Abstract: The present invention relates to coumarins of the formula (I): that are useful as inhibitors of nitric oxide synthase. Pharmaceutical compositions and methods of using these compounds as inhibitors of nitric oxide synthase are described herein.
Type:
Grant
Filed:
August 24, 2004
Date of Patent:
May 26, 2009
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
Sharon Jackson, Thaddeus Nieduzak, Sam Rebello, Guyan Liang, Yulin Chiang, Jean Merrill
Abstract: This invention discloses and claims diary heterocycles of formula (I) and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and methods of using said compounds of formula (I) for the treatment or prevention of excessive weight or obesity, and for treatment of Type II diabetes, arteriosclerosis, high blood pressure, depression, anxiety, anxiety neuroses, and schizophrenia. Methods for treatment of excessive weight or obesity and for treatment of Type II diabetes with a mixture of a compound of formula I and antiobesity agents or appetite-regulating active ingredients, or with a mixture of a compound of formula I and antidiabetics or hypoglycemic active ingredients are also disclosed and claimed.
Type:
Grant
Filed:
July 24, 2003
Date of Patent:
November 28, 2006
Assignee:
Sanofi-Aventis Deutschland GmbH
Inventors:
Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Thomas Boehme, Gerhard Hessler, Gerard Rosse, Armin Walser
Abstract: Substituted thiophenes, processes for their preparation, their use as medicament or diagnostic agent. The substituted thiophene derivatives have the following backbone structure: Medicaments comprising compounds of this type are of use for preventing or treating various disorders, such as, respiratory disorders and snoring, acute and chronic disorders, disorders induced by ischemic and/or reperfusion events and by proliferative or fibrotic events, disorders of the central nervous system and lipid metabolism, diabetes, blood coagulation and infection by parasites.
Type:
Grant
Filed:
May 30, 2003
Date of Patent:
May 23, 2006
Assignee:
Sanofi-aventis Deutschland GmbH
Inventors:
Hans-Jochen Lang, Uwe Heinelt, Armin Hofmeister, Klaus Wirth, Michael Gekle, Markus Bleich
Abstract: The present invention relates to the combination of a CB1 receptor antagonist and of sibutramine, to the pharmaceutical compositions comprising them and to their use in the treatment of obesity.
Type:
Grant
Filed:
September 15, 2004
Date of Patent:
May 2, 2006
Assignee:
Aventis Pharma S.A.
Inventors:
Odile Piot-Grosjean, Philippe Picaut, François Petitet
Abstract: The invention relates to compounds of the formula (I) process for their preparation starting from the plant Beilschmiedia fulva, PLA 101037, and the use thereof for producing a medicament, in particular for the treatment of allergic disorders, of asthmatic disorders, of inflammatory concomitant symptoms of asthma and/or of diseases which can be treated by inhibiting c-maf and NFAT.
Type:
Grant
Filed:
July 25, 2003
Date of Patent:
March 28, 2006
Assignees:
Aventis Pharma Deutschland GmbH, Aventis Pharmaceuticals Inc.
Inventors:
Claudia Eder, Herbert Kogler, Sabine Haag-Richter
Abstract: The present invention relates to compounds of the formula (I): which are produced by the plant Garcinia punctata, chemical derivatives derived therefrom, a process for their preparation, and their use as pharmaceuticals, in particular for the treatment and/or prophylaxis of bacterial infectious diseases.
Type:
Grant
Filed:
July 31, 2003
Date of Patent:
October 18, 2005
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Matthias Schiell, Michael Kurz, Sabine Haag-Richter
Abstract: The invention relates to compounds of formula (I) in which R5 is chosen from the group consisting of: in which R2 is a C1-C3 alkyl group in which X may be Cl, Br, or F in which n is between 1 and 3, in the E or Z form, or a mixture of the two isomeric forms, possessing antimitotic, antiproliferative and antivascular properties through inhibition of the polymerization of tubulin into microtubules
Type:
Grant
Filed:
September 10, 2003
Date of Patent:
August 16, 2005
Assignee:
Aventis Pharma S. A.
