Additional Hetero Ring Which Is Unsaturated Patents (Class 544/331)
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Publication number: 20130320262Abstract: The present invention relates to a compound of a formula (I), (II) or (III), to the use of this compound in an electronic device, and to an electronic device comprising one or more compounds of the formula (I), (II) or (III). The invention furthermore relates to a process for the preparation of a compound of the formula (I), (II) or (III) and to a formulation comprising one or more compounds of the formula (I), (II) or (III).Type: ApplicationFiled: January 18, 2012Publication date: December 5, 2013Applicant: MERCK PATENT GMBHInventors: Irina Martynova, Amir Hossain Parham, Christof Pflumm
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Patent number: 8598360Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).Type: GrantFiled: September 14, 2012Date of Patent: December 3, 2013Assignee: Gilead Sciences, Inc.Inventors: Britton Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, Jr., Gregory Notte
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Patent number: 8598189Abstract: Benzoimidazol-2-yl pyrimidines and pyrazines, pharmaceutical compositions and methods for H4 receptor activity modulation and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritis.Type: GrantFiled: November 14, 2012Date of Patent: December 3, 2013Assignee: Janssen Pharmaceutica NVInventors: James P. Edwards, David E. Kindrachuk, Christopher M. Mapes, Daniel J. Pippel, Jennifer D. Venable
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Patent number: 8592440Abstract: Crystalline forms of imatinib mesylate (F, G, H, I and K) and their respective characterizations are disclosed.Type: GrantFiled: July 15, 2011Date of Patent: November 26, 2013Assignee: Novartis AGInventor: Michael Mutz
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Patent number: 8592441Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: April 16, 2012Date of Patent: November 26, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Marc Gustaaf Celine Verdonck, Patrick René Angibaud, Bruno Roux, Isabelle Noëlle Constance Pilatte, Peter Ten Holte, Janine Arts, Kristof Van Emelen
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Patent number: 8592442Abstract: Crystalline forms of Nilotinib HCl are described.Type: GrantFiled: June 27, 2012Date of Patent: November 26, 2013Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Greta Sterimbaum, Sigalit Levi, Adi Yeori, Tamas Koltai, Valerie Niddam-Hildesheim, Maytal Piran, Shay Asis, Hagit Eisen-Nevo, David Malcolm Crowe
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Patent number: 8592583Abstract: The invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. The process allows to obtain the desired products in high yields and purity. The synthesis is starting from the coupling of an acetal with a beta-ketoester; the resultant compound is acetylated and then reacted with a dialkyl acetal of N,N-dimethylformamide to give an intermediate which is cyclized to 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxylic ester; the carboxylic ester is then hydrolyzed and the resultant carboxylic acid is finally condensed with an appropriate form of ammonia to give the desired carboxamide. The compounds prepared according to the process of the invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity.Type: GrantFiled: October 27, 2010Date of Patent: November 26, 2013Assignee: Nerviano Medical SciencesInventors: Matteo D'Anello, Marco Re
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Patent number: 8592582Abstract: The present invention provides a method for producing a pyrimidinylpyrazole compound (1), wherein aminoguanidine (2) or its salt is reacted with a ?-diketone compound (3) to produce the pyrimidinylpyrazole compound: wherein R1 and R3 are each independently an alkyl group having 1 to 4 carbon atoms, and R2 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms. The method is excellent in the environmental compatibility and economic efficiency.Type: GrantFiled: January 5, 2011Date of Patent: November 26, 2013Assignee: Shiseido Company, Ltd.Inventors: Hirotada Fukunishi, Naoto Hanyu, Masaru Suetsugu, Takuya Hiruma
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Publication number: 20130310342Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway.Type: ApplicationFiled: October 24, 2012Publication date: November 21, 2013Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Stephane A. Dumas, Yvonne L. Flanders
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Publication number: 20130303507Abstract: The present invention provides a compound of formula (II): where R1 is a substituted alkyl, heterocyclic, or cycloalkyl, group, and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof, and pharmaceutical compositions comprising these compounds. Also provided are methods of using these compounds to treat a disease or condition mediated by CDK9, such as cancers and other conditions described herein.Type: ApplicationFiled: January 20, 2012Publication date: November 14, 2013Applicant: Novartis AGInventors: William R. Antonios-McCrea, Paul A. Barsanti, Cheng Hu, Xianming Jin, Eric Martin, Yue Pan, Xiaodong Lin, Keith B. Pfister, Paul A. Renhowe, Martin Sendzik, James Sutton, Lifeng Wan
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Patent number: 8580806Abstract: Salts of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes.Type: GrantFiled: January 22, 2013Date of Patent: November 12, 2013Assignee: Novartis AGInventors: Paul W Manley, Wen-Chung Shieh, Paul Allen Sutton, Piotr H Karpinski, Raeann Wu, Stéphanie Monnier, Jörg Brozio
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Patent number: 8580957Abstract: Tetrahydroquinoline compounds of formula (I) or a salt thereof, pharmaceutical compositions containing such compounds and their use in therapy, in particular in the treatment of diseases or conditions for which a bromodomain inhibitor is indicted.Type: GrantFiled: November 3, 2010Date of Patent: November 12, 2013Assignee: GlaxoSmithKline LLCInventors: Emmanuel Hubert Demont, Romain Luc Marie Gosmini
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Publication number: 20130292659Abstract: A compound for an organic optoelectronic device, an organic light emitting diode including the same, and a display device including the organic light emitting diode are disclosed, and the compound for an organic optoelectronic device represented by Chemical Formula 1 is provided to manufacture an organic optoelectronic device having improved life-span characteristics due to excellent electrochemical and thermal stability, and high luminous efficiency at a low driving voltage.Type: ApplicationFiled: June 10, 2013Publication date: November 7, 2013Inventors: Hyung-Sun KIM, Eun-Sun YU, Mi-Young CHAE
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Publication number: 20130296355Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: ApplicationFiled: July 3, 2013Publication date: November 7, 2013Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Publication number: 20130296307Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:Type: ApplicationFiled: July 10, 2013Publication date: November 7, 2013Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Patent number: 8575338Abstract: A compound of formula (A); wherein ring A is an aromatic ring or a heteroaromatic ring; R1 is independently halogen, cyano, etc., each of X1, X2 and X3 is CR2 or nitrogen, R2 is independently hydrogens, etc., n is 0, 1, 2, 3 or 4; -D-Y is —O—CH2COOH, etc, and G is a substituted amino, a substituted heterocyclic group, etc, or a pharmaceutical acceptable salt thereof, has activities of opening BK channels.Type: GrantFiled: April 8, 2009Date of Patent: November 5, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Yasuyuki Tsuzuki, Miki Hirai
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Patent number: 8575145Abstract: Compounds of Formula (I), in which A, B, R1, R1a, R2, R3, R4, R5, R6, and R7 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of immune cell-associated diseases and disorders, such as inflammatory and autoimmune diseases.Type: GrantFiled: August 18, 2009Date of Patent: November 5, 2013Assignee: Array BioPharma Inc.Inventors: Shelley Allen, Laura L. Celeste, T. Gregg Davis, Robert Kirk DeLisle, Julie Marie Greschuk, Stefan D. Gross, Erik James Hicken, Leila J. Jackson, Nicholas C. Kallan, Joseph P. Lyssikatos, Fredrik P. Marmsater, Mark C. Munson, Jed Pheneger, Bryson Rast, John E. Robinson, Stephen T. Schlachter, George T. Topalov, A. Dale Wright, Qian Zhao
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Publication number: 20130289058Abstract: The invention relates to compounds of formula (I): useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.Type: ApplicationFiled: April 26, 2013Publication date: October 31, 2013Inventors: Sejal Patel, Justin Mao, Qian Lui, Rui Zheng, Tyler Harrison, Rohit Duvadie, Xin Chen, Frederic Zecri, Jay Larrow, Xuchun Zheng, Yizong Zhou, Jiong Ye, Yiping Ding, Yu Gai
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Patent number: 8569306Abstract: Compounds of formula (I) modulate JNK wherein X1 and X2 are each simultaneously N or CH; X3 is CH—R2 Or N—SO2R, where R is lower alkyl; R1 is aryl or heteroaryl, substituted with 0-3 lower alkyl radicals; R2 is (II), where R3 is H, lower acyl, or an amino acid, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 19, 2010Date of Patent: October 29, 2013Assignee: Hoffmann-La Roche, Inc.Inventors: Bernd Buettelmann, Bindu Goyal, Wylie Solang Palmer
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Patent number: 8569310Abstract: In its many embodiments, the present invention provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (a) and pharmaceutically acceptable salts thereof. Compounds of Formula (a) have the general structure: (a) wherein each variable is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers Disease, are also disclosed.Type: GrantFiled: October 6, 2010Date of Patent: October 29, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Ulrich Iserloh, Andrew W. Stamford, Jared N Cumming
