1,2,4-oxadiazoles (including Hydrogenated) Patents (Class 548/131)
  • Publication number: 20120291159
    Abstract: The present invention relates to azoline compounds which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
    Type: Application
    Filed: December 20, 2010
    Publication date: November 15, 2012
    Applicant: BASF SE
    Inventors: Karsten Koerber, Florian Kaiser, Wolfgang von Deyn, Steffen Gross, Prashant Deshmukh, Joachim Dickhaut, Nina Gertrud Bandur, Arun Narine, Carsten Beyer, Deborah L. Culbertson, Douglas D. Anspaugh, Franz Josef Braun, Ronan Le Vezouet
  • Patent number: 8309584
    Abstract: A novel sulfur containing heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The prevention also provide a method for preparing same, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.
    Type: Grant
    Filed: September 25, 2008
    Date of Patent: November 13, 2012
    Assignee: Green Cross Corporation
    Inventors: Jinhwa Lee, Hee Jeong Seo, Min-Ah Kim, Jeongmin Kim, Sung-Han Lee, Myung Eun Jung, Mi-Soon Kim
  • Publication number: 20120283295
    Abstract: The invention provides an indazole derivative of formula (1), or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1, R2, R3 and R4 are as defined herein. The indazole derivatives are capable of blockading voltage dependent sodium channels and they are useful in the treatment or prevention of normal tension glaucoma, multiple sclerosis, a motorneurone disease, stroke, spinal cord injury, Alzheimer's disease, Parkinson's disease or pain.
    Type: Application
    Filed: September 30, 2010
    Publication date: November 8, 2012
    Applicant: University College London
    Inventors: Cristina Garcia Posada, David Selwood, John Garthwaite, David Baker, Lisa Clutterbuck
  • Publication number: 20120283297
    Abstract: Oxadiazole substituted indazole derivatives of formula (I) or pharmaceutical salts thereof having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptors are disclosed.
    Type: Application
    Filed: December 16, 2010
    Publication date: November 8, 2012
    Applicant: GLAXO WELLCOME HOUSE
    Inventors: James Bailey, Nigel Paul King, Xichen Lin, Feng Ren, Kheng-Chuan Tan, Sing Yeung Mak
  • Patent number: 8304554
    Abstract: A compound represented by the following formula (DII): wherein Y31, Y32 and Y33 each independently represents a methine group or a nitrogen atom; R31, R32 and R33 each independently represents the following formula (DII-R):
    Type: Grant
    Filed: February 23, 2010
    Date of Patent: November 6, 2012
    Assignee: FUJIFILM Corporation
    Inventors: Makoto Takahashi, Hideyuki Nishikawa, Ichiro Nagata, Satoshi Tanaka, Shigeki Uehira
  • Publication number: 20120277234
    Abstract: 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: Application
    Filed: June 22, 2012
    Publication date: November 1, 2012
    Inventors: Gary Mitchell Karp, Seongwoo Hwang, Guangming Chen, Neil Gregory Almstead, Young-Choon Moon
  • Patent number: 8299104
    Abstract: The invention relates to substituted aryl-substituted heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to process for their preparation and to their use as medicaments. Compounds of the formula I in which the radicals have the stated meanings, the N-oxides thereof, and the physiologically tolerated salts thereof, and process for the preparation thereof are described. The compounds bring about for example a weight reduction in mammals and are suitable for example for the prevention and treatment of obesity and diabetes.
    Type: Grant
    Filed: November 28, 2007
    Date of Patent: October 30, 2012
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Lothar Schwink, Siegfried Stengelin, Thomas Boehme, Matthias Gossel, Gerhard Hessler, Petra Stahl
  • Publication number: 20120269864
    Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.
