Plural Hetero Atoms In The Bicyclo Ring System Patents (Class 514/300)
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Publication number: 20140235666Abstract: The present invention relates to substituted imidazo [1,2-a]pyridines of formula I where R is —CH2COOH or —COOH, which inhibits exogenously or endogenously stimulated gastric acid secretion and can be used in the prevention and treatment of gastric acid related diseases and gastrointestinal inflammatory diseases.Type: ApplicationFiled: February 19, 2014Publication date: August 21, 2014Inventor: Mikael DAHLSTRÖM
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Patent number: 8809335Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: July 27, 2012Date of Patent: August 19, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Luca Settimo, Damien Fraysse, Guy Brenchley, Christopher John Davis, Andrew W. Miller
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Publication number: 20140228320Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):Type: ApplicationFiled: April 15, 2014Publication date: August 14, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Takahiko TANIGUCHI, Masato YOSHIKAWA, Kasei MIURA, Tomoaki HASUI, Eiji HONDA, Keisuke IMAMURA, Makoto KAMATA, Haruhi KAMISAKI, John F. QUINN, Joseph RAKER, Fatoumata CAMARA, Yi WANG
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Publication number: 20140228367Abstract: The present disclosure relates to compounds of the Formula (I): and pharmaceutically acceptable salts, as kinase modulators, compatible with the Type-II inhibition of kinases.Type: ApplicationFiled: February 5, 2014Publication date: August 14, 2014Inventor: Gary A. Flynn
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Publication number: 20140228393Abstract: Disclosed are solid forms of 8-chloro-N-[(2-chloro-5-methoxyphenyl)sulfonyl]-6-(trifluoromethyl)-imidazo[1,2-a]pyridine-2-carboxamide (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed. Disclosed are nematocidal compositions comprising a nematocidally effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other nematicide, insecticide and/or fungicide are also disclosed. Also disclosed are methods for protecting a plant from nematodes comprising applying to the plant, or portion, or seed thereof, or to the growing medium of the plant, a nematocidally effective amount of Compound 1 comprising the polymorph Form A.Type: ApplicationFiled: October 5, 2012Publication date: August 14, 2014Inventors: Christian Hoffmann, William J. Marshall, Rafael Shapiro, Richard A. Berger
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PYRROLO[2,3-b]PYRIDIN-4-YL-AMINES AND PYRROLO[2,3-b]PYRIMIDIN-5-YL-AMINES AS JANUS KINASE INHIBITORS
Publication number: 20140228346Abstract: The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.Type: ApplicationFiled: April 17, 2014Publication date: August 14, 2014Applicant: Incyte CorporationInventors: James D. Rodgers, Haisheng Wang, Andrew P. Combs, Richard B. Sparks -
Publication number: 20140228321Abstract: The present invention provides compounds of Formula (I): (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 24, 2012Publication date: August 14, 2014Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Jennifer X. Qiao, Heather Finlay, Ji Jiang, John Lloyd, Carol Hui Hu, Zulan Pi, George O. Tora, James Neels, Jon J. Hangeland, Todd J. Friends
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Publication number: 20140228347Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.Type: ApplicationFiled: April 22, 2014Publication date: August 14, 2014Applicant: IRM LLCInventors: Valentina MOLTENI, Hank Michael James PETRASSI, Xiaolin LI, Xiaodong LIU, Jon LOREN, Juliet NABAKKA, Bao NGUYEN, Vince YEH
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Publication number: 20140228359Abstract: The present invention relates to novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.Type: ApplicationFiled: July 20, 2012Publication date: August 14, 2014Applicant: UNIVERSITE JOSEPH FOURIERInventors: Jean-Noël Denis, Marcelle Claude Jolivalt, Louis Max Maurin, Nikolaevna Olga Burchak
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Publication number: 20140228395Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)-heterocyclo penta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 21, 2014Publication date: August 14, 2014Applicant: Allergan, Inc.Inventors: SANTOSH C. SINHA, LIMING WANG, KEN CHOW, MOHAMMED I. DIBAS, MICHAEL E. GARST
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Patent number: 8802695Abstract: The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: GrantFiled: January 21, 2011Date of Patent: August 12, 2014Assignee: Takeda Pharmaceutical Company LimitedInventor: Edcon Chang
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Patent number: 8802694Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).Type: GrantFiled: December 3, 2010Date of Patent: August 12, 2014Assignee: Targacept, Inc.Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Ronald Joseph Heemstra, Srinivasa V. Murthy, Jon-Paul Strachan, Yunde Xiao
