Additional Hetero Ring Attached Directly Or Indirectly To The 1,4-diazine Ring By Nonionic Bonding Patents (Class 514/255.05)
  • SMALL MOLECULE INHIBITORS FOR TREATING PARASITIC INFECTIONS
    Publication number: 20140045860
    Abstract: The invention relates to a compound of Formula I or a pharmaceutically acceptable ester, salt, prodrug or metabolite thereof;
    Type: Application
    Filed: August 13, 2013
    Publication date: February 13, 2014
    Applicants: NEW YORK UNIVERSITY, THE BROAD INSTITUTE, INC.
    Inventors: Leigh C. Carmody, Ana Rodriguez, Esther Bettiol, Michelle Palmer, Andrew Germain, Benito Munoz, Sivaraman Dandapani, Michael Foley
  • N-CYCLOPROPYL-N-PIPERIDINYL-AMIDES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USES THEREOF
    Publication number: 20140045823
    Abstract: The present invention relates to compounds of general formula I, wherein R1, LP, HetAr1, (Het)Ar2 and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Application
    Filed: July 31, 2013
    Publication date: February 13, 2014
    Applicants: Neurocrine Biosciences, Inc., Boehringer Ingelheim International GmbH
    Inventors: Bernd NOSSE, Matthias ECKHARDT, Frank HIMMELSBACH, Elke LANGKOPF, Neil J. ASHWEEK, Nicole HARRIOTT
  • SUBSTITUTED 1,3-BENZOTHIAZOL-2(3H)-ONES AND [1,3]THIAZOLO[5,4-B]PYRIDIN-2(1H)-ONES AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2
    Publication number: 20140045829
    Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: October 8, 2013
    Publication date: February 13, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: MARK E. LAYTON, Michael J. Kelly
  • COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE AND COMBINATION THERAPIES THEREOF
    Publication number: 20140044802
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase and combination therapies thereof. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Application
    Filed: April 5, 2013
    Publication date: February 13, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventor: Vertex Pharmaceuticals Incorporated
  • CHROMAN DERIVATIVES AS TRPM8 INHIBITORS
    Publication number: 20140045855
    Abstract: Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: August 2, 2013
    Publication date: February 13, 2014
    Applicant: AMGEN INC.
    Inventors: Kaustav BISWAS, Jian J. CHEN, Vijay Keshav GORE, Scott HARRIED, Daniel B. HORNE, Matthew R. KALLER, Vu Van MA, Kelvin SHAM, Wenge ZHONG
  • Inhibitors of PI3K-Delta and Methods of Their Use and Manufacture
    Publication number: 20140045825
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Application
    Filed: September 14, 2011
    Publication date: February 13, 2014
    Applicant: Exelixis, Inc.
    Inventor: James William Leahy
  • Glucokinase Activators
    Publication number: 20140045859
    Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as 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 said compounds.
    Type: Application
    Filed: October 2, 2013
    Publication date: February 13, 2014
    Applicant: Takeda California, Inc.
    Inventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Mingnam Tang, Haixia Wang, Jeffrey A. Stafford
  • PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS
    Publication number: 20140045849
    Abstract: This invention relates to pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections such as HCV or HBV.
    Type: Application
    Filed: April 10, 2012
    Publication date: February 13, 2014
    Inventors: David McGowan, Pierr Jeane-Marie Bernar Raboisson, Werner Embrechts, Tim Hugo Maria Jonckers, Stefaan Julien Last, Serge Maria Aloysius Pieters, Jaromir Vlach
  • COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES
    Publication number: 20140045861
    Abstract: The invention relates to certain compounds according to Formula (I): or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders and immune disorders.
    Type: Application
    Filed: October 15, 2013
    Publication date: February 13, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Jun Jiang, Junyi Zhang, Shoujun Chen, Lijun Sun
  • INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/BETA-CATENIN SIGNALING PATHWAY INHIBITORS
    Publication number: 20140045815
    Abstract: Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Application
    Filed: September 5, 2013
    Publication date: February 13, 2014
    Applicant: Samumed, LLC
    Inventors: John Hood, Sunil Kumar KC
  • Selective substituted pyrazine ligands for neuronal nicotinic receptors
    Patent number: 8648084
    Abstract: The present application describes selective ligands of formula (I) for neuronal nicotinic receptors (NNRs), more specifically for the ?4?2 NNR subtype, compositions thereof, and methods of using the same, wherein X, R1, X, R2, R3, L1, m, n, p, and q are defined in the specification.
