Sanofi-aventis

Nunzia Viviani

Roberto Cecchi

Tiziano Croci

Gilles Courtemanche

Ambrogio Oliva

Philippe R Bovy

Philippe Bovy

Laura Barzaghi

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 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

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Cantu, Italy

Nunzia Viviani