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Publication number: 20140221203Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; and R1, R2, R3, Q and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: April 10, 2014Publication date: August 7, 2014Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: George Philip LAHM, Renee Marie LETT, Brenton Todd SMITH, Benjamin Kenneth SMITH, Clarice Anne TYLER
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Publication number: 20140221322Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: November 5, 2013Publication date: August 7, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: J. Guy Breitenbucher, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Selerstad
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Publication number: 20140221341Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.Type: ApplicationFiled: April 15, 2014Publication date: August 7, 2014Applicant: NAEJA PHARMACEUTICAL INC.Inventors: Samarendra N. MAITI, Dai NGUYEN, Jehangir KHAN, Rong LING
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Publication number: 20140221421Abstract: 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: Steven S. BONDY, Carina E. CANNIZZARO, Chien-Hung CHOU, John O. LINK, Qi LIU, Scott D. SCHROEDER, Winston C. TSE, Jennifer R. ZHANG
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Publication number: 20140221371Abstract: The invention relates to compounds of general formula (I), corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof and the prodrugs of said compounds. The invention also relates to the use of said compounds as binding partners for 5-HT5 receptors for treating diseases that are modulated by a 5-HT5 receptor activity, in particular, for treating neurodegenerative and neuropsychiatric disorders as well as signs, symptoms and dysfunctions.Type: ApplicationFiled: December 23, 2013Publication date: August 7, 2014Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Charles W. Hutchins, Franciso Javier Garcia-Ladona, Wolfgang Wernet
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Publication number: 20140221382Abstract: Pyrrolo[2,3-c]pyridine or pyrrolo[3,2-c]pyridine compounds having the general formula (A), wherein the dashed lines, X, Y and R1 through R5 are as defined in the specification. The compounds are useful in the prophylaxis or treatment of viral infections.Type: ApplicationFiled: April 8, 2014Publication date: August 7, 2014Applicant: GILEAD SCIENCES, INC.Inventors: Steven S. BONDY, David A. OARE, Gerhard PUERSTINGER
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Publication number: 20140221348Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.Type: ApplicationFiled: March 17, 2014Publication date: August 7, 2014Applicant: Basilea Pharmaceutica AGInventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
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Publication number: 20140221332Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.Type: ApplicationFiled: May 25, 2012Publication date: August 7, 2014Applicant: SUNOVION PHARMACEUTICALS INC.Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat
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Publication number: 20140221410Abstract: The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.Type: ApplicationFiled: February 7, 2014Publication date: August 7, 2014Applicant: SCIFLUOR LIFE SCIENCES, LLCInventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan
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Publication number: 20140220032Abstract: Described herein are methods for diagnosing melanoma or basal cell carcinoma based on mutations in the DDR2 gene. Further, a distinct subgroup of BRAF-mutated melanomas have somatic mutations in the DDR2 gene as well. Applications of this finding to routine diagnostics include the molecular stratification of melanoma, and the tissue identification of targetable DDR2 kinase mutations in routine formalin-fixed paraffin-embedded sections. Described herein are methods, compositions and kits related to the discovery that DDR2 mutations may be markers for melanoma generally, and BRAF-mediated melanoma in particular, opening up the possibility of dual therapy for melanoma by targeting both DDR2 and BRAF.Type: ApplicationFiled: December 26, 2013Publication date: August 7, 2014Applicant: QUEST DIAGNOSTICS INVESTMENTS INCORPORATEDInventors: DANIEL M. JONES, YONGBAO WANG, SHERE BILLOUIN-FRAZIER, JUSTIN WINDHAM
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Publication number: 20140221420Abstract: Compounds that modulate the CCR5 chemokine receptor, pharmaceutical compositions containing them, and uses therefor in the treatment of HIV and related diseases are described.Type: ApplicationFiled: March 18, 2011Publication date: August 7, 2014Applicant: PURDUE RESEARCH FOUNDATIONInventors: Arun K. Ghosh, Hiroaki Mitsuya, Venkateswararao Kalapala, Jianfeng Li
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Publication number: 20140219995Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.Type: ApplicationFiled: July 13, 2012Publication date: August 7, 2014Applicant: MICROBIOTIX, INC.Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams, Matthew Torhan
