Additional Hetero Ring Attached Directly Or Indirectly To The 1,4-diazine Ring By Nonionic Bonding Patents (Class 514/255.05)
  • PYRIDIN-2(1H)-ONE DERIVATIVES AS JAK INHIBITORS
    Publication number: 20140271543
    Abstract: New pyridin-2(1H)-one derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
    Type: Application
    Filed: July 23, 2012
    Publication date: September 18, 2014
    Applicant: ALMIRALL, S.A.
    Inventors: Paul Robert Eastwood, Jordi Bach Taña, Lluis Miquel Pages Santacana
  • PYRROLIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY
    Publication number: 20140275087
    Abstract: The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: March 17, 2014
    Publication date: September 18, 2014
    Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying X. Wang, Hongyu H. Zhao, Huan-Qiu Li, Jason T. Brewer, Irini Zanze, Justin Dietrich, Anil Vasudevan, Stevan W. Djuric, Yanbin Lao, Charles W. Hutchins
  • SUBSTITUTED PIPERIDINE COMPOUNDS AND THEIR USE AS OREXIN RECEPTOR MODULATORS
    Publication number: 20140275095
    Abstract: The present invention is directed to compounds of Formula I: wherein X is CR1 or N; Y is CR2 or N; Z is NH or O; R1 is alkoxy, triazolyl, oxazolyl, isoxazolyl, oxadiazolyl, or pyrimidinyl; R2 is H, alkyl, or halo; R3 is H, alkyl, alkoxy, halo, triazolyl, oxazolyl, or pyrimidinyl; R4 is alkyl; R5 is pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl; wherein the pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl is optionally substituted with one or two substituents independently selected from the group consisting of alkyl, halo, or phenyl; and R6 is H or alkyl. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Curt A. Dvorak, Brock T. Shireman
  • Mandelamide heterocyclic compounds
    Patent number: 8835470
    Abstract: Disclosed are compounds of Formula (I) or stereoisomers, salts, or prodrugs thereof, wherein: Q is, or R1 is phenyl substituted with zero to 3 substituents; and R1, R2, R3, R4, R5, and G are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Grant
    Filed: April 21, 2011
    Date of Patent: September 16, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert J. Cherney, Yanlei Zhang
  • Pharmaceutical composition containing (2R)-methyl-1-3-[2-(3-pyridinyloxy)ethoxy]-2-pyrazinylpiperazine L-malate for treatment of serotonin-related diseases
    Patent number: 8835439
    Abstract: The present invention relates to a process for the preparation of compounds which are therapeutically active in the central nervous system. In one aspect, the invention relates to a process for the preparation of compounds of the general formula (I): wherein HA is a pharmaceutically acceptable acid and R1-R4 are each independently selected from the group consisting of hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, and di-C1-C6-alkylamino-C2-C6-alkoxy. The invention also relates to the use of said compound to manufacture a medicament for the treatment of a serotonin-related disorder.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: September 16, 2014
    Assignee: Proximagen Limited
    Inventors: Tom Fleck, Magnus Cernerud, Helena Lundstrom, Claes Lofstrom, Margit Pelcman, Alexander Paptchikhine, Emma Andersson, Alf Nygren
  • Fungicidal heterocyclic compounds
    Patent number: 8835427
    Abstract: Disclosed are compounds of Formula 1 and Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein E, Y1, Y2, Y3, G, J, X1 and X2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 or Formula 1A and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: January 7, 2011
    Date of Patent: September 16, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Andris Juris Liepa, Robert James Pasteris, Thomas Martin Stevenson
  • Compounds as cannabinoid receptor ligands
    Patent number: 8835475
    Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: September 16, 2014
    Assignee: AbbVie Inc.
