Abstract: The present invention relates to a new racecadotril formulation in the form of tablets, the preparation process thereof and the use thereof to treat diarrhoea.
Abstract: The invention relates to new crystalline 1-[3-[3-(4-chlorophenyl)propoxy]propyl]-piperidine monohydrochloride, the respective manufacture and methods of use, and compositions containing such a compound.
Type:
Grant
Filed:
February 6, 2006
Date of Patent:
June 26, 2012
Assignee:
Bioprojet
Inventors:
Manuel Raga, Juan Sallares, Marta Guerrero, Antonio Guglietta, Jean-Michel Arrang, Jean-Charles Schwartz, Holger Stark, Walter Schunack, Xavier Ligneau, Jeanne-Marie Lecomte, Charon Ganellin
Abstract: The present invention concerns novel pharmaceutical compositions of immethridine, in particular of novel pharmaceutically acceptable salts thereof, such as the dioxalate salt of immethridine, as well as its therapeutical uses and novel process of preparation.
Type:
Application
Filed:
May 18, 2010
Publication date:
May 24, 2012
Applicant:
BIOPROJET
Inventors:
Marc Capet, Olivier Labeeuw, Isabelle Berrebi-Bertrand, Philippe Robert, Xavier Ligneau, Jeanne-Marie Lecomte, Jean-Charles Schwartz
Abstract: Medicament comprising, in a pharmaceutically acceptable vehicle, an anti-psychotic or an antidepressant (A), which, on its own, has an undesirable effect of a gain in body weight or sedation, and an antagonist and/or inverse agonist (B) of the histamine H3 receptor, the antagonist and/or inverse agonist of the histamine H3 receptor being present in a therapeutically effective amount for ensuring at least one of the following three effects: suppression or at least limitation of the undesirable effect of weight gain, suppression or limitation of the undesirable effect on alertness, epilepsy/convulsions, increase in the precognitive effect of the treatment. Use of such an antagonist or inverse agonist for the preparation of a medicament which is to ensure at least one of the said three effects in a patient treated by such an antipsychotic or antidepressant.
Abstract: The present patent application concerns compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.
Type:
Grant
Filed:
April 25, 2006
Date of Patent:
December 13, 2011
Assignee:
Bioprojet
Inventors:
Isabelle Bertrand, Marc Capet, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Olivia Poupardin-Olivier, Philippe Robert, Jean-Charles Schwartz, Olivier Labeeuw
Abstract: The present patent application concerns new compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a saturated nitrogen-containing ring, A is a saturated C1-4 alkylene and B a C3-4 alkylene or alkenylene chain; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.
Type:
Grant
Filed:
April 26, 2006
Date of Patent:
September 13, 2011
Assignee:
Bioprojet
Inventors:
Isabelle Bertrand, Marc Capet, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Olivia Poupardin-Olivier, Philippe Robert, Jean-Charles Schwartz
Abstract: Use of a compound of formula (A), wherein: W is a residue which imparts antagonistic and/or agonistic activity at histamine H3-receptors when attached to an imidazole ring in 4(5) position; R1 and R2 may be identical or different and represent each independently a lower alkyl or cycloalkyl, or taken together with the nitrogen atom to which they are attached, a saturated nitrogen-containing ring (i) as defined, a non-aromatic unsaturated nitrogen-containing ring (ii) as defined, a morpholino group, or a N-substituted piperazino group as defined for preparing medicaments acting as antagonists and/or agonists at the H3-receptors of histamine.
Type:
Grant
Filed:
July 3, 2006
Date of Patent:
March 22, 2011
Assignee:
Societe Civile Bioprojet
Inventors:
Jean-Charles Schwartz, Jean-Michel Arrang, Monique Garbarg, Jeanne-Marie Lecomte, Xavier Ligneau, Walter G. Schunack, Holger Stark, Charon Robin Ganellin, Fabien Leurquin, Sigurd Elz
Abstract: The invention relates to a combination of modafinil and at least one histamine H3 receptor antagonist or inverse agonist, which can be used in particular for the treatment of narcolepsy-cataplexy and more generally for disorders of sleep, wakefulness and vigilance.
Abstract: The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent having the property of being selective ligands for the dopamine D3 receptor. These selective D3 ligands are useful as medicines in neuropsychiatry, in particular in the treatment of psychotic or depressive states, or in the treatment of motor disorders, such as dyskinesia or essential tremor. They are furthermore useful in the treatment of dependency on nicotine, cocaine, alcohol, opioids and for facilitating withdrawal in drug-dependent individuals.
Type:
Grant
Filed:
October 19, 2005
Date of Patent:
October 7, 2008
Assignee:
Bioprojet
Inventors:
Marc Capet, Denis Danvy, Nicolas Levoin, Marcel Morvan, Isabelle Berrebi-Bertrand, Thierry Calmels, Philippe Robert, Jean-Charles Schwartz, Jeanne-Marie Lecomte
Abstract: Use of a compound of formula (A), wherein: W is a residue which imparts antagonistic and/or agonistic activity at histamine H3-receptors when attached to an imidazole ring in 4(5) position; R1 and R2 may be identical or different and represent each independently a lower alkyl or cycloalkyl, or taken together with the nitrogen atom to which they are attached, a saturated nitrogen-containing ring (i) as defined, a non-aromatic unsaturated nitrogen-containing ring (ii) as defined, a morpholino group, or a N-substituted piperazino group as defined for preparing medicaments acting as antagonists and/or agonists at the H3-receptors of histamine
Type:
Grant
Filed:
July 29, 1999
Date of Patent:
November 21, 2006
Assignee:
Societe Civile Bioprojet
Inventors:
Jean-Charles Schwartz, Monique Garbarg, Jeanne-Marie Lecounte, Xavier Ligneau, Walter G Schunacx, Hulger Stark, Charon Robin Ganellin, Fabien Leurquin, Sigurd Elz, Jean-Michel Arrang
Abstract: The invention relates to compounds which constitute a class of medicaments which have an anti-inflammatory activity and which act by inhibiting leukotriene A4 (LTA4), and enzyme which is responsible for the biosynthesis of leukotriene LTB4, a major proinflammatory mediator. The invention also relates to therapeutic anti-inflammatory, applications of these compounds as well as for methods of preparing these compounds.
