Abstract: The invention relates to the compounds of formula (I): ##STR1## in which: R.sub.1 denotes hydrogen, acyl, alkoxycarbonyl, benzyloxycarbonyl, phenoxycarbonyl or linear or branched C.sub.1 -C.sub.6 alkyl, substituted or unsubstituted, or R.sub.6 SO.sub.2 -- in which R.sub.6 denotes alkyl, naphthyl, phenyl, benzyl or morpholine,R.sub.2 denotes hydrogen or phenyl, substituted or unsubstituted benzyl, thienylmethyl, (pyridyl)methyl, diphenylmethyl, fluorenyl, naphthylmethyl, benzocyclobutyl, (dicyclopropylmethyl)methyl, indanyl or (C.sub.3 -C.sub.7 cycloalkyl)methyl,R'.sub.2 denotes hydrogen or elseR.sub.2 and R'.sub.2 together denote C.sub.6 H.sub.5 --CH.dbd.,R.sub.3 denotes any one of the groups as defined in the description, each of R.sub.4 and R.sub.5 denotes hydrogen or alkyl, or ##STR2## forms a boronic ester of pinanediol, A denotes the following group: ##STR3## in which n and A.sub.2 are as defined in the description, and medicinal products containing the same are useful as thrombin inhibitors.
Type:
Grant
Filed:
June 2, 1995
Date of Patent:
December 17, 1996
Assignee:
Adir et Compagnie
Inventors:
Guillaume de Nanteuil, Christine Lila, Philippe Gloanec, Michel Laubie, Tony Verbeuren, Serge Simonet, Alain Rupin
Abstract: Compounds of the general formula: ##STR1## wherein m, X, Y, A, R.sub.2 and R.sub.3 are defined in the description, and medicaments containing the same.
Type:
Grant
Filed:
May 9, 1995
Date of Patent:
December 17, 1996
Assignee:
Adir Et Compagnie
Inventors:
Muriel Duflos, Sylvie Robert-Piessard, Lucien Welin, Guillaume Le Baut, Daniel-Henri Caignard, Pierre Renard, G erard Adam
Abstract: The invention relates to a compound selected from those of formula (I) (SEQ ID NO:1): ##STR1## in which R.sub.1, R.sub.2, X.sub.1 and X.sub.2 are as defined in the description, useful as inhibitor of the proliferation component of vascular smooth muscle cells.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
October 29, 1996
Assignee:
Adir et Compagnie
Inventors:
Jean-Luc Fauchere, Christophe Thurieau, Jean-Paul Vilaine, Philip Janiak
Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.2', R.sub.2", R.sub.2'", R.sub.3 and n are as defined in the description, an optical isomer, and an addition salt thereof with a pharmaceutically-acceptable acid or base,and medicinal product containing the same useful for treating a mammal afflicted with a disorder associated to 5-HT.sub.1A or 5-HT.sub.2C receptors.
Type:
Grant
Filed:
March 10, 1995
Date of Patent:
October 29, 1996
Assignee:
Adir et Compagnie
Inventors:
G erald Guillaumet, Marie-Claude Viaud, Pierre Renard, G erard Adam, Daniel-Henri Caignard, B eatrice Guardiola-Lemaitre, Marie-Claire Rettori
Abstract: Compounds of formula (I): ##STR1## wherein R.sub.3, R.sub.4, R.sub.5, R.sub.6, X and Y are defined in the description.Those compounds are used therapeutically in the treatment of cancerous tumours.
Abstract: Compounds of formula (I): ##STR1## in which: R.sub.1 represents alkyl or (C.sub.3 -C.sub.7) cycloalkylR.sub.2 represents alkyl, or (C.sub.3 -C.sub.7) cycloalkyl,R.sub.3 represents hydrogen or alkyl,R.sub.4 represents halogen or alkyl or alkoxy,R.sub.5 represents alkyl,X and Y, which are different, represent CO or SO.sub.2,n represents 1, 2 or 3,p represents 0 or 1,Z represents sulfur or oxygen,A represents any one of the following groups: ##STR2## in which: A.sub.1 represents, with the nitrogen and carbon atoms to which it is attached, a mono- or bicyclic heterocycle,.cndot. or, ##STR3## in which: R.sub.6 represents hydrogen, alkyl or cycloalkyl or 2-indanyl,R.sub.7 represents hydrogen or alkyl,which compounds of formula (I) comprise thereof corresponding hydrates of the ketone function COCF.sub.3,the enantiomers, diastereoisomers and epimers thereof and the addition salts thereof with a pharmaceutically acceptable base and medical products containing the same are useful as HLE inhibitor.
