via the reaction of a bromo-intermediate with a protected pyran-2-one intermediate followed by deprotection and reduction <strong>to</strong> product.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 16


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Canagliflozin<br />

Patent Specification<br />

Number: WO 2017/084644<br />

Publication Date:<br />

2017-05-26<br />

First Filing<br />

Priority Details: 20151120CZ824<br />

Patentee: Zentiva, K.S.<br />

Patent Description: Canagliflozin is obtained via deacetylation of canagliflozin tetraacetate in methanol in the presence of sodium methoxide. X-ray defined crystalline Form X-C of canagliflozin<br />

is claimed.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 17


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Canagliflozin<br />

Patent Specification<br />

Number: WO 2017/06<strong>36</strong>17<br />

Publication Date:<br />

2017-04-20<br />

First Filing<br />

Priority Details: 20151013CZ729<br />

Patentee: Zentiva, K.S.<br />

Patent Description: Canagliflozin is obtained via the preparation of intermediate 1a employing a lithium magnesate complex. Dapagliflozin is also prepared.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 18


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Cangrelor<br />

Patent Specification<br />

Number: WO 2017/076266<br />

Publication Date:<br />

2017-05-11<br />

First Filing<br />

Priority Details: 20151106CN10752115<br />

Patentee: Jiangsu Hengrui Medicine Co., Ltd. and Suncadia Pharmaceuticals Co., Ltd<br />

Patent Description: Cangrelor is obtained via the reaction of a 2-halogenated adenosine intermediate XI with a 3,3,3-trifluoropropyl sulfide.<br />

Significant Step:<br />

Claimed Comment: Not Clear<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 19


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Carboprost<br />

Patent Specification<br />

Number: WO 2017/093770<br />

Publication Date:<br />

2017-06-08<br />

First Filing<br />

Priority Details: 20151201HU584<br />

Patentee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara ZRT.<br />

Patent Description: Carboprost is obtained via a selective alkylation of a protected intermediate, an enol reduction, deprotection and a Wittig reaction. Chroma<strong>to</strong>graphic epimer separation is<br />

obtained by the preparation of carboprost methyl.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 20


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Carfilzomib<br />

Patent Specification<br />

Number: WO 2017/098532<br />

Publication Date:<br />

2017-06-15<br />

First Filing<br />

Priority Details: 20151211IN6647/CHE<br />

Patentee: Mylan Labora<strong>to</strong>ries Limited<br />

Patent Description: Carfilzomib is obtained as shown. X-ray defined crystalline carfilzomib form M1 is claimed.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 21


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Cariprazine<br />

Patent Specification<br />

Number: WO 2017/096997<br />

Publication Date:<br />

2017-06-15<br />

First Filing<br />

Priority Details: 20151209CN10906807<br />

Patentee: Suzhou Miracpharma Technology Co., Ltd<br />

Patent Description: Cariprazine is obtained via a reducing ammonolysis <strong>to</strong> produce a trans-intermediate.<br />

Significant Step:<br />

Claimed Comment: Not Clear<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 22


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Cobimetinib<br />

Patent Specification<br />

Number: WO 2017/096996<br />

Publication Date:<br />

2017-06-15<br />

First Filing<br />

Priority Details: 20151209CN10906811<br />

Patentee: Suzhou Miracpharma Technology Co., Ltd<br />

Patent Description: Cobimetinib is obtained from (2S)-2-piperidinecarboxylic acid via various steps followed by azetinidation and conversion <strong>to</strong> product.<br />

Significant Step:<br />

Claimed Comment: Not Clear<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 23


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Dapagliflozin<br />

Patent Specification<br />

Number: WO 2017/060925<br />

Publication Date:<br />

2017-04-13<br />

First Filing<br />

Priority Details: 20151009IN3848/MUM<br />

Patentee: Harman Finochem Limited<br />

Patent Description: Dapagliflozin is obtained via prepared and isolated claimed intermediate A and 2-prop-2-ynyl analogue as defined.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 24


