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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Patent number: 8653091Abstract: Fused heterocyclic compounds are provided according to formula 1a or 1b: where R1, R2, and R3 are as defined herein. Provided 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, cognitive disorders, anxiety, depression, and others.Type: GrantFiled: March 31, 2008Date of Patent: February 18, 2014Assignee: Evotec AGInventors: Zhi-Liang Wei, John Kincaid, Michael G. Kelly, Donogh John Roger O'Mahony, Carl Kaub
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Patent number: 8653092Abstract: The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.Type: GrantFiled: July 1, 2011Date of Patent: February 18, 2014Assignee: Novartis AGInventors: Nigel Graham Cooke, Paulo Fernandes Gomes Dos Santos, Nadege Graveleau, Christina Hebach, Klemens Högenauer, Gregory Hollingworth, Alexander Baxter Smith, Nicolas Soldermann, Frank Stowasser, Ross Strang, Nicola Tufilli, Anette Von Matt, Romain Wolf, Frédéric Zecri
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Publication number: 20140044788Abstract: A solid oral dosage pharmaceutical formulation of (R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one or its salt; and a surfactant or an acid.Type: ApplicationFiled: October 22, 2013Publication date: February 13, 2014Applicant: Novartis AGInventors: Daya Verma, Yue (Helen) Teng, Rajinder Singh, Dan Thompson
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Publication number: 20140038991Abstract: The present invention is directed to compounds of the Formula I as well as pharmaceutically acceptable salts, hydrates, isomers, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula I, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.Type: ApplicationFiled: August 6, 2012Publication date: February 6, 2014Applicant: Astar Biotech LLCInventors: Chunrong Yu, Yong Huang
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Publication number: 20140038957Abstract: This invention relates to pyrrolopyrimidine derivatives of formula (I): where R1, X, p, R4, R2 and R3 are as defined herein, and their use as pharmaceuticals.Type: ApplicationFiled: December 15, 2011Publication date: February 6, 2014Inventors: David R. Witty, David Norton, Jason Paul Tierney, Ghislaine Lorthioir, Mairi Sime, Karen Louise Philpott
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Patent number: 8637531Abstract: This invention provides pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (I), wherein: R1 is amino, R4 is hydrogen, and 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 24, 2007Date of Patent: January 28, 2014Assignee: Gilead Sciences, Inc.Inventors: Steven S. Bondy, William J. Watkins, Lee S. Chong, Piet Andre Maurits Maria Herdewijn, Steven Cesar Alfons De Jonghe
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Publication number: 20140024661Abstract: A group of fused two ring pyrimidine compounds having a heterocycles substituent at the 2 position and a substituted amine at the 4 position as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the pyrimidine and other ring are disclosed. In addition a group of quinazoline compounds having similar substituents at the 2 and 4 positions as well as at other positions are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity.Type: ApplicationFiled: July 19, 2013Publication date: January 23, 2014Applicant: Cleave Biosciences, Inc.Inventors: Han-Jie Zhou, Francesco Parlati
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Patent number: 8633204Abstract: The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I), and to salts thereof, their synthesis, and their use as inhibitors of phosphoinositide 3-kinase alpha (PI3-K?).Type: GrantFiled: August 16, 2012Date of Patent: January 21, 2014Assignee: Pfizer Inc.Inventors: Hengmiao Cheng, Dilip Bhumralkar, Klaus Ruprecht Dress, Jacqui Elizabeth Hoffman, Mary Catherine Johnson, Robert Steven Kania, Phuong Thi Quy Le, Mitchell David Nambu, Mason Alan Pairish, Michael Bruno Plewe, Khanh Tuan Tran
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Publication number: 20130343988Abstract: The invention is directed to Compounds of Formula (I). The invention provides compounds that inhibit, regulate, and/or modulate P13K that are useful in the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: January 3, 2013Publication date: December 26, 2013Applicant: Exelixis, Inc.Inventor: Exelixis, Inc.
