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1. 发明授权

US5348967A Diaminotrifluoromethylpyridine derivatives, process for their production and phospholipase A.sub.2 inhibitor containing them 失效
标题翻译：二氨基三氟甲基吡啶衍生物，其制备方法和含有它们的磷脂酶A2抑制剂
公开(公告)号：US5348967A
公开(公告)日：1994-09-20
申请号：US35622
申请日：1993-03-23
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 , A61K31/44
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 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, as defined herein.
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（= 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。

2. 发明授权

US5260320A Diaminotrifluoromethylpyridine compounds and phospholipase A.sub.2 inhibitor containing them 失效
标题翻译：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。

3. 发明授权

US5229403A Diaminotrifluoromethylpyridine derivatives and phospholipase A.sub.2 inhibitor containing them 失效
标题翻译：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。

4. 发明授权

US5492908A Diaminotrifluoromethylpyridine derivatives, process for their production and phospholipase A.sub.2 inhibitor containing them 失效
标题翻译：二氨基三氟甲基吡啶衍生物，其制备方法和含有它们的磷脂酶A2抑制剂
公开(公告)号：US5492908A
公开(公告)日：1996-02-20
申请号：US285271
申请日：1994-08-03
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 , A61K31/44 , A61K31/495 , A61K31/54
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 method of treating rheumatoid arthritis using 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 as further defined herein.
摘要翻译：一种使用式（I）的二氨基三氟甲基吡啶衍生物或其盐进行类风湿性关节炎的方法：其中X为-CW1R1，-COCOR2，-CW1NHCOR2，-C（= W1）W2R3或-CW1N（R4 ）R5，Y是烷基，-CW3R6，-COCOR7，-NHCOR7，-C（= W3）W4R8， - （NH）mSO2R9， - （NH）mSO2OR10或 - （NH）mSO2N（R11）R12， 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，可被取代的单环杂环基或可以如本文进一步定义的可被取代的多环杂环基团。

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