1,2,4-oxadiazoles (including Hydrogenated) Patents (Class 548/131)
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Patent number: 8883801Abstract: The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds.Type: GrantFiled: August 22, 2011Date of Patent: November 11, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Lianyun Zhao, Duan Liu, Shuyi Tang, Amit K. Mandal, Umar Faruk Mansoor, Lalanthi Dilrukshi Vitharana, Panduranga Adulla P. Reddy, M. Arshad Siddiqui
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Publication number: 20140329796Abstract: The present invention aims to provide a novel compound having a TRPA1 antagonist activity, and a medicament containing the compound. Moreover, the present invention aims to provide a TRPA1 antagonist and a medicament useful for the prophylaxis or treatment of diseases involving TRPA1. A medicament containing a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: July 16, 2014Publication date: November 6, 2014Applicant: Ajinomoto Co., Inc.Inventors: Tamotsu SUZUKI, Kaori Kobayashi, Sayaka Asari, Seiji Shiraishi, Tatsuya Okuzumi
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Patent number: 8877751Abstract: Compounds of the formula I, in which R1, R2, R3, R3?, R4, R4?, E, E?, E? and E?? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: December 8, 2009Date of Patent: November 4, 2014Assignee: Merck Patent GmbHInventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
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Patent number: 8877759Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: GrantFiled: September 4, 2012Date of Patent: November 4, 2014Assignee: Vertex Pharnaceuticals IncorporatedInventors: Jean-Damien Charrier, David Kay, Somhairle MacCormick, Pierre-Henri Storck, Joanne Pinder, Michael Edward O'Donnell, Ronald Marcellus Alphonsus Knegtel, Stephen Clinton Young, Philip Michael Reaper, Steven John Durrant, Heather Clare Twin, Christopher John Davis
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Publication number: 20140309238Abstract: The present invention relates to compounds of Formula (I), wherein R1 is chosen among the following radicals: (II); (III); (IV), (V), (VI) (VII) and n=1 or 2 and m=1 or 2 with the proviso that m=2 when R1 is (VIII). The present invention also relates to the use thereof as drugs, more particularly in the treatment of mycobacterial infections and more particularly in the treatment of tuberculosis.Type: ApplicationFiled: October 24, 2012Publication date: October 16, 2014Applicants: Universite de Droit et de la Sante de Lille 2, INSERM (Institut National de la Sante et de la Recherche Medicale), Institut Pasteur de LilleInventors: Benoit Deprez, Nicolas Willand, Marion Flipo, Matthieu Desroses, Alain Baulard, Florence Leroux
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Patent number: 8859598Abstract: The present invention relates to 1,2,4-oxadiazoles azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: September 30, 2013Date of Patent: October 14, 2014Assignee: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
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Publication number: 20140303372Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.Type: ApplicationFiled: March 28, 2014Publication date: October 9, 2014Applicant: ABBVIE BHAMAS LTD.Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A.W. Van Der Neut, Cornelis G. Kruse
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Patent number: 8853219Abstract: Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function.Type: GrantFiled: January 11, 2011Date of Patent: October 7, 2014Assignee: NeuroSolis, Inc.Inventors: Michael L. Hendrickson, Jeffrey C. Ockuly, Trevor M. Twose, Melinda L. Verdone, Brent D. Abraham, Richard R. Copp, James G. Farnham, Seth A. Hanson
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Publication number: 20140296177Abstract: A new class of biotin protein ligase (BPL) inhibitors that have antibacterial activity against multiple Staphylococcus aureus isolates, including clinically important methicillin-resistant S. aureus (MRSA) are disclosed that are non-toxic.Type: ApplicationFiled: September 21, 2012Publication date: October 2, 2014Inventors: Andrew Abel, Steven Polyak, Grant Booker, John Wallace, Tatiana Soares Da Costa, Angie Jarrad, William Tieu, Kelly Lee Keeling, Daniel Sejer Pederson, Nicole Pendini, Matthew Wilce, Min Yin Yap
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Publication number: 20140275191Abstract: The present invention relates to novel oxazolidinone compounds of general formula (I) having antibiotic activity also against multiresistant bacterial strains.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: I.E.ME.S.T-ISTITUTO EURO MEDITERRANEO DI SCIENZA E TECNOLOGIA, UNIVERSITA DEGLI STUDI DI MILANO-BICOCCA
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Publication number: 20140275173Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Inventors: Hao Zhang, Peter T.W. Cheng, Sean Chen, Shiwei Tao, Shung C. Wu, Lidet A. Negash