Inventors:
Cécile Combeau, Patrick Mailliet, Marielle Chiron
Abstract: The present invention relates to an efficient process for preparing derivatives of 1-(pyridinyl)-1,1-dialkoxy-2-aminoethane of the formula (I), with which compounds of the formula (I) can be prepared in high purity and yield and in the form of the free base without isolating the acetylpyridine oxime of the formula (XI) which is a critical product from a safety point of view as a solid.
Type:
Grant
Filed:
January 26, 2004
Date of Patent:
July 12, 2005
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Hans-Wolfram Flemming, Gerhard Korb, Juergen Mueller-Lehar, Walter Weber
Abstract: The present invention provides various processes for the preparation of (R)-&agr;-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol.
Type:
Grant
Filed:
January 11, 2002
Date of Patent:
March 30, 2004
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
Edward D. Daugs, Jonathan C. Evans, Hans-Wolfram Flemming, Thomas Heinz Eduard Hilpert, Johannes Nicolaas Koek, Frederick M. Laskovics, Sandra K. Stolz-Dunn, Ian A. Tomlinson
Abstract: This invention relates to compounds which are inhibitors of elastase, particularly human neutrophil elastase. The inhibitors are short, synthetic peptides in which the P2 moiety is substituted with various nitrogen-containing heterocyclic groups. As inhibitors of human neutrophil elastase, the compounds are useful in the treatment of a patient afflicted with a neutrophil associated inflammatory disease.
Type:
Grant
Filed:
December 20, 2000
Date of Patent:
February 17, 2004
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
Steven L. Gallion, William A. Metz Jr., Joseph P. Burkhart, Michael R. Angelastro, Norton P. Peet
Abstract: The present invention comprises 6-9-Disubstituted 2-[trans-(4-aminocyclohexyl]aminopurines that are useful in inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms.
Type:
Grant
Filed:
June 24, 2002
Date of Patent:
November 4, 2003
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
Jennifer A. Dumont, Alan J. Bitonti, David R. Borcherding, Norton P. Peet, H. Randall Munson, Jr., Patrick W. Shum
Abstract: Novel aminoalkylphenols, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the aminoalkylphenols or compositions thereof are disclosed.
Type:
Grant
Filed:
December 10, 1999
Date of Patent:
November 12, 2002
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
Raymond W. Kosley, Jr., Mark G. Palermo, Stephen J. Shimshock, Veronica Wolf
Abstract: The present invention provides novel compounds of the formula (I)
wherein
R is selected from the group consisting of R2, R2NH—, or R3R4N—R5- wherein
R2 is selected from the group consisting of C9-C12 alkyl,
Z is selected from the group consisting of phenyl, heterocycle, cycloalkyl, and naphthanlene; and M is selected from the group consisting of hydrogen, C1-C4 alkyl, and
wherein each C9-C12 alkyl or Z is optionally substituted with 1 to 3 substituents, which may be the same or different, and which are selected from the group consisting of D, E,
wherein each D is independently selected from the group consisting of trifluoromethyl, trifluoromethoxy, and C1-C4 alkoxy; each E is independently selected from the group consisting of Hal, OH, and C1-C8 alkyl;
R3 and R4 are selected from the group consisting of hydrogen, C1-C4 alkyl and (CH2)y-phenyl, wherein y is an integer 0-8, with the proviso that R3 and R4 not both be hydrogen
Type:
Grant
Filed:
February 9, 1999
Date of Patent:
November 12, 2002
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
Jennifer A. Dumont, Alan J. Bitonti, David R. Borcherding, Norton P. Peet, H. Randall Munson, Jr., Patrick W. Shum
Abstract: Novel [[(aminocarbonyloxy)-1-indan]-2-yl]methylpiperidines of the formula
wherein R is hydrogen, loweralkyl, or a group of the formula
R1 is hydrogen or a group of the formula
W, X and Y are hydrogen, loweralkyl, loweralkoxy, halogen, nitrogen, or trifluoromethyl; n is 1 or 2; the pharmaceutically acceptable acid addition salts thereof intermediates of the formula
and process for the preparation thereof, and a method of relieving memory dysfunction, employing compounds and compositions thereof are disclosed.
Type:
Grant
Filed:
May 8, 1995
Date of Patent:
July 2, 2002
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
Raymond W. Kosley, Jr., Bettina Spahl, Richard C. Effland