Additional Hetero Ring Which Is Unsaturated Patents (Class 544/331)
  • Publication number: 20130320262
    Abstract: 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: Application
    Filed: January 18, 2012
    Publication date: December 5, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Irina Martynova, Amir Hossain Parham, Christof Pflumm
  • Patent number: 8598360
    Abstract: 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: Grant
    Filed: September 14, 2012
    Date of Patent: December 3, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, Jr., Gregory Notte
  • Patent number: 8598189
    Abstract: 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: Grant
    Filed: November 14, 2012
    Date of Patent: December 3, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: James P. Edwards, David E. Kindrachuk, Christopher M. Mapes, Daniel J. Pippel, Jennifer D. Venable
  • Patent number: 8592440
    Abstract: Crystalline forms of imatinib mesylate (F, G, H, I and K) and their respective characterizations are disclosed.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: November 26, 2013
    Assignee: Novartis AG
    Inventor: Michael Mutz
  • Patent number: 8592441
    Abstract: 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: Grant
    Filed: April 16, 2012
    Date of Patent: November 26, 2013
    Assignee: 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
  • Patent number: 8592442
    Abstract: Crystalline forms of Nilotinib HCl are described.
    Type: Grant
    Filed: June 27, 2012
    Date of Patent: November 26, 2013
    Assignee: 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
  • Patent number: 8592583
    Abstract: 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: Grant
    Filed: October 27, 2010
    Date of Patent: November 26, 2013
    Assignee: Nerviano Medical Sciences
    Inventors: Matteo D'Anello, Marco Re
  • Patent number: 8592582
    Abstract: 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: Grant
    Filed: January 5, 2011
    Date of Patent: November 26, 2013
    Assignee: Shiseido Company, Ltd.
    Inventors: Hirotada Fukunishi, Naoto Hanyu, Masaru Suetsugu, Takuya Hiruma
  • Publication number: 20130310342
    Abstract: 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: Application
    Filed: October 24, 2012
    Publication date: November 21, 2013
    Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Stephane A. Dumas, Yvonne L. Flanders
  • Publication number: 20130303507
    Abstract: 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: Application
    Filed: January 20, 2012
    Publication date: November 14, 2013
    Applicant: Novartis AG
    Inventors: 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
  • Patent number: 8580806
    Abstract: 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: Grant
    Filed: January 22, 2013
    Date of Patent: November 12, 2013
    Assignee: Novartis AG
    Inventors: Paul W Manley, Wen-Chung Shieh, Paul Allen Sutton, Piotr H Karpinski, Raeann Wu, Stéphanie Monnier, Jörg Brozio
  • Patent number: 8580957
    Abstract: 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: Grant
    Filed: November 3, 2010
    Date of Patent: November 12, 2013
    Assignee: GlaxoSmithKline LLC
    Inventors: Emmanuel Hubert Demont, Romain Luc Marie Gosmini
  • Publication number: 20130292659
    Abstract: 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: Application
    Filed: June 10, 2013
    Publication date: November 7, 2013
    Inventors: Hyung-Sun KIM, Eun-Sun YU, Mi-Young CHAE
  • Publication number: 20130296355
    Abstract: 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: Application
    Filed: July 3, 2013
    Publication date: November 7, 2013
    Inventors: 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
  • Publication number: 20130296307
    Abstract: 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: Application
    Filed: July 10, 2013
    Publication date: November 7, 2013
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
  • Patent number: 8575338
    Abstract: 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: Grant
    Filed: April 8, 2009
    Date of Patent: November 5, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Yasuyuki Tsuzuki, Miki Hirai
  • Patent number: 8575145
    Abstract: 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: Grant
    Filed: August 18, 2009
    Date of Patent: November 5, 2013
    Assignee: 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
  • Publication number: 20130289058
    Abstract: 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: Application
