Nitrogen Bonded Directly To Ring Carbon Of The 1,3-diazine Ring Of The Bicyclo Ring System Patents (Class 514/264.11)
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Publication number: 20150031672Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: October 10, 2014Publication date: January 29, 2015Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
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Publication number: 20150031693Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of Fragile X syndrome.Type: ApplicationFiled: November 2, 2012Publication date: January 29, 2015Applicant: AFRAXIS HOLDINGS, INC.Inventors: John C. Mckew, Wenwei Huang, David Campbell, Sergio G. Durön, Mark Behnke, Min Shen
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Publication number: 20150031674Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd, Re, n, r, s and t are as defined herein and which compounds are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.Type: ApplicationFiled: July 25, 2014Publication date: January 29, 2015Applicant: GENENTECH, INC.Inventors: Joachim Rudolph, Lewis J. Gazzard, James J. Crawford, Chudi Ndubaku, Joy Drobnick, Wendy Lee
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Publication number: 20150025090Abstract: The present application relates to novel substituted azabicycles, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: March 5, 2013Publication date: January 22, 2015Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Alexandros Vakalopoulos, Dieter Lang, Frank Wunder, Walter Hübsch, Michael Hahn
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Publication number: 20140377285Abstract: The present invention provides for methods and pharmaceutical compositions for treating disorders using treatment regimens involving multiple agents. In one aspect, a method of treatment is provided resulting in reduced toxicity and/or synergistic effect by administration according to a described dosing schedule.Type: ApplicationFiled: November 8, 2012Publication date: December 25, 2014Inventors: Yi Liu, Shunyou Wang, Matthew R. Janes, Lucy Lan, Pingda Ren, Christian Rommel
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Publication number: 20140378481Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.Type: ApplicationFiled: June 27, 2014Publication date: December 25, 2014Applicant: BLUEPRINT MEDICINES CORPORATIONInventors: Neil Bifulco, JR., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu
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Patent number: 8912203Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders.Type: GrantFiled: June 9, 2011Date of Patent: December 16, 2014Assignee: Afraxis Holdings, Inc.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
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Publication number: 20140364430Abstract: Provided herein are PAK inhibitors.Type: ApplicationFiled: August 14, 2014Publication date: December 11, 2014Inventors: Jay LICHTER, David CAMPBELL, Benedikt VOLLRATH, Sergio G. DURÓN
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Patent number: 8901137Abstract: The invention provides compounds of Formula I: that inhibit the PI3Ks and mTOR that are useful in the treatment of cancer in humans when used in combination with autophagy inhibitors.Type: GrantFiled: February 9, 2011Date of Patent: December 2, 2014Assignee: Exelixis, Inc.Inventors: Dana T. Aftab, Wolfgang M. Korn, Olga K. Mirzoeva
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Publication number: 20140350031Abstract: This invention relates to piperidino-pyhmidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.Type: ApplicationFiled: February 7, 2013Publication date: November 27, 2014Inventors: David Craig Mc Gowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers, Mourad Daoubi Khamlichi
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Publication number: 20140350020Abstract: The present application relates to novel fused pyrimidines and triazines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: July 5, 2011Publication date: November 27, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Walter Kroh, Lars Bärfacker
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Patent number: 8889696Abstract: Compounds useful as antiproliferative agents according to Formula (I), wherein n, A, R1, R2, and Ar1 are as defined herein, and salts thereof; antibody conjugates, pharmaceutical compositions, methods of treatment, and synthetic methods are provided.Type: GrantFiled: December 17, 2010Date of Patent: November 18, 2014Assignee: Temple University—Of The Commonwealth System Of Higher EducationInventors: E. Premkumar Reddy, M. V. Ramana Reddy
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Patent number: 8877763Abstract: Compounds of Formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to a subject a therapeutically effective amount of the compound of Formula (I).Type: GrantFiled: March 15, 2013Date of Patent: November 4, 2014Assignees: Genosco, Oscotec, Inc.Inventors: Hong Woo Kim, Hee Kyu Lee, Ho-Juhn Song, Jaekyoo Lee, Jong Sung Koh, Jung-Ho Kim, Se Won Kim, In Yong Lee