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Publication number: 20130281475Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: June 13, 2013Publication date: October 24, 2013Inventors: Carl R. Illig, Shelly K. Ballentine, Jinsheng Chen, Renee Louise, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson
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Publication number: 20130281402Abstract: The disclosure includes hydroxamic compounds of Formula I: (Formula I) wherein Z, L, R1, R2, and R3 are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.Type: ApplicationFiled: January 6, 2012Publication date: October 24, 2013Applicant: CRYSTAL BIOPHARMACEUTICAL LLCInventors: Yi Chen, Yu Chen
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Publication number: 20130281433Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Publication number: 20130281430Abstract: The invention relates to new amino-indole-substituted imidazolyl-pyrimidines of formula 1 wherein R1, R2, R3, R4 and R5 are defined as in claim 1 and pharmaceutically acceptable salts thereof and the use of these compounds for the preparation of a medicament for treating a disease selected from asthma, COPD, rheumatoid arthritis, specific lymphomas and specific diseases of the nervous system.Type: ApplicationFiled: April 17, 2013Publication date: October 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Georg DAHMANN, Horst DOLLINGER, Christian GNAMM, Dennis FIEGEN, Matthias HOFFMANN, Jasna KLICIC, David James LAMB, Andreas SCHNAPP
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Patent number: 8563539Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.Type: GrantFiled: December 23, 2010Date of Patent: October 22, 2013Assignee: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger, Yvonne L. Flanders, Stephane A. Dumas
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Patent number: 8563741Abstract: The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The compounds of the invention may further act as HDAC inhibitors.Type: GrantFiled: September 10, 2008Date of Patent: October 22, 2013Assignee: Curis, Inc.Inventors: Changgeng Qian, Xiong Cai, Haixiao Zhai
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Patent number: 8563567Abstract: The present invention relates to substituted heterocyclic compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted heterocyclic compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: December 29, 2010Date of Patent: October 22, 2013Assignee: ArQule, Inc.Inventors: Syed M. Ali, Mark A. Ashwell, Yanbin Liu, Magdi Moussa, Jianqiang Wang, Hui Wu
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Publication number: 20130274255Abstract: The present invention relates to a compound of formula (I): or hydrates, solvates, prodrugs, or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, ring A, R3 and R4 are as defined in the detailed description and claims. The compound of formula (I) are receptor tyrosine kinase (RTK) inhibitors and have efficacy for the treatment, prevention, or amelioration of RTK-related diseases.Type: ApplicationFiled: April 12, 2012Publication date: October 17, 2013Applicant: DEVELOPMENT CENTER FOR BIOTECHNOLOGYInventors: Chu-Bin LIAO, Chao-Cheng CHIANG, Huei-Ru YANG, Yuan-Chun LIAO, Paonien CHEN
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Publication number: 20130274242Abstract: 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: January 18, 2013Publication date: October 17, 2013Inventors: Jang-Sik Choi, Hae-Jun Hwang, Eunho Lee, Jaekyoo Lee, Ho-Juhn Song, Se Won Kim, Jung-Ho Kim, Jong Sung Koh, Sunhwa Chang, Tae-im Lee, Yung-geun Choi, Ik-hwan Han, Jaesang Lee
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Patent number: 8557826Abstract: In its many embodiments, the present invention provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (I): and tautomers thereof, and solvates, prodrugs, esters, and deuterates of said compounds and said tautomers, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, R11, ring A, ring B, m, n, p, q, r, -L1-, L2-, and L3- is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers Disease, are also disclosed.Type: GrantFiled: October 6, 2010Date of Patent: October 15, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Andrew W. Stamford, Jared N Cumming
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Publication number: 20130264548Abstract: A material for organic EL device which includes a compound having a specific structure: an azine ring having a cyano-substituted aromatic hydrocarbon group, an azine ring having a cyano-substituted heterocyclic group, or an azine ring having a cyano group directly bonded to the azine ring. An organic electroluminescence device including an organic thin film layer between a cathode and an anode, wherein the organic thin film layer includes a light emitting layer and at least one layer containing the material for organic electroluminescence device, has a long lifetime.Type: ApplicationFiled: February 27, 2013Publication date: October 10, 2013Inventors: Yumiko MIZUKI, Tetsuya INOUE, Nobuhiro YABUNOUCHI, Kumiko HIBINO, Kazuki NISHIMURA
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Publication number: 20130267491Abstract: C Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases IKK? and/or TBK-1: in which: R1 represents an aliphatic heterocyclyl group having 4, 5, 6 or 7 ring atoms, bonded to the phenyl group shown in formula I through a ring nitrogen atom, and optionally substituted by one or more substituents defined in the Specification; R2 represents a phenyl or heteroaryl group which is optionally substituted by one or more substituents defined in the Specification; and each of R3 and R4 independently represents a hydrogen atom or a C1-4 alkyl group.Type: ApplicationFiled: July 18, 2011Publication date: October 10, 2013Applicant: DOMAINEX LIMITEDInventors: Trevor Robert Perrior, Gary Karl Newton, Mark Richard Stewart, Rehan Aqil
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Patent number: 8552196Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).Type: GrantFiled: September 13, 2012Date of Patent: October 8, 2013Assignee: Gilead Sciences, Inc.Inventors: Britton Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, Jr., Gregory Notte
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Patent number: 8551984Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.Type: GrantFiled: December 15, 2010Date of Patent: October 8, 2013Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Michael H. Reutershan, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hua Zhou
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Patent number: 8552022Abstract: Substituted cyclopropyl compounds of the formula I: are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: GrantFiled: August 3, 2010Date of Patent: October 8, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Harold B. Wood, Alan D. Adams, Jason W. Szewczyk, Yong Zhang, Meng Yang
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Publication number: 20130261118Abstract: The present disclosure relates to novel indole and tetrahydroindole core compounds useful for the treatment of disorders associated with a defect in vesicular transport (e.g., axonal transport).Type: ApplicationFiled: March 13, 2013Publication date: October 3, 2013Inventor: John Manfredi
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Publication number: 20130256644Abstract: A compound for an organic optoelectronic device, the compound being represented by the following Chemical Formula 1:Type: ApplicationFiled: June 3, 2013Publication date: October 3, 2013Inventors: Hyung-Sun KIM, Soo-Hyun MIN, Eun-Sun YU, Mi-Young CHAE
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Publication number: 20130261116Abstract: The present invention provides, inter alia, compounds of formula I as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: ApplicationFiled: May 10, 2013Publication date: October 3, 2013Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant VISWANADHA, Govindarajulu BABU, Swaroop Kumar V.S. VAKKALANKA
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Patent number: 8546567Abstract: This disclosure relates to a novel process for obtaining a compound of formula I: wherein the values of R1, R2, and R3 and P are as described in the specification, and intermediates thereof.Type: GrantFiled: July 3, 2012Date of Patent: October 1, 2013Assignee: SanofiInventors: Joachim Graeser, Guenter Billen, Adolf Linkies, Tobias Metzenthin
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Patent number: 8546390Abstract: Compounds of the formula (I), in which R1, R2, R3 and R4 have the meanings indicated in claim (1), are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumors.Type: GrantFiled: May 23, 2008Date of Patent: October 1, 2013Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Margarita Wucherer-Plietker, Lars T. Burgdorf, Christian Sirrenberg, Christina Esdar, Thomas J. J. Mueller, Eugen Merkul
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Publication number: 20130252882Abstract: This invention provides novel 4-oxoquinolizine compounds and their uses for a series of broad-spectrum antibiotics having no cross-resistance to existing or emerging classes of antibiotics. In addition the novel 4-oxoquinolizine compounds are useful against CDC Category A and B pathogens The invention also provides pharmaceutical compositions comprising certain 4-oxoquinolizines in combination with subinhibitory concentrations of polymyxin B against clinical isolates which are resistant to quinolones, carbapenems and other antimicrobial agents.Type: ApplicationFiled: January 31, 2012Publication date: September 26, 2013Applicant: EVOLVA SAInventors: Jutta Heim, Peter Schneider, Patrick Roussel, Daniel Milligan, Christian Bartels, Glenn Dale
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Publication number: 20130252944Abstract: The present invention relates to novel compounds of Formula (I), wherein M, A and Y are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: July 11, 2011Publication date: September 26, 2013Inventors: Christelle Bolea, Sylvain Celanire, Lam Tang, Philip Jones, Nigel J. Liverton, Richard Soll, Jingchao Dong, Zhiyu Lei, Fuqing Liu, Yanling Kong, Yi Ju, Haoyong Zhang, Jieping Wei, Qiaoxin Wei, Minxiang Zhang, Yunfu Luo
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Publication number: 20130252934Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: March 1, 2013Publication date: September 26, 2013Applicants: Genentech, Inc., Array BioPharma Inc.Inventors: James F. Blake, Mark Joseph Chicarelli, Rustam Ferdinand Garrey, John Gaudino, Jonas Grina, David A. Moreno, Peter J. Mohr, Li Ren, Jacob Schwarz, Huifen Chen, Kirk Robarge, Aihe Zhou
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Patent number: 8541402Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: GrantFiled: May 3, 2012Date of Patent: September 24, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
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Patent number: 8541434Abstract: The present invention provides compounds of Formula (I): and tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and pro-drugs of said compounds, wherein each of R, R1, X, Y, Z, R2, R3, R4, R5, R6, R7, R8, R9, R18, R19 and n is selected independently and as defined herein. Compositions comprising such compounds are also provided. The compounds of the invention are effective as inhibitors of HCV, and are useful, alone and together with other therapeutic agents, in treating or preventing diseases or disorders such as viral infections and virus-related disorders.Type: GrantFiled: August 19, 2009Date of Patent: September 24, 2013Assignees: Merck Sharp & Dohme Corp., Southern Research InstituteInventors: Cecil D. Kwong, F. George Njoroge, Subramaniam Ananthan, Ashok Arasappan, Frank Bennett, Jeremy Clark, Anita T. Fowler, Feng Geng, Hollis S. Kezar, III, Joseph A. Maddry, John J. Piwinski, Robert C. Reynolds, Abhijit Roychowdhury, John A. Secrist, III, Neng-Yang Shih
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Publication number: 20130244262Abstract: The present invention provides a cardiomyocyte- and/or cardiac progenitor cell-proliferating agent comprising at least one compound selected from the group consisting of: a GSK3? inhibitor, ERK dephosphorylation inhibitor, Raf activator, CaMK2 inhibitor and p38 inhibitor; and a method for proliferating cardiomyocytes and/or cardiac progenitor cells using the agent.Type: ApplicationFiled: November 17, 2011Publication date: September 19, 2013Applicant: KYOTO UNIVERSITYInventors: Jun Yamashita, Hideki Uosaki
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Publication number: 20130245000Abstract: The present invention relates to compounds of Formula (I) that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of GPR119 receptor activity. The invention also relates to the process for preparation of the compounds, pharmaceutical compositions thereof. The invention further relates to methods of treating, preventing and/or managing diseases, disorders syndromes or conditions associated with the modulation of GPR119 receptor by using either alone or in combinations of Formula (I).Type: ApplicationFiled: November 24, 2011Publication date: September 19, 2013Applicant: LUPIN LIMITEDInventors: Rajesh Thotapally, Onkar Gangaram Kachi, Atish Harishchandra Rodge, Ashok Bhau Pathak, Bhavana Shrirang Kardile, Milind Dattatraya Sindkhedkar, Venkata P. Palle, Rajender Kumar Kamboj
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Publication number: 20130245016Abstract: Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: ApplicationFiled: November 30, 2011Publication date: September 19, 2013Inventors: Steven David Knight, William Henry Miller, Kenneth Allen Newlander, Sharad Kumar Verma
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Publication number: 20130245052Abstract: The present invention provides a novel crystalline form of nilotinib hydrochloride, process for its preparation and pharmaceutical compositions comprising it.Type: ApplicationFiled: November 11, 2011Publication date: September 19, 2013Applicant: Hetero Research FoundationInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivasa Rao, Bandi Vamsi Krishna
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Patent number: 8536180Abstract: Described herein are compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, wherein G1, L1, R2, R3, n, p, Ar1, and Ar2 are defined in the description. Methods of making said compounds, and compositions comprising said compounds which are useful for inhibiting kinases such as IGF-1R are also disclosed.Type: GrantFiled: May 26, 2010Date of Patent: September 17, 2013Assignee: AbbVie Inc.Inventors: Richard F. Clark, Nwe Y. Ba-maung, Scott A. Erickson, Steve D. Fidanze, Robert A. Mantei, George S. Sheppard, Bryan K. Sorensen, Gary T. Wang, Jieyi Wang, Randy L. Bell