    Type: Grant
    Filed: March 6, 2012
    Date of Patent: February 11, 2014
    Assignee: AbbVie Inc.
    Inventors: William H. Bunnelle, Lei Shi, Marc J. C. Scanio
  • Imidazole, Pyrazole, and Triazole Derivatives Useful As Antibacterial Agents
    Publication number: 20140038975
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.
    Type: Application
    Filed: March 27, 2012
    Publication date: February 6, 2014
    Inventors: Matthew Frank Brown, Jinshan Michael Chen, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
  • Heteroaryl-Ketone Fused Azadecalin Glucocorticoid Receptor Modulators
    Publication number: 20140038926
    Abstract: The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: May 24, 2013
    Publication date: February 6, 2014
    Applicant: Corcept Therapeutics, Inc.
    Inventors: Hazel Hunt, Tony Johnson, Nicholas Ray, Iain Walters
  • SUBSTITUTED 1,2,3,4-TETRAHYDROCYCLOPENTA[b]INDOL-3-YL)ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS
    Publication number: 20140038987
    Abstract: The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
    Type: Application
    Filed: October 8, 2013
    Publication date: February 6, 2014
    Inventors: Robert M. Jones, Daniel J. Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Brett Ullman, Jeanne V. Moody, Xiuwen Zhu, Scott Stirn
  • RING-FUSED HETEROCYCLIC DERIVATIVE
    Publication number: 20140038941
    Abstract: A ring-fused heterocyclic derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof having a T-type calcium channel regulatory effect and useful as a pruritus therapeutic and/or preventive agent, and the like are provided. In the general formula (I), R1 represents optionally substituted lower alkyl, and the like; R2 represents an optionally substituted cycloalkyl, and the like; Q represents a hydrogen atom, and the like; R3 represents —C(?O)NR8R9 (wherein R8 and R9 may be the same or different, and each represents a hydrogen atom, and the like), and the like; L1 represents —CR11AR11B— (wherein R11A and R11B may be the same or different, and each represents a hydrogen atom, and the like), and the like; and W1 and W2 may be the same or different, and each represents C—R12 (wherein R12 represents a hydrogen atom, and the like), and the like.
    Type: Application
    Filed: February 1, 2012
    Publication date: February 6, 2014
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Takashi Sawada, Tomohiro Danjo, Keiichi Motosawa, Takayuki Furuta, Maki Ichioka, Masamori Sugawara, Noriaki Uesaka
  • HETEROARYL AMIDE ANALOGUES AS P2X7 ANTAGONISTS
    Publication number: 20140038955
    Abstract: Heteroaryl amide analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: October 2, 2013
    Publication date: February 6, 2014
    Applicant: H. Lundbeck A/S
    Inventors: David C. IHLE, Qin GUO, Kevin HODGETTS, Jun YUAN
  • Indanyloxydihydrobenzofuranylacetic acids
    Patent number: 8642585
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: February 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Sara Frattini, Dieter Hamprecht, Frank Himmelsbach, Elke Langkopf, Iain Lingard, Stefan Peters, Holger Wagner
  • BICYCLIC COMPOUNDS AS PIM INHIBITORS
    Publication number: 20140031360
    Abstract: The invention relates to bicyclic compounds of formula (1?), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
    Type: Application
    Filed: December 7, 2011
    Publication date: January 30, 2014
    Applicant: AMGEN INC.
    Inventors: Hui-Ling Wang, Kaustav Biswas, Victor J. Cee, Frank Chavez, JR., Bradley J. Herberich, Claire L.M. Jackson, Brian A. Lanman, Matthew Lee, Thomas Nixey, Liping H. Pettus, Anthony B. Reed, Robert M. Rzasa, Shannon Rumfelt, Andrew Tasker, Bin Wu, Ryan Wurz
  • QUINAZOLINES AS POTASSIUM ION CHANNEL INHIBITORS
    Publication number: 20140031345
    Abstract: A compound of formula I wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Application
    Filed: September 27, 2013
    Publication date: January 30, 2014
    Inventors: James A. Johnson, John Lloyd, Heather Finlay, Ji Jiang, James Neels, Naveen Kumar Dhondi, Prashantha Gunaga, Abhisek Banerjee
  • N-CYCLOPROPYL-N-PIPERIDINYL-AMIDE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USES THEREOF
    Publication number: 20140031369
    Abstract: The present invention relates to compounds of general formula I, wherein R1, LP, (Het)Ar1, (Het)Ar2 and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Application
    Filed: July 22, 2013
    Publication date: January 30, 2014
    Applicants: NEUROCRINE BIOSCIENCES, INC., BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Neil J. ASHWEEK, Nicole HARRIOTT
  • POLY AROMATIC SODIUM CHANNEL BLOCKERS
    Publication number: 20140031371
    Abstract: Polyaromatic sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.