    Inventors: William A. Carroll, Michael J. Dart, Teodozyj Kolasa, Tongmei Li, Derek W. Nelson, Meena Patel, Sridhar Peddi, Arturo Perez-Medrano, Xueqing Wang
  • COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM
    Publication number: 20140256745
    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: October 19, 2012
    Publication date: September 11, 2014
    Applicant: CalciMedica, Inc.
    Inventors: Jianguo Cao, Jeffrey P. Whitten, Zhijun Wang, Evan Rogers, Jonathan Grey
  • POLYCYCLIC COMPOUNDS AS LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS
    Publication number: 20140256744
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: May 21, 2014
    Publication date: September 11, 2014
    Inventors: Ryan Clark, Brian Andrew Stearns, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie M. Arruda
  • BROMODOMAIN INHIBITORS
    Publication number: 20140256705
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Y have any of the values defined 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 11, 2014
    Publication date: September 11, 2014
    Inventors: Lisa A. Hasvold, Dachun Liu, Keith F. McDaniel, John Pratt, George S. Sheppard, Carol K. Wada, Kevin R. Woller
  • SPECTINAMIDES AS ANTI-TUBERCULOSIS AGENTS
    Publication number: 20140249155
    Abstract: Novel 3?-deoxy-3?-acylaminospectinomycin compounds are described. Also described are methods of using the 3?-deoxy-3-acylaminospectinomycin compounds and other spectinomycin analogs in treating tuberculosis and in treating microbial infections.
    Type: Application
    Filed: March 23, 2014
    Publication date: September 4, 2014
    Applicant: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
    Inventors: Richard E. Lee, Jianjun Qi, Julian G. Hurdle, Bernd Meibohm, VNR Pavan Kumar Vaddady, Rakesh, Jiuyu Liu
  • Treatment Of Blood Lipid Abnormalities And Other Conditions
    Publication number: 20140249156
    Abstract: There is provided a method of treatment of a patient suffering from blood lipid abnormality comprises the administration of a GPR119 agonist.
    Type: Application
    Filed: October 31, 2012
    Publication date: September 4, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Kathleen Brown, Andrew James Carpenter, Derek J.R. Nunez, Andrew Young
  • SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF CANCERS, INCLUDING HEPATOCELLULAR CARCINOMA, AND AS INHIBITORS OF HEPATITIS VIRUS REPLICATION
    Publication number: 20140249154
    Abstract: Pharmaceutical compositions of the invention are presented which comprise substituted aminothiazoles derivatives. The substituted aminothiazoles derivatives have a disease-modifying action in the treatment of diseases associated with unregulated cell growth. Such diseases include cancers such as hepatocellular carcinoma, and viral infections from a hepatitis virus.
    Type: Application
    Filed: October 4, 2012
    Publication date: September 4, 2014
    Inventors: Andrea Cuconati, Xiaodong Xu, Timothy M. Block
  • COMPOUNDS, COMPOSITIONS, AND METHODS FOR PREVENTING METASTASIS OF CANCER CELLS
    Publication number: 20140249100
    Abstract: Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.
    Type: Application
    Filed: March 3, 2013
    Publication date: September 4, 2014
    Applicant: Aerpio Therapeutics Inc.
    Inventors: Robert Shalwitz Shalwitz, Kevin Gene Peters
  • TRIAZOLYL PDE10 INHIBITORS
    Publication number: 20140249134
    Abstract: The present invention is directed to substituted triazolyl compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: October 3, 2012
    Publication date: September 4, 2014
    Inventors: Christopher D. Cox, Vadim Y. Dudkin, June J. Kim, Scott D. Kuduk, Carol A. McVean, Thomas Reger, Justin T. Sheen, Thomas Steele
  • PIM KINASE INHIBITORS AND METHODS OF THEIR USE
    Publication number: 20140249135
    Abstract: New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
    Type: Application
    Filed: May 9, 2014
    Publication date: September 4, 2014
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Mika Lindvall, Wooseok Han, Jiong Lan, Gisele Nishiguchi, Cynthia Shafer, Cornelia Bellamacina, Kay Huh, Gordana Atallah, Christopher McBride, William Antonios-McCrea, JR., Tatiana Zavorotinskaya, Annette Walter, Pablo Dominguez Garcia
  • NOVEL ANTIVIRAL PYRROLOPYRIDINE DERIVATIVES AND METHOD FOR PREPARING THE SAME
    Publication number: 20140249162
    Abstract: The present invention relates to a pyrrolopyridine derivative represented by the Chemical Formula I, and a racemate or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and relates to an antiviral composition including the same as an active ingredient. The compound of the Chemical Formula I has excellent antiviral activity and selectivity for wild type and resistant HIV-1, and thereby is useful as a therapeutic agent for acquired immune deficiency syndrome (AIDS).
