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    Remedies or preventives for digestive diseases containing diaminotrifluoromethylpyridine derivatives
    2.
    发明授权
    Remedies or preventives for digestive diseases containing diaminotrifluoromethylpyridine derivatives 有权
    含二氨基三氟甲基吡啶衍生物的消化疾病的补救措施或预防措施

    公开(公告)号：US06653333B2

    公开(公告)日：2003-11-25

    申请号：US10182374

    申请日：2002-07-29

    申请人： Shuichi Yotsuya ,  Hirohiko Kimura ,  Tadao Bamba

    发明人： Shuichi Yotsuya ,  Hirohiko Kimura ,  Tadao Bamba

    IPC分类号： A61K3144

    CPC分类号： A61K31/44

    摘要： A digestive system disease therapeutic or preventive agent containing as an active ingredient a diaminotrifluoromethylpyridine derivative represented by the formula (I) or its salt: wherein X is a —CW1R1 group, a —COCOR2 group, a —CW1NHCOR2 group, a —C(═W1)W2R3 group or a —CW1N(R4)R5 group; Y is an alkyl group, a —CW3R6 group, a —COCOR7 group, a —NHCOR7 group, a —C(═W3)W4R8 group, a —(NH)mSO2R9 group, a —(NH)mSO2OR10 group or a —(NH)mSO2N(R11)R12 group; each of R1, R6 and R9 is a chain hydrocarbon group, a monocyclic hydrocarbon group, a polycyclic hydrocarbon group, a monocyclic heterocycle group or a polycyclic heterocycle group; each of R2 and R7 is an-alkyl group, an alkoxy group, a phenyl group or a phenoxy group; each of R3, R8 and R10 is an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a phenyl group or a benzyl group; each of R4, R5, R11 and R12 is an alkyl group; each of W1, W2, W3 and W4 is an oxygen atom or a sulfur atom; and m is 0 or 1.

    摘要翻译： 一种消炎系统疾病治疗或预防剂，其含有式（I）表示的二氨基三氟甲基吡啶衍生物或其盐：其中X为-CW 1 R 1基团，-COCOR 2基团， -CW 1 NHCOR 2基团，-C（= W 1）W 2 R 3基团或-CW 1 N（R 4）R 5基团 ; Y是烷基，-CW 3 R 6基团，-COCOR 7基团，-NHCOR 7基团，-C（= W 3）W 4， （NH）m SO 2 R 9基团， - （NH）m SO 2 OR 10基团或 - （NH）m SO 2 N（R 11）R 12基团; R 1，R 6和R 9各自为链烃基，单环烃基，多环烃基，单环杂环基或多环杂环基; R 2和R 7各自为烷基，烷氧基，苯基或苯氧基; R 3，R 8和R 10各自为烷基，烯基，炔基，环烷基，苯基或苄基; R 4，R 5，R 11和R 12各自为烷基; W 1，W 2，W 3和W 4中的每一个为氧原子或硫原子; m为0或1。

    Diaminotrifluoromethylpyridine compounds and phospholipase A.sub.2 inhibitor containing them
    9.
    发明授权
    Diaminotrifluoromethylpyridine compounds and phospholipase A.sub.2 inhibitor containing them 失效
    二氨基三氟甲基吡啶化合物和含有它们的磷脂酶A2抑制剂

    公开(公告)号：US5260320A

    公开(公告)日：1993-11-09

    申请号：US921083

    申请日：1992-07-29

    申请人： Takahiro Haga ,  Hideo Sugi ,  Itaru Shigehara ,  Shinji Odawara ,  Syuichi Yotsuya ,  Hirohiko Kimura ,  Kazuhiro Yamamoto

    发明人： Takahiro Haga ,  Hideo Sugi ,  Itaru Shigehara ,  Shinji Odawara ,  Syuichi Yotsuya ,  Hirohiko Kimura ,  Kazuhiro Yamamoto

    IPC分类号： C07D213/75 ,  C07D213/76 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D453/02 ,  C07D495/04 ,  A61K31/44

    CPC分类号： C07D213/75 ,  C07D213/76 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/10 ,  C07D417/12 ,  C07D453/02 ,  C07D495/04

