Thrombin receptor antagonists
    11.
    发明授权
    Thrombin receptor antagonists 有权
    凝血酶受体拮抗剂

    公开(公告)号:US07713999B2

    公开(公告)日:2010-05-11

    申请号:US11733635

    申请日:2007-04-10

    IPC分类号: A61K31/443 C07D307/78

    摘要: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the dotted line represents an optional single bond;  represents an optional double bond, n is 0-2; Q is cycloalkyl, optionally substituted by R13 and R14; R13 and R14 are independently selected from (C1-C6)alkyl, (C3-C8)cycloalkyl, —OH, (C1-C6)alkoxy, R27-aryl(C1-C6)alkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, halogen and haloalkyl; or R13 and R14 together form a spirocyclic or a heterospirocyclic ring of 3-6 atoms, Het is a mono- or bi-cyclic optionally substituted heteroaryl group; and B is a bond, alkylene, or optionally substituted alkenylene or alkynylene, wherein the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.

    摘要翻译: 具有下式的杂环取代的三环或其药学上可接受的盐,其中:虚线表示任选的单键; 表示可选的双键,n为0-2; Q是环烷基,任选被R 13和R 14取代; R 13和R 14独立地选自(C 1 -C 6)烷基,(C 3 -C 8)环烷基,-OH,(C 1 -C 6)烷氧基,R 27 - 芳基(C 1 -C 6)烷基,杂芳基,杂芳基烷基,杂环基,杂环基烷基,卤素 和卤代烷基; 或R 13和R 14一起形成3-6个原子的螺环或异环环,Het是单或双环任选取代的杂芳基; 和B是键,亚烷基或任选取代的亚烯基或亚炔基,其中剩余的取代基如说明书中所定义,以及含有它们的药物组合物和治疗与血栓形成,动脉粥样硬化,再狭窄有关的疾病的方法, 高血压,心绞痛,心律失常,心力衰竭和癌症。 还要求与其它心血管药物联合治疗。

    Oxazoloisoquinoline derivatives as thrombin receptor antagonists
    14.
    发明授权
    Oxazoloisoquinoline derivatives as thrombin receptor antagonists 有权
    恶唑啉异喹啉衍生物作为凝血酶受体拮抗剂

    公开(公告)号:US07888369B2

    公开(公告)日:2011-02-15

    申请号:US11642170

    申请日:2006-12-20

    CPC分类号: C07D487/04 C07D471/04

    摘要: This application provides for oxazolisoquinoline derivatives of the formula or a pharmaceutically acceptable salt of said compound wherein: B is —CH═CH—; M is —C(R1)(R2)—; and the remaining substituents are as defined in the specification as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. This application also provides for combination therapy with the compounds of Ib or pharmaceutically acceptable salts thereof with other cardiovascular agents.

    摘要翻译: 本申请提供了下式的恶唑啉喹啉衍生物或所述化合物的药学上可接受的盐,其中:B是-CH = CH-; M是-C(R 1)(R 2) - ; 并且其余的取代基如本说明书中所定义,以及含有它们的药物组合物以及通过施用所述化合物治疗与血栓形成,动脉粥样硬化,再狭窄,高血压,心绞痛,心律失常,心力衰竭和癌症相关的疾病的方法。 本申请还提供了将Ib化合物或其药学上可接受的盐与其它心血管药物组合治疗。

    Oxazoloisoquinoline derivatives as thrombin receptor antagonists
    18.
    发明申请
    Oxazoloisoquinoline derivatives as thrombin receptor antagonists 有权
    恶唑啉异喹啉衍生物作为凝血酶受体拮抗剂

    公开(公告)号:US20070149518A1

    公开(公告)日:2007-06-28

    申请号:US11642170

    申请日:2006-12-20

    CPC分类号: C07D487/04 C07D471/04

    摘要: Heterocyclic-substituted bi or tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein An, Mn, Un, Gn, Jn, Kn, R9, R10, R11, R32, R33, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.

    摘要翻译: 异构体或外消旋混合物的式I化合物或其药学上可接受的盐或溶剂化物,其中表示可选的双键,虚线是可选的键或无键,导致 双键或单键,如价格要求所允许的,并且其中A是N,N,N, N,N,N,R 9,R 10,R 11, 本文中定义了11,32,R 32,R 33,B和Het,并且其余取代基如说明书中所定义,以及药物 含有它们的组合物和治疗与血栓形成,动脉粥样硬化,再狭窄,高血压,心绞痛,心律失常,心力衰竭和消除相关的疾病的方法 通过施用所述化合物。 还要求与其它心血管药物联合治疗。