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    Thrombin receptor antagonists
    2.
    发明申请
    Thrombin receptor antagonists 有权
    凝血酶受体拮抗剂

    公开(公告)号：US20060079684A1

    公开(公告)日：2006-04-13

    申请号：US11243708

    申请日：2005-10-05

    申请人： Samuel Chackalamannil ,  Mariappan Chelliah ,  Yan Xia ,  Keith Eagen

    发明人： Samuel Chackalamannil ,  Mariappan Chelliah ,  Yan Xia ,  Keith Eagen

    IPC分类号： C07D413/02 ,  C07D405/02

    CPC分类号： C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D491/10

    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 A, B, G, M, X, J, n, Het, 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： 式中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化物，其中表示可选的双键，虚线是可选的键或无键，导致双重 键或单键，如价格要求所允许的，并且其中A，B，G，M，X，J，n，Het，R 3，R 10， 本文定义了R 11，R 32和R 33，并且其余的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。

    Bicyclic And Tricyclic Derivatives As Thrombin Receptor Antagonists
    3.
    发明申请
    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：US20080090830A1

    公开(公告)日：2008-04-17

    申请号：US11865793

    申请日：2007-10-02

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

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

    IPC分类号： A61K31/4427 ,  A61K31/435 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/502 ,  A61P1/00 ,  A61P11/00 ,  A61P15/00 ,  A61P17/00 ,  A61P35/00 ,  A61P9/00 ,  C07D221/06 ,  C07D401/06 ,  C07D413/02 ,  C07D487/00

    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 bonds the dotted line is optionally a bond or no bonds 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 failures 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下式的杂环取代三环或其药学上可接受的盐或溶剂合物，其中表示可选的双键，虚线可选地是一个键或没有导致双键或单键的键，如允许 通过化合价要求，其中E，A，GM，Het，B，X，R 3，R 10，R 11， 本文定义了SUP 32和33 SS，其余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有关的疾病的方法 ，动脉粥样硬化，再狭窄，高血压，心绞痛，心律失常，心脏衰竭和癌症。 还要求与其它心血管药物联合治疗。

    Spirocyclic thrombin receptor antagonists
    4.
    发明申请
    Spirocyclic thrombin receptor antagonists 有权
    螺环状凝血酶受体拮抗剂

    公开(公告)号：US20060223808A1

    公开(公告)日：2006-10-05

    申请号：US11392324

    申请日：2006-03-29

    申请人： Samuel Chackalamannil ,  Mariappan Chelliah ,  Yan Xia

    发明人： Samuel Chackalamannil ,  Mariappan Chelliah ,  Yan Xia

    IPC分类号： A61K31/4747 ,  A61K31/502 ,  C07D413/02

    CPC分类号： C07D263/52 ,  C07D413/08

    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 An, En, 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下式的杂环取代三环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，导致双重 债券或单一债券，如价格要求所允许的，并且其中A N，N，N，N， N，N，N，N，R 9，R 10， 在本文中定义，其余取代基如本说明书中所定义，其中R 11，R 32，R 32和/ ，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，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。

    THROMBIN RECEPTOR ANTAGONISTS
    5.
    发明申请
    THROMBIN RECEPTOR ANTAGONISTS 审中-公开
    硫蛋白受体拮抗剂

    公开(公告)号：US20070270439A1

    公开(公告)日：2007-11-22

    申请号：US11774358

    申请日：2007-07-06

    申请人： Samuel Chackalamannil ,  Martin Clasby ,  William Greenlee ,  Yuguang Wang ,  Yan Xia ,  Enrico Veltri ,  Mariappan Chelliah

    发明人： Samuel Chackalamannil ,  Martin Clasby ,  William Greenlee ,  Yuguang Wang ,  Yan Xia ,  Enrico Veltri ,  Mariappan Chelliah

    IPC分类号： A61K31/4427 ,  A61K31/506 ,  A61P29/00 ,  A61P35/00 ,  A61P9/00 ,  A61P9/02 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  C07D221/00 ,  C07D239/26

    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; “img id =”custom-character-00001“he =”2.79mm“wi =”7.03mm“file =”US20070270439A1-20071122-P00002.TIF“img-content =”character“img-format =”tif“/> 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 -C 6）烷基，（C

    THROMBIN RECEPTOR ANTAGONISTS
    6.
    发明申请
    THROMBIN RECEPTOR ANTAGONISTS 有权
    硫蛋白受体拮抗剂

    公开(公告)号：US20070179187A1

    公开(公告)日：2007-08-02

    申请号：US11733635

    申请日：2007-04-10

    申请人： Samuel Chackalamannil ,  Martin Clasby ,  William Greenlee ,  Yuguang Wang ,  Yan Xia ,  Enrico Veltri ,  Mariappan Chelliah

    发明人： Samuel Chackalamannil ,  Martin Clasby ,  William Greenlee ,  Yuguang Wang ,  Yan Xia ,  Enrico Veltri ,  Mariappan Chelliah

    IPC分类号： A61K31/4433 ,  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： 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; “img id =”custom-character-00001“he =”3.13mm“wi =”7.37mm“file =”US20070179187A1-20070802-P00001.TIF“alt =”custom character“img-content =”character“img-format =“tif”/>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 -C 6）烷基，（C

    Thrombin receptor antagonists
    9.
    发明申请
    Thrombin receptor antagonists 审中-公开
    凝血酶受体拮抗剂

    公开(公告)号：US20060106050A1

    公开(公告)日：2006-05-18

    申请号：US11311083

    申请日：2005-12-19

    申请人： Samuel Chakalamannil ,  Mariappan Chelliah ,  Martin Clasby ,  Yan Xia

    发明人： Samuel Chakalamannil ,  Mariappan Chelliah ,  Martin Clasby ,  Yan Xia

    IPC分类号： A61K31/4741 ,  C07D491/02

    CPC分类号： C07D491/04 ,  C07D493/04 ,  C07D495/04

    摘要： Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salts thereof, wherein: n1 and n2 are independently 0-2; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is alkyl or optionally substituted alkenyl; R22 is —COR23 or a carboxy, sulfinyl, sulfonyl, sulfonamide or amino acid derivative; R23 is haloalkyl; alkenyl; haloalkenyl; alkynyl; optionally substituted cycloalkyl; cycloalkyl-alkyl; aryl; arylalkyl; heteroaryl; heterocycloalkyl; or —COOH and/or —SO3H substituted alkyl; R1, R2, R3, R9, R10 and R11 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.

    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：n 1和n 2个独立地为0-2; Het是任选取代的单，双或三环杂芳族基团; B是烷基或任选取代的烯基; R 22是-COR 23或羧基，亚磺酰基，磺酰基，磺酰胺或氨基酸衍生物; R 23是卤代烷基; 烯基; 卤代烯基 炔基; 任选取代的环烷基 环烷基 - 烷基; 芳基; 芳烷基 杂芳基; 杂环烷基; 或-COOH和/或-SO 3 H取代的烷基; R 1，R 2，R 3，R 9，R 10和R 9， R 11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。