    摘要： A diaminotrifluoromethylpyridine derivative of the formula (I) or its salt: ##STR1## wherein X is --CW.sup.1 R.sup.1, --COCOR.sup.2, --CW.sup.1 NHCOR.sup.2, --C(.dbd.W.sup.1)W.sup.2 R.sup.3 or --CW.sup.1 N(R.sup.4)R.sup.5, and Y is alkyl, --CW.sup.3 R.sup.6, --COCOR.sup.7, --NHCOR.sup.7, --C(.dbd.W.sup.3)W.sup.4 R.sup.8, --(NH).sub.m SO.sub.2 R.sup.9, --(NH).sub.m SO.sub.2 OR.sup.10 or --(NH).sub.m SO.sub.2 N(R.sup.11)R.sup.12, wherein each of R.sup.1, R.sup.6 and R.sup.9, which are independent from one another, is a chain hydrocarbon group which may be substituted, a monocyclic hydrocarbon group which may be substituted, a polycyclic hydrocarbon group which may be substituted, a monocyclic heterocycle group which may be substituted or a polycyclic heterocycle group which may be substituted, each of R.sup.2 and R.sup.7, which are independent from each other, is alkyl which may be substituted, alkoxy which may be substituted, phenyl which may be substituted or phenoxy which may be substituted, each of R.sup.3, R.sup.8 and R.sup.10, which are independent from one another, is alkyl which may be substituted, alkenyl which may be substituted, alkynyl which may be substituted, cycloalkyl which may be substituted, phenyl which may be substituted or benzyl which may be substituted, each of R.sup.4, R.sup.5, R.sup.11 and R.sup.12, which are independent from one another, is alkyl which may be substituted, each of W.sup.1, W.sup.2, W.sup.3 and W.sup.4, which are independent from one another, is an oxygen atom or a sulfur atom, and m is 0 or 1, provided that a combination wherein one of X and Y is --COCF.sub.2 X.sup.1 wherein X.sup.1 is a hydrogen atom, a halogen atom, alkyl or haloalkyl, and the other is --COCF.sub.2 X.sup.2 wherein X.sup.2 is a hydrogen atom, a halogen atom, alkyl, haloalkyl or alkylcarbonyl, or --COOX.sup.3 wherein X.sup.3 is alkyl which may be substituted or phenyl which may be substituted, is excluded.

    摘要翻译： 式（I）的二氨基三氟甲基吡啶衍生物或其盐：其中X为-CW1R1，-COCOR2，-CW1NHCOR2，-C（= W1）W2R3或-CW1N（R4）R5，Y为烷基 ，-CW 3 R 6，-COCOR 7，-NHCOR 7，-C（= W3）W 4 R 8， - （NH）m SO 2 R 9， - （NH）m SO 2 OR 10或 - （NH）m SO 2 N（R 11）R 12，其中R 1，R 6和R 9各自 彼此独立，可以被取代的链状烃基，可以被取代的单环烃基，可以被取代的多环烃基，可以被取代的单环杂环基或可以被取代的多环杂环基 取代的，R 2和R 7各自独立地为可以被取代的烷基，可以被取代的烷氧基，可以被取代的苯基或可被取代的苯氧基，R 3，R 8和R 10各自为 彼此独立地是可以被取代的烷基，可以被取代的链烯基，可被取代的炔基，其中的环烷基 可被取代的苯基或可被取代的苄基，R 4，R 5，R 11和R 12各自彼此独立地是可以被取代的烷基，各自为W1，W2，W3和W4， 其彼此独立的是氧原子或硫原子，并且m为0或1，条件是其中X和Y之一是-COCF 2 X 1的组合，其中X 1是氢原子，卤素原子，烷基或卤代烷基 另一个是-COCF 2 X 2，其中X 2是氢原子，卤原子，烷基，卤代烷基或烷基羰基，或-COOX 3，其中X 3是可被取代的烷基或可被取代的苯基。

    Diaminotrifluoromethylpyridine derivatives and phospholipase A.sub.2 inhibitor containing them
    10.
    发明授权
    Diaminotrifluoromethylpyridine derivatives and phospholipase A.sub.2 inhibitor containing them 失效
    含有它们的二氨基三氟甲基吡啶衍生物和磷脂酶A2抑制剂

    公开(公告)号：US5229403A

    公开(公告)日：1993-07-20

    申请号：US723377

    申请日：1991-06-28

    申请人： Takahiro Haga ,  Hideo Sugi ,  Itaru Shigehara ,  Shinji Odawara ,  Syuichi Yotsuya ,  Hirohiko Kimura ,  Kazuhiro Yamamoto

