1,2-diazole (including Hydrogenated) Patents (Class 546/211)
  • Patent number: 9340522
    Abstract: The compounds of Formula (I), are novel effective inhibitors of the type 4 phosphodiesterase.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: May 17, 2016
    Assignee: TAKEDA GMBH
    Inventors: Imre Schlemminger, Beate Schmidt, Dieter Flockerzi, Hermann Tenor, Christof Zitt, Armin Hatzelmann, Degenhard Marx, Clemens Braun, Raimund Kuelzer, Anke Heuser, Hans-Peter Kley, Geert Jan Sterk
  • Patent number: 9198425
    Abstract: Sulfinylaminobenzamides of the general formula (I) as herbicides are described. In this formula (I), R, R?, R?, X, W and Z are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a tetrazolyl, triazolyl or oxadiazolyl radical.
    Type: Grant
    Filed: February 18, 2013
    Date of Patent: December 1, 2015
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Hartmut Ahrens, Ralf Braun, Arnim Koehn, Stefan Lehr, Hansjoerg Dietrich, Dirk Schmutzler, Elmar Gatzweiler, Christopher Hugh Rosinger
  • Publication number: 20150126364
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Q is and Z1, Z2, J1, J2, M, R1a, R1b, R2a, R2b, R2c, R2d, R14 and R14a are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: May 13, 2013
    Publication date: May 7, 2015
    Applicant: E I Du Pont de Nemours and Company
    Inventors: Thomas Francis Pahutski, JR., Matthew James Campbell, Dominic Ming-Tak Chan, Jeffrey Keith Long, Thomas Martin Stevenson
  • Publication number: 20150126516
    Abstract: A piperidine compound represented by the following Formula (1): wherein ring A, ring B, and ring C are the same or different and each represent a benzene ring or a nitrogen-containing heteroaromatic ring; W represents a C1-C4 alkylene or alkenylene group; X, Y, and Z are the same or different and each represent a halogen atom, a C1-C6 alkyl group, a halo C1-C6 alkyl group, a C1-C6 alkoxy group, or a halo C1-C6 alkoxy group; m, n, and p are the same or different and each represent an integer of 0 to 5; when m is greater than or equal to 2, the Xs are the same or different; when n is greater than or equal to 2, the Ys are the same or different; and when p is greater than or equal to 2, the Zs are the same or different has an excellent controlling efficacy against pests.
    Type: Application
    Filed: April 12, 2013
    Publication date: May 7, 2015
    Inventor: Sadayuki Arimori
  • Publication number: 20150111922
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: (I) in which m, n, W, X, Y, Z, R1, R2, R3 and R4 are as defined in the specification, for use in the treatment or prevention of a diseases o conition mediated by a prokineticin, such as psychiatric and neurological conditions.
    Type: Application
    Filed: May 29, 2013
    Publication date: April 23, 2015
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Colm Carroll, Anne Goldby, Martin Teall
  • Patent number: 8993752
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: March 31, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Roland Gendron, Adam D. Hughes
  • Patent number: 8987248
    Abstract: The invention relates to novel substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular disorders and tumor disorders.
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: March 24, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Mario Jeske, Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Kersten Matthias Gericke
  • Publication number: 20150073141
    Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders and the like.
    Type: Application
    Filed: July 15, 2014
    Publication date: March 12, 2015
    Inventors: Bradley Teegarden, Honnappa Jayakumar, Hongmei Li, Sonja Strah-Pleynet, Peter I. Dosa
  • Patent number: 8962845
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, and X are defined herein. Also disclosed are pharmaceutical compositions and methods related to use of these compounds.
    Type: Grant
    Filed: September 25, 2012
    Date of Patent: February 24, 2015
    Assignee: National Health Research Institutes
    Inventors: Kak-Shan Shia, Chun-Ping Chang, Yu-Sheng Chao
  • Patent number: 8957066
    Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3) using compounds of formula (I), wherein the substituents are as defined herein.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: February 17, 2015
    Assignee: Biomarin Pharmaceutical Inc.
    Inventors: Vincent Jacques, James R Rusche, Norton P. Peet, Jasbir Singh
  • Patent number: 8933102
    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 b3-adrenoceptor. Formula (I).
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: January 13, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gregori J. Morriello, Lehua Chang, Scott D. Edmondson
  • Publication number: 20150005275
    Abstract: The present invention discloses compounds according to Formula I: wherein R1, R2, R3, L, and the subscript m are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions, and methods of treatment using the same, for the treatment of cystic fibrosis by administering a compound of the invention.