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Publication number: 20130345192Abstract: The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same.Type: ApplicationFiled: October 28, 2011Publication date: December 26, 2013Applicants: SUNESIS PHARMACEUTICALS, INC., BIOGEN IDEC MA INC.Inventors: Brian T. Hopkins, Daniel Scott, Patrick Conlon, Tracy J. Jenkins, Noel Powell, Bing Guan, Julio H. Cuervo, Deping Wang, Art Taveras
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Publication number: 20130345164Abstract: This invention concerns methods of identifying treatments for treating various disorders and related computer products and systems. Also disclosed are methods for treating cellular proliferative disorders and use of compounds identified for such treatment.Type: ApplicationFiled: April 21, 2011Publication date: December 26, 2013Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventors: Alexei Vazquez, Darren Carpizo, Arnold Levine
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Publication number: 20130338153Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.Type: ApplicationFiled: June 10, 2011Publication date: December 19, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
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Publication number: 20130338140Abstract: Compounds having the formula I wherein Z, Z1 Z2 Z, R3a, R3b and Rb and as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.Type: ApplicationFiled: February 28, 2012Publication date: December 19, 2013Applicants: Genetech, Inc., Array BioPharma Inc.Inventors: James F. Blake, Huifen Chen, Mark Joseph Chcarelli, Jason Demeese, Rustam Garrey, John J. Gaudino, Robert J. Kaus, Gabrielle R. Kolakowski, Allison L. Marlow, Peter J. Mohr, Li Ren, Jacob Schwartz, Christopher S. Siedem, Allen A. Thomas, Eli Wallace, Steven Mark Wenglowsky
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Publication number: 20130324516Abstract: The invention provides novel compounds having the general formula: wherein A, R1, R2 and R3 are as defined herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: May 31, 2013Publication date: December 5, 2013Inventors: Huifen Chen, Terry Crawford, Seth F. Harris, Steven R. Magnuson, Chudi Ndubaku, Lan Wang
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Patent number: 8586505Abstract: Novel 4-(3-butynyl)aminopyrimidine derivatives represented by general formula [I] are useful as pest control agents. In general formula [I], R1 is a mono- or bi-cyclic ring which may contain 0 to 3 heteroatoms, for example, phenyl or oxazolyl; R2 is a hydrogen atom, —R, —OR, —C(O)OR, —C(O)NHR, —CONR2 (wherein R is straight-chain or branched C1-8 alkyl, or the like), hydroxyalkyl, or the like; R3 is a hydrogen atom, a halogen atom, acyloxy represented by (straight-chain or branched C1-8 aliphatic hydrocarbon group) —CO—O—, or the like; and R4 is a hydrogen atom, a halogen atom, C1-6 alkyl, or the like, or alternatively, R4 and R3 together with the carbon atoms on the pyrimidine ring may form a thiophene ring, a pyrrole ring, an imidazole ring, a benzene ring, a pyrimidine ring, a furan ring, a pyrazine ring, or a pyrrolidine ring.Type: GrantFiled: July 15, 2010Date of Patent: November 19, 2013Assignee: SDS Biotech K. K.Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Ryutaro Katsuki, Tomoko Muraki
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Publication number: 20130296333Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).Type: ApplicationFiled: July 9, 2013Publication date: November 7, 2013Inventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
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Publication number: 20130296338Abstract: A series of quinoline and quinoxaline derivatives comprising a fluorinated ethyl side-chain, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: ApplicationFiled: September 2, 2011Publication date: November 7, 2013Applicant: UCB PHARMA S.A.Inventors: Andrew Harry Parton, Mezher Hussein Ali, Daniel Christopher Brookings, Julien Alistair Brown, Daniel James Ford, Richard Jeremy Franklin, Barry John Langham, Judi Charlotte Neuss, Joanna Rachel Quincey
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Publication number: 20130296271Abstract: Agri-horticultural pest control compositions having outstanding control effect on pests, in particular, agri-horticultural pests, which comprise as active ingredients one or more 4-(3-butynyl)aminopyrimidine derivatives represented by the general formula [I], namely, where R1 is typically selected from among: a) phenyl c) —SiR5R6R7 (R5, R6, and R7 which may be the same or different represent a linear or branched alkyl having 1-6 carbon atoms, a linear or branched haloalkyl having 1-3 carbon atoms which is substituted by one halogen atom, a linear or branched cyanoalkyl having 1-3 carbon atoms which is substituted by one cyano group, and phenyl); d) hydropgen atom; R2 typically represents a hydrogen atom; R3 typically represents a hydrogen atom; R4 represents a hydrogen atom and one or more agri-horticultural pest control compounds selected from among agri-horticultural antimicrobial compounds, say, multi-site contact active compouns, nucleic acids synthesis inhibitory active compounds, mitosis and cellType: ApplicationFiled: December 27, 2011Publication date: November 7, 2013Applicant: SDS Biotech K.K.Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Tomoko Muraki, Ryutaro Katsuki
