The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/362)
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Publication number: 20110003806Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: January 28, 2010Publication date: January 6, 2011Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company LimitedInventors: Masaaki Hirose, Steven P. Langston, Hirotake Mizutani, Stepan Vyskocil
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Publication number: 20110003798Abstract: The invention provides a novel class of 2,7-naphthyridin derivatives; pharmaceutical compositions comprising such compounds and methods of using such compounds to treat o prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT*, c-Kit, RET, TrkA, TrkB, TrkC-GR-1R, Alk, c-FMS or combinations thereof.Type: ApplicationFiled: January 27, 2009Publication date: January 6, 2011Applicant: IRM LLCInventors: Barun Okram, Tetsuo Uno, Qiang Ding, Yahua Liu, Yunho Jin, Qihui Jin, Xu Wu, Jianwei Che, S. Frank Yan, Xueshi Hao
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Publication number: 20110003828Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.Type: ApplicationFiled: June 24, 2010Publication date: January 6, 2011Inventors: Laura Cook Blumberg, Julius F. Remenar, Örn Almarsson, Tarek A. Zeidan
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Publication number: 20110003794Abstract: The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: ApplicationFiled: August 30, 2010Publication date: January 6, 2011Inventor: Brian A Johns
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Publication number: 20110003807Abstract: The present invention relates to a compound represented by the formula (I) or (I?): wherein each symbol is as defined in the specification, or a salt thereof, and a PI3K and(or) mTOR inhibitor containing the compound or a prodrug thereof.Type: ApplicationFiled: January 28, 2010Publication date: January 6, 2011Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company LimitedInventors: Hiroshi Banno, Masaaki Hirose, Osamu Kurasawa
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Patent number: 7863271Abstract: Compounds of formulae I, II and III: are disclosed as 5-HT3 inhibitors. The compounds are useful in treating CINV, IBS-D and other diseases and conditions.Type: GrantFiled: August 7, 2007Date of Patent: January 4, 2011Assignee: Albany Molecular Research, Inc.Inventors: Zhicai Yang, David D. Manning
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Patent number: 7863279Abstract: The invention relates to the triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives of general formula (I): Wherein X, A, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.Type: GrantFiled: October 13, 2009Date of Patent: January 4, 2011Assignee: sanofi-aventisInventors: Luc Even, Christian Hoornaert
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Publication number: 20100324041Abstract: Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. Formula, (I).Type: ApplicationFiled: January 8, 2009Publication date: December 23, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: James F. Blake, Indrani W. Gunawardana, Yvan Le Huerou, Peter J. Mohr, Eli M. Wallace, Bin Wang
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Patent number: 7855202Abstract: The present disclosure relates to imidazopyridine derivatives of formula (I): The present disclosure also relates to a method for treating a subject afflicted with a pathological condition or disease susceptible to amelioration by antagonism of the A2B adenosine receptor.Type: GrantFiled: October 5, 2006Date of Patent: December 21, 2010Assignee: Laboratorios Almirall, S.A.Inventors: Bernat Vidal Juan, Silvia Fonquerna Pou, Paul Robert Eastwood, Jose Aiguade Bosch, Aranzazu Cardus Figueras, Ines Carranco Moruno, Jacob Gonzalez Rodriguez, Sergio Paredes Aparicio
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Publication number: 20100317646Abstract: A compound of formula I, or a pharmaceutically acceptable salt or ester thereof, wherein R1 is selected from: aryl; heteroaryl; —NHR3; fused aryl-C4-7-heterocycloalkyl; —CONR4R5; —NHCOR6; —C3-7-cycloalkyl; —O—C3-7-cycloalkyl; —NR3R6; and optionally substituted —C1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C4-7-heterocycloalkyl and C4-7-heterocycloalkyl are each optionally substituted; R2 is selected from hydrogen, aryl, C1-6-alkyl, C2-6-alkenyl, C3-7-cycloalkyl, heteroaryl, C4-7 heterocycloalkyl and halogen, wherein said C1-6-alkyl, C2-6-alkenyl, aryl, heteroaryl and C4-7-heterocycloalkyl are each optionally substituted; R3 is selected from aryl, heteroaryl, C4-7-heterocycloalkyl, C3-7-cycloalkyl, fused aryl-C4-7-heterocycloalkyl and C1-6-alkyl, each of which is optionally substituted; R4 and R5 are each independently hydrogen, or optionally substituted C3-7-cycloalkyl, aryl, heteroaryl, C1-6-alkyl or C3-6-heterocycloalkyl; or R4 and R5 together with the N to which they are attached form a C3-6-hType: ApplicationFiled: March 19, 2010Publication date: December 16, 2010Applicant: Medical Research Council TechnologyInventors: Edward Giles Mciver, Ela Smiljanic, Denise Jamilla Harding, Joanne Hough
