Abstract: Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.
Type:
Grant
Filed:
February 16, 2001
Date of Patent:
February 7, 2006
Assignee:
Neurogen Corporation
Inventors:
Taeyoung Yoon, Ping Ge, Raymond F. Horvath, Stephane DeLombaert, Kevin J. Hodgetts, Dario Doller, Cunyu Zhang
Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Type:
Grant
Filed:
January 10, 2002
Date of Patent:
February 7, 2006
Assignee:
Amgen Inc.
Inventors:
Guoqing Chen, Jeffrey Adams, Jean Bemis, Shon Booker, Guolin Cai, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Stephanie Geuns-Meyer, Michael Handley, Qi Huang, Joseph L. Kim, Tae-Seong Kim, Alexander Kiselyov, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Markian Stec, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan
Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) useful in treating Alzheimer's disease and other similar diseases.
Type:
Grant
Filed:
September 21, 2001
Date of Patent:
January 31, 2006
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Roy Hom, Shumeye Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Fang
Abstract: A compound selected from those of formula (I): wherein: Ra represents linear or branched (C1–C6)alkylene, X represents a group selected from W1, —C(W1)—W2—, —W2—C(W1)—, —W2—C(W1)W2—, —W2—Ra— and —CH(OR1)— wherein W1, W2 and R1 are as defined in the description, when Y represents aryl or heteroaryl, or X represents a group selected from single bond, —C(W1)—, —W2—C(W1)—, —W2—Ra and —CH(OR1)— wherein W1, W2, Ra and R1 are as defined hereinbefore, when Y represents a fused bicyclic group, of formula: wherein: A represents nitrogen-containing heterocycle having from 4 to 7 ring members that is unsaturated or partially saturated and optionally contains a second hetero atom, B represents phenyl ring optionally substituted by one or more groups as defined in the description, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base, medicinal products containing the same are useful in the treatment of cognitive deficiencies.
Type:
Grant
Filed:
July 12, 2002
Date of Patent:
January 31, 2006
Assignee:
Les Laboratories Servier
Inventors:
Solo Goldstein, Guillaume Poissonnet, Jean-Gilles Parmentier, Pierre Lestage, Brian Lockhart
Abstract: The invention provides compounds of formula I: wherein A, B, W, Y, Z, and R1 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.
Type:
Grant
Filed:
May 14, 2004
Date of Patent:
January 17, 2006
Assignee:
Rutgers, The State University of New Jersey
Inventors:
Edmond J. LaVoie, Alexander L. Ruchelman
Abstract: A liquid-phase chemical reaction medium comprises one or more reactants, optionally in the presence of a reaction product(s) and one or more solvents, diluents or other form of liquid carrier, a catalyst system comprising at least a metal or metal compound and optionally further compounds such as ligands or complexing agents; characterized in that the reaction medium further comprises a polymeric dispersant dissolved in said liquid carrier, said polymeric dispersant being capable of stabilizing a colloidal suspension of particles of said metal or metal compound within the liquid carrier. The presence of the polymeric dispersant enables metal formed by catalyst deactivation to be more easily recovered and recycled. Preferably, the polymeric dispersant has sufficiently acidic or basic functionality to stabilize the colloidal suspension of said metal or metal compound.
Type:
Grant
Filed:
August 2, 2000
Date of Patent:
January 10, 2006
Assignee:
Lucite International UK Limited
Inventors:
Graham Ronald Eastham, Raymond Anthony Hadden, David William Johnson
Abstract: A process for the preparation of a 4-(4-flourophenyl)-6-alkyl-2-N-alkansulfonyl-N-alkylamino)pyrimidine-5-carboxylic acid ester of formula (Ib), in which R1, R2, R3 and R4 are identical or different and are each a C1-6-alkyl. A 2-[-1-amino-1-(4-flourophenyl)methylene]-4-alkyl-3-oxo-alkanoic acid ester of formula (IIIb), in which R3 and R4 have the above-mentioned meanings, is reacted with an N-cyano-N-alkylalkanesulfonamide, optionally isolated or prepares in situ, of formula (IVb), in which R1 and R2 have the above-mentioned meanings, to give the final product of formula (Ib).
Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
Type:
Grant
Filed:
November 21, 2003
Date of Patent:
January 10, 2006
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
Abstract: The invention relates to substituted alcohol compounds of the formula (I): wherein X, R1, R2, R3, RN, R20 and RC are defined herein. The compounds are useful in the treatment or prevention of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers.
