Gruppo Lepetit

Elvio Bellasio

Ambrogio Campi

Nunzio Di Mola

Emiliana Baldoli

Franco Cristiani

A process for the preparation of tertiary diphenyl carbinols containing a primary or secondary amine substituent on the aliphatic moiety attached to the carbinol function which consists in contacting a Grignard phenyl reagent with an aminoacid wherein the mobile protons are not masked in an aprotic inert organic solvent or a mixture thereof at a temperature between 20.degree. C. and the boiling temperature by the reaction mixture. The reaction products are useful as active ingredients of medicaments and intermediates for the manufacture thereof.

Process for the preparation of tertiary carbinols containing an amino

The present invention refers to a new process for preparing N-2,3,4,5-substituted-1H-pyrrol-1-yl)-6-substituted amino-3-pyridazineamine, known as antihypertensive agents. The process is characterized in that a suitable 3,6-dihalogenopyridazine is reacted with hydrazine hydrate or other hydrazine derivatives of formula NH.sub.2 NHR, the obtained compound is reacted with a suitable dicarbonyl compound yielding first an alcandione-bis-[6-halogen-3-pyridazininyl]hydrazone, and then a 6-halogen-3-pyrrolylpyridazineamine derivative which is in turn reacted with an amine to yield the desired compounds.

Process for preparing N-pyrrolyl-pyridazineamine derivatives

New-pyrrolyl-3-pyridazineamines having a further aminic substituent in the position 6. The compounds are useful as antihypertensive agents and may be prepared from 6-amino substituted-3-hydrazino pyridazines and .beta.-dicarbonyl compounds. The use of the novel compounds as antihypertensives and compositions containing the novel compounds as active ingredients are also claimed.

N-Pyrrolyl-pyridazineamines and their use as antihypertensive agents

The compounds 2-Aryl-3-amino-1-butanol derivatives of the formula ##STR1## wherein R represents hydrogen or acyl; R.sup.1 and R.sup.2 each independently represents hydrogen, phenyl lower alkyl, or lower alkoxy substituted phenyl lower alkyl, or both R.sup.1 and R.sup.2 are lower alkyl; and their pharmaceutically acceptable acid salts. The compounds are crystalline solids or liquids which, having two asymmetry centers, can be obtained in their stereoisomeric forms as racemic mixtures or in their optically active forms. The compounds have cardiovascular activity as coronary dilators. The compounds can be prepared by reacting an .alpha.-arylcrotonate with ammonia or with an amine followed by hydrogenation of the carbalkoxy group to give the corresponding butanol. The butanols are acylated in usual ways to give the compounds of formula (I) wherein R represents an acyl group.

2-(Aryl)-3-(dimethylamino)butyl-3,4,5-trimethoxybenzoates

6-Morpholino-3-substituted phenyl triazolopyridazine compounds such as 8-methyl-6-morpholino-3-phenyl-s-triazolo[4,3-b]pyridazine or 8-methyl-6-morpholino-3-(3,4,5-trimethoxyphenyl)-s-triazolo[4,3-b]pyridazi ne are prepared by the reaction of the corresponding substituted benzoyl halide with a 3-hydrazino-6-morpholinopyridazine in the presence of a hydrogen chloride acceptor or by the reaction of a 3-halo-6-morpholinopyridazine with a corresponding substituted benzoyl hydrazide. The compounds have pharmacological activity as bronchodilators.

6-Morpholino-3-substituted phenyl-S-triazolo[4,3-b]pyridazines

Aminopropanols with .beta.-blocking activity having the general formula ##SPC1## Wherein R is hydrogen, C.sub.1 -C.sub.4 alkyl or hydroxy-(C.sub.2 -C.sub.4) alkyl, R.sub.1 is C.sub.1 -C.sub.4 alkyl or hydroxy-(C.sub.2 -C.sub.4) alkyl; R.sub.2 and R.sub.3 each independently represent hydrogen or C.sub.1 -C.sub.2 alkyl, R.sub.4 is hydrogen or alkoxy of 1 to 4 C, n is the number 1 or 2; and their pharmaceutically acceptable acid addition salts.

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Como, Italy

Elvio Bellasio