    Type: Application
    Filed: October 1, 2013
    Publication date: January 30, 2014
    Applicant: PARION SCIENCES, Inc.
    Inventor: Michael Ross JOHNSON
  • HETEROCYCLIC COMPOUNDS AND THEIR USES
    Publication number: 20140031355
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity.
    Type: Application
    Filed: November 4, 2011
    Publication date: January 30, 2014
    Applicant: Amgen Inc.
    Inventor: Amy Kaizerman
  • SELECTIVE HDAC INHIBITORS
    Publication number: 20140031368
    Abstract: This disclosure is related to compounds having the structure wherein Ar1, Ar2, R1-R6, Z, m, n, o, and p are defined herein. This disclosure also relates to pharmaceutical compositions comprising the above compounds and methods for their use.
    Type: Application
    Filed: July 8, 2013
    Publication date: January 30, 2014
    Applicants: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK, SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Ronald Breslow, Paul A. Marks, K. G. Abhilash, Jianing Wang
  • Tetrahydroquinoline Derivatives Useful As Bromodomain Inhibitors
    Publication number: 20140031336
    Abstract: Tetrahydroquinoline compounds, pharmaceutical compositions containing such compounds and their use in therapy.
    Type: Application
    Filed: April 19, 2012
    Publication date: January 30, 2014
    Applicant: Glaxosmithkline LLC
    Inventors: Dominique Amans, Emmanuel Hubert Demont, Darren Jason Mitchell, Jonathan Thomas Seal
  • AMIDE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND USE THEREOF AS INSECTICIDE
    Publication number: 20140031370
    Abstract: A compound represented by Formula (1): The compound can be used as insecticides.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 30, 2014
    Applicant: MITSUI CHEMICALS, INC.
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
  • INHIBITORS OF FLAVIVIRIDAE VIRUSES
    Publication number: 20140030223
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: September 25, 2013
    Publication date: January 30, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael Martzman, Philip Anthony Morganelli, William J. Watkins, Hong Ye
  • Aminopyridine and carboxypyridine compounds as phosphodiesterase 10 inhibitors
    Patent number: 8637500
    Abstract: Pyridine and pyrimidine compounds: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, R6, R7, X1, X2, X3, X4, X5, X6, X7, X8, and Y are as defined in the specification; or a pharmaceutically acceptable salt thereof, wherein ring A, m, n, y, R2, R3, R4, R5, R6, R7, R8, R9, X1, X2, and ring A are as defined in the specification; and or a pharmaceutically acceptable salt thereof, wherein m, n, y, R2, R3, R4, R5, R6, R7, R9, X1, X2, and ring A are as defined in the specification; compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: December 16, 2009
    Date of Patent: January 28, 2014
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Ning Chen, James R. Falsey, Michael J. Frohn, Paul E. Harrington, Essa Hu Harrington, Matthew R. Kaller, Roxanne K. Kunz, Thomas T. Nguyen, Alexander J. Pickrell, Andreas Reichelt, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Aaron C. Siegmund, Guomin Yao
  • Heterocycle phenyl amide T-type calcium channel antagonists
    Patent number: 8637513
    Abstract: The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
    Type: Grant
    Filed: October 23, 2008
    Date of Patent: January 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Paul J. Coleman, Thomas S. Reger, Kelly-Ann S. Schlegel, Youheng Shu, Zhi-Qiang Yang
  • Oxazole compound and pharmaceutical composition
    Patent number: 8637559
    Abstract: The present invention provides a oxazole compound represented by Formula (1), or a salt thereof: wherein R1 is an aryl group which may have one or more substituents; R2 is an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by —Y1-A1- or —Y2—C(?O)— wherein Y1 is a group such as —C(?O)—, A1 is a group such as a lower alkylene group, and Y2 is a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.
    Type: Grant
    Filed: November 14, 2006
    Date of Patent: January 28, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Minoru Okada, Masaya Kato, Norifumi Sato, Tetsuyuki Uno, Hideki Kitagaki, Junpei Haruta, Hidetaka Hiyama, Tomonori Shibata
  • Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of TRPV1
    Patent number: 8637527
    Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: January 28, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C Rech, Wei Xiao
  • Pyrazinone derivatives as insulin secretion stimulators, methods for obtaining them and use thereof for the treatment of diabetes
    Patent number: 8637522
    Abstract: The present invention relates to pyrazinone derivatives of formula (I), wherein n, R1, R2, R3 and R4 are as defined in claim 1, as insulin secretion stimulators. The invention also relates to the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.
