Sanofi

Sanofi-aventis

Elf Sanofi

Sanofi-synthelabo

Tiziano Croci

Umberto Guzzi

Roberto Cecchi

Alberto Bianchetti

Marco Baroni

Costantino Palmieri

Philippe Bovy

Dino Nisato

Gilles Courtemanche

Luciano Manara

Marco Landi

Ambrogio Oliva

Nunzia Viviani

Philippe R Bovy

Olivier Venier

Robert Boigegrain

Eric Marsault

Stefano Romagnano

Antonina Giudice

Philippe Soubrie

Elena Poggesi

Jacques Simiand

Laura Barzaghi

Roberta Avallone

Peter-Eugene Keane

G Erard Le Fur

Constantino Palmieri

The present disclosure relates to the use of a (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivative or (heterocycle-fused pyrrolidine)-(piperazinyl)-1-alkanone derivative or a pharmaceutically acceptable salt thereof as a p75 receptor antagonist in the treatment and/or prevention of overactive bladder.

Therapeutic use of P75 receptor antagonists

The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an &#x2014;S(O)(C-C)alkyl group, an &#x2014;NHSO(C-C)alkyl group, an &#x2014;SONH(C-C)alkyl group, an &#x2014;NHSOphenyl-(C-C)alkyl group or an &#x2014;NHSOphenyl group, said phenyl possibly being substituted with a halogen atom, with a (C-C)alkyl group or with a (C-C)alkoxy group; Rrepresents a hydrogen atom or a (C-C)alkyl group, a &#x2014;CO(C-C)alkyl group, a phenyl-(C-C)alkyl group or a &#x2014;COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C-C)alkoxy group; Ris a hydrogen atom or an &#x2014;SO(C-C)alkyl group, an &#x2014;SOphenyl-(C-C)alkyl group or an &#x2014;SOphenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C-C)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; Rrepresents a hydrogen or halogen atom, a (C-C)alkyl group, a (C-C)alkoxy group, a &#x2014;COO(C-C)alkyl group, a &#x2014;CO(C-C)alkyl group, an &#x2014;NHSO(C-C)alkyl group, an &#x2014;NHSOphenyl-(C-C)alkyl groups, &#x2014;NO, &#x2014;CN, &#x2014;CONRR, &#x2014;COOH, or a 4,5-dihydro-1,3-oxazol-2-yl or 4,4-dimethyl-4,5-dihydro-1,3-oxazol-2-yl group; Rand Rrepresent, independently, a hydrogen atom, a phenyl, a (C-C)alkyl group or a phenyl-(C-C)alkyl group or Rand Rwith the nitrogen atom to which they are attached, may form a ring of 5 to 7 atoms in total; and to the salts or solvates thereof, to the pharmaceutical compositions containing them, to a process for the preparation thereof and to intermediates in this process.

Cyclohexyl(alkyl)propanolamines, preparation method and pharmaceutical compositions containing same

The invention relates to the compounds of general formula (I) where Rrepresents H, a (C1-C4)alkyl, &#x2014;CO(C1-C4)alkyl, (C1-C4)alkylphenyl or &#x2014;CO-phenyl group, said phenyl being optionally substituted, Rrepresents H, a halogen atom, an &#x2014;S(O)R, &#x2014;NHSOR, &#x2014;NHSO-phenyl or &#x2014;NHSO&#x2014;(C1-C4)alkylphenyl group where z is equal to 0, 1 or 2 and where Rrepresents a (C1-C4)alkyl group, said phenyl being optionally substituted; where n is equal to 0, 1 or 2, Rand Rrepresent H, a (C1-C4)alkyl, hydroxyl, cyano, phenyl, benzyl, piperidyl, &#x2014;CONH, &#x2014;CO-phenyl, &#x2014;COOR, &#x2014;CH(phenyl) (OH) and &#x2014;C(phenyl)(OH) group, or Rand Rform together an optionally substituted 6-membered aromatic ring, Rrepresents H, a (C1-C4)alkyl, phenyl or benzyl group, and B represents a 5- or 6-membered nitrogen-containing heterocycle or homocycle optionally fused with a phenyl Group or optionally substituted; their addition salts; their method of preparation and their therapeutic application.

