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1. 发明申请

US20120264823A1 SUBSTITUTED HETEROARYL- AND ARYL-CYCLOPROPYLAMINE ACETAMIDES AND THEIR USE 有权
标题翻译：取代的杂芳基和芳基环丙基氨基甲酸酯及其用途
公开(公告)号：US20120264823A1
公开(公告)日：2012-10-18
申请号：US13500687
申请日：2010-04-19
申请人： Alberto Ortega Muñoz , Julio Castro-Palomino Laria , Matthew Colin Thor Fyfe
发明人： Alberto Ortega Muñoz , Julio Castro-Palomino Laria , Matthew Colin Thor Fyfe
IPC分类号： A61K31/165 , A61K31/277 , C07C237/20 , A61P25/28 , A61P25/16 , C07C255/60 , A61P35/00
CPC分类号： C07C237/06 , C07C255/54 , C07C2601/02 , C07D213/36
摘要： The invention relates to compounds of Formula (I): (A′)x-(A)-(B)—(Z)-(L)-C(═O)NH2 or pharmaceutically acceptable salts or solvates thereof, wherein: (A) is heteroaryl or aryl; each (A′), if present, is indepedently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A′) is substituted with 0, 1, 2 or 3 substituents independently chosen from halo, haloalkyl, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, sulfinyl, and carboxamide; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; and (L) is —(CH2)mCR1,R2—, wherein m is 0, 1, 2, 3, 4, 5, or 6, and wherein R1 and R2 are each independently hydrogen or C1-C6 alkyl; provided that, if (L) is —CH2— or —CH(CH3)—, then X is not 0. The compounds of the invention are useful in the treatment of diseases such as cancer and neurodegenerative diseases.
摘要翻译：本发明涉及式（I）化合物：（A'）x-（A） - （B） - （Z） - （L）-C（= O）NH 2或其药学上可接受的盐或溶剂合物，其中： A）是杂芳基或芳基; 每个（A'）如果存在，独立地选自芳基，芳基烷氧基，芳烷基，杂环基，芳氧基，卤素，烷氧基，卤代烷基，环烷基，卤代烷氧基和氰基，其中每个（A'）被0,1,2 或3个独立地选自卤素，卤代烷基，芳基，芳基烷氧基，烷基，烷氧基，氰基，磺酰基，亚磺酰基和羧酰胺的取代基; X为0,1,2或3; （B）是环丙基环，其中（A）和（Z）与（B）的不同碳原子共价结合; （Z）为-NH-; 和（L）是 - （CH 2）m CR 1，R 2 - ，其中m是0,1,2,3,4,5或6，并且其中R 1和R 2各自独立地是氢或C 1 -C 6烷基; 条件是，如果（L）是-CH 2 - 或-CH（CH 3） - ，则X不为0.本发明的化合物可用于治疗疾病如癌症和神经变性疾病。

2. 发明申请

US20120172358A1 GPCR Agonists 审中-公开
标题翻译： GPCR激动剂
公开(公告)号：US20120172358A1
公开(公告)日：2012-07-05
申请号：US13396193
申请日：2012-02-14
申请人： Stuart Edward Bradley , Matthew Colin Thor Fyfe , Lisa Sarah Bertram , William Gattrell , Revathy Perpetua Jeevaratnam , John Keily , Martin James Procter , Chrystelle Marie Rasamison , Philip John Rushworth , Colin Peter Sambrook-Smith , David French Stonehouse , Simon Andrew Swain , Geoffrey Martyn Williams
发明人： Stuart Edward Bradley , Matthew Colin Thor Fyfe , Lisa Sarah Bertram , William Gattrell , Revathy Perpetua Jeevaratnam , John Keily , Martin James Procter , Chrystelle Marie Rasamison , Philip John Rushworth , Colin Peter Sambrook-Smith , David French Stonehouse , Simon Andrew Swain , Geoffrey Martyn Williams
IPC分类号： A61K31/445 , C07D401/10 , C07D413/12 , C07D401/04 , A61K31/454 , A61P3/06 , A61K31/496 , A61K31/5377 , A61K31/506 , A61P3/00 , A61P3/04 , A61P3/10 , C07D211/34 , A61K31/4545
CPC分类号： C07D401/14 , C07D211/20 , C07D211/22 , C07D211/24 , C07D211/26 , C07D211/28 , C07D211/34 , C07D211/48 , C07D401/04 , C07D401/10 , C07D401/12
摘要： Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.
摘要翻译：式（I）化合物或其药学上可接受的盐是GPCR激动剂，可用于治疗肥胖症和糖尿病。

