Exactly Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/303)
  • Fused Pyrazoles as FGFR Inhibitors
    Publication number: 20140171405
    Abstract: The present invention relates to fused pyrazole derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Incyte Corporation
    Inventors: Jincong Zhuo, Meizhong Xu, Ding-Quan Qian
  • Fused heterocyclic compounds as ion channel modulators
    Patent number: 8754103
    Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: July 26, 2010
    Date of Patent: June 17, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
  • Antiviral drugs for treatment of infection
    Patent number: 8754082
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.
    Type: Grant
    Filed: May 9, 2013
    Date of Patent: June 17, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Ryan A. Larson
  • Nitrogen-containing fused heterocyclic compounds and their use as beta amyloid production inhibitors
    Patent number: 8754100
    Abstract: A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a non-aromatic ring group, which may be substituted, Ring B represents a phenyl group or the like which may be substituted, X1 represents a single bond or the like, R1 and R2 each represent a C1-6 alkyl group or the like, m represents an integer of 0 to 3, and n represents an integer of 0 to 2, is effective as a therapeutic agent for a disease caused by A?.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: June 17, 2014
    Assignee: EISAI R&D Management Co., Ltd.
    Inventors: Noritaka Kitazawa, Daisuke Shinmyo, Koichi Ito, Nobuaki Sato, Daiju Hasegawa, Toshiyuki Uemura, Toru Watanabe
  • DIBENZOOXEPIN DERIVATIVE
    Publication number: 20140163008
    Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.
    Type: Application
    Filed: August 3, 2011
    Publication date: June 12, 2014
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
  • BROMODOMAIN INHIBITORS
    Publication number: 20140162971
    Abstract: The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, X1, X2, Y1, L1, G1, Rx, and Ry have any of the values defined thereof in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: March 14, 2013
    Publication date: June 12, 2014
    Inventors: Le WANG, John K PRATT, Keith F. McDANIEL, Yujia DAI, Steven D FIDANZE, Lisa HASVOLD, John H. Holms, Warren M. KATI, Dachun LIU, Robert A Mantei, William J. McCLELLAN, George S. SHEPPARD, Carol K. Wada
  • Pyrazolo piperidine derivatives as NADPH oxidase inhibitors
    Patent number: 8748456
    Abstract: The present invention is related to pyrazolo piperidine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: June 10, 2014
    Assignee: Genkyotex SA
    Inventors: Patrick Page, Benoît Laleu, Francesca Gaggini, Mike Orchard
  • SUBSTITUTED AZA-BICYCLIC IMIDAZOLE DERIVATIVES USEFUL AS TRPM8 RECEPTOR MODULATORS
    Publication number: 20140155395
    Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.
    Type: Application
    Filed: February 4, 2014
    Publication date: June 5, 2014
    Applicant: Janssen Pharmaceutica, NV
    Inventors: Mark R. Player, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel Parks, William Parsons, Scott Ballentine, Shawn Branum
  • 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
    Publication number: 20140155393
    Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
    Type: Application
    Filed: November 8, 2011
    Publication date: June 5, 2014
    Applicant: Janssen Pharmaceuticals, Inc.
    Inventors: José Maria Cid-Núñez, Andrés Avelino Trabanco-Suárez, Juan Antonio Vega Ramiro, Daniel Oehlrich, Gary John Tresadern, Gregor James Macdonald
  • Chemical Compounds - 759
    Publication number: 20140155394
    Abstract: The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.
    Type: Application
    Filed: June 21, 2013
    Publication date: June 5, 2014
    Applicant: Astrazeneca AB
    Inventors: Audrey DAVIES, Stephanos IOANNIDIS, Michelle LAMB, Mei SU, Tao WANG, Hai-Jun ZHANG
  • N-(imidazolidin-2-ylidene)-heterocyclopenta[b]pyridine derivatives as modulators of alpha 2 adrenergic receptors
    Patent number: 8741921
    Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)-heterocyclo penta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: July 18, 2013
    Date of Patent: June 3, 2014
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
  • PYRAZOLOPYRIDINE KINASE INHIBITORS
    Publication number: 20140148434
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. 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. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: September 18, 2013
    Publication date: May 29, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Dean Boyall, Guy Brenchley, Damien Fraysse, Juan-Miguel Jimenez, Luca Settimo
  • Method of Treatment or Prophylaxis of Inflammatory Pain
    Publication number: 20140142116
    Abstract: A method of treatment, reversal and/or symptomatic relief of inflammatory pain, including hyperalgesia, thermal or mechanical allodynia, in vertebrate animals, particularly in human subjects, comprising administering angiotensin II receptor 2 (AT2 receptor) antagonists is disclosed. The AT2 receptor antagonist may be provided alone or in combination with other compounds such as those that are useful in the control of inflammatory pain.
