Abstract: The present invention relates to a method for making a compound of the structure: ##STR1## comprising the steps: (a) adding 6-deoxy-.alpha.-L-mannopyranosyl bromide, 2,3,4-tri-O-benzoate; DMSO; a base, selected from the group including tertiary amines, amidines, bicarbonates, carbonates, heteroaryl amine, and a solvent, hydrocarbons, esters, and ethers, in a slurry heated to 50.degree.-150.degree. C.;(b) stirring the reaction mixture at 50.degree.-150.degree. C. for 5 minutes to 30 minutes,(c) pouring the reaction mixture over ice water; and(d) extracting the product with a solvent selected from the group consisting of chlorinated solvents, aromatic hydrocarbons, esters, ethers, and evaporating said layer to give a solid.

Abstract: Disclosed are 14-aminosteroid compounds, including pharmaceutically acceptable acid salts and esters thereof, useful in treating individuals afflicted with congestive heart failure, which compounds have the general formula: ##STR1## wherein R.sub.3 is a deoxy or oxygen-substituted monosaccharide sugar residue and R.sub.1, R.sub.2 and R.sub.4 are various other substituents as defined herein.

Abstract: An optically active isomer or a racemate of a compound of general formula (I) ##STR1## in which either R.sub.1 represents a methoxy or cyclopropylmethoxy group andR.sub.2 represents a hydrogen, chlorine or bromine atom, orR.sub.1 and R.sub.2 together form, and in this order, a group of formula --O--CH.sub.2 --O--, --O--(CH.sub.2).sub.2 --, --O--(CH.sub.2).sub.2 --O-- or --O--(CH.sub.2).sub.3 --O--,R.sub.3 represents a hydrogen atom or an amino group, andR.sub.4 represents a hydrogen, chlorine or bromine atom,in the form of a free base or of a pharmaceutically acceptable acid addition salt.

Abstract: 3,3a,4,5-Tetrahydro-1H-oxazolo[3,4-a]quinolin-1-one derivatives of formula (I) ##STR1## in which: n is 0 or 1,R.sub.1 represents a hydrogen atom or an ethenyl, methyl, ethyl, phenyl, hydroxymethyl or methoxymethyl group, and(i) R.sub.2 is a methyl, trifluoromethyl or cyano group, R.sub.3 is a hydrogen atom or a hydroxyl or benzyloxy group and R.sub.4 and R.sub.5 are hydrogen atoms,or (ii) R.sub.2 and R.sub.4 together form a --(CH.sub.2).sub.4 -- group, R.sub.3 is a hydroxyl group and R.sub.5 is a hydrogen atom,or (iii) R.sub.2 and R.sub.5 together form an --O--(CH.sub.2).sub.3 -- group, and R.sub.3 and R.sub.4 are hydrogen atoms,or (iv) R.sub.2 and R.sub.5 together form a --(CH.sub.2).sub.4 group, R.sub.3 is a hydroxyl group and R.sub.4 is a hydrogen atom,are useful as selective inhibitors of MAO-A or as mixed inhibitors of MAO-A and MAO-B.

Abstract: 1,3,4-Oxadiazol-2(3H)-one derivatives, of formula ##STR1## in which R.sub.1 represents either a hydrogen atom or a linear or branched (C.sub.1-4)alkyl group which is substituted with a hydroxyl group, a phenoxy group, a (C.sub.1-4)alkoxy group, a (C.sub.1-4)alkylthio group, a mercapto group, a (C.sub.1-4)alkoxy-(C.sub.1-4)alkoxy group, a di(C.sub.1-4)alkylamino group or an N-(C.sub.1-4)alkyl-N-propynylamino group, or represents a (C.sub.3-4)alkynyl group, andR.sub.2 either represents a linear or branched (C.sub.1-8)alkyl group which is substituted with one or more halogen atoms and/or a hydroxyl group, a 1-imidazolyl group or a 3-tetrahydropyranyl group, or represents a trifluoro(C.sub.3-5)alkenyl group,in the form of pure enantiomers or mixtures of enantiomers, including racemic mixtures, as well as the addition salts thereof with pharmaceutically acceptable acids, are useful as inhibitors of monoamine oxidase B.

