Sanofi

Societe Anonyme Sanofi

Paul Worms

Camille G Wermuth

Dominique Olliero

Jean-Jacques Bourguignon

Roger Brodin

Robert Boigegrain

Kathleen Biziere

Jean P Kan

The present invention relates to pyridazine derivatives of formula: ##STR1## which are useful as ligands of cholinergic receptors, in particular, receptors of the M.sub.1 type.

Pyridazine derivatives

The invention relates to thiazole derivatives corresponding to the general formula: ##STR1## in which: - R.sub.1 and R.sub.2 each independently represent hydrogen; a C.sub.1 -C.sub.4 alkyl group; a phenyl group or a phenyl group monosubstituted or polysubstituted by a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy, nitro or hydroxyl group; or one of the groups R.sub.1 and R.sub.2 denotes hydrogen and the other represents a naphthyl group; a benzyl group; an .alpha.,.alpha.-dimethyl-benzyl group; a cyclohexyl group; a biphenyl group; a thienyl group or an adamantyl group; or alternatively R.sub.1 and R.sub.2, taken together, represent a group; ##STR2## in which the phenyl group is bonded to the 4-position of the thiazole and the group (CH.sub.2).sub.m to the 5-position, m represents an integer equal to 2 or 3 and R.sub.5 denotes hydrogen or a nitro group, R.sub.3 is H or an alkyl group and R.sub.4 is notably an alkyl substituted by an amino group, a pyrrolidino, or a pydridino group.

Fused-thiazole derivatives active on the cholinergic system, and

The invention relates to thiazole derivatives corresponding to the general formula: ##STR1## in which: R.sub.1 and R.sub.2 each independently represent hydrogen; a C.sub.1 -C.sub.4 alkyl group; a phenyl group or a phenyl group monosubstituted or polysubstituted by a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy, nitro or hydroxyl group; or one of the groups R.sub.1 and R.sub.2 denotes hydrogen and the other represents a naphthyl group; a benzyl group; an .alpha.,.alpha.-dimethyl-benzyl group; a cyclohexyl group; a biphenyl group; a thienyl group of an adamantyl group; or alternatively R.sub.1 and R.sub.2, taken together, represent a group; ##STR2## in which the phenyl group is bonded to the 4-position of the thiazole and the group (CH.sub.2).sub.m to the 5-position, m represents an integer equal to 2 or 3 and R.sub.5 denotes hydrogen or a nitro group, R.sub.3 is H or an alkyl group and R.sub.4 is notably an alkyl substituted by an amino group, a pyrrolidino, or a pyridino group.

Thiazole derivatives active on the cholinergic system, process for

The present invention relates to thiadiazole derivatives having the formula: ##STR1## in which: R.sub.1 represents a phenyl group, non-substituted or substitued 1 to 3 times by a halogen atom, preferably chlorine or fluorine, or by a C.sub.1 -C.sub.4 alkyl group, preferably the methyl group, or by a C.sub.1 -C.sub.4 alkoxy group, preferably the methoxy group, or by a hydroxy group or by a trifluoromethyl group or a phenyl group substituted simultaneously by 1 to 3 halogen atoms and by 1 or 2 methyl groupings;

Derivatives of 1,3,4-thiadiazole, a method of obtaining them and

The invention relates to the use of 5-alkylpyridazine derivatives of the formula ##STR1## in which R.sub.1 is a C.sub.1 -C.sub.4 alkyl group or a phenyl group and R.sub.2 and R.sub.3 independently are a C.sub.1 -C.sub.4 alkyl group, or R.sub.2 and R.sub.3, taken with the nitrogen atom to which they are bonded, form a morpholino group, or one of their pharmaceutically acceptable salts, for the preparation of pharmaceutical compositions for combating pathological conditions associated with a cortical cholinergic deficiency, especially for the treatment of degenerative syndromes associated with senescence.

Use of 5-alkylpyridazine derivatives as drugs active on the cholinergic

The invention relates to novel tricyclic derivatives which are agonists of cholinergic receptors. These derivatives have the formula ##STR1## in which X=O, S, --OCH.sub.2 -- or --SCH.sub.2 --; R.sub.1 =H or halogen; and R.sub.2 = ##STR2## in which Alk is an alkylene group and R.sub.3, an R.sub.4, which are identical or different, are hydrogen or a lower alkyl group, or R.sub.3 and R.sub.4, with the nitrogen atom to which they are bonded, form a 5- or 6-membered cyclic amino group optionally containing a second heteroatom; or R.sub.2 is a group ##STR3## where R.sub.5 =C.sub.1 -C.sub.4 -alkyl. Application: agonists of cholinergic receptors.

Tricyclic cholinergic receptor agonists

The invention relates to novel tricyclic derivatives which are agonists of cholinergic receptors and to drugs containing them. These derivatives have the following formula: ##STR1## in which: X represents a group (CH.sub.2).sub.n, n representing an integer equal to 2, 3 or 4, or alternatively a vinylene group or a methylvinylene group;

Novel tricyclic derivatives which are agonists of cholinergic receptors,

The present invention relates to imidazo[1,2-b]-pyridazines having the formula: ##STR1## in which: R.sub.1 represents hydrogen, a halogen atom, a C.sub.1 -C.sub.4 alkoxy group or a C.sub.1 -C.sub.4 alkyl group occupying one of the free positions of the benzene ring; R.sub.2 represents hydrogen, a C.sub.1 -C.sub.4 alkyl group or a phenyl group; R.sub.3 denotes hydrogen, a C.sub.1 -C.sub.4 alkyl group or a phenyl group; and R.sub.4 R.sub.5 represent hydrogen or a C.sub.1 -C.sub.4 alkyl group, or R.sub.4 and R.sub.5 form, together with the nitrogen atom to which they are bonded, a 5-membered or 6-membered heterocycle optionally containing a second heteroatom. Application: drugs, especially for the treatment of cortical cholinergic deficiencies.

Imidazo[1,2-]pyridazines for cortical cholinergic deficiencies

The invention relates to thiadiazole derivatives corresponding to the formula: ##STR1## in which R represents: a linear or branched alkyl group having from 1 to 5 carbon atoms;

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St Gely Du Fesc, France

Paul Worms