Additional Hetero Ring Patents (Class 514/397)
  • Patent number: 8889726
    Abstract: Disclosed are compounds of Formula I, Formula II, and Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: November 18, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Subramanian Baskaran, Richard Martin Grimes, Wieslaw Mieczyslaw Kazmierski, Martin Robert Leivers
  • Publication number: 20140336232
    Abstract: The present invention relates to novel 2-iodoimidazole derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.
    Type: Application
    Filed: November 23, 2012
    Publication date: November 13, 2014
    Inventors: Hendrik Helmke, Sebastian Hoffmann, Carl Friedrich Nising, Alexander Sudau, Tomoki Tsuchiya, Jürgen Benting, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Stephane Brunet, Marie-Claire Grosjean-Cournoyer, Hélène Lachaise, Philippe Rinolfi
  • Publication number: 20140335153
    Abstract: A method of preparing a thin film, the method comprising: (a) mixing a lipid, emulsifier, and solvent to provide a uniform first mixture; (b) contacting an active ingredient with the uniform first mixture to provide a thickened second mixture; (c) contacting a binder with the thickened second mixture to provide a slurry; and (d) hot extruding, casting, and condensing the slurry to provide the thin film; or cooling, shearing, mixing, casting, and condensing the slurry to provide the thin film.
    Type: Application
    Filed: October 31, 2013
    Publication date: November 13, 2014
    Applicant: CURE Pharmaceutical Corporation
    Inventors: Eric Allen, Robert Steven Davidson, Jose Bernardo
  • Publication number: 20140336184
    Abstract: The present invention concerns methods and compositions regarding suppression of double stranded RNA-activated protein kinase (PKR) to enhance cognition in an individual. In specific cases, an inhibitor of PKR is provided to the individual such that cognition is enhanced thereby, including by enhancing memory, for example. Kits are encompassed in certain embodiments.
    Type: Application
    Filed: November 29, 2012
    Publication date: November 13, 2014
    Inventors: Mauro Costa-Mattioli, Ping Jun Zhu, Jeremy A. May
  • Publication number: 20140329796
    Abstract: The present invention aims to provide a novel compound having a TRPA1 antagonist activity, and a medicament containing the compound. Moreover, the present invention aims to provide a TRPA1 antagonist and a medicament useful for the prophylaxis or treatment of diseases involving TRPA1. A medicament containing a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and the like.
    Type: Application
    Filed: July 16, 2014
    Publication date: November 6, 2014
    Applicant: Ajinomoto Co., Inc.
    Inventors: Tamotsu SUZUKI, Kaori Kobayashi, Sayaka Asari, Seiji Shiraishi, Tatsuya Okuzumi
  • Publication number: 20140329815
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are 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. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Application
    Filed: July 21, 2014
    Publication date: November 6, 2014
    Inventors: Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
  • Publication number: 20140329812
    Abstract: The present invention relates to aryl triazole derivatives of Formula I having antitumoural activity through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical composition containing such compounds.
    Type: Application
    Filed: December 13, 2011
    Publication date: November 6, 2014
    Applicant: SIGMA-TAU RESEARCH SWITZERLAND S.A.
    Inventors: Giuseppe Giannini, Walter Cabri, Loredana Vesci, Maria Luisa Cervoni, Claudio Pisano, Maurizio Taddei, Serena Ferrini
  • Publication number: 20140323458
    Abstract: The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D??(Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.
    Type: Application
    Filed: July 10, 2014
    Publication date: October 30, 2014
    Inventors: Jason Allan Wiles, Qiuping Wang, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Venkat Gadhachanda, Avinash Phadke, Milind Deshpande, Dawei Chen
  • Publication number: 20140322247
    Abstract: Disclosed herein are immunoconjugates comprising an inhibitor of Eg5 linked to an antigen binding moiety such as an antibody, that are useful for treating cell proliferative disorders. Also disclosed are novel inhibitors of Eg5 that can be used either alone or as part of an immunoconjugate to treat cell proliferation disorders. The Eg5 inhibitors include compounds of this formula as described herein: The invention further provides pharmaceutical compositions comprising these compounds and immunoconjugates, and compositions comprising the immunoconjugates or compounds with a therapeutic co-agent, and methods to use these compounds, conjugates and compositions for treating cell proliferation disorders.