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Publication number: 20140323477Abstract: Compounds having the formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, X1, X2, and Ar are as defined herein, are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders using such compounds.Type: ApplicationFiled: April 30, 2014Publication date: October 30, 2014Applicant: GENENTECH, INC.Inventors: James J. CRAWFORD, Wendy LEE, Joachim RUDOLPH
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Publication number: 20140323478Abstract: Compounds having the formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, X1, X2, and Ar are as defined herein, are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.Type: ApplicationFiled: April 30, 2014Publication date: October 30, 2014Applicant: AFRAXIS HOLDINGS, INC.Inventors: Sergio DURÓN, David CAMPBELL, Chudi NDUBAKU, Joachim RUDOLPH
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Publication number: 20140323464Abstract: Provided herein are kinase inhibiting compounds and methods of using the same.Type: ApplicationFiled: May 16, 2012Publication date: October 30, 2014Inventors: John William Taunton, JR., Kenneth Albert Brameld, David Michael Goldstein, Jesse Mcfarland, Shyam Krishnan, Jonathan Choy
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Patent number: 8859545Abstract: Tetrahydronaphthyridine and tetrahydropyrido[4,3-d]pyrimidine compounds are disclosed that have formula 1: where A, B, L, N, R1, R3, R4?, Y and Z are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, respiratory conditions, and others.Type: GrantFiled: March 1, 2010Date of Patent: October 14, 2014Assignee: Evotec AGInventors: Michael G. Kelly, John Kincaid, Carl J. Kaub
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Publication number: 20140302012Abstract: The invention provides a method for treating cancers including hematologic malignancies comprising administering a compound of Formula (I): in combination with one or both of bendamustine and rituximab.Type: ApplicationFiled: June 15, 2012Publication date: October 9, 2014Applicants: Sanofi, Exelixis, Inc.Inventors: Arthur DeCillis, Joanne Lager, Tal Zaks
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Publication number: 20140296265Abstract: The invention provides a method for treating cancers including hematologic malignancies comprising administering a compound of formula I:Type: ApplicationFiled: April 27, 2012Publication date: October 2, 2014Applicants: Sanofi, Exelixis, Inc.Inventors: Arthur DeCillis, Joanne Lager, Tal Zaks
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Publication number: 20140296233Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: March 14, 2014Publication date: October 2, 2014Applicants: Sanofi, Celgene Avilomics Research, Inc.Inventors: Laura Akullian D'Agostino, Robert Tjin Tham Sjin, Deqiang Niu, Joseph John McDonald, Zhendong Zhu, Haibo Liu, Hormoz Mazdiyasni, Russell C. Petter, Juswinder Singh, Matthieu Barrague, Alexandre Gross, Mark Munson
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Patent number: 8846656Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: July 19, 2012Date of Patent: September 30, 2014Assignee: Novartis AGInventors: Christopher Michael Adams, Veronique Darsigny, Alec Nathanson Flyer, Christine Fang Gelin, Timothy Brian Hurley, Nan Ji, Rajeshri Ganesh Karki, Toshio Kawanami, Erik Meredith, Chang Rao, Michael H. Serrano-Wu, Catherine Fooks Solovay
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Publication number: 20140275120Abstract: The present invention is directed to a compound of Formula (I) The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Manuel Jesus Alcazar Vaca, Jose Ignacio Andres Gil, Michael A. Letavic, Dale A. Rudolph, Brock T. Shireman, Brice M. Stenne, Jeannie M. Ziff
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Patent number: 8829011Abstract: Certain 2-aminopyrimidine compounds of formula (I) are serotonin receptor modulators useful in the treatment of diseases mediated by serotonin receptors.Type: GrantFiled: October 29, 2009Date of Patent: September 9, 2014Assignee: Janssen Pharmaceutica NVInventors: Nicholas I. Carruthers, Gregor J. MacDonald, Brock T. Shireman, Vi T. Tran
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Publication number: 20140249131Abstract: The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer.Type: ApplicationFiled: February 26, 2014Publication date: September 4, 2014Inventors: Andrew TASKER, Ryan WURZ, Liping H. PETTUS, Bradley J. HERBERICH
