Plural Ring Nitrogens In The Additional Hetero Ring (e.g., Imidazole, Pyrazine, Etc.) Patents (Class 514/235.8)
Three or more ring hetero atoms in the additional hetero ring (Class 514/236.2)
The ring nitrogens are bonded directly to each other (e.g., pyridazine, etc.) (Class 514/236.5)
  • APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES
    Publication number: 20140088106
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: October 14, 2013
    Publication date: March 27, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Yujia Dai, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Todd M. Hansen
  • Disulfide Chemotherapeutic Agents and Methods of Use Thereof
    Publication number: 20140079812
    Abstract: Compositions and methods for the treatment of cancer are provided.
    Type: Application
    Filed: November 19, 2013
    Publication date: March 20, 2014
    Applicant: Lankenau Institute for Medical Research
    Inventors: Iraimoudi S. Ayene, George C. Prendergast
  • Aminopyrimidine Kinase Inhibitors
    Publication number: 20140080799
    Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.
    Type: Application
    Filed: September 20, 2013
    Publication date: March 20, 2014
    Applicant: Jasco Pharmaceuticals, LLC
    Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger, Yvonne L. Flanders, Stephane A. Dumas
  • PYRIMIDINONE COMPOUNDS AND METHODS FOR PREVENTING AND TREATING INFLUENZA
    Publication number: 20140079666
    Abstract: In one aspect, the invention relates to novel, broad-spectrum anti-viral, pyrimidinone compounds, methods of use, compositions and kits useful in treating and/or preventing influenza. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: May 5, 2012
    Publication date: March 20, 2014
    Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL
    Inventors: Thomas R. Webb, Vincent A. Boyd
  • Inhibitors of C-FMS kinase
    Patent number: 8674100
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are as set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. The compounds of formula I are useful for treating a variety of disorders including autoimmune diseases such as rheumatoid arthritis, multiple sclerosis and psoriasis.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: March 18, 2014
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJariais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
  • Aminopyrazine derivative and medicine
    Patent number: 8673891
    Abstract: The present invention relates to a compound represented by general formula [1] satisfying the following (I) or (II), or a pharmaceutical acceptable salt of the compound. (I) X is CH or N; R1 is a halogen atom, and R2 is H, a halogen atom, CN, [2], [3], [8], [9], an —O-alkyl, an —O-(saturated ring), etc. [2]: —C(RC)(RD)(RE) (RC to RE each are H, an alkyl, etc.) [3]: —N(RF)(RG) (RF and RG each are H, OH, amino, a (hetero)aryl, etc.) [8]: —C(?O)RL (RL is an alkyl, OH, an alkoxy, amino, etc.) [9]: a (substituted)phenyl; (II) X is >C—C(—O)RB (RB is a (substituted)amino, an alkoxy, OH, etc.); R1 is a halogen atom; R2 is H; R3 is H or OH; and R3 and R4 each are H or an alkyl.
    Type: Grant
    Filed: February 5, 2010
    Date of Patent: March 18, 2014
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Hidetaka Fujihara, Tetsuo Asaki, Katsutoshi Hori, Haruna Naito
  • INHIBITION OF ANTIMICROBIAL TARGETS WITH REDUCED POTENTIAL FOR RESISTANCE
    Publication number: 20140073639
    Abstract: The application describes targets and methods that can inhibit bacterial growth in Gram-positive and Gram-negative bacteria. A bacterial enzyme, 2-epimerase, is common to both Gram-positive and Gram-negative bacteria and contains an allosteric site that can be targeted to disrupt the enzyme. The allosteric site is present on the bacterial 2-epimerase, but the analogous mammalian enzyme does not contain the allosteric site, providing a route for attacking bacterial infections without affecting the mammalian enzyme.
    Type: Application
    Filed: August 8, 2013
    Publication date: March 13, 2014
    Applicants: The Rockefeller University, Avacyn Pharmaceuticals, Inc.
    Inventors: Vincent A. FISCHETTI, Allan R. GOLDBERG, Raymond SCHUCH
  • CHEMOKINE RECEPTOR ANTAGONISTS AND USE THEREOF
    Publication number: 20140072576
    Abstract: The present invention relates to a compound represented by formula (I): wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.