    Type: Application
    Filed: May 15, 2014
    Publication date: September 4, 2014
    Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Jong Chan SON, Bong Jin KIM, Jae Hak KIM, Ill Young LEE, Chang Soo YUN, Sang Ho LEE, Chong Kgo LEE
  • PIM kinase inhibitors and methods of their use
    Patent number: 8822497
    Abstract: New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
    Type: Grant
    Filed: March 3, 2008
    Date of Patent: September 2, 2014
    Assignee: Novartis AG
    Inventors: Matthew Burger, Mika Lindvall, Wooseok Han, Jiong Lan, Gisele Nishiguchi, Cynthia Shafer, Cornelia Bellamacina, Kay Huh, Gordana Atallah, Christopher McBride, William Antonios-McCrea, Jr., Tatiana Zavorotinskaya, Annette Walter, Pablo Garcia
  • Compounds, pharmaceutical compositions and uses thereof
    Patent number: 8822471
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, LP, LQ, Ar, m 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: Grant
    Filed: March 13, 2012
    Date of Patent: September 2, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Bernd Nosse, Andreas Blum, Steffen Breitfelder, Armin Heckel, Frank Himmelsbach, Elke Langkopf, Bernd Wellenzohn, Neil J. Ashweek, Nicole Harriott
  • BICYCLIC COMPOUND
    Publication number: 20140243310
    Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: October 23, 2012
    Publication date: August 28, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tohru Yamashita, Takuya Fujimoto, Ryo Mizojiri, Kazuko Yonemori, Hideki Hirose, Zenichi Ikeda, Ikuo Fujimori, Kyoko Toyofuku, Tsuneo Yasuma, Nobuyuki Matsunaga
  • COMPOUNDS, COMPOSITIONS, AND METHODS FOR PREVENTING METASTASIS OF CANCER CELLS
    Publication number: 20140242026
    Abstract: Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Inventors: Robert Shalwitz, Kevin Gene Peters
  • USE OF NRF2 INDUCERS TO TREAT EPIDERMOLYSIS BULLOSA SIMPLEX AND RELATED DISEASES
    Publication number: 20140243267
    Abstract: The present invention relates to methods and compositions for the prevention and treatment of keratin-based skin diseases. In particular, the application describes compositions and methods of treating a patient suffering from skin blistering comprising the use of phase II enzyme inducers.
    Type: Application
    Filed: September 12, 2013
    Publication date: August 28, 2014
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Pierre A. Coulombe, Michelle L. Kerns
  • SUBSITUTED 2-(CHROMAN-6-YLOXYL)-THIAZOLES AND THEIR USE AS PHARMACEUTICALS
    Publication number: 20140243292
    Abstract: The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: March 11, 2014
    Publication date: August 28, 2014
    Applicant: Sanofi
    Inventors: Werngard CZECHTIZKY, John WESTON, Nils RACKELMANN, Michael PODESCHWA, Petra ARNDT, Klaus WIRTH, Heinz GOEGELEIN, Olaf RITZELER, Volker KRAFT, Patrice BELLEVERGUE, Gary McCORT
  • 5- OR 6-SUBSTITUTED 3-HYDROXY-2(1H)-PYRIDINONES AS D-AMINO ACID OXIDASE (DAAO) INHIBITORS IN THERAPY OF DISEASES SUCH AS SCHIZOPHRENIA, COGNITIVE DISORDER AND PAID
    Publication number: 20140243353
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 is hydrogen or fluorine, one of A and B is R2, the other is a group —X—Y—R3. R3 represents a carbocyclic or heterocyclic ring. Further variables are as defined in the specification. Also claimed are—processes for their preparation, pharmaceutical compositions containing them and their use in therapy of diseases such as schizophrenia, cognitive disorders and pain by modulating the D-amino acid oxidase enzyme (DAAO).