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Publication number: 20140275186Abstract: This invention relates to novel 4,5-dihydroisoxazoles and 4,5-dihydro[1,2,4]-oxadiazoles of formula (I), to their use as androgenic or antiandrogenic agents or androgen receptor modulators, and to methods of their preparation.Type: ApplicationFiled: October 17, 2012Publication date: September 18, 2014Inventors: Juha Pulkkinen, Pekka Poutiainen, Tuomas Oravilahti, Jorma Palvimo, Mikael Perakyla, Reino Laatikainen, Tarja Ihalainen
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Patent number: 8835470Abstract: Disclosed are compounds of Formula (I) or stereoisomers, salts, or prodrugs thereof, wherein: Q is, or R1 is phenyl substituted with zero to 3 substituents; and R1, R2, R3, R4, R5, and G are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.Type: GrantFiled: April 21, 2011Date of Patent: September 16, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Robert J. Cherney, Yanlei Zhang
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Patent number: 8835469Abstract: The present invention relates to substituted benzamide derivatives of the Formula I and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites, and polymorphs and can be useful for treating disease states mediated by glucokinase. Compounds disclosed herein can be used for reducing blood glucose levels and for increasing insulin secretion for treating type II diabetes. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds, and their use.Type: GrantFiled: July 22, 2010Date of Patent: September 16, 2014Assignee: Cadila Healthcare LimitedInventors: Rajendra Kharul, Mukul R. Jain, Pankaj R. Patel
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Publication number: 20140255386Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.Type: ApplicationFiled: July 24, 2012Publication date: September 11, 2014Applicants: NORTH CAROLINA STATE UNIVERSITY, THE WISTAR INSTITUTEInventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
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Publication number: 20140256740Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.Type: ApplicationFiled: July 27, 2012Publication date: September 11, 2014Applicant: Tempero Pharmaceuticals, Inc.Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt
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Publication number: 20140249159Abstract: The invention relates to compounds of Formula I: wherein Ar1, Ar2, Ar3, L1, L2, Y, Z and v are defined in the specification, and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.Type: ApplicationFiled: May 16, 2012Publication date: September 4, 2014Inventors: Noriyuki Kurose, Kayoko Hata, Yasuyoshi Iso, Naoko Yamaguchi, Bin Shao, Laykea Tafesse, Xiaoming Zhou, Jianming Yu
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Publication number: 20140243366Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: May 1, 2014Publication date: August 28, 2014Applicant: CalciMedica, Inc.Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Patent number: 8815919Abstract: The invention relates to oxadiazole compounds of formula I. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.Type: GrantFiled: March 29, 2010Date of Patent: August 26, 2014Assignee: Merck Serono SAInventors: Anna Quattropani, Cyril Montagne, Wolfgang Sauer, Stefano Crosignani, Agnès Bombrun
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Publication number: 20140235588Abstract: The present invention relates to substituted 1H-pyrazol-1,2,4-oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: February 13, 2014Publication date: August 21, 2014Applicant: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, KEN CHOW
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Publication number: 20140235586Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.Type: ApplicationFiled: April 28, 2014Publication date: August 21, 2014Applicant: PTC Therapeutics, Inc.Inventors: Jeffrey A. Campbell, Atiyya Kahn, James Takasugi, Ellen Welch
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Publication number: 20140235679Abstract: The present invention relates to crystalline forms of 3-[5-(2-fluorophenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid, pharmaceutical compositions and dosage forms comprising the crystalline forms, methods of making the crystalline forms and methods for their use for the treatment, prevention or management of diseases ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay.Type: ApplicationFiled: April 25, 2014Publication date: August 21, 2014Applicant: PTC Therapeutics, Inc.Inventors: Neil G. Almstead, Peter Seongwoo Hwang, Young-Choon Moon
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Publication number: 20140235439Abstract: Provided herein are new 3,5-disubstituted-4,5-dihydro-1,2,4-oxadiazoles that exhibit nematicidal activity and are useful, for example, in compositions and methods for the control of unwanted nematodes.Type: ApplicationFiled: February 14, 2014Publication date: August 21, 2014Applicant: Monsanto Technology LLCInventors: Urszula J. Slomczynska, William P. Haakenson
