公开(公告)号：US20110218197A1

公开(公告)日：2011-09-08

申请号：US13034922

申请日：2011-02-25

Applicant: Mark R. PLAYER ,  Raul Calvo ,  Jinsheng Chen ,  Sanath Meegalla ,  Daniel Parks ,  William Parsons ,  Scott Ballentine ,  Shawn Branum

Inventor： Mark R. PLAYER ,  Raul Calvo ,  Jinsheng Chen ,  Sanath Meegalla ,  Daniel Parks ,  William Parsons ,  Scott Ballentine ,  Shawn Branum

IPC: A61K31/5377 ,  C07D471/04 ,  A61K31/437 ,  A61P29/00 ,  A61P9/00 ,  C07D473/00 ,  A61K31/52 ,  C07D487/04 ,  A61K31/4985

CPC classification number: C07D471/04 ,  C07B2200/13 ,  C07C53/18 ,  C07C309/04 ,  C07D473/00 ,  C07D487/04

Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.

Abstract translation: 本发明涉及取代的氮杂 - 双环咪唑衍生物，含有它们的药物组合物及其用于治疗由TRP M8调节的病症和状况的用途，包括例如炎症性疼痛，炎性痛觉过敏，炎症性超敏反应性病症，神经性疼痛，神经性 冷异常性疼痛，炎性体痛痛觉过敏，炎性内脏痛觉过敏，由寒冷和肺部疾病加重的心血管疾病加重。

公开(公告)号：US20110190364A1

公开(公告)日：2011-08-04

申请号：US13084718

申请日：2011-04-12

Applicant: Mark R. Player ,  Scott L. Dax ,  William H. Parsons ,  Michael Richard Brandt ,  Raul R. Calvo ,  Sharmila Patel ,  Jian Liu ,  Wing S. Cheung ,  Michele C. Jetter ,  Yu-Kai Lee ,  Mark A. Youngman ,  Wenxi Pan ,  Kenneth M. Wells ,  Derek A. Beauchamp

Inventor： Mark R. Player ,  Scott L. Dax ,  William H. Parsons ,  Michael Richard Brandt ,  Raul R. Calvo ,  Sharmila Patel ,  Jian Liu ,  Wing S. Cheung ,  Michele C. Jetter ,  Yu-Kai Lee ,  Mark A. Youngman ,  Wenxi Pan ,  Kenneth M. Wells ,  Derek A. Beauchamp

IPC: A61K31/4184 ,  A61P29/00

CPC classification number: C07D401/06 ,  C07D235/08 ,  C07D403/06

Abstract: The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them.

Abstract translation: 本发明涉及式（I）的化合物：含有这些化合物的药物组合物和使用它们的治疗方法。

公开(公告)号：US07608622B2

公开(公告)日：2009-10-27

申请号：US11233725

申请日：2005-09-23

Applicant: Jian Liu ,  Raymond J. Patch ,  Mark R. Player ,  Huaping Hu

Inventor： Jian Liu ,  Raymond J. Patch ,  Mark R. Player ,  Huaping Hu

IPC: A01N43/58 ,  A61K31/50 ,  A01N43/60 ,  A61K31/495 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00 ,  C07D495/00 ,  C07D497/00

CPC classification number: C07D487/04

Abstract: The invention is directed to compounds of Formula I: wherein Q, Y, A are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein kinases, especially Aurora-1, Aurora-2 and Aurora-3 kinases.

Abstract translation: 本发明涉及式I化合物：其中Q，Y，A在本说明书中列出，以及其抑制蛋白激酶，特别是Aurora-1，Aurora-2的溶剂合物，水合物，互变异构体或其药学上可接受的盐 和Aurora-3激酶。

公开(公告)号：US20070259936A1

公开(公告)日：2007-11-08

申请号：US11734984

申请日：2007-04-13

Applicant: Mark R. Player ,  Scott L. Dax ,  William H. Parsons ,  Michael Richard Brandt ,  Raul R. Calvo ,  Sharmila Patel ,  Jian Liu ,  Wing S. Cheung ,  Michele C. Jetter ,  Yu-Kai Lee ,  Mark A. Youngman ,  Wenxi Pan ,  Kenneth M. Weils ,  Derek A. Beauchamp

