发明公开
EP1663190A1 ((((1H-INDOL-3YL) METHYLIDENE)AMINO)OXY)ACETIC ACID DERIVATIVES AND RELATED COMPOUNDS AS PAI-1 INHIBITORS FOR THE TREATMENT OF INPAIREMENT OF THE FIBRINOLYTIC SYSTEM AND OF THROMBOSIS
审中-公开
（（（（1H-吲哚-3-基）亚甲基）氨基）氧基）乙酸 - 其衍生物和相关化合物AS PAI-1抑制剂用于损伤的治疗纤溶系统和血栓形成的
- 专利标题： ((((1H-INDOL-3YL) METHYLIDENE)AMINO)OXY)ACETIC ACID DERIVATIVES AND RELATED COMPOUNDS AS PAI-1 INHIBITORS FOR THE TREATMENT OF INPAIREMENT OF THE FIBRINOLYTIC SYSTEM AND OF THROMBOSIS
- 专利标题（中）： （（（（1H-吲哚-3-基）亚甲基）氨基）氧基）乙酸 - 其衍生物和相关化合物AS PAI-1抑制剂用于损伤的治疗纤溶系统和血栓形成的
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申请号： EP04788983.7申请日： 2004-09-24
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公开(公告)号： EP1663190A1公开(公告)日： 2006-06-07
- 发明人: GOPALSAMY, Ariamala , KINCAID, Scott, Lee
- 申请人： Wyeth
- 申请人地址： Five Giralda Farms Madison, New Jersey 07940 US
- 专利权人： Wyeth
- 当前专利权人： Wyeth
- 当前专利权人地址： Five Giralda Farms Madison, New Jersey 07940 US
- 代理机构： Connelly, Michael John
- 优先权： US505913P 20030925; US947711 20040923
- 国际公布： WO2005030191 20050407
- 主分类号： A61K31/15
- IPC分类号： A61K31/15 ; C07D209/14 ; C07C251/60 ; A61P7/02
摘要：
The present invention relates to indole oxime derivatives of formula (I) wherein: R1 is -OH, -OC1-C8 alkyl, or NH2; R2 and R3 are, independently, hydrogen, C1-C8 alkyl, -CH2-C3-C6 cycloalkyl, -CH2-pyridinyl, phenyl, or benzyl; R4 is hydrogen, C1-C8 alkyl, C3-C6 cycloalkyl, -CH2-C3-C6 cycloalkyl, phenyl, benzyl, heteroaryl, or -CH2-heteoraryl; X is: formula (II), (III), (IV) or (V).The other substituents are defined in claim 1. The present compounds are PAI-1 inhibitors for the treatment of e.g. impairment of the fibrinolytic system, thrombosis or cardiovascular diseases.
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