发明名称 Acyl hydrazides as kinase inhibitors, in particular for SGK
摘要 Acylhydrazide compounds (I) or their derivatives, salts, solvates and/or stereoisomers, are new. Acylhydrazide compounds of formula (I) or their derivatives, salts, solvates and/or stereoisomers, are new. Either R 1>-R 9>H, A, OSO 2A, hal, NO 2, OR 10>, N(R 10>) 2, CN, [C(R 10>) 2] nCOOR 10>, O-[C(R 10>) 2] oCOOR 10>, SO 3H, [C(R 10>) 2]nAr, CO-Ar, O-[C(R 10>) 2] nAr, [C(R 10>) 2] nHet, [C(R 10>) 2] nC=CH, O-[C(R 10>) 2] nC=CH, [C(R 10>) 2] nCON(R 10>) 2, [C(R 10>) 2] nCONR 10>N(R 10>) 2, O-[C(R 10>) 2] nCON(R 10>) 2, O-[C(R 10>) 2] oCONR 10>N(R 10>) 2, NR 10>COA, NR 10>CON(R 10>) 2, NR 10>SO 2A, N(SO 2A) 2, COR 10>, S(O) mAr, SO 2NR 10> or S(O) mA; or R 1>+R 2>, R 2>+R 3>, R 3>+R 4>, R 4>+R 5>CH=CH-CH=CH; A : 1-6C-alkyl or cyclic 3-7C-alkyl, where 1-7H atoms are substituted by F; Ar : (bi)phenyl or naphthyl, optionally substituted by hal, A, OR 10>, N(R 10>) 2, NO 2, CN, phenyl, CON(R 10>) 2, NR 10>COA, NR 10>CON(R 10>) 2, NR 10>SO 2A, COR 10>, SO 2N(R 10>) 2, S(O) mA,[C(R 10>) 2] n-COOR 10> or O[C(R 10>) 2] o-COOR 10> ; Het : one or two optionally saturated or aromatic heterocyclic 1-4 N, O and/or S substituted by hal, A, OR 10>, N(R 10>) 2, NO 2, CN, COOR 10>, CON(R 10>) 2, NR 10>COA, NR 10>SO 2A, COR 10>, SO 2NR 10>, S(O) mA, (=S), (=NR 10>) or (=O) (carboxylicacid); R 10>H or A ; hal : F, Cl, Br or I; m : 0-2; and n, o : 0-3. Independent claims are included for: (1) a method for the preparation of (I); and (2) a set (Kit) consisting of several packages, comprising (I) and further a medical active agent. [Image] ACTIVITY : Antidiabetic; Vasotropic; Cardiant; Neuroprotective; Antiinflammatory; Cytostatic; Ophthalmological; Antibacterial; Tranquilizer; Nephrotropic; Angiogenesis-Inhibitor / Angiogenesis Stimulator; Antiarteriosclerotic; Hepatotropic; Respiratory-Gen.; Antirheumatic; Antiarthritic; Dermatological; CNS-Gen.; Vulnerary; Nootropic. MECHANISM OF ACTION : Signal transduction kinase inhibitor; Signal transduction kinase regulator; Signal transduction kinase modulator; Serum and glucocoritcoid regulated protein kinase (SGK) inhibitor. No biological data given.
申请公布号 ZA200709482(B) 申请公布日期 2008.11.26
申请号 ZA20070009482 申请日期 2007.11.02
申请人 MERCK PATENT GMBH 发明人 GERICKE, ROLF;MEDERSKI, WERNER;BEIER, NORBERT;DORSCH, DIETER;KLEIN, MARKUS;LANG, FLORIAN
分类号 A61K;A61P;C07C 主分类号 A61K
代理机构 代理人
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