    Type: Application
    Filed: March 13, 2014
    Publication date: October 30, 2014
    Applicant: NOVARTIS AG
    Inventors: Paul A. Barsanti, Sylvie Chamoin, Lionel Doumampouom-Metoul, Stephanie Guerro-Lagasse, Robert Martin Grotzfeld, Alexei Karpov, Marc Lafrance, Cristina Montserrat Nieto-Oberhuber, Grazia Piizzi
  • Publication number: 20140322325
    Abstract: A drug in a solubility-improved form is combined with a concentration-enhancing polymer in a sufficient amount so that the combination provides substantially enhanced drug concentration in a use environment relative to a control comprising the same amount of the same solubility-improved form of drug without the concentration-enhancing polymer.
    Type: Application
    Filed: July 14, 2014
    Publication date: October 30, 2014
    Applicant: Bend Research, Inc.
    Inventors: William J. Curatolo, Ravi M. Shanker, Walter C. Babcock, Dwayne T. Friesen, James A. S. Nightingale, Douglas A. Lorenz
  • Patent number: 8871210
    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: Grant
    Filed: November 8, 2013
    Date of Patent: October 28, 2014
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Masaya Kokubo, Motoyuki Tanaka, Hiroshi Ochiai, Yoshikazu Takaoka, Shiro Shibayama
  • Publication number: 20140315808
    Abstract: A method of treating a disease or condition in which up-regulating GAGs is therapeutically beneficial is disclosed. The method comprises locally administering to a subject a therapeutically effective amount of an agent capable of down-regulating activity or expression of a component of the renin-angiotensin system.
    Type: Application
    Filed: June 30, 2014
    Publication date: October 23, 2014
    Inventors: Talia WEINSTEIN, Uzi GAFTER, Zvi NEVO, Dror ROBINSON, Zoharia EVRON
  • Publication number: 20140315892
    Abstract: The present invention relates to (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable salts thereof, compositions comprising (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and methods for treating or preventing an alcohol-related or addictive disorder. The (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.
    Type: Application
    Filed: January 31, 2014
    Publication date: October 23, 2014
    Inventors: Anthony Alexander McKinney, Franklin Porter Bymaster
  • Publication number: 20140315889
    Abstract: The present invention relates to a novel hydroxamate derivatives, more specifically, to novel hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC), isomers thereof, pharmaceutically acceptable salts thereof, hydrates or solvates thereof, use for preparing pharmaceutical compositions, pharmaceutical compositions comprising the same, treatment method using said composition, and a preparing method of novel hydroxamate derivatives. The novel selective hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC) compositions can be used for treatment of inflammatory disease, rheumatoid arthritis, or degenerative disease.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 23, 2014
    Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: Yuntae Kim, Changsik Lee, Hyun-mo Yang, Hojin Choi, Jaeki Min, Soyoung Kim, Dal-Hyun Kim, Nina Ha, Jung-Min Kim, Hyojin Lim, Eunhee Ko
  • Publication number: 20140315899
    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 A, B, G, Y, R1, R2, R3, and R4 are defined herein.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Andraka, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
  • Publication number: 20140315945
    Abstract: The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Applicant: EPIZYME, INC.
    Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
  • Publication number: 20140315792
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
    Type: Application
    Filed: February 14, 2014
    Publication date: October 23, 2014
    Inventors: Rolf Wagner, John K. Pratt, Dachun Liu, Michael D. Tufano, David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Dooner, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, David A. Betebenner, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, Yi Gao, Allan C. Krueger
  • Patent number: 8865756
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Grant
    Filed: December 2, 2009
    Date of Patent: October 21, 2014
    Assignee: Presidio Pharmaceuticals, Inc.
