Abstract: The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1—R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B is CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description.
Type:
Grant
Filed:
October 11, 2006
Date of Patent:
May 11, 2010
Assignee:
sanofi-aventis Deutschland GmbH
Inventors:
Hartmut Strobel, Paulus Wohlfart, Alena Safarova, Armin Walser, Teri Suzuki, Karl Schoenafinger, Ramalinga M. Dharanipragada
Abstract: The invention relates to a dose of 2.5 mg of the pentasaccharide methyl O-(2,3,4-tri-O-methyl-6-O-sulfo-?-D-glucopyranosyl)-(1?4)-O-(2,3-di-O-methyl-?-D-glucopyranosyl uronic acid)-(1?4)-O-(2,3,6-tri-O-sulfo-?-D-glucopyranosyl)-(1?4)-O-(2,3-di-O-methyl-?-L-idopyranosyl uronic acid)-(1?4)-2,3,6-tri-O-sulfo-?-D-glucopyranoside or a pharmaceutically acceptable salt thereof for use in therapy, in particular for the treatment of venous thromboembolic events in patients with deep venous thrombosis.
Abstract: The present invention is directed to dihydrogen phosphate salt 2-(3-{6-[2-(2,4-dichloro-phenyl)-ethylamino]-2-methoxy-pyrimidin-4-yl}-phenyl)-2-methyl-propionic acid of Formula (III), a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of Formula (III), and a pharmaceutically acceptable carrier; and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obs
Type:
Grant
Filed:
April 11, 2008
Date of Patent:
January 5, 2010
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
Beverly Langevin, Edward Orton, Daniel Sherer
Abstract: This invention is directed to oxoazaheterocycyl compounds which inhibit Factor Xa, to oxoazaheterocycyl compounds which inhibit both Factor Xa and Factor IIa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds, to a method of directly inhibiting Factor Xa and to a method of simultaneously directly inhibiting Factor Xa and Factor IIa.
Type:
Grant
Filed:
July 25, 2003
Date of Patent:
November 3, 2009
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
William R. Ewing, Michael R. Becker, Yong Mi Choi-Sledeski, Heinz W. Pauls, Wei He, Stephen M. Condon, Roderick S. Davis, Barbara A. Hanney, Alfred P. Spada, Christopher J. Burns, John Z. Jiang, Michael R. Myers, Wan F. Lau, Aiwen Li, Gregory B. Poli, Mark A. Bobko, Robert L. Morris, Joseph M. Karpinski, Timothy F. Gallagher, Kent W. Neuenschwander, Robert D. Groneberg, Jean-Francois Sabuco
Abstract: The present invention relates to a method for analyzing oligosaccharides constituting the heparins of low molecular weight and the heparins of very low molecular weight from blood plasma.
Abstract: The present invention relates compounds of the formula A oligosaccharide-spacer-GpIIb/IIIa antagonist ??(A). The compounds of the invention have antithrombotic activity and can be used in treating or preventing thrombotic diseases.
Type:
Grant
Filed:
August 31, 2006
Date of Patent:
August 18, 2009
Assignee:
sanofi-aventis
Inventors:
Rogier Christian Buijsman, Martin De Kort, Dirk Gerrit Meuleman, Constant Van Boeckel
Abstract: The invention is directed to a compound of formula I, wherein R, R1, R2, R3 and R4 are as defined herein, or a pharmaceutically acceptable salt thereof, and its pharmaceutically composition, preparation and uses as an inhibitor of FGFs (fibroblast growth factors).
Abstract: The present invention is directed to a compound of Formula (I) wherein Cy1, Cy2, L1, L2, and R1 are as defined herein, a pharmaceutical composition comprising a pharmaceutically effective amount of one or more compounds according to Formula (I) in admixture with a pharmaceutically acceptable carrier, and a method of treating a patient suffering from a PGD2-mediated disorder including, but not limited to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischem
Abstract: Compounds of the formula I, in which R(1), R(2), R(3), R(4), R(5), R(6), R(7), R(8), R(30) and R(31) have the meanings indicated in the claims, are very particularly suitable as novel and antiarrythmic active compounds, in particular for the treatment and prophylaxis of atrial arrythmias, e.g. atrial fibrillation (AF), or atrial flutter.
Type:
Grant
Filed:
October 24, 2003
Date of Patent:
April 7, 2009
Assignee:
Sanofi-Aventis Deutschland GmbH
Inventors:
Joachim Brendel, Wolfgang Schmidt, Peter Below
Abstract: Compound corresponding to general formula (I): in which, R1 represents a hydrogen or halogen atom, an NH2, NHR2, NHCOR2, NO2, CN, CH2NH2 and CH2NHR2; or alternatively R1 represents an optionally substituted phenyl or an optionally substituted heteroaromatic group; Ar represents an optionally substituted phenyl group or an optionally substituted heteroaromatic group; n represents 0, 1, 2 or 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. Application in therapy.