    Type: Application
    Filed: July 5, 2012
    Publication date: August 28, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: William Farnaby, Charlotte Fieldhouse, Catrina Kerr, Natasha Kinsella, David Livermore, Kevin Merchant, David Miller, Katherine Hazel
  • Co-crystal intermediates of rosuvastatin and methods of using same
    Patent number: 8815862
    Abstract: Methods for the preparation of Rosuvastatin by co-crystals of Rosuvastatin or intermediates are provided. Also provided are co-crystals, pharmaceutical compositions which include such co-crystals and methods for treating conditions associated with hypercholesterolemia by administering such compositions.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: August 26, 2014
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Clark Ferrari, Andrea Castellin, Marco Galvagni, Nicolas Tesson, Jordi De Mier, Llorenç Rafecas
  • N,N-substituted 3-aminopyrrolidine compounds useful as monoamines reuptake inhibitors
    Patent number: 8815871
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: August 26, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Muneaki Kurimura, Shinichi Taira, Takahiro Tomoyasu, Nobuaki Ito, Kuninori Tai, Noriaki Takemura, Takayuki Matsuzaki, Yasuhiro Menjo, Shin Miyamura, Yohji Sakurai, Akihito Watanabe, Yasuyo Sakata, Takumi Masumoto, Kohei Akazawa, Haruhiko Sugino, Naoki Amada, Satoshi Ohashi, Tomoichi Shinohara, Hirofumi Sasaki, Chisako Morita, Junko Yamashita, Satoko Nakajima
  • Substituted 4-hydroxypyrimidine-5-carboxamides
    Patent number: 8815865
    Abstract: The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: June 21, 2010
    Date of Patent: August 26, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew J. Clements, John S. Debenham, Jeffrey J. Hale, Christina Madsen-Duggan
  • Indanyloxydihydrobenzofuranylacetic acids
    Patent number: 8815864
    Abstract: The present invention relates to compounds of general formula I, wherein the group (Het)Ar is 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: November 25, 2013
    Date of Patent: August 26, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Elke Langkopf, Holger Wagner
  • Pyridine Derivatives
    Publication number: 20140235652
    Abstract: The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.
    Type: Application
    Filed: November 13, 2013
    Publication date: August 21, 2014
    Applicant: Endo Pharmaceuticals Inc.
    Inventors: Roger A. Smith, Nicholas James Laping, Aranapakam M. Venkatesan, Raghava Reddy Kethiri, Chandregowda Venkateshappa, Bheemashankar Kulkarni, Purushottam Dewang, Rajendra Kristam, Rajesh Devraj
  • Novel Dihydropyrimidin-2(1H)-one Compounds as S-Nitrosoglutathione Reductase Inhibitors
    Publication number: 20140235640
    Abstract: The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: N30 PHARMACEUTICALS, INC.