    Inventors: Leping Li, Min Zhong
  • Patent number: 8859602
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are 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. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: October 14, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Bruce E. Tomczuk, Mark Wall, Kenneth Wilson
  • Patent number: 8859611
    Abstract: The present invention is directed to novel thiophene inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: November 5, 2013
    Date of Patent: October 14, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventor: Xicheng Sun
  • Patent number: 8859595
    Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing hepatitis C virus (HCV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment or prevention of HCV infection.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: October 14, 2014
    Assignees: RFS Pharma, LLC, Emory University
    Inventors: Steven J. Coats, Franck Amblard, Hongwang Zhang, Longhu Zhou, Richard Anthony Whitaker, Tamara Rosario McBrayer, Raymond F. Schinazi, Junxing Shi
  • Publication number: 20140303221
    Abstract: A pharmaceutical composition for treating sudden discomfort associated with nausea and vomiting is disclosed which comprises a therapeutically effective amount of Ondansetron or a pharmaceutical salt thereof formulated for intranaal administration in combination with an antimicrobial preservative yielding enhanced stability of the Ondansetron or pharmaceutical salt thereof with a long chain polymer enhancing the viscosity of the composition.
    Type: Application
    Filed: April 8, 2013
    Publication date: October 9, 2014
    Inventors: Abdul Zahir, Ryan John Welter
  • Publication number: 20140302141
    Abstract: This invention pertains to a multi-layered tablet for a triple combination release of active agents to an environment of use. More particularly, the invention pertains to a multi-layered tablet (1) comprising two external drug-containing layers (2 and 3) in stacked arrangement with respect to and on opposite sides of an oral dosage form (4) that provides a triple combination release of at least one active agent. In one embodiment of the invention the dosage form is an osmotic device. In another embodiment of the invention the dosage form is a gastro-resistant coated core. In yet another embodiment of the invention the dosage form is a matrix tablet. In a different embodiment the dosage form is a hard capsule.
    Type: Application
    Filed: February 24, 2014
    Publication date: October 9, 2014
    Applicant: OSMOTICA KERESKEDELMI ES SZOLGALTATO KFT
    Inventors: FERNANDO G. TONEGUZZO, GLENN A. MEYER, Marcelo A. RICCI, Marcelo A. COPPARI, ANA C. PASTINI, GUSTAVO A. FISCHBEIN
  • Patent number: 8853196
    Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: October 7, 2014
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Wilhelm Amberg, Udo Lange, Frauke Pohlki
  • Patent number: 8853416
    Abstract: Disclosed are compounds of Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: October 7, 2014
    Assignee: Janssen Pharmaceuticals, Inc.
    Inventors: Pingyun Chen, Ricky Couch, Maosheng Duan, Beth Adams Norton
  • Publication number: 20140296313
    Abstract: The present invention is directed to imidazole derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new imidazole NaV1.8 modulators of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description. NaV1.8 modulators useful in the treatment of a wide range of disorders, particularly pain.
    Type: Application
    Filed: October 15, 2012
    Publication date: October 2, 2014
    Applicant: Pfizer Limited
    Inventors: Sharanjeet Kaur Bagal, Mark Ian Kemp, Duncan Charles Miller, Yoshihisa Murata
  • Publication number: 20140294767
    Abstract: A method of treating an Hepatitis C Virus infection in a patient, comprising providing a therapeutically effective amount, to a patient in need thereof, of a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: G1 is a group of the formula or where n is 0, 1, 2, 3, or 4 and Het is a 5- or 6-membered heteroaryl group containing 1 to 4 heteroatoms independently chosen from N, O, and S, which Het is optionally substituted.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 2, 2014
    Inventors: David Waugh, Christopher Self, Guangtao Zhang, Yves Pommier, Robert H. Shoemaker, Michael Currens, John Cardellina, Andrew Jobson, George Lountos, Dominic Scudiero
  • Publication number: 20140296217
    Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.
    Type: Application
    Filed: February 20, 2014
    Publication date: October 2, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: John Edward PARK, Gerald Juergen ROTH, Armin HECKEL, Nveed CHAUDHARY, Trixi BRANDL, Georg DAHMANN, Matthias GRAUERT
  • Patent number: 8846948
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3, R3a have meanings given in the description.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: September 30, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Rudolf, Daniel Bischoff, Georg Dahmann, Matthias Grauert, Raimund Kuelzer
  • Patent number: 8846741
    Abstract: The present invention relates to N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives of the formula (I), (II), (III) or (IV) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such N-substituted amino-benzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives, and the use of such N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives for therapeutic purposes. The N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives are GlyT1 inhibitors.
