Abstract: The present invention provides compounds according to formula I and formula II and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity.
Type:
Grant
Filed:
December 11, 2002
Date of Patent:
May 11, 2004
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Norman Kong, Emily Aijun Liu, Binh Thanh Vu
Abstract: A compound of the formula
Compounds of formula I have a good affinity to the A2A receptor and are useful for the treatment of diseases mediated by this receptor.
Abstract: The present invention provides a thermodynamically stable modification of (±)1-(4-carbazolyloxy)-3-[2-(2-methoxyphenoxy)ethylamino]-2-propanole and pharmacologically acceptable salts or optically active forms thereof as well as processes for their preparation and pharmaceutical compositions containing one or more of them.
Abstract: A compound of formula I and a method of treatment of diseases, related to modulation of the adenosine A2 receptor system comprising administering a compound of formula
to a person in need of such treatment.
Type:
Grant
Filed:
December 3, 2002
Date of Patent:
April 27, 2004
Assignee:
Hoffman-La Roche Inc.
Inventors:
Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
Abstract: A pharmaceutical composition for oral administration of an active compound having a bioavailability of 20% or less. The composition comprises, based on its total weight, from 0.01% to about 15% (w/w) of said active compound molecularly dissolved in the composition, from 30 to 80% (w/w) of an edible lipid matrix and from 1 to 20% (w/w) of an edible emulsifier, the ratio between the dose weight of the active compound and its solubility in the composition being equal to or greater than 0.6 ml. The high percentage of fat (30-80%) enables a considerable increase the amount of the drug that is molecularly dispersed in the dosage form, thus allowing a significant reduction in the number of unit doses that must be taken daily-by patients.
Abstract: The present invention pertains to derivatives of 5,5-disubstituted pyrimidine-2,4,6,-trianones having the formula:
wherein R1, R2, R3, and R4 are described herein. These compounds have antitumor and antimetastatic activity.
Type:
Grant
Filed:
February 25, 2002
Date of Patent:
April 6, 2004
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Dagmar Geppert, Frank Grams, Hans-Willi Krell, Herbert Leinert, Ernesto Menta, Gerd Zimmermann
Abstract: The present invention relates to compounds of the formula
wherein R1, R2 and R3 are as described herewithin. The compounds of formula I have been found to be adenosine receptor ligands. Specifically, the compounds of the present invention have a good affinity to the A2A-receptor and they are therefore useful in the treatment of diseases, related to this receptor.
Type:
Grant
Filed:
December 2, 2002
Date of Patent:
March 30, 2004
Assignee:
Hoffman-La Roche Inc.
Inventors:
Alexander Flohr, Roland Jakob-Roetne, Roger David Norcross, Claus Riemer
Abstract: A pharmaceutical composition comprising 250-20,000 U of an EPO preparation and 5-20 mg of a Fe(III) complex is disclosed. This pharmaceutical composition is useful in treating anaemias as well or as haemodialysis patients.
Abstract: This invention relates to a compound and the use of the compound of the formula
wherein R1, R2, R3, R4 and R5 are as defined in the description, A signifies —CH═CH— or —C≡C—; and B signifies
wherein R6 to R26, X and Y are as defined in the specification or a pharmaceutically acceptable salt thereof, for use in pharmaceutical compositions for the treatment or prevention of mGluR5 receptor mediated disorders.
Type:
Grant
Filed:
November 28, 2001
Date of Patent:
March 16, 2004
Assignee:
Hoffman-La Roche Inc.
Inventors:
Vincent Mutel, Jens-Uwe Peters, Juergen Wichmann
Abstract: The present application relates to compounds of the formula
wherein
R1 is hydrogen, halogen or lower alkoxy;
R2 is hydrogen or is —C(O)-lower alkyl or —C(O)-phenyl, wherein the phenyl ring is unsubstituted or substituted by one or two substituents selected from the group consisting of halogen, lower alkyl, lower alkoxy and trifluoromethyl, or is —C(O)-furanyl or —C(O)-thiophenyl, wherein the rings are unsubstituted or substituted by halogen;
or a pharmaceutically acceptable salt thereof. The compounds are useful in the treatment of diseases associated with the adenosine A2 receptor.
Type:
Grant
Filed:
September 18, 2002
Date of Patent:
February 17, 2004
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Matthias Heinrich Nettekoven, Sebastien Schmitt
Abstract: The present invention relates to a rapid and readily reproducible process for stabilizing biologically active substances by combining the biologically active substance witha a stabilizingmixture and drying the resulting mixture into a dry, amorphous product by means of convection drying. The invention also relates to the amorphous, microscopically homogeneous products which are obtained by this process, are in the form of powders and have a uniform geometric, in particular spherical, shape. The invention furthermore relates to the use of substance mixtures for stabilizing biologically active material, in particular proteins by means of spray drying.
Type:
Grant
Filed:
November 3, 1998
Date of Patent:
February 10, 2004
Assignee:
Boehringer Mannheim GmbH
Inventors:
Rolf-Dieter Gabel, Markus Mattern, Gerhard Winter, Alexander Wirl, Heinrich Woog
Abstract: A compound of formula
wherein
R1 is —NR′R″, wherein R′ and R″ are independently selected from the group consisting of lower alkyl, —(CH2)n—C(O)NRaRb, —(CH2)n,-heteroaryl, —(CH2)n-aryl, —(CH2)n—CN, —(CH2)n—O-lower alkyl or —(CH2)n-cycloalkyl, or R′ and R″ form together with the N-atom a five or six-membered non-aromatic ring, containing no or one additional heteroatom selected from the group consiting of
O and S, and said ring being unsubstituted or substituted by one or two substituents, selected from the group consisting of lower alkyl, —C(O)NRaRb and —(CH2)n—O-lower alkyl, and RaRb are independently from each other hydrogen or lower alkyl;
R2 is aryl or heteroaryl, unsubstituted or substituted by lower alkyl or halogen; and
n is 0, 1, 2 or 3;
or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
October 7, 2002
Date of Patent:
February 10, 2004
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Matthias Heinrich Nettekoven, Sebastien Schmitt
Abstract: The present invention relates to a medical device adhering to the skin comprising a housing with a rigid base fixable on a patient's skin by means of an adhesive layer which has an adhesive surface, essentially co-extensive with the base, contacting the skin and which is fixed to the base by a reduced surface in comparison to the adhesive surface contacting the skin.
Abstract: The present invention is a compound of formula
wherein
R1 is halogen or lower alkyl;
R2 is hydrogen, lower alkyl, cycloalkyl, —(CH2)m-phenyl, wherein the phenyl ring may be substituted by lower alkoxy, or is —(CH2)m-indolyl;
R3 is —C(O)O-lower alkyl, —C(O)OH, or a five membered heteroaromatic group, which rings may be substituted by lower alkyl or cycloalkyl;
n is 0, 1 or 2;
m is 0, 1 or 2;
or a pharmaceutically acceptable acid addition salt thereof. Compound I shows high affinity and selectivity for GALA A &agr;5 receptor binding sites.
Type:
Grant
Filed:
April 9, 2002
Date of Patent:
February 3, 2004
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Raffaello Masciadri, Andrew William Thomas, Juergen Wichmann
Abstract: The present invention relates to compounds of formula (I)
wherein U, Y, V, W, L, X, A1, A2, A3, A4, A5 and A6 are as defined in the description and claims 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, parasite infections, gallstones, tumors and/or hyperproliferative disorders, and/or treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
Type:
Grant
Filed:
July 16, 2001
Date of Patent:
January 27, 2004
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Jean Ackermann, Johannes Aebi, Alexander Chucholowski, Henrietta Dehmlow, Olivier Morand, Sabine Wallbaum, Thomas Weller
Abstract: Novel imidazole derivatives are disclosed. These compounds have a good affinity to the NMDA (N-methyl-D-aspartate)-receptor subtype selective blockers, which have a key function in modulating neuronal activity and plasticity which makes them key players in mediating processes underlying development of CNS as well as learning and memory formation. These compounds are useful in the control or treatment of diseases mediated by this receptor.
Type:
Grant
Filed:
February 11, 2003
Date of Patent:
January 27, 2004
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard, Rene Wyler
Abstract: The invention relates to use of ibandronic acid (1-hydroxy-3-(N-methyl-N-pentyl)aminopropyl-1,1-diphosphonic acid) or physiologically compatible salts or esters thereof for improving the osseointegration of cement-free anchored endoprostheses. Ibandronate or salts thereof is applied for a short time immediately after insertion of an endoprosthesis, with the surprising result that secondary stability of the implant is obtained in only 5 weeks or less after the operation.
Abstract: Novel polycyclic compounds of the formula [I],
wherein R1, R2, R3, R4, R5, R6, R7, ring A, ring B, X, Y and Z are as defined herein and the pharmaceutically acceptable salts thereof. These compounds have antitumor activity and useful for the treatment of cancer.
Abstract: The invention is concerned with a pharmaceutical preparation for subcutaneous, parenteral administration, which contains bisphosphonic acids or their salts as the active substance, as well as the production of this preparation. By means of the preparation in accordance with the invention it is possible to administer locally relatively high concentrations of bisphosphonates without the occurrence of incompatibilities.
Type:
Grant
Filed:
May 3, 2001
Date of Patent:
January 13, 2004
Assignee:
Hoffman-La Roche Inc.
Inventors:
Rainer Bader, Petra Bastian, Achim Goepferich, Wolfgang Roedel, Gerhard Winter