公开(公告)号：US09156789B2

公开(公告)日：2015-10-13

申请号：US14401191

申请日：2013-05-21

Applicant: HETERO RESEARCH FOUNDATION

Inventor： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Dasari Muralidhara Reddy ,  Thungathurthy Srinivasa Rao ,  Bandi Vamsi Krishna

IPC: A61K31/44 ,  C07D213/63 ,  C07D213/81

CPC classification number: C07D213/81

Abstract: The present invention provides a novel process for the preparation of sorafenib tosylate polymorph III.

Abstract translation: 本发明提供了制备索拉非尼甲苯磺酸盐多晶型III的新方法。

公开(公告)号：US20150133670A1

公开(公告)日：2015-05-14

申请号：US14401191

申请日：2013-05-21

Applicant: HETERO RESEARCH FOUNDATION

Inventor： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Dasari Muralidhara Reddy ,  Thungathurthy Srinivasa Rao ,  Bandi Vamsi Krishna

IPC: C07D213/81

CPC classification number: C07D213/81

Abstract: The present invention provides a novel process for the preparation of sorafenib tosylate polymorph III.

Abstract translation: 本发明提供了制备索拉非尼甲苯磺酸盐多晶型III的新方法。

公开(公告)号：US09518020B2

公开(公告)日：2016-12-13

申请号：US15026694

申请日：2014-09-29

Applicant: Hetero Research Foundation

Inventor： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Dasari Muralidhara Reddy ,  Thungathurthy Srinivasa Rao ,  Bandi Vamsi Krishna

IPC: C07D213/68 ,  C07D213/81

CPC classification number: C07D213/81 ,  C07B2200/13

Abstract: The present invention provides processes for the preparation of i) Regorafenib (4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide, BAY 73-4506, Stivarga®) and its pharmaceutically acceptable salt thereof; ii) a crystalline solid of Regorafenib tosylate; iii) Regorafenib Polymorph I from Regorafenib tosylate, and iv) a pure 4-(4-amino-3-fluorophenoxy)-N-methylpicolinamide from 4-amino-3-fluorophenol and 4-chloro-N-methylpicolinamide in the presence of potassium tert-butoxide.

Abstract translation: 本发明提供了制备i）雷卡非尼（4- [4 - （{[4-氯-3-（三氟甲基）苯基]氨基甲酰基}氨基）-3-氟苯氧基] -N-甲基吡啶-2-甲酰胺的方法， BAY 73-4506，Stivarga？）及其药学上可接受的盐; ii）瑞波非尼甲苯磺酸盐的结晶固体; iii）从罗非拉布甲苯磺酸盐获得的瑞考非非多晶型I，和iv）在钾存在下，由4-氨基-3-氟苯酚和4-氯-N-甲基吡啶酰胺制得纯的4-（4-氨基-3-氟苯氧基）-N-甲基吡啶酰胺 叔丁醇盐。