公开(公告)号：US07825111B2

公开(公告)日：2010-11-02

申请号：US11857954

申请日：2007-09-19

Applicant: Min A. Xiang ,  Mona Patel ,  Philip Rybczynski ,  Joseph Gunnet ,  Keith T. Demarest ,  Richard Look ,  Bruce Maryanoff ,  Michael J. Costanzo ,  Stephen C. Yabut

Inventor： Min A. Xiang ,  Mona Patel ,  Philip Rybczynski ,  Joseph Gunnet ,  Keith T. Demarest ,  Richard Look ,  Bruce Maryanoff ,  Michael J. Costanzo ,  Stephen C. Yabut

IPC: A61P9/00 ,  A61K31/55 ,  C07D223/14

CPC classification number: C07D487/10

Abstract: The invention is directed to nonpeptide substituted spiroheterobenzazepine of Formula I, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency, including congestive heart failure, hyponatremia, and hypertension. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, hyponatremia, renal vasospasm, renal failure, diabetic nephropathy, cerebral edema, cerebral ischemia, stroke, thrombosis, or water retention are also disclosed.

Abstract translation: 本发明涉及式I的非肽取代的螺杂肼苯并氮平，其可用作加压素受体拮抗剂，用于治疗与加压素受体活性相关的病症，例如涉及增加的血管阻力和心脏功能不全（包括充血性心力衰竭，低钠血症和高血压）的那些。 包含式I化合物的药物组合物和治疗诸如高血压，充血性心力衰竭，心脏功能不全，冠状动脉血管痉挛，心脏缺血，肝硬化，低钠血症，肾血管痉挛，肾衰竭，糖尿病性肾病，脑水肿，脑缺血， 中风，血栓形成或保水性也被公开。

公开(公告)号：US20100227857A1

公开(公告)日：2010-09-09

申请号：US12782280

申请日：2010-05-18

Applicant: Gee-Hong Kuo ,  Thomas Rano ,  Aihua Wang ,  Catherine Prouty ,  Keith T. Demarest ,  Patricia Pelton

Inventor： Gee-Hong Kuo ,  Thomas Rano ,  Aihua Wang ,  Catherine Prouty ,  Keith T. Demarest ,  Patricia Pelton

IPC: A61K31/538 ,  A61P9/12 ,  A61P9/10 ,  A61P9/00 ,  A61P3/06

CPC classification number: C07D265/36 ,  C07D279/16

Abstract: The invention is directed to compounds of Formula (I) described herein useful as CETP inhibitors, compositions containing them, and methods of using them.

Abstract translation: 本发明涉及用作CETP抑制剂的本文所述的式（I）化合物，含有它们的组合物及其使用方法。

公开(公告)号：US20070265304A1

公开(公告)日：2007-11-15

申请号：US11746755

申请日：2007-05-10

Applicant: Thomas Rano ,  Gee-Hong Kuo ,  Ellen Sieber-McMaster ,  Keith T. Demarest ,  Patricia Pelton ,  Aihua Wang

Inventor： Thomas Rano ,  Gee-Hong Kuo ,  Ellen Sieber-McMaster ,  Keith T. Demarest ,  Patricia Pelton ,  Aihua Wang

IPC: A61K31/47

CPC classification number: C07D215/12 ,  C07D215/04 ,  C07D215/14 ,  C07D401/04 ,  C07D409/04

Abstract: The invention is directed to compounds of Formula (I) described herein useful as CETP inhibitors, compositions containing them, and methods of using them.

Abstract translation: 本发明涉及用作CETP抑制剂的本文所述的式（I）化合物，含有它们的组合物及其使用方法。

公开(公告)号：US06903109B2

公开(公告)日：2005-06-07

申请号：US10259139

申请日：2002-09-27

Applicant: Geoffrey R. Heintzelman ,  Kristin M. Averill ,  John H. Dodd ,  Keith T. Demarest ,  Yuting Tang ,  Paul F. Jackson

Inventor： Geoffrey R. Heintzelman ,  Kristin M. Averill ,  John H. Dodd ,  Keith T. Demarest ,  Yuting Tang ,  Paul F. Jackson

IPC: A61K31/496 ,  A61K31/5377 ,  C07D221/16 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D413/02 ,  C07D491/04 ,  A61K31/438

CPC classification number: C07D221/16 ,  A61K31/473 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D491/04

Abstract: This invention provides novel arylindenopyridines of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing Adensine A2a receptors or reducing PDE activity in appropriate cells. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.

Abstract translation: 本发明提供了新颖的具有下列结构式的Ar 3吲哚并吡啶：和包含该化合物的药物组合物，其可用于治疗通过拮抗Adensine A2a受体或降低适当细胞中PDE活性而改善的病症。 本发明还提供了使用本发明的药物组合物的治疗和预防方法。

公开(公告)号：US06653478B2

公开(公告)日：2003-11-25

申请号：US10047841

申请日：2001-10-23

Applicant: Maud J. Urbanski ,  Joseph W. Gunnet, Jr. ,  Keith T. Demarest

Inventor： Maud J. Urbanski ,  Joseph W. Gunnet, Jr. ,  Keith T. Demarest

IPC: C07D40104

CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14

Abstract: The invention is directed to substituted benzimidazol-2-ones of Formula I, wherein A, X, Y, m, n, R1, R2, R3, R4, and R5 are as described in the specification, which are useful as vasopressin receptor antagonists or Neuropeptide Y Modulators for treating conditions such as aggression, obsessive-compulsive disorders, hypertension, dysmenorrhea, congestive heart failure/cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, edema, ischemia, stroke, thrombosis, water retention, nephrotic syndrome, central nervous injuries, obesity, anorexia, hyperglycemia, diabetes, anxiety, depression, asthma, memory loss, sexual dysfunction, disorders of sleep and other circadian rhythms, and Cushing's disease.

Abstract translation: 本发明涉及式I的取代的苯并咪唑-2-酮，其中A，X，Y，m，n，R 1，R 2，R 3，R 4和R 5如说明书中所述，其可用作加压素受体拮抗剂 或神经肽Y调节剂，用于治疗诸如侵略，强迫症，高血压，痛经，充血性心力衰竭/心脏功能不全，冠状动脉血管痉挛，心脏缺血，肝硬化，肾血管痉挛，肾衰竭，水肿，缺血，中风，血栓形成， 保水性，肾病综合征，中枢神经损伤，肥胖症，厌食症，高血糖症，糖尿病，焦虑症，抑郁症，哮喘，记忆丧失，性功能障碍，睡眠障碍和其他昼夜节律以及库欣氏病。