Additional Hetero Ring Which Is Unsaturated Patents (Class 544/331)
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Publication number: 20140249024Abstract: The present invention relates to pesticidal methods for the use and application of substituted 3-pyridyl thiazole compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to insecticidal substituted 3-pyridyl thiazole compounds or of the compositions comprising such compounds for combating invertebrate pests and uses thereof. The substituted 3-pyridyl thiazole compounds of the present invention are defined by the following general formula (I): wherein R1, R2 A and m are defined as in the description.Type: ApplicationFiled: July 13, 2012Publication date: September 4, 2014Applicant: BASF SEInventors: Florian Kaiser, Gemma Veitch, Arun Narine, Joachim Dickhaut, Karsten Körber, Prashant Deshmukh, Nina Gertrud Bandur
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Patent number: 8822451Abstract: 4-amido-pyrimidine compounds, derivatives and compositions thereof, and synthetic methods described herein are useful for modulating ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: May 22, 2006Date of Patent: September 2, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Anna R. Hazlewood, Peter D. J. Grootenhuis, Ashvani Kumar Singh, Thomas Cleveland, Frederick F. Van-Goor
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Publication number: 20140243336Abstract: The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: October 1, 2012Publication date: August 28, 2014Inventors: Michael D. Altman, Corey E. Bienstock, John W. Butcher, Kaleen Konrad Childers, Maria Emilia Di Francesco, Anthony Donofrio, John Michael Ellis, Christian Fischer, Andrew M. Haidle, James P. Jewell, Sandra Lee Knowles, Alan B. Northrup, Ryan D. Otte, Scott L. Peterson, Graham Frank Smith
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Publication number: 20140243302Abstract: Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.Type: ApplicationFiled: June 26, 2012Publication date: August 28, 2014Applicants: MERCK SHARP & DOHME CORPORATION, KYORIN PHARMACEUTICAL CO., LTD.Inventors: Yasumichi Fukuda, David E. Kaelin, JR., Sheo B. Singh
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Publication number: 20140243290Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.Type: ApplicationFiled: April 17, 2014Publication date: August 28, 2014Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon D. Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric T. Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
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Patent number: 8815886Abstract: Crystalline salts of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine, compositions thereof, methods for their preparation, and methods for their use are disclosed.Type: GrantFiled: March 28, 2013Date of Patent: August 26, 2014Assignee: Cymabay Therapeutics, Inc.Inventors: Jiangao Song, Charles A. McWherter, Fang Ma, Mark Andres, Igor Ivanisevic, Ekaterina Albert, Patricia Andres
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Publication number: 20140235586Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.Type: ApplicationFiled: April 28, 2014Publication date: August 21, 2014Applicant: PTC Therapeutics, Inc.Inventors: Jeffrey A. Campbell, Atiyya Kahn, James Takasugi, Ellen Welch
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Publication number: 20140231794Abstract: A compound represented by the following formula (1): wherein in the formula (1), Ar1 and Ar2 are independently a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or a substituted or unsubstituted alkyl group; X1 to X4 and X13 to X16 are independently CR1, CH or N; one of X5 to X8 is a carbon atom bonding to one of X9 to X12, and at least one of X5 to X8 that is adjacent to the carbon atom bonding to one of X9 to X12 is CR2; one of X9 to X12 is a carbon atom bonding to one of X5 to X8, and X9 to X12 that is adjacent to the carbon atom bonding to one of X5 to X8 is CH or N; and the remaining X5 to X8 and the remaining X9 to X12 are CR1, CH or N.Type: ApplicationFiled: September 25, 2012Publication date: August 21, 2014Applicant: Idemitsu Kosan Co., Ltd.Inventors: Toshihiro Iwakuma, Kei Yoshida
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Patent number: 8809359Abstract: The present invention relates to phenyl amino pyrimidine bicyclic compounds formula I which are inhibitors of protein kinases including JAK kinases. In particular the compounds are active against JAK1, JAK2, JAK3 and TYK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.Type: GrantFiled: March 14, 2013Date of Patent: August 19, 2014Assignee: YM Biosciences Australia Pty LtdInventor: Christopher John Burns
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Publication number: 20140228386Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds of the present invention have been found to be useful as 17?-hydroxylase/C17,20-lyase inhibitors.Type: ApplicationFiled: April 27, 2012Publication date: August 14, 2014Applicant: NOVARTIS AGInventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Saumitra Sengupta
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Publication number: 20140228387Abstract: The present invention relates to disubstituted 5-fluoro-pyrimidines of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).Type: ApplicationFiled: September 13, 2012Publication date: August 14, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ulrich Lücking, Dirk Kosemund, Arne Scholz, Philip Lienau, Gerhard Siemeister, Ulf Bömer, Rolf Bohlmann
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Publication number: 20140227260Abstract: The present invention relates to new aminopyrimidine inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 21, 2014Publication date: August 14, 2014Applicant: Auspex Pharmaceuticals, Inc.Inventor: Chengzhi Zhang
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Publication number: 20140228340Abstract: Compounds of the formula I, in which R1, R2, X and Y have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.Type: ApplicationFiled: August 13, 2012Publication date: August 14, 2014Applicant: MERCK PATENT GMBHInventors: Guenter Hoelzemann, Dieter Dorsch, Hans-Michael Eggenweiler
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Publication number: 20140225088Abstract: A compound for an organic optoelectronic device represented by Chemical Formula 1 wherein, in Chemical Formula 1, variables A, Y1 to Y4, X1, m, R1 to R4, L1 to L3, n1 to n3, Ar1 and Ar2 are described in the specification.Type: ApplicationFiled: February 10, 2014Publication date: August 14, 2014Applicants: CHEIL INDUSTRIES INC., SAMSUNG ELECTRONICS CO., LTD.Inventors: Kyu Young HWANG, Sang Mo KIM, Young Kwon KIM, Joo Hee SEO, Jhun Mo SON, Yong Sik JUNG, Seok-Hwan HONG
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Patent number: 8802861Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: GrantFiled: January 11, 2005Date of Patent: August 12, 2014Assignee: Merck Serono SAInventors: Anna Quattropani, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
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Publication number: 20140221346Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are 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 a Retroviridae viral infection including an infection caused by the HIV virus.Type: ApplicationFiled: January 9, 2014Publication date: August 7, 2014Applicant: Gilead Sciences, Inc.Inventors: Randall L. HALCOMB, Yunfeng Eric HU, Qi LIU, Jennifer R. ZHANG
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Publication number: 20140219989Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.Type: ApplicationFiled: July 3, 2012Publication date: August 7, 2014Inventors: Craig Boyle, William Greenlee, Samuel Chackalamannil, Claire Lankin
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Publication number: 20140221374Abstract: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of RAF kinase mediated signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human disease and disorders.Type: ApplicationFiled: March 16, 2012Publication date: August 7, 2014Applicant: Ruga CorporationInventors: Jean-Michel Vernier, Stephanie Hopkins, Pierre-Yves Bounaud, Patrick O'Connor, David Matthews, Steve Bender
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Patent number: 8796298Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.Type: GrantFiled: October 8, 2010Date of Patent: August 5, 2014Assignee: GlaxoSmithKline LLCInventors: Melissa Dumble, Tona Gilmer, Rakesh Kumar, Peter F. Lebowitz, Shannon Renae Morris, Sylvie Laquerre
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Patent number: 8796314Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, CY, X1, X2, and X3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: January 28, 2010Date of Patent: August 5, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Zhan Shi, Irache Visiers, Tricia J. Vos, Stepan Vyskocil
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Patent number: 8796297Abstract: Compounds of the formula wherein R1 and R2 are as disclosed herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor full or partial agonists. Also disclosed are pharmaceutical compositions, methods for using such compounds and compositions, and processes for preparing the compounds.Type: GrantFiled: June 30, 2010Date of Patent: August 5, 2014Assignee: AbbVie Inc.Inventors: Lawrence A. Black, Gregory A. Gfesser, Marlon D. Cowart
