公开(公告)号：US20080312281A1

公开(公告)日：2008-12-18

申请号：US11794219

申请日：2005-12-23

Applicant: Matthew Colin Thor Fyfe ,  Lisa Sarah Bertram ,  Gerard Hugh Thomas ,  Geoffrey Martyn Williams

Inventor： Matthew Colin Thor Fyfe ,  Lisa Sarah Bertram ,  Gerard Hugh Thomas ,  Geoffrey Martyn Williams

IPC: A61K31/44 ,  C07D401/00 ,  A61P3/10

CPC classification number: C07D213/83 ,  C07D213/32 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14

Abstract: Compounds of formula (I), or pharmaceutically acceptable salts thereof, are agonists of GPR116 and are useful for the treatment of obesity, and for the treatment of diabetes.

Abstract translation: 式（I）化合物或其药学上可接受的盐是GPR116的激动剂，可用于治疗肥胖症和治疗糖尿病。

公开(公告)号：US20120264823A1

公开(公告)日：2012-10-18

申请号：US13500687

申请日：2010-04-19

Applicant: Alberto Ortega Muñoz ,  Julio Castro-Palomino Laria ,  Matthew Colin Thor Fyfe

Inventor： Alberto Ortega Muñoz ,  Julio Castro-Palomino Laria ,  Matthew Colin Thor Fyfe

IPC: A61K31/165 ,  A61K31/277 ,  C07C237/20 ,  A61P25/28 ,  A61P25/16 ,  C07C255/60 ,  A61P35/00

CPC classification number: C07C237/06 ,  C07C255/54 ,  C07C2601/02 ,  C07D213/36

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20120172358A1

公开(公告)日：2012-07-05

申请号：US13396193

申请日：2012-02-14

Applicant: 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

Inventor： 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: 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 classification number: C07D401/14 ,  C07D211/20 ,  C07D211/22 ,  C07D211/24 ,  C07D211/26 ,  C07D211/28 ,  C07D211/34 ,  C07D211/48 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.

Abstract translation: 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。

公开(公告)号：US20120077793A1

公开(公告)日：2012-03-29

申请号：US13255525

申请日：2010-03-12

Applicant: Oscar Barba ,  Peter Timothy Fry ,  Matthew Colin Thor Fyfe ,  William Gattrell ,  Revathy Perpetua Jeevaratnam ,  Thomas Martin Krulle ,  Martin James Procter ,  Colin Peter Sambrook-Smith ,  Karen Lesley Schofield ,  Donald Smyth ,  Alan John William Stewart ,  David French Stonehouse ,  Simon Andrew Swain

Inventor： Oscar Barba ,  Peter Timothy Fry ,  Matthew Colin Thor Fyfe ,  William Gattrell ,  Revathy Perpetua Jeevaratnam ,  Thomas Martin Krulle ,  Martin James Procter ,  Colin Peter Sambrook-Smith ,  Karen Lesley Schofield ,  Donald Smyth ,  Alan John William Stewart ,  David French Stonehouse ,  Simon Andrew Swain

IPC: A61K31/4439 ,  A61K31/4545 ,  C07D401/12 ,  A61K31/454 ,  A61K31/497 ,  A61P9/12 ,  A61K31/4725 ,  A61P3/10 ,  A61P3/04 ,  A61P3/00 ,  A61P3/08 ,  A61P3/06 ,  C07D401/14 ,  C07D413/14

CPC classification number: C07D401/12 ,  C07D213/64 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

Abstract: The present invention is directed to therapeutic compounds which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes.

公开(公告)号：US20110269734A1

公开(公告)日：2011-11-03

申请号：US13003546

申请日：2009-07-10

Applicant: 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

Inventor： 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: A61K31/397 ,  A61K31/506 ,  C07D401/14 ,  A61P9/12 ,  A61K31/4545 ,  A61P3/04 ,  A61P3/10 ,  A61P3/06 ,  C07D401/04 ,  A61K31/501

CPC classification number: C07D401/04 ,  C07D401/14

Abstract: Compounds of formula (I):or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of diabetes and obesity.

Abstract translation: 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。

公开(公告)号：US20100286112A1

公开(公告)日：2010-11-11

申请号：US12677153

申请日：2008-09-10

Applicant: 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

Inventor： 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: 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 classification number: C07D401/12 ,  C07D211/18 ,  C07D211/22 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20100286110A1

公开(公告)日：2010-11-11

申请号：US12738468

申请日：2008-10-10

Applicant: Matthew Colin Thor Fyfe ,  William Gattrell ,  Colin Peter Sambrook-Smith

Inventor： Matthew Colin Thor Fyfe ,  William Gattrell ,  Colin Peter Sambrook-Smith

IPC: 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 classification number: C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20100048632A1

公开(公告)日：2010-02-25

申请号：US12522015

申请日：2008-01-04

Applicant: Matthew Colin Thor Fyfe ,  John Keily ,  Simon Andrew Swain

Inventor： Matthew Colin Thor Fyfe ,  John Keily ,  Simon Andrew Swain

IPC: A61K31/454 ,  C07D413/04 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10

CPC classification number: C07D413/04

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.

Abstract translation: 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。

公开(公告)号：US20100048625A1

公开(公告)日：2010-02-25

申请号：US12522030

申请日：2008-01-04

Applicant: Matthew Colin Thor Fyfe ,  Revathy Perpetua Jeevaratnam ,  John Keily ,  Simon Andrew Swain

Inventor： Matthew Colin Thor Fyfe ,  Revathy Perpetua Jeevaratnam ,  John Keily ,  Simon Andrew Swain

IPC: A61K31/4545 ,  C07D413/14 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10

CPC classification number: C07D413/14

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.

公开(公告)号：US20080261952A1

公开(公告)日：2008-10-23

申请号：US11660405

申请日：2005-08-16

Applicant: Jason Bloxham ,  Matthew Colin Thor Fyfe ,  James Horswill ,  Revathy Perpetua Jeevaratnam ,  John Keily ,  Martin James Procter ,  Karen Lesley Schofield ,  Salam Shaaban ,  Andrew Simon Swain ,  Phillppe Wong-Kai-In

Inventor： Jason Bloxham ,  Matthew Colin Thor Fyfe ,  James Horswill ,  Revathy Perpetua Jeevaratnam ,  John Keily ,  Martin James Procter ,  Karen Lesley Schofield ,  Salam Shaaban ,  Andrew Simon Swain ,  Phillppe Wong-Kai-In

IPC: A61K31/167 ,  A61P1/00

CPC classification number: A61K31/381 ,  A61K31/341 ,  A61K31/404 ,  A61K31/426 ,  A61K31/428 ,  A61K31/44 ,  A61K31/455

Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.

Abstract translation: 通过向需要这种治疗的受试者施用有效量的芳基脲CB-1受体调节化合物来治疗与CB-1受体相关的病症，特别是肥胖症的方法。