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Dapagliflozin<br />

Patent Specification<br />

Number: WO 2017/06<strong>36</strong>17<br />

Publication Date:<br />

2017-04-20<br />

First Filing<br />

Priority Details: 20151013CZ729<br />

Patentee: Zentiva, K.S.<br />

Patent Description: Dapagliflozin is obtained via the preparation of intermediate 1b employing a lithium magnesate complex. Canagliflozin is also prepared.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 25


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Dasatinib<br />

Patent Specification<br />

Number: WO 2017/098391<br />

Publication Date:<br />

2017-06-15<br />

First Filing<br />

Priority Details: 20151211IN6648/CHE<br />

Patentee: Shilpa Medicare Limited<br />

Patent Description: Dasatinib is obtained via two steps - the first in the presence of a solvent and base, the second in amyl alcohol without base. X-ray defined crystalline dasatinib Form SDN is<br />

claiimed.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 26


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Dolutegravir<br />

Patent Specification<br />

Number: WO 2017/109649<br />

Publication Date:<br />

2017-06-29<br />

First Filing<br />

Priority Details: 20151221IN4792/MUM<br />

Patentee: Lupin Limited<br />

Patent Description: Dolutegravir is obtained via prepared claimed intermediate XVIIa and analogues as defined.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 27


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Droxidopa<br />

Patent Specification<br />

Number: EP 3168208<br />

Publication Date:<br />

2017-05-17<br />

First Filing<br />

Priority Details: 20151111EP382562<br />

Patentee: Quimica Sintetica, S.A.<br />

Patent Description: Droxidopa is obtained via preparation of a chiral oxazoline intermediate followed by ring opening and conversion <strong>to</strong> product.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 28


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Efinaconazole<br />

Patent Specification<br />

Number: US 2017/0129874<br />

Publication Date:<br />

2017-05-11<br />

First Filing<br />

Priority Details: 20151110IN5438/CHE + 20151110IN5439/CHE<br />

Patentee: Virupaksha Organics Limited<br />

Patent Description: Efinaconazole is obtained via the preparation of prepared claimed intermediate IIA where X is O (IIB) or S.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 29


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Eliglustat<br />

Patent Specification<br />

Number: WO 2017/068496<br />

Publication Date:<br />

2017-04-27<br />

First Filing<br />

Priority Details: 20151020IN5655/CHE<br />

Patentee: Dr. Reddy's Labora<strong>to</strong>ries Limited<br />

Patent Description: Eliglustat is obtained via the preparation of prepared intermediate III.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 30


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Eltrombopag<br />

Patent Specification<br />

Number: WO 2017/081014<br />

Publication Date:<br />

2017-05-18<br />

First Filing<br />

Priority Details: 20151110IN4299/MUM<br />

Patentee: Amneal Pharmaceuticals Company GmbH<br />

Patent Description: Eltrombopag is obtained via a diazotisation and a condensation reaction.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 31


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Enzalutamide<br />

Patent Specification<br />

Number: WO 2017/081702<br />

Publication Date:<br />

2017-05-18<br />

First Filing<br />

Priority Details: 20151109IN4279/MUM<br />

Patentee: Sun Pharmaceutical Industries Limited<br />

Patent Description: Enzalutamide is obtained via the condensation of prepared intermediate II with intermediate III.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 32


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Epirubicin<br />

Patent Specification<br />

Number: WO 2017/075994<br />

Publication Date:<br />

2017-05-11<br />

First Filing<br />

Priority Details: 20151105CN10744980<br />

Patentee: Zhejiang Hisun Pharmaceutical Co., Ltd. and Shanghai Institute of Pharmaceutical Industry<br />

Patent Description: Epirubicin is obtained as shown and separated and purified utilising a macroporous absorption resin.<br />

Significant Step:<br />

Claimed Comment: Not Clear<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page <strong>33</strong>


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Fexofenadine<br />

Patent Specification<br />

Number: WO 2017/068129<br />

Publication Date:<br />

2017-04-27<br />

First Filing<br />

Priority Details: 20151022EP191020<br />

Patentee: Sanofi-Aventis Deutschland GmbH<br />

Patent Description: Fexofenadine is obtained via the reaction of azacyclonol with a cyclopropane-nitrile &c derivative followed by reduction and hydrolysis <strong>to</strong> product.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 34