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Publication number: 20140235587Abstract: The present invention relates to substituted pyrazoles, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: February 13, 2014Publication date: August 21, 2014Applicant: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, KEN CHOW
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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: 20140227302Abstract: Disclosed herein are compounds of Formula (I) (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.Type: ApplicationFiled: September 4, 2012Publication date: August 14, 2014Inventors: Wen-Lian Wu, Duane A. Burnett
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Publication number: 20140228345Abstract: The present invention relates to substituted pyrazole azetidines, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: February 13, 2014Publication date: August 14, 2014Applicant: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, KEN CHOW
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Patent number: 8802663Abstract: The present invention relates to pyrazole oxadiazoles derivatives of Formula (I), and their use for treating multiple sclerosis and other diseases, wherein R1, R2 and R3 are as defined in the description.Type: GrantFiled: June 7, 2010Date of Patent: August 12, 2014Assignee: Merck Serono SAInventors: Anna Quattropani, Charles Baker-Glenn, Wesley Blackaby, Chris Knight
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Patent number: 8802704Abstract: The invention relates to oxadiazole compounds of formula I. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.Type: GrantFiled: March 29, 2010Date of Patent: August 12, 2014Assignee: Merck Serono SAInventors: Anna Quattropani, Cyril Montagne, Wolfgang Sauer, Stefano Crosignani, Agnès Bombrun
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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: 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: 20140221437Abstract: Compounds having an excellent hypoglycemic effect and ? cell- or pancreas-preserving effects or pharmaceutically acceptable salts thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause hyperglycemia due to abnormal glucose metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed.Type: ApplicationFiled: July 27, 2012Publication date: August 7, 2014Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Shigeo Yamanoi, Madoka Hatta, Hidenori Namiki, Koji Matsumoto, Tomomi Yoshitomi
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Patent number: 8796321Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-IV) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.Type: GrantFiled: June 18, 2012Date of Patent: August 5, 2014Assignee: PATH Drug SolutionsInventors: Graham Peter Jones, Kevin James Doyle
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Patent number: 8796322Abstract: Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.Type: GrantFiled: June 19, 2013Date of Patent: August 5, 2014Assignee: PTC Therapeutics, Inc.Inventors: Gary Mitchell Karp, Seongwoo Hwang, Guangming Chen, Neil Gregory Almstead, Young-Choon Moon
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Patent number: 8796318Abstract: Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.Type: GrantFiled: May 14, 2009Date of Patent: August 5, 2014Assignee: The Scripps Research InstituteInventors: Edward Roberts, Hugh Rosen, Steven Brown, Miguel A. Guerrero, Xuemei Peng, Ramulu Poddutoori
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Patent number: 8796253Abstract: This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures.Type: GrantFiled: May 8, 2008Date of Patent: August 5, 2014Assignee: Bayer Intellectual Property GmbHInventors: Stephen Boyer, Michael Härter, Philip Wickens, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Ajay Kumar Bhargava, Karl-Heinz Thierauch, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Patrick Paulus, Holger Hess-Stumpp
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Patent number: 8796256Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: GrantFiled: May 24, 2011Date of Patent: August 5, 2014Assignee: Janssen Pharmaceutica NVInventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
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Publication number: 20140213573Abstract: The present invention relates to novel benzyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: April 2, 2014Publication date: July 31, 2014Applicant: Allergan, Inc.Inventors: Wenkui K. Fang, Liming Wang, Ken Chow, Evelyn G. Corpuz, Wha Bin Im
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Patent number: 8785489Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.Type: GrantFiled: October 13, 2009Date of Patent: July 22, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Asitha Abeywardane, Bennett Farmer, Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Lana Louise Smith Keenan, Ingo Andreas Mugge, Steven John Taylor, Zhaoming Xiong, Yang Yu, Qiang Zhang
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Patent number: 8772323Abstract: The present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and R1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: GrantFiled: May 6, 2011Date of Patent: July 8, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Grauert, Remko Bakker, Steffen Breitfelder, Frank Buettner, Peter Eickelmann, Thomas Fox, Marc Grundl, Thorsten Lehmann-Lintz, Wolfgang Rist
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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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Patent number: 8754112Abstract: Provided are a compound having an excellent hypoglycemic action, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause an increase in the blood sugar level due to abnormal sugar metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed.Type: GrantFiled: August 4, 2010Date of Patent: June 17, 2014Assignee: Daiichi Sankyo Company, LimitedInventors: Shigeo Yamanoi, Hidenori Namiki, Takahiro Katagiri, Mayuko Akiu, Katsuji Kagechika, Takeshi Honda, Koji Matsumoto, Ryutaro Nakashima
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Patent number: 8748625Abstract: The present invention relates to crystalline forms of 3-[5-(2-fluorophenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid, pharmaceutical compositions and dosage forms comprising the crystalline forms, methods of making the crystalline forms and methods for their use for the treatment, prevention or management of diseases ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay.Type: GrantFiled: February 12, 2013Date of Patent: June 10, 2014Assignee: PTC Therapeutics, Inc.Inventors: Neil G. Almstead, Peter Seongwoo Hwang, Young-Choon Moon
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Patent number: 8748412Abstract: Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.Type: GrantFiled: February 2, 2011Date of Patent: June 10, 2014Assignee: Argusina Bioscience Inc.Inventors: Jiayu Liao, Yufeng Hong, Yong Wang, Thomas W. Von Geldern, Kanyin E. Zhang
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Patent number: 8748627Abstract: The present invention relates to compounds of formula (I), which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.Type: GrantFiled: February 15, 2007Date of Patent: June 10, 2014Assignee: AbbVie Inc.Inventors: Yu Gui Gu, Moshe Weitzberg, Xiangdong Xu, Richard F. Clark, Tianyuan Zhang, Qun Li, Todd M. Hansen, Hing Sham, Bruce A. Beutel, Heidi S. Camp, Xiaojun Wang
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Publication number: 20140155614Abstract: The present invention relates to a process for the preparation of dabigatran etexilate of the formula or pharmaceutically accepted salts thereof.Type: ApplicationFiled: May 10, 2012Publication date: June 5, 2014Applicant: EGIS GYOGYSZERGYAR NYILVANOSAN MUKODO RESZVENYTARSASAGInventors: Imre Kiraly, Tibor Szabo, Gyula Simig, Balazs Volk, Laszlo Szlavik, Jozsef Barkoczy, Gyorgy Ruzsics, Gyula Lukacs, Laszlo Pongo, Andras Boza, Maria Tothne Lauritz, Maria Kovacs
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Publication number: 20140155440Abstract: The present invention provides cysteine and cystine bioisosteres for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing such bioisosteres and methods of using the bioisosteres for treatment of schizophrenia and drug addiction.Type: ApplicationFiled: January 7, 2014Publication date: June 5, 2014Applicants: MARQUETTE UNIVERSITY, UWM RESEARCH FOUNDATION, INC.Inventors: James M. Cook, David A. Baker, Edward Merle Johnson, II, Wenyuan Yin, Ranjit Singh Verma
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Patent number: 8741923Abstract: The invention provides compounds of Formula (I) for the treatment of multiple sclerosis and other diseases.Type: GrantFiled: December 15, 2009Date of Patent: June 3, 2014Assignee: Merck Serono SAInventors: Mathilde Muzerelle, Anna Quattropani, Cyril Montagne, Jérôme Dorbais
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Patent number: 8735433Abstract: The present invention relates to aryl oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: November 7, 2013Date of Patent: May 27, 2014Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Ken Chow, Wha-Bin Im
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Publication number: 20140142105Abstract: The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, (I) in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or metabolic syndrome via inhibition of HDAC4.Type: ApplicationFiled: July 6, 2012Publication date: May 22, 2014Applicant: NOVARTIS AGInventors: Christina Hebach, Emilie Joly, Joerg Kallen, James Gilbert Ternois, Marina Tintelnot-Blomley