Ring Sulfur Or Ring Oxygen In The Additional Hetero Ring Patents (Class 546/209)
  • OXADIAZOLE COMPOUNDS, THEIR PREPARATION AND USE
    Publication number: 20130005771
    Abstract: The present invention relates to oxadiazole compounds in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable prodrugs and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the oxadiazole compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the treatment of cancer, particularly chronic myeloid leukemia (CML). The present invention further provides a method of treatment of cancer by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.
    Type: Application
    Filed: February 24, 2011
    Publication date: January 3, 2013
    Inventors: Meenakshi Sivakumar, Kalpana Sanjay Joshi, Valmik Sopan Aware, Ankush Gangaram Sarde, Sandeep Maruti Bagul, Sonal Mohan Manohar
  • ANILINOPIPERAZINE DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20120328691
    Abstract: The present invention relates to novel Anilinopiperazine Derivatives of Formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, cancer, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.
    Type: Application
    Filed: October 29, 2007
    Publication date: December 27, 2012
    Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards, Hongbo Zeng, Binyuan Sun, Panduranga Adulla Reddy, Tzu T. Wong, Praveen K. Tadikonda, M. Arshad Siddiqui, Marc A. Labroli, Cory Poker, Timothy J. Guzi
  • Compounds having a potentiating effect on the activity of ethionamide and uses thereof
    Patent number: 8338599
    Abstract: The present invention relates to the use of compounds with a potentiating effect on the activity of antibiotics that are activatable via the EthA enzymatic pathway, for the preparation of a medicament for preventing and/or treating mycobacterial infections such as tuberculosis and leprosy, to pharmaceutical compositions comprising them in combination with an antibiotic that is activatable via the EthA pathway, to compounds having a potentiating effect on the activity of antibiotics that are activatable via the EthA enzymatic pathway, to pharmaceutical compositions comprising them and to their use as medicaments, especially medicaments for preventing and/or treating mycobacterial infections such as tuberculosis and leprosy.
    Type: Grant
    Filed: July 4, 2007
    Date of Patent: December 25, 2012
    Assignees: Institut Pasteur de Lille, Centre National de la Recherche Scientifique, Universite de Lille 2, Universite du Droit et de la Sante, Institut National de la Sante et de la Recherche Medicale (Inserm)
    Inventors: Benoît Deprez, Nicolas Willand, Bertrand Dirie, Patrick Toto, Vincent Villeret, Camille Locht, Alain Baulard
  • N-LINKED HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS
    Publication number: 20120322804
    Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.
    Type: Application
    Filed: May 3, 2012
    Publication date: December 20, 2012
    Inventors: Jingyuan Ma, Christopher J. Rabbat, Jiangao Song, Xin Chen, Imad Nashashibi, Zuchun Zhao, Aaron Novack, Dong Fang Shi, Peng Cheng, Yan Zhu, Alison Murphy
  • COMPOUNDS AND METHODS
    Publication number: 20120322827
    Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, n and L are as defined herein, and methods of making and using the same.
    Type: Application
    Filed: January 13, 2011
    Publication date: December 20, 2012
    Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
  • Thiadiazolyloxyphenylamidines and use thereof as fungicides
    Patent number: 8334235
    Abstract: The present invention relates to thiadiazolyloxyphenylamidines of the general formula (I), to a process for the preparation thereof, to the use of the amidines according to the invention in combating undesirable microorganisms and to a composition for this purpose comprising the thiadiazolyloxyphenylamidines according to the invention. The invention furthermore relates to a method for combating undesirable microorganisms by application of the compounds according to the invention to the microorganisms and/or to the habitat thereof.
    Type: Grant
    Filed: June 19, 2009
    Date of Patent: December 18, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Pierre Cristau, Jörg Nico Greul, Ulrich Heinemann, Klaus Kunz, Oswald Ort, Thomas Seitz, Arnd Voerste, Peter Dahmen, Ulrike Wachendorff-Neumann, Klaus-Günther Tietjen, Hiroyuki Hadano
  • PROTEOSTASIS REGULATORS
    Publication number: 20120316193
    Abstract: The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.
