摘要:
Aminoalkoxyphenyl derivatives useful in the treatment of certain pathological syndromes of the cardiovascular system of formula: ##STR1## in which: B represents a --S--, --SO-- or --SO.sub.2 -- group,R.sub.1 and R.sub.2, which are identical or different, each denote hydrogen, a methyl or ethyl radical or a halogen,A denotes a straight- or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical, in which the hydroxy is optionally substituted by a lower alkyl radical,R.sub.3 denotes an alkyl radical or a radical of formula:--Alk--R.sub.5in which Alk denotes a single bond or a linear- or branched-alkylene radical having from 1 to 5 carbon atoms and R.sub.5 denotes a pyridyl, phenyl, 2,3-methylenedioxyphenyl or 3,4-methylenedioxyphenyl radical or a phenyl group substituted with one or more substituents, which may be identical or different, selected from halogen atoms, lower alkyl groups or lower alkoxy groups,R.sub.4 denotes hydrogen or an alkyl radical orR.sub.3 and R.sub.4 when taken together, denote an alkylene or alkenylene radical having from 3 to 6 carbon atoms and optionally substituted with a phenyl radical or optionally interrupted by --O--, ##STR2## R.sub.6 denoting hydrogen or a lower alkyl or pheny radical, Cy represents a cyclic group with the proviso that when Cy represents a benzo[b]furyl or benzo[b]thienyl group and B represents a --SO.sub.2 -- group, R.sub.3 represents a radical --Alk--R.sub.5, as well as the N-oxide derivative thereof and a pharmaceutically acceptable salt thereof.
摘要:
Novel benzo[b]thiophene derivatives corresponding to the general formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein R represents a branched- or straight-chain alkyl group containing from 1 to 4 carbon atoms, or a cyclohexyl group, n is an integer in the range of from 3 to 6 inclusive, and Am represents a dimethylamino, diethylamino, di-n-propylamino or di-n-butylamino group.These derivatives are useful for the treatment of pathological conditions of the heart and in particular angina pectoris.
摘要:
The present invention is directed to the use of aminoalkoxyphenyl derivatives for reducing and/or controlling excessive intraocular pressure and compositions suitable for this case.
摘要:
Aminoalkoxyphenyl derivatives useful in the treatment of certain pathological syndromes of the cardiovascular system of formula: ##STR1## in which: B represents a --S--, --SO-- or --SO.sub.2 -- group,R.sub.1 and R.sub.2, which are identical or different, each denote hydrogen, a methyl or ethyl radical or a halogen,A denotes a straight- or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical, in which the hydroxy is optionally substituted by a lower alkyl radical,R.sub.3 denotes an alkyl radical or a radical of formula:--Alk--R.sub.5 in which Alk denotes a single bond or a linear- or branched-alkylene radical having from 1 to 5 carbon atoms and R.sub.5 denotes a phenyl, 2,3-methylenedioxyphenyl or 3,4-methylenedioxyphenyl radical or a phenyl group substituted with one or more substituents, which may be identical or different, selected from halogen atoms, lower alkyl groups or lower alkoxy groups,R.sub.4 denotes hydrogen or an alkyl radicalCy represents a benzo[b]furyl, as well as the N-oxide derivative thereof and a pharmaceutically acceptable salt thereof.
摘要:
The present invention relates to aminoalkoxyphenyl compounds of formula: ##STR1## in which: B is selected from --S--, --SO-- and --SO.sub.2 --,R.sub.1 and R.sub.2, which are identical or different, are selected from hydrogen, methyl, ethyl and halogen,A is selected from a straight- or branched-alkylene radical having from 2 to 5 carbon atoms, a 2-hydroxypropylene radical, and a 2-(lower alkoxy) propylene radical,R.sub.3 is selected from C.sub.1 -C.sub.8 alkyl and a radical of formula:--Alk--Ar in which Alk is selected from a single bond and a linear- or branched-alkylene radical having from 1 to 5 carbon atoms; and Ar is selected from pyridyl, phenyl, 2-3-methyleneoxyphenyl, 3,4-methylenedioxyphenyl and phenyl substituted with one or more substituents, which may be identical or different, selected from halogen atoms, C.sub.1 -C.sub.8 alkyl groups and C.sub.1 -C.sub.8 alkoxy groups,R.sub.4 is selected from hydrogen and C.sub.1 -C.sub.8 alkyl, orR.sub.3 and R.sub.4, when taken together, denote a 1,4-tetra-methylene, 1,5-pentamethylene, 3-oxa-1,5-pentamethylene, 3-aza-1,5-pentamethylene, 3-methylaza-1,5-pentamethylene, 3-phenylaza-1,5-pentamethylene or --CH.dbd.CH--N.dbd.CH-- radical,R is selected from hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.6, cycloalkyl, benzyl, phenyl optionally substituted with one or more substituents, which may be identical or different, selected from halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy as well as a pharmaceutically acceptable salt thereof.
摘要:
The object of the invention is a process for the preparation of derivatives of 3-sulfonyl indolizine of general formula: ##STR1## in which: R is selected from hydrogen, alkyl, cycloalkyl, substituted or unsubstituted phenyl,R.sub.1 is a protecting group for hydroxyl,R.sub.2 and R.sub.3, identical or different, is each selected from hydrogen, methyl or ethyl or halogen.These compounds are intermediates which can be used for the preparation of 3-aminoalkoxyphenylsulfonyl-indolizines, which are useful in the treatment of certain diseases of the cardiovascular system.
摘要:
The subject of the invention is 4-hydroxyphenylthio derivatives of general formula: ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, each represent hydrogen, a methyl or ethyl radical or a halogen atom,R represents a (C.sub.1 -C.sub.6) alkyl, (C.sub.3 -C.sub.6) cycloalkyl or phenyl radical,R.sub.3 represents hydrogen or a halogen atom, X represents --O--, --S-- or --NR.sub.4 -- in which R.sub.4 represents hydrogen or a (C.sub.1 -C.sub.4) alkyl group, useful as synthetic intermediates, especially for the preparation of aminoalkoxyphenylsulphonyl derivatives which are pharmaceutically active compounds.
摘要:
An aminoalkoxyphenyl derivative of general formula:Cy--B--Ph--O--A--Am (1)as well as a pharmaceutically acceptable salt thereof in whichB represents a --S--, --SO-- or --SO.sub.2 -- group,Ph represents an optionally substituted phenyl radical,A denotes a straight or branched alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxy propylene radical in which the hydroxy is optionally substituted by a C.sub.1 -C.sub.4 alkyl radical.Am represents a group: ##STR1## and Cy is a cyclic group, provided that when Cy represents either a benzo[b]furyl group substituted at position 4 by a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or a benzo[b]thienyl group substituted at position 4 by a halogen atom or by a C.sub.1 -C.sub.4 alkyl group and when B represents a --SO.sub.2 -- group, R.sub.3 represents a --Alk--Ar radical.
摘要:
The invention relates to indolizine derivatives of general formula: ##STR1## in which: X denotes an --S or --SO.sub.2 -- group, each of R.sub.1 and R.sub.2, which are identical or different, denotes hydrogen, the methyl or ethyl radical or a halogen atom,R.sub.3 denotes hydrogen or a C.sub.1 -C.sub.4 alkyl radical,R.sub.4 denotes a precursor radical of a carboxyl group,R denotes a C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or phenyl radical, and their use as intermediates for the preparation of pharmaceutically active aminoalkoxybenzenesulphonylindolizine derivatives.