Type:
Grant
Filed:
April 1, 2005
Date of Patent:
January 27, 2009
Assignee:
sanofi-aventis
Inventors:
Hugues D'Orchymont, Luc Van Hijfte, Andre Zimmermann
Abstract: The present invention relates to compounds of the formulae I and Ia, wherein R0; R1; R3; R4; R22, Q; V, G and M have the meanings indicated in the claims. The compounds of the formulae I and Ia are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formulae I and Ia, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
Type:
Grant
Filed:
August 25, 2006
Date of Patent:
December 16, 2008
Assignee:
SANOFI-AVENTIS Deutschland GmbH
Inventors:
Armin Bauer, Michael Wagner, Marc Nazare, Volkmar Wehner, Matthias Urmann, Hans Matter
Abstract: The invention is directed to a compound of the formula I wherein the variables are as defined herein, or a stereoisomeric form thereof, mixture of stereoisomeric forms, in any ratio, or a salt thereof. Another aspect of the present invention is directed to a pharmaceutical composition comprising, a pharmaceutically effective amount of one or more compounds of formula I according to claim 1 in admixture with a pharmaceutically acceptable carrier.
Type:
Grant
Filed:
July 31, 2006
Date of Patent:
July 15, 2008
Assignee:
SANOFI-AVENTIS Deutschland GmbH
Inventors:
Manfred Schudok, Hans Matter, Armin Hofmeister, Maxime Lampilas
Abstract: The present invention is related to a process for preparing anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).
Type:
Grant
Filed:
November 9, 2006
Date of Patent:
February 19, 2008
Assignee:
SANOFI-AVENTIS Deutschland GmbH
Inventors:
Joachim Brendel, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
Abstract: This invention is directed to physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; and N-oxides thereof, and pharmaceutically acceptable salts of the compounds of formula (I) and N-oxides thereof, Such compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmnaceutical compositions comprising compoundS of formula (I), their phatmaceUtical use and methods for their preparation.
Type:
Grant
Filed:
September 1, 2004
Date of Patent:
February 12, 2008
Assignee:
Aventis Pharma Limited
Inventors:
Paul Joseph Cox, Shelley Bower, David John Aldous, Peter Charles Astles, Daniel Gerard McGarry, Christopher Hulme, John Robinson Regan, Fu-Chih Huang, Stevan Wakefield Djuric, Kevin Joseph Moriarty, Rose Mappilakunnel Mathew, Gregory Bernard Poli
Abstract: The present invention is related to anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).
Type:
Grant
Filed:
April 26, 2002
Date of Patent:
June 26, 2007
Assignee:
Sanofi-Aventis Deutschland GmbH
Inventors:
Joachim Brendel, Bernard Pirard, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
Abstract: The present invention relates to processes for preparing certain piperidine derivatives, including fexofenadine (F), the active ingredient in the non-sedating antihistamine sold in the U.S. under the designation “Allegra®”. This invention also relates to novel synthetic intermediates useful in the processes of the present invention.
Type:
Grant
Filed:
April 22, 2004
Date of Patent:
June 26, 2007
Assignee:
Sanofi-Aventis Deutschland GmbH
Inventors:
Collin H. Schroeder, Ryan R. Huddleston, Richard H. Charles
Abstract: The present invention is directed to a compound of formula (I), or a stereoisomer or a mixture of stereoisomer thereof in any ratio, or its physiologically tolerable salt, which is useful as an inhibitor of matrix metalloproteinase. The present invention is also directed to a pharmaceutical preparation comprising a pharmaceutically effective amount of at least one compound of formula (I); processes for their preparation; the use of a compound of formula (I) having activity as an matrix metalloproteinase inhibitor; and for the prophylaxis and therapy of disease states that involve an increase in the activity of matrix metalloproteinase.
Type:
Grant
Filed:
September 27, 2004
Date of Patent:
April 17, 2007
Assignee:
Sanofi-Aventis Deutschland GmbH
Inventors:
Manfred Schudok, Hans Matter, Armin Hofmeister
Abstract: The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1–R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1–C3-alkyl), B is CH2 or CH—(C1–C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description.
Type:
Grant
Filed:
February 13, 2002
Date of Patent:
February 20, 2007
Assignee:
Sanofi-Aventis Deutschland GmbH
Inventors:
Hartmut Strobel, Paulus Wohlfart, Alena Safarova, Armin Walser, Teri Suzuki, Karl Schönafinger