Patents Examined by Venkataraman Balasubram
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Patent number: 7442700Abstract: The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.Type: GrantFiled: June 27, 2006Date of Patent: October 28, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Harold Mastalerz, Dolatrai M. Vyas, George L. Trainor, Ashvinikumar V. Gavai
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Patent number: 7442705Abstract: This invention concerns HIV replication inhibitors of formula (I), The N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.Type: GrantFiled: February 20, 2004Date of Patent: October 28, 2008Assignee: Tibotec Pharmaceuticals LtdInventors: Jerôme Emile Georges Guillemont, Elisabeth Thérese Jeanne Pasquier, Jan Heeres, Kurt Hertogs, Eva Bettens, Paulus Joannes Lewi, Marc René De Jonge, Lucien Maria Henricus Koymans, Frederik Frans Desiré Daeyaert, Hendrik Maarten Vinkers, Frank Xavier Jozef Herwig, legal representative, Paul Adriaan Jan Janssen
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Patent number: 7442792Abstract: The present invention provides novel processes and intermediates for preparing corticotropin releasing factor (CRF) receptor antagonists having the structure below which are useful in treating CRF-related disorders such as anxiety and depression.Type: GrantFiled: March 13, 2007Date of Patent: October 28, 2008Assignee: Bristol-Myers Squibb Pharma CompanyInventors: James P. Sherbine, Shawn K. Pack, Jaan A. Pesti, Robert E. Yule, Kenneth C. McNulty
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Patent number: 7432373Abstract: The present invention is directed to intermediates that are useful for preparing pyrrolotriazines, and processes for preparing such intermediates.Type: GrantFiled: June 24, 2005Date of Patent: October 7, 2008Assignee: Bristol-Meyers Squibb CompanyInventors: Gerard Crispino, Stephanie Barbosa, Junying Fan, Zhen-wei Cai
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Patent number: 7427628Abstract: Disclosed are compounds which bind ?4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by ?4 integrins, preferably VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: September 26, 2006Date of Patent: September 23, 2008Assignee: Elan Pharmaceuticals, Inc.Inventors: Andrei W. Konradi, Christopher M. Semko, Ying-zi Xu, Frank Stappenbeck, Brian P. Stupi, Jenifer Smith, Michael A. Pleiss, Eugene D. Thorsett
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Patent number: 7427626Abstract: Compounds of the formula (I), and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti cell proliferation) effect in a warm blooded animal, such as man.Type: GrantFiled: May 12, 2004Date of Patent: September 23, 2008Assignee: AstraZeneca ABInventor: Andrew Peter Thomas
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Patent number: 7423049Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: May 8, 2006Date of Patent: September 9, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Vincent Galullo, Steven Bellon, Guy Bemis, John Cochran
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Patent number: 7423048Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -a1?a2-a3?a4- is a bivalent radical wherein one or two of a1 to a4 are nitrogen and the remaining a1 to a4 are —CH?; -Z1-Z2- is a bivalent radical; -A- is a bivalent radical of formula —N(R6)-Alk2- or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alType: GrantFiled: February 16, 2006Date of Patent: September 9, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Kristol Van Emelen, Marcel Frans Leopold De Bruyn, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Maria Encamacion Matesanz-Ballesteros, José Manuel Bartolomé-Nebreda
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Patent number: 7423148Abstract: Compounds having formula I are provided where the variables have the values described herein. Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and combinations with other agents. A method of treating a patient comprises administering a pharmaceutical formulation according to the invention to a patient in need thereof.Type: GrantFiled: November 21, 2003Date of Patent: September 9, 2008Assignee: Chiron CorporationInventors: John N. Nuss, Sabina Pecchi, Paul A. Renhowe
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Patent number: 7419978Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R, R1, R2, R5, R6a, R6b, J, K, X and Z are as described in the specification.Type: GrantFiled: October 21, 2004Date of Patent: September 2, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Jagabandhu Das, John Hynes, Katerina Leftheris, Shuqun Lin, Stephen T. Wrobleski, Hong Wu