    Type: Application
    Filed: May 6, 2014
    Publication date: January 1, 2015
    Inventors: Steven Emiel Van der Plas, Oscar Mammoliti, Christel Jeanne Marie Menet, Giovanni Alessandro Tricarico, Ann De De Blieck, Caroline Martine Andrée Marie Joannesse, Hans Kelgtermans, Tom Roger Lisette De Munck
  • Publication number: 20150005277
    Abstract: The invention is compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
    Type: Application
    Filed: June 21, 2014
    Publication date: January 1, 2015
    Inventors: Zhiwei Wang, Yunhang Guo
  • Publication number: 20140371176
    Abstract: This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.
    Type: Application
    Filed: September 3, 2014
    Publication date: December 18, 2014
    Inventors: Neil W. Johnson, Jiri Kasparec, Meagan B. Rouse, Xinrong Tian
  • Patent number: 8906938
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Grant
    Filed: May 14, 2013
    Date of Patent: December 9, 2014
    Assignee: ChemoCentryx, Inc.
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay P. Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Publication number: 20140329857
    Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q 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: Application
    Filed: July 18, 2014
    Publication date: November 6, 2014
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
  • Publication number: 20140329817
    Abstract: This disclosure relates to antiviral compounds disclosed herein and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions. Typically, the pharmaceutical composition comprises a compound of formula I: Formula I, or salt, prodrug, or ester thereof wherein X, Y, and R1 and R10 to R13 are described herein.
    Type: Application
    Filed: October 24, 2012
    Publication date: November 6, 2014
    Applicants: CHILDREN'S HEATLHCARE OF ATLANTA, INC., EMORY UNIVERSITY
    Inventors: Richard K. Plemper, James P. Snyder, Aiming Sun
  • Patent number: 8871790
    Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: October 28, 2014
    Assignee: 3-V Biosciences, Inc.
    Inventors: Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu
  • Publication number: 20140315904
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
  • Patent number: 8865745
    Abstract: The compound 1-(2-{4-[3-(3,4-dimethoxyphenyl)-4,4-dimethyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl]piperidin-1-yl}-2-oxoethyl)pyrrolidine-2,5-dione is a novel effective inhibitor of the type 4 phosphodiesterase.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: October 21, 2014
    Assignee: Takeda GmbH
    Inventors: Beate Schmidt, Christian Scheufler, Juergen Volz, Martin Feth, Rolf-Peter Hummel, Armin Hatzelmann, Christof Zitt, Andrea Wohlsen, Degenhard Marx, Hans-Peter Kley, Deborah Ockert, Anke Heuser, Johannes A. M. Christiaans, Geert Jan Sterk, Wiro M. P. B. Menge
  • Patent number: 8853205
    Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or CB2 cannabinoid receptors. Aspects disclose hetero pyrrole analogs acting as CB1 and/or CB 1 receptor antagonists, having selectivity for the CB 1 or CB2 receptor, acting as neutral antagonists, acting preferentially on CB 1 receptors located in the peripheral nervous system, and/or acting as nitric oxide donors. Pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect are also disclosed.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: October 7, 2014
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Venkata Kiran Vemuri
  • Patent number: 8846675
    Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.
    Type: Grant
    Filed: May 3, 2012
    Date of Patent: September 30, 2014
    Assignee: Cymabay Therapeutics, Inc.
    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
  • Publication number: 20140275126
    Abstract: Disclosed is a process for the preparation of the following compounds: where R1, R1a and R2a have the definitions in the description, as well as a process to prepare other intermediates that may be useful to synthesise downstream products, especially compounds that are useful as medicaments, for instance Bruton's tyrosine kinase (Btk) inhibitors such as ibrutinib. Also disclosed are other processes, other intermediates and compounds per se.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Inventors: Philip PYE, Cyril BEN HAIM, Matteo CONZA, Ioannis Nicolaos HOUPIS
  • Publication number: 20140275049
    Abstract: The present invention provides compounds of Formula I or a pharmaceutical salt thereof; methods of treating osteoarthritis and the pain associated with osteoarthritis using the compounds; and processes for preparing the compounds.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 18, 2014
    Inventors: Thomas John Bleisch, David Andrew Coates, Norman Earle Hughes, Scott Alan Jones, Bryan Hurst Norman
  • Patent number: 8835437
    Abstract: The invention further relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —S(?O)p—; C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —O—C(?O)—; —C(?O)—C(?O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5-or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxlyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzo-dioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-m
    Type: Grant
    Filed: June 5, 2008
    Date of Patent: September 16, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-Pierre André Marc Bongartz, Lieven Meerpoel, Gustaaf Maria Boeckx, Guy Rosalia Eugeen Van Lommen, Christophe Francis Robert Nestor Buyck, Daniel Obrecht, Philipp Ermert, Anatol Luther
  • Publication number: 20140249025
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Q is and Z1, Z2, J1, J2, M, R1a, R1b, R2a, R2b, R2c, R2d and R14 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 4, 2014
    Applicant: E.I. Dupont De Nemours and Company
    Inventors: Thomas Francis Pahutski, JR., George Philip Lahm, Moumita Kar, Omar Khaled Ahmad
  • Publication number: 20140249183
    Abstract: Treatments are described for stress disorders and substance use disorders, for example, substance use disorders associated with use of alcohol, cocaine, amphetamines, and the like.