    Type: Application
    Filed: November 8, 2013
    Publication date: March 13, 2014
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Masaya KOKUBO, Motoyuki TANAKA, Hiroshi OCHIAI, Yoshikazu TAKAOKA, Shiro SHIBAYAMA
  • 5-ALKYNYL-PYRIMIDINES
    Publication number: 20140073621
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: November 22, 2013
    Publication date: March 13, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Siegfried SCHNEIDER, Dirk KESSLER, Lars van der VEEN, Tobias WUNBERG
  • TREATMENT OF JAK2-MEDIATED CONDITIONS
    Publication number: 20140073643
    Abstract: Described herein is a method for treating a subject experiencing anemia, comprising administering to the subject an amount of N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-benzamide [CYT387 ] or a related compound effective to maintain or elevate the hemoglobin level. The anemic subjects including those afflicted with a myeloproliferative disorder, such as primary myelofibrosis.
    Type: Application
    Filed: November 29, 2011
    Publication date: March 13, 2014
    Applicant: YM BIOSCIENCES AUSTRALIA PTY LTD
    Inventors: Gregg D. Smith, Rose Fida, Mark M. Kowalski
  • VEGFR3 INHIBITORS
    Publication number: 20140073620
    Abstract: This invention relates to a compound of the formula (I): The invention also relates to processes for the preparation of the compound of the formula (I), pharmaceutical agents or compositions containing the compound or a method of using the compound for the treatment of proliferative diseases, such as cancer, as well as the treatment of diseases ameliorated by the control and/or inhibition of lymphangiogenesis.
    Type: Application
    Filed: August 16, 2013
    Publication date: March 13, 2014
    Applicant: CANCER THERAPEUTICS CRC PTY LIMITED
    Inventors: Richard Charles FOITZIK, Benjamin Joseph Morrow, Catherine Fae Hemley, Gillian Elizabeth Lunniss, Michelle Ang Camerino, Danny Ganame, Paul Anthony Stupple, Romina Lessene, Wilhelmus Johannes Antonius Kersten, Andrew John Harvey, Ian Peter Holmes
  • Prolylcarboxypeptidase inhibitors
    Patent number: 8669252
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: March 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
  • PHENOXY-SUBSTITUTED PYRIMIDINES AS OPIOID RECEPTOR MODULATORS
    Publication number: 20140066422
    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, Y, R2, R3, and Ra are defined herein.
    Type: Application
    Filed: February 13, 2013
    Publication date: March 6, 2014
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Janssen Pharmaceutica, NV
  • ANDROGEN RECEPTOR ANTAGONISTS AND USES THEREOF
    Publication number: 20140066425
    Abstract: Disclosed are substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds. The compounds and compositions can be used for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss and hypertrichosis.
    Type: Application
    Filed: March 8, 2012
    Publication date: March 6, 2014
    Applicants: SUZHOU KINTOR PHARMACEUTICALS, INC.
    Inventor: Youzhi Tong
  • Aminopyrimidines useful as inhibitors of protein kinases
    Patent number: 8664219
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
    Type: Grant
    Filed: June 2, 2010
    Date of Patent: March 4, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Juan-Miguel Jimenez, Andrew Miller, Jeremy Green, Huai Gao, Gregory Henkel, Michael Liu, Timothy Neuberger
  • Thiazole derivatives and their use as P2Y12 receptor antagonists
    Patent number: 8664203
    Abstract: The present invention relates to thiazole derivatives of formula I and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
    Type: Grant
    Filed: April 21, 2010
    Date of Patent: March 4, 2014
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Eva Caroff, Kurt Hilpert, Francis Hubler, David Lehmann, Emmanuel Meyer, Dorte Renneberg
  • PYRIMIDINE-4,6-DIAMINE DERIVATIVES AS PI3K INHIBITORS
    Publication number: 20140057912
    Abstract: The present invention provides pyrimidine-4,6-diamine derivatives of Formula (I): wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Application
    Filed: March 23, 2012
    Publication date: February 27, 2014
    Applicant: INCYTE CORPORATION
    Inventors: Andrew P. Combs, Yun-Long Li, Eddy W. Yue, Song Mei
  • BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE DISEASES
    Publication number: 20140057889
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 27, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
  • HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS
    Publication number: 20140057910
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: February 22, 2012
    Publication date: February 27, 2014
    Applicant: Schering Corporation
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voight, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
  • AURORA KINASE INHIBITORS AND METHODS OF MAKING AND USING THEREOF
    Publication number: 20140057913
    Abstract: Described herein are inhibitors of Aurora kinase and their use in the treatment of cancer. Methods of screening for selective inhibitors of Aurora kinases are also disclosed.