4. 发明申请

US20110269734A1 PIPERIDINYL GPCR AGONISTS 审中-公开
公开(公告)号：US20110269734A1
公开(公告)日：2011-11-03
申请号：US13003546
申请日：2009-07-10
申请人： Lisa Sarah Bertram , Matthew Colin Thor Fyfe , Revathy Perpetua Jeevaratnam , John Keily , Thomas Martin Krulle , Chrystelle Marie Rasamison , Colin Peter Sambrook-Smith , Simon Andrew Swain
发明人： Lisa Sarah Bertram , Matthew Colin Thor Fyfe , Revathy Perpetua Jeevaratnam , John Keily , Thomas Martin Krulle , Chrystelle Marie Rasamison , Colin Peter Sambrook-Smith , Simon Andrew Swain
IPC分类号： A61K31/397 , A61K31/506 , C07D401/14 , A61P9/12 , A61K31/4545 , A61P3/04 , A61P3/10 , A61P3/06 , C07D401/04 , A61K31/501
CPC分类号： C07D401/04 , C07D401/14
摘要： Compounds of formula (I):or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of diabetes and obesity.
摘要翻译：式（I）化合物或其药学上可接受的盐是GPCR激动剂，可用于治疗糖尿病和肥胖症。

5. 发明申请

US20100286112A1 COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS 审中-公开
标题翻译：用于治疗代谢性疾病的化合物
公开(公告)号：US20100286112A1
公开(公告)日：2010-11-11
申请号：US12677153
申请日：2008-09-10
申请人： Oscar Barba , Stuart Edward Bradley , Matthew Colin Thor Fyfe , Patrick Eric Hanrahan , Thomas Martin Krulle , Martin James Procter , Christine Reynet McCormack , Karen Lesley Schofield , Donald Smyth , Alan John William Stewart , Simon Andrew Swain , Peter Widdowson
发明人： Oscar Barba , Stuart Edward Bradley , Matthew Colin Thor Fyfe , Patrick Eric Hanrahan , Thomas Martin Krulle , Martin James Procter , Christine Reynet McCormack , Karen Lesley Schofield , Donald Smyth , Alan John William Stewart , Simon Andrew Swain , Peter Widdowson
IPC分类号： A61K31/454 , C07D417/14 , A61P3/10 , A61P3/04 , A61P3/06 , A61P9/12 , C07D401/04 , A61K31/506 , C07D207/04 , A61K31/40 , C07D277/04 , A61K31/426
CPC分类号： C07D401/12 , C07D211/18 , C07D211/22 , C07D401/14 , C07D413/04 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention is directed to therapeutic compounds which have dual activity as agonists of GPR119 and inhibitors of DPP-IV and are useful for the treatment of metabolic disorders including type II diabetes.
摘要翻译：本发明涉及作为GPR119的激动剂和DPP-IV的抑制剂具有双重作用的治疗性化合物，并且可用于治疗包括II型糖尿病的代谢性疾病。

6. 发明申请

US20100286110A1 AZETIDINYL G-PROTEIN COUPLED RECEPTOR AGONISTS 审中-公开
标题翻译： AZETIDINYL G蛋白偶联受体激动剂
公开(公告)号：US20100286110A1
公开(公告)日：2010-11-11
申请号：US12738468
申请日：2008-10-10
申请人： Matthew Colin Thor Fyfe , William Gattrell , Colin Peter Sambrook-Smith
发明人： Matthew Colin Thor Fyfe , William Gattrell , Colin Peter Sambrook-Smith
IPC分类号： A61K31/4427 , C07D401/14 , A61K31/444 , A61K31/4439 , C07D417/14 , C07D401/12 , C07D405/14 , A61K31/443 , C07D413/14 , A61K31/4433 , A61P3/04 , A61P3/06 , A61P9/12
CPC分类号： C07D401/14 , C07D413/14 , C07D417/14
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful for the treatment of diabetes and as peripheral regulators of satiety, e.g. for the treatment of obesity and metabolic syndrome.
摘要翻译：式（I）化合物或其药学上可接受的盐是GPR119的激动剂，可用于治疗糖尿病和作为饱腹感的外周调节剂，例如，用于治疗肥胖和代谢综合征。