    Type: Grant
    Filed: January 15, 2009
    Date of Patent: January 28, 2014
    Assignee: Merck Patent GmbH
    Inventors: Gérard Botton, Micheline Kergoat, Christine Charon, Samer Elbawab
  • INDAZOLES
    Publication number: 20140024634
    Abstract: A method of treating a disease or condition for which a JAK inhibitor is indicated in a subject in need of such treatment, comprising administering to the subject a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, and particularly, a method for the treatment of various inflammatory diseases, particularly psoriasis, asthma and COPD.
    Type: Application
    Filed: September 30, 2013
    Publication date: January 23, 2014
    Inventors: Jotham Wadsworth Coe, Christoph Martin Dehnhardt, Peter Jones, Steven Wade Kortum, Yogesh Anil Sabnis, Florian Michel Wakenhut, Gavin Alistair Whitlock
  • Substituted Benzamides and Their Uses
    Publication number: 20140024649
    Abstract: Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use.
    Type: Application
    Filed: October 10, 2011
    Publication date: January 23, 2014
    Applicants: Auckland UniServices Limited, The Board of Trustees of the Leland Stanford Junior University
    Inventors: Amato Giaccia, Edwin Lai, Olga Razorenova, Denise Chan, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Ray Tabibiazar, Po-wai Yuen
  • ORGANIC COMPOUNDS
    Publication number: 20140024583
    Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: July 15, 2013
    Publication date: January 23, 2014
    Inventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Duanjie Hou, Rajender Kamboj, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Zaihui Zhang
  • Methods for Treating HCV
    Publication number: 20140024613
    Abstract: In one aspect, the present invention features HCV therapies comprising administering to a patient in need thereof an HCV protease inhibitor and ritonavir, wherein ritonavir is used as a pharmacokinetic booster to improve the pharmacokinetics of the HCV protease inhibitor. The HCV therapies do not require the testing of total cholesterol and triglyceride levels prior to and after the therapies.
    Type: Application
    Filed: June 26, 2013
    Publication date: January 23, 2014
    Inventors: Daniel E. COHEN, Thomas J. PODSADECKI, Barry M. BERNSTEIN, Martin S. KING
  • Spirolactam derivatives and uses of same
    Patent number: 8633190
    Abstract: The present invention provides spirolactam derivatives of formula (I): wherein R1-R7 are as defined herein; or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and uses of the same.
    Type: Grant
    Filed: October 26, 2010
    Date of Patent: January 21, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Hao Zhou, Guiying Li, Dario Doller, Gil Ma
  • Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds
    Patent number: 8633193
    Abstract: Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.
    Type: Grant
    Filed: January 26, 2011
    Date of Patent: January 21, 2014
    Assignee: Novartis AG
    Inventors: Jun Yuan, Peter Hrnciar, Qin Guo, George D. Maynard
  • Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
    Publication number: 20140018371
    Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
    Type: Application
    Filed: March 30, 2012
    Publication date: January 16, 2014
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Robert M. Jones, Sangdon Han, Juerg Lehmann, Lars Thoresen
  • Therapeutic agent for spinal canal stenosis
    Patent number: 8629145
    Abstract: The main object of the present invention is to provide a novel agent for the treatment of spinal canal stenosis. The present invention relates to an agent for the treatment of spinal canal stenosis containing the heterocyclic derivative represented by the following general formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient; In the formula (1), R1 and R2 are the same or different and each represents an optionally substituted aryl; R3 and R4 are the same or different and each represents hydrogen atom or alkyl; R5 represents hydrogen atom, alkyl or halogen atom; Y represents N or N?O; A represents NR6, and R6 represents hydrogen atom, alkyl, etc.; D represents alkylene or alkenylene which is optionally substituted with hydroxy; E represents phenylene or a single bond; G represents O, S, etc.; and Q represents carboxy, alkoxycarbonyl, etc.
    Type: Grant
    Filed: June 22, 2009
    Date of Patent: January 14, 2014
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventor: Keiichi Kuwano
  • Pyrazine derivatives for optical imaging and therapy
    Patent number: 8628751
    Abstract: The invention provides compounds, including compositions, preparations and formulations, and methods of using and making such compounds. Compounds of the present invention include pyrazine derivatives having a pyrazine core and a plurality of substituents. In some embodiments, pyrazine derivatives of the invention are pyrazine core compounds having one or more electron donating groups and one or more electron withdrawing groups optionally functionalized to provide useful optical, biological, pharmacokinetic and/or physical properties.