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Patent number: 8569316Abstract: The present invention encompasses compounds of general formula (1), wherein the groups R1 to R4, X1, X2, X3, X4, X5, Q, L1 and L2 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, as well as pharmaceutical preparations and formulations of these compounds.Type: GrantFiled: February 17, 2010Date of Patent: October 29, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Peter Ettmayer, Andreas Mantoulidis
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Publication number: 20130274274Abstract: 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: ApplicationFiled: March 15, 2013Publication date: October 17, 2013Inventors: Hong Woo Kim, Hee Kyu Lee, Ho-Juhn Song, Jaekyoo Lee, Jong Sung Koh, Youngsam Kim, Jung-Ho Kim, Se Won Kim, In Yong Lee
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Publication number: 20130266563Abstract: Selenophene compounds of formula (I) are described herein. In the compounds of Formula (I), ring A is a 6-membered aromatic fused ring, optionally containing one, two or three nitrogen atoms; a 5-membered heteroaromatic fused ring; or a mono- or bicyclic saturated heterocyclic fused ring having at least one ring member selected from the group consisting of N, O, S, SO and SO2; Y in ring B is nitrogen or substituted carbon; X is NR6, O, S, S(O), or S(O)2. R1, R2, R3, R4, and R6 are defined in the specification. Selenophene compounds of formula (I) may be used in methods of treating cell proliferative disorders, particularly cancer. Pharmaceutical compositions containing selenophene compounds of formula (I) may be used for treatment, inhibition, or control of cancer.Type: ApplicationFiled: May 17, 2013Publication date: October 10, 2013Inventors: Ganga Raju Gokaraju, Sudhakar Kasina, Venkateswarlu Somepalli, Rama Raju Gokaraju, Venkata Kanaka Ranga Raju Gokaraju, Kiran Bhupathiraju, Trimurtulu Golakoti, Krishanu Sengupta, Venkata Krishna Raju Alluri
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Patent number: 8546405Abstract: 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: GrantFiled: December 22, 2009Date of Patent: October 1, 2013Assignee: Abbott LaboratoriesInventors: 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: 20130252977Abstract: 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: ApplicationFiled: March 5, 2013Publication date: September 26, 2013Applicants: DECIPHERA PHARMACEUTICALS, LLC, ELI LILLY AND COMPANYInventors: Matthew Carl Allgeier, Daniel L. Flynn, Michael D. Kaufman, Phenil J. Patel, Craig D. Wolfangel
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Patent number: 8541424Abstract: 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: GrantFiled: December 22, 2009Date of Patent: September 24, 2013Assignee: Abbott LaboratoriesInventors: 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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Patent number: 8536187Abstract: Pyrido(3,2-d)pyrimidine derivatives represented by the structural formula (Ia): wherein, R1, R2 and R3 are defined herein, pharmaceutical acceptable addition salts, stereochemical isomeric forms, N-oxides, solvates and pro-drugs thereof, for use in the treatment of hepatitis C.Type: GrantFiled: July 1, 2009Date of Patent: September 17, 2013Assignee: Gilead Sciences, Inc.Inventors: Eda Canales, Lee S. Chong, Michael O' Neil Hanrahan Clarke, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael L. Mitchell, William J. Watkins, Jennifer R. Zhang
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Publication number: 20130237537Abstract: The present invention relates to a method of treating ophthalmic diseases and conditions, e.g. diabetic retinopathy, age-related macular degeneration, retinopathy of prematurity, etc., in a subject comprising administering to said subject a therapeutically effective amount of at least one compound of formula I or a prodrug, pharmaceutically acceptable salt, racemic mixtures or enantiomers of said compound. The compounds of formula I are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: March 12, 2013Publication date: September 12, 2013Applicant: ALLERGAN, INC.Inventors: Clarence E. Hull, III, Thomas C. Malone
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Publication number: 20130237538Abstract: The present invention relates to compounds of formulae I and II wherein the variables are as defined herein. These compounds are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: March 12, 2013Publication date: September 12, 2013Applicant: ALLERGAN, INC.Inventors: Clarence E. Hull, III, Thomas C. Malone