Abstract: The invention relates to the use of arsenic compounds to treat a variety of leukemia, lymphoma and solid tumors. Further, the arsenic compounds may be used in combination with other therapeutic agents, such as a retinoid. The invention also provides a process for producing arsenic trioxide formulations.
Type:
Grant
Filed:
January 16, 2004
Date of Patent:
January 3, 2006
Assignee:
Memorial Sloan-Kettering Cancer Center
Inventors:
Raymond P. Warrell, Jr., Pier Paolo Pandolfi, Janice L. Gabrilove
Abstract: The present invention is directed to a pharmaceutical composition comprising a compound of Formula I dissolved in propylene glycol and water. The present invention also relates to a pharmaceutical composition containing a compound of Formula I dissolved in propylene glycol and a buffer that has a pH between about 3 and about 5.
Type:
Grant
Filed:
September 26, 2002
Date of Patent:
December 27, 2005
Assignees:
Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.
Inventors:
Yuichi Sato, David T. Breslin, Shyam B. Karki
Abstract: A water soluble derivative of buckministerfullerene (C50) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.
Type:
Grant
Filed:
February 1, 2003
Date of Patent:
December 27, 2005
Assignee:
The Regents of the University of California
Inventors:
Simon H. Friedman, Raymond F. Schinazi, Fred Wudl, Craig L. Hill, Diane L. DeCamp, Rintje P. Sijbesma, George L. Kenyon
Abstract: This invention is directed to acyl piperazine derivatives of formula (Ia): wherein R1a, R2, R3, R4, R5 and R6 are defined herein, which are useful as anti-inflammatory agents. This invention is also directed to other acyl piperazine derivatives, pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.
Type:
Grant
Filed:
January 17, 2003
Date of Patent:
December 20, 2005
Assignee:
Schering Aktiengesellschaft
Inventors:
John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Kenneth J. Shaw, Guo Ping Wei, Wei Xu, Zuchun Zhao, Wei Zheng
Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.
Type:
Grant
Filed:
December 20, 2002
Date of Patent:
December 13, 2005
Assignee:
AstraZeneca AB
Inventors:
David Hardern, Anthony Ingall, Brian Springthorpe, Paul Willis, Simon Guile
Abstract: A compound of the formula or the pharmaceutically acceptable salt thereof; wherein X, Y, a, b, c, d, R1, R2, R3 and R5 are as defined above useful to treat inflammation and other immune disorders.
Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rd, A to G and X are defined as in claim 1, the tautomers, the steroisomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly an inhibiting effect on signal transduction mediated by tyrosine kinases, their use for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract, and the preparation thereof.
Type:
Grant
Filed:
February 24, 2000
Date of Patent:
December 6, 2005
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Frank Himmelsbach, Elke Langkopf, Birgit Jung, Thomas Metz, Flavio Solca, Stefan Blech
Abstract: This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.
Type:
Grant
Filed:
January 17, 2003
Date of Patent:
December 6, 2005
Assignee:
Schering Aktiengesellschaft
Inventors:
John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Kenneth J. Shaw, Guo Ping Wei, Wei Xu, Zuchun Zhao, Wei Zheng
Abstract: This invention provides a novel class of substituted macrocyclic metallic complexes. The complexes are useful as peroxynitrite decomposition catalysts. Pharmaceutical compositions, and methods of making and using the compounds, or a pharmaceutically acceptable salt, hydrate, prodrug, or mixture thereof are also described.
Abstract: The invention provides compounds of formula I: wherein A, B, W, Y, Z, R1, R3 and R4 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating cancer using compounds of formula I.
Type:
Grant
Filed:
May 14, 2004
Date of Patent:
November 15, 2005
Assignee:
Rutgers The State University of New Jersey
Inventors:
Edmond J. LaVoie, Alexander L. Ruchelman
Abstract: A chiral catalyst is disclosed together with methods of using it for enantioselective syntheses. The chiral catalyst includes a nucleus with two metal atoms that has four bridging ligands oriented radially to the axis of the nucleus. Each of these ligands includes a two complexing atoms each complexed to one of the metal atoms. At least one of the bridging ligands includes a chiral center which is bonded to one of the complexing atoms. Preferably, all four of the bridging ligands include a chiral center bonded to one of the complexing atoms. The catalyst of the invention has been found to be useful in catalyzing carbenoid transformation reactions such as cyclopropanation.