Inventor： Mark R. Player ,  Scott L. Dax ,  William H. Parsons ,  Michael Richard Brandt ,  Raul R. Calvo ,  Sharmila Patel ,  Jian Liu ,  Wing S. Cheung ,  Michele C. Jetter ,  Yu-Kai Lee ,  Mark A. Youngman ,  Wenxi Pan ,  Kenneth M. Weils ,  Derek A. Beauchamp

IPC: A61K31/4184

CPC classification number: C07D401/06 ,  C07D235/08 ,  C07D403/06

Abstract: The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them.

Abstract translation: 本发明涉及式（I）的化合物：含有这些化合物的药物组合物和使用它们的治疗方法。

公开(公告)号：US20100292276A1

公开(公告)日：2010-11-18

申请号：US12773083

申请日：2010-05-04

Applicant: Raul R. Calvo ,  Sanath K. Meegalla ,  Mark R. Player

Inventor： Raul R. Calvo ,  Sanath K. Meegalla ,  Mark R. Player

IPC: A61K31/4184 ,  C07D235/08 ,  C07D405/06 ,  C07D405/10 ,  C07D409/06 ,  C07D405/14 ,  A61K31/4439 ,  C07D401/10 ,  A61P29/00 ,  A61P9/00 ,  A61P9/12 ,  A61P25/24 ,  A61P25/00

CPC classification number: C07D235/08 ,  C07D235/10 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06

Abstract: The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8 (transient receptor potential M8 channel). More particularly, the compounds of the present invention are useful in the treatment of inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold, anxiety and depression.

Abstract translation: 本发明涉及苯并咪唑衍生物，含有它们的药物组合物及其在治疗由TRP M8（瞬时受体电位M8通道）调节的病症和状况中的用途。 更具体地说，本发明的化合物可用于治疗炎症性疼痛，炎性痛觉过敏，炎性过敏症状，神经性疼痛，神经性寒冷异常性疼痛，炎症性体征痛觉过敏，炎性内脏痛觉过敏，由冷，焦虑和抑郁加重的心血管疾病。

公开(公告)号：US07427683B2

公开(公告)日：2008-09-23

申请号：US10970865

申请日：2004-10-22

Applicant: Mark R. Player ,  Nand Baindur ,  Benjamin Brandt ,  Naresh Chadha ,  Raymond J. Patch ,  Davoud Asgari ,  Taxiarchis Georgiadis

Inventor： Mark R. Player ,  Nand Baindur ,  Benjamin Brandt ,  Naresh Chadha ,  Raymond J. Patch ,  Davoud Asgari ,  Taxiarchis Georgiadis

IPC: A61K31/454 ,  C07D401/12

CPC classification number: C07D405/12 ,  C07D207/416 ,  C07D233/90 ,  C07D307/68 ,  C07D409/12

Abstract: The invention is directed to compounds of Formulae I: wherein A, R1, R2, R3, R4, X, and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.

Abstract translation: 本发明涉及式I的化合物：其中A，R 1，R 2，R 3，R 4， 说明书中列出了SUB，X和W，以及其抑制蛋白酪氨酸激酶，特别是c-fms激酶的溶剂合物，水合物，互变异构体或其药学上可接受的盐。

公开(公告)号：US08680098B2

公开(公告)日：2014-03-25

申请号：US13034922

申请日：2011-02-25

Applicant: Mark R. Player ,  Raul Calvo ,  Jinsheng Chen ,  Sanath Meegalla ,  Daniel Parks ,  William Parsons ,  Scott Ballentine ,  Shawn Branum

Inventor： Mark R. Player ,  Raul Calvo ,  Jinsheng Chen ,  Sanath Meegalla ,  Daniel Parks ,  William Parsons ,  Scott Ballentine ,  Shawn Branum

IPC: C07D471/04 ,  A61K31/5377 ,  A61K31/437 ,  A61K31/52 ,  A61K31/4985 ,  A61P29/00 ,  C07D487/04

CPC classification number: C07D471/04 ,  C07B2200/13 ,  C07C53/18 ,  C07C309/04 ,  C07D473/00 ,  C07D487/04

Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.

