Preparation of azetidinones via novel protected intermediates
    51.
    发明授权
    Preparation of azetidinones via novel protected intermediates 失效
    通过新型受保护的中间体制备氮杂环丁酮

    公开(公告)号:US5008404A

    公开(公告)日:1991-04-16

    申请号:US496468

    申请日:1990-03-20

    CPC分类号: A47F5/02

    摘要: A multistep process is disclosed for preparing azetidinone intermediates used in the making penems and carbapenems wherein intermediates containing ##STR1## R' is independently hydrogen or 1, 2 or 3 of lower alkyl or lower alkoxy, preferably hydrogen, wherein R" is methyl, ethyl, a phenyl or alkyl, preferably ethyl, as a readily removable nitrogen protecting group are made.

    摘要翻译: 公开了一种用于制备用于制备青蒿素和碳青霉烯类似物的氮杂环丁酮中间体的多步法,其中含有R 1的中间体独立地为氢或低级烷基或低级烷氧基,优选氢,或其中R“为甲基的1,2或3, 乙基,苯基或烷基,优选乙基,作为容易除去的氮保护基。

    Fused ring thrombin receptor antagonists
    56.
    发明授权
    Fused ring thrombin receptor antagonists 有权
    融合环凝血酶受体拮抗剂

    公开(公告)号:US08372980B2

    公开(公告)日:2013-02-12

    申请号:US13188520

    申请日:2011-07-22

    CPC分类号: C07D405/06 C07D498/04

    摘要: Fused-ring, 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, and wherein An, En, Mn, Gn, Jn, R3, n7, R8, R9, R10, R11, R32, R33, X, Y, 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: 具有下式的稠环,杂环取代的三环或所述化合物的药学上可接受的盐或溶剂合物,异构体或外消旋混合物,其中表示任选的双键,并且其中An,En,Mn,Gn,Jn,R 3,n 7,R 8 本文定义了R9,R10,R11,R32,R33,X,Y,B和Het,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以及治疗与 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。

    Bicyclic And Tricyclic Derivatives As Thrombin Receptor Antagonists
    58.
    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

    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。

    Thrombin receptor antagonists
    59.
    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

    IPC分类号: A61K31/443 C07D405/02

    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

    Fused Ring Thrombin Receptor Antagonists
    60.
    发明申请
    Fused Ring Thrombin Receptor Antagonists 有权
    融合环凝血酶受体拮抗剂

    公开(公告)号:US20070244163A1

    公开(公告)日:2007-10-18

    申请号:US11734057

    申请日:2007-04-11

    IPC分类号: A61K31/4439 C07D491/02

    CPC分类号: C07D405/06 C07D498/04

    摘要: Fused-ring, 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, and wherein An, En, Mn, Gn, Jn, R3, n7, R8, R9, R10, R11, R32, R33, X, Y, 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: 熔融环,具有下式的杂环取代的三环或所述化合物的药学上可接受的盐或溶剂合物,异构体或外消旋混合物,其中表示可选的双键,并且其中A N,N, M,N,N,N,N,N,N,N,N, R 8,R 9,R 10,R 11,R 32,R 12, 本文中定义了R32,X,Y,B和Het,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 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。 还要求与其它心血管药物联合治疗。