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Publication number: 20140213554Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and/or mutant c-kit protein kinases.Type: ApplicationFiled: December 20, 2013Publication date: July 31, 2014Inventors: Guoxian Wu, Katrina Chan, Todd Ewing, Prabha N. Ibrahim, Jack Lin, Marika Nespi, Wayne Spevak, Ying Zhang
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Publication number: 20140213549Abstract: The present invention provides a substituted pyridine compound or a pharmacologically acceptable salt thereof which has excellent CETP inhibition activity and is useful as a medicament. The present invention provides a compound represented by a general formula (I), wherein R1 is H, optionally substituted alkyl, OH, optionally substituted alkoxy, alkylsulfonyl, optionally substituted amino, carboxy, optionally substituted carbonyl, CN, halogeno, optionally substituted phenyl, optionally substituted aromatic heterocyclyl, optionally substituted saturated heterocyclyl, optionally substituted saturated heterocyclyloxy or optionally substituted saturated heterocyclylcarbonyl, etc., and the like.Type: ApplicationFiled: July 8, 2011Publication date: July 31, 2014Applicants: UBE INDUSTRIES, LTD., DAIICHI SANKYO COMPANY, LIMITEDInventors: Tsuyoshi Nakamura, Hidenori Namiki, Naoki Terasaka, Akiko Shima, Masahiko Hagihara, Noriaki Iwase, Katsunori Takata, Osamu Kikuchi, Kazunari Tsuboike, Hiroyuki Setoguchi, Kenji Yoneda, Hidetoshi Sunamoto, Koji Ito
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Patent number: 8791114Abstract: Novel dihydropyrazole derivatives of formula (I) wherein L, R, R3, R4, R5, R6, R7, X1, X2, X3, X4, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: GrantFiled: June 26, 2012Date of Patent: July 29, 2014Assignee: Merck Patent GmbHInventors: Henry Yu, Thomas E. Richardson, Robert James Foglesong, Lizbeth Celeste DeSelm, Andreas Goutopoulos
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Publication number: 20140206709Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 20, 2014Publication date: July 24, 2014Inventors: Zhe Yang, Alex R. Muci, Jeffrey Warrington, Gustave Bergnes, Bradley P. Morgan, Chihyuan Chuang, Antonio Romero, Scott Collibee, Xiangping Qian, Pu-Ping Lu
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Publication number: 20140206585Abstract: A compound of Formula I, Formula IA, Formula IB, or Formula II, or an acid or base addition salt thereof, and use of these compounds as antioxidants. In one embodiment, a compound of Formula II, wherein each of X, Y, and Z are independently a carbon or nitrogen atom; R1 and R2 are each independently a hydrogen or an electron donating group, but are not both hydrogen, and wherein R1, and R2 are each bonded to a carbon atom in their own respective aryl ring.Type: ApplicationFiled: June 4, 2012Publication date: July 24, 2014Applicants: UNIVERSITA DI BOLOGNA, Queen's University at KingstonInventors: Derek A. Pratt, Jason J. Hanthorn, Luca Valgimigli
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Patent number: 8785630Abstract: The present invention describes novel triazines, their related pyrimidines and their use in controlling insects. This invention also includes new synthetic procedures, intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects using the compounds.Type: GrantFiled: February 6, 2013Date of Patent: July 22, 2014Assignee: Vestaron CorporationInventors: Robert M. Kennedy, Bruce A. Steinbaugh
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Patent number: 8778977Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.Type: GrantFiled: July 2, 2007Date of Patent: July 15, 2014Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
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Patent number: 8778955Abstract: The present invention relates to indole derivatives or benzimidazole derivatives, to processes for preparing such compounds, to pharmaceutical compositions comprising such compounds, and methods for the prophylaxis and therapy of a disease associated with an increased activity of I?B kinase comprising administering such compounds.Type: GrantFiled: June 6, 2007Date of Patent: July 15, 2014Assignee: Sanofi-Aventis Deutschland GmbHInventors: Olaf Ritzeler, Gerhard Jaehne
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Publication number: 20140194406Abstract: The present invention relates to alkynyl substituted pyrimidinyl-pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak and/or Src family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.Type: ApplicationFiled: July 18, 2012Publication date: July 10, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maria Gabriella Brasca, Jay Aaron Bertrand, Paola Gnocchi, Ilaria Motto, Marcella Nesi, Achille Panzeri, Paola Vianello
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Publication number: 20140191225Abstract: A biscarbazole derivative is represented by the following formula (1). A1 and A2 of the following formula (1) represent an aromatic hydrocarbon group having 6 to 30 ring carbon atoms or an aromatic heterocyclic group having 1 to 30 ring carbon atoms. However, at least one of A1 and A2 represents an aromatic heterocyclic group having 1 to 30 ring carbon atoms. Y1 to Y15 represent CR or a nitrogen atom. One of Y8 to Y11 is C (carbon atom) obtained by removing R from CR. The obtained C is bonded to L3. R each independently represents a hydrogen atom, an aromatic hydrocarbon group or the like. L1 to L3 represent a single bond or a divalent linking group. When L3 is a single bond and is bonded to Y11, L1 and L2 are divalent linking groups.Type: ApplicationFiled: August 15, 2012Publication date: July 10, 2014Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Tetsuya Inoue, Mitsunori Ito, Kazuki Nishimura, Kumiko Hibino
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Patent number: 8772305Abstract: The invention relates to new substituted pyridinyl-pyrimidines of formula 1 wherein ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O, wherein R1, R2, R4, R3, R5 and R6 are defined as in claim 1 and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.Type: GrantFiled: January 25, 2012Date of Patent: July 8, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Georg Dahmann, Dennis Fiegen, Martin Fleck, Matthias Hoffmann, Jasna Klicic, Stephen Peter East, Spencer Charles R. Napier, John Scott
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Patent number: 8772304Abstract: The present invention relates to compounds of formula (IA), (IB) and (IC): and pharmaceutically acceptable salts thereof, wherein R1-R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: October 26, 2011Date of Patent: July 8, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Stephane De Lombaert, Weimin Liu, Ho Yin Lo, Peter Allen Nemoto
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Patent number: 8772302Abstract: The present invention relates to novel GPR 119 agonists of the general Formula (I), their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, stereoisomers, and polymorphs. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds and to methods for treating one or both of diabetes and obesity using the compounds of the invention. The present invention is directed to G-protein coupled receptor (GPCR) agonists that are useful for the treatment of obesity, diabetes and related metabolic disorders.Type: GrantFiled: June 17, 2010Date of Patent: July 8, 2014Assignee: Cadila Healthcare LimitedInventors: Harikishore Pingali, Pandurang Zaware, Mukul Jain
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Patent number: 8772280Abstract: The present invention relates to substituted pyrrolyl-pyrimidines which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular MPS1. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: March 23, 2010Date of Patent: July 8, 2014Assignee: Nerviano Medical Sciences S.R.L.Inventors: Marina Caldarelli, Stefano Adele Nuvoloni, Francesca Quartieri
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Patent number: 8765731Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: GrantFiled: November 16, 2012Date of Patent: July 1, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: James A. Henderson, John Maxwell, Louis Vaillancourt, Mark Morris, Ronald Grey, Jr., Simon Giroux, Laval Chan Chun Kong, Sanjoy Kumar Das, Bingan Liu, Carl Poisson, Caroline Cadilhac, Monica Bubenik, T. Jagadeeswar Reddy, Guy Falardeau, Constantin Yannopoulos, Jian Wang, Oswy Z. Pereira, Youssef L. Bennani, Albert C. Pierce, Govinda Rao Bhisetti, Kevin M. Cottrell, Valerie Marone
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Patent number: 8765940Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphobType: GrantFiled: June 25, 2010Date of Patent: July 1, 2014Assignee: Amgen Inc.Inventors: Matthew Brown, Yi Chen, Timothy David Cushing, Felix Gonzalez Lopez De Turiso, Xiao He, Todd J. Kohn, Julia Winslow Lohman, Vatee Pattaropong, Jennifer Seganish, Youngsook Shin, Jillian L. Simard
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Publication number: 20140179698Abstract: The present invention relates to compounds of formula I or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, A, Q, W and X are as defined in the description. These compounds selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective native and/or mutant c-kit inhibitors.Type: ApplicationFiled: July 24, 2012Publication date: June 26, 2014Applicant: AB SCIENCEInventors: Abdellah Benjahad, Alain Moussy, Emmanuel Chevenier, Willy Picoul, Anne Lermet, Didier Pez, Jason Martin, Franck Sandrinelli
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Publication number: 20140179667Abstract: This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.Type: ApplicationFiled: December 18, 2013Publication date: June 26, 2014Applicant: PFIZER INC.Inventors: Martin Paul EDWARDS, Robert Arnold KUMPF, Pei-Pei KUNG, Indrawan James MCAPLINE, Sacha NINKOVIC, Eugene Yuanjin RUI, Scott Channing SUTTON, John Howard TATLOCK, Martin James WYTHES, Luke Raymond Zehnder
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Publication number: 20140179675Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.Type: ApplicationFiled: February 28, 2014Publication date: June 26, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
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Patent number: 8759332Abstract: 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. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.Type: GrantFiled: September 10, 2010Date of Patent: June 24, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Patent number: 8759347Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: GrantFiled: June 13, 2013Date of Patent: June 24, 2014Assignee: Janssen Pharmaceutica NVInventors: Carl R. Illig, Shelly K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson
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Patent number: 8759365Abstract: The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.Type: GrantFiled: December 1, 2008Date of Patent: June 24, 2014Assignee: Novartis AGInventors: Muneto Mogi, Toshio Kawanami, Ken Yamada, Kayo Yasoshima, Hidetomo Imase, Takahiro Miyake, Osamu Ohmori
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Patent number: 8759519Abstract: This invention provides novel crystalline forms of mono-HCl salts and a mono-HCl salt hydrate of JNJ-26481585, an inhibitor of histone deacetylases. The invention also relates to processes for production of these forms, to intermediates used in these processes, to pharmaceutical compositions comprising these forms, and to the use of these forms in medical treatment for instance as a medicine to inhibit proliferative conditions, such as cancer and leukemia.Type: GrantFiled: May 30, 2012Date of Patent: June 24, 2014Assignee: Janssen Pharmaceutica NVInventors: Julius W. J. Dickens, Ioannes Nicolaos Houpis, Yolande Lydia Lang, Carina Leys, Sigrid Carl Maria Stokbroekx, Johan Erwin Edmond Weerts
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Patent number: 8759366Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.Type: GrantFiled: December 15, 2010Date of Patent: June 24, 2014Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.Inventors: Kaleen Konrad Childers, Andrew M. Haidle, Michelle R. Machacek, Alan B. Northrup
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Publication number: 20140171430Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: April 20, 2012Publication date: June 19, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Michael A. Letavic, Rudolph A. Dale, Brad M. Savall, Brock T. Shireman, Devin Swanson
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Publication number: 20140167007Abstract: A pyrene-based compound and an organic light-emitting diode including the pyrene-based compound are provided.Type: ApplicationFiled: October 8, 2013Publication date: June 19, 2014Applicant: SAMSUNG DISPLAY CO., LTD.Inventors: Hye-Jin Jung, Seok-Hwan Hwang, Young-Kook Kim, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jun-Ha Park, Eun-Young Lee, Chang-Ho Lee, Jong-Hyuk Lee
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Publication number: 20140155401Abstract: The present invention relates to novel substituted 2,4?- and 3,4?-bipyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.Type: ApplicationFiled: February 7, 2014Publication date: June 5, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Peter NELL, Walter Hübsch, Barbara ALBRECHT-KÜPPER, Jörg KELDENICH, Andreas KNORR
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Publication number: 20140155421Abstract: The present invention relates to substituted pyrimidinyl-pyrrole compounds of formula (I) which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Janus kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.Type: ApplicationFiled: April 5, 2012Publication date: June 5, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maria Gabriella Brasca, Tiziano Bandiera, Jay Aaron Bertrand, Paola Gnocchi, Danilo Mirizzi, Marcella Nesi, Achille Panzeri
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Publication number: 20140155413Abstract: The present invention is directed to compounds of formula I and 1a: which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.Type: ApplicationFiled: July 6, 2012Publication date: June 5, 2014Inventors: Barbara Hanney, Peter Manley, Michael T. Rudd, John M. Sanders, Shawn J. Stachel, Darrell Henze