    Type: Application
    Filed: March 30, 2012
    Publication date: February 27, 2014
    Applicant: H. Lee Moffitt Cancer Center and Research Institute, Inc.
    Inventors: Said M. Sebti, Ernst Schönbrunn, Nicholas J. Lawrence, Harshani R. Lawrence, Matthew P. Martin
  • BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE DISEASES
    Publication number: 20140057890
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 27, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
  • NOVEL 4,6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES HAVING BOTH AROMATIC AND HALOGENIC SUBSTITUENTS
    Publication number: 20140057911
    Abstract: Certain 4,6-disubstituted aminopyrimidine derivatives having both aromatic and halogenic substituents.
    Type: Application
    Filed: August 23, 2013
    Publication date: February 27, 2014
    Inventors: Franco Lori, James Chafouleas, Davide De Forni, Antonio Solinas, Zoltán Varga, Zoltán Greff, László Örfi, György Kéri
  • Arylsulfonamide CCR3 antagonists
    Patent number: 8658642
    Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: February 25, 2014
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Jared Andrew Forrester
  • THIOPYRIMIDINE-BASED COMPOUNDS AND USES THEREOF
    Publication number: 20140051703
    Abstract: The present invention relates to thiopyrimidine-based compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2 or JAK3 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases and vascular diseases.
    Type: Application
    Filed: April 11, 2013
    Publication date: February 20, 2014
    Applicant: Cytopia Research Pty Ltd.
    Inventors: David Gerard BOURKE, Xianyong Bu, Christopher John Burns, Anthony Nicholas Cuzzupe, John Thomas Feutrill, Tracy Leah Nero, Beata Maria Blannin, Jun Zeng, Shaun Patrick Gaynor
  • NEW COMPOUNDS
    Publication number: 20140051674
    Abstract: The present invention encompasses compounds of general formula (1) wherein B, R1 to R5, Rx, m and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use in such treatment.
    Type: Application
    Filed: October 23, 2013
    Publication date: February 20, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Ioannis SAPOUNTZIS, Daniel KUHN, Heinz STADTMUELLER
  • 4-(4-CYANO-2-THIOARYL)DIHYDROPYRIMIDINONES AND THEIR USE
    Publication number: 20140045802
    Abstract: The present invention relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.
    Type: Application
    Filed: September 12, 2012
    Publication date: February 13, 2014
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig, Jens Schamberger
  • 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
  • THIOPYRIMIDINE-BASED COMPOUNDS AND USES THEREOF
    Publication number: 20140045848
    Abstract: The present invention relates to thiopyrimidine-based compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2 or JAK3 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases and vascular diseases.
    Type: Application
    Filed: April 11, 2013
    Publication date: February 13, 2014
    Applicant: Cytopia Research Pty Ltd.
    Inventors: David Gerard Bourke, Xianyong Bu, Christopher John Burns, Anthony Nicholas Cuzzupe, John Thomas Feutrill, Tracy Leah Nero, Beata Maria Blannin, Jun Zeng, Shaun Patrick Gaynor
  • Bicyclic ring system substituted sulfonamide functionalised phenols as medicaments
    Patent number: 8648070
    Abstract: This invention relates to bicyclic ring system substituted sulfonamide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: February 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Riccardo Giovannini, Dieter Hamprecht, Barbara Kistler, Iain Lingard
  • MOLECULAR SUBTYPING, PROGNOSIS AND TREATMENT OF PROSTATE CANCER
    Publication number: 20140037647
    Abstract: Disclosed herein are new prognostic molecular markers for prostate cancer. More specifically, the invention has identified that overexpression or amplification of at least one of AURKA or MYCN define a distinct subgroup of prostate cancer that is predisposed to the development of lethal NEPC, who will benefit from early intervention.
