| 摘要 |
<p>1490952 1,2 - Diphenyl - 4 - butyl - pyrazoline - 3 - ones INTERX RESEARCH CORP 6 Jan 1976 [6 Jan 1975] 00392/76 Heading C2C The invention comprises novel compounds I, II and III wherein R represents a C 1 -C 2 O-alkylsulphonyl group, an aryl sulphonyl group, a nicotinoyl group, an iso-nicotinoyl group, a picolinoyl group, an N-protected naturally occurring amino acid residue, wherein the protective group on the amino group of the amino acid residue is removable via hydrogenolysis or hydrolysis, or an amino acid residue containing a C 1 -C 2 N,N-dialkylamino or a C 4 -C 6 cycloalkylamino group; X and Y with respect to Formula II each represent a hydrogen atom or a -OR 1 group, with the proviso that either X or Y is a hydrogen atom and that R 2 is a member selected from the same or different groups represented by R 1 wherein R 1 represents a hydrogen atom, a C 1 -C 2 O-alkylsulphonyl group, an aryl sulphonyl group, a -CH 2 COOM group, wherein M represents an alkali or alkaline earth metal, a -CO-R 3 group, wherein R 3 represents a straight or branched C 1 -C 5 alkyl group, a C 1 -C 2 alkoxy group, a phenyl group, a substituted phenyl group whose substituents are selected from a 2-, 3-, or 4- hydroxy group, a 2-, 3-, or 4-acetyloxy group, and a 2-, 3-, or 4-acetylamino group, a 2-, 3-, or 4-pyridyl group, a 1-, 2-, or 5-imidazolyl group, a residue of an N-protected naturally occurring amino acid, wherein the protective group on the amino group of the amino acid is removable via hydrogenolysis or hydrolysis, or an amino acid residue containing a C 1 -C 2 N,N-dialkylamino or C 4 -C 5 cycloalkylamino group; X and Y with respect to Formula III represent a hydrogen atom or a -OR 1 group, wherein R 1 is as defined above with the proviso that either X or Y is a hydrogen atom, R 4 represents a hydrogen atom, a C 1 -C 5 alkyl group, an aryl group a 2-, 3-, or 4-methoxyphenyl group, or a -CH = CH 2 group, R 5 represents a -OOC-R 6 group, a group, or a -COOM group, wherein M represents an alkali or alkaline earth metal, wherein R 6 represents a member selected from R 4 as defined above, with the proviso that R 6 cannot be a hydrogen atom and wherein R 7 and R 8 each represent a C 1 -C 3 alkyl group. They are made by standard methods from phenylbutazone and oxyphenylbutazone. The following compounds are also prepared: novel 1,2 - diphenyl - 3,5 - ditrifluoroacetoxy - 4- butyl - 5 - hydroxy - 3 - pyrazoline, 1,2 - diphenyl- 4 - butyl - 4 - pivaloyloxymethyl - 3,5 - pyrazolidinedione and 1,2 - diphenyl - 4 - butyl - 4- (N,N - diethylcarbamoylmethyl) - 3,5 - pyrazolidinedione. Pharmaceutical preparations having antiinflammatory action contain (I), (II) and/or (III) as active ingredient. Administration is orally.</p> |