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Publication number: 20130225589Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, R4, and B are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: February 22, 2013Publication date: August 29, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
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Publication number: 20130225575Abstract: Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from certain neurological conditions.Type: ApplicationFiled: June 16, 2011Publication date: August 29, 2013Applicant: AFRAXIS, INC.Inventors: Jay Lichter, David Campbell, Sergio G. Duron, Benedikt Vollrath
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Patent number: 8518958Abstract: 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: GrantFiled: October 16, 2007Date of Patent: August 27, 2013Assignee: Forma Therapeutics, Inc.Inventors: Krishna K. Murthi, Rebecca Casaubon, Arthur F. Kluge, Chase C. Smith, Joachim Vogt
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Patent number: 8513265Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, A, B, D, E, G, Y, Z, R1 and R2 are defined herein.Type: GrantFiled: October 10, 2012Date of Patent: August 20, 2013Assignee: Bristol-Myers Squibb CompanyInventors: John M. Fevig, Dean A. Wacker
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Patent number: 8513266Abstract: The present invention provides methods of treating cancer by administering a compound of Formula I, optionally as a pharmaceutically acceptable salt, solvate and/or hydrate thereof, in combination with other cancer treatments.Type: GrantFiled: April 9, 2008Date of Patent: August 20, 2013Assignee: Exelixis, Inc.Inventors: Peter Lamb, David Matthews
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Publication number: 20130210819Abstract: Compounds of the formula I in which R, X, L2 and A1-A6 have the meanings indicated in Claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours.Type: ApplicationFiled: September 22, 2011Publication date: August 15, 2013Applicant: MERCK PATENT GMBHInventor: Markus Klein
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Publication number: 20130210771Abstract: This invention provides a combination of antagonists of the hedgehog signaling pathway with a BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with protein tyrosine kinases such as, for example, Src, BCR-ABL and c-kit.Type: ApplicationFiled: February 13, 2013Publication date: August 15, 2013Applicant: IRM LLCInventor: Novartis AG
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Publication number: 20130210824Abstract: The present application relates to novel substituted fused imidazoles and pyrazoles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof producing medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: January 8, 2013Publication date: August 15, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventor: BAYER INTELLECTUAL PROPERTY GMBH
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Publication number: 20130184253Abstract: 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: ApplicationFiled: July 19, 2012Publication date: July 18, 2013Applicant: 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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Patent number: 8486952Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: GrantFiled: July 28, 2010Date of Patent: July 16, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Richard E. Olson, Jianliang Shi, Lorin A. Thompson, III, Yong-Jin Wu, Li Xu, Yunhui Zhang, Dmitry S. Zuev
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Publication number: 20130178462Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: ApplicationFiled: March 5, 2013Publication date: July 11, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Publication number: 20130172371Abstract: 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: ApplicationFiled: February 9, 2011Publication date: July 4, 2013Applicant: EXELIXIS, INCInventors: Dana T. Aftab, Wolfgang M. Korn, Olga K. Mirzoeva
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Publication number: 20130172372Abstract: The present application relates to novel fused 4-aminopyrimidines, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: July 5, 2011Publication date: July 4, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li
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Publication number: 20130158043Abstract: Provided herein are methods of utilizing PAK inhibitors for the treatment of cancer. Further provided herein are compounds and formulations utilized for the treatment of cancer.Type: ApplicationFiled: December 7, 2012Publication date: June 20, 2013Applicant: AFRAXIS, INC.Inventor: Afraxis, Inc.