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Flibanserin<br />

Patent Specification<br />

Number: WO 2017/076213<br />

Publication Date:<br />

2017-05-11<br />

First Filing<br />

Priority Details: 20151102CN107<strong>36</strong>356<br />

Patentee: Vigonvita Life Sciences Suzhou Co., Ltd. and Shanghai Institute of Materia Medica, Chines Academy of Sciences<br />

Patent Description: Flibanserin is obtained via the formation of benzimidazole intermediate I and analogues as defined.<br />

Significant Step:<br />

Claimed Comment: Not Clear<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 35


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Flurbiprofen<br />

Patent Specification<br />

Number: WO 2017/057642<br />

Publication Date:<br />

2017-04-06<br />

First Filing<br />

Priority Details: 20150930JP194284<br />

Patentee: Taisho Pharmaceutical Co., Ltd.<br />

Patent Description: (S)-Flurbiprofen is obtained via an alkylation reaction in the presence of a defined chiral catalyst and a nickel compound.<br />

Significant Step:<br />

Claimed Comment: Not Clear<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page <strong>36</strong>


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Flutemetamol<br />

Patent Specification<br />

Number: WO 2017/071980<br />

Publication Date:<br />

2017-05-04<br />

First Filing<br />

Priority Details: 20151028JP211413<br />

Patentee: GE Healthcare Limited and Nihon Medi-Physics Co., Ltd<br />

Patent Description: Flutemetamol is obtained via an 18F labelling step and a precursor decomposition step.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 37


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Fosaprepitant<br />

Patent Specification<br />

Number: WO 2017/093899<br />

Publication Date:<br />

2017-06-08<br />

First Filing<br />

Priority Details: 20151201IN4518/MUM<br />

Patentee: Piramal Enterprises Limited<br />

Patent Description: Fosaprepitant and fosaprepitant dimeglumine are obtained via the prepared intermediate fosaprepitant dibenzyl ester II.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 38


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Fulvestrant<br />

Patent Specification<br />

Number: WO 2017/064724<br />

Publication Date:<br />

2017-04-20<br />

First Filing<br />

Priority Details: 20151012IN5454/CHE<br />

Patentee: Natco Pharma Ltd<br />

Patent Description: Fulvestrant is obtained via the preparation of intermediate IV.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 39


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Gadoteric acid<br />

Patent Specification<br />

Number: WO 2017/103258<br />

Publication Date:<br />

2017-06-22<br />

First Filing<br />

Priority Details: 20151218GB22412<br />

Patentee: GE Healthcare AS<br />

Patent Description: Gadoteric acid is obtained via the preparation of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA). The preparation of gadoterate meglumine is referred <strong>to</strong>.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 40


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Hydrocodone<br />

Patent Specification<br />

Number: US 2017/0137432<br />

Publication Date:<br />

2017-05-18<br />

First Filing<br />

Priority Details: 20151104US62/250856<br />

Patentee: Noramco Inc.<br />

Patent Description: Hydrocodone is obtained from thebaine via continuous flow olefin reduction and batch hydrolysis steps.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 41


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Ibrutinib<br />

Patent Specification<br />

Number: WO 2017/074265<br />

Publication Date:<br />

2017-05-04<br />

First Filing<br />

Priority Details: 20151028US62/285035<br />

Patentee: Scinopharm Taiwan, Ltd.<br />

Patent Description: Ibrutinib is obtained via the preparation of claimed co-intermediates 12 and 12a.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 42


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Idelalisib<br />

Patent Specification<br />

Number: WO 2017/093773<br />

Publication Date:<br />

2017-06-08<br />

First Filing<br />

Priority Details: 20151130HU577<br />

Patentee: Egis Gyogyszergyar ZRT.<br />

Patent Description: Idelalisib is obtained via the reaction of quinazolin-4(3H)-one intermediate with 6-chloropurine. X-ray defined idelalisib Form E polymorph and ace<strong>to</strong>nitrile solvate Form<br />