    Type: Application
    Filed: February 22, 2014
    Publication date: September 4, 2014
    Applicant: Baylor College of Medicine
    Inventors: Thomas F. Newton, Colin N. Haile
  • Patent number: 8822693
    Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols are each as defined in the description, and agrochemically active salts thereof, and use thereof for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: February 1, 2012
    Date of Patent: September 2, 2014
    Assignee: Bayer CropScience AG
    Inventors: Sebastian Hoffmann, Pierre Wasnaire, Tomoki Tsuchiya, Pierre Cristau, Thomas Seitz, Joachim Kluth, Jürgen Benting, Ulrike Wachendorff-Neumann
  • Publication number: 20140243371
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, G1, G2, G3, Y1, Y2, n, and p are as defined in the claims. The invention also relates to methods of using the compounds of formula I to control or prevent infestation of plants, propagation material thereof, harvested crops or non-living materials by phytopathogenic or spoilage microorganisms or organisms potentially harmful to man.
    Type: Application
    Filed: September 14, 2012
    Publication date: August 28, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jayant Umarye, Guillaume Berthon, Fredrik Emil Malcolm Cederbaum, Torsten Luksch, Clemens Lamberth, Sarah Sulzer-Mosse, Pranab Kanjilal, Ravindra Sonawane
  • Patent number: 8815910
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: August 26, 2014
    Assignee: Ardelyx, Inc.
    Inventors: Jason G. Lewis, Jeffrey W. Jacobs, Nicholas Reich, Michael R. Leadbetter, Noah Bell, Han-Ting Chang, Tao Chen, Marc Navre, Dominique Charmot, Christopher Carreras, Eric Labonte
  • Publication number: 20140235641
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: September 21, 2012
    Publication date: August 21, 2014
    Inventors: Jason Brubaker, Joshua Close, Tony Siu, Graham Frank Smith, Luis E. Torres, Hyun Chong Woo, Jonathan R. Young, Zhongyong Wei, Feng Shi
  • Publication number: 20140228358
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: September 21, 2012
    Publication date: August 14, 2014
    Inventors: Jason Brubaker, Joshua T. Close, Joon Jung, Michelle Martinez, Catherine White, Kevin Wilson, Jonathan R. Young, Hongjun Zhang
  • Publication number: 20140228348
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: September 21, 2012
    Publication date: August 14, 2014
    Inventors: Jason Brubaker, Matthew Lloyd Childers, Matthew Christopher, Joshua T. Close, Jason David Katz, Joon Jung, Scott Peterson, Phieng Siliphaivanh, Tony Siu, Graham Frank Smith, Luis E. Torres, Hyun Chong Woo, Jonathan R. Young, Hongjun Zhang
  • Patent number: 8802712
    Abstract: The invention relates to compounds of the formulae (I), (II) and (III), and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: August 12, 2014
    Assignee: Merck Patent GmbH
    Inventors: Thomas Fuchss, Werner Mederski, Frank Zenke
  • Publication number: 20140221373
    Abstract: The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof, wherein A1, A2, A3, L1, L2 and D are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the Compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Application
    Filed: July 17, 2012
    Publication date: August 7, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alexander Heim-Riether, Anil Kumar Padyana, Shuang Liang, Steven John Taylor, Qiang Zhang
  • Patent number: 8791137
    Abstract: The invention provides a compound of formula I: wherein R1-R6, 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 MAO-B enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: July 29, 2014
    Assignee: Dart Neuroscience (Cayman) Ltd.
    Inventors: Xianbo Zhou, Roderick E. M. Scott, Rusiko Bourtchouladze, Alan P Kaplan, Terence P Keenan, Andrew McRiner
  • Publication number: 20140205596
    Abstract: The invention relates to compounds and methods of treatment relating to nicotinic receptor antagonists. For example, the compounds and methods of treatment function block the activity of certain acetylcholine receptors and subtypes therein, and are useful treating diseases and conditions mediated by nicotinic receptor stimulation, e.g., small cell lung cancer.
    Type: Application
    Filed: June 22, 2012
    Publication date: July 24, 2014
    Applicant: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Youyi Peng, John Tomesch, Lawrence P. Wennogle, Qiang Zhang
  • Patent number: 8779147
    Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof, and combinations thereof with other anti-cancer agents, for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3.
    Type: Grant
    Filed: November 4, 2011
    Date of Patent: July 15, 2014
    Assignee: Astex Therapeutics, Ltd.
    Inventors: Valerio Berdini, Michael Alistair O'Brien, Maria Grazia Carr, Theresa Rachel Early, Adrian Liam Gill, Gary Trewartha, Alison Jo-Anne Woolford, Andrew James Woodhead, Paul Graham Wyatt
  • Publication number: 20140171420
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Application
    Filed: December 6, 2013
    Publication date: June 19, 2014
    Applicant: ChemoCentryx, Inc.
    Inventors: Xi Chen, Pingchen Fan, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang, Dean Dragoli
  • Publication number: 20140163032
    Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
    Type: Application
    Filed: February 18, 2014
    Publication date: June 12, 2014
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: BRADLEY TEEGARDEN, Dennis Chapman, Marc Decaire, Peter I. Dosa, Konrad Feichtinger, HONNAPPA JAYAKUMAR, THUY-ANH Tran, Sonja Strah-Pleynet, Jay Xu
  • Publication number: 20140162997
    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 R1, R2, ring A, and G are defined herein.
    Type: Application
    Filed: August 16, 2013
    Publication date: June 12, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Mark Wall, Nalin Subasinghe, Zhihua Sui, Christopher Flores
  • Patent number: 8748432
    Abstract: The present invention provides compounds of formula (I): wherein the substituents are as defined in claim 1, are useful as active ingredients, which have microbiocidal activity, in particular fungicidal activity.
    Type: Grant
    Filed: February 8, 2012
    Date of Patent: June 10, 2014
    Assignee: Syngenta Participations AG
    Inventors: Clemens Lamberth, Sarah Sulzer-Mosse, Fredrik Cederbaum, Guillaume Berthon
  • Publication number: 20140142139
    Abstract: 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 GPR40 G protein-coupled receptor modulators which may be used as medicaments.
    Type: Application
    Filed: November 15, 2013
    Publication date: May 22, 2014
    Inventors: Bruce A. Ellsworth, Jun Shi, William R. Ewing, Elizabeth A. Jurica, Andres S. Hernandez, Ximao Wu
  • Patent number: 8722678
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein E, X, G, W2 and Z are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Also disclosed are compounds of Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein E, X, G and Z1 are as defined in the disclosure. Also disclosed is the use of the compounds of Formula 1A as intermediates for preparing compounds of Formula 1.
    Type: Grant
    Filed: April 15, 2011
    Date of Patent: May 13, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Mary Ann Hanagan, Eric Allen Marshall
  • Patent number: 8722887
    Abstract: 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: Grant
    Filed: February 16, 2010
    Date of Patent: May 13, 2014
    Assignee: Abbvie Bahamas, Ltd.
    Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A. W. Van Der Neut, Cornelis G. Kruse
  • Publication number: 20140128406
    Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or x-N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.
    Type: Application
    Filed: June 27, 2012
    Publication date: May 8, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Fredrik Emil Malcolm Cederbaum
  • Patent number: 8710049
    Abstract: 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 agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.
    Type: Grant
    Filed: July 16, 2012
    Date of Patent: April 29, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu
  • Publication number: 20140107335
    Abstract: The present invention is directed to novel cyclic amines which inhibit the P2X7 receptor.
    Type: Application
    Filed: October 10, 2013
    Publication date: April 17, 2014
    Applicant: H. Lundbeck A/S
    Inventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohammed Eldemenky, Bin Chen, Yu Jiang
  • Publication number: 20140107157
    Abstract: The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: Such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation.
    Type: Application
    Filed: June 15, 2012
    Publication date: April 17, 2014
    Applicant: Research Triangle Institute
    Inventors: Alan Bradley Fulp, Rangan Maitra, Yanan Zhang, Herbert H. Seltzman
  • Publication number: 20140107125
    Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.
    Type: Application
    Filed: April 29, 2013
    Publication date: April 17, 2014
    Applicant: Dermira (Canada), Inc.
    Inventor: Dermira (Canada), Inc.