    Type: Application
    Filed: May 10, 2012
    Publication date: December 13, 2012
    Inventors: Megan Foley, Bradley Tait, Matthew Cullen
  • Compositions and Methods for Modulating a Kinase
    Publication number: 20120316148
    Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase signaling cascade.
    Type: Application
    Filed: June 7, 2012
    Publication date: December 13, 2012
    Applicant: Dynamix Pharmaceuticals LTD.
    Inventors: Oren M. Becker, Itai Bloch, Efrat Ben-Zeev, Alina Shitrit, Avihai Yacovan, Sharon Gazal, Vered Behar, Alexander Konson, Nili Schutz, Sima Mirilashvili, Gali Golan
  • CHARGE CONTROLLING AGENT AND TONER USING SAME
    Publication number: 20120315576
    Abstract: The present invention provides a charge control agent containing, as an active substance(s), one or two or more rhodanine compounds represented by the following formula (1). where R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, a linear or branched alkyl group having 1 to 8 carbon atoms which may have a substituent, a substituted or unsubstituted heterocyclic group, etc.; R3 to R7, which may be identical to or different from each other, represent a hydrogen atom, a linear or branched alkyl group having 1 to 10 carbon atoms which may have a substituent, a linear or branched alkyloxy group having 1 to 20 carbon atoms which may have a substituent, etc., and may be joined to each other to form a ring; and V, W, X, Y and Z represent a carbon atom or a nitrogen atom, and 0 to 3 of any of V, W, X, Y and Z are nitrogen atoms which do not have the substituents of R3 to R7.
    Type: Application
    Filed: February 21, 2011
    Publication date: December 13, 2012
    Applicant: HODOGAYA CHEMICAL CO., LTD.
    Inventors: Masateru Yasumura, Masami Ito, Masaya Tojo, Kanae Hiraishi, Masaki Okubo, Hideyuki Otsuka
  • CYTOCHROME P450 OXIDASE INHIBITORS AND USES THEREOF
    Publication number: 20120309762
    Abstract: The present invention features compounds of formula I or pharmaceutically acceptable salts, solvates or prodrugs thereof, and methods of using the same to inhibit the metabolizing activities of CYP enzymes. The present invention also features methods of using these compounds, salts, solvates or prodrugs to improve the pharmacokinetics of drugs that are metabolized by CYP enzymes.
    Type: Application
    Filed: August 16, 2012
    Publication date: December 6, 2012
    Applicant: Abbott Laboratories
    Inventors: Larry L. Klein, Hui-Ju Chen, Ming C. Yeung, Charles A. Flentge, John T. Randolph, Peggy P. Huang, Douglas K. Hutchinson, Dale J. Kempf
  • SYNTHETIC INTERMEDIATE OF OXAZOLE COMPOUND AND METHOD FOR PRODUCING THE SAME
    Publication number: 20120302757
    Abstract: An object of the present invention is to provide a method for producing an oxazole compound in a high yield.
    Type: Application
    Filed: January 28, 2011
    Publication date: November 29, 2012
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro Yamamoto, Koichi Shinhama, Nobuhisa Fujita, Shinji Aki, Shin Ogasawara, Naoto Utsumi
  • 1,3,4-OXADIAZOLE-2-CARBOXAMIDE COMPOUND
    Publication number: 20120302524
    Abstract: Provided is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Provided is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof (in the formula, Ar represents a furyl group or the like; R1 represents a hydrogen atom or the like; and —X—Y represents a diaryl group such as a biphenyl group).
