Ishihara Sangyo Kaisha, Ltd.

Shinji Odawara

Itaru Shigehara

Hirohiko Kimura

Takahiro Haga

Hideo Sugi

Kazuhiro Yamamoto

Syuichi Yotsuya

Hiroshi Okada

Masato Omatsu

Hitoshi Nakayama

Rie Higuchi

Taki Takenami

Pyridazinone derivatives or their salts, processes for their production,

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.

Diaminotrifluoromethylpyridine derivatives, process for their production

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.

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.

Diaminotrifluoromethylpyridine compounds and phospholipase A.sub.2

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.

Diaminotrifluoromethylpyridine derivatives and phospholipase A.sub.2

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Kusatsu, Japan

Shinji Odawara