Oxophenyl-cyclohexyl-propanolamine derivatives, production and use thereof in therapeutics

The invention relates to compounds of general formula (I): 

Phenylcyclohexylpropanolamine derivatives, preparation and therapeutic application thereof

The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an &#x2014;S(O)(C&#x2013;C)alkyl group, an &#x2014;NHSO(C&#x2013;C)alkyl group, an &#x2014;SONH(C&#x2013;C)alkyl group, an &#x2014;NHSOphenyl-(C&#x2013;C)alkyl group or an &#x2014;NHSOphenyl group, said phenyl possibly being substituted with a halogen atom, with a (C&#x2013;C)alkyl group or with a (C&#x2013;C)alkoxy group; Rrepresents a hydrogen atom or a (C&#x2013;C)alkyl group, a &#x2014;CO(C&#x2013;C)alkyl group, a phenyl-(C&#x2013;C)alkyl group or a &#x2014;COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C&#x2013;C)alkoxy group; Ris a hydrogen atom or an &#x2014;SO(C&#x2013;C)alkyl group, an &#x2014;SOphenyl-(C&#x2013;C)alkyl group or an &#x2014;SOphenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C&#x2013;C)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; Rrepresents a hydrogen or halogen atom, a (C&#x2013;C)alkyl group, a (C&#x2013;C)alkoxy group, a &#x2014;COO(C&#x2013;C)alkyl group, a &#x2014;CO(C&#x2013;C)alkyl group, an &#x2014;NHSO(C&#x2013;C)alkyl group, an &#x2014;NHSOphenyl-(C&#x2013;C)alkyl groups, &#x2014;NO, &#x2014;CN, &#x2014;CONRR, &#x2014;COOH, or a 4,5-dihydro-1,3-oxazol-2-yl or 4,4-dimethyl-4,5-dihydro-1,3-oxazol-2-yl group; Rand Rrepresent, independently, a hydrogen atom, a phenyl, a (C&#x2013;C)alkyl group or a phenyl-(C&#x2013;C)alkyl group or Rand Rwith the nitrogen atom to which they are attached, may form a ring of 5 to 7 atoms in total; and to the salts or solvates thereof, to the pharmaceutical compositions containing them, to a process for the preparation thereof and to intermediates in this process.

Cyclohexyl(alkyl)-propanolamines, preparation method and pharmaceutical compositions containing same

The invention relates to phenoxypropanolamines, to pharmaceutical compositions containing them, to processes for preparing them, and to the method of use thereof in the treatment of diseases that are improved by beta-3 agonist action.

Propanolaminotetralines, preparation thereof and compositions containing same

Phenoxylpropanolamines, method for the production thereof and pharmaceutical compositions containing the same

This invention relates to the treatment of edematous conditions in an animal by administering a neurotensin antagonist having diuretic activity.

Use of neurotensin antagonists for the treatment of edematous conditions

A compound of formula (VIII): ##STR1## in which Alk is a (C.sub.1 -C.sub.4)alkyl group, R.cndot. is hydrogen or a protecting group cleavable by hydrolysis and R is hydrogen, a protecting group cleavable by reduction or a heterocycle of structure (IX): ##STR2## in which Hal is a halogen atom and X, Y and Z are each --CH.dbd. or one of them is a nitrogen atom and the others are --CH.dbd., and its salts, R.cndot. being other than hydrogen if R is hydrogen or a group of structure (IX).

Heteroarylpiperidines

A method is disclosed for the treatment of neuronal degenerative processes. The method comprises administering 1-[4-(3-trifluoromethylphenyl)-1, 2, 3, 6-tetrahydropyrid-1-yl]-2-)6, 7-dimethoxynaphth-2-yl)ethane or a pharmaceutically acceptable salt thereof to a mammal suffering from a neuronal degenerative process.

N-substituted trifluoromethylphenyltetrahydropyridines, process for the

The present invention concerns the use of 4-amino-1-(2-pyridyl)piperidines of general formula (I') ##STR1## wherein R' represents hydrogen, a halogen atom, a methyl, methylthio, trifluoromethyl, trifluoromethylthio, (C.sub.1 -C.sub.3)alkoxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, or phenoxy group optionally substituted with a halogen atom, a trifluoromethyl, (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, (C.sub.1 -C.sub.3)alkylthio, or cyano group, or of a pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment or prophylaxis of those conditions deriving from disorders of the serotoninergic systems wherein a serotoninergic action selectively mediated by the 5-HT.sub.3 receptors is required, e.g. affective disorders, anxiety, psychotic troubles, constipation.

Use of 4-amino-1-(2-pyridyl)piperidines for the preparation of a

New N-substituted 4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridines useful in the treatment of intestinal motility disorders, of the following general formula ##STR1## wherein A represents a group -E-G or -L-M, where

N-substituted trifluoromethylphenyltetrahydropyridines process for the

The present invention relates to novel heteroarylpiperidines of formula (I): ##STR1## in which Hal is a halogen atom, Alk is a C.sub.1-4 alkyl group and one of X, Y and Z is a nitrogen atom while the others are .dbd.CH--, and their salts. These compounds are useful as 5-HT.sub.3 agonists.

1-Halopyrazin- and 1-halopyrimidin-4-amino-4-alkylpiperidines

New N-substituted 4-(3-trifluoromethylpheny1)-1,2,3,6-tetrahydropyridines useful in the treatment of intestinal motility disorders, of the following general formula ##STR1## wherein A represents a group --E--G or --L--M, where

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Milan, Italy

Tiziano Croci