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Patent number: 8796305Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, 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: GrantFiled: March 7, 2013Date of Patent: August 5, 2014Assignee: Bayer Pharma AktiengesellschaftInventors: Alexandros Vakalopoulos, Ingo Hartung, Markus Follman, Rolf Jautelat, Niels Lindner, Dirk Schneider, Frank Wunder, Johannes-Peter Stasch, Gorden Redlich, Volkhart Min-Jian Li
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Patent number: 8796257Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.Type: GrantFiled: November 30, 2012Date of Patent: August 5, 2014Assignee: Naeja Pharmaceutical Inc.Inventors: Samarendra N. Maiti, Dai Nguyen, Jehangir Khan, Rong Ling
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Patent number: 8796244Abstract: The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: June 12, 2009Date of Patent: August 5, 2014Assignee: Astex Therapeutics LtdInventors: Valerio Berdini, Maria Grazia Carr, Miles Stuart Congreve, Martyn Frederickson, Charlotte Mary Griffiths-Jones, Christopher Charles Frederick Hamlett, Andrew Madin, Christopher William Murray, Rajdeep Kaur Benning, Gordon Saxty, Emma Vickerstaffe, Andrew James Woodhead, Steven John Woodhead, Eddy Jean Edgard Freyne, Tom Cornelis Hortense Govaerts, Patrick René Angibaud, Marian Williams
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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: 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: 20140213586Abstract: The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds.Type: ApplicationFiled: September 26, 2012Publication date: July 31, 2014Applicant: KATHOLIEKE UNIVERSITEIT LEUVEN, K.U. Leuven R&DInventors: Dorothee Bardiot, Gunter Carlens, Kai Dallmeier, Suzanne Kaptein, Michael McNaughton, Arnaud Marchand, Johan Neyts, Wim Smets, Mohamed Koukni
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Patent number: 8791113Abstract: The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.Type: GrantFiled: May 31, 2011Date of Patent: July 29, 2014Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Alfred Jonczyk, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
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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: 20140206680Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, p, R1, R2, R3a, R4, and R5 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, cancer, and other disorders, diseases, and conditions for which inhibition of SYK is indicated.Type: ApplicationFiled: June 20, 2012Publication date: July 24, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Mark E. Adams, Rongliang Chen, Mitsunori Kono, Betty Lam, Matthew Lardy, Srinivasa Reddy Natala, Steven James Wilkens, Zhe Nie
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Publication number: 20140206661Abstract: The present invention provides a compound of Formula (X) or a pharmaceutically acceptable salt thereof; 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: January 21, 2014Publication date: July 24, 2014Applicant: NOVARTIS AGInventors: Jake AXFORD, Natalie DALES, Moo Je SUNG
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Publication number: 20140205680Abstract: Methods of treating, preventing or managing cancer, including certain leukemias are disclosed. The methods encompass the administration of enantiomerically pure (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid. Also provided are methods of treatment using this compound with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods are also disclosed.Type: ApplicationFiled: October 17, 2013Publication date: July 24, 2014Applicant: SUNESIS PHARMACEUTICALS, INC.Inventors: Daniel C. Adelman, Jeffrey A. Silverman, Michelle Arkin, Jennifer Hyde, Duncan Walker, Jasmin Wright
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Publication number: 20140206715Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6?R7?); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7? are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.Type: ApplicationFiled: March 26, 2014Publication date: July 24, 2014Applicants: MERCK SHARP & DOHME CORP.Inventors: Andrew W. Stamford, Guoqing Li, William Greenlee, Zhaoning Zhu, Brian McKittrick, Robert Mazzola, Ying Huang, Tao Guo, Thuy X.E. Le, Gang Qian, Yuefei Shao
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Publication number: 20140206662Abstract: A method of treating inflammation, an inflammatory disease, an immune or an autoimmune disorder comprising administering to a patient in need thereof compounds of formula (I): and their pharmaceutically acceptable salts and solvates, which are inhibitors of SSAO activity. The compounds inhibit SSAO activity.Type: ApplicationFiled: March 13, 2014Publication date: July 24, 2014Applicant: PROXIMAGEN LTD.Inventors: Marianne Nilsson, Martin Haraldsson, Sofia Henriksson, Rikard Emond, Edward Savory, Iain Simpson
