公开(公告)号：WO1998024784A1

公开(公告)日：1998-06-11

申请号：PCT/US1997022414

申请日：1997-12-01

Applicant: RHONE-POULENC RORER PHARMACEUTICALS INC. ,  EWING, William, R. ,  BECKER, Michael, R. ,  CHOI-SLEDESKI, Yong, Mi ,  PAULS, Heinz, W. ,  MCGARRY, Daniel, G. ,  DAVIS, Roderick, S. ,  SPADA, Alfred, P.

Inventor： RHONE-POULENC RORER PHARMACEUTICALS INC.

IPC: C07D403/02

CPC classification number: C07D207/273 ,  C07D205/085 ,  C07D207/14 ,  C07D207/416 ,  C07D211/76 ,  C07D223/12 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14

Abstract: The compounds of formula (I) exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula (I), compositions containing compounds of formula (I), and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

Abstract translation: 式（I）化合物显示出有用的药理学活性，因此并入药物组合物中并用于治疗患有某些医学病症的患者。 更具体地说，它们是因子Xa活性的抑制剂。 本发明涉及式（I）化合物，含有式（I）化合物的组合物及其用途，其用于治疗患有或受生理条件影响的患者，其可以通过施用 因子Xa的活性抑制剂。

公开(公告)号：WO0107436A3

公开(公告)日：2001-08-23

申请号：PCT/IB0001156

申请日：2000-07-26

Applicant: AVENTIS PHARM PROD INC ,  EWING WILLIAM R ,  BECKER MICHAEL R ,  CHOI SLEDESKI YONG MI ,  PAULS HEINZ W ,  HE WEI ,  CONDON STEPHEN M ,  DAVIS RODERICK S ,  HANNEY BARBARA A ,  SPADA ALFRED P ,  BURNS CHRISTOPHER J ,  JIANG JOHN Z ,  LI AIWEN ,  MYERS MICHAEL R ,  LAU WAN F ,  POLI GREGORY B

Inventor： EWING WILLIAM R ,  BECKER MICHAEL R ,  CHOI-SLEDESKI YONG MI ,  PAULS HEINZ W ,  HE WEI ,  CONDON STEPHEN M ,  DAVIS RODERICK S ,  HANNEY BARBARA A ,  SPADA ALFRED P ,  BURNS CHRISTOPHER J ,  JIANG JOHN Z ,  LI AIWEN ,  MYERS MICHAEL R ,  LAU WAN F ,  POLI GREGORY B

IPC: C07D241/08 ,  A61K31/495 ,  A61K31/496 ,  A61K31/498 ,  A61K31/502 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61P7/02 ,  A61P9/02 ,  A61P9/04 ,  A61P9/10 ,  A61P19/02 ,  A61P25/28 ,  A61P35/00 ,  A61P41/00 ,  A61P43/00 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D491/04

CPC classification number: C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D409/14 ,  C07D471/04 ,  Y02P20/582

Abstract: This invention is directed to oxoazaheterocyclyl compounds which inhibit Factor Xa, to oxoazaheterocyclyl compounds which inhibit both Factor Xa and Factor IIa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds, to a method of directly inhibiting Factor Xa and to a method of simultaneously directly inhibiting Factor Xa and Factor IIa.

公开(公告)号：WO1992018117A1

公开(公告)日：1992-10-29

申请号：PCT/US1991002471

申请日：1991-04-11

Applicant: RHONE-POULENC RORER INTERNATIONAL (HOLDINGS), ... ,  KLEIN, Scott, I. ,  MOLINO, Bruce, F. ,  DENER, Jeffrey, M. ,  CZEKAJ, Mark ,  BECKER, Michael, R.

Inventor： RHONE-POULENC RORER INTERNATIONAL (HOLDINGS), ...

IPC: A61K31/195

CPC classification number: C07K5/0819 ,  A61K38/00 ,  C07C279/18 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/0207 ,  C07K5/021 ,  C07K5/06113 ,  C07K5/0806

Abstract: Disclosed are novel peptide and pseudopeptide derivatives that inhibit platelet aggregation and thrombos formation in mammalian blood thereby being useful in the prevention and treatment of thrombosis associated with certain disease states, such as, Myocardial infraction, stroke, peripheral arterial disease and disseminated intravascular coagulation.