Type:
Grant
Filed:
May 5, 1995
Date of Patent:
October 22, 1996
Assignee:
Adir et Compagnie
Inventors:
Guillaume de Nanteuil, Bernard Portevin, Emmanuel Canet
Abstract: Compounds of formula (I): ##STR1## wherein: R.sub.1 represents an unsubstituted or substituted alkyl,R.sub.2 represents an unsubstituted or substituted alkyl,A represents, with the nitrogen and carbon atoms to which it is attached, a nitrogenous mono- or polycyclic structure, andB represent any one of the radicals a through j as defined in the description, and medicaments containing the same, are useful as human leucocyte elastase inhibitors.
Type:
Grant
Filed:
May 11, 1995
Date of Patent:
October 15, 1996
Assignee:
Adir et Compagnie
Inventors:
Michel Vincent, Guillaume de Nanteuil, Georges Remond, Bernard Portevin, Yolande Herve, Emmanuel Canet, Michel Lonchampt
Abstract: The compounds are N-(2,3,4-trimethoxybenzyl)piperazines N'-substituted by a radical containing a sulfonamide group, and pharmaceutically tolerable salts thereof, useful for treating myocardial ischaemic pathologies, cerebral vascular accident and manifestations of deficiency associated with chronic cerebral circulatory disorders.A compound disclosed is : N-benzyl-N-{3,3-dimethyl-4-[4-(2,3,4-trimethoxybenzyl) piperazin-1-yl]butyl}-(isoquinolin-5-yl)sulfonamide and its fumarate.
Abstract: The invention relates to peptide compounds of formula (I):R.sub.1 --A--Gly--Asp--Trp--R.sub.2 (I)in which R.sub.1, R.sub.2 and A are as defined in the description, and anti-aggregation medicaments containing the same.
Type:
Grant
Filed:
August 11, 1994
Date of Patent:
October 15, 1996
Assignee:
Adir et Compagnie
Inventors:
Jean-Luc Fauchere, Angela D. Morris, Christophe Thurieau, Tony Verbeuren, Serge Simonet
Abstract: A compound of formula (I): ##STR1## in which: R represents naphthyl, 5,6,7,8-tetrahydronaphthyl, 1,2,3,4-tetrahydronaphthyl, thienyl, optionally substituted phenyl or (C.sub.3 -C.sub.7)cycloalkyl,n represents an integer such that 1.ltoreq.n.ltoreq.8, their enantiomers, diastereoisomers and epimers as well as their addition salts with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as antagonists of substance P.
Type:
Grant
Filed:
April 26, 1995
Date of Patent:
October 1, 1996
Assignee:
Adir ET Compagnie
Inventors:
Jean-Luc Fauchere, Nathalie Kucharczyk-Gentric, Joseph Paladino, Jacqueline Bonnet, Emmanuel Canet, Graham Birrell
Abstract: A compound which is selected from those of formula (I): ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description,its optical isomers and its addition salts thereof with a pharmaceuticaliy-accepable acid or base,and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.
Type:
Grant
Filed:
May 22, 1995
Date of Patent:
September 10, 1996
Assignee:
Adir et Compagnie
Inventors:
Michel Langlois, Pierre Renard, G erard Adam
Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification,and a medicinal product containing said compound for treating a disorder of the melatoninergic system.
Type:
Grant
Filed:
May 23, 1995
Date of Patent:
September 3, 1996
Assignee:
Adir et Compagnie
Inventors:
Patrick Depreux, Hamid Ait Mansour, Daniel Lesieur, Fran.cedilla.ois Lefoulon, Pierre Renard, G erard Adam, Philippe Delagrange
Abstract: A compound of formula (I): ##STR1## in the form of its S enantiomer, its addition salts with a pharmaceutically acceptable acid or base and medicinal product containing the same are useful for the treatment or prevention of pathologies associated with dysfunction of glutamatergic neurotransmission.