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Publication number: 20100311740Abstract: This invention relates to newly identified imidazopyridine compounds of formula (I), to the use of such compounds in treating GERD and the like.Type: ApplicationFiled: June 28, 2006Publication date: December 9, 2010Inventors: Mark James Bamford, Richard Leonard Elliott, Gerard Martin Paul Giblin, Antoinette Naylor, Terence Aaron Chal, Andrew Kenneth Takle, Jason Witherington
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Publication number: 20100311693Abstract: This application relates to compounds of the general Formula I and salts thereof, wherein X, R1A, R1B, R2, R3, R4, and R5 are as defined herein. The application also relates to compositions and methods of treatment of hyperproliferative diseases or disorders.Type: ApplicationFiled: June 4, 2010Publication date: December 9, 2010Applicant: CEPHALON, INC.Inventors: Matthew A. Curry, Bruce D. Dorsey, Benjamin J. Dugan, Diane E. Gingrich, Eugen F. Mesaros, Karen L. Milkiewicz
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Patent number: 7846928Abstract: The invention relates to substituted pyrazolopyridines according to the general formula (I): in which A, B, D, E, Ra, R1, R2, R3, R4, R5 and q are as defined in the claims, and salts thereof, to pharmaceutical compositions comprising said substituted pyrazolopyridine compounds, to methods of preparing said substituted pyrazolopyridines, as well as to uses thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.Type: GrantFiled: June 12, 2007Date of Patent: December 7, 2010Assignee: Bayer Schering Pharma AGInventors: Ingo Hartung, Stuart Ince, Georg Kettschau, Karl-Heinz Thierauch, Hans Briem, Ulf Boemer
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Publication number: 20100305122Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: May 26, 2010Publication date: December 2, 2010Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Robert A. Mantei, Todd M. Hansen
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Publication number: 20100298301Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: ApplicationFiled: May 9, 2008Publication date: November 25, 2010Applicant: SAREUM LIMITEDInventors: John Charles Reader, John Mark Ellard, Helen Boffey, Susanne Taylor, Andrew David Carr, Michael Cherry, Michelle Wilson, Richard Boakye Owoare
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Publication number: 20100298339Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain triazolo compounds (referred to herein as TAZ compounds), and especially certain [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-c]pyrimidine compounds, which, inter alia, inhibit AXL receptor tyrosine kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit AXL receptor tyrosine kinase function, and in the treatment of diseases and conditions that are mediated by AXL receptor tyrosine kinase, that are ameliorated by the inhibition of AXL receptor tyrosine kinase function, etc., including proliferative conditions such as cancer, etc.Type: ApplicationFiled: October 10, 2008Publication date: November 25, 2010Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Grégoire Alexandre Pavé, James Donald Firth, Lorna Stewart, Laurent Jean Martin Rigoreau, Emma Louise Wynne
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Publication number: 20100298314Abstract: Disclosed are substituted imidazo[1,2-a]pyridines, imidazo[1,2-a]pyrazines, imidazo[1,2-c]pyrimidines and imidazo[1,2-d]triazines compounds of the formula: (1.0) Also disclosed are methods for treating JNK1 and ERK mediated diseases using the compounds of formula 1.0.Type: ApplicationFiled: December 17, 2007Publication date: November 25, 2010Inventors: Panduranga Adulla P. Reddy, M. Arshad Siddiqui, Praveen K. Tadikonda, Umar Faruk Mansoor, Gerald W. Shipps, JR., David B. Belanger, Lianyun Zhao
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Publication number: 20100292234Abstract: The present invention comprises a new class of compounds useful for modulating the activity of p38 MAP kinase. The compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, R1 and R5 are defined herein. The invention further provides pharmaceutical compositions including one or more compounds of Formula I, use of such compounds and compositions for treatment of p38 MAP kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: September 19, 2008Publication date: November 18, 2010Applicant: Amgen Inc.Inventors: Liping H. Pettus, Kelvin K.C. Sham, Andrew Tasker, Shimin Xu
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Publication number: 20100286133Abstract: The invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof: Wherein X, R1 and R2 are as defined herein. The invention also relates to the use of these compounds as pharmaceutical products.Type: ApplicationFiled: July 20, 2010Publication date: November 11, 2010Applicant: SANOFI-AVENTISInventors: Gerhard ZOLLER, Stefan PETRY, Gunter MÜLLER, Hubert HEUER, Norbert TENNAGELS