Abstract: Derivatives having the formula: ##STR1## in which R.sub.1 =C.sub.1 -C.sub.4 alkyl and Ar is an aryl or heteroaryl group chosen from among the following: ##STR2## where R.sub.2 represents a hydrogen atom one or two halogen atoms, a CN, NO.sub.2 or CF.sub.3 group, one, two or three C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy groups or an amino group substituted by two C.sub.1 -C.sub.4 alkyl groups, in which case the --W--V-- chain represents --N.dbd.N-- or ##STR3## and n=2-6; (ii) pyridyl, in which case the --W--V-- chain represents --N.dbd.N-- and n= 1-6, and acid addition salts of those derivatives (I) which are salt-forming.These derivatives are of use in therapy as agents for inhibiting type B monoamine oxydase.

Abstract: Derivatives having the formula: ##STR1## where R.sub.1 denotes C.sub.1 -C.sub.4 alkyl; X denotes oxygen or methylene; R.sub.2 denotes C.sub.1 -C.sub.4 alkyl or CF.sub.3 ; R.sub.3 denotes a CH.sub.2 R.sub.4 group in which R.sub.4 is (i) a pentagonal or hexagonal aromatic heterocyclic group comprising one or two nitrogen atoms and optionally fused with a benzene ring or (ii) a group having the formula ##STR2## where n=0 or 1, and R.sub.5 and R.sub.6 independently denote C.sub.1 -C.sub.4 alkyl or benzyl, and R.sub.5 and R.sub.6 also, together with the nitrogen atom to which they are bonded, form a piperidino or pyrrolidino or morpholino or N-methyl piperazino radical, and their N-oxide forms and acid addition salts of these derivatives and their N-oxide forms, the derivatives being in various stereoisomeric forms or in the form of a mixture of these forms, including the racemic form.

Abstract: Derivatives having the formula: ##STR1## in which R.sub.1 =C.sub.1 -C.sub.4 alkyl and Ar is an aryl or heteroaryl group chosen from among the following:(i) ##STR2## where R.sub.2 represents a hydrogen atom one or two halogen atoms, a CN, NO.sub.2 or CF.sub.3 group, one, two or three C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy groups or an amino group substituted by two C.sub.1 -C.sub.4 alkyl groups, in which case the --W--V-- chain represent ##STR3## and n=2-6; (ii) pyridyl, in which case the --W--V-- chain represents --N.dbd.N--and n=1-6, and acid addition salts of those derivatives (I) which are salt-forming.These derivatives are of use in therapy as agents for inhibiting type B monoamine oxydase.

Abstract: The derivatives of the formula: ##STR1## wherein: R.sub.1 is H or C.sub.1 -C.sub.4 alkyl;X is an oxygen atom, a methylene group or a --CH.dbd.CH-- group;n is 1 or 2 when X is an oxygen atom or a methylene group and is 0 or 1 when X is a --CH.dbd.CH-- group;R.sub.3 is a C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl, benzyl, CHF.sub.2, CF.sub.3 or CF.sub.3 CF.sub.2 group;each of R.sub.2 and R'.sub.2 independently is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl, C.sub.4 -C.sub.7 cycloalkyl, phenyl or benzyl group;R'.sub.2 and R.sub.3 may further form together a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- chain; andeach of R.sub.4 and R'.sub.4 independently is a C.sub.1 -C.sub.4 alkyl group or R.sub.4 and R'.sub.4 form together either a --(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.3 -- chain, a --(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.3 -- chain substituted by one or two C.sub.1 -C.sub.4 alkyl groups, or a --(CH.sub.2).sub.2 -- chain substituted by one or two --CH.sub.2 --NH.sub.

