| 摘要 |
1353357 Benzoic acid derivatives PFIZER Inc 19 April 1971 [14 Sept 1970] 26540/71 Heading C2C Novel compounds (I) (including amides, esters and salts thereof) where A is H, C 1-6 alkyl, C 5-8 cycloalkyl, benzyl or Ph, B is the group (II) where n is 0 to 3 and R<SP>2</SP> and R<SP>3</SP> are H, Cl, Br, C 1-4 alkyl, C 1-4 alkoxy CO 2 H, CF 3 , Ph, benzyl or benzyloxy, W is Cl, Br, OH, alkoxy, NH 2 , mono- or di-alkylamino, benzylamino, phenethylamino, piperidino, mono- or di-alkylpiperidino, pyrrolidinyl, hexamethylene-imino or morpholino, and when A is H or alkyl B is also C 5-8 cycloalkyl, or NAB signifies morpholino, thiamorpholino and the S-oxide thereof, piperazinyl, hexa-, hepta- and octa - methyleneimino, 3 - azabicyclo[3,2,2]- nonanyl, tetrahydropyridyl or mono- and disubstituted derivatives thereof (the substituents are alkyl, alkoxy, alkoxyalkyl, OH, Cl, Br, CF 3 , Ph, tolyl, benzyl, benzyloxy, chloromethyl and/or hydroxymethyl) or NAB signifies unsubstituted-, mono- or di-substituted-piperidino (the substituents are alkyl, alkoxy, alkoxyalkyl, OH, Cl, Br, CF 3 , oxo, methylene, Ph, tolyl, benzyl, benzyloxy, benzyloxymethyl, chloromethyl or hydroxymethyl) are made by standard methods. The following compounds are also prepared:- 2-chloro-, -bromo-, and -fluoro-5-chlorosulphonyl benzoic acids, cis- and trans-3,5-dimethylpiperidine hydrochlorides, 1-acetyl-3-(benzyloxy- and -hydroxy)-piperidines, 3-benzyloxypiperidine, 2- fluoro - 5 - (3,5 - dimethylpiperidinosulphonyl)- benzoic acid, 2-fluoro-5(2-[p-chlorophenyl]ethylaminosulphonyl) - benzoic acid, 2 - fluoro - 5- (3 - methylpiperidinosulphonyl) - benzoic acid and 2 - chloro - 5 - (4 - carboxy- and 4 - chloroformyl - butyl - sulphamoyl) - benzoic acids. Pharmaceutical preparations effective in treating atherosclerosis and related cardiovascular diseases associated with elevated lipid levels contain (I) as active ingredient; administration is orally or parenterally. |