7. 发明授权

US07745491B2 Substituted phenylacetamides and their use as glucokinase activators 失效
标题翻译：取代苯乙酰胺及其作为葡萄糖激酶激活剂的用途
公开(公告)号：US07745491B2
公开(公告)日：2010-06-29
申请号：US11573464
申请日：2005-08-09
申请人： Matthew Colin Thor Fyfe , Vilasben Kanji Shah
发明人： Matthew Colin Thor Fyfe , Vilasben Kanji Shah
IPC分类号： A61K31/165
CPC分类号： C07C317/44 , C07C2601/02 , C07C2601/08 , C07D231/40 , C07D237/20 , C07D241/20
摘要： Compounds of Formula (I) wherein R1 is a cycloalkylsulphonyl group, or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.
摘要翻译：其中R1是环烷基磺酰基的式（I）化合物或其药学上可接受的盐可用于预防和治疗高血糖症和糖尿病。

8. 发明申请

US20100048632A1 Piperidine GPCR Agonists 审中-公开
标题翻译：哌啶GPCR激动剂
公开(公告)号：US20100048632A1
公开(公告)日：2010-02-25
申请号：US12522015
申请日：2008-01-04
申请人： Matthew Colin Thor Fyfe , John Keily , Simon Andrew Swain
发明人： Matthew Colin Thor Fyfe , John Keily , Simon Andrew Swain
IPC分类号： A61K31/454 , C07D413/04 , A61P3/00 , A61P3/04 , A61P3/10
CPC分类号： C07D413/04
摘要： Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.
摘要翻译：式（I）化合物或其药学上可接受的盐是GPCR激动剂，可用于治疗肥胖症和糖尿病。

9. 发明申请

US20100048625A1 PIPERIDINE GPCR AGONISTS 审中-公开
公开(公告)号：US20100048625A1
公开(公告)日：2010-02-25
申请号：US12522030
申请日：2008-01-04
申请人： Matthew Colin Thor Fyfe , Revathy Perpetua Jeevaratnam , John Keily , Simon Andrew Swain
发明人： Matthew Colin Thor Fyfe , Revathy Perpetua Jeevaratnam , John Keily , Simon Andrew Swain
IPC分类号： A61K31/4545 , C07D413/14 , A61P3/00 , A61P3/04 , A61P3/10
CPC分类号： C07D413/14
摘要： Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.

10. 发明申请

US20090325924A1 GPCR Agonists 审中-公开
标题翻译： GPCR激动剂
公开(公告)号：US20090325924A1
公开(公告)日：2009-12-31
申请号：US11922765
申请日：2006-06-29
申请人： Stuart Edward , Graham John Dawson , Matthew Colin Thor Fyfe Oxford , Lisa Sarah Bertram , William Gattrell , Revathy Perpetua Jeevaratnam , John Keily , Neela Sumit Mistry , Martin James Procter , Chrystelle Marie Rasamison , Philip John Rushworth , Colin Peter Sambrook-Smith , David French Stonehouse
发明人： Stuart Edward , Graham John Dawson , Matthew Colin Thor Fyfe Oxford , Lisa Sarah Bertram , William Gattrell , Revathy Perpetua Jeevaratnam , John Keily , Neela Sumit Mistry , Martin James Procter , Chrystelle Marie Rasamison , Philip John Rushworth , Colin Peter Sambrook-Smith , David French Stonehouse
IPC分类号： A61K31/4245 , C07D413/14 , C07D413/12 , C07D271/06 , A61K31/454 , A61K31/5377 , A61K31/496 , A61K31/506 , A61P3/00
CPC分类号： C07D271/06 , C07D401/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.
摘要翻译：式（I）化合物或其药学上可接受的盐是GPCR激动剂，可用于治疗肥胖症和糖尿病。

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