    Type: Grant
    Filed: November 19, 2012
    Date of Patent: September 30, 2014
    Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KG
    Inventors: Wilhelm Amberg, Udo Lange, Frauke Pohlki, Ernesto Santandrea, Charles Hutchins
  • Patent number: 8846023
    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: September 9, 2013
    Date of Patent: September 30, 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, Gan Wang, Lawrence G. Hamann
  • Publication number: 20140288084
    Abstract: In one aspect, the invention relates to substituted 2-(4-heterocyclylbenzyl)isoindolin-1-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. 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: October 28, 2012
    Publication date: September 25, 2014
    Applicant: VANDERBILT UNIVERSITY
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Woods, Corey R. Hopkins, Bruce J. Melancon, Michael S. Poslusney, Darren W. Engers
  • Publication number: 20140288050
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as pain, neurological disorders, psychiatric disorders, and neuromuscular disorders. Compounds provided herein modulate the activity of opioid receptor (e.g., ?-opioid receptor) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: November 7, 2012
    Publication date: September 25, 2014
    Inventors: Scott Malcolm, Carrie Bowen, Laurence Melnick, Linghong Xie
  • Publication number: 20140288139
    Abstract: Compositions and methods are provided that are useful for diagnosing, treating, and monitoring alcohol dependence and disorders, susceptibility to alcohol dependence disorders, as well as drug related dependence and disorders. The methods include treating patients with an antagonist of the serotonin receptor 5-HT3 for such disorders, wherein the patient's serotonin transporter gene SLC6A4 is known to have particular genotypes.
    Type: Application
    Filed: April 30, 2014
    Publication date: September 25, 2014
    Inventor: Bankole A. Johnson
  • Patent number: 8841278
    Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: October 3, 2013
    Date of Patent: September 23, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Elizabeth M. Bacon, Eda Canales, Aesop Cho, Jeromy J. Cottell, Manoj C. Desai, Michael Graupe, Hongyan Guo, Randall L. Halcomb, Darryl Kato, Choung U. Kim, Thorsten A. Kirschberg, Evan S. Krygowski, Scott E. Lazerwith, John O. Link, Hongtao Liu, Qi Liu, Richard L. Mackman, Michael L. Mitchell, Jay P. Parrish, Hyung-Jung Pyun, Joseph H. Saugier, Scott D. Schroeder, Jianyu Sun, James G. Taylor, James D. Trenkle, Winston C. Tse, Randall W. Vivian, William J. Watkins, Lianhong Xu
  • Publication number: 20140271851
    Abstract: A pharmaceutical formulation includes (1) a first dosage component comprising: a core comprising a non-ionic polymer matrix, a first amount of ondansetron or an equivalent amount of an ondansetron salt thereof dispersed within the matrix, and an electrolyte dispersed within the matrix; a first seal coat surrounding the core, the first seal coat comprising a non-ionic polymer matrix; and an immediate release drug layer surrounding the first seal coat, wherein the immediate release drug layer comprises a non-ionic polymer and a second amount of ondansetron or an equivalent amount of an ondansetron salt thereof dispersed therein; and (2) a second dosage component comprising: a core comprising a third amount of ondansetron or an equivalent amount of an ondansetron salt thereof, at least one filler, and a lubricant; and a coating surrounding the core, the coating comprising water and a mixture of methacrylic acid-alkyl acrylate copolymers with alkaline groups.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: RedHill Biopharma Ltd.
    Inventors: Reza Fathi, Gilead Raday, Patrick Gosselin, Guy Goldberg
  • Publication number: 20140274689
    Abstract: Provided herein are new N-,C-disubstituted azoles and derivatives thereof that exhibit nematicidal activity and are useful, for example, in methods for the control of unwanted nematodes.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Monsanto Technology LLC
    Inventors: Urszula J. Slomczynska, William P. Haakenson, JR.
  • Publication number: 20140271887
    Abstract: A solid oral dosage form includes a core comprising a non-ionic polymer matrix, a first amount of a first antiemetic drug or a pharmaceutically acceptable salt thereof dispersed within the matrix, and a salt dispersed within the matrix; a first seal coat of a non-ionic polymer matrix surrounding the core; and an immediate release drug layer surrounding the first seal coat, wherein the immediate release drug layer comprises a non-ionic polymer and a second amount of a second antiemetic drug or a pharmaceutically acceptable salt thereof dispersed therein, wherein the drug layer is sufficiently designed to release the second amount of the antiemetic drug over a period of at least 1 hour, wherein the solid oral dosage form is sufficiently designed to release the first amount of the first antiemetic drug and the second amount of the second antiemetic drug over a minimum period of 16 hours.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: RedHill Biopharma Ltd.