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Publication number: 20140228355Abstract: The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.Type: ApplicationFiled: February 11, 2013Publication date: August 14, 2014Applicants: University of Medicine and Dentistry New Jersey Medical School, Philadelphia Health & Education Corporation d/b/a Drexel University College of MedicineInventors: Philadelphia Health & Education Corporation d/b/a Drexel University College of Medicine, University of Medicine and Dentistry New Jersey Medical School
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Publication number: 20140228380Abstract: The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.Type: ApplicationFiled: August 2, 2013Publication date: August 14, 2014Applicants: University of Medicine and Dentistry New Jersey Medical School, Philadelphia Health & Education Corporation d/b/a Drexel University College of MedicineInventors: Sandhya Kortagere, Eldo V. Kuzhikandahil
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Patent number: 8802697Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.Type: GrantFiled: July 11, 2013Date of Patent: August 12, 2014Assignee: Blueprint Medicines CorporationInventors: Neil Bifulco, Jr., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu
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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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Publication number: 20140213595Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: September 4, 2013Publication date: July 31, 2014Applicant: ABBVIE INC.Inventors: David A. DEGOEY, Pamela L. DONNER, Warren M. KATI, Charles W. HUTCHINS, Allan C. KRUEGER, John T. RANDOLPH, Christopher E. MOTTER, Preethi KRISHNAN, Neeta C. MISTRY, Tami J. PILOT-MATIAS, Sachin V. PATEL, Xiaoyan LI, Todd N. SOLTWEDEL, Lissa T. NELSON
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Publication number: 20140213574Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: April 16, 2014Publication date: July 31, 2014Applicant: Celgene Avilomics Research, Inc.Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
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Publication number: 20140213601Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: September 9, 2013Publication date: July 31, 2014Applicant: ABBVIE INC.Inventors: David A. DEGOEY, Pamela L. DONNER, Warren M. KATI, Charles W. HUTCHINS, Mark A. MATULENKO, Tammie K. JINKERSON, Ryan G. KEDDY
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Publication number: 20140200231Abstract: The present invention provides compounds of the Formula I: wherein X is a bond or CH2; R is selected from the group consisting of R1 and R2 are each independently selected from the group consisting of CH and N; R3 is H or CH3; R4 is H or CH3; L is selected from the group consisting of —O(CH2)3—, —C(O)NH(CH2)2—, —CH2C(O)NH(CH2)2—, —(CH2)3N(C(O)CH3)CH2—, —(CH2)2N(C(O)CH3)CH2—, —(CH2)3NH—, (CH2)2OCH2—, —(CH2)4—, —(CH2)2NHCH2—, —(CH2)3O—, and —CH2O(CH2)2—; or a pharmaceutically acceptable salt thereof. Compounds of this invention are autotaxin inhibitors.Type: ApplicationFiled: January 7, 2014Publication date: July 17, 2014Applicant: Eli Lilly and CompanyInventors: Thomas James Beauchamp, Yen Dao, Spencer Brian Jones, Bryan Hurst Norman, Lance Allen Pfeifer
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Publication number: 20140187559Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.Type: ApplicationFiled: December 26, 2013Publication date: July 3, 2014Applicant: BLUEPRINT MEDICINES CORPORATIONInventor: Chandrasekhar V. Miduturu
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Patent number: 8759362Abstract: The invention relates to compounds of formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof.Type: GrantFiled: October 22, 2009Date of Patent: June 24, 2014Assignee: Purdue Pharma L.P.Inventor: Laykea Tafesse
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Publication number: 20140163005Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Publication number: 20140163026Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders or neurofibromatosis. Also described herein are methods of utilizing PAK inhibitors for the treatment of cancer.Type: ApplicationFiled: April 9, 2012Publication date: June 12, 2014Applicant: Afraxis Holdings, Inc.Inventors: David Campbell, Sergio G. Duron
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Publication number: 20140163006Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Publication number: 20140163003Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Publication number: 20140163007Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Publication number: 20140163004Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Patent number: 8741911Abstract: The present invention provides a pyrido[2,3-d]pyrimidine compound, or a pharmaceutically acceptable salt thereof, that inhibits Raf and, therefore, may be useful in treating cancer.Type: GrantFiled: March 5, 2013Date of Patent: June 3, 2014Assignees: Eli Lilly and Company, Deciphera Pharmaceuticals, LLCInventors: Matthew Carl Allgeier, Daniel L. Flynn, Michael D. Kaufman, Phenil J. Patel, Craig D. Wolfangel
