Abstract: The present invention is concerned with isoxazol-4-yl-oxadiazole derivatives of formula wherein R1, R2, and R3, are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has high affinity and selectivity for GABA A ?5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
Type:
Grant
Filed:
April 13, 2009
Date of Patent:
June 7, 2011
Assignee:
Hoffman-La Roche Inc.
Inventors:
Bernd Buettelmann, Bo Han, Henner Knust, Andreas Koblet, Andrew Thomas
Abstract: The present invention relates to novel pyridine-2-carboxyamide derivatives of formula (I) useful as metabotropic glutamate receptor antagonists: wherein Y, Z, R1, R2 and R3 are as defined in the specification herein.
Type:
Grant
Filed:
January 30, 2007
Date of Patent:
May 31, 2011
Assignee:
Hoffman-La Roche Inc.
Inventors:
Georg Jaeschke, Will Spooren, Eric Vieira
Abstract: This invention is concerned with compounds of the formula wherein A, R1 to R5 are as defined in the specification and G is a pyridine, quinoline or pyrimidine group as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
Type:
Grant
Filed:
August 30, 2007
Date of Patent:
May 10, 2011
Assignee:
Hoffman-La Roche Inc.
Inventors:
Andreas D. Christ, Rainer E. Martin, Peter Mohr
Abstract: The present invention provides compounds of the general formula (I), having affinity and selectivity for the dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the therapeutic and/or prophylactic treatment of cognitive disorders.
Type:
Grant
Filed:
September 16, 2009
Date of Patent:
May 10, 2011
Assignee:
Hoffman-La Roche Inc.
Inventors:
Luca Gobbi, Georg Jaeschke, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
Abstract: The invention is concerned with novel imidazole derivatives of formula (I), wherein m, E, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.
Type:
Grant
Filed:
June 25, 2008
Date of Patent:
May 3, 2011
Assignee:
Hoffman-La Roche Inc.
Inventors:
Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
Abstract: There are provided compounds of the formula wherein R1, R2, R3, X, ring A and ring B are as described. The compounds exhibit anticancer properties.
Type:
Grant
Filed:
June 18, 2007
Date of Patent:
April 26, 2011
Assignee:
Hoffman-La Roche Inc.
Inventors:
Yi Chen, Kin-Chun Luk, Pamela Loreen Rossman, Sung-Sau So
Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Type:
Grant
Filed:
March 30, 2009
Date of Patent:
April 19, 2011
Assignees:
Genentech, Inc., Hoffman-La Roche Inc.
Inventors:
Steven Do, Richard Goldsmith, Tim Heffron, Aleksandr Kolesnikov, Steven Staben, Alan G. Olivero, Michael Siu, Daniel P. Sutherlin, Bing-Yan Zhu, Paul Goldsmith, Tracy Bayliss, Adrian Folkes, Neil Pegg
Abstract: The present invention is directed to a combination therapy involving a type II anti-CD20 antibody and an anti-Bcl-2 active agent for the treatment of a patient suffering from cancer, particularly a CD20-expressing cancer. An aspect of the invention is a composition comprising a type II anti-CD20 antibody and an anti-Bcl-2 active agent. Another aspect of the invention is a kit comprising a type II anti-CD20 antibody and an anti-Bcl-2 active agent. Yet another aspect of the invention is a method for the treatment of a patient suffering from cancer comprising co-administering, to a patient in need of such treatment, a type II anti-CD20 antibody and an anti-Bcl-2 active agent.
Type:
Application
Filed:
May 14, 2010
Publication date:
April 14, 2011
Applicant:
Hoffman-La Roche. Inc.
Inventors:
Thomas Friess, Christian Klein, Pamela Strein, Pablo Umana
Abstract: The present invention relates to compounds of the formula and the pharmaceutically acceptable salts and esters thereof, a process for their manufacture, medicaments containing them as well as the use of these compounds as pharmaceutically active agents. The compounds show antiproliferative activity and may be especially useful for the treatment of cancer.
Type:
Grant
Filed:
June 2, 2005
Date of Patent:
February 22, 2011
Assignee:
Hoffman-La Roche Inc.
Inventors:
Gregory Jay Haley, Norman Kong, Emily Aijun Liu, Binh Thanh Vu
Abstract: The invention relates to a compound of formula (I) wherein A1 and R1 to R5 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
Type:
Grant
Filed:
June 2, 2010
Date of Patent:
February 22, 2011
Assignee:
Hoffman-La Roche Inc.
Inventors:
David Banner, Simona M. Ceccarelli, Uwe Grether, Wolfgang Haap, Hans Hilpert, Holger Kuehne, Harald Mauser, Jean-Marc Plancher, Ruben Alvarez Sanchez
Abstract: The invention relates to 3,3 disubstituted pyrrole derivatives useful for treatment of diseases associated with monoamine reuptake inhibitors. Also provided pharmaceutical compositions, methods of using, and methods of preparing the compounds.
Type:
Application
Filed:
March 10, 2009
Publication date:
January 27, 2011
Applicant:
Hoffman-La Roche, Inc.
Inventors:
Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
Abstract: The present invention relates a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, R1, R2, A and n are as defined in the specification and to their pharmaceutically active salts. The invention also relates to novel compounds of formula I, pharmaceutical compositions containing them, and methods for their preparation.
Type:
Grant
Filed:
January 19, 2007
Date of Patent:
January 25, 2011
Assignee:
Hoffman-La Roche Inc.
Inventors:
Guido Galley, Katrin Groebke Zbinden, Marius Hoener, Sabine Kolczewski, Roger Norcross, Henri Stalder
Abstract: The present invention relates to compounds of formula I, wherein X is —CH2— or —NH—; Y is —CH(lower alkoxy)-, —CH(lower alkyl)-, —O—, —S—, —S(O)—, —S(O)2— or —CH2—; and Ar is phenyl or naphthyl, which rings are optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkoxy, lower alkyl and lower alkyl substituted by halogen; or a pharmaceutically-acceptable acid-addition salt thereof; with the proviso that, when X is —NH—, Y is —CH(lower alkyl)- or —CH2—; and the further proviso that the compound is not 2-phenethyl-1H-imidazole hydrochloride, 2-(3,4-dichloro-phenoxymethyl)-1H-imidazole hydrochloride, 2-(2-chloro-phenoxymethyl)-1H-imidazole hydrochloride, 2-(2,3-dichloro-phenoxymethyl)-1H-imidazole, benzyl-(1H-imidazol-2-yl)-amine, (4-chloro-benzyl)-(1H-imidazol-2-yl)-amine, or (2-chloro-benzyl)-(1H-imidazol-2-yl)-amine.
Type:
Grant
Filed:
December 5, 2007
Date of Patent:
December 28, 2010
Assignee:
Hoffman-La Roche Inc.
Inventors:
Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
Abstract: The present invention is directed to a pharmaceutical composition comprising: (A) a type II anti-CD20 antibody with increased antibody dependent cellular cytotoxicity (ADCC); and (B) a chemotherapeutic agent selected from the group consisting of: cyclophosphamide, vincristine and doxorubicine. The present invention is also directed to a method for the treatment of a CD20 expressing cancer, comprising administering to a patient in need of such treatment (i) an effective first amount of a type II anti-CD20 antibody with increased antibody dependent cellular cytotoxicity; and (ii) an effective second amount of one or more chemotherapeutic agents selected from the group consisting of cyclophosphamide, vincristine and doxorubicine.
Type:
Application
Filed:
May 10, 2010
Publication date:
December 9, 2010
Applicant:
Hoffman-La Roche. Inc.
Inventors:
Charles Dumontet, Thomas Friess, Frank Herting, Christian Klein, Pablo Umana
Abstract: The present invention provides a conjugate consisting essentially of a NK4 molecule and a polyethylene glycol group having a molecular weight of from about 20 to about 40 kDa. The invention also provides a composition in which the monoPEGylated conjugates comprise at least 90% of the total of pegylated NK4 molecules and unpegylated NK4 molecules in the composition. Also provided is a composition in which the monoPEGylated conjugates comprise conjugates in which the PEG groups are attached to groups randomly selected from the lysine side chains of NK4 molecules and the N-terminal amino groups of NK4 molecules. A method for the treatment of cancer by administering 1 to 30 mg monoPEGylated NK4 per kg per day is further provided.
Abstract: The present invention relates to compounds of formula wherein R1, R2, X, Y and Ar are as defined herein and to their pharmaceutically active salts, with the exclusion of the racemic compound 4-benzyl-4,5-dihydro-1H-imidazole or its tautomer (CAS 131548-83-9).
Type:
Grant
Filed:
June 26, 2008
Date of Patent:
October 12, 2010
Assignee:
Hoffman-La Roche Inc.
Inventors:
Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
Abstract: The present invention relates to a process for preparation of a compound of formula I wherein Het, R1, R2, R3, and n are as defined herein and pharmaceutically acceptable acid addition salts thereof, which comprises reacting a compound of formula 21 with a compound of formula 8 to obtain a compound of formula 11 and coupling the compound of formula 11 in the presence of a coupling reagent or the corresponding acid halogenide with a compound of formula 15 to obtain a compound of formula I.
Type:
Grant
Filed:
February 27, 2008
Date of Patent:
October 12, 2010
Assignee:
Hoffman-La Roche Inc.
Inventors:
Christophe Pfleger, Pius Waldmeier, Shaoning Wang
Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R1, R2, R3, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
Abstract: The present invention provides novel compounds of the general formula (I) and pharmaceutically acceptable salts thereof, processes for the manufacture of these novel compounds and medicaments containing such compounds. The compounds of the present invention show anti-proliferative and differentiation-inducing activity, which results in inhibition of tumor cell proliferation, induction of apoptosis and inhibition of invasion. The invention also covers the use of such compounds for the treatment of diseases such as cancer and for the manufacture of corresponding medicaments.
Type:
Grant
Filed:
January 23, 2009
Date of Patent:
September 14, 2010
Assignee:
Hoffman-La Roche Inc.
Inventors:
Li Chen, Yun He, Jason Christopher Wong