    Type: Grant
    Filed: April 15, 2010
    Date of Patent: January 14, 2014
    Assignee: Medi Beacon Development, LLC
    Inventors: William L. Neumann, John N. Freskos
  • PIPERIDINONE DERIVATIVES AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER
    Publication number: 20140011796
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: September 12, 2013
    Publication date: January 9, 2014
    Applicant: AMGEN INC.
    Inventors: Michael David BARTBERGER, Ana Gonzalez Buenrostro, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason Duquette, John Eksterwicz, Benjamin Fisher, Brian Matthew Fox, Jiasheng Fu, Zice Fu, Felix Gonzalez Lopez De Turiso, Michael William Gribble, Dann James Gustin, Julie Anne Heath, Xin Huang, Xianyun Jiao, Michael Johnson, Frank Kayser, David John Kopecky, Sujen Lai, Yihong Li, Zhihong Li, Jiwen Liu, Jonathan Dante Low, Brian Stuart Lucas, Zhihua Ma, Lawrence R. McGee, Joel McIntosh, Dustin McMinn, Julio Cesar Medina, Jeffrey Thomas Mihalic, Steven Howard Olson, Yosup Rew, Philip Marley Roveto, Daqing Sun, Xiaodong Wang, Yingcai Wang, Xuelei Yan, Ming Yu, Jiang Zhu
  • HETEROARYL QUINAZOLINE DERIVATIVES
    Publication number: 20140011801
    Abstract: Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).
    Type: Application
    Filed: September 9, 2013
    Publication date: January 9, 2014
    Applicant: MSD K.K.
    Inventors: Tomoharu Iino, Aklo Ohno, Norikazu Otake, Takuya Suga, Masanori Asai
  • Nitrogen containing heteroaryl compounds
    Patent number: 8623866
    Abstract: The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: January 7, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Felix Gruber, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento
  • INHIBITORS OF INFLUENZA VIRUSES REPLICATION
    Publication number: 20140005197
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Application
    Filed: June 14, 2013
    Publication date: January 2, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, Michael P. Clark, Ioana Davies, Huai Gao, Joseph M. Kennedy, Mark W. Ledeboer, Francois Maltais, Emanuele Perola
  • 5-AZAINDAZOLE COMPOUNDS AND METHODS OF USE
    Publication number: 20140005168
    Abstract: 5-Azaindazole compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: June 26, 2013
    Publication date: January 2, 2014
    Inventors: Steven Do, Huiyong Hu, Aleksandr Kolesnikov, Vickie H. Tsui, Xiaojing Wang
  • 1H-IMIDAZO[4,5-C]QUINOLINONE DERIVATIVES
    Publication number: 20140005163
    Abstract: The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c]quinolinone derivatives for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H-imidazo[4,5-c]quinolinone derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c]quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1H-imidazo[4,5-c]quinolinone derivatives; and a process for the preparation of the novel 1H-imidazo[4,5-c]quinolinone derivatives.
    Type: Application
    Filed: May 24, 2013
    Publication date: January 2, 2014
    Applicant: NOVARTIS AG
    Inventors: Pascal Furet, Frank Stephan Kalthoff, Robert Mah, Christian Ragot, Frederic Stauffer
  • Bridged diazepan orexin receptor antagonists
    Patent number: 8618102
    Abstract: The present invention is directed to bridged diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: July 13, 2007
    Date of Patent: December 31, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Christopher D. Cox, Georgia B. McGaughey, Anthony J. Roecker, John D. Schreier
  • Arylethynyl derivatives
    Patent number: 8618296
    Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Grant
    Filed: June 10, 2013
    Date of Patent: December 31, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • PYRROLOPYRIDINEAMINO DERIVATIVES AS MPS1 INHIBITORS
    Publication number: 20130345181
    Abstract: The present invention relates to the use of certain pyrrolopyridineamino derivatives (hereinafter referred to as “PPA derivatives”), particularly 1H-pyrrolo[3,2-c]pyridine-6-amino derivatives, to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps kinase itself. In particular, the present invention relates to PPA derivatives for use as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of the PPA derivatives, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 14, 2012
    Publication date: December 26, 2013
    Applicant: CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Vassilios Bavetsias, Butrus Atrash, Sébastien Gaston André Naud, Peter William Sheldrake, Julian Blagg
  • COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM
    Publication number: 20130345240
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: August 16, 2013
    Publication date: December 26, 2013
    Applicant: CALCIMEDICA, INC.
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey