公开(公告)号：US07244738B2

公开(公告)日：2007-07-17

申请号：US10884768

申请日：2004-07-02

申请人： Terrence Joseph Connolly ,  Paul Francis Keitz ,  Eun Kyung Lee ,  Jim Li ,  Francisco Javier Lopez-Tapia ,  Patrick Finbar McGarry ,  Chris Richard Melville ,  Dov Nitzan ,  Counde O'Yang ,  Fernando Padilla ,  Klaus Kurt Weinhardt

发明人： Terrence Joseph Connolly ,  Paul Francis Keitz ,  Eun Kyung Lee ,  Jim Li ,  Francisco Javier Lopez-Tapia ,  Patrick Finbar McGarry ,  Chris Richard Melville ,  Dov Nitzan ,  Counde O'Yang ,  Fernando Padilla ,  Klaus Kurt Weinhardt

IPC分类号： A61K31/517 ,  A01N43/54 ,  C07D239/72 ,  A61K31/549 ,  C07D417/02 ,  C07D285/26

CPC分类号： C07D401/12 ,  C07D239/90 ,  C07D239/95 ,  C07D285/24 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

摘要： Compounds represented by Formula I: which are useful as are alpha-1A/B adrenoceptor antagonists, to methods of treating conditions associated with the activity of alpha-1A/B adrenoceptors, and to methods of making said compounds, wherein Ar, Z, R, R′, R5 and R10 are as defined herein.

摘要翻译： 由式I表示的化合物：其可用作α-1A / B肾上腺素受体拮抗剂，用于治疗与α-1A / B肾上腺素受体的活性相关的病症的方法，以及制备所述化合物的方法，其中Ar，Z，R R'，R 5和R 10如本文所定义。

公开(公告)号：US07214699B2

公开(公告)日：2007-05-08

申请号：US10724971

申请日：2003-12-01

申请人： Richard Leo Cournoyer ,  David Garrett Loughhead ,  Counde O'Yang

发明人： Richard Leo Cournoyer ,  David Garrett Loughhead ,  Counde O'Yang

IPC分类号： A61K31/416 ,  C07D231/56

CPC分类号： C07D209/44 ,  C07D231/56 ,  C07D401/04

摘要： This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II: wherein R3 is optionally substituted aryl or heteroaryl, R1 and R2 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts thereof. The invention further relates to processes for preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for their use as therapeutic agents.

公开(公告)号：US07141584B2

公开(公告)日：2006-11-28

申请号：US10731607

申请日：2003-12-09

申请人： Keith Roger Bley ,  Robin Douglas Clark ,  Alam Jahangir ,  Bruce Andrew Kowalczyk ,  Francisco Javier Lopez-Tapia ,  Alexander Victor Muehldorf ,  Counde O'Yang ,  Thomas Weitao Sun

发明人： Keith Roger Bley ,  Robin Douglas Clark ,  Alam Jahangir ,  Bruce Andrew Kowalczyk ,  Francisco Javier Lopez-Tapia ,  Alexander Victor Muehldorf ,  Counde O'Yang ,  Thomas Weitao Sun

IPC分类号： A61K31/454 ,  C07D401/12

CPC分类号： C07D401/10 ,  C07D233/50 ,  C07D403/12 ,  C07D405/12 ,  C07D409/10 ,  C07D409/12 ,  C07D417/10

摘要： This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I: where: R1 is a group represented by formula (A), (B) or (C); and other substituents as defined in the specification, and their pharmaceutically acceptable salts or crystal forms thereof; and pharmaceutical compositions containing them; and methods for their use as therapeutic agents.

摘要翻译： 本发明涉及选自由式I表示的化合物组的IP受体拮抗剂：其中：R 1是由式（A），（B）或（C）表示的基团; 和说明书中定义的其它取代基及其药学上可接受的盐或晶体形式; 和含有它们的药物组合物; 以及用作治疗剂的方法。

公开(公告)号：US06472536B1

公开(公告)日：2002-10-29

申请号：US09666065

申请日：2000-09-19

申请人： Keith Roger Bley ,  Robin Douglas Clark ,  Alam Jahangir ,  Bruce Andrew Kowalczyk ,  Francisco Javier Lopez-Tapia ,  Alexander Victor Muehldorf ,  Counde O'Yang ,  Thomas Weitao Sun

发明人： Keith Roger Bley ,  Robin Douglas Clark ,  Alam Jahangir ,  Bruce Andrew Kowalczyk ,  Francisco Javier Lopez-Tapia ,  Alexander Victor Muehldorf ,  Counde O'Yang ,  Thomas Weitao Sun

IPC分类号： C07D23350

CPC分类号： C07D401/10 ,  C07D233/50 ,  C07D403/12 ,  C07D405/12 ,  C07D409/10 ,  C07D409/12 ,  C07D417/10

摘要： This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I: where: R1 is a group represented by formula (A), (B) or (C); and other substituents as defined in the specification, and their pharmaceutically acceptable salts or crystal forms thereof; and pharmaceutical compositions containing them; and methods for their use as therapeutic agents.

摘要翻译： 本发明涉及选自由式I表示的化合物组的IP受体拮抗剂：其中：R1是由式（A），（B）或（C）表示的基团;以及本说明书中定义的其它取代基，它们 药学上可接受的盐或其晶体形式; 和含有它们的药物组合物; 以及用作治疗剂的方法。

公开(公告)号：US06184242B2

公开(公告)日：2001-02-06

申请号：US09137507

申请日：1998-08-20

申请人： Keith Roger Bley ,  Robin Douglas Clark ,  Alam Jahangir ,  Bruce Andrew Kowalczyk ,  Francisco Javier Lopez-Tapia ,  Alexander Victor Muehldorf ,  Counde O'Yang ,  Thomas Weitao Sun

发明人： Keith Roger Bley ,  Robin Douglas Clark ,  Alam Jahangir ,  Bruce Andrew Kowalczyk ,  Francisco Javier Lopez-Tapia ,  Alexander Victor Muehldorf ,  Counde O'Yang ,  Thomas Weitao Sun

IPC分类号： A61K314168

CPC分类号： C07D401/10 ,  C07D233/50 ,  C07D403/12 ,  C07D405/12 ,  C07D409/10 ,  C07D409/12 ,  C07D417/10

摘要： This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I: where: R1 is a group represented by formula (A), (B) or (C); and other substituents as defined in the specification, and their pharmaceutically acceptable salts or crystal forms thereof; and pharmaceutical compositions containing them; and methods for their use as therapeutic agents.

摘要翻译： 本发明涉及选自由式I表示的化合物组的IP受体拮抗剂：其中：R1是由式（A），（B）或（C）表示的基团;以及本说明书中定义的其它取代基， 药学上可接受的盐或其晶体形式; 和含有它们的药物组合物; 以及用作治疗剂的方法。

公开(公告)号：US4983627A

公开(公告)日：1991-01-08

申请号：US269811

申请日：1988-11-10

申请人： Counde O'Yang ,  Walter Kurz ,  Keith A. M. Walker ,  Helen Y. Wu

发明人： Counde O'Yang ,  Walter Kurz ,  Keith A. M. Walker ,  Helen Y. Wu

IPC分类号： C07C33/042 ,  C07C33/05 ,  C07C33/14 ,  C07C33/30 ,  C07C35/31 ,  C07C45/29 ,  C07C45/42 ,  C07C45/45 ,  C07C45/59 ,  C07C45/62 ,  C07C45/67 ,  C07C45/68 ,  C07C49/513 ,  C07C49/557 ,  C07C49/633 ,  C07C49/693 ,  C07C49/743 ,  C07C62/32 ,  C07C69/732 ,  C07C251/44 ,  C07C405/00 ,  C07D317/72 ,  C07F7/18

CPC分类号： C07F7/1864 ,  C07C251/44 ,  C07C33/042 ,  C07C33/05 ,  C07C33/14 ,  C07C33/30 ,  C07C35/31 ,  C07C405/0083 ,  C07C45/292 ,  C07C45/42 ,  C07C45/455 ,  C07C45/59 ,  C07C45/62 ,  C07C45/67 ,  C07C45/673 ,  C07C45/68 ,  C07C49/513 ,  C07C49/557 ,  C07C49/633 ,  C07C49/693 ,  C07C49/743 ,  C07C62/32 ,  C07C69/732 ,  C07D317/72 ,  C07F7/1852 ,  C07F7/1856 ,  C07C2102/22 ,  Y10S514/824

摘要： Compounds useful in treating or preventing gastrointestinal ulcers and in treating cardiovascular disorders such as thrombosis, hypertension and atherosclerosis are depicted in formulas (1), (2) and (3): ##STR1## wherein: A is --C.tbd.C--, trans --HC.dbd.CH--, trans --CH.dbd.CHCH.sub.2 -- or --CH.sub.2 CH.sub.2 --;X is lower alkyl of 1-6 carbon atoms;Y is hydrogen, exo-(lower alkyl) or endo-(lower alkyl);n is an integer from 2-4;R.sub.1 is --CH.sub.2 OH, --CHO, --CO.sub.2 R or --CO.sub.2 H, and the olefin formed by the R.sub.1 (CH.sub.2).sub.n CH.dbd. moiety is either (E) or (Z);R.sub.2 is hydrogen or methyl, or optionally --CH.dbd.CH.sub.2 when A is trans --CH.dbd.CHCH.sub.2 --; andR.sub.3 is linear or branched alkyl, alkenyl or alkynyl having 5-10 carbon atoms, ##STR2## --(CH.sub.2).sub.m -phenyl or CH.sub.2 O-phenyl; in which each phenyl may be optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen. in which:a is an integer of 0, 1 or 2;b is an integer of 3-7;m is an integer of 0, 1 or 2; andR is ##STR3## wherein X' is ##STR4## in which each R.sub.4 is independently hydrogen or lower alkyl having 1-6 carbon atoms, or a pharmaceutically acceptable, non-toxic salt or ester thereof.