    Inventors: Xicheng Sun, Jian Qiu
  • SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS
    Publication number: 20140235647
    Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is 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: Application
    Filed: September 27, 2012
    Publication date: August 21, 2014
    Inventors: James Aaron Balog, Audris Huang, Upender Velaparthi, Peiying Liu
  • HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
    Publication number: 20140235579
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Inventors: John M. McCall, Donna L. Romero, Michael Clare
  • PYRAZOLE CARBOXAMIDES AS JANUS KINASE INHIBITORS
    Publication number: 20140235641
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: September 21, 2012
    Publication date: August 21, 2014
    Inventors: Jason Brubaker, Joshua Close, Tony Siu, Graham Frank Smith, Luis E. Torres, Hyun Chong Woo, Jonathan R. Young, Zhongyong Wei, Feng Shi
  • HYDRAZIDE CONTAINING NUCLEAR TRANSPORT MODULATORS AND USES THEREOF
    Publication number: 20140235653
    Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Application
    Filed: March 19, 2014
    Publication date: August 21, 2014
    Applicant: Karyopharm Therapeutics, Inc.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
  • PRIMARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
    Publication number: 20140235622
    Abstract: The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.
    Type: Application
    Filed: January 28, 2014
    Publication date: August 21, 2014
    Applicant: Arena Pharmaceuticals, Inc.
    Inventors: Bradley Teegarden, Dennis Chapman, Juyi Choi, Konrad Feichtinger, Sangdon Han, Honnappa Jayakumar, Thuy-Anh Tran, Jay Xu, Ning Zou
  • Crystalline form
    Patent number: 8809340
    Abstract: This invention relates to a new crystalline form of the succinate salt of the epithelial sodium channel (ENaC) blocker 3-(3-{2-[(E)-3,5-Diamino-6-chloro-pyrazine-2-carbonylimino]-1,3,8-triaza-spiro[4.5]decane-8-carbonyl}-benzenesulfonylamino)-propionic acid dipropylcarbamoylmethyl ester, pharmaceutical compositions comprising said crystalline form, uses of said crystalline form and pharmaceutical compositions, and methods for preparing said crystalline form.
    Type: Grant
    Filed: March 12, 2013
    Date of Patent: August 19, 2014
    Assignee: Novartis AG
    Inventors: Catherine Howsham, Christian Lindenberg, Anett Perlberg, Nicola Tufilli
  • Imidazole, pyrazole, and triazole derivatives useful as antibacterial agents
    Patent number: 8809333
    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: Grant
    Filed: March 27, 2012
    Date of Patent: August 19, 2014
    Assignee: Pfizer Inc.
    Inventors: Matthew Frank Brown, Jinshan Michael Chen, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
  • Compounds and methods for inhibiting phosphate transport
    Patent number: 8809339
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: August 19, 2014
    Assignee: Ardelyx, Inc.
    Inventors: Jason G. Lewis, Jeffrey W. Jacobs, Nicholas Reich, Michael R. Leadbetter, Noah Bell, Han-Ting Chang, Tao Chen, Marc Navre, Dominique Charmot, Christopher Carreras, Eric Labonte
  • Heterocyclic compounds, medicaments containing said compounds, use thereof and processes for the preparation thereof
    Publication number: 20140228374
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 14, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Armin HECKEL, Sara FRATTINI, Dieter HAMPRECHT, Joerg KLEY
  • PREPARATION AND METHODS OF USE FOR ORTHO-ARYL 5-MEMBERED HETEROARYL-CARBOXAMIDE CONTAINING MULTI-TARGETED KINASE INHIBITORS
    Publication number: 20140228367
    Abstract: The present disclosure relates to compounds of the Formula (I): and pharmaceutically acceptable salts, as kinase modulators, compatible with the Type-II inhibition of kinases.
    Type: Application
    Filed: February 5, 2014
    Publication date: August 14, 2014
    Inventor: Gary A. Flynn
  • BENZONITRILE DERIVATIVES AS KINASE INHIBITORS
    Publication number: 20140228340
    Abstract: Compounds of the formula I, in which R1, R2, X and Y have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.
