Etablissements Nativelle, S.a.

Jean J Koenig

Francois X Jarreau

Francois-Xavier Jarreau

Francois-Xaver Jarreau

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

The invention relates to medicinally useful steroid derivatives, particularly amino-14 steroids substituted at the 17-position by a functional group represented by the general formula: ##STR1## wherein R.sub.1 is a hydroxy, hydroxyalkyl, alkoxy, acyloxy, carboxy or carbalkoxy group, or a hydrogen atom, and R.sub.2 is a hydroxy, alkoxy, or acyloxy group. These amino-14 steroids are prepared from the corresponding hydroxy-14 steroids, by the action of hydrazoic acid in the presence of boron trifluoride etherate to form the azido-14 derivative which is reduced.

Amino-14 steroid derivatives and process for preparation of the same

Aminocardenolides of formula (I): ##STR1## in which 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, hydroxyalkyl, acyloxyalkyl, haloalkyl or ethylenedioxyalkyl group; R.sub.7 represents a hydrogen atom, or an alkyl or acyl group, and R.sub.8 represents a hydrogen atom, an alkyl group or an amino acid residue; a process for preparation of the compounds with the above formula by reaction of an oxo-3 genin with an ammonium salt in the presence of a borocyanohydride in an organic solvent. The aminocardenolides of formula (I) are useful especially for the treatment of cardiac ailments.

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Vernou La Celle, France

Jean J Koenig