| 摘要 |
1,148,229. Quinazoline derivatives. F. HOFFMANN-LA ROCHE & CO. A.G. 5 Dec., 1967 [12 Dec., 1966], No. 55296/67. Heading C2C. Compounds of the general formula (B = phenyl, substituted phenyl, pyridyl or substituted pyridyl, R<SP>1</SP>, R<SP>2</SP>= halogen, NO 2 , CF 3 , CN, C 1-7 alkyl, C 1-7 alkoxy or C 1-7 alkylthio, R<SP>3</SP> = C 1-7 alkyl, C 3-7 cycloalkyl or (C 3-7 cycloalkyl)- (C 1-7 alkyl), R<SP>4</SP>=C 1-7 alkyl, halo-(C 1-7 alkyl), dihalo-(C 1-7 alkyl), trihalo-(C 1-7 alkyl), amino- (C 1-7 alkyl), phenyl, phenyl-(C 1-7 alkyl) or aza- (C 3-7 cyoloalkyl)-(C 1-7 alkyl), R<SP>5</SP>=C 1-7 alkyl, halo - (C 1-7 alkyl), dihalo - (C 1-7 alkyl), trihalo- (C 1-7 alkyl), amino-(C 1-7 alkyl) or aza-(C 3-7 cycloalkyl)-(C 1-7 alkyl) or R<SP>4</SP>+R<SP>5</SP>=C 2-6 alkylene, aza-(C 2-6 alkylene) or N-(C 1-7 alkyl)-aza- (C 2-6 alkylene), and the broken lines denote optional substituents) and their acid addition salts are prepared by treating a compound of the formula with a compound (or a polymer thereof) of the formula (X=imino, hydroxylimino, oxo or acetalized oxo), introducing a C 1-7 alkyl, C 3-7 cycloalkyl or (C 3-7 cycloalkyl)-(C 1-7 alkyl) substituent at the 1-position of the product, if desired, and/or also if desired converting the product into a salt; the treatment being carried out in the presence of ammonia, hydroxylamine or a salt thereof when X=oxo or acetalized oxo. If the product contains an N-oxide group it may be deoxygenated. The products in which B= pyridyl or substituted pyridyl are analgesics and antiinflammatory agents, and may be administered in the form of pharmaceutical preparations containing them in association with a carrier.
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