    Filed: April 26, 2013
    Publication date: October 31, 2013
    Inventors: 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
  • Patent number: 8569306
    Abstract: 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: Grant
    Filed: February 19, 2010
    Date of Patent: October 29, 2013
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Bernd Buettelmann, Bindu Goyal, Wylie Solang Palmer
  • Patent number: 8569310
    Abstract: 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: Grant
    Filed: October 6, 2010
    Date of Patent: October 29, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ulrich Iserloh, Andrew W. Stamford, Jared N Cumming
  • Publication number: 20130281475
    Abstract: 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: Application
    Filed: June 13, 2013
    Publication date: October 24, 2013
    Inventors: Carl R. Illig, Shelly K. Ballentine, Jinsheng Chen, Renee Louise, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson
  • Publication number: 20130281402
    Abstract: 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: Application
    Filed: January 6, 2012
    Publication date: October 24, 2013
    Applicant: CRYSTAL BIOPHARMACEUTICAL LLC
    Inventors: Yi Chen, Yu Chen
  • Publication number: 20130281433
    Abstract: 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: Application
    Filed: April 19, 2013
    Publication date: October 24, 2013
    Inventors: 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
  • Publication number: 20130281430
    Abstract: 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: Application
    Filed: April 17, 2013
    Publication date: October 24, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Georg DAHMANN, Horst DOLLINGER, Christian GNAMM, Dennis FIEGEN, Matthias HOFFMANN, Jasna KLICIC, David James LAMB, Andreas SCHNAPP
  • Patent number: 8563539
    Abstract: 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: Grant
    Filed: December 23, 2010
    Date of Patent: October 22, 2013
    Assignee: Jasco Pharmaceuticals, LLC
    Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger, Yvonne L. Flanders, Stephane A. Dumas
  • Patent number: 8563741
    Abstract: 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: Grant
    Filed: September 10, 2008
    Date of Patent: October 22, 2013
    Assignee: Curis, Inc.
    Inventors: Changgeng Qian, Xiong Cai, Haixiao Zhai
  • Patent number: 8563567
    Abstract: 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: Grant
    Filed: December 29, 2010
    Date of Patent: October 22, 2013
    Assignee: ArQule, Inc.
    Inventors: Syed M. Ali, Mark A. Ashwell, Yanbin Liu, Magdi Moussa, Jianqiang Wang, Hui Wu
  • Publication number: 20130274255
    Abstract: 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: Application
    Filed: April 12, 2012
    Publication date: October 17, 2013
    Applicant: DEVELOPMENT CENTER FOR BIOTECHNOLOGY
    Inventors: Chu-Bin LIAO, Chao-Cheng CHIANG, Huei-Ru YANG, Yuan-Chun LIAO, Paonien CHEN
  • Publication number: 20130274242
    Abstract: 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: Application
    Filed: January 18, 2013
    Publication date: October 17, 2013
    Inventors: 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
  • Patent number: 8557826
    Abstract: 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: Grant
    Filed: October 6, 2010
    Date of Patent: October 15, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Andrew W. Stamford, Jared N Cumming
  • Publication number: 20130264548
    Abstract: 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: Application
    Filed: February 27, 2013
    Publication date: October 10, 2013
    Inventors: Yumiko MIZUKI, Tetsuya INOUE, Nobuhiro YABUNOUCHI, Kumiko HIBINO, Kazuki NISHIMURA
  • Publication number: 20130267491
    Abstract: 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: Application
    Filed: July 18, 2011
    Publication date: October 10, 2013
    Applicant: DOMAINEX LIMITED
    Inventors: Trevor Robert Perrior, Gary Karl Newton, Mark Richard Stewart, Rehan Aqil
  • Patent number: 8552196
    Abstract: 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: Grant
    Filed: September 13, 2012
    Date of Patent: October 8, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, Jr., Gregory Notte
  • Patent number: 8551984
    Abstract: 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: Grant
    Filed: December 15, 2010
    Date of Patent: October 8, 2013
    Assignees: 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
  • Patent number: 8552022
