Pyrazole derivative
    2.
    发明授权
    Pyrazole derivative 失效
    吡唑衍生物

    公开(公告)号:US07247635B2

    公开(公告)日:2007-07-24

    申请号:US11154591

    申请日:2005-06-17

    IPC分类号: C07D231/12 A61K31/415

    摘要: Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4═CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more substituents).

    摘要翻译: 药物,特别是具有钙释放依赖性钙通道抑制作用的药物组合物,特别是含有上述化合物作为活性成分的钙释放依赖性钙通道抑制剂的下述通式(I)表示的吡唑衍生物, (在该式中,每个符号具有以下含义:B:亚苯基,含氮,二价饱和环基或可被Alk,X:-NR 1取代的单环,二价杂芳族环基团 其中R 1,R 2,R 3,R 3,R 3,R 3, -NR 2 - , - SO 2 - , - SO 2 - , - SO 2 - , - SO 2 - , - SO 2 - 可以具有一个或多个取代基的一个 - 二环或三环稠合杂芳基,其可以具有一个或多个 取代基;可具有一个或多个取代基的环烷基;可具有一个或多个取代基的含氮饱和环基团 ents 可以具有一个或多个取代基的低级烯基; 可以具有一个或多个取代基的低级炔基; 或Alk,其可以具有一个或多个取代基)。

    Pyrazole derivative
    3.
    发明申请
    Pyrazole derivative 失效
    吡唑衍生物

    公开(公告)号:US20060264430A1

    公开(公告)日:2006-11-23

    申请号:US11399379

    申请日:2006-04-07

    摘要: Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: D: pyrazolyl which may have 1 to 3 substituents selected from the group consisting of -Alk, -lower alkenyl, -lower alkynyl, -halogeno-lower alkyl, -Alk-cycloalkyl, -Alk-O-Alk, -cycloalkyl, —O-Alk, —COOH, —COO-Alk and -Hal, n: 0 or 1, B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4═CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more substituents).

    摘要翻译: 药物,特别是具有钙释放激活的钙通道抑制作用的以下通式(I)表示的吡唑衍生物和药物组合物,特别是含有上述化合物作为活性成分的钙释放激活的钙通道抑制剂, (式中,每个符号具有以下含义:D:吡唑基,其可以具有1〜3个选自-Alk, - 低级烯基, - 低级炔基, - 卤代 - 低级烷基,-Al-环烷基, -Alk-O-Alk, - 环烷基,-O-Alk,-COOH,-COO-Alk和-Hal,n:0或1,B:亚苯基,含氮二价饱和环基或单环 可以被Alk取代的二价杂芳族环基团,X:-NR 1 -CR 2,R 3,..., 2,-NR 3 -NR 1 - , - NR 1 -SO 2 - , - SO 2 - , - SO 2 或者-CR 4 -CR 5 - ,以及可以具有的A:苯环 一个o 更多取代基; 可以具有一个或多个取代基的单 - ,二 - 或三环稠合杂芳基; 可以具有一个或多个取代基的环烷基; 可具有一个或多个取代基的含氮饱和环基; 可以具有一个或多个取代基的低级烯基; 可以具有一个或多个取代基的低级炔基; 或Alk,其可以具有一个或多个取代基)。

    Pyrazole derivative
    4.
    发明授权
    Pyrazole derivative 失效
    吡唑衍生物

    公开(公告)号:US07285554B2

    公开(公告)日:2007-10-23

    申请号:US11399379

    申请日:2006-04-07

    IPC分类号: C07D231/12 A61K31/415

    摘要: Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: D: pyrazolyl which may have 1 to 3 substituents selected from the group consisting of -Alk, -lower alkenyl, -lower alkynyl, -halogeno-lower alkyl, -Alk-cycloalkyl, -Alk-O-Alk, -cycloalkyl, —O-Alk, —COOH, —COO-Alk and -Hal, n: 0 or 1, B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4═CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more substituents).

    摘要翻译: 药物,特别是具有钙释放激活的钙通道抑制作用的以下通式(I)表示的吡唑衍生物和药物组合物,特别是含有上述化合物作为活性成分的钙释放激活的钙通道抑制剂, (式中,每个符号具有以下含义:D:吡唑基,其可以具有1〜3个选自-Alk, - 低级烯基, - 低级炔基, - 卤代 - 低级烷基,-Al-环烷基, -Alk-O-Alk, - 环烷基,-O-Alk,-COOH,-COO-Alk和-Hal,n:0或1,B:亚苯基,含氮二价饱和环基或单环 可以被Alk取代的二价杂芳族环基团,X:-NR 1 -CR 2,R 3,..., 2,-NR 3 -NR 1 - , - NR 1 -SO 2 - , - SO 2 - , - SO 2 或者-CR 4 -CR 5 - ,以及可以具有的A:苯环 一个o 更多取代基; 可以具有一个或多个取代基的单 - ,二 - 或三环稠合杂芳基; 可以具有一个或多个取代基的环烷基; 可具有一个或多个取代基的含氮饱和环基; 可以具有一个或多个取代基的低级烯基; 可以具有一个或多个取代基的低级炔基; 或Alk,其可以具有一个或多个取代基)。

    Hexahydro-1,4-diazepine derivatives or salts thereof
    7.
    发明授权
    Hexahydro-1,4-diazepine derivatives or salts thereof 失效
    六氢-1,4-二氮杂衍生物或其盐

    公开(公告)号:US06333320B1

    公开(公告)日:2001-12-25

    申请号:US09463017

    申请日:2000-01-19

    IPC分类号: A61K3155

    CPC分类号: C07D405/12 C07D243/08

    摘要: Hexahydro-1,4-diazepine derivatives represented by general formula (I); pharmaceutically acceptable salts thereof; and drugs containing the same as the active ingredient, such as activated blood coagulation factor X inhibitor, wherein A: phenylene, pyridylene, or the like; B: a 5- or 6-membered aryl or heteroaryl ring; X: —CO—, —CONH—, —CSNH—, —SO2—, —SO2NH—, or the like; Y: a bond or alkylene; R1: hydrogen, alkyl, —Y—(hetero) aryl, or the like; R2: hydrogen, alkoxy, —COOH, or the like; R3: amidino or a group capable of being converted into amidino; and R4, R5: each independently hydrogen or lower alkyl.

    摘要翻译: 由通式(I)表示的六氢-1,4-二氮杂衍生物; 其药学上可接受的盐; 以及与活性成分相同的药物,例如活化凝血因子X抑制剂,其中A:亚苯基,亚吡啶基等; B:5-或6-元芳基或杂芳基环; X:-CO - , - CONH - , - CSH - , - SO 2 - , - SO 2 NH-等; Y:一个键或亚烷基; R1:氢,烷基,-Y-(杂)芳基等; R2:氢,烷氧基,-COOH等; R3:脒基或能够转化为脒基的基团; 和R 4,R 5:各自独立地为氢或低级烷基。