    Type: Application
    Filed: September 3, 2013
    Publication date: May 22, 2014
    Applicant: Spinifex Pharmaceuticals Pty Ltd
    Inventor: Maree Therese Smith
  • Pyridines for treating injured mammalian nerve tissue
    Patent number: 8729107
    Abstract: Embodiments of the present disclosure provide a novel pyridine, pharmaceutical compositions comprising such pyridine, and the use of such compositions in treating injured mammalian nerve tissue, including but not limited to an injured spinal cord. In at least one embodiment of the method, the method comprises the step of administering to the mammal in need thereof with a pharmaceutical composition, or pharmaceutically acceptable salt, comprising 4-aminopyridine-3-methanol.
    Type: Grant
    Filed: September 9, 2010
    Date of Patent: May 20, 2014
    Assignee: Purdue Research Foundation
    Inventors: Richard B. Borgens, Riyi Shi, Stephen R. Byrn, Daniel T. Smith
  • NOVEL BENZYLAMINE DERIVATIVES AND THEIR UTILITY AS CHOLESTEROL ESTER-TRANSFER PROTEIN INHIBITORS
    Publication number: 20140134235
    Abstract: The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.
    Type: Application
    Filed: October 14, 2013
    Publication date: May 15, 2014
    Applicant: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima BARUAH, Dibyendu DE, Ish Kumar KHANNA, Sivaram PILLARISETTI, Santanu MAITRA, Christopher W. ALEXANDER, Jennepalli SREENU, Indu Dagar, Shanavas Alikunju
  • HETEROAROMATIC COMPOUNDS AS PI3 KINASE MODULATORS AND METHODS OF USE
    Publication number: 20140134133
    Abstract: The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: November 10, 2013
    Publication date: May 15, 2014
    Applicants: Calitor Sciences, LLC
    Inventor: Ning Xi
  • Fused amino pyridines for the treatment of brain tumors
    Patent number: 8722703
    Abstract: The present invention relates to the use of compounds with fused amino pyridine core for the treatment of malignancies associated with brain and lung. The oral administration of compounds of the instant application results in effective brain penetration and provides for non-intrusive treatment of brain and lung tumors.
    Type: Grant
    Filed: January 15, 2010
    Date of Patent: May 13, 2014
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Changgeng Qian
  • GENETIC POLYMORPHISMS ASSOCIATED WITH VENOUS THROMBOSIS AND STATIN RESPONSE, METHODS OF DETECTION AND USES THEREOF
    Publication number: 20140128362
    Abstract: The present invention provides compositions and methods based on genetic polymorphisms that are associated with response to statin treatment (particularly for reducing the risk of venous thrombosis). For example, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by these nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and variant proteins, and methods of using the nucleic acid molecules and proteins as well as methods of using reagents for their detection.
    Type: Application
    Filed: March 20, 2013
    Publication date: May 8, 2014
    Applicant: CELERA CORPORATION
    Inventors: Lance BARE, James J. DEVLIN, Frits R. ROSENDAAL, Pieter H. REITSMA, Irene D. BEZEMER
  • Antiviral Drugs for Treatment of Arenavirus Infection
    Publication number: 20140128426
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 8, 2014
    Applicant: Siga Technologies Inc.
    Inventor: Siga Technologies Inc.
  • DERIVATIVES OF PURINE OR DEAZAPURINE USEFUL FOR THE TREATMENT OF (INTER ALIA) VIRAL INFECTIONS
    Publication number: 20140128389
    Abstract: The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.
    Type: Application
    Filed: October 15, 2010
    Publication date: May 8, 2014
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Randall L. Halcomb, Paul A. Roethle
  • Boron-containing small molecules
    Patent number: 8716478
    Abstract: Compounds, pharmaceutical formulations, and methods of treating anti-inflammatory conditions and/or helminth-associated diseases are disclosed.
    Type: Grant
    Filed: January 27, 2011
    Date of Patent: May 6, 2014
    Assignee: Anacor Pharmaceuticals, Inc.