Abstract: The derivatives of the formula: ##STR1## wherein: R.sub.1 is H or C.sub.1 -C.sub.4 alkyl;X is either an oxygen atom, in which case R.sub.2 =H or halogen, or a methylene group or a --CH.dbd.CH-- group, in which case R.sub.2 =H;n is 1 or 2 when X is an oxygen atom or a methylene group and 0 or 1 when X is a --CH.dbd.CH-- group; each of R.sub.3 and R.sub.4 is independently H, C.sub.1 -C.sub.4 alkyl, C.sub.4 -C.sub.7 cycloalkyl, phenyl or benzyl;R.sub.5 is H or C.sub.1 -C.sub.4 alkyl;R.sub.6 is C.sub.1 -C.sub.4 alkyl, CHF.sub.2, CF.sub.3, CF.sub.3 CF.sub.2, C.sub.4 -C.sub.7 cycloalkyl, phenyl or benzyl;R.sub.4 and R.sub.6 may further form together a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --chain;R.sub.5 and R.sub.6 may further form together a --(CH.sub.2).sub.4 --or --(CH.sub.2).sub.5 --chain; andR.sub.7 is H, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.5 acyl or benzyl,useful as drugs, prepared by cyclizing N ethoxy carbonyl anilines with substituted 1, 3 dioxolane-2-ones.

Abstract: The derivatives of the formula: ##STR1## wherein: R.sub.1 is H or C.sub.1 -C.sub.4 alkyl;X is an oxygen atom, a methylene group or a --CH.dbd.CH-- group;n is 1 or 2 when X is an oxygen atom or a methylene group and 0 or 1 when X is a --CH.dbd.CH-- group;D is an oxygen atom or a NOR group, wherein R.dbd.H or C.sub.1 -C.sub.4 alkyl;R.sub.3 is a C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl or benzyl group;each of R.sub.2 and R'.sub.2 independently is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl or benzyl group; andR'.sub.2 and R.sub.3 may further form together a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- chain,useful as drugs.

Abstract: The derivatives of the formula: ##STR1## wherein: R.sub.1 is H or C.sub.1 -C.sub.4 alkyl;X is an oxygen atom, a methylene group or a --CH.dbd.CH-- group;n is 1 or 2 when X is an oxygen atom or a methylene group and is 0 or 1 when X is a --CH.dbd.CH-- group;R.sub.3 is a C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl, benzyl, CHF.sub.2, CF.sub.3 or CF.sub.3 CF.sub.2 group;each of R.sub.2 and R'.sub.2 independently is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl, C.sub.4 -C.sub.7 cycloalkyl, phenyl or benzyl group;R'.sub.2 and R.sub.3 may further form together a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- chain; andeach of R.sub.4 and R'.sub.4 independently is a C.sub.1 -C.sub.4 alkyl group or R.sub.4 and R'.sub.4 form together either a --(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.3 -- chain, a --(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.3 -- chain substituted by one or two C.sub.1 -C.sub.4 alkyl groups, or a --(CH.sub.2).sub.2 -- chain substituted by one or two --CH.sub.2 --NH.sub.

Abstract: The derivatives of the formula: ##STR1## wherein: R.sub.1 is H or C.sub.1 -C.sub.4 alkyl;X is either an oxygen atom, in which case R.sub.2 =H or halogen, or a methylene group or a --CH.dbd.CH-- group, in which case R.sub.2 =H;n is 1 or 2 when X is an oxygen atom or a methylene group and 0 or 1 when X is a --CH.dbd.CH-- group;each of R.sub.3 and R.sub.4 is independently H, C.sub.1 -C.sub.4 alkyl, C.sub.4 -C.sub.7 cycloalkyl, phenyl or benzyl;R.sub.5 is H or C.sub.1 -C.sub.4 alkyl;R.sub.6 is C.sub.1 -C.sub.4 alkyl, CHF.sub.2, CF.sub.3, CF.sub.3 CH.sub.2, C.sub.4 -C.sub.7 cycloalkyl, phenyl or benzyl;R.sub.4 and R.sub.6 may further form together a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- chain;R.sub.5 and R.sub.6 may further form together a --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 -- chain; andR.sub.7 is H, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.5 acyl or benzyl,useful as drugs.