    Type: Application
    Filed: December 28, 2010
    Publication date: November 29, 2012
    Applicants: GENERAL INCORPORATED ASSOCIATION PHARMA VALLEY PROJECT SUPPORTING ORGANIZATION, PHARMA DESIGN, INC., KABUSHIKI KAISHA YAKULT HONSHA, KUMAMOTO HEALTH SCIENCE UNIVERSITY, SHIZUOKA PREFECTURE
    Inventors: Akira Asai, Kenji Matsuno, Naohisa Ogo, Osamu Takahashi, Yoshiaki Masuda, Ayumu Muroya, Yasuto Akiyama, Tadashi Ashizawa, Tadashi Okawara
  • 3-(4-((1H-IMIDAZOL-1-YL)METHYL)PHENYL)-5-ARYL-1,2,4-OXADIAZOLE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS
    Publication number: 20120302606
    Abstract: Substituted 3-(4-((1H-imidazol-1-yl)methyl)phenyl)-5-phenyl-1,2,4-oxadiazole derivatives which are useful as sphingosine-1-phosphate modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: August 6, 2012
    Publication date: November 29, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Janet A. Takeuchi, Ken Chow, Ling Li
  • PHENYL-THIAZOLYL INHIBITORS OF PRO-MATRIX METALLOPROTEINASE ACTIVATION
    Publication number: 20120302569
    Abstract: This invention relates to phenyl thiazole I and its therapeutic and prophylactic uses, wherein the variables Rz, Q, J, R1, R3, R5, R6, and R7 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.
    Type: Application
    Filed: May 24, 2012
    Publication date: November 29, 2012
    Inventors: Paul Francis JACKSON, Kristi Anne Leonard, Joseph Kent Barbay, Aihua Wang, Brett Andrew Tounge, Yan Zhang, Umar S.M. Maharoof
  • Compounds involving mGluR5 receptor regulation and methods of making the compounds
    Patent number: 8318774
    Abstract: 3-((Thiazol-2-yl)amino)propylproiolamide compounds of the formula I: wherein the variables are as defined herein, are useful to prevent or treat a disease or disorder involving mGluR5 receptor regulation. Also disclosed are pharmaceutical compositions containing the compounds and methods of making the compounds.
    Type: Grant
    Filed: June 26, 2008
    Date of Patent: November 27, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Michael Haurand, Klaus Schiene, Sven Kühnert, Melanie Reich
  • PYRROLIDINE COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF
    Publication number: 20120295894
    Abstract: Described herein are novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.
    Type: Application
    Filed: December 1, 2011
    Publication date: November 22, 2012
    Inventors: Geoffrey M. BILCER, Thippeswamy Devasamudram, Sudha V. Ankala, John C. Lilly, Chunfeng Liu, Hui Lei, Arun K. Ghosh, Makoto Inoue
  • Sultam derivatives
    Patent number: 8314250
    Abstract: The present invention relates to compounds according to formula 1, which exhibit cytotoxic activity. The compounds may be used in the treatment of cancer.
    Type: Grant
    Filed: October 15, 2010
    Date of Patent: November 20, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kevin W. Anderson, Paul Gillespie, Nicholas J. S. Huby, Norman Kong, John L. Roberts, Pamela L. Rossman, Sung-Sau So
  • CERTAIN HETEROCYCLES, COMPOSITIONS THEREOF, AND METHODS FOR THEIR USE
    Publication number: 20120289698
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 13, 2012
    Publication date: November 15, 2012
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
  • Quinuclidine compounds as ?-7 nicotinic acetylcholine receptor ligands
    Patent number: 8309577
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic ?7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: November 13, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: James H. Cook, II, Ivar M. McDonald, Dalton King, Richard E. Olson, Nenghui Wang, Christiana I. Iwuagwu, F. Christopher Zusi, John E. Macor
  • Thiazolyl-dihydro-indazoles
    Patent number: 8304556
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: January 11, 2012
    Date of Patent: November 6, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Darryl McConnell, Maria Impagnatiello, Dirk Kessler, Oliver Kraemer, Siegfried Schneider, Lars Van Der Veen, Ulrike Weyer-Czernilofsky, Tobias Wunberg
  • 1,2,4-OXADIAZOLE BENZOIC ACIDS
    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
  • INHIBITORS OF DIACYLGLYCEROL O-ACYLTRANSFERASE TYPE 1 ENZYME
    Publication number: 20120277223
    Abstract: The present invention relates to compounds of formula (I): wherein Q, G1, G2, and G3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.