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Patent number: 8741910Abstract: Compounds of Formula I are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the Formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the Formula I.Type: GrantFiled: November 16, 2009Date of Patent: June 3, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Linda L. Brockunier, Jian Guo, Emma R. Parmee, Subharekha Raghavan, Keith Rosauer, Darby Schmidt, John E. Stelmach
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Patent number: 8729089Abstract: Pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (I): wherein: R4 is hydrogen, and R1, R2 and R3 together provide a specific substitution pattern, pharmaceutical acceptable addition salts, stereochemical isomeric forms, N-oxides, solvates and pro-drugs thereof, are useful in the treatment of hepatitis C.Type: GrantFiled: December 21, 2007Date of Patent: May 20, 2014Assignee: Gilead Sciences, Inc.Inventors: Steven S. Bondy, Chien-hung Chou, William John Watkins, Lee S. Chong, Jennifer R. Zhang, Ruchika Mishra
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Patent number: 8722692Abstract: Provided herein are a novel class of compounds of Formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated Syk kinase activity.Type: GrantFiled: July 30, 2010Date of Patent: May 13, 2014Inventors: Jianwei Che, Qiang Ding, Xiaohui He, Hong Liu, Yahua Liu, Pierre-Yves Michellys, Barun Okram, Xu Wu, Kunyong Yang, Xuefeng Zhu
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Patent number: 8716302Abstract: The present invention provides isoquinoline, tetrahydroisoquinoline and tetrahydropyridopyrimidine compounds that induce cell death by apoptosis and uses of the compounds in medicine, especially their use for treating cancer and other diseases.Type: GrantFiled: April 28, 2010Date of Patent: May 6, 2014Assignee: Queen Mary & Westfield CollegeInventor: Finbarr Edward Cotter
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Publication number: 20140113915Abstract: The invention provides novel substituted pyridopyrimidines represented by Formula I or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of the phosphoinositide 3? OH kinase family (PI3K) for the treatment of inflammatory diseases, cancer, cardiovascular diseases, allergy, asthma and autoimmune disorders.Type: ApplicationFiled: December 20, 2013Publication date: April 24, 2014Applicant: THE ASAN FOUNDATIONInventors: Gilnam Lee, Chul Soo Lim, Han Won Cho, Jeongbeob Seo, Albert C. Gyorkos, Suk Young Cho, Eun Kyung Choi, Choung Soo Kim, Jung Jin Hwang
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Publication number: 20140113882Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R7, R8, R9, G, and X are as defined herein. This application further describes compositions comprising the same. Compounds of formula (I) and their salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.Type: ApplicationFiled: September 27, 2013Publication date: April 24, 2014Applicants: Cancer Research Technology Limited, Cephalon, Inc.Inventors: Henry J. Breslin, Bruce D. Dorsey, Benjamin J. Dugan, Katherine M. Fowler, Robert L. Hudkins, Eugen F. Mesaros, Nathaniel J.T. Monck, Emma L. Morris, Ikeoluwa Olowoye, Gregory R. Ott, Gregoire A. Pave, Jonathan R. Roffey, Christelle N. Soudy, Ming Tao, Craig A. Zificsak, Allison L. Zulli
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Patent number: 8703781Abstract: A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl;-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, with a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophen-}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf is beneficial, eg. cancer.Type: GrantFiled: October 15, 2010Date of Patent: April 22, 2014Assignee: GlaxoSmithKline LLCInventors: Melissa Dumble, Rakesh Kumar, Sylvie Laquerre, Peter Lebowitz
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Publication number: 20140088056Abstract: The invention provides for a method of inhibiting interferon-beta gene expression and/or reducing the level of interferon-beta in a cell by contacting the cell with a Na+, Ca2+, or K+ ion-channel modulator. The invention also provides for a method of treating a disease or disorder characterized by elevated interferon beta levels or elevated levels of interferon-beta gene expression. Additionally, the invention provides a method for treating pathogenic or non-pathogenic infections.Type: ApplicationFiled: September 28, 2011Publication date: March 27, 2014Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Junqiang Ye, Shuibing Chen, Tom Maniatis
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Publication number: 20140088100Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.Type: ApplicationFiled: July 11, 2013Publication date: March 27, 2014Applicant: BLUEPRINT MEDICINESInventors: Neil Bifulco, JR., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu