公开(公告)号：US5795905A

公开(公告)日：1998-08-18

申请号：US468799

申请日：1995-06-06

Applicant: James R. McCarthy ,  Yun Feng Xie ,  Jeffrey P. Whitten ,  Thomas R. Webb ,  Chen Chen ,  John Y. Ramphal

Inventor： James R. McCarthy ,  Yun Feng Xie ,  Jeffrey P. Whitten ,  Thomas R. Webb ,  Chen Chen ,  John Y. Ramphal

IPC: A61K31/41 ,  A61K31/433 ,  A61K31/505 ,  A61K31/53 ,  A61P1/12 ,  A61P3/04 ,  A61P5/38 ,  A61P9/00 ,  A61P11/00 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/30 ,  A61P29/00 ,  A61P37/00 ,  A61P43/00 ,  C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D249/14 ,  C07D251/14 ,  C07D251/16 ,  C07D251/18 ,  C07D251/22 ,  C07D285/08 ,  C07D491/052

CPC classification number: C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D249/14 ,  C07D251/16 ,  C07D251/18 ,  C07D251/22 ,  C07D285/08

Abstract: CRF receptor antagonists are disclosed. Such receptor antagonists are thiadiazole-, pyrimidine-, triazine-, and triazole-containing compounds substituted with both a C3-C14 monocyclic or fused, homoaryl or heteroaryl group and a substituted amine group. The CFR receptor antagonists have utility in the treatment of a variety of disorders, including disorders associated with the hypersecretion of CRF.

Abstract translation: 公开了CRF受体拮抗剂。 这样的受体拮抗剂是被C3-C14单环或稠合，均芳基或杂芳基和取代胺基取代的噻二唑，嘧啶，三嗪和三唑化合物。 CFR受体拮抗剂可用于治疗多种疾病，包括与CRF过度分泌相关的疾病。

公开(公告)号：US5656600A

公开(公告)日：1997-08-12

申请号：US37574

申请日：1993-03-25

Applicant: Matthew M. Abelman ,  Daniel A. Pearson ,  George P. Vlasuk ,  Thomas R. Webb

Inventor： Matthew M. Abelman ,  Daniel A. Pearson ,  George P. Vlasuk ,  Thomas R. Webb

IPC: A61K38/00 ,  A61K49/00 ,  A61K51/08 ,  A61P7/02 ,  C07K5/02 ,  C07K7/02 ,  C07K14/815 ,  C07K5/00 ,  C07K7/00 ,  C07K17/00

CPC classification number: C07K5/0202 ,  A61K51/088 ,  C07K14/815 ,  A61K2123/00 ,  A61K38/00

Abstract: .alpha.-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions, diagnostic compositions and pharmaceutical compositions, which are useful for preventing or treating in a mammal a pathological condition characterized by thrombosis are described..alpha.-Ketoamide derivatives, their pharmaceutically acceptable salts, compositions and diagnostic compositions, which are useful for in vivo imaging of thrombi in a mammal are also described.Methods of preventing or treating in a mammal a pathological condition characterized by thrombosis and methods of in vivo imaging of thrombi in a mammal are also disclosed.

Abstract translation: 描述了可用于预防或治疗哺乳动物特征在于血栓形成的病理状态的α-甲基酰胺衍生物，其药学上可接受的盐，组合物，诊断组合物和药物组合物。 还描述了可用于哺乳动物血栓体内成像的α-甲基酰胺衍生物，其药学上可接受的盐，组合物和诊断组合物。 还公开了在哺乳动物中预防或治疗血栓形成的特征的病理状态和哺乳动物血栓体内成像方法。

公开(公告)号：US5597804A

公开(公告)日：1997-01-28

申请号：US139300

申请日：1993-10-18

Applicant: Thomas R. Webb ,  Todd A. Miller ,  George P. Vlasuk ,  Matthew M. Abelman

Inventor： Thomas R. Webb ,  Todd A. Miller ,  George P. Vlasuk ,  Matthew M. Abelman

IPC: A61K38/55 ,  A61K31/195 ,  A61K31/198 ,  A61K31/695 ,  A61K38/00 ,  A61K38/06 ,  A61P7/02 ,  C07C279/12 ,  C07C279/36 ,  C07C307/02 ,  C07C307/06 ,  C07C307/08 ,  C07C307/10 ,  C07C311/06 ,  C07C311/13 ,  C07C311/19 ,  C07C317/26 ,  C07D207/16 ,  C07D211/60 ,  C07D257/04 ,  C07D403/06 ,  C07D403/12 ,  C07F7/10 ,  C07K5/06 ,  C07K5/068 ,  C07K5/072 ,  C07K5/078 ,  C07K5/083 ,  C07K5/093 ,  C07K5/097 ,  C07K5/113 ,  C07K14/75 ,  A61K37/00 ,  C07K5/08 ,  A61K37/02

CPC classification number: C07D207/16 ,  C07D211/60 ,  C07D257/04 ,  C07K14/75 ,  C07K5/0606 ,  C07K5/06086 ,  C07K5/06113 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/0806 ,  C07K5/081 ,  C07K5/0819 ,  C07K5/1021 ,  A61K38/00 ,  Y10S514/822

Abstract: The present invention is directed to N-sulfonyl arginine alpha-keto-amide derivatives, their pharmaceutically acceptable salts and compositions thereof which are useful as antithrombotic agents in mammals and also the use of these compounds as antithrombotic agents. Also, disclosed are methods of using these inhibitors in their various embodiments as therapeutic agents for disease states characterized by disorders of the blood coagulation process. Further disclosed are compounds useful as intermediates in the preparation of these compounds.

Abstract translation: 本发明涉及在哺乳动物中用作抗血栓形成剂的N-磺酰基精氨酸α-酮酰胺衍生物及其药学上可接受的盐和组合物，以及这些化合物作为抗血栓形成剂的用途。 还公开了在各种实施方案中使用这些抑制剂作为以凝血过程紊乱为特征的疾病状态的治疗剂的方法。 进一步公开的是可用作制备这些化合物的中间体的化合物。