Type:
Grant
Filed:
July 11, 1995
Date of Patent:
July 16, 1996
Assignee:
Adir et Compagnie
Inventors:
Alex Cordi, Michael Spedding, Bernard Serkiz, Jean Lepagnol, Patrice Desos, Philippe Morain
Abstract: Compound of formula (I): ##STR1## in which R.sub.1, R.sub.2 and R.sub.3, which are identical or different, represent hydrogen or halogen or alkyl, nitro, cyano or aminosulfonyl, or alternatively, when two of them are located on adjacent carbons, form, with the carbon atoms to which they are attached, (C.sub.3 -C.sub.7) cycloalkyl ring or substituted or unsubstituted benzene ring,R.sub.4 represents hydrogen, linear or branched (C.sub.1 -C.sub.6) alkyl, substituted or unsubstituted phenyl or a group ##STR2## in which R.sub.6 and R.sub.7, which are identical or different, represent hydrogen or substituted or unsubstituted, linear or branched (C.sub.1 -C.sub.6) alkyl,R.sub.5 represents hydrogen, hydroxyl, linear or branched (C.sub.1 -C.sub.6) alkoxy, phenoxy, mercapto, linear or branched (C.sub.1 -C.sub.6) alkylthio, substituted or unsubstituted, linear or branched (C.sub.1 -.sub.6) alkyl, substituted or unsubstituted phenyl or substituted or unsubstituted amino; or a group ##STR3## in which R.sub.6 and R.sub.
Type:
Grant
Filed:
August 30, 1994
Date of Patent:
July 16, 1996
Assignee:
Adir et Compagnie
Inventors:
Alex Cordi, Patrice Desos, Jean Lepagnol
Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## wherein Ar, n, B and A are as defined in the description, to their optical isomers, and to their addition salts there of with a pharmaceutically-acceptable acid or base. The compounds are useful for treating or preventing anxiety and depression.
Type:
Grant
Filed:
August 26, 1994
Date of Patent:
July 9, 1996
Assignee:
Adir Et Compagnie
Inventors:
Ousmane Diouf, Daniel Lesieur, Patrick Depreux, Beatrice Guardiola-Lemaitre, Daniel-Henri Caignard, Pierre Renard, Gerard Adam
Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.3, X and n are as defined in the description, the optical isomers thereof, and the addition salts thereof with a pharmaceutically acceptable acid or base and medicinal product containing the same, useful for treating a mammal afflicted with a pathology associated with the sigma receptors.
Type:
Grant
Filed:
March 21, 1995
Date of Patent:
July 9, 1996
Assignee:
Adir et Compagnie
Inventors:
Ange Mouithys-Mickalad, Patrick Depreux, Daniel Lesieur, Gerard Adam, Daniel-Henri Caignard, Pierre Renard, Marie-Claire Rettori
Abstract: The invention relates to compounds of the general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and Z are as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base and medicaments containing the same, useful in the treatment and prevention of stress, anxiety, and related ailments.
Type:
Grant
Filed:
July 2, 1993
Date of Patent:
May 21, 1996
Assignee:
Adir et Compagnie
Inventors:
Marc Payard, Genevieve Baziard-Mouysset, Gilbert De Saqui-Sannes, Beatrice Guardiola, Daniel-Henri Caignard, Pierre Renard, Gerard Adam
Abstract: The invention relates to the compounds of formula (I): ##STR1## in which R.sub.1 and R.sup.2 are as defined in the description, the optical isomers thereof,and an addition salt thereof with a pharmaceutically-acceptable acid or base, and medicinal product useful for treating a mammal afflicted with a disease associated with sigma receptors.
Type:
Grant
Filed:
March 21, 1995
Date of Patent:
April 30, 1996
Assignee:
Adir et Compagnie
Inventors:
Hamid A. Mansour, Thierry Taverne, Raymond Houssin, Isabelle Lesieur, Patrick Depreux, Geard Adam, Daniel-Henri Caignard, Pierre Renard, Marie-Claire Rettori
Abstract: New substituted phenoxyisobutyric acids and esters that can be used as medicaments and correspond to the formula: ##STR1## wherein X, A, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and Z are as defined in the description.Those compounds and their physiologically tolerable salts can be used therapeutically.
Type:
Grant
Filed:
April 19, 1994
Date of Patent:
April 30, 1996
Assignee:
Adir et Compagnie
Inventors:
Gilbert Regnier, Claude Guillonneau, Jean-Paul Vilaine, Albert Lenaers, Christine Breugnot