    Abstract: 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: Grant
    Filed: August 3, 2010
    Date of Patent: October 8, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harold B. Wood, Alan D. Adams, Jason W. Szewczyk, Yong Zhang, Meng Yang
  • Publication number: 20130261118
    Abstract: 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: Application
    Filed: March 13, 2013
    Publication date: October 3, 2013
    Inventor: John Manfredi
  • Publication number: 20130256644
    Abstract: A compound for an organic optoelectronic device, the compound being represented by the following Chemical Formula 1:
    Type: Application
    Filed: June 3, 2013
    Publication date: October 3, 2013
    Inventors: Hyung-Sun KIM, Soo-Hyun MIN, Eun-Sun YU, Mi-Young CHAE
  • Publication number: 20130261116
    Abstract: 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: Application
    Filed: May 10, 2013
    Publication date: October 3, 2013
    Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Srikant VISWANADHA, Govindarajulu BABU, Swaroop Kumar V.S. VAKKALANKA
  • Patent number: 8546567
    Abstract: 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: Grant
    Filed: July 3, 2012
    Date of Patent: October 1, 2013
    Assignee: Sanofi
    Inventors: Joachim Graeser, Guenter Billen, Adolf Linkies, Tobias Metzenthin
  • Patent number: 8546390
    Abstract: 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: Grant
    Filed: May 23, 2008
    Date of Patent: October 1, 2013
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Margarita Wucherer-Plietker, Lars T. Burgdorf, Christian Sirrenberg, Christina Esdar, Thomas J. J. Mueller, Eugen Merkul
  • Publication number: 20130252882
    Abstract: 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: Application
    Filed: January 31, 2012
    Publication date: September 26, 2013
    Applicant: EVOLVA SA
    Inventors: Jutta Heim, Peter Schneider, Patrick Roussel, Daniel Milligan, Christian Bartels, Glenn Dale
  • Publication number: 20130252944
    Abstract: 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: Application
    Filed: July 11, 2011
    Publication date: September 26, 2013
    Inventors: 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
  • Publication number: 20130252934
    Abstract: 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: Application
    Filed: March 1, 2013
    Publication date: September 26, 2013
    Applicants: 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
  • Patent number: 8541402
    Abstract: 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: Grant
    Filed: May 3, 2012
    Date of Patent: September 24, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
  • Patent number: 8541434
    Abstract: 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: Grant
    Filed: August 19, 2009
    Date of Patent: September 24, 2013
    Assignees: Merck Sharp & Dohme Corp., Southern Research Institute
    Inventors: 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
  • Publication number: 20130244262
    Abstract: 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: Application
    Filed: November 17, 2011
    Publication date: September 19, 2013
    Applicant: KYOTO UNIVERSITY
    Inventors: Jun Yamashita, Hideki Uosaki
  • Publication number: 20130245000
    Abstract: 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: Application
    Filed: November 24, 2011
    Publication date: September 19, 2013
    Applicant: LUPIN LIMITED
    Inventors: Rajesh Thotapally, Onkar Gangaram Kachi, Atish Harishchandra Rodge, Ashok Bhau Pathak, Bhavana Shrirang Kardile, Milind Dattatraya Sindkhedkar, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20130245016
    Abstract: Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Application
    Filed: November 30, 2011
    Publication date: September 19, 2013
    Inventors: Steven David Knight, William Henry Miller, Kenneth Allen Newlander, Sharad Kumar Verma
  • Publication number: 20130245052
    Abstract: The present invention provides a novel crystalline form of nilotinib hydrochloride, process for its preparation and pharmaceutical compositions comprising it.
    Type: Application
    Filed: November 11, 2011
    Publication date: September 19, 2013
    Applicant: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivasa Rao, Bandi Vamsi Krishna
  • Patent number: 8536180
    Abstract: 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: Grant
    Filed: May 26, 2010
    Date of Patent: September 17, 2013
    Assignee: 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