摘要翻译： （1），（2）和（3）中描述了可用于治疗或预防胃肠溃疡和治疗心血管疾病如血栓形成，高血压和动脉粥样硬化的化合物：（2） + TR 。

公开(公告)号：US07799816B2

公开(公告)日：2010-09-21

申请号：US12365247

申请日：2009-02-04

申请人： Counde O'Yang ,  Robert Greenhouse

发明人： Counde O'Yang ,  Robert Greenhouse

IPC分类号： A61K31/4164 ,  A61P13/00 ,  C07D233/06

CPC分类号： C07D233/24 ,  C07D233/06

摘要： This invention relates to an alpha-1 A receptor partial agonist, which is represented by Formula I: and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing formula I, methods for their use as therapeutic agents, and methods of preparation thereof.

摘要翻译： 本发明涉及由式I表示的α-1A受体部分激动剂及其药学上可接受的盐或溶剂化物。 本发明还涉及含有式I的药物组合物，其用作治疗剂的方法及其制备方法。

公开(公告)号：US07741326B2

公开(公告)日：2010-06-22

申请号：US11983319

申请日：2007-11-08

申请人： Joe Timothy Bamberg ,  Counde O'Yang ,  Meng Sui ,  Shu-Hai Zhao

发明人： Joe Timothy Bamberg ,  Counde O'Yang ,  Meng Sui ,  Shu-Hai Zhao

IPC分类号： A61K31/404 ,  C07D209/42 ,  A61K31/4524 ,  A61K31/454 ,  C07D401/04 ,  C07D405/04

CPC分类号： C07D209/42 ,  C07D209/30 ,  C07D307/80 ,  C07D307/82 ,  C07D307/85 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04

摘要： Compounds of formula I or formula II: or pharmaceutically acceptable salts thereof, wherein m, n, p, Ar R1, R2, R4, and R5 are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds.

摘要翻译： 式I或式II化合物或其药学上可接受的盐，其中m，n，p，Ar 1，R 2，R 4和R 5如本文所定义。 本发明还提供了制备方法，组合物和使用化合物的方法。

公开(公告)号：US20090197932A1

公开(公告)日：2009-08-06

申请号：US12365260

申请日：2009-02-04

申请人： Counde O'Yang ,  Dennis Mitsugu Yasuda

发明人： Counde O'Yang ,  Dennis Mitsugu Yasuda

IPC分类号： A61K31/4164 ,  C07D233/06 ,  A61P13/00

CPC分类号： C07D233/24

摘要： This invention relates to an alpha-1A receptor partial agonist, which is represented by Formula I: and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing formula I, methods for their use as therapeutic agents, and methods of preparation thereof.

公开(公告)号：US07312230B2

公开(公告)日：2007-12-25

申请号：US11240547

申请日：2005-09-30

申请人： Richard Leo Cournoyer ,  Paul Francis Keitz ,  Lee Edwin Lowrie, Jr. ,  Alexander Victor Muehldorf ,  Counde O'Yang ,  Dennis Mitsugu Yasuda

发明人： Richard Leo Cournoyer ,  Paul Francis Keitz ,  Lee Edwin Lowrie, Jr. ,  Alexander Victor Muehldorf ,  Counde O'Yang ,  Dennis Mitsugu Yasuda

IPC分类号： A61K31/44 ,  A61K31/435 ,  C07D215/38 ,  C07D215/00 ,  C07D215/02

CPC分类号： C07D263/56 ,  C07C271/22 ,  C07C311/08 ,  C07C311/21 ,  C07D209/08 ,  C07D215/14 ,  C07D235/18 ,  C07D307/12 ,  C07D307/80 ,  C07D405/14 ,  C07D409/04

摘要： This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein: R1, R2, and R3 are each independently in each occurrence aryl or heteroaryl; R4 is —COOH or tetrazolyl; A, B, m, n, and r are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and processes for their preparation.

摘要翻译： 本发明涉及通常为IP受体拮抗剂并由式I表示的化合物：其中：R 1，R 2和R 3， 各自独立地为芳基或杂芳基; R 4是-COOH或四唑基; A，B，m，n和r如说明书中所定义; 或各异构体，异构体的外消旋或非外消旋混合物，或其药学上可接受的盐或溶剂合物。 本发明还涉及含有这些化合物的药物组合物，其用作治疗剂的方法及其制备方法。