New benzo-condensed heterocyclic compounds useful in treatment of thrombosis and prevention of vascular occlusion
Benzo-condensed five-membered heterocyclic compounds (I) are new. Benzo-condensed five-membered heterocyclic compounds (I) and their tautomers, stereoisomers and salts are new: A = O, S, CO, SO, SO2, imino (optionally substituted with alkyl) or methylene (optionally substituted); Ar = phenylene, nap...
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Format: | Patent |
Sprache: | eng ; ger |
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Zusammenfassung: | Benzo-condensed five-membered heterocyclic compounds (I) are new. Benzo-condensed five-membered heterocyclic compounds (I) and their tautomers, stereoisomers and salts are new: A = O, S, CO, SO, SO2, imino (optionally substituted with alkyl) or methylene (optionally substituted); Ar = phenylene, naphthylene, thienylene, thiazolylene, pyridylene, pyrimidinylene, pyrazinylene or pyridazinylene (each optionally substituted); X = N or -R1C=; R1 = halo, alkyl or alkoxy; Y1 = O, S or -R2N-; R2 = H, alkyl or phenyl-alkyl (both optionally substituted); Ra = H or alkyl; Rb = R3-CO-cycloalkylene, R3-SO2-NR4-, R3-CO-NR4-, R5NR6-CO-, R5NR6-SO2-, R5NR6-CO-cycloalkylene, amino or (1-3C alkyl or 5-7C cycloalkyl)amino, 4-(alkyl)2N-piperidino;4-(alkyl)-piperazino, 2-, 3- or 4-(alkyl)N-alkyl-SO2,4-oxo-3,4-dihydro-phthalazin-1-yl, 4-oxo-2,3-diaza-spiro(5.5)undec-1-en-1-yl, (cycloalkyleneiminocarbonyl) (substituted alkyl)-CH, CO or methyl substituted with optionally substituted cycloalkyl or with substituted alkyl, cycloalkyl-N-(substituted alkoxy)-iminomethylene (cycloalkyl is optionally substituted), disubstituted phosphinyl, 2-substituted-piperidino, tetrazolyl (optionally substituted), phenyl (optionally substituted) or phenyl-SO2, S-substituted and sulphimidoyl (optionally n-substituted), substituted imidazolyl, alkoxycarbonyl)(cycloalkyl-NH-CO)-alkyl, (substituted imidazolyl or benzimidazolyl)-alkyl or furanyl-1-pyrazolyl (optionally substituted); Rc = CN or amidino (optionally substituted); R3 = alkyl, phenyl, naphthyl, pyridyl, pyrazolyl, quinolyl or isoquinolyl (each optionally substituted) or cycloalkyl; R4 = H, alkyl (optionally substituted), cycloalkyl or substituted phenyl-alkyl; R5 = H, alkyl (optionally substituted), cycloalkyl, phenyl-alkyl (optionally substituted), phenyl (optionally substituted), naphthyl, pyridyl, pyrazolyl, quinolyl or isoquinolyl; R6 = H, alkyl (optionally substituted); NR5R6 = optionally substituted or benzo-fused pyrrolidino or piperidino; and provided that R5 and R6 can not be both H. The full definitions are given in the DEFINITION (Full Definitions) Field. An Independent claim is also included for the preparation (I). |
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