    Inventors: Reza Fathi, Gilead Raday
  • Publication number: 20140275006
    Abstract: The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia, and so forth.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 18, 2014
    Applicant: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Mitsukane Yoshinaga, Takeshi Kuwada, Naoki Miyakoshi, Tomoko Ishizaka, Daisuke Wakasugi, Shin-ichi Shirokawa, Nobutaka Hattori, Youichi Shimazaki
  • Publication number: 20140275074
    Abstract: The present invention is related to a compound represented by formula (I), wherein X1, X2, X3, X4, X5, R5, R6, R7, R8, n, p, q, ring A and ring B are as described in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 24, 2012
    Publication date: September 18, 2014
    Inventors: Kayoko Hata, Manami Masuda, Hiromi Nakai, Daisuke Taniyama, Hiroyuki Tobinaga, Yoshio Hato, Motohiro Fujiu
  • Publication number: 20140271662
    Abstract: The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom ? with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom ? with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.
    Type: Application
    Filed: February 14, 2014
    Publication date: September 18, 2014
    Applicants: Astex Therapeutics Ltd, Cancer Research Technology Limited, The Institute of Cancer Research: Royal Cancer Hospital
    Inventors: Valerio BERDINI, Gordon SAXTY, Marinus Leendert VERDONK, Steven John WOODHEAD, Paul Graham WYATT, Robert George BOYLE, Hannah Fiona SORE, David Winter WALKER, Ian COLLINS, Robert DOWNHAM, Robin Arthur Ellis CARR
  • 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
  • Patent number: 8835479
    Abstract: The invention provides a method for the treatment of fungal dermatitis. The treatment method involves administering an effective amount of luliconazole or a pharmaceutically acceptable salt thereof to a target in need of a treatment of fungal dermatitis.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: September 16, 2014
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Hiroyasu Koga, Yasuko Nanjoh, Hideo Kaneda
  • Patent number: 8829037
    Abstract: The present disclosure describes compositions which improve visual acuity and to methods for their use.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: September 9, 2014
    Inventor: Anant Sharma
  • Patent number: 8822520
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for treatment of hepatitis C.
    Type: Grant
    Filed: September 21, 2011
    Date of Patent: September 2, 2014
    Assignee: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Patent number: 8822449
    Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula (I) and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.
    Type: Grant
    Filed: August 25, 2009
    Date of Patent: September 2, 2014
    Assignee: Sanofi
    Inventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
  • Patent number: 8822444
    Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: September 2, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Omar D. Lopez, Qi Chen, Makonen Belema, Lawrence G. Hamann
  • Patent number: 8822513
    Abstract: The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.
    Type: Grant
    Filed: August 24, 2011
    Date of Patent: September 2, 2014
    Assignees: GTX, Inc., University of Tennessee Research Foundation
    Inventors: Yan Lu, Chien-Ming Li, Zhao Wang, Jianjun Chen, Wei Li, James T. Dalton, Duane D. Miller, Charles Duke, Sunjoo Ahn
  • Patent number: 8822430
    Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: July 31, 2013
    Date of Patent: September 2, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Elizabeth M. Bacon, Eda Canales, Aesop Cho, Jeromy J. Cottell, Manoj C. Desai, Michael Graupe, Hongyan Guo, Randall L. Halcomb, Darryl Kato, Choung U. Kim, Thorsten A. Kirschberg, Evan S. Krygowski, Scott E. Lazerwith, John O. Link, Hongtao Liu, Qi Liu, Richard L. Mackman, Michael L. Mitchell, Jay P. Parrish, Hyung-Jung Pyun, Joseph H. Saugier, Scott D. Schroeder, Jianyu Sun, James G. Taylor, James D. Trenkle, Winston C. Tse, Randall W. Vivian, William J. Watkins, Lianhong Xu
  • Publication number: 20140243382
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are 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. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Application
    Filed: May 12, 2014
    Publication date: August 28, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson