Substituted bicyclic piperidinyl- and piperazinyl-sulfonamides useful to inhibit 11β-hydroxysteroid dehydrogenase type-1
    3.
    发明授权
    Substituted bicyclic piperidinyl- and piperazinyl-sulfonamides useful to inhibit 11β-hydroxysteroid dehydrogenase type-1 有权
    用于抑制1型11β-羟类固醇脱氢酶的二取代的双环哌啶基和哌嗪基 - 磺酰胺

    公开(公告)号:US08604195B2

    公开(公告)日:2013-12-10

    申请号:US12672825

    申请日:2008-08-12

    CPC分类号: C07D451/04 C07D491/08

    摘要: In its many embodiments, the present invention relates to a novel class of substituted bicyclic piperidinyl- and piperazinylsulfonamide compounds useful to inhibit 11β-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11β-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.

    摘要翻译: 在其许多实施方案中,本发明涉及一类新颖的取代的双环哌啶基和哌嗪基磺酰胺化合物,其可用于抑制含有该化合物的11β-羟类固醇脱氢酶I型药物组合物,以及治疗,预防,抑制或改善 与使用这些化合物或药物组合物的-11β-羟基类固醇脱氢酶I型的表达相关的一个或多个条件。

    Bicyclic and tricyclic derivatives as thrombin receptor antagonists
    5.
    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

    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。

    Substituted bicyclic and tricyclic thrombin receptor antagonists
    8.
    发明授权
    Substituted bicyclic and tricyclic thrombin receptor antagonists 有权
    取代的双环和三环凝血酶受体拮抗剂

    公开(公告)号:US08022088B2

    公开(公告)日:2011-09-20

    申请号:US11769018

    申请日:2007-06-27

    CPC分类号: C07D405/06

    摘要: Substituted bicyclic and tricyclic modified himbacine derivative of the formula: or a pharmaceutically acceptable salt or solvate of said compound wherein represents an optional double bond and wherein En, Fn, Gn, Zn, Jn, X, R3, R9, R10, R11, R32, R33, B and Het are herein defined 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 agents is also claimed.

    摘要翻译: 其中代表任选的双键的取代的双环和三环修饰的烟草衍生物,或其药学上可接受的盐或溶剂化物,其中En,Fn,Gn,Zn,Jn,X,R3,R9,R10,R11,R32 本文定义的R33,B和Het以及含有它们的药物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。 还声称与其他药剂组合治疗。