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123 条记录 (耗时 0.048 秒)

    Thrombin receptor antagonists
    1.
    发明授权
    Thrombin receptor antagonists 有权
    凝血酶受体拮抗剂

    公开(公告)号：US07304078B2

    公开(公告)日：2007-12-04

    申请号：US10412982

    申请日：2003-04-14

    申请人： Samuel Chackalamannil ,  William J. Greenlee ,  Yuguang Wang ,  Wenxue Wu ,  Enrico P. Veltri ,  Yan Xia

    发明人： Samuel Chackalamannil ,  William J. Greenlee ,  Yuguang Wang ,  Wenxue Wu ,  Enrico P. Veltri ,  Yan Xia

    IPC分类号： A61K31/443 ,  C07D405/02

    CPC分类号： C07D405/06 ,  C07D405/14 ,  C07D417/14

    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： 式中的杂环取代三环

    Thrombin receptor antagonists
    3.
    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

    申请人： Samuel Chackalamannil ,  Martin C. Clasby ,  William J. Greenlee ,  Yuguang Wang ,  Yan Xia ,  Enrico P. Veltri ,  Mariappan V. Chelliah

    发明人： Samuel Chackalamannil ,  Martin C. Clasby ,  William J. Greenlee ,  Yuguang Wang ,  Yan Xia ,  Enrico P. Veltri ,  Mariappan V. Chelliah

    IPC分类号： A61K31/443 ,  C07D307/78

    CPC分类号： C07D405/06 ,  C07D405/14 ,  C07D417/14

    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。

    Bicyclic and tricyclic derivatives as thrombin receptor antagonists
    6.
    发明授权
    Bicyclic and tricyclic derivatives as thrombin receptor antagonists 有权
    双环和三环衍生物作为凝血酶受体拮抗剂

    公开(公告)号：US08153664B2

    公开(公告)日：2012-04-10

    申请号：US11865793

    申请日：2007-10-02

    申请人： Samuel Chackalamannil ,  Mariappan V. Chelliah ,  Yuguang Wang ,  Yan Xia

    发明人： Samuel Chackalamannil ,  Mariappan V. Chelliah ,  Yuguang Wang ,  Yan Xia

    IPC分类号： C07D401/06 ,  A61K31/4439 ,  A61P7/02 ,  A61P7/12 ,  A61P9/10 ,  A61P29/00 ,  A61P19/02 ,  A61P3/10 ,  A61P3/14 ,  A61P11/06 ,  A61P11/08

    CPC分类号： C07D401/06 ,  C07D417/06

    摘要： Heterocyclic-substituted 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 E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 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： 所述式的杂环取代三环或所述化合物，异构体或外消旋混合物的药学上可接受的盐或溶剂合物，其中代表任选的双键，虚线任选是键或无键，导致双键或单键， 如价格要求所允许的，其中E，A，GM，Het，B，X，R 3，R 10，R 11，R 32和R 33在本文中定义，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。 还要求与其它心血管药物联合治疗。