Abstract: Quinoline derivatives are useful as neuropeptide Y (NPY) receptor ligands and are particularly effective as neuropeptide Y (NPY) antagonists. These compounds are useful in pharmaceutical preparations for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders, or obesity.
Type:
Grant
Filed:
May 20, 2002
Date of Patent:
November 16, 2004
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Werner Mueller, Werner Neidhart, Philippe Pflieger, Jean-Marc Plancher
Abstract: The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.
Type:
Grant
Filed:
February 25, 2003
Date of Patent:
September 14, 2004
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Johannes Aebi, Daniel Bur, Alexander Chucholowski, Henrietta Dehmlow, Eric Argirios Kitas, Ulrike Obst, Hans Peter Wessel
Abstract: A process for the preparation heterocyclic indene analogs, especially with the preparation of 4-hydroxycarbazole or N-protected 4-hydroxycarbazole, involves cyclocarbonylation followed by saponification. This process avoids high temperatures and high catalyst loadings.
Type:
Grant
Filed:
January 22, 2002
Date of Patent:
August 17, 2004
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Michelangelo Scalone, Thomas Albert Zeibig
Abstract: A pharmaceutical combination or composition containing a lipase inhibitor, preferably orlistat, and a bile acid sequestrant is useful for treating obesity.
Type:
Grant
Filed:
July 25, 2001
Date of Patent:
June 29, 2004
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Pierre Barbier, Paul Hadvary, Hans Lengsfeld
Abstract: The present invention relates to pharmaceutical compositions that contain a solid pharmaceutically active compound having a melting point ≧37° C. and a fatty acid or a fatty acid salt or a mixture of a fatty acid and a fatty acid salt. Such composition results in a depression in melting point to ≦37° C. upon contact with an aqueous solution thereby providing an improved outlook for absorption.
Type:
Grant
Filed:
May 23, 2002
Date of Patent:
May 4, 2004
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Karsten Maeder, Lukas Christoph Scheibler, Hans Steffen
Abstract: The present invention relates to novel dihydroindole and tetrahydroquinoline derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
Type:
Grant
Filed:
December 11, 2001
Date of Patent:
March 16, 2004
Assignee:
Hoffman-La Roche Inc.
Inventors:
Johannes Aebi, Jean Ackermann, Alexander Chucholowski, Henrietta Dehmlow, Olivier Morand, Sabine Wallbaum, Thomas Weller, Narendra Panday
Abstract: A pharmaceutical composition contains at least one inhibitor of lipases and at least one fatty acid ester of polyol. In this composition, the fatty acid ester has a melting point above the body temperature and the polyols are chosen from the group consisting of sugars, sugar derivatives, and mixtures thereof.
Type:
Grant
Filed:
September 13, 2000
Date of Patent:
March 9, 2004
Assignee:
Hoffman-La Roche Inc.
Inventors:
Passchier Christiaan de Smidt, Paul Hadvary, Hans Lengsfeld, Marcel Schmid, Donald MacFarland Small, Hans Steffen, Joseph Tardio
Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula:
wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
Type:
Grant
Filed:
October 4, 2002
Date of Patent:
January 27, 2004
Assignee:
Hoffman-La Roche Inc.
Inventors:
Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans Peter Wessel
Abstract: The combination of erythropoietin and calcium, with or without phosphates, is useful for treating haemochromatoses. A method for treating primary haemochromatoses in a patient involves administering to the patient a combination therapy including an erythropoietin preparation and a calcium preparation, where the erythropoietin preparation and the calcium preparation are each administered from 1 to 5 times weekly. Beneficially, this combination therapy further administers a phosphorus preparation.
Abstract: The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.
Type:
Grant
Filed:
July 17, 2001
Date of Patent:
December 9, 2003
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Johannes Aebi, Daniel Bur, Alexander Chucholowski, Henrietta Dehmlow
Abstract: Pyrimidine derivatives have been found to be useful as neuropeptide Y receptor ligands and particularly as antagonists. These pyrimidine derivatives may be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, diabetes, eating disorders, and obesity.
Type:
Grant
Filed:
November 8, 2001
Date of Patent:
December 2, 2003
Assignee:
Hoffman-La Roche Inc.
Inventors:
Volker Breu, Frank Dautzenberg, Patrizio Mattei, Werner Neidhart, Philippe Pflieger
Abstract: The invention is concerned with water soluble N-(4-carbamimidoyl-phenyl)-glycine derivatives of formula (I)
wherein R1 to R4 and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.
Type:
Grant
Filed:
January 24, 2003
Date of Patent:
November 4, 2003
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Leo Alig, Katrin Groebke Zbinden, Ulrike Obst
Abstract: Retinoids with retinoid receptor antagonistic activity, pharmaceutically acceptable salts and pharmaceutically acceptable hydrolyzable esters thereof, have been found efficacious in treating T-helper cell type 2 (Th2)-mediated immune diseases, such as immunoglobulin E (IgE)-mediated allergic diseases.
Type:
Grant
Filed:
August 3, 2000
Date of Patent:
August 26, 2003
Assignee:
Hoffman-La Roche Inc.
Inventors:
Werner Bollag, Michael Klaus, Paola Panina-Bordignon, Francesco Sinigaglia
Abstract: Compounds of the formula
wherein R1 is a residue of the formula
and R2-R10 have the significance given in the specification can be used as pharmaceuticals, particularly for the repair of photodamaged skin, other dermatological conditions, and oncological indications.
Abstract: A process for producing a compound of the formula:
where Ph is phenyl, X1 and X2 are both hydrogen or X1 and X2 taken together are CH2, R1 is a protecting group, R2 is fluorine, hydrogen, or OR3, where R3 is a protecting group, and the squiggly line represents a bond that results in the adjacent double bond being in either the E or Z configuration, involves:
(a) chlorinating a compound of the formula:
where X1, X2, R1, R2, and the squiggly line are as above, using triphosgene in the presence of an organic base to obtain the compound of the formula:
where X1, X2, R1, R2, and the squiggly line are as above; and
(b) reacting the compound of formula 3 with a salt of diphenyl phosphine oxide to obtain the compound of formula 1. Each of the above steps (a) and (b) are individually useful.
Abstract: A method prevents or treats diseases associated with high plasma cholesterol levels. In addition, this method reduces plasma cholesterol levels. The method comprises administering a lipase inhibitor, e.g. orlistat, and a pharmaceutically acceptable bile acid sequestrant.
Type:
Grant
Filed:
July 25, 2001
Date of Patent:
May 13, 2003
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Paul Hadvary, Hans Lengsfeld, Hans Steffen
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: A method for the preparation of compositions, preferably pharmaceutical compositions, in form of expanded, mechanically stable, lamellar, porous, sponge-like or foam structures out of solutions and dispersions results in a favored pharmaceutical product. This method comprises the steps of a) preparing a solution or a homogeneous dispersion of a liquid and a compound selected from the group consisting of one or more pharmaceutically active compounds, one or more pharmaceutically suitable excipients, and mixtures thereof, followed by b) the expansion of the solution or the homogeneous dispersion without boiling.
Abstract: New compounds have the formula:
wherein R, R1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.
Type:
Grant
Filed:
August 10, 2000
Date of Patent:
January 28, 2003
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger David Norcross