    Type: Application
    Filed: March 28, 2012
    Publication date: February 6, 2014
    Applicant: CORNELL UNIVERSITY
    Inventors: Mark A. Rubin, Himisha Beltran
  • IMIDAZOLE BASED LXR MODULATORS
    Publication number: 20140038964
    Abstract: Methods of using compounds of the invention, such as compounds of Formulae IIa, IIb, IIc, or IId and pharmaceutically acceptable salts thereof are disclosed. The compounds are useful in treating, preventing, inhibiting or ameliorating the symptoms of a disease or disorder that is modulated or otherwise affected by nuclear receptor activity, or in which nuclear receptor activity is implicated.
    Type: Application
    Filed: July 25, 2013
    Publication date: February 6, 2014
    Applicant: Exelixis Patent Company LLC
    Inventors: Brett B. Busch, Brenton T. Flatt, Xiao-Hui Gu, Shao Po Lu, Richard Martin, Raju Mohan, Michael Charles Nyman, Edwin J. Schweiger, William C. Stevens, JR., Tie-Lin Wang, Yinong Xie
  • Hepatitis C virus inhibitors
    Patent number: 8642025
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: February 4, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
  • 2,4-Pyrimidinediamine Compounds and Their Uses
    Publication number: 20140031350
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Application
    Filed: September 26, 2013
    Publication date: January 30, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
  • HETEROARYL SULFONAMIDES AND CCR2/CCR9
    Publication number: 20140031348
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.
    Type: Application
    Filed: July 9, 2013
    Publication date: January 30, 2014
    Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M.K. Pennell, John J. Wright
  • Aminopyrimidines useful as kinase inhibitors
    Patent number: 8637511
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
    Type: Grant
    Filed: June 8, 2010
    Date of Patent: January 28, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Hayley Binch, Michael Mortimore, Chris Davis, Dean Boyall, Simon Everitt, Daniel Robinson, Sham Ramaya, Damien Fraysse, John Studley, Andrew Miller, Michael O'Donnell, Alistair Rutherford, Joanne Pinder
  • 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
  • Heterocyclic derivatives and their use in the treatment of neurological disorders
    Patent number: 8637508
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
    Type: Grant
    Filed: January 11, 2012
    Date of Patent: January 28, 2014
    Assignee: Novartis AG
    Inventors: Sangamesh Badiger, Murali Chebrolu, Konstanze Hurth, Sébastien Jacquier, Rainer Martin Lueoend, Rainer Machauer, Heinrich Rueeger, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle
  • 1-(Arylmethyl)quinazoline-2,4(1H,3H)-diones as PARP Inhibitors and the Use Thereof
    Publication number: 20140023642
    Abstract: Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones thereof, represented by the Formula (I) wherein Ar, R1-R6 are defined herein. Compounds having Formula (I) are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity.
    Type: Application
    Filed: March 31, 2012
    Publication date: January 23, 2014
    Applicant: Impact Therapeutics, Inc.
    Inventors: Sui Xiong Cai, Ye Edward Tian, Haijun Dong, Qingbing Xu, Lizhen Wu, Lijun Liu, Yangzhen Jiang, Qingli Bao, Guoxiang Wang, Feng Yin, Chengyun Gu, Xiuhua Hu, Xiaozhu Wang, Sishun Kang, Shengzhi Chen
  • AROMATIC HETEROCYCLIC DERIVATIVE HAVING TRPV4-INHIBITING ACTIVITY
    Publication number: 20140024647
    Abstract: A compound having TRPV4 inhibitory activity or a pharmaceutically acceptable salt thereof is provided. The present invention is related to a compound represented by the formula (I), wherein R1a is substituted or unsubstituted alkyl or the like; R1b is hydrogen or substituted or unsubstituted alkyl; R1c is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted nonaromatic heterocyclic group or the like; -L- is —C(=0)—NR2? or the like; X is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or the like, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 18, 2012
    Publication date: January 23, 2014
    Inventor: Akira Yukimasa
  • 5-alkynyl-pyrimidines
    Patent number: 8633183
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: January 24, 2011
    Date of Patent: January 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Siegfried Schneider, Dirk Kessler, Lars van der Veen, Tobias Wunberg
  • Kinase inhibitors
    Patent number: 8629132
    Abstract: The present invention provides a new group of protein kinase inhibitors, pyrropyrimidine and pyrazolopyrimidine derivatives, and pharmaceutically acceptable salts and prodrugs thereof that are useful for treating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrropyrimidine and pyrazolopyrimidine derivatives.