    Type: Application
    Filed: June 11, 2012
    Publication date: October 25, 2012
    Inventors: Haiyan Jia, Ian ZACHARY, Michelle TICKNER, Lili CHENG, Chris CHAPMAN, Katie ELLARD, Basil HARTZOULAKIS, Ashley JARVIS, Rosemary LYNCH, Jamie NALLY, David SELWOOD, Mark STEWART
  • Publication number: 20120264717
    Abstract: 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: Application
    Filed: June 18, 2012
    Publication date: October 18, 2012
    Inventors: Graham Peter Jones, Kevin James Doyle
  • Publication number: 20120252776
    Abstract: Disclosed herein are novel C4-monomethyl triterpenoid compounds and derivatives thereof, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example as antioxidant inflammation modulators, and compositions thereof are also provided.
    Type: Application
    Filed: March 12, 2012
    Publication date: October 4, 2012
    Inventors: Eric Anderson, Christopher F. Bender, Xiaofeng Liu, Xin Jiang, Melean Visnick
  • Publication number: 20120252853
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: March 30, 2012
    Publication date: October 4, 2012
    Applicant: H. Lundbeck A/S
    Inventors: Anette Graven Sams, Jørgen Eskildsen, Jesper Frank Bastlund
  • Patent number: 8273776
    Abstract: The present invention relates to novel biphenyl oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: April 13, 2011
    Date of Patent: September 25, 2012
    Assignee: Allergan, Inc
    Inventors: Janet A. Takeuchi, Ken Chow, Ling Li
  • Publication number: 20120232118
    Abstract: Potent and selective ligands for the dopamine 3 (D3) receptor are disclosed. The D3 receptor ligands have a structural formula: wherein R1 is C1-6 alkyl or C3-6cycloalkyl; or wherein R2 is substituted with one or two halogen(s) or OC1-3alkyl.
    Type: Application
    Filed: February 28, 2012
    Publication date: September 13, 2012
    Applicants: UNIVERSITY OF KANSAS, THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Jianyong Chen, Gregory Collins, Beth Levant, James H. Woods
  • Publication number: 20120232277
    Abstract: The present invention discloses processes for the preparation and isolation of [1,2,4]oxadiazo-3-yl derivatives of carboxylic acids. The derivatives are useful in the treatment of inflammatory diseases and conditions.
    Type: Application
    Filed: March 8, 2012
    Publication date: September 13, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Kirill A. Lukin, Vimal Kishore, Thomas D. Gordon
  • Patent number: 8263629
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: May 27, 2010
    Date of Patent: September 11, 2012
    Assignee: Novartis AG
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Patent number: 8263630
    Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein R1, R2, and R3 are defined herein.
    Type: Grant
    Filed: February 11, 2009
    Date of Patent: September 11, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventor: James J. Li
  • Patent number: 8258310
    Abstract: An object is to provide a novel material having a bipolar property. Another object is to provide an oxadiazole derivative having a wide band gap. Another object is to reduce power consumption of a light-emitting element, a light-emitting device, and an electronic device. The present invention provides an oxadiazole derivative represented by General Formula (1). In the formula, Ar1 represents a substituted or unsubstituted aryl group having 6 to 10 carbon atoms in a ring, A represents a substituted or unsubstituted phenylene group, R11 to R15 and R21 to R25 are independently any of hydrogen, an alkyl group having 1 to 4 carbon atoms, an aryl group having 6 to 10 carbon atoms in a ring, and a substituted or unsubstituted 9H-carbazol-9-yl group.
    Type: Grant
    Filed: March 17, 2010
    Date of Patent: September 4, 2012
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroko Nomura, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
  • Publication number: 20120214848
    Abstract: The present invention relates to salts and crystalline forms of [1,2,4]oxadiazol-3-yl]-phenoxy}-cycloalkyl carboxylic acids, processes for their preparation, pharmaceutical compositions comprising such compounds, and methods of using them.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 23, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Geoff G. Zhang, Paul J. Brackemeyer, Shaung Chen, Thomas D. Gordon
  • Patent number: 8247401
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Grant
    Filed: October 29, 2008
    Date of Patent: August 21, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Diem Nguyen, Zhengwu Deng, Daniel V. Paone, Craig M. Potteiger, Joseph P. Vacca
  • Publication number: 20120208828
    Abstract: The present invention relates to new compounds of formula I, to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy. Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway. For example, these may be used in preventing and/or retarding proliferation of tumor cells, for example carcinomas such as colon carcinomas.