    发明人： Takahiro Haga ,  Hideo Sugi ,  Itaru Shigehara ,  Shinji Odawara ,  Syuichi Yotsuya ,  Hirohiko Kimura ,  Kazuhiro Yamamoto

    IPC分类号： A61K31/4427 ,  A61P5/48 ,  A61P29/00 ,  C07D213/75 ,  C07D213/76 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D453/02 ,  C07D495/04

    CPC分类号： C07D213/75 ,  C07D213/76 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12 ,  C07D417/12 ,  C07D453/02 ,  C07D495/04

    摘要： A diaminotrifluoromethylpyridine derivative of the formula (I) or its salt: ##STR1## wherein X is --CW.sup.1 R.sup.1, --COCOR.sup.2, --CW.sup.1 NHCOR.sup.2, --C(.dbd.W.sup.1 (W.sup.2 W.sup.3 or --CW.sup.1 N(R.sup.4)R.sup.5, and Y is alkyl, --CW.sup.3 R.sup.6, --COCOR.sup.7, --NHCOR.sup.7, --C(.dbd.W.sup.3)W.sup.4 R.sup.8, --(NH).sub.m SO.sub.2 R.sup.9, --(NH).sub.m SO.sub.2 OR.sup.10 or --(NH).sub.m SO.sub.2 N R.sup.11)R.sup.12, wherein each of R.sup.1, R.sup.6 and R.sup.9, which are independent from one another, is a chain hydrocarbon group which may be substituted, a monocyclic hydrocarbon group which may be substituted, a polycyclic hydrocarbon group which may be substituted, a monocyclic heterocycle group which may be substituted or a polycyclic heterocycle group which may be substituted, each of R.sup.2 and R.sup.7, which are independent from each other, is alkyl which may be substituted, alkoxy which may be substituted, phenyl which may be substituted or phenoxy which may be substituted, each of R.sup.3, R.sup.8 and R.sup.10, which are independent from one another, is alkyl which may be substituted, alkenyl which may be substituted, alkynyl which may be substituted, cycloalkyl which may be substituted, phenyl which may be substituted or benzyl which may be substituted, each of R.sup.4, R.sup.5, R.sup.11 and R.sup.12, which are independent from one another, is alkyl which may be substituted, each of W.sup.1, W.sup.2, W.sup.3 and W.sup.4, which are independent from one another, is an oxygen atom or a sulfur atom, and m is 0 or 1, provided that a combination wherein one of X and Y is --COCF.sub.2 X.sup.1 wherein X.sup.1 is a hydrogen atom, a halogen atom, alkyl or haloalkyl, and the other is --COCF.sub.2 X.sup.2 wherein X.sub.2 is a hydrogen atom, a halogen atom, alkyl, haloalkyl or alkylcarbonyl, or --COOX.sup.3 wherein X.sup.3 is alkyl which may be substituted or phenyl which may be substituted, is excluded.

    摘要翻译： 式（I）的二氨基三氟甲基吡啶衍生物或其盐：其中X为-CW1R1，-COCOR2，-CW1NHCOR2，-C（= W1（W2W3或-CW1N（R4）R5，Y为烷基 ，-CW 3 R 6，-COCOR 7，-NHCOR 7，-C（= W 3）W 4 R 8， - （NH）m SO 2 R 9， - （NH）m SO 2 OR 10或 - （NH）m SO 2 N R 11）R 12，其中R 1，R 6和R 9 彼此独立地是可以被取代的链状烃基，可以被取代的单环烃基，可以被取代的多环烃基，可以被取代的单环杂环基或可以被取代的多环杂环基 相互独立的R 2和R 7各自为可被取代的烷基，可被取代的烷氧基，可被取代的烷氧基，可被取代的苯基或可被取代的苯氧基，R 3，R 8和R 10各自独立地 可以是可以被取代的烷基，可以被取代的链烯基，可被取代的炔基，其中的环烷基 可被取代的苯基或可被取代的苄基，R 4，R 5，R 11和R 12各自彼此独立地是可以被取代的烷基，各自为W1，W2，W3和W4， 其彼此独立的是氧原子或硫原子，并且m为0或1，条件是其中X和Y之一是-COCF 2 X 1的组合，其中X 1是氢原子，卤素原子，烷基或卤代烷基 另一个是-COCF 2 X 2，其中X 2是氢原子，卤原子，烷基，卤代烷基或烷基羰基，或-COOX 3，其中X 3是可被取代的烷基或可被取代的苯基。