    Inventors: Kurt Jarnagin, Tsutomu Akama
  • TRIAZOLOPYRIDINES
    Publication number: 20140120087
    Abstract: The present invention relates to triazolopyridine compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
    Type: Application
    Filed: April 16, 2012
    Publication date: May 1, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Volker Schulze, Dirk Kosemund, Antje Margret Wengner, Gerhard Siemeister, Detlef Stöckigt, Philip Lienau, Hartmut Schirok, Hans Briem
  • New Compounds I
    Publication number: 20140121219
    Abstract: The present invention relates to compounds of formula (I), and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases and immune disorders.
    Type: Application
    Filed: October 25, 2013
    Publication date: May 1, 2014
    Applicant: Proximagen Limited
    Inventors: Edward Savory, Michael Higginbottom, Kathryn Oliver, Viet-Anh Anne Horgan
  • LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS
    Publication number: 20140113892
    Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4-P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
    Type: Application
    Filed: May 10, 2013
    Publication date: April 24, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Donald J.P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y.S. Lam, Stephanie L. Koch
  • PYRAZOLE COMPOUNDS AS CRTH2 ANTAGONISTS
    Publication number: 20140113917
    Abstract: The present invention relates to pyrazole compounds of formula (I) and pharmaceutically acceptable salts thereof having CRTH2 antagonistic activity, wherein L, Y1, Y2, Y3, Y4, Y5, Z, R1, R2, R3 and n have one of the meanings as indicated in the specification and claims, to their use as medicaments, to pharmaceutical compositions containing said compounds and to pharmaceutical compositions containing said compounds in combination with one or more active substances.
    Type: Application
    Filed: March 15, 2012
    Publication date: April 24, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Boehringer Ingelheim International GmbH
  • CRYSTAL OF FUSED HETEROCYCLIC COMPOUND
    Publication number: 20140113932
    Abstract: The present invention relates to a crystal of 1-ethyl-7-methyl-3-{4-[(3-methyl-3H-imidazo[4,5-b]pyridin-2-yl)oxy]phenyl}-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one useful as a prophylactic or therapeutic agent for schizophrenia and the like, which shows an X-ray powder diffraction pattern having characteristic peaks at interplaner spacings (d) of 13.59 plus or minus 0.2 and 6.76 plus or minus 0.2 Angstroms in powder X-ray diffraction.
    Type: Application
    Filed: June 21, 2012
    Publication date: April 24, 2014
    Inventor: Katsuhiko Yamamoto
  • Condensed ring pyridine compounds as subtype-selective modulators of sphingosine-1-phosphate-2 (S1P) receptors
    Patent number: 8703797
    Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity, wherein these compounds selected from the group consisting of wherein A, B, C, D, X, Y, Z and R3 are defined in the specification. Said compounds are useful for treating a disease or condition of a mammal selected from the group consisting of ocular diseases; systemic vascular barrier related diseases; allergies and other inflammatory diseases; cardiac diseases or conditions; fibrosis; pain and wounds.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: April 22, 2014
    Assignee: Allergan, Inc.
    Inventors: Wenkui K. Fang, Evelyn G. Corpuz, Wha-Bin Im, Ken Chow, Liming Wang
  • Antiplatelet agent
    Patent number: 8703760
    Abstract: The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: wherein, X is N, or CR1d, Xb1-Xb5 are the same or different, and are nitrogen or carbon, R1a-R1d are the same or different, and are hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an optionally substituted alkylthio, an alkenyl, a cycloalkyl, a halogen, cyano, or hydroxyl or optionally substituted by 1 or 2 alkylamino, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R3 is an optionally substituted aryl or an optionally substituted heteroaryl, or pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: April 22, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Sato, Kazutoshi Yokoyama, Kazushi Sato
  • Fused heterocyclic compounds as ion channel modulators
    Patent number: 8703759
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: April 22, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Tetsuya Kobayashi, Dmitry Koltun, Gregory Notte, Eric Parkhill, Jeff Zablocki
  • 3H-imidazo [4, 5-B] pyridine-6-carboxamides as anti-inflammatory agents
    Patent number: 8703796
    Abstract: There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: April 22, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer
  • New Compounds II
    Publication number: 20140107150
    Abstract: The present invention relates to compounds of formula (I), and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment of medical conditions wherein inhibition of SSAO activity is beneficial, such as such as inflammatory diseases and immune disorders.
    Type: Application
    Filed: December 13, 2013
    Publication date: April 17, 2014
    Applicant: Proximagen Ltd
    Inventors: Edward Savory, Iain Simpson
  • USE OF SIGMA LIGANDS IN DIABETES TYPE-2 ASSOCIATED PAIN
    Publication number: 20140107111
    Abstract: The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and/or treat type-2 diabetes-associated pain and related symptoms.
    Type: Application
    Filed: May 18, 2012
    Publication date: April 17, 2014
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Jose Miguel Vela Hernandez, Maria Isabel Martin Fontelles
  • GDF-8 Inhibitors
    Publication number: 20140107073
    Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.
    Type: Application
    Filed: October 4, 2013
    Publication date: April 17, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
  • TYROSINE KINASE INHIBITORS
    Publication number: 20140107151
    Abstract: The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, JAK3, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts.
    Type: Application
    Filed: May 16, 2012
    Publication date: April 17, 2014
    Applicant: Principia Biophama Inc.
    Inventors: David Michael Goldstein, Kenneth Albert Brameld
  • Antiviral Drugs for Treatment of Arenvirus Infection
    Publication number: 20140100245
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family is disclosed.
    Type: Application
    Filed: November 27, 2013
    Publication date: April 10, 2014
    Applicant: SIGA TECHNOLOGIES, INC.
    Inventors: Dongcheng Dai, DENNIS E. HRUBY, TOVE C. BOLKEN, SEAN M. AMBERG, TRAVIS K. WARREN
  • Deazapurines and uses thereof
    Patent number: 8691814
    Abstract: The present invention provides compounds having formula (I): wherein R1, R2, R3 and n are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of inflammatory or autoimmune and proliferative disorders and as inhibitors of cell adhesion molecule expression and inflammatory cytokine signal transduction generally.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: April 8, 2014
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Jane Daun, Heather A. Davis, Bruce DeCosta, Fabian Gusovsky, Ieharu Hishinuma, Yimin Jiang, Toshihiko Kaneko, Kouichi Kikuchi, Seiichi Kobayashi, André Lescarbeau, Xiang-Yi Li, Kenzo Muramoto, Norihito Ohi, Marc Pesant, Boris M. Seletsky, Motohiro Soejima, Mark Spyvee, Lynda Tremblay, Ye Yao, Hiromitsu Yokohama, Yan (Janet) Zhao, Wanjun Zheng
  • 6-(4-hydroxy-phenyl)-3-alkyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
    Patent number: 8686150
    Abstract: The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: April 1, 2014
    Assignee: Sanofi
    Inventors: Stephanie Hachtel, Oliver Plettenburg, Christian Schoenau, Matthias Loehn, Stefania Pfeiffer-Marek, Maria Mendez-Perez, Aimo Kannt, Juergen Dedio, Markus Kohlmann, Alexander Schiffer, Guillaume Begis, Olivier Duclos, Frederic Jeannot
  • Substituted triazolopyridines and analogs thereof
    Patent number: 8685967
    Abstract: The present invention relates to substituted triazolopyridines and analogs thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds.
    Type: Grant
    Filed: April 5, 2010
    Date of Patent: April 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ginny D. Ho, Elizabeth M. Smith, Eugenia Y. Kiselgof, Kallol Basu, Zheng Tan, Brian McKittrick, Deen Tulshian
  • FUSED BICYCLIC IMIDAZOLES
    Publication number: 20140088110
    Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.
    Type: Application
    Filed: November 26, 2013
    Publication date: March 27, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Swen HÖLDER, Armin ZÜLCH, Thomas BÄR, Thomas MAIER, Astrid ZIMMERMANN, Thomas BECKERS, Volker GEKELER, Hemant JOSHI, Yogesh MUNOT, Umesh BHISE, Sunil CHAVAN, Sachin SHIVATARE, Sarvesh PATEL, Vikas GORE
  • COMPOSITIONS AND METHODS OF USE OF AN INAPPETANCE-CONTROLLING COMPOUND
    Publication number: 20140088139
    Abstract: The invention provides for a method of treating inappetance-induced weight loss in one or more companion animals or livestock. The method provides for administering a therapeutically effective amount of a capromorelin-containing composition to the companion animal or livestock. Optionally, one or more flavoring agents or flavor-masking agents can be added to the capromorelin-containing composition to enhance or mask the flavoring of the composition for the companion animal or livestock.
    Type: Application
    Filed: September 27, 2013
    Publication date: March 27, 2014
    Applicant: Aratana Therapeutics, Inc.