Abstract translation: 公开了抑制哺乳动物血液中的血小板聚集和血栓形成的新型肽和假肽衍生物，从而可用于预防和治疗与某些疾病状态如心肌梗死，中风，外周动脉疾病和弥散性血管内凝血相关的血栓形成。

公开(公告)号：WO1996040679A1

公开(公告)日：1996-12-19

申请号：PCT/US1996009816

申请日：1996-06-07

Applicant: RHONE-POULENC RORER PHARMACEUTICALS INC. ,  EWING, William, R. ,  BECKER, Michael, R. ,  PAULS, Henry, W. ,  CHENEY, Daniel, L. ,  MASON, Jonathan, Stephen ,  SPADA, Alfred, P. ,  CHOI-SLEDESKI, Yong, Mi

Inventor： RHONE-POULENC RORER PHARMACEUTICALS INC.

IPC: C07D401/06

CPC classification number: C07D207/273 ,  C07D205/085 ,  C07D207/14 ,  C07D207/416 ,  C07D211/76 ,  C07D223/12 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14

Abstract: The compounds of formula (I) exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula (I), compositions containing compounds of formula (I), and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

Abstract translation: 式（I）的化合物显示出有用的药理活性，因此并入药物组合物中并用于治疗患有某些医学病症的患者。 更特别地，它们是因子Xa的活性的抑制剂。 本发明涉及式（I）化合物，含有式（I）化合物的组合物及其用途，其用于治疗患有或经受生理条件的患者，其可以通过给予 因子Xa的活性抑制剂。

公开(公告)号：WO1992017196A1

公开(公告)日：1992-10-15

申请号：PCT/US1992002637

申请日：1992-03-30

Applicant: RHONE-POULENC RORER INTERNATIONAL (HOLDINGS) INC. ,  KLEIN, Scott, I. ,  MOLINO, Bruce, F. ,  CZEKAJ, Mark ,  GARDNER, Charles ,  BECKER, Michael, R. ,  DENER, Jeffrey, M. ,  PELLETIER, Jeffrey, C.

Inventor： RHONE-POULENC RORER INTERNATIONAL (HOLDINGS) INC.

IPC: A61K37/02

CPC classification number: C07K14/75 ,  A61K38/00 ,  C07K5/0207 ,  C07K5/021 ,  C07K5/06113 ,  C07K5/0817 ,  C07K5/0821 ,  C07K5/1019

Abstract: This invention relates to novel peptides and pseudopeptides that inhibit platelet aggregation and thrombus formation in mammalian blood thereby being useful in the prevention and treatment of thrombosis associated with disease states such as myocardial infarction, stroke, peripheral arterial disease and disseminated intravascular coagulation, to pharmaceutical compositions including such compounds and to their use in inhibiting thrombus formation and platelet aggregation in mammals.

Abstract translation: 本发明涉及抑制哺乳动物血液中的血小板聚集和血栓形成的新型肽和假肽，从而可用于预防和治疗与诸如心肌梗死，中风，外周动脉疾病和弥散性血管内凝血之类的疾病状态相关的血栓形成。 包括这些化合物及其在抑制哺乳动物血栓形成和血小板聚集中的用途。

公开(公告)号：WO1998025611A1

公开(公告)日：1998-06-18

申请号：PCT/US1997022406

申请日：1997-12-03

Applicant: RHONE-POULENC RORER PHARMACEUTICALS INC. ,  CHOI-SLEDESKI, Yong, Mi ,  PAULS, Henry, W. ,  BARTON, Jeffrey, N. ,  EWING, William, R. ,  GREEN, Daniel, M. ,  BECKER, Michael, R.

Inventor： RHONE-POULENC RORER PHARMACEUTICALS INC.

IPC: A61K31/40

CPC classification number: C07D401/06 ,  A61K31/4184 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/519 ,  C07D403/06 ,  C07D409/14 ,  C07D471/04 ,  C07D491/04 ,  C07D495/04

Abstract: The compounds of formula (I) herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula (I), compositions containing compounds of formula (I), and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

Abstract translation: 本文所述的式（I）化合物表现出有用的药理活性，因此并入药物组合物中并用于治疗患有某些医学病症的患者。 更具体地说，它们是因子Xa活性的抑制剂。 本发明涉及式（I）化合物，含有式（I）化合物的组合物及其用途，其用于治疗患有或受生理条件影响的患者，其可以通过施用 因子Xa的活性抑制剂。