    Type: Application
    Filed: June 7, 2010
    Publication date: August 16, 2012
    Applicant: OSLO UNIVERSITY HOSPITAL HF
    Inventors: Daniel Holsworth, Jo Waaler, Ondrej Machon, Stefan Krauss
  • Publication number: 20120208852
    Abstract: The present application relates to new, heterocyclyl-substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: August 24, 2010
    Publication date: August 16, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Chantal Fürstner, Joerg Keldenich, Armin Kern, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
  • Patent number: 8236963
    Abstract: The present invention is related to the use of spiro derivatives of Formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of spiro derivatives for the modulation of CRTH2 activity.
    Type: Grant
    Filed: May 23, 2006
    Date of Patent: August 7, 2012
    Assignee: Merck Serono SA
    Inventors: Matthias Schwarz, Eric Sebille, Christophe Cleva, Cedric Merlot, Dennis Church, Patrick Page, Jacqueline A. Macritchie, John Frederick Atherall, Stefano Crosignani, Doris Pupowicz
  • Publication number: 20120190695
    Abstract: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).
    Type: Application
    Filed: April 4, 2012
    Publication date: July 26, 2012
    Applicant: SANOFI
    Inventors: Christopher L. VANDEUSEN, Franz J. WEIBERTH, Harpal S. GILL, George LEE, Andrea HILLEGASS
  • Patent number: 8227494
    Abstract: 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: Grant
    Filed: March 8, 2010
    Date of Patent: July 24, 2012
    Assignee: PTC Therapeutics, Inc.
    Inventors: Gary Mitchell Karp, Seongwoo Hwang, Guangming Chen, Neil Gregory Almstead, Young-Choon Moon
  • Patent number: 8227495
    Abstract: The present disclosure provides 2,4-disubstituted thiazoles of the general structure shown below that are agonists of G-protein coupled receptor (IC-GPCR2). Also, provided are compositions comprising these compounds as well as methods for using these compounds in a variety of applications including diabetes and metabolic disorders.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: July 24, 2012
    Assignee: Metabolex Inc.
    Inventors: Xin Chen, Peng Cheng, L. Edward Clemens, Jeffrey D. Johnson, Jingyuan Ma, Alison Murphy, Imad Nashashibi, Christopher J. Rabbat, Jiangao Song, Maria E. Wilson, Yan Zhu, Zuchun Zhao
  • Publication number: 20120184544
    Abstract: The present invention relates to substituted benzamide derivatives of the general 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: Application
    Filed: July 22, 2010
    Publication date: July 19, 2012
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Rajendra Kharul, Makul R. Jain, Pankaj R. Patel
  • Patent number: 8217028
    Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
    Type: Grant
    Filed: June 18, 2009
    Date of Patent: July 10, 2012
    Assignee: Glaxo Group Limited
    Inventors: Jose Luis Castro Pineiro, Xichen Lin, Qian Liu, Kevin Meng, Feng Ren, David R Vesey, Baowei Zhao
  • Publication number: 20120165338
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and A are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: December 19, 2011
    Publication date: June 28, 2012
    Inventors: Johannes Aebi, Alfred Binggeli, Cornelia Hertel, Anish Ashok Konkar, Holger Kuehne, Bernd Kuhn, Hans P. Maerki, Haiyan Wang
  • Patent number: 8207205
    Abstract: 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: Grant
    Filed: April 20, 2009
    Date of Patent: June 26, 2012
    Assignee: Institute for OneWorld Health
    Inventors: Graham Peter Jones, Kevin James Doyle
  • Patent number: 8207183
    Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: June 26, 2012
    Assignee: Novartis AG
    Inventors: Mark G. Palermo, Sushil Kumar Sharma, Christopher Sean Straub, Run-Ming Wang, Leigh Zawel, Yanling Zhang, Zhuoliang Chen, Yaping Wang, Fan Yang, Wojciech Wrona, Gang Liu, Mark G. Charest, Feng He
  • Publication number: 20120157432
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Application
    Filed: August 17, 2010
    Publication date: June 21, 2012
    Applicant: Merck Sharp & Dohme, Corp.
