Etablissements Nativelle, S.a.

Norwich Eaton Pharmaceuticals, Inc.

Francois-Xavier Jarreau

Jean-Jacques Koenig

Jean J Koenig

Roger Gerard Sarfati

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. Such esters are prepared by coupling reaction of the corresponding 14-azido-derivatives with a sugar, followed by a reduction. Application in therapy, especially in the treatment of heart failure.

Novel 14-amino steroids

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.

Antiarrhythmic quinidine derivatives

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

14-aminosteroid derivatives, application in therapy and process of

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.

14-Amino steroid derivatives, a process for the preparation thereof and

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.

3-Pyridyl-5-alkoxy-pyrazole derivatives and pharmaceutical composition

An aminoalkoxypyrazole of the general formula (I) ##STR1## wherein Ar is a phenyl, benzyl or naphthyl group, or a phenyl group substituted by one or more halogen atoms, or by one or more alkyl, cyano, nitro, hydroxy or alkoxy groups; R.sub.1 is a hydrogen atom or an alkyl group; R.sub.2 and R.sub.3, which may be the same or different, are a hydrogen atom or an alkyl group, or form, with the nitrogen atom to which they are attached, a 5- to 7-membered heterocyclic ring; n is an integer of from 1 to 4; as well as the mineral or organic acid salts thereof. A further embodiment of the invention is the application of the derivatives of the general formula (I) as medications, in particular, for the treatment of depression, polyfunctional disorders, migraines and cardiovascular diseases.

Amino-alkoxy pyrazoles and pharmaceutical compositions

Amino-3-cardenolide derivatives represented by the general formula (I) ##STR1## wherein n and m, which may be the same or different, each represents an integer from 0 to 4; R.sub.1, R.sub.2, R.sub.4, R.sub.5 and R.sub.6, which may be the same or different, each represents a hydrogen atom or a hydroxy, alkoxy or acyloxy group; R.sub.3 represents a lower alkyl, aldehyde, haloalkyl, hydroxyalkyl, acyloxyalkyl, or ethylenedioxyalkyl group; R.sub.7 represents a hydrogen atom or an alkyl group; R.sub.8 represents a hydrogen atom or an alkyl, acyl, alkyloxycarbonyl or aralkoxycarbonyl group; R.sub.9 represents a hydrogen atom or an alkyl group; R.sub.8 and R.sub.9 can combine and form with the nitrogen atom a heterocyclic ring; R.sub.10 represents a hydroxy, alkoxy or aralkoxy group, an amino residue of amino acid or of an oligo-peptide, useful especially for the treatment of cardiac ailments.

Amino-3-cardenolide derivatives, process for their preparation, and

Cardiotonic cardenolide derivatives of the formula ##STR1## wherein n, m, R.sub.1 to R.sub.9 are as hereinafter defined, the mineral or organic salts thereof and a process for their preparation.

Growing community of inventors

Versailles, France

Francois-Xavier Jarreau