G.d. Searle & Company

Monsanto Company

Sanofi-aventis

Sanofi-synthelabo

Synthelabo

Pharmacia Corporation

Philippe R Bovy

Joseph Gerace Rico

Thomas Edward Rogers

Jeffery A Zablocki

Robert E Manning

Foe S Tjoeng

Joe T Collins

Masateru Miyano

Roberto Cecchi

Robert B Garland

Joan M O'Neal

David B Reitz

Tiziano Croci

Gilles Courtemanche

Claude L Gillet

Christophe Philippo

Ambrogio Oliva

Nunzia Viviani

Timothy S Chamberlain

Steven P Adams

Mihaly V Toth

Dudley E McMackins

Olivier Venier

Joseph L Roba

Georges E Lambelin

Alain Jean Braun

Olivier Crespin

Paul J Niebes

Michel P Snyers

Hugo J Gorissen

Marie Claire Orts

Albert Lenaers

Henry E Dayringer

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 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

2-arylquinoline derivatives, preparation and therapeutic use thereof

N-substituted (&agr;-imidazolyl-toluyl)pyrrole compounds for treatment of circulatory disorders

Benzylamine derivatives, their preparation and their application in

This invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutical compositions of such compounds and a method of treatment to inhibit aggregation of platelets.

Aminobenzamidinosuccinyl lactone derivatives useful as inhibitors of

Pharmaceutical compositions comprising a compound selected from a class of N-substituted (.alpha.-imidazolyl-toluyl)pyrrole compounds are described for use in treatment of circulatory disorders. Compositions of particular interest comprise angiotensin II antagonist compounds of the formula ##STR1## wherein m is one; wherein R.sup.0 is selected from CH.sub.2 OH, CO.sub.2 H, CHO, CO.sub.2 CH.sub.3, CO.sub.2 C.sub.2 H.sub.5, CH.sub.2 OCH.sub.3, CH.sub.2 OCHOCH.sub.3 and CH.sub.2 --CO.sub.2 C.sub.2 H.sub.5 ; wherein R.sup.1 is selected from Cl, CF.sub.3, CHO, n-butyl, cyano, CO.sub.2 CH.sub.3 and CO.sub.2 CH.sub.2 CH.sub.3 ; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, propylthio, butylthio and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.9 and R.sup.10 is hydrido; wherein each of R.sup.5 and R.sup.8 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl, methoxycarbonyl with the proviso that at least one of R.sup.5 and R.sup.8 is an acidic group selected from C02H and tetrazolyl; or a tautomer thereof or a pharmaceutically-aceptable salt thereof. These compositions are particularly useful in treatment or control of hypertension and congestive heart failure.

Pharmaceutical compositions for treatment of circulatory disorders using

Novel substituted .beta. amino acid derivatives are provided which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.

Substituted .beta.-amino acid derivatives useful as platelet aggregation

Pyrimidinylamidino .beta.-amino acid derivatives useful as inhibitors of

The invention relates to platelet aggregation inhibitors which are substituted beta amino acid derivatives of the formula: ##STR1## wherein Z, A, Z', Z', W, q, R.sup.1 and R.sup.2 are as defined in the specification.

A class of .omega.-amino-.alpha.-phenylalkanonitrile derivatives is described having use in treatment of cardiovascular dysfunctions such as hypertension. Compounds of most interest are those of the formula: ##STR1## wherein each of R.sub.1 and R.sub.2 is methoxy, R.sub.3 is hydrido, R.sub.4 is isopropyl, R.sub.5 is methyl and R.sub.6 is selected from linear alkyl, phenylpropyl, phenylbutyl and phenylpentyl.

.omega.-amino-.alpha.-phenylalkanonitrile derivatives

This invention relates to compounds having the following formula ##STR1## or pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.

Peptide mimics useful as platelet aggregation inhibitors

This invention relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.

Platelet aggregation inhibitors

A class of N-substituted N-(.alpha.-triazolyltoluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein m is one; wherein R.sup.1 is selected from alkyl; and wherein R.sup.2 is selected from alkyl; and wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 is independently selected from hydrido, halo, nitro, trifluoromethyl, hydroxy, alkoxy, cyano, carboxyl and methoxycarbonyl; with the proviso that at least one of R.sup.5 and R.sup.8 must be selected from COOH, SH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, OH, ##STR2## wherein each of R.sup.42 and R.sup.43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.

N-substituted N-(.alpha.-triazolyl-toluyl)pyrrole compounds for

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St. Louis, MO, United States of America

Philippe R Bovy