Sanofi

Sanofi-Aventis

Sanofi-Synthelabo

Elf Sanofi

Roberto Cecchi

Tiziano Croci

Umberto Guzzi

Robert Boigegrain

Sergio Boveri

Philippe Bovy

Ambrogio Oliva

Nunzia Viviani

Laura Barzaghi

Philippe R Bovy

Gilles Courtemanche

Olivier Venier

Domenico Badone

Marco Baroni

Eric Marsault

Alberto Bianchetti

Stefano Romagnano

Luciano Manara

Elena Poggesi

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 concerns compounds of formula (I), wherein A is a group of formula (a) or (b), wherein: R represents a hydrogen or halogen atom, a &#x2014;S(O)(C&#x2013;C)Alk wherein z is 0, 1 or 2, a &#x2014;NHSO(C&#x2013;C)Alk, &#x2014;SONH(C&#x2013;C)Alk, &#x2014;NHSO&#x2014;(C&#x2013;C)Alk-phenyl or &#x2014;NHSO-phenyl group, said phenyl capable of bearing a halogen atom, a (C&#x2013;C)Alk group or a (C&#x2013;C)alkoxy group; Rrepresents a hydrogen atom or a &#x2014;(C&#x2013;C)Alk, &#x2014;CO(C&#x2013;C)Alk, &#x2014;(C&#x2013;C)Alk-phenyl or &#x2014;CO-phenyl group, said phenyl capable of bearing a halogen atom or a &#x2014;(C&#x2013;C)Alk or (C&#x2013;C)alkoxy group; Ris a hydrogen atom, a &#x2014;SO(C&#x2013;C)Alk, &#x2014;SO&#x2014;(C&#x2013;C)Alk-phenyl, &#x2014;SO-phenyl group, or a &#x2014;(C&#x2013;C)Alk group; X completes a saturated or unsaturated cycle of 5 to 8 atoms, capable of bearing one or two &#x2014;(C&#x2013;C)Alk groups and/or two carbonyl groups; Rand R'represent each independently a hydrogen or halogen atom, a &#x2014;(C&#x2013;C)Alk, hydroxy, &#x2014;CN, &#x2014;(C&#x2013;C)alkoxy, &#x2014;CORor Y&#x2014;CRR&#x2014;CORgroup; Y represents O or CH; Rrepresents a hydroxy, (C&#x2013;C)alkoxy or &#x2014;NRRgroup; Rand Rindependently represent a hydrogen atom, a &#x2014;(C&#x2013;C)Alk, group, aryl or heteroaryl optionally substituted by a Rgroup, aralkyl or heteroaralkyl optionally substituted by a Rgroup; or Rand R, with the nitrogen atom which bears them, form a saturated or unsaturated cycle of 5 to 7 atoms optionally substituted by a Rgroup; and Rrepresents a hydrogen or halogen atom, a hydroxy, &#x2014;(C&#x2013;C)Alk, &#x2014;(C&#x2013;C)alkoxy, &#x2014;NH(C&#x2013;C)Alk, &#x2014;N(C&#x2013;C)Alk, &#x2014;COO(C&#x2013;C)Alk, aralkyl or heteroaryl group; Rand Rindependently represent a hydrogen atom or a &#x2014;(C&#x2013;C)Alk group; their salts or solvates, the pharmaceutical compositions containing them, a method for preparing them and synthesis intermediates  

Propanolaminomethyltetralines, their preparation and pharmaceutical composition comprising 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

The invention relates to compounds of formula (I)where

Phenoxypropanolamines, method for producing them and pharmaceutical compositions containing them

Compounds of formula (I):where X is N or CH;

Heteroaryloxy propanolamines, preparation method and pharmaceutical compositions containing same

The invention concerns phenoxypropanolamines of formula (I)in which Rrepresents a hydrogen, a group &#x2014;S(O)&#x2014;(C-C)alk-R', (R&#x2032; being H, phenyl or (C-C)alkoxy), &#x2014;NHSO&#x2014;(C-C)alk or NHCO(C-C)alk; m and n are each independently 0, 1 or 2; Rand Rindependently represent a hydrogen, a (C-C)alkyl, (C-C)cycloalkyl, (C-C)alkoxy, hydrogen(C-C)alkoxy-(C-C)alkyl, mono- or di(C-C)alkamino(C-C)alkyl, pyrrolidino(C-C)alkyl, phenylamino or (C-C)alkenyl group, an aromatic or heteroaromatic group optionally substituted with a group R, an aralkyl or heteroaralkyl group optionally substituted with a group R, Rand Rcan also together constitute a saturated or unsaturated ring of 3 to 8 atoms possibly bearing a (C-C)alkyl, amino (C-C)alkyl, carbamoyl or benzyl substituent; Rrepresents a hydrogen or a halogen, or a group &#x2014;CO(C-C)alk or a group &#x2014;NHSO&#x2014;(C-C)alk; a group (C-C)alk, a group (C-C)alkoxy, a halogen, &#x2014;COOH, &#x2014;COO(C-C)alk, &#x2014;CN, &#x2014;CONRR, &#x2014;NO, &#x2014;SONHor &#x2014;NHSO(C-C)alk; z is 1 or 2; and the salts or solvates thereof. The compounds have agonist activity toward &#x3b2;-3 adrenergic receptors.

Phenoxypropanolamines, preparation and therapeutic use thereof

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

The present invention relates to an enzymatic process for the preparation of optically active tetrahydro-2-naphthoic acids from the corresponding racemic esters by reaction with a lipase.

Enzymatic process for the preparation of optically active tetralin

Enzymatic process for the preparation of optically active

The present invention relates to the novel compound {(7S)-7-[(2R)-2-(3-chlorophenyl)-2-hydroxyethylamino]-5,6,7,8-tetrahydrona phthalen-2-yloxy}acetic acid of formula (I): ##STR1## and its pharmaceutically acceptable salts, which act as .beta..sub.3 -adrenergic agonists, and to the pharmaceutical compositions and laboratory reagents in which it is present.

{(7S)-7-[(2R

Phenylethanolamino- and phenylethanolaminomethyltetralines of formula (I) ##STR1## wherein X represents a hydrogen atom, a halogen atom,a (C.sub.1 -C.sub.4)alkyl group or a trifluoromethyl group,

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Lodi, Italy

Roberto Cecchi