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Publication number: 20100286152Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof,Type: ApplicationFiled: June 5, 2008Publication date: November 11, 2010Applicant: Glaxo Group LimitedInventors: Giovanni Bernasconi, Steven Mark Bromidge, Andrew James Carpenter, Lucilla D'Adamo, Romano Di Fabio, Sebastien Guery, Francesca Pavone, Alfonso Pozzan, Marilisa Rinaldi, Fabio Maria Sabbatini, Yves St-Denis
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Patent number: 7829568Abstract: Substituted 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-ylamine compounds corresponding to formula I, methods for the preparation thereof, pharmaceutical compositions containing said compounds, the use of said compounds for preparing pharmaceutical compositions and related treatment methods.Type: GrantFiled: October 5, 2007Date of Patent: November 9, 2010Assignee: Gruenenthal GmbHInventors: Robert Frank, Bernd Sundermann, Corinna Sundermann
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Publication number: 20100280043Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, 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: ApplicationFiled: January 8, 2009Publication date: November 4, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: James F. Blake, Indrani W. Gunawardana, Yvan Le Huerou, Peter J. Mohr, Eli M. Wallace, Bin Wang
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Publication number: 20100278833Abstract: The invention relates to thiophene-imidazopyridine compounds according to formula (I), wherein the substituents and symbols are as defined in the description. The compounds are inhibitors of PIk1.Type: ApplicationFiled: June 26, 2008Publication date: November 4, 2010Inventors: Thomas Stengel, Mathias Schmidt, Steffen Weinbrenner, Alexander Weber, Petra Gimmnich, Volker Gekeler, Thomas Beckers, Astrid Zimmermann, Thomas Maier, Beata Schmidt, Florian Dehmel
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Publication number: 20100280013Abstract: [Object] It is to provide a novel LXR? agonist useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate: (wherein, each V and W independently show N or C—R7; each X and Y independently show CH2, C?O, SO2, etc; Z shows CH or N; each R1, R2 and R7 independently show a hydrogen atom, C1-8 alkyl group, etc.; R3 shows C1-8 alkyl group; R4 shows an optionally substituted C6-10 aryl group or an optionally substituted 5- to 11-membered heterocyclic group; R5 and R6 show a hydrogen atom, etc.; L shows a C1-8 alkyl chain optionally substituted with an oxo group, etc.; and n shows any integer of 0 to 2.Type: ApplicationFiled: April 28, 2010Publication date: November 4, 2010Applicant: KOWA COMPANY, LTD.Inventors: Minoru Koura, Hisashi Sumida, Sayaka Kurobuchi, Takayuki Matsuda, Yuichiro Watanabe, Takashi Enomoto, Kimiyuki Shibuya, Sumiko Kurobuchi
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Publication number: 20100280030Abstract: Compounds of the formula (I), in which R1, R2, R3, R3?, R4, R4?, E, E?, E? and E?? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: May 8, 2008Publication date: November 4, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Publication number: 20100275389Abstract: Provided herein is a method for dyeing keratin fibers, comprising applying to the keratin fibers, at least one composition comprising at least one compound chosen from compounds of leuco type of formula (I), dyes of azomethine type containing a pyrazolopyridine unit of formula (II) corresponding to the compounds of formula (I), mesomeric forms, isomers and tautomers thereof, and also acid-addition salts thereof and solvates thereof:Type: ApplicationFiled: April 28, 2010Publication date: November 4, 2010Inventors: Aziz FADLI, Stéphane Blais
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Patent number: 7825123Abstract: The present invention provides compounds of 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: GrantFiled: September 17, 2009Date of Patent: November 2, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Georg Jaeschke, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
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Patent number: 7820820Abstract: A method of preparing azaindole compounds for antiviral use having the formulaType: GrantFiled: August 24, 2009Date of Patent: October 26, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Wansheng Liu, Sunil S. Patel, Nicolas Cuniere, Yvonne Lear, Prashant P. Deshpande, Jeffrey N. Simon, Chiajen Lai, Annie J. Pullockaran, Nachimuthu Soundararajan, Jeffrey T. Bien
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Publication number: 20100266509Abstract: Heteroaryl amide analogues are provided, of Formula (I), wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: April 9, 2008Publication date: October 21, 2010Applicant: H. Lindbeck A/SInventors: David C. Ihle, Qin Guo, Kevin Hodgetts, Jun Yuan