E-S are claimed<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 43


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Indacaterol<br />

Patent Specification<br />

Number: WO 2017/055506<br />

Publication Date:<br />

2017-04-06<br />

First Filing<br />

Priority Details: 20150929EP187430<br />

Patentee: Labora<strong>to</strong>rios Lesvi, S.L.<br />

Patent Description: Indacaterol is obtained via the use of a mixed solvate of ethanol and water with an indacaterol salt, eg maleate.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 44


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Indacaterol<br />

Patent Specification<br />

Number: WO 2017/055905<br />

Publication Date:<br />

2017-04-06<br />

First Filing<br />

Priority Details: 20150928IT3978<br />

Patentee: Olon S.P.A.<br />

Patent Description: Indacaterol is obtained via dibromination of 1H-inden-2-ylamine with N-bromosuccinimide. Analogues of intermediate II with an amine protecting or activating group are<br />

claimed.<br />

Significant Step:<br />

Claimed Comment: Not Clear<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 45


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Indocyanine green<br />

Patent Specification<br />

Number: WO 2017/093889<br />

Publication Date:<br />

2017-06-08<br />

First Filing<br />

Priority Details: 20151201IN45<strong>36</strong>/MUM<br />

Patentee: Dishman Pharmaceuticals and Chemicals Limited<br />

Patent Description: Indocyanine green is obtained in high purity as shown.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 46


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Ivacaf<strong>to</strong>r<br />

Patent Specification<br />

Number: US 2017/0096397<br />

Patentee: Optimus Drugs Private Limited<br />

Patent Description: Ivacaf<strong>to</strong>r is obtained as shown.<br />

Publication Date:<br />

2017-04-06<br />

First Filing<br />

Priority Details: 20151006IN5<strong>33</strong>3/CHE<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 47


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Labetalol<br />

Patent Specification<br />

Number: WO 2017/098520<br />

Publication Date:<br />

2017-06-15<br />

First Filing<br />

Priority Details: 20151209IN6885/CHE<br />

Patentee: Davaluri Ramamohan Rao<br />

Patent Description: Labetalol is obtained as shown in high yield and purity.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 48


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Lacosamide<br />

Patent Specification<br />

Number: WO 2017/082396<br />

Publication Date:<br />

2017-05-18<br />

First Filing<br />

Priority Details: 20151113JP222754<br />

Patentee: API Corporation<br />

Patent Description: Lacosamide is obtained via amination, resolution and desalt/acetylation steps.<br />

Significant Step:<br />

Claimed Comment: Not Clear<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 49


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Ledipasvir<br />

Patent Specification<br />

Number: WO 2017/072596<br />

Publication Date:<br />

2017-05-04<br />

First Filing<br />

Priority Details: 20151026IN5716/CHE<br />

Patentee: Optimus Drugs (P) Ltd<br />

Patent Description: Ledipasvir is obtained with reduced impurities via the synthesis shown.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 50


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Lisdexamfetamine<br />

Patent Specification<br />

Number: WO 2017/0985<strong>33</strong><br />

Publication Date:<br />

2017-06-15<br />

First Filing<br />

Priority Details: 20151211IN4670/MUM<br />

Patentee: Sun Pharmaceutical Industries Limited<br />

Patent Description: Lisdexamfetamine is obtained via the preparation of claimed intermediate IV and analogues as defined.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 51


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Lisinopril<br />

Patent Specification<br />

Number: WO 2017/097193<br />

Publication Date:<br />

2017-06-15<br />

First Filing<br />

Priority Details: 20151211CN10920150<br />

Patentee: Zhejiang Huahai Pharmaceuticals Co., Ltd.<br />

Patent Description: Lisinopril is obtained as shown and refined by means of defined solvent crystallisation.<br />

Significant Step:<br />

Claimed Comment: Not Clear<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 52


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Lomitapide<br />

Patent Specification<br />

Number: WO 2017/098522<br />

Publication Date:<br />

2017-06-15<br />

First Filing<br />

Priority Details: 20151208IN6561<br />

Patentee: MSN Labor<strong>to</strong>ries Private Limited<br />

Patent Description: Lomitapide is obtained as shown. X-ray defined lomitapide methanesulfonate crystalline polymorph is claimed.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 53


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Luliconazole<br />

Patent Specification<br />

Number: WO 2017/108972<br />

Publication Date:<br />

2017-06-29<br />

First Filing<br />

Priority Details: 20151221EP382654<br />

Patentee: Labora<strong>to</strong>rios Lesvi, S.L.<br />

Patent Description: Luliconazole is obtained via the reaction of prepared intermediate 3a with a prepared dithiolate intermediate.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 54


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Luliconazole<br />

Patent Specification<br />

Number: WO 2017/094204<br />

Publication Date:<br />

2017-06-08<br />

First Filing<br />

Priority Details: 20151204JP237951<br />

Patentee: Pola Pharma Inc. and Nihon Nohyaku Co., Ltd.<br />

Patent Description: Luliconazole is obtained via the reaction of 1-cyanomethylimidazole with carbon disulfide followed by a cyclisation step.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 55


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Lumacaf<strong>to</strong>r<br />

Patent Specification<br />

Number: WO 2017/056031<br />

Publication Date:<br />

2017-04-06<br />

First Filing<br />

Priority Details: 20151001IN3746/MUM<br />

Patentee: Glenmark Pharmaceuticals Limited<br />

Patent Description: Lumacaf<strong>to</strong>r is obtained via the preparation of claimed intermediate IIa.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 56


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Macitentan<br />

Patent Specification<br />

Number: WO 2017/093903<br />

Publication Date:<br />

2017-06-08<br />

First Filing<br />

Priority Details: 20151130IN6404/CHE<br />

Patentee: Laurus Labs Private Limited<br />

Patent Description: Macitentan is obtained via the multi-step synthesis shown. X-ray defined macitentan methylene chloride solvate is claimed.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 57


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Nintedanib<br />

Patent Specification<br />

Number: WO 2017/077551<br />

Publication Date:<br />

2017-05-11<br />

First Filing<br />

Priority Details: 20151103IN5942/CHE<br />

Patentee: Mylan Labora<strong>to</strong>ries Limited<br />

Patent Description: Nintedanib is obtained as shown. Amorphous nintedanib esylate is claimed.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 58


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Obeticholic acid<br />

Patent Specification<br />

Number: WO 2017/079062<br />

Publication Date:<br />

2017-05-11<br />

First Filing<br />

Priority Details: 20151106US62/252077<br />

Patentee: Intercept Pharmaceuticals Inc.<br />

Patent Description: Obeticholic acid is obtained via protecting, alkylating and reducing steps. Obeticholic acid salts, solvates and amino acid conjugates are also prepared.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 59


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Obeticholic acid<br />

Patent Specification<br />

Number: WO 2017/111979<br />

Publication Date:<br />

2017-06-29<br />

First Filing<br />

Priority Details: 20151222US14/979005<br />

Patentee: Intercept Pharmaceuticals, Inc<br />

Patent Description: Obeticholic acid is obtained via the reaction steps shown. X-ray defined crystalline form of obeticholic acid is claimed.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 60


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Olmutinib<br />

Patent Specification<br />

Number: WO 2017/074147<br />

Publication Date:<br />

2017-05-04<br />

First Filing<br />

Priority Details: 20151030KR151993<br />

Patentee: Hanmi Pharm. Co., Ltd.<br />

Patent Description: Olmutinib is obtained via the preparation of claimed intermediate II.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 61


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Omarigliptin<br />

Patent Specification<br />

Number: WO 2017/093209<br />

Publication Date:<br />

2017-06-08<br />

First Filing<br />

Priority Details: 20151203EP197856<br />

Patentee: F.I.S. - Fabbrica Italiana Sintetici S.P.A.<br />

Patent Description: Omarigliptin is obtained via the preparation of claimed intermediates IV and V and analogues as defined.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 62


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Omarigliptin<br />

Patent Specification<br />

Number: WO 2017/081590<br />

Publication Date:<br />

2017-05-18<br />

First Filing<br />

Priority Details: 20151109IN<strong>36</strong>65/DEL<br />

Patentee: Sun Pharmaceutical Industries Limited<br />

Patent Description: Omarigliptin is obtained via the multi-step synthesis shown.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 63