Type:
Grant
Filed:
July 28, 2004
Date of Patent:
August 22, 2006
Assignee:
Institut National de la Santa et de la rescherche Medicale Bioprojet
Abstract: The invention concerns compounds inhibiting LTA4 hydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications.
Type:
Grant
Filed:
April 6, 2000
Date of Patent:
April 12, 2005
Assignees:
Institut National de la Sante et de la rescherche Medicale (INSERM), Bioprojet
Abstract: The instant invention relates to a process for preparing a compound of formula (I):
said process comprising a step (B) which consists in performing a Michael addition of a thioacid RS4H on to an &agr;-substituted acrylamide derivative.
Abstract: The invention concerns LTA4 hydrolase inhibiting compositions of formula (1) as set forth below. It also concerns their therapeutic, in particular anti-inflammatory, applications.
Type:
Grant
Filed:
June 11, 2001
Date of Patent:
August 20, 2002
Assignees:
Bioprojet, Institut National de la Sante et de la Recherche Medicale
(Inserm)
Abstract: The invention is relative to a compound of formula (I) and its use as an inhibitor of the CCK-inactivating peptidase tripeptidyl peptidase (TPP II). The invention concerns in particular the treatment of eating disorder, obesity, psychotic syndrome and associated psychiatric disorders. It concerns also the cosmetic use of a compound (I) in particular to aid slimming.
Type:
Grant
Filed:
September 18, 2000
Date of Patent:
January 1, 2002
Assignees:
Institut National de la Sante et de la Recherche Medicale
(INSERM), Bioprojet
Inventors:
Jean-Charles Schwartz, Rose Christiania, Froylan Vargas, Charon Robin Ganellin, Lihua Zhao, Samad Sanjeeda, Yondjun Chen
Abstract: Novel imidazole derivatives as histamine receptor H3 antagonists and/or agonists, preparation thereof and therapeutical uses thereof. Chemical compounds for use as histamine receptor H3 agonists, partial agonists or antagonists, having general formula (Ia) or (Ib), the use thereof for making drugs, and methods for revealing the agonist, partial agonist or antagonist activity of such compounds in vivo, are disclosed.
Type:
Grant
Filed:
January 9, 1997
Date of Patent:
June 19, 2001
Assignees:
Institut National de la Sante et de la Recherche
Medical, Societe Civile Bioprojet
Inventors:
Jean-Charles Schwartz, Jean-Michel Arrang, Monique Garbarg, Agnes Quemener, Jeanne-Marie Lecomte, Xavier Ligneau, Walter G. Schunack, Holger Stark, Katja Purand, Annette Huls, Reidemeister Sybille, Athmani Salah, Charon Robbin Ganellin, Nadia Pelloux-Leon, Wasyl Tertiux, Michael C. O. Krause, Sadek Bassem
Abstract: Process for the asymmetric synthesis of S-acyl derivatives of 2-mercaptomethyl-3-phenylpropanoic acid of formula (I): characterized in that it comprises the steps consisting in:a) preparing the diol (VI) by reduction of a malonic ester (V) in the presence of a hydride;b) preparing the monoacetates (VII R) or (VII S) respectively;c) subjecting these monoacetates to an oxidation in order to form the acids (IX S) or (IX R);d) saponifying the compounds (IX S) or (IX R) in order to form the hydroxy acids (X S) or (X R);e) thioacylating the hydroxy acids (X S) or (X R) with a mercapto acid R.sub.1 SH (XI), according to a Mitsunobu-type reaction, in order to lead to the desired acids (I R) (I S) respectively and application to the synthesis of N-(mercaptoacyl)amino acid derivatives (II).
Type:
Grant
Filed:
November 26, 1997
Date of Patent:
January 11, 2000
Assignee:
Societe Civile Bioprojet
Inventors:
Denis Danvy, Thierry Monteil, Pierre Duhamel, Lucette Duhamel, Jeanne-Marie Lecomte, Jean-Charles Schwartz, Nadine Noel-Lefebvre, Claude Gros, Jean-Christophe Plaquevent
Abstract: A compound selected from the group consisting of a compound of the formula
wherein the substituents are defined as in the specification having antagonist properties to histamine H3-receptors.
Type:
Grant
Filed:
April 6, 2000
Date of Patent:
July 31, 2001
Assignees:
Institut National del la Sante et de la Recherche
Medicale, Societe Civile Bioprojet
Inventors:
Jean-Charles Schwartz, Jean-Michel Arrang, Monique Garbarg, Jeanne-Marie Lecomte, Charon R. Ganellin, Abdellatif Fkyerat, Wasyl Tertiuk, Walter Schunack, Ralph Lipp, Holger Stark, Katja Purand