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Patent number: 7816360Abstract: The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.Type: GrantFiled: December 22, 2008Date of Patent: October 19, 2010Assignee: Janssen Pharmaceutica NVInventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Libuse Jaroskova, Peter Walter Maria Roevens, Louis Jozef Elisabeth Van Der Veken, Marcel Viellevoye, Joannes Theodorus Maria Linders
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Publication number: 20100261730Abstract: The invention relates to alkynylaryl compounds according to the general formula (I) in which A, B, D, E, Ra, R1, R3, R4, R5 and q are as defined in the claims, and salts, N-oxides, solvates and prodrugs thereof, to pharmaceutical compositions comprising said alkynylaryl compounds, to methods of preparing said alkynylaryl compounds, to intermediate compounds useful in said methods, to uses of said intermediate compounds in the preparation of said alkynylaryl compounds, as well as to uses of said alkynylaryl compounds for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth.Type: ApplicationFiled: December 4, 2008Publication date: October 14, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Ingo Hartung, Hans Briem, Georg Kettschau, Karl-Heinz Thierauch, Ulf Bömer
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Publication number: 20100260715Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: March 1, 2010Publication date: October 14, 2010Inventors: Yat Sun Or, Ce Wang, Lu Ying, Xiaowen Peng, Yao-Ling Qiu
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Publication number: 20100256365Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: ApplicationFiled: November 10, 2009Publication date: October 7, 2010Inventors: Prabha N. Ibrahim, Dean R. Artis, Ryan Bremer, Gaston Habets, Shumeye Mamo, Marika Nespi, Chao Zhang, Jiazhong Zhang, Yong-Liang Zhu, Rebecca Zuckerman, Brian West, Yoshisa Suzuki, James Tsai, Klaus-Peter Hirth, Gideon Bollag, Wayne Spevak, Hanna Cho, Samuel J. Gillette, Guoxian Wu, Hongyao Zhu, Shenghua Shi
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Publication number: 20100256356Abstract: Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, 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: ApplicationFiled: January 26, 2010Publication date: October 7, 2010Applicants: Array BioPharma Inc., Genentech, Inc.Inventors: James F. Blake, Steven Armen Boyd, Jason De Meese, Kin Chiu Fong, John J. Gaudino, Tomas Kaplan, Allison L. Marlow, Jeongbeob Seo, Allen A. Thomas, Hongqi Tian, Frederick Cohen, Wendy B. Young
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Publication number: 20100256141Abstract: Disclosed are compounds of formula (I): wherein R1, R2, R3, R4, and R5 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and the use thereof as protein kinase inhibitors.Type: ApplicationFiled: June 23, 2010Publication date: October 7, 2010Applicant: Aventis Pharma S.A.Inventors: Conception NEMECEK, William A. METZ, Sylvie WENTZLER, Dominique LESUISSE, Youssef EL-AHMAD
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Publication number: 20100256133Abstract: Novel compounds having indazole frameworks, as well as a method for preparing the same and a pharmaceutical composition comprising the same are provided. The compounds of the present invention can inhibit protein kinase activity and thus the pharmaceutical composition of the present invention can be used to prevent or treat diseases or disorders which are related to protein kinase activity.Type: ApplicationFiled: September 19, 2008Publication date: October 7, 2010Inventors: Jeom-Yong Kim, Mi-Ra Ma, Kyung-Yun Jung, Jin-Seok Choi, Young-Seok Cho, Sang-Hak Lee
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Patent number: 7807676Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.Type: GrantFiled: October 23, 2007Date of Patent: October 5, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, John F. Kadow, Zhongxing Zhang, Zhiwei Yin, Nicholas A. Meanwell, Alicia Regueiro-Ren, Jacob Swidorski, Ying Han, David J. Carini, Lawrence G. Hamann
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Patent number: 7807671Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity useful for the treatment of HIV and AIDS.Type: GrantFiled: April 10, 2007Date of Patent: October 5, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, John F. Kadow, Zhongxing Zhang, Zhiwei Yin, Nicholas A. Meanwell, Alicia Regueiro-Ren, Jacob Swidorski, Ying Han, David J. Carini
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Publication number: 20100249118Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: ApplicationFiled: June 21, 2006Publication date: September 30, 2010Inventors: Prabha N. Ibrahim, Dean R. Artis, Ryan Bremer, Shumeye Mamo, Chao Zhang, Jiazhong Zhang, James Tsai, Klaus-Peter Hirth, Gideon Bollag, Wayne Spevak, Hanna Cho, Samuel J. Gillette, Shenghua Shi
