87460-09-1Relevant articles and documents
PHOSPHINIC ACID DERIVATIVES WITH METALLOPEPTIDASE INHIBITORY ACTIVITY
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, (2008/06/13)
Compounds of formula (I), STR1 wherein R is a biphenyl group optionally substituted, by one or more substituents, the same or different selected among halogen atoms, hydroxy groups, alkoxy, alkyl thioalkyl or alkoxycarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety, C 1-C 3 alkyl groups containing one or more fluorine atoms, carboxy groups, nitro groups, amino or aminocarbonyl groups, acylamino groups, aminosulphonyl groups, momo-or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety, mono-or di-alkylamino-carbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; R 1 is a hydrogen atom, a straight or branched C 1-C 6 alkyl group or an arylalkyl group having from 1 to 6 carbon atoms in the alkyl moiety wherein the aryl is a phenyl, a biphenyl, a napthyl or a 5 or 6 membered aromatic heterocycle with one or two heteroatoms selected among nitrogen, oxygen and sulphur, optionally substituted with one or more substituents, the same or different, selected among halogen atoms, hydroxy groups, alkoxy, alkyl, thioalkyl or alkoxycarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety, C 1-C 3 alkyl groups containing one or more fluorine atoms, carboxy groups, nitro groups, amino or aminocarbonyl groups, acylamino groups, aminosulphonyl groups, mono-or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety, mono-or di-alkylaminocarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; R 2 is a straight or branched C. sub.1-C 6 alkyl group, optionally containing one or more fluorine atoms or one or more--NH--groups, an arylalkyl, an arylcarbonylaminoalkyl, an arylalkylcarbonylaminoalkyl or an arylaminocarbonylalkyl group having from 1 to 6 carbon atoms and optionally one or more--NH--groups in the alkyl moiety, the aryl being optionally substituted by one or more substituents, the same or different, selected among halogen atoms, hydroxy groups, alkoxy, alkyl, thioalkyl or alkoxycarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety, C 1-C. sub.3 alkyl groups containing one or more fluorine atoms, carboxy groups, nitro groups, amino or aminocarbonyl groups, acylamino groups, aminosulphonyl groups, mono-or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety, mono-or di-alkylaminocarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; m is 0 or 1; X is a hydrogen or fluorine atom; the carbon atom marked with an asterisk is an asymmetric carbon atom; and their pharmaceutically acceptable salts, are described. The compounds of formula (I) are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.
Method for making phosphinic acid intermediates
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, (2008/06/13)
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ESTERS OF PHOSPHINYLALKANOYL SUBSTITUTED PROLINES
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, (2008/06/13)
Hypotensive activity is exhibited by compounds having the formula STR1 and salts thereof wherein R 1 is alkyl, aryl, arylalkyl, cycloalkyl, or cycloalkylalkyl;R 2 is cycloalkyl, 3-cyclohexenyl or 2-alkyl-3-cyclohexenyl;R. sub.3 is alkyl, cycloalkyl, phenyl or alkoxy;R 4 is hydrogen or alkyl;one of R 5 and R 6 is hydrogen and the other is alkyl-X-, phenyl-X-, alkoxy, phenyloxy, phenyl, cycloalkyl, alkyl, or phenylalkyl; or together R 5 and R 6 are--XCH 2 CH. sub.2 X--;R. sub.7 is hydrogen or STR2 and n is 0 or 1.