    Type: Application
    Filed: August 13, 2012
    Publication date: August 14, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Guenter Hoelzemann, Dieter Dorsch, Hans-Michael Eggenweiler
  • BIOMARKERS AND THERAPY FOR CANCER
    Publication number: 20140228423
    Abstract: In embodiments of the present invention, there are methods and compositions related to diagnosis and treatment of serous ovarian cancer. In specific embodiments, the invention encompasses methods related to miR-34c in diagnosis and treatment methods for serous ovarian cancer. In specific embodiments, the invention encompasses treatment methods for pancreatic cancer and other responsive cancers.
    Type: Application
    Filed: June 1, 2012
    Publication date: August 14, 2014
    Applicant: BAYLOR COLLEGE OF MEDICINE
    Inventors: Martin M. Matzuk, Jaeyeon Kim, Zhifeng Yu
  • 1-ARYLCARBONYL-4-OXY-PIPERIDINE COMPOUNDS USEFUL FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
    Publication number: 20140228373
    Abstract: The present invention provides a compound useful as an agent for the prophylaxis or treatment of neurodegenerative disease and the like, or a salt thereof. The present invention relates to a compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: October 3, 2012
    Publication date: August 14, 2014
    Inventors: Tatsuki Koike, Masato Yoshikawa, Haruhi Ando, William John Farnaby
  • TETRASUBSTITUTED CYCLOHEXYL COMPOUNDS AS KINASE INHIBITORS
    Publication number: 20140228363
    Abstract: The present invention provides a compound of formula (I): as further described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: April 22, 2014
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Yu Ding, Wooseok Han, Gisele Nishiguchi, Alice Rico, Robert Lowell Simons, Aaron R. Smith, Victoriano Tamez, JR., Huw Tanner, Lifeng Wan
  • GAMMA SECRETASE INHIBITORS
    Publication number: 20140227302
    Abstract: Disclosed herein are compounds of Formula (I) (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
    Type: Application
    Filed: September 4, 2012
    Publication date: August 14, 2014
    Inventors: Wen-Lian Wu, Duane A. Burnett
  • Heterocyclic Compounds for the Treatment of CF
    Publication number: 20140228376
    Abstract: The present invention provides pyridin-oxadiazole/thiadiazole derivatives of Formula I wherein A is N or CR 4a; and (ii) or (iii) which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: September 14, 2012
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: Kamlesh Jagdis Bala, Rebecca Butler, Stephen Paul Collingwood, Edward Charles Hall, Lee Edwards, Darren Mark Legrand, Katrin Spiegel
  • Pyrrolidine derivatives
    Patent number: 8802665
    Abstract: The invention relates to a compound of formula (I) wherein A1 to A3 and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: August 12, 2014
    Assignee: Genentech, Inc.
    Inventors: David Banner, Wolfgang Haap, Thomas Luebbers, Jens-Uwe Peters
  • TUBULIN INHIBITORS
    Publication number: 20140221396
    Abstract: Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).
    Type: Application
    Filed: February 28, 2014
    Publication date: August 7, 2014
    Applicant: YM Biosciences Australia Pty Ltd.
    Inventors: Christopher John BURNS, Andrew Frederick WILKS, Michael Francis HARTE, Harrison SIKANYIKA, Emmanuelle FANTINO
  • PYRROLINONE CARBOXAMIDE COMPOUNDS USEFUL AS ENDOTHELIAL LIPASE INHIBITORS
    Publication number: 20140221357
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: September 25, 2012
    Publication date: August 7, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
    Publication number: 20140221379
    Abstract: The present invention relates to N-(hetero)aryl-pyrrolidine derivatives of Formula I: which are JAK inhibitors, such as selective JAK1 inhibitors, useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
    Type: Application
    Filed: April 11, 2014
    Publication date: August 7, 2014
    Applicant: Incyte Corporation
    Inventors: James D Rodgers, Stacey Shepard, Argyrios G Arvanitis, Haisheng Wang, Louis Storace, Beverly Folmer, Wenyu Zhu, Joseph Glenn, Lixin Shao