    Inventors: Scott D. Edmondson, Richard Berger, Lehua Chang, Vincent j. Colandrea, Jeffrey J. Hale, Bart Harper, Nam Fung Kar, Bing Li, Greg J. Morriello, Christopher R. Moyes, Deyou Sha, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu
  • Patent number: 8202865
    Abstract: The invention relates to compounds of formula I: wherein R1, R2, Ra, Rb, W, Q and S have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
    Type: Grant
    Filed: October 1, 2008
    Date of Patent: June 19, 2012
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, Cyril Montagne, Wolfgang Sauer, Stefano Crosignani, Agnes Bombrun, Mathilde Muzerelle, Jermone Dorbais, Delphine Marin, Jerome Gonzalez, Patrick Gerber
  • Patent number: 8202856
    Abstract: The invention relates to compounds of formula I: wherein R1, R2,Ra, Rb, X have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: June 19, 2012
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, Christophe Cleva, Eric Sebille, Matthias Schwarz, Delphine Marin, Agnes Bombrun, Wesley Blackaby, Charles Baker-Glenn, Chris Knight, Craig Rouse
  • Publication number: 20120142663
    Abstract: The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 10, 2011
    Publication date: June 7, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha Bin Im
  • Publication number: 20120142664
    Abstract: 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: Application
    Filed: November 11, 2011
    Publication date: June 7, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Wenkui K. FANG, Liming WANG, Evelyn G. CORPUZ, Ken CHOW, Wha Bin IM
  • Publication number: 20120142639
    Abstract: The present invention relates to novel oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 14, 2011
    Publication date: June 7, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha Bin Im
  • Publication number: 20120142745
    Abstract: The present invention relates to novel phenyl oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 14, 2011
    Publication date: June 7, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha Bin Im
  • Publication number: 20120129832
    Abstract: 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: Application
    Filed: August 4, 2010
    Publication date: May 24, 2012
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Shigeo Yamanoi, Hidenori Namiki, Takahiro Katagiri, Mayuko Akiu, Katsuji Kagechika, Takeshi Honda, Koji Matsumoto, Ryutaro Nakashima
  • Publication number: 20120129891
    Abstract: 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: Application
    Filed: August 4, 2010
    Publication date: May 24, 2012
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Shigeo Yamanoi, Hidenori Namiki, Takahiro Katagiri, Mayuko Akiu, Katsuji Kagechika, Takeshi Honda, Koji Matsumoto, Ryutaro Nakashima
  • Publication number: 20120129829
    Abstract: The present invention relates to novel indole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 10, 2011
    Publication date: May 24, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, Michael M. Garst, Wha Bin Im
  • Patent number: 8183262
    Abstract: The present invention relates to compounds of formula (I), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: wherein A, B, X, Y, R1, R2, R3 and R4 are as defined in the description and claims.