    Inventors: Bill ZOLLERS, Linda RHODES, Ernst HEINEN, Gopinath DEVARAJ
  • IMIDAZOLE DERIVATIVES
    Publication number: 20140088124
    Abstract: Described herein are compounds of formula (I), The compounds of formula I act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
    Type: Application
    Filed: June 1, 2012
    Publication date: March 27, 2014
    Inventors: Robert J. DeVita, QingMei Hong, Zhong Lai, Kevin D. Dykstra, Yang Yu, Jian Liu, Donald M. Sperbeck, Tianying Jian, Deodial Guiadeen, Ginger Xu-qiang Yang, Zhicai Wu, Shuwen He, Pauline C. Ting, Robert Aslanian, Jeffrey T. Kuethe, James Balkovec, Rongze Kuang, Gang Zhou, Heping Wu
  • CRYSTALLINE FORMS OF FUSED AMINO PYRIDINES AS HSP90 INHIBITORS
    Publication number: 20140088138
    Abstract: This invention relates to the discovery of novel forms of Compound 1, including solvates, hydrates, and other crystalline forms. These novel forms of Compound 1 may impart advantages in pharmaceutical formulations incorporating them, including improved stability and bioavailability.
    Type: Application
    Filed: September 23, 2013
    Publication date: March 27, 2014
    Applicant: Debiopharm International SA
    Inventors: Noel Hamill, James Moody, Sébastien Chabaud, Arnaud Hamel
  • Fused pyridine derivatives
    Patent number: 8680089
    Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.
    Type: Grant
    Filed: January 17, 2011
    Date of Patent: March 25, 2014
    Assignee: Xuanzhu Pharma Co., Ltd.
    Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
  • Substituted aza-bicyclic imidazole derivatives useful as TRPM8 receptor modulators
    Patent number: 8680098
    Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: March 25, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Mark R. Player, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel Parks, William Parsons, Scott Ballentine, Shawn Branum
  • ARYLOAZOL-2-YL CYANOETHYLAMINO COMPOUNDS, METHOD OF MAKING AND METHOD OF USING THEREOF
    Publication number: 20140080862
    Abstract: The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives of formula (I): wherein R3, R4, R5, R6, R7, P, Q, V, W, X, Y, Z and a are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.
    Type: Application
    Filed: September 19, 2012
    Publication date: March 20, 2014
    Applicants: AVENTIS AGRICULTURE, MERIAL LIMITED
    Inventors: Mark David Soll, Loic Patrick Le Hir de Fallois, Scot Kevin Huber, Hyoung Ik Lee, Douglas Edward Wilkinson, Robert Toms Jacobs
  • Indazole inhibitors of the Wnt signal pathway and therapeutic uses thereof
    Patent number: 8673936
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease 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: Grant
    Filed: March 13, 2013
    Date of Patent: March 18, 2014
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
  • Azaindazole compounds
    Patent number: 8673922
    Abstract: Disclosed are azaindazole compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein W is CR4 or N; and R1, R2, R3, and R4 are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: March 18, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Upender Velaparthi, David B. Frennesson, Mark G. Saulnier, Joel F. Austin, Audris Huang, James Aaron Balog, Dolatrai M. Vyas
  • ETHYNYL COMPOUNDS USEFUL FOR TREATMENT OF CNS DISORDER
    Publication number: 20140073638
    Abstract: The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.
    Type: Application
    Filed: October 16, 2013
    Publication date: March 13, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Substituted Imidazopyridinyl-Aminopyridine Compounds
    Publication number: 20140073635
    Abstract: The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: November 8, 2013
    Publication date: March 13, 2014
    Inventors: Mark A. Ashwell, Chris Brassard, Anton Filikov, Jason Hill, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Robert Nicewonger, Rocio Palma, Manish Tandon, David Vensel, Akihisa Matsuda, Shin Iimura, Kenichi Yoshida, Takanori Yamazaki, Takahiro Kitamura, Takeshi Isoyama
  • TREATMENT OF POLYCYSTIC DISEASE
    Publication number: 20140066462
    Abstract: The present invention provides methods of treating polycystic disorders. In particular, methods include the use of inhibitors targeting certain protein kinases, such as mTOR, to treat polycystic disease.
    Type: Application
    Filed: November 6, 2013
    Publication date: March 6, 2014
    Applicants: Intellikine LLC, The Regents of the University of California
    Inventors: David Pearce, Yi Liu, Michael Martin, Christian Rommel, Pingda Ren, Troy Edward Wilson