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1. 发明授权

EP2358724B1 TIOTROPIUM BROMIDE HAVING A LOW DEGREE OF CRYSTALLINITY 有权
标题翻译：噻托溴铵结晶度低
公开(公告)号：EP2358724B1
公开(公告)日：2012-08-29
申请号：EP09749173.2
申请日：2009-10-29
申请人： CIPLA LIMITED
发明人： KANKAN, Rajendra, Narayanrao , RAO, Dharmaraj, Ramachandra , GHAGARE, Maruti
IPC分类号： C07D491/08 , A61K31/46 , A61P11/00
CPC分类号： C07D491/08 , A61K31/79

2. 发明公开

EP2882752A1 PROCESS FOR THE PREPARATION OF SITAGLIPTIN AND INTERMEDIATE COMPOUNDS 审中-公开
标题翻译： VERFAHREN ZUR HERSTELLUNG VON SITAGLIPTIN SOWIE ZWISCHENPRODUKTEN DAVON
公开(公告)号：EP2882752A1
公开(公告)日：2015-06-17
申请号：EP13750356.1
申请日：2013-08-08
申请人： Cipla Limited
发明人： RAO, Dharmaraj, Ramachandra , KANKAN, Rajendra, Narayanrao , GHAGARE, Maruti , KADAM, Swati, Atul
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： There is provided a process for the preparation of sitagliptin or a pharmaceutically acceptable salt thereof, and a process for the preparation of intermediate compounds useful in the preparation of sitagliptin. In particular, there is provided a process comprising condensing 3-tert-butoxycarbonylamino-4-(2,4,5-trifluorophenyl) butyric acid of formula (II) with 3-(trifluoromethyl)-5,6,7,8-tetrahydro-[l,2,4]triazolo[4,3-a] pyrazine of formula (III) or a salt thereof in presence of a catalyst to obtain (R)-tert-butyl-4-oxo-4-(3- (trifluoromethyl)-5,6-dihydro-[ 1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl)- 1 -(2,4,5- trifluorophenyl)butan-2-yl-carbamate of formula (IV) or a pharmaceutically acceptable salt thereof. The catalyst is represented by the compound of formula (V). Compound of formula (IV) or its pharmaceutically acceptable salt obtained may be deprotected to obtain a compound of formula (I).
摘要翻译：提供了西他列汀或其药学上可接受的盐的制备方法，以及制备可用于制备西格列汀的中间体化合物的方法。特别地，提供了一种方法，其包括将式（II）的3-叔丁氧基羰基氨基-4-（2,4,5-三氟苯基）丁酸与3-（三氟甲基）-5,6,7,8-四氢 - [1,2,4]三唑并[4,3-a]吡嗪或其盐在催化剂存在下反应，得到（R） - 叔丁基-4-氧代-4-（3- （三氟甲基）-5,6-二氢 - [1,2,4] - 三唑并[4,3-a]吡嗪-7（8H） - 基）-1-（2,4,5-三氟苯基）丁-2- （Ⅳ）的 - - - - 氨基甲酸酯或其药用盐。催化剂由式（V）化合物表示。可以将得到的式（IV）化合物或其药学上可接受的盐脱保护，得到式（I）化合物。

3. 发明公开

EP2195286A2 PROCESS FOR THE PREPARATION OF A RAF KINASE INHIBITOR AND INTERMEDIATES FOR USE IN THE PROCESS 审中-公开
标题翻译：用于生产RAF激酶抑制剂和中间体使用过程中
公开(公告)号：EP2195286A2
公开(公告)日：2010-06-16
申请号：EP08806217.9
申请日：2008-09-10
申请人： Cipla Limited
发明人： RAO, Dharmaraj, Ramachandra , KANKAN, Rajendra, Narayanrao , GHAGARE, Maruti , CHIKHALIKAR, Sandip
IPC分类号： C07C233/65 , C07C271/58 , C07C275/30 , C07C275/64 , C07D213/81
CPC分类号： C07C271/58 , C07C233/15 , C07C275/30 , C07C275/34 , C07C275/64 , C07D213/81
摘要： There is provided a process for preparing sorafenib or a salt thereof comprising the use of a compound of formula (A), wherein R' is selected from the group consisting of hydrogen, -C(O)OA, -C(O)CX3, - OH C(O)NH2, -C(O)-NHOH or (a). There is also provided intermediate compounds of general formula (A), N-methyl-4-(4-ureidophenoxy)picolinamide, 4-(2- (methylcarbamoyl)pyridin-4-yloxy)phenylcarbamate derivative and N-methyl-4-(4-(2,2,2- trihaloacetamido)phenoxy)picolinamide, processes for their preparation and their use in the preparation of sorafenib.

