Thrombin receptor antagonists
    33.
    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

    IPC分类号: C07D413/02 C07D405/02

    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。

    Thrombin receptor antagonists
    35.
    发明授权
    Thrombin receptor antagonists 有权
    凝血酶受体拮抗剂

    公开(公告)号:US06326380B1

    公开(公告)日:2001-12-04

    申请号:US09545720

    申请日:2000-04-07

    IPC分类号: A61K3147

    摘要: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt thereof, wherein: the single dotted line represents an optional double bond; the double dotted line represents an optional single bond; n is 0-2; Q is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; Het is an optionally substituted mono-, bi- or tricyclic heteroaromatic group; B is —(CH2)n3—, wherein n3 is 0-5, —CH2—O—, —CH2S—, —CH2—NR6—, —C(O)NR6—, —NR6C(O)—,  optionally substituted alkenyl or optionally substituted alkynyl; X is —O— or —NR6— when the double dotted line represents a single bond, or X is —OH or —NHR20 when the bond is absent; Y is ═O, ═S, (H, H), (H, OH) or (H, C1-C6 alkoxy) when the double dotted line represents a single bond, or when the bond is absent, Y is ═O, (H, H), (H, OH), (H, SH) or (H, C1-C6 alkoxy); R15 is absent when the double dotted line represents a single bond and is H, —NR18R19, or —OR17 when the bond is absent; or Y is  or  and R15 is H or C1-C6 alkyl; 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: 式2的杂环取代的三环或其药学上可接受的盐,其中:单点线表示任选的双键;双点划线表示任选的单键; n为0-2; Q为任选取代的环烷基,杂环烷基,芳基 或杂芳基; Het是任选取代的单,双或三环杂芳族基团; B是 - (CH 2)n3-,其中n3是0-5,-CH2-O-,-CH2S-,-CH2-NR6-, -C(O)NR 6 - ,-NR 6 C(O) - ,任选取代的烯基或任选取代的炔基;当双点划线表示单键时,X为-O-或-NR6-,或X为-OH或-NHR20 当双键虚线表示单键时,当不存在键时,Y为= O,= S,(H,H),(H,OH)或(H,C 1 -C 6烷氧基) ,Y为= O,(H,H),(H,OH),(H,SH)或(H,C1-C6烷氧基);当双点表示单键且为H时, NR18R19或-OR17,当该键不存在时; 或Y为或R 15为H或C 1 -C 6烷基;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,心力衰竭和癌症相关的疾病的方法 通过施用所述化合物。

    Method for the synthesis of huperzine A and analogs thereof and
compounds useful therein
    36.
    发明授权
    Method for the synthesis of huperzine A and analogs thereof and compounds useful therein 失效
    合成石杉碱甲及其类似物的方法及其中有用的化合物

    公开(公告)号:US5106979A

    公开(公告)日:1992-04-21

    申请号:US499122

    申请日:1990-03-23

    IPC分类号: C07D215/48 C07D221/22

    CPC分类号: C07D221/22 C07D215/48

    摘要: The present invention relates to a method for the synthesis of certain bridged fused ring pyridines. Such bridged fused ring pyridines can be converted to huperzine A and analogs of huperzine A. The present invention also covers such bridged fused ring pyridines, compounds utilized for the preparation of the bridged fused ring pyridines and analogs of huperzine A.

    摘要翻译: 本发明涉及合成某些桥连稠环吡啶的方法。 这种桥连稠环吡啶可以转化为石杉碱甲和石杉碱甲类似物。本发明还涵盖了这种桥连稠环吡啶,用于制备桥连稠环吡啶的化合物和石杉碱甲的类似物。