    Type: Application
    Filed: July 16, 2012
    Publication date: November 1, 2012
    Inventors: Andrew S. Judd, Mathew M. Mulhern, Rajesh R. lyengar, Philip R. Kym, Andrew J. Souers
  • ALKALOID ESTER AND CARBAMATE DERIVATIVES AND MEDICINAL COMPOSITIONS THEREOF
    Publication number: 20120276018
    Abstract: Compounds according to formula (I) are effective for the treatment of broncho-obstructive and inflammatory diseases.
    Type: Application
    Filed: April 27, 2012
    Publication date: November 1, 2012
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele AMARI, Mauro Riccaboni, Daniele De Zani
  • Compounds, Compositions and Methods Comprising Oxadiazole Derivatives
    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
  • INHIBITORS OF SPHINGOSINE KINASE
    Publication number: 20120252815
    Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, Y1, Y2, V, W, n, m and o have the gleanings given herein, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.
    Type: Application
    Filed: November 18, 2010
    Publication date: October 4, 2012
    Applicant: Merck Patent Gesellschaft MIT Beschrankter Haftung
    Inventors: Frank Stieber, Dirk Wienke
  • Isoxazole Compounds As Inhibitors Of Heat Shock Proteins
    Publication number: 20120252797
    Abstract: Isoxazoles of formula (A) or (B) wherein R1 is a group of formula (IB) The isoxazoles are inhibitors of HSP90 activity, and useful for the treatment of, for example, cancers.
    Type: Application
    Filed: June 18, 2012
    Publication date: October 4, 2012
    Applicants: Vernalis (Cambridge) Limited, The Institute of Cancer Research, Cancer Research Technology Ltd.
    Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
  • (1, 1, 1,3,3,3 -HEXAFLUORO-2 HYDROXYPROPAN- 2 -YL) PHENYL DERIVATIVE, PHARMACEUTICAL COMPOSITIONS THEREOF AND THEIR USE FOR THE TREATMENT OF ATHEROSCLEROSIS
    Publication number: 20120238574
    Abstract: The present invention relates to (1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl derivatives having the general formula (I) to pharmaceutical compositions comprising the same and to the use of these (1,1,1,3,3,3-hexafluoro-2-hydroxy-propan-2-yl)phenyl derivatives in the treatment of atherosclerosis.
    Type: Application
    Filed: October 26, 2010
    Publication date: September 20, 2012
    Applicant: N.V. ORGANON
    Inventors: Andrew John Cooke, Emma Louise Carswell, David Jonathan Bennett
  • Inhibitors of C-MET and uses thereof
    Patent number: 8268818
    Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: September 4, 2007
    Date of Patent: September 18, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Tiansheng Wang, Jeremy Green, Brian Ledford, François Maltais, Andreas P. Termin, Mark Cornebise, Jonathan Parsons, Adam Tanner, James Westcott
  • SELECTIVE CALCIUM CHANNEL MODULATORS
    Publication number: 20120220564
    Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed using a series of compounds containing N-acylated cyclic amines linked to an a?l ring as shown in formula (I).
    Type: Application
    Filed: September 17, 2010
    Publication date: August 30, 2012
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan Pajouhesh, Yongbao Zhu, Yuanxi Zhou, Michael E. Grimwood, Eric Simonson
  • Substituted piperidines
    Publication number: 20120220563
    Abstract: The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders.
    Type: Application
    Filed: May 19, 2010
    Publication date: August 30, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Eckhard Bender, Katja Zimmermann, Anja Buchmüller, Christoph Gerdes, Mark Jean Gnoth, Kersten Matthias Gericke, Mario Jeske
  • 5-substituted-2-imino-thiazolidinone compounds and their use as inhibitors of bacterial infection
    Patent number: 8252940
    Abstract: A method for inhibiting Gram-negative bacterial pathogenesis, a method of screening for compounds that inhibit type III secretion in Gram-negative bacteria, and compounds that inhibit type III secretion in Gram-negative bacteria.
    Type: Grant
    Filed: August 16, 2010
    Date of Patent: August 28, 2012
    Assignee: University of Washington
    Inventors: Heather B. Felise, Samuel I. Miller, Toni Kline
  • PYRROLIDINE COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF
    Publication number: 20120214802
    Abstract: Described herein are novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.
    Type: Application
    Filed: October 9, 2009
    Publication date: August 23, 2012
    Inventors: Geoffrey M. Bilcer, Thippeswamy Devasamudram, Sudha V. Ankala, John C. Lilly, Chunfeng Liu, Hui Lei, Arun K. Ghosh, Makoto Inoue
  • ACETAMIDE DERIVATIVES AS GLUCOKINASE ACTIVATORS, THEIR PROCESS AND MEDICINAL APPLICATIONS
    Publication number: 20120214735
    Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 23, 2012
    Applicant: Advinus Therapeutics Limited
    Inventors: Debnath Bhuniya, Anil Deshpande, Sachin Kandalkar, Balasaheb Kobal, Santosh Kurhade, Vinod Vyavahare, Rahul Kaduskar
  • Inhibitors of diacylglycerol O-acyltransferase type 1 enzyme
    Patent number: 8242139
    Abstract: The present invention relates to compounds of formula (I): wherein Q, G1, G2, and G3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.
    Type: Grant
    Filed: April 30, 2008
    Date of Patent: August 14, 2012
    Assignee: Abbott Laboratories
    Inventors: Andrew S. Judd, Mathew M. Mulhern, Rajesh R. Iyengar, Philip R. Kym, Andrew J. Souers
  • THERAPEUTIC ISOXAZOLE COMPOUNDS
    Publication number: 20120202786
    Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.
    Type: Application
    Filed: April 16, 2012
    Publication date: August 9, 2012
    Applicant: Dart Neuroscience (Cayman) Ltd.
    Inventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
  • IL17 AND IFN-GAMMA INHIBITION FOR THE TREATMENT OF AUTOIMMUNE INFLAMMATION
    Publication number: 20120196861
    Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.
    Type: Application
    Filed: January 27, 2012
    Publication date: August 2, 2012
    Applicant: 4SC Discovery GmbH
    Inventors: Johann LEBAN, Stefan TASLER, Roland BAUMGARTNER, Wael SAEB, Carine CHEVRIER
  • PROPHYLACTIC OR THERAPEUTIC AGENT FOR CANCER
    Publication number: 20120196864
    Abstract: A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof has a superior activity as an estrogen-related receptor-? modulator, and is useful as a prophylactic or therapeutic agent for cancer.
    Type: Application
    Filed: August 4, 2010
    Publication date: August 2, 2012
    Inventors: Atsushi Hasuoka, Koji Ono, Masanori Kawasaki
  • 2-aminothiazole-4-carboxylic amides as protein kinase inhibitors
    Patent number: 8227605
    Abstract: The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.
    Type: Grant
    Filed: October 29, 2007
    Date of Patent: July 24, 2012
    Assignee: Schering Corporation
    Inventors: Gerald W. Shipps, Jr., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards
  • 2,4-disubsituted thiazoles and pharmaceutical compositions thereof
    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
  • SUBSTITUTED AMIDE COMPOUND
    Publication number: 20120184521
    Abstract: A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: In this formula, A is an optionally substituted aryl, etc.; B is an optionally substituted 5-membered aromatic hetero ring group; X is a single bond or —(CRX1RX2)n—; n is 1, 2, 3, or 4; RX1 and RX2 are hydrogen, etc.; Y1 to Y5 are each CRY or N; each RY is hydrogen, etc.; R1 and R2 are hydrogen, etc.; m is 1, 2, or 3; R3 is hydrogen, etc.; and R4 is an optionally substituted lower alkyl, etc.
    Type: Application
    Filed: September 24, 2010
    Publication date: July 19, 2012
    Applicant: Astellas Pharma Inc.
    Inventors: Eiji Kawaminami, Tatsuhisa Takahashi, Takatoshi Kanayama, Yuta Fukuda, Hiroyuki Kaizawa, Yutaka Kondoh, Ryushi Seo, Kazuyuki Kuramoto, Kazuhiko Take, Kazuyuki Sakamoto
  • SUBSTITUTED BENZAMIDE DERIVATIVES AS GLUCOKINASE (GK) ACTIVATORS
    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
  • Therapeutic isoxazole compounds
    Patent number: 8222243
    Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.
    Type: Grant
    Filed: August 26, 2008
    Date of Patent: July 17, 2012
    Assignee: Dart NeuroScience (Cayman) Ltd
    Inventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
  • PHENYL SULPHONAMIDES AS MODULATORS OF ION CHANNELS
    Publication number: 20120178713
    Abstract: The present invention relates to phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.
    Type: Application
    Filed: March 14, 2012
    Publication date: July 12, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Esther Martinborough, Lev T.D. Fanning, Urvi Sheth, Dean Wilson, Andreas P. Termin, Timothy D. Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson
  • FACTOR XA INHIBITORS
    Publication number: 20120178733
    Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
    Type: Application
    Filed: August 19, 2011
    Publication date: July 12, 2012
    Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
  • Substituted piperidino phenyloxazolidinones
    Patent number: 8217058
    Abstract: The present invention relates to certain substituted piperidino phenyloxazolidinones. Specifically, the invention relates to geminally disubstituted piperidino phenyloxazolidinones having antimicrobial activity with improved pharmacokinetic profile. The invention also relates to processes for the preparation of compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the methods for treating or preventing microbial infections using the compounds of the present invention.
    Type: Grant
    Filed: May 8, 2007
    Date of Patent: July 10, 2012
    Assignee: Wockhardt Ltd.
    Inventors: Mahesh Vithalbhai Patel, Mahesh Phansalkar, Vijaykumar Jagdishwar Patil, Milind Dattatraya Sindkhedkar, Prasad Keshav Deshpande
  • Inhibitors of diacylglycerol acyltransferase
    Patent number: 8211914
    Abstract: Provided herein are amides containing at least a four ring structure, which are inhibitors of diacylglycerol acyltransferase and are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: July 3, 2012
    Assignee: Madrigal Pharmaceuticals, Inc.
    Inventors: David Robert Bolin, Adrian Wai-Hing Cheung, Fariborz Firooznia, Nicholas Marcopulos, Yimin Qian
  • NOVEL 3-HYDROXY-5-ARYLISOTHIAZOLE DERIVATIVE
    Publication number: 20120157459
    Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of solving the problem] A compound of Formula (I): (where n is 0 to 2; p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is an aryl group which is optionally substituted with L or a heterocyclic group which is optionally substituted with L; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is O, S, —NR7—; and R1 to R7 are specific groups), a salt of the compound, or a solvate of the salt or the compound.
    Type: Application
    Filed: December 24, 2010
    Publication date: June 21, 2012
    Inventors: Akihiro Okano, Naoto Kosuga, Munetaka Ohkouchi, Daido Hotta, Muneyoshi Makabe
  • Oxadiazole derivatives
    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
  • Sulfonamide Derivatives
    Publication number: 20120149679
    Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.
    Type: Application
    Filed: February 20, 2012
    Publication date: June 14, 2012
    Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
  • Guanidine-containing compounds useful as muscarinic receptor antagonists
    Patent number: 8198304
    Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: September 9, 2011
    Date of Patent: June 12, 2012
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li