Abstract: The present invention is a series of novel compounds of formula I and a method of treatment or prevention of a mGluR5 receptor mediated disease by administering an therapeutically effective amount of a compound formula
wherein R1 and R2 are selected from hydrogen, (C1-6)-alkyl, halogen, hydroxy, (C1-6)-alkoxy and A is defined the description, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
March 8, 2002
Date of Patent:
July 22, 2003
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Vincent Mutel, Jens-Uwe Peters, Juergen Wichmann
Abstract: The present invention is a series of compounds that are derivatives of 1-sulfonyl-pyrrolidine and that demonstrate affinity towards metabotropic glutamate receptors. The invention further relates to medicaments containing these compounds and to a process for their preparation. The compounds possess affinity towards metabotropic glutamate receptors and are therefore useful in the treatment or prevention of acute and/or chronic neurological disorders.
Abstract: The invention relates to compounds which are represented by the formula
wherein R1, R2, R3, R4, X and Y are as defined in the specification, as well as pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing these compounds and to a process for their preparation. The compounds possess affinity towards metabotropic glutamate receptors and are therefore useful in the treatment or prevention of acute and/or chronic neurological disorders.
Type:
Grant
Filed:
December 12, 2001
Date of Patent:
July 1, 2003
Assignee:
Hoffman-La Roche Inc.
Inventors:
Alfred Binggeli, Hans-Peter Maerki, Vincent Mutel, Maurice Wilhelm, Wolfgang Wostl
Abstract: Disclosed are cephalosporin derivatives of the general formula
wherein R is an organic residue with a molecular weight not exceeding 400 bonded to the adjacent sulphur atom via carbon and consisting of carbon, hydrogen, and optional oxygen, sulfur, nitrogen and/or halogen atoms; R1 is hydrogen, lower alkyl or phenyl; and A is a secondary, tertiary or quaternary nitrogen atom bound directly to the propenyl group and being substituted by an organic residue with a molecular weight not exceeding 400 and consisting of carbon, hydrogen, and optional oxygen, sulfur, nitrogen and/or halogen atoms,
as well as readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts.
Type:
Grant
Filed:
June 22, 1999
Date of Patent:
June 24, 2003
Assignee:
Basilea Pharmaceutica AG
Inventors:
Peter Angehrn, Erwin Götschi, Ingrid Heinze-Krauss, Hans G. F. Richter
Abstract: The present invention relates to compositions containing lipase inhibitors, e.g. orlistat, and the use of such compositions for treating, reducing or preventing functional dyspepsiaafter ingestion of meals, especially of fat containing or fat rich meals.
Type:
Grant
Filed:
August 6, 2001
Date of Patent:
March 18, 2003
Assignee:
Hoffman-La Roche Inc.
Inventors:
Christine Feinle, Michael Fried, Hans Lengsfeld, Thomas Rades
Abstract: The present invention is concerned with a novel process for the preparation of compounds of formula I
comprising bromomethylation or chloromethylation of a compound of formula II
and subsequent reaction with a compound of formula IV
The compounds of formula I and the corresponding salts, e.g. the sodium salts, are pharmaceutically active substances.
Abstract: Compounds of the formula:
wherein R1 to R7 and Y are as defined in the specification, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof, are useful for treating diseases associated with cystein proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.
Type:
Grant
Filed:
December 21, 2000
Date of Patent:
March 11, 2003
Assignee:
Hoffman-La Roche Inc.
Inventors:
Tobias Gabriel, Michael Pech, Sabine Wallbaum
Abstract: The compounds of formula (I)
wherein R1 has the significance as given in the description, are inhibitors of endothelin receptors and can therefore be used for the treatment of disorders which are associated with abnormal vascular tone and endothelial dysfunction.
Type:
Grant
Filed:
March 8, 2002
Date of Patent:
February 18, 2003
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Volker Breu, Philippe Coassolo, Werner Neidhart, Sébastien Roux, Peter Weiss