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Patent number: 7414011Abstract: Disclosed are compounds of the formula (I) or salts thereof in which R1, R2, R3, R4, I, R5, Q, R4, W, X, Y, V and Z, are as defined in the specification, which are suitable for use as herbicides or plant growth regulators. Also disclosed are processes for preparing the compounds of formula (I) or salts thereof.Type: GrantFiled: September 12, 2005Date of Patent: August 19, 2008Assignee: Hoechst Schering Agrevo GmbHInventors: Hansjörg Dietrich, Christian Waldraff, Lothar Willms, Hermann Bieringer, Christopher Rosinger, Felix Thürwächter, Thomas Auler
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Patent number: 7414057Abstract: Certain novel piperazine urea derivatives are agonists of the human melanocortin-4 receptor (MC-4R) and, in particular, are receptor-subtype selective agonists of MC-4R. They are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity and diabetes.Type: GrantFiled: September 5, 2003Date of Patent: August 19, 2008Assignee: Merck & Co., Inc.Inventors: Raman Kumar Bakshi, Ravi P. Nargund, Brenda L. Palucki, Min K. Park, Zhixiong Ye
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Patent number: 7410594Abstract: The present invention relates to a process for the trichromatic dyeing or printing of hydroxy-group-containing or nitrogen-containing organic substrates with dye mixtures and also to such dye mixtures and hydroxy-group-containing or nitrogen-containing organic substrates dyed or printed therewith.Type: GrantFiled: October 14, 2002Date of Patent: August 12, 2008Assignee: Clariant Finance (BVI) LimitedInventors: Markus Gisler, Roland Wald
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Patent number: 7411065Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oglimers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.Type: GrantFiled: July 15, 2005Date of Patent: August 12, 2008Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
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Patent number: 7407964Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.Type: GrantFiled: June 7, 2001Date of Patent: August 5, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Guy Brenchley
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Patent number: 7407956Abstract: The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1-R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.Type: GrantFiled: January 8, 2007Date of Patent: August 5, 2008Assignee: Pfizer, Inc.Inventors: Mark A. Dombrowski, Allen J. Duplantier
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Patent number: 7407962Abstract: The present invention provides compounds that are inhibitors of protein kinase, particularly inhibitors of ERK2, GSK3, PKA, CDK2 protein kinases, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of utilizing those compositions in the treatment of various disorders.Type: GrantFiled: February 3, 2004Date of Patent: August 5, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alex Aronov, Michael R. Hale, Francois Maltais, Qing Tang
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Patent number: 7405296Abstract: Compounds of formula wherein Rf is a (per)fluoropolyoxyalkylene chain having a number average molecular weight in the range 500-10,000; W1, W2, equal to or different from each other, are —F or —CF3; T1 is equal to —CHAa—Ba (CH2CH2O)na— wherein Aa=H, CF3; Ba=O, S, NH; na=0 or an integer between 1 and 6; T2 is equal to —F, —CF3, —C2 F5, —(C2 F4) Cl, or a group of formula: Q1, Q2 equal to or different from each other, are a chain of formula -T1-l -CFW1—O—Rf—CFW2-T?2, wherein: T?2 is equal to —F, —CF3, —C2 F5, —(C2F4) Cl; or is a group of formula: wherein B is equal to O, S, NH; R1, R2, R3, R4, R5 equal to or different from each other are selected from H, F, NO2, CN, C1-C8 perfluoroalkyl, carboxyl, phenyl (Ph), O- Ph, NH-Ph, S-Ph; wherein B is equal to O, S, NH; R1, R2, R3, R4, R5 equal to or different from each other are selected from H, F, NO2, CN, C1-C8 perfluoroalkyl, carboxyl, phenyl (Ph), O- Ph, NH-Ph, S-Ph; with the proviso that at least one of Q1 and Q2a is equal to:Type: GrantFiled: April 13, 2006Date of Patent: July 29, 2008Assignee: Solvay Solexis S.p.A.Inventors: Antonio Russo, Patrizia Maccone
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Patent number: 7402588Abstract: A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5? or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.Type: GrantFiled: March 28, 2006Date of Patent: July 22, 2008Assignee: Emory UniversityInventors: Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
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Patent number: RE40558Abstract: The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.Type: GrantFiled: October 20, 2005Date of Patent: October 28, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Zaid Jayyosi, Gerard M. McGeehan, Michael F. Kelley, Richard F. Labaudiniere, Litao Zhang, Robert D. Groneberg, Daniel G. McGarry, Thomas J. Caulfield, Anne Minnich, Mark Bobko