4. 发明公开

EP2768811A1 PROCESS FOR THE PREPARATION OF AN ENDOTHELIN RECEPTOR ANTAGONIST 审中-公开
标题翻译： VERFAHREN ZUR HERSTELLUNG EINES内皮素激动剂 - 拮抗剂
公开(公告)号：EP2768811A1
公开(公告)日：2014-08-27
申请号：EP12780256.9
申请日：2012-10-19
申请人： Cipla Limited
发明人： RAO, Dharmaraj Ramachandra , KANKAN, Rajendra Narayanrao , NAIK, Sanjay , GHAGARE, Maruti , CHIKHALIKAR, Sandip Vasant
IPC分类号： C07D239/34 , C07D239/46 , C07C69/00
CPC分类号： C12P7/62 , C07C67/313 , C07C69/716 , C07D239/34 , C07D239/46 , C12P17/12
摘要： The present invention relates to a novel process for the preparation of a compound of formula (I) wherein R is a methyl or methoxy group; to certain novel intermediates prepared in such a process and their use.
摘要翻译：本发明涉及一种制备式（I）化合物的新方法，其中R是甲基或甲氧基; 对于在这种方法中制备的某些新型中间体及其用途。

5. 发明授权

EP2467373B1 A PROCESS FOR THE SYNTHESIS OF NARATRIPTAN 有权
标题翻译：用于生产曲坦
公开(公告)号：EP2467373B1
公开(公告)日：2013-10-02
申请号：EP10747476.9
申请日：2010-08-18
申请人： Cipla Limited
发明人： RAO, Dharmaraj Ramachandra , KANKAN, Rajendra Narayanrao , CHIKHALIKAR, Sandip Vasant , GHAGARE, Maruti
IPC分类号： C07D401/04 , A61K31/404 , A61K31/405
CPC分类号： C07D401/04 , Y02P20/55

6. 发明公开

EP2307392A2 PROCESSES FOR THE SYNTHESIS OF LEVOCETIRIZINE AND INTERMEDIATES FOR USE THEREIN 审中-公开
标题翻译：方法左西替利的合成
公开(公告)号：EP2307392A2
公开(公告)日：2011-04-13
申请号：EP09757761.3
申请日：2009-06-02
申请人： Cipla Limited
发明人： RAO, Dharmaraj Ramachandra , KANKAN Rajendra Narayanrao , GHAGARE, Maruti , CHIKHALIKAR, Sandip Vasant
IPC分类号： C07D295/088
CPC分类号： C07D295/096 , C07C217/58 , C07C309/66 , C07D295/073 , C07D295/088
摘要： The present invention provides a compound of formula (IV) wherein R is Cl, Br, NO
2 , OH or OR', and R' is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (-)-1-[(4-chlorophenyl)-phenyl methyl] piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).

7. 发明公开

EP2467373A2 A PROCESS FOR THE SYNTHESIS OF NARATRIPTAN 有权
标题翻译：用于生产曲坦
公开(公告)号：EP2467373A2
公开(公告)日：2012-06-27
申请号：EP10747476.9
申请日：2010-08-18
申请人： Cipla Limited
发明人： RAO, Dharmaraj Ramachandra , KANKAN, Rajendra Narayanrao , CHIKHALIKAR, Sandip Vasant , GHAGARE, Maruti
IPC分类号： C07D401/04 , A61K31/404 , A61K31/405
CPC分类号： C07D401/04 , Y02P20/55
摘要： The present invention relates to a process for preparing naratriptan or a salt thereof, the process comprising: (a) reacting a compound of formula (3) with a compound of the formula HCCR wherein Z is a protecting group, Y is a leaving group and R is a trialkyl silyl group, a trialkylstannyl group or a zinc (II) halide, to obtain the compound of formula (4); (b) converting the compound of formula (4) to a compound of formula (5) wherein Z' is hydrogen or a benzyl group; (c) converting the compound of formula (5) to naratriptan; and (d) optionally converting naratriptan to a salt thereof. The present invention also provides novel compounds (3) and (4) and processes for their preparation.

8. 发明公开

EP2358724A1 Tiotropium bromide having a low degree of crystallinity 有权
标题翻译：噻托溴铵结晶度低
公开(公告)号：EP2358724A1
公开(公告)日：2011-08-24
申请号：EP09749173.2
申请日：2009-10-29
申请人： CIPLA LIMITED
发明人： KANKAN, Rajendra, Narayanrao , RAO, Dharmaraj, Ramachandra , GHAGARE, Maruti
IPC分类号： C07D491/08 , A61K31/46 , A61P11/00
CPC分类号： C07D491/08 , A61K31/79
摘要： The present invention provides tiotropium bromide having a low degree of crystallinity. The present invention also provides a complex of tiotropium bromide and polyvinylpyrrolidone, processes for preparing it and pharmaceutical formulations including it.

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