Abstract: The invention relates to androstane-17-carboxylic acid esters, represented by general formula (I): ##STR1## wherein R.sub.1 represents a lower alkyl group containing 1 to 4 carbon atoms, a lower alkyl group containing 2 to 4 carbon atoms substituted by an amino group, or an aralkyl group from 6 to 12 carbon atoms, R.sub.2 and R.sub.3, which may be the same or different, represent a hydrogen atom or a lower alkyl group containing 1 to 4 carbon atoms, R.sub.4 represents a hydrogen atom, a hydroxy group or an acetoxy group, R.sub.5 represents a hydroxy or acetoxy group, or R.sub.4 and R.sub.5 represent together a divalent alkylenedioxy group, R.sub.6 represents a hydroxy group, a methoxy group, or an acetoxy group, R.sub.7 represents a methyl group or a hydroxymethyl group, R.sub.8 represents an hydrogen atom or a hydroxy group and ##STR2## represents either a ##STR3## group or a ##STR4## carbon atom having the double linkage in the 4- or 5-position of the steroid nucleus.

Abstract: Quinidine derivatives of general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, or an acyl group, and R.sub.2 represents a hydrogen atom, a hydroxy group, an alkoxy group, an acyloxy group or an aroyloxy group, as well as the acid addition salts thereof, useful in therapy, particularly, for the treatment of cardiac arrhythmia.

Abstract: The present invention relates to new 14-aminosteroids and their application in therapy and also to a process for their preparation.

Abstract: The invention relates to 4-acylamino-1-azaadamantanes represented by general formula (I): ##STR1## wherein R represents an alkyl group, a substituted alkyl group, an aryl group or a substituted aryl group, useful in particular, for the treatment of cardiovascular diseases.

Abstract: The invention relates to 14-amino steroid derivatives of formula (I): ##STR1## wherein R represents a hydrogen atom or a lower alkyl group with 1 to 4 carbon atoms, R.sub.1 represents a substituted or unsubstituted sugar residue, and R.sub.2 represents a hydrogen atom, a hydroxyl group or an --OR.sub.3 group, wherein R.sub.3 is a substituted or unsubstituted sugar residue; and acid salts thereof useful in the treatment of cardiac incapacity.

Abstract: The invention relates to new 3-pyridyl-5-alkoxy-pyrazole derivatives of the following formula: ##STR1## wherein R.sub.1 represents a 4-pyridyl, 3-pyridyl or 2-pyridyl group which is unsubstituted or which may be substituted with one or two lower alkyl groups; R.sub.2 represents a hydrogen atom or a lower alkyl group; and R.sub.3 represents a lower alkyl group, a phenyl group or an aralkyl group; and the acid addition salts thereof. The derivatives may be prepared by alkylation of a 3-pyridyl-5-pyrazolone. The derivatives are medicinally useful, particularly for the treatment of cardiac deficiency.

Abstract: The invention relates to 3-aryl-5-alkoxy-pyrazoles, represented by general formula (I): ##STR1## wherein Ar represents an aryl group which may be substituted; R represents a hydrogen atom or an alkyl, phenyl or benzyl group; R.sub.1 and R.sub.2 which may be the same or different, each represent a hydrogen atom or an alkyl group, or together form a 5 or 7 membered heterocyclic ring with the nitrogen atom to which they are attached; and n is an integer of from 1 to 4; and the pharmaceutically acceptable acid salts thereof, useful in particular, in the treatment of cardiac arrhythmias.