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Publication number: 20100249119Abstract: The present invention provides a heterocyclic compound having a strong Raf inhibitory activity, which is represented by the following formula wherein each substituent is as defined in the present specification, or a salt thereof.Type: ApplicationFiled: August 28, 2008Publication date: September 30, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masaaki Hirose, Masanori Okaniwa, Yoko Hayashi, Terufumi Takagi
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Publication number: 20100249145Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling.Type: ApplicationFiled: March 25, 2010Publication date: September 30, 2010Inventors: Oscar Mario Saavedra, Stephen William Claridge, Lijie Zhan, Franck Raeppel, Arkadii Vaisburg, Stephane Raeppel, Robert Deziel, Michael Mannion, Nancy Z. Zhou, Ljubomir Isakovic
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Publication number: 20100234369Abstract: Novel 5-cyanothienopyridines of the formula (I), in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of TGF-beta receptor kinase, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: September 19, 2008Publication date: September 16, 2010Inventors: Guenter Hoelzemann, Ulrich Graedler, Hartmut Greiner, Christiane Amendt, Djordje Musil, Per Hillertz
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Patent number: 7795256Abstract: A series of thieno[2,3-b]pyridin-6(7H)-one derivatives, substituted in the 3-position by an arylcarbonyl or heteroaryl-carbonyl moiety, being inhibitors of p38 MAP kinase, are accordingly of use in medicine, for example in the treatment and/or prevention of immune or inflammatory disorders.Type: GrantFiled: October 22, 2004Date of Patent: September 14, 2010Assignee: UCB Pharma S.A.Inventors: Rikki Peter Alexander, Jeremy Martin Davis, Martin Clive Hutchings, Victoria Elizabeth Laing, Graham Peter Trevitt
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Patent number: 7795257Abstract: The present invention provides compounds of the formula which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed for the prevention and the treatment of impaired glucose tolerance, type 2 diabetes and obesity.Type: GrantFiled: September 28, 2006Date of Patent: September 14, 2010Assignee: Novartis AGInventor: Gregory Raymond Bebernitz
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Patent number: 7795264Abstract: The invention relates to substituted arylpyrazolopyridines according to the general formula (I): in which A, B, D, E, Ra, R1, R2, R3, R4, R5 and q are as defined in the claims, and salts thereof, to pharmaceutical compositions comprising said substituted arylpyrazolopyridines, to methods of preparing said substituted arylpyrazolopyridines as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.Type: GrantFiled: June 12, 2007Date of Patent: September 14, 2010Assignee: Bayer Schering Pharma AGInventors: Ingo Hartung, Georg Mendelstr Kettschau, Karl-Heinz Thierauch, Hans Briem, Philip Lienau, Antonius Ter Laak
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Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
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Publication number: 20100222357Abstract: The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: wherein the residues R1 to R3 are as defined herein. The invention also relates to pharmaceutical compositions containing such compounds, and methods for preparation of the compounds and compositions. The invention further relates to methods for treating dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders.Type: ApplicationFiled: May 13, 2010Publication date: September 2, 2010Inventors: Caterina Bissantz, Christophe Grundschober, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Patent number: 7786114Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, and R5 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and the use thereof as protein kinase inhibitors.Type: GrantFiled: March 28, 2007Date of Patent: August 31, 2010Assignee: Aventis Pharma S.A.Inventors: Conception Nemecek, William A. Metz, Sylvie Wentzler, Dominique Lesuisse, Youssef El-Ahmad
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Publication number: 20100216763Abstract: Heteroaryl amide derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: November 27, 2007Publication date: August 26, 2010Applicant: H. LUNDBECK A/SInventors: Alan J. Hutchison, Hongbin Li, Jianmin Mao, David J. Wustrow, Jun Yuan, He Zhao
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Patent number: 7781430Abstract: Compounds of formulae I and II: are disclosed as 5-HT3 inhibitors. Those compounds that exhibit central activity are useful in treating CINV; those that inhibit peripheral receptors are useful to treat IBS-D.Type: GrantFiled: November 2, 2007Date of Patent: August 24, 2010Assignee: Albany Molecular Research, Inc.Inventors: David J. Fairfax, Zhicai Yang