    Type: Grant
    Filed: November 12, 2010
    Date of Patent: January 14, 2014
    Assignees: Genosco, Oscotec, Inc.
    Inventors: Jaekyoo Lee, Ho-Juhn Song, Jong Sung Koh, Hee Kyu Lee, Youngsam Kim, Hong Woo Kim, Sunhwa Chang, Sun-Hee Lim, Jang-Sik Choi, Jung-Ho Kim, Se-Won Kim
  • COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY
    Publication number: 20140011770
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Application
    Filed: September 10, 2013
    Publication date: January 9, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
  • PHENYL AMINO PYRIMIDINE COMPOUNDS AND USES THEREOF
    Publication number: 20140011803
    Abstract: The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
    Type: Application
    Filed: June 7, 2013
    Publication date: January 9, 2014
    Inventors: Christopher John BURNS, Andrew Craig DONOHUE, John Thomas FEUTRILL, Thao Lien Thi NGYGEN, Andrew Frederick WILKS, Jun ZENG
  • N-phenyl imidazole carboxamide inhibitors of 3-phosphoinositide-dependent protein kinase-1
    Patent number: 8623857
    Abstract: The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R1, R2, R3, and R6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: January 7, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hon-Chung Tsui, Sunil Paliwal, Hyunjin M. Kim, Angela D. Kerekes, Mary Ann Caplen, Sara J. Esposite, Brian A. McKittrick, Thierry Olivier Fischmann, Ronald J. Doll, Matthew Paul Rainka, Ang Li
  • Acylpiperazinones and their use as pharmaceuticals
    Patent number: 8623865
    Abstract: The invention relates to novel acylpiperazinone compounds, to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.
    Type: Grant
    Filed: January 15, 2013
    Date of Patent: January 7, 2014
    Assignee: Fab Pharma S.A.S.
    Inventors: Vincent Gerusz, Sonia Escaich, Mayalen Oxoby, Francois Moreau
  • SULFONAMIDE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG
    Publication number: 20140005103
    Abstract: The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.
    Type: Application
    Filed: June 25, 2013
    Publication date: January 2, 2014
    Inventors: Craig A. Coburn, Milana Maletic, Richard Soll, Chunsing Li, Yunfu Luo, Zhiqi Qi
  • PHENYL AMINO PYRIMIDINE COMPOUNDS AND USES THEREOF
    Publication number: 20140005180
    Abstract: The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
    Type: Application
    Filed: June 7, 2013
    Publication date: January 2, 2014
    Inventors: Christopher John BURNS, Andrew Craig DONOHUE, John Thomas FEUTRILL, Thao Lien Thi NGUYEN, Andrew Frederick WILKS, Jun ZENG
  • Pyrazolyl-pyrimidine derivatives and their use as potassium channel modulators
    Patent number: 8618099
    Abstract: This invention relates to novel pyrazolyl-pyrimidine derivatives and their use as potassium channel modulating agents. In another aspect the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.
    Type: Grant
    Filed: August 26, 2009
    Date of Patent: December 31, 2013
    Assignee: Ataxion, Inc.
    Inventors: Birgitte L. Eriksen, Charlotte Hougaard, Dan Peters, Palle Christophersen
  • ION CHANNEL MODULATORS AND METHODS OF USE
    Publication number: 20130345208
    Abstract: In general, the invention relates to novel 4-phenylpyrimidine compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels and/or calcium channels for the treatment of pain.
    Type: Application
    Filed: August 23, 2013
    Publication date: December 26, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: ESTHER MARTINBOROUGH, Nicole Zimmerman, Robert B. Perni, Michael Arnost, Upul K. Bandarage, Francois Maltais, Guy Bemis
  • 2,4- DIAMINOPYRIMIDINE DERIVATIVES
    Publication number: 20130345180
    Abstract: There are provided compounds of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as indicated in claim 1, useful in disorders where ZAP-70 and/or Syk inhibition plays a role or caused by a malfunction of signal cascades connected with FAK.
    Type: Application
    Filed: March 15, 2013
    Publication date: December 26, 2013
    Applicant: NOVARTIS AG
    Inventor: Novartis AG