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Publication number: 20130143899Abstract: The invention provides a novel class of compounds of Formula (I) (wherein A, Y, R2, R3, R4 and R5 are defined in the summary of the invention), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.Type: ApplicationFiled: February 4, 2011Publication date: June 6, 2013Inventors: Shifeng Pan, John E. Tellew, Yongqin Wan, Yongping Xie, Xing Wang, Xia Wang, Shenlin Huang, Zuosheng Liu, Qiong Zhang
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Publication number: 20130143895Abstract: The present invention relates to substituted aromatic bicyclic compounds containing pyrimidine and pyridine rings of formula (I) having the structure as well as pharmaceutically acceptable salts thereof. The compounds of the present invention are useful as tyrosine kinase inhibitors, preferably SRC family kinases (SFKs) inhibitors, in particular as multi SFK/JAK. kinases inhibitors and even preferably as dual c-SRC/JAK kinases inhibitors, thereby inhibiting the STAT3 activation and therefore abnormal growth of particular cell types. Notably, the compounds of the present invention are useful for the treatment or inhibition of certain diseases that are the result of deregulation of STAT3.Type: ApplicationFiled: January 14, 2013Publication date: June 6, 2013Inventors: Andrès Mc Allister, Maximilien Murone, Saumitra Sengupta, Shankar Jayaram Shetty
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Patent number: 8455504Abstract: The present invention provides a method of treating diseases or disorders benefiting from inactivating or down-regulating the activity of the capsaicin receptor in a mammal by inhibiting the activity of the capsaicin receptor. The present invention also provides a method of treating obesity and obesity-related diseases and disorders in a mammal by inhibiting the activity of the capsaicin receptor.Type: GrantFiled: December 22, 2010Date of Patent: June 4, 2013Assignee: Xenia PharmaInventors: Dorte Xenia Gram, Anker Jon Hansen
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Publication number: 20130131058Abstract: Compounds according to Formula (I), as well salts thereof: wherein R1 and R2 are as defined herein, are useful as antiproliferative agents and kinase inhibitors. Synthetic methods for preparing the compounds of Formula (I) are also provided.Type: ApplicationFiled: July 21, 2011Publication date: May 23, 2013Inventors: E. Premkumar Reddy, M. V. Ramana Reddy
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Publication number: 20130116263Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of cell proliferative disorders and/or CNS disorders.Type: ApplicationFiled: November 2, 2012Publication date: May 9, 2013Applicant: AFRAXIS, INC.Inventor: AFRAXIS, INC.
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Publication number: 20130102590Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, R4, and B are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: October 18, 2012Publication date: April 25, 2013Applicant: AbbVie IncInventor: AbbVie Inc.
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Publication number: 20130085133Abstract: The present disclosure relates to novel compounds of formulas (1) through (19) and to a method for treating humans infected with a virus including various respiratory viruses such as members of the Paramyxoviridae family (respiratory syncytial virus (RSV), human metapneumovirus (HMPV), human parainfluenza virus (HPIV), measles virus, and mumps virus) with a compound of formulas (1) through (19). The present disclosure also relates to a cytopathic effect (CPE)-based assay that will assess virus-induced CPE for screening of compounds for treating viral diseases or inhibiting a virus.Type: ApplicationFiled: February 8, 2011Publication date: April 4, 2013Applicant: Sourthern Research Institute Office of Commercialization and Intellectual Prop.Inventors: Bill Severson, Dong Hong Chung, Colleen B. Jonsson, Ellie Lucile White, Lynn Rasmussen, Clinton Boykin Maddox, Subramaniam Ananthan, Ashish K. Pathak, Joseph A. Maddry
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Patent number: 8404677Abstract: The present invention provides a new group of protein kinase inhibitors, pyrido[4,3,-d]pyrimidin-5-one derivatives, and pharmaceutically acceptable salts thereof that are useful for intreating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrido[4,3,-d]pyrimidin-5-one derivatives.Type: GrantFiled: October 29, 2010Date of Patent: March 26, 2013Assignees: Genosco, Oscotec, Inc.Inventors: Hong Woo Kim, Jong Sung Koh, Jaekyoo Lee, Ho-Juhn Song, Youngsam Kim, Hee Kyu Lee, Jang-Sik Choi, Sun-Hee Lim, Sunhwa Chang
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Patent number: 8404695Abstract: This application discloses novel pyrimidinyl pyridone derivatives according to Formula I, wherein R1, R2, and R3 are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of Formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of Formula I to a subject in need thereof.Type: GrantFiled: October 22, 2009Date of Patent: March 26, 2013Assignee: Roche Palo Alto LLCInventors: Genevieve N. Boice, Leyi Gong, Kristen Lynn McCaleb, Wylie Solang Palmer