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Pimavanserin<br />

Patent Specification<br />

Number: WO 2017/054786<br />

Publication Date:<br />

2017-04-06<br />

First Filing<br />

Priority Details: 20151002CZ688<br />

Patentee: Zentiva, K.S.<br />

Patent Description: Pimavanserin is obtained via the preparation of claimed intermediate XIa and analogues as defined.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 64


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Pimecrolimus<br />

Patent Specification<br />

Number: EP 3178824<br />

Publication Date:<br />

2017-06-14<br />

First Filing<br />

Priority Details: 20151208CN10893907<br />

Patentee: Medichem, S.A. and BrightGene Bio-Medical Technology Co., Ltd.<br />

Patent Description: Pimecrolimus is obtained from activated ascomycin via reaction with two chloride ion sources.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 65


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Pirfenidone<br />

Patent Specification<br />

Number: WO 2017/072216<br />

Publication Date:<br />

2017-05-04<br />

First Filing<br />

Priority Details: 20151029IT67092<br />

Patentee: Procos S.p.A.<br />

Patent Description: Pirfenidone is obtained via an arylation reaction in the presence of an inert gas and a catalyst comprising a copper salt and a defined ethylenediamine ligand.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 66


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Riociguat<br />

Patent Specification<br />

Number: WO 2017/103760<br />

Publication Date:<br />

2017-06-22<br />

First Filing<br />

Priority Details: 20151215IN4697/MUM<br />

Patentee: Alembic Pharmaceuticals Limited<br />

Patent Description: Riociguat is obtained via methylation of the prepared methyl carbamate intermediate in the presence of a base and a solvent.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 67


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Rivaroxaban<br />

Patent Specification<br />

Number: WO 2017/076844<br />

Publication Date:<br />

2017-05-11<br />

First Filing<br />

Priority Details: 20151104US62/250587 + 20151104EP192880<br />

Patentee: Lonza Ltd<br />

Patent Description: Rivaroxaban is obtained via the preparation of 5-chloro-2-thiophenecarbonyl chloride from thiophene or 2-chlorothiophene with oxalyl chloride at a temperature of 160-<br />

250 degrees C.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 68


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Romidepsin<br />

Patent Specification<br />

Number: WO 2017/068596<br />

Publication Date:<br />

2017-04-27<br />

First Filing<br />

Priority Details: 20151020IN5640/CHE<br />

Patentee: MSN Labora<strong>to</strong>ries Private Limited and Venkat Reddy, Ghojala<br />

Patent Description: Romidepsin is obtained via the reaction of prepared intermediates II and III in the presence of a defined condensing agent, eg HATU, and an organic base.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 69


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Sacubitril<br />

Patent Specification<br />

Number: WO 2017/059759<br />

Publication Date:<br />

2017-04-13<br />

First Filing<br />

Priority Details: 20151010CN10654835<br />

Patentee: Chiral Quest (Suzhou) Co., Ltd. and Jiangxi Long Life Bio-Pharmaceutical Co., Ltd.<br />

Patent Description: Sacubitril is obtained via the prepared claimed intermediate 3 or the (R)-enantiomer, in the presence of a defined Rhodium catalyst.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 70


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Sacubitril<br />

Patent Specification<br />

Number: WO 2017/098430<br />

Publication Date:<br />

2017-06-15<br />

First Filing<br />

Priority Details: 20151210EP199378<br />

Patentee: Novartis AG<br />

Patent Description: Sacubitril is obtained as exemplified in the synthesis shown via claimed intermediates XV and XVII. Other intermediates are claimed.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 71


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Sacubitril<br />

Patent Specification<br />

Number: WO 2017/097275<br />

Publication Date:<br />

2017-06-15<br />

First Filing<br />

Priority Details: 20151211CZ891<br />

Patentee: Zentiva, K.S.<br />

Patent Description: Sacubitril is obtained with reduced impurities by converting the crude free acid <strong>to</strong> an amine salt and releasing the free acid <strong>to</strong> product. X-ray defined crystalline form of<br />

sacubitril is claimed.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 72


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Saroglitazar<br />

Patent Specification<br />

Number: WO 2017/064635<br />

Publication Date:<br />

2017-04-20<br />

First Filing<br />

Priority Details: 20151014IN3901/MUM<br />

Patentee: Cadila Healthcare Limited<br />

Patent Description: Saroglitazar is obtained eg as saroglitazar magnesium with increased purity and reduced dimer impurity.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 73


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Selexipag<br />

Patent Specification<br />

Number: WO 2017/060827<br />

Publication Date:<br />

2017-04-13<br />

First Filing<br />

Priority Details: 20151007IN3817/MUM<br />

Patentee: Lupin Limited<br />

Patent Description: Selexipag is obtained via the reaction of 4-amino-1-butanol with ace<strong>to</strong>ne in the presence of Pd/C <strong>to</strong> obtain 4-(isopropylamino)-1-butanol.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 74


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Silodosin<br />

Patent Specification<br />

Number: WO 2017/080414<br />

Publication Date:<br />

2017-05-18<br />

First Filing<br />

Priority Details: 20151109CN10759873<br />

Patentee: Huang, Huan<br />

Patent Description: Silodosin is obtained via the preparation of intermediate 1 or salt thereof, eg L-(+)-tartrate.<br />

Significant Step:<br />

Claimed Comment: Not Clear<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 75


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Silodosin<br />

Patent Specification<br />

Number: WO 2017/055664<br />

Publication Date:<br />

2017-04-06<br />

First Filing<br />

Priority Details: 20150930ES31398<br />

Patentee: Urquima, S.A.<br />

Patent Description: Silodosin is obtained via the prepared claimed intermediate salt I.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 76


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Simeprevir<br />

Patent Specification<br />

Number: WO 2017/064680<br />

Publication Date:<br />

2017-04-20<br />

First Filing<br />

Priority Details: 20151016IN3942/MUM<br />

Patentee: Lupin Limited<br />

Patent Description: Simeprevir is obtained via the preparation of intermediate VII.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 77


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Sitagliptin<br />

Patent Specification<br />

Number: EP 3159343<br />

Publication Date:<br />

2017-04-26<br />

First Filing<br />

Priority Details: 20151022EP191125<br />

Patentee: F.I.S. - Fabbrica Italiana Sintetici S.p.A.<br />

Patent Description: Sitagliptin is obtained via the preparation of triazole intermediate II.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 78


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Sofosbuvir<br />

Patent Specification<br />

Number: WO 2017/077552<br />

Publication Date:<br />

2017-05-11<br />

First Filing<br />

Priority Details: 20151103IN5940/CHE<br />

Patentee: Mylan Labora<strong>to</strong>ries Limited<br />

Patent Description: Sofosbuvir is obtained via prepared claimed intermediate 12a.<br />

Significant Step:<br />

Claimed Comment: Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 79


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Sofosbuvir<br />

Patent Specification<br />

Number: WO 2017/093973<br />

Publication Date:<br />

2017-06-08<br />

First Filing<br />

Priority Details: 20151202IN3928/DEL<br />

Patentee: Sun Pharmaceutical Industries Limited<br />

Patent Description: Sofosbuvir is obtained with reduced impurities via hydrogenation of prepared bromo-sofosbuvir in the presence of an organic base.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 80


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Sonidegib<br />

Patent Specification<br />

Number: WO 2017/096998<br />

Publication Date:<br />

2017-06-15<br />

First Filing<br />

Priority Details: 20151209CN10907246<br />

Patentee: Suzhou Miracpharma Technology Co., Ltd<br />

Patent Description: Sonidegib is obtained via a cyclisation reaction with a prepared bisulfonated intermediate.<br />

Significant Step:<br />

Claimed Comment: Not Clear<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 81


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Tedizolid<br />

Patent Specification<br />

Number: WO 2017/099530<br />

Publication Date:<br />

2017-06-15<br />

First Filing<br />

Priority Details: 20151211KR177169<br />

Patentee: St Pharm Co., Ltd.<br />

Patent Description: Tedizolid is obtained via the preparation of the intermediate 5-bromo-2-(2-methyl-2H-tetrazol-5-yl)pyridine.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 82


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Tedizolid<br />

Patent Specification<br />

Number: WO 2017/076285<br />

Publication Date:<br />

2017-05-11<br />

First Filing<br />

Priority Details: 20151103CN10739910<br />

Patentee: Zheijiang Huahai Pharmaceutical Co., Ltd. and Shanghai Syncores Technologies Inc. Ltd.<br />

Patent Description: Tedizolid and phosphates are obtained via the synthesis of intermediates D and C and analogues as defined.<br />

Significant Step:<br />

Claimed Comment: Not Clear<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 83


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Teriflunomide<br />

Patent Specification<br />

Number: WO 2017/103942<br />

Publication Date:<br />

2017-06-22<br />

First Filing<br />

Priority Details: 20151214IN6909/CHE<br />

Patentee: Natco Pharma Ltd<br />

Patent Description: Teriflunomide is obtained via the reaction of purified 4-trifluoromethyl aniline with cyanoacetic acid followed by acetylation.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 84


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Tes<strong>to</strong>sterone<br />

Patent Specification<br />

Number: WO 2017/093980<br />

Publication Date:<br />

2017-06-08<br />

First Filing<br />

Priority Details: 20151205IN4612/MUM<br />

Patentee: Lupin Limited<br />

Patent Description: Tes<strong>to</strong>sterone is obtained from purified 4-androsten-3,17-dione via 17-ke<strong>to</strong>-3-enol ether intermediate.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 85


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Thalidomide<br />

Patent Specification<br />

Number: WO 2017/081701<br />

Publication Date:<br />

2017-05-18<br />

First Filing<br />

Priority Details: 20151112IN6099/CHE<br />

Patentee: Natco Pharma Ltd<br />

Patent Description: Thalidomide is obtained via the reaction of phthallic anhydride with 3-aminopiperidine-2,6-dione in the presence of triethylamine followed by purification by crystallisation<br />

of the crude product in an organic/water mixture.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 86


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Ticagrelor<br />

Patent Specification<br />

Number: WO 2017/072790<br />

Publication Date:<br />

2017-05-04<br />

First Filing<br />

Priority Details: 20151026IN5743<br />

Patentee: Avra Labora<strong>to</strong>ries Pvt. Ltd.<br />

Patent Description: Ticagrelor is obtained via the improved and cost-effective synthesis as shown. X-ray defined ticagrelor polymorphic Form V is claimed.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 87


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Valbenazine<br />

Patent Specification<br />

Number: WO 2017/112857<br />

Publication Date:<br />

2017-06-29<br />

First Filing<br />

Priority Details: 20151223US62/387442<br />

Patentee: Neurocrine Biosciences, Inc.<br />

Patent Description: Valbenazine is obtained via the synthesis shown. Methods of forming valbenazine di(4-methylbenzenesulfonate) or a solvate, hydrate or polymorph are claimed.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 88


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Velpatasvir<br />

Patent Specification<br />

Number: WO 2017/060820<br />

Publication Date:<br />

2017-04-13<br />

First Filing<br />

Priority Details: 20151008IN3829/MUM<br />

Patentee: Mylan Labora<strong>to</strong>ries Limited<br />

Patent Description: Velpatasvir is obtained via the preparation of tetracyclic intermediate 8.<br />

Significant Step:<br />

Claimed Comment: None Claimed<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 89


New process patents for named, marketed, pharmaceutical drugs<br />

published in the Quarter 2, April <strong>to</strong> June 2017<br />

Drug Name: Voriconazole<br />

Patent Specification<br />

Number: WO 2017/108010<br />

Publication Date:<br />

2017-06-29<br />

First Filing<br />

Priority Details: 20151223CN10984590<br />

Patentee: Zhejiang Huahai Pharmaceutical Co., Ltd<br />

Patent Description: Voriconazole is obtained via the preparation of intermediate II without the use of highly <strong>to</strong>xic metal lead.<br />

Significant Step:<br />

Claimed Comment: Not Clear<br />

Claimed<br />

Intermediate:<br />

Basic Patent Status: Application Stage<br />

Page 90


This Marketed Drug Process Patent <strong>Report</strong> has been extracted from the<br />

Claimed Intermediate Structure Searchable Database<br />

The Database contains some <strong>36</strong>00+ Text/Structure Searchable Syntheses since January 2010<br />

Bespoke <strong>Report</strong>s can be supplied by Drug, Patentee or Period<br />

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