Abstract translation: 本发明涉及取代的氮杂 - 双环咪唑衍生物，含有它们的药物组合物及其用于治疗由TRP M8调节的病症和状况的用途，包括例如炎症性疼痛，炎性痛觉过敏，炎症性超敏反应性病症，神经性疼痛，神经性 冷异常性疼痛，炎性体痛痛觉过敏，炎性内脏痛觉过敏，由寒冷和肺部疾病加重的心血管疾病加重。

公开(公告)号：US20120202856A1

公开(公告)日：2012-08-09

申请号：US13364352

申请日：2012-02-02

Applicant: Mark R. PLAYER ,  Raul CALVO ,  Jinsheng CHEN ,  Carl ILLIG ,  Sanath MEEGALLA ,  Daniel PARKS ,  William PARSONS

Inventor： Mark R. PLAYER ,  Raul CALVO ,  Jinsheng CHEN ,  Carl ILLIG ,  Sanath MEEGALLA ,  Daniel PARKS ,  William PARSONS

IPC: A61K31/4184 ,  C07D413/04 ,  A61K31/422 ,  C07D405/04 ,  A61P9/12 ,  A61K31/427 ,  A61K31/4196 ,  A61K31/4245 ,  A61P25/00 ,  A61P9/00 ,  C07D403/04 ,  C07D417/04

CPC classification number: C07D413/04 ,  C07D403/04 ,  C07D405/04 ,  C07D417/04

Abstract: The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.

Abstract translation: 本发明涉及苯并咪唑衍生物，含有它们的药物组合物及其用于治疗由TRP M8调节的病症和状况的用途，包括例如炎症性疼痛，炎性痛觉过敏，炎症性超敏反应性病症，神经性疼痛，神经性冷性异常性疼痛，炎性反应 体温痛觉过敏，炎性内脏痛觉过敏，寒冷和肺部疾病加重的心血管疾病加重。

公开(公告)号：US07790724B2

公开(公告)日：2010-09-07

申请号：US11407605

申请日：2006-04-20

Applicant: Mark R. Player ,  Nand Baindur ,  Benjamin Brandt ,  Naresh Chadha ,  Raymond J. Patch ,  Davoud Asgari ,  Taxiarchis M. Georgiadis

Inventor： Mark R. Player ,  Nand Baindur ,  Benjamin Brandt ,  Naresh Chadha ,  Raymond J. Patch ,  Davoud Asgari ,  Taxiarchis M. Georgiadis

IPC: A61K31/4439 ,  C07D403/02

CPC classification number: C07D405/12 ,  C07D307/68 ,  C07D409/12

Abstract: The invention is directed to compounds of Formula II: wherein A, R1, R2, R3, R4, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.

Abstract translation: 本发明涉及式II化合物：其中A，R 1，R 2，R 3，R 4，X，Y和W在说明书中列出，以及其抑制蛋白质的溶剂合物，水合物，互变异构体或其药学上可接受的盐 酪氨酸激酶，特别是c-fms激酶。

公开(公告)号：US20100093788A1

公开(公告)日：2010-04-15

申请号：US12576283

申请日：2009-10-09

Applicant: Mark R. Player ,  Daniel J. Parks ,  William Parsons ,  Senath K. Meegalla ,  Carl R. Illig ,  Shelley K. Ballentine

Inventor： Mark R. Player ,  Daniel J. Parks ,  William Parsons ,  Senath K. Meegalla ,  Carl R. Illig ,  Shelley K. Ballentine

IPC: A61K31/437 ,  C07D261/20 ,  A61K31/42 ,  C07D498/10 ,  C07D263/52 ,  A61K31/421 ,  C07D471/02 ,  A61P29/00 ,  A61P25/24 ,  A61P9/00

CPC classification number: C07D261/20 ,  C07D263/52 ,  C07D403/04 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D498/10

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein W1, W2, W3, R1, R1a, R2, R2a, R3, V, Q, and X are defined herein.

Abstract translation: 公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。 这样的化合物由式I表示如下：其中W1，W2，W3，R1，R1a，R2，R2a，R3，V，Q和X如本文所定义。