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Publication number: 20140206682Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of PDGFR (PDGFR?, PDGFR?) kinases or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.Type: ApplicationFiled: August 31, 2012Publication date: July 24, 2014Applicants: NOVARTIS PHARMACEUTICALS UK LIMITED, IRM LLCInventors: Fang Liang, Michael Gibney, Vince Yeh, Xiaolin Li, Valentina Molteni, Duncan Shaw, Ashley Mitchell Berman, Sarah Lewis, Jon Loren, Vikki Furminger
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Publication number: 20140205537Abstract: Provided herein are compounds that inhibit or partially inhibit the activity of leucine rich repeat kinases. Also provided herein are methods of treatment of CNS disorders comprising administration of inhibitors of leucine rich repeat kinases.Type: ApplicationFiled: June 22, 2012Publication date: July 24, 2014Applicant: ZENOBIA THERAPEUTICS, INC.Inventors: Pierre-Yves Bounaud, Vicki Nienaber, Ruo W. Steensma, John A. Lowe, III
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Publication number: 20140205679Abstract: Methods of treating, preventing or managing cancers are disclosed. The methods encompass the administration of SNS-595 in combination with a second active agent. In certain embodiments, the method of treatment comprise administering SNS-595 in combination with cisplatin, carboplatin, gemcitabine or a combination thereof.Type: ApplicationFiled: August 21, 2013Publication date: July 24, 2014Applicant: SUNESIS PHARMACEUTICALS, INC.Inventor: Jeffrey A. Silverman
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Publication number: 20140199263Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: August 16, 2012Publication date: July 17, 2014Inventors: Casey Cameron McComas, Nigel J. Liverton, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Xing Dai, Hong Liu, Shuwen He, Zhong Lai, Qun Dang, Nicolas Zorn
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Publication number: 20140200216Abstract: The present disclosure describes bicyclic aromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.Type: ApplicationFiled: January 14, 2014Publication date: July 17, 2014Applicant: INCYTE CORPORATIONInventors: Yun-Long Li, David M. Burns, Hao Feng, Chu-Biao Xue, Anlai Wang, Jun Pan
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Publication number: 20140200227Abstract: The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.Type: ApplicationFiled: January 14, 2014Publication date: July 17, 2014Applicant: INCYTE CORPORATIONInventors: Chu-Biao Xue, Yun-Long Li, Hao Geng, Jun Pan, Anlai Wang, Ke Zhang, Wenqing Yao, Fenglei Zhang, Jincong Zhuo
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Publication number: 20140200239Abstract: The present invention provides new compounds of formula I, II or III, which have Src homology-2 containing protein tyrosine phosphatase-1 (SHP-1) agonist activity. Also provided are treatment methods using the compounds of formula I, II or III.Type: ApplicationFiled: August 3, 2012Publication date: July 17, 2014Applicant: National Taiwan UniversityInventors: Chung-Wai Shiau, Kuen-Feng Chen
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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: 8778964Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, 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: GrantFiled: March 7, 2013Date of Patent: July 15, 2014Assignee: Bayer Pharma AktiengesellschaftInventors: Alexandros Vakalopoulos, Ingo Hartung, Markus Follmann, Rolf Jautelat, Alexander Straub, Jorma Haβfeld, Niels Lindner, Dirk Schneider, Frank Wunder, Johannes-Peter Stasch, Gorden Redlich, Volkhart Min-Jian Li, Eva-Maria Becker, Andreas Knorr
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Publication number: 20140194418Abstract: Compounds of formula (I) or pharmaceutical acceptable salts are provided, wherein X1˜X5, R1˜R3, A, B, Z and n are defined in the description. And compositions containing said compounds, and the uses for inhibitors of kinases such as ALK, and the uses for treating cancer thereof are provided.Type: ApplicationFiled: January 20, 2012Publication date: July 10, 2014Applicant: ABBVIE INC.Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Fengchun Wu, Yan Shen, Cuihua Liu, Zhenguang Zou, Marina Pliushchev
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Publication number: 20140194432Abstract: The present invention relates to a compound having the general formula (V), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.Type: ApplicationFiled: January 7, 2014Publication date: July 10, 2014Inventors: Andrea Wolkerstorfer, Oliver Szolar, Norbert Handler, Helmut Buschmann, Stephen Cusack, Mark Smith, Sung-Sau So, Ronald Charles Hawley, Achyutharao Sidduri
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Patent number: 8772288Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: GrantFiled: April 3, 2009Date of Patent: July 8, 2014Assignee: Almirall, S.A.Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernet Vidal Juan, Nuria Aguilar Izquierdo
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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