    Type: Grant
    Filed: September 1, 2009
    Date of Patent: May 22, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Silvia Gatti McArthur, Erwin Goetschi, Juergen Wichmann, Thomas Johannes Woltering
  • Publication number: 20120122896
    Abstract: A 2,1,3-benzoxadiazole compound as a medicament according to the invention is one of the following compounds: 4-[(4-methoxybenzyl)thio]-7-nitro-2,1,3-benzoxadiazole, 2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)thio]ethyl 4-methoxybenzene-1-sulfonate, 4-[(4-methylphenyl)thio]-7-nitro-2,1,3-benzoxadiazole, 4-[(2,4-dichlorophenyl)thio]-7-nitro-2,1,3-benzoxadiazole, 2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)thio]ethan-1-ol, 4-[(4-methylbenzyl)thio]-7-nitro-2,1,3-benzoxadiazole, 4-[(4-fluorophenyl)thio]-7-nitro-2,1,3-benzoxadiazole, 4-[(3-chlorophenyl)-thio]-7-nitro-2,1,3-benzoxadiazole, 2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)thio]ethyl-4-methoxy-benzoate, 5-[4-(tert-butyl)-1,3-thiazol-2-yl]-2,1,3-benzoxadiazole, N-benzyl-4-nitro-2,1,3-benzoxadiazol-5-amine, 4-nitro-7-(phenylmethylsulfanyl)-2,1,3-benzoxadiazole, 4-nitro-7-(phenylmethylsulfonyl)-2,1,3-benzoxadiazole, 2-(hydroxymethyl)-5-[6-[(4-nitro-2,1,3-benzoxadiazol-7-yl)sulfanyl]purin-9-yl]oxolane-3,4-diole, or 2-[2-amino-6-[(4-nitro-2,1,3-benzoxadiazol-7-yl)sulfanyl]purin-9
    Type: Application
    Filed: May 7, 2010
    Publication date: May 17, 2012
    Applicant: PIKE PHARMA GMBH
    Inventors: Ulrich Kessler, Charlene Ranadheera
  • Publication number: 20120108595
    Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.
    Type: Application
    Filed: June 28, 2010
    Publication date: May 3, 2012
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
  • Publication number: 20120101134
    Abstract: 5-membered heteroaryl derivatives of formula (I) or salts thereof, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptors are disclosed.
    Type: Application
    Filed: June 24, 2010
    Publication date: April 26, 2012
    Applicant: GLAXO GROUP LIMITED
    Inventors: Guanghui Deng, Xichen Lin, Qinghua Meng, Feng Ren, Jia-Ning Xiang, Heng Xu, Haibo Zhang, Baowei Zhao
  • Publication number: 20120101136
    Abstract: 5-membered heteroaryl derivatives of formula (I) or salts thereof, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptors are disclosed.
    Type: Application
    Filed: June 24, 2010
    Publication date: April 26, 2012
    Inventors: Guanghui Deng, Xichen Lin, Feng Ren, Jia-Ning Xiang
  • Publication number: 20120101091
    Abstract: The present application provides compounds of formula I wherein X, Y, R2, n, R5 and R6 are defined herein, useful as inhibitors of the hepatitis C virus NS5B polymerase The present application also provides pharmaceutical compositions containing said compounds, methods of using said compounds as pharmaceuticals alone or with other antiviral agent in the treatment of a hepatitis C viral infection in a mammal having or at risk of having the infection.
    Type: Application
    Filed: October 1, 2009
    Publication date: April 26, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Pierre Beaulieu, Pierre Bonneau, René Coulombe, Pasquale Forgione, James Gillard, Araz Jakalian, Jean Rancourt
  • Publication number: 20120101124
    Abstract: 1,2,4-Oxadiazol derivatives represented by formula (I) useful as sphingosine 1-phosphate 1 (S1P1) receptor agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders mediated via S1P1 receptor are disclosed.
    Type: Application
    Filed: June 17, 2010
    Publication date: April 26, 2012
    Applicant: GLAXO GROUP LIMITED
    Inventors: Xichen Lin, Feng Ren, Yugui Si
  • Patent number: 8163782
    Abstract: 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: Grant
    Filed: August 18, 2011
    Date of Patent: April 24, 2012
    Assignee: PTC Therapeutics, Inc.
    Inventors: Gary Mitchell Karp, Seongwoo Hwang, Guangming Chen, Neil Gregory Almstead, Young-Choon Moon
  • Publication number: 20120088716
    Abstract: Method for increasing half-life of compounds in plasma and novel derivatives of such compounds.
    Type: Application
    Filed: December 15, 2011
    Publication date: April 12, 2012
    Applicant: Novo Nordisk A/S
    Inventors: Florencio Zaragoza Dörwald, Christine Bruun Schiødt, Thomas Kruse Hansen, Kjeld Madsen
  • Patent number: 8153682
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.
    Type: Grant
    Filed: July 18, 2008
    Date of Patent: April 10, 2012
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman