Nitrogen Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 514/426)
  • Patent number: 10259786
    Abstract: Novel amisulpride derivatives and pharmaceutical compositions thereof are disclosed. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may have better membrane permeability compared to amisulpride. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for antagonizing dopamine and/or serotonin (e.g., 5-HT2a) and/or ?2 receptor in a subject. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more conditions responsive to modulation of dopamine and/or serotonin (e.g., 5-HT2a) and/or ?2 receptor in a subject. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more disorders associated with an abnormality in levels of dopamine and/or serotonin in the brain.
    Type: Grant
    Filed: November 28, 2017
    Date of Patent: April 16, 2019
    Assignee: LB PHARMACEUTICALS INC.
    Inventors: Andrew R. Vaino, Vincent T. Grattan, Zachary Prensky
  • Patent number: 9827228
    Abstract: Disclosed is an in vitro screening method for identifying an antagonist-to-agonist allosteric modifier of a mu-opioid receptor and an in vivo method for confirming that a test compound is such a modifier of a mu-opioid receptor. Also disclosed is a method for treating an opioid receptor-associated condition using a compound of Formula (I) and a pharmaceutical composition containing the same.
    Type: Grant
    Filed: July 12, 2016
    Date of Patent: November 28, 2017
    Assignees: National Health Research Institutes, Regents of the University of Minnesota
    Inventors: Shau-Hua Ueng, Shiu-Hwa Yeh, Horace Loh, Yu-Sheng Chao
  • Patent number: 9604949
    Abstract: Prostaglandin conjugates and derivatives and methods for their use to treat glaucoma and/or lower intraocular pressure are disclosed. Additionally, ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma and elevated intraocular pressure are disclosed. Such compositions comprise an effective amount of prostaglandin conjugates or derivatives of the present invention.
    Type: Grant
    Filed: October 15, 2015
    Date of Patent: March 28, 2017
    Assignee: Novartis AG
    Inventors: David Archer Ellis, Lukas Scheibler, Najam A. Sharif
  • Patent number: 9550749
    Abstract: An object of the present invention is to provide a novel endoparasite control agent as a parasiticide, an antiprotozoal or the like. Provided is an endoparasite control agent comprising a carboxamide derivative represented by the general formula (I): or a salt thereof as an active ingredient.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: January 24, 2017
    Assignees: The University of Tokyo, Nihon Nohyaku Co., Ltd.
    Inventors: Kiyoshi Kita, Akiyuki Suwa, Masatsugu Oda, Koji Tanaka
  • Patent number: 9346786
    Abstract: The present application relates to compounds of formula wherein R1, R2, R3, R4, and n are defined herein or to a pharmaceutically active salt thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: May 24, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Andreas Koblet, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • Patent number: 9226916
    Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: January 5, 2016
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Henner Knust, Andreas Koblet, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • Patent number: 9150558
    Abstract: The invention relates to the design and synthesis of novel anabaseine-based compounds, which are useful in treating or preventing a wide variety of conditions, including nervous system diseases or disorders, such as, schizophrenia, Alzheimer's disease, Parkinson's disease, drug dependence, and substance addiction, and compositions, kits, and methods thereof. The invention also provides novel anabaseine-based compounds, compositions, kits, and methods thereof for treating or preventing non-nerve system diseases or disorders (such as, inflammation and cancer) in a subject identified in need thereof. Certain enantiomeric compounds of the invention exhibited enhanced selectivity toward ?7 nAChRs relative to alpha4beta2 nAChRs. Other enantiomeric compounds of the invention exhibited enhanced selectivity for alpha4beta2 nAChRs relative to ?7 nAChRs.
    Type: Grant
    Filed: December 11, 2012
    Date of Patent: October 6, 2015
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: William R. Kem, Ferenc Soti, Hong Xing
  • Publication number: 20150119396
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: April 30, 2015
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • Patent number: 9000190
    Abstract: The present invention provides a new amide compound and salt thereof that is capable of inhibiting biofilm formation or removing deposited biofilms. The present invention also provides a biofilm formation inhibitor or a biofilm remover containing the amide compound or salt thereof as an active ingredient. An amide compound or salt thereof according to the present invention is denoted by General Formula (1): wherein R1 is a hydrogen atom or a hydroxyl group, R2 is a C5-12 alkyl group, and Q is a substituent denoted by Formula (Q1) or (Q2), wherein n and m are 0 or 1.
    Type: Grant
    Filed: April 29, 2014
    Date of Patent: April 7, 2015
    Assignees: University of Tokyo, Otsuka Chemical Co., Ltd.
    Inventors: Hiroaki Suga, Jun Igarashi
  • Publication number: 20150025042
    Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: December 16, 2013
    Publication date: January 22, 2015
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Shoujun Chen, Keizo Koya, Zachary Demko, Lijun Sun
  • Publication number: 20150025054
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: January 22, 2015
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estirate Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Lar
  • Publication number: 20140341986
    Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
    Type: Application
    Filed: August 4, 2014
    Publication date: November 20, 2014
    Inventors: Alain D. Baron, Mark S. Fineman, Nigel R.A. Beeley
  • Patent number: 8889736
    Abstract: Formulations and methods are provided for the treatment of pain, and neuropathic pain in particular. The formulations are eutectic mixtures of a capsaicinoid and a local anesthetic agent and/or an anti-pruritic agent.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: November 18, 2014
    Assignee: Acorda Therapeutics, Inc.
    Inventor: Manoj Maniar
  • Publication number: 20140336158
    Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
    Type: Application
    Filed: July 25, 2014
    Publication date: November 13, 2014
    Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
  • Patent number: 8883852
    Abstract: Provided herein are methods, for reducing, preventing, mitigating and treating damage caused by radiation. The methods comprise delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation or to mitigate apoptosis. The compounds comprise glyburide or other sulfonylurea hypoglycemic compounds or potassium channel inhibitors.
    Type: Grant
    Filed: October 21, 2009
    Date of Patent: November 11, 2014
    Assignee: University of Pittburgh—Of the Commonwealth System of Higher Education
    Inventors: Michael Epperly, Joel Greenberger, Jianfei Jiang, Valerian Kagan, John Lazo, Peter McDonald
  • Publication number: 20140329871
    Abstract: The present invention provides compounds having the general structural Formula (I): and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis or dysproliferation.
    Type: Application
    Filed: December 2, 2012
    Publication date: November 6, 2014
    Applicant: ANGION BIOMEDICA CORP.
    Inventors: Rama K. Mishira, Bijoy Panicker, James G. Tarrant, Dong Sung Lim, Lambertus J.W.M. Oehlen, Dawoon Jung
  • Publication number: 20140329833
    Abstract: The invention relates to methods and compositions for the treatment or prevention of inflammation and inflammatory diseases or conditions. In particular, the invention relates to an LSD1 inhibitor, such as a 2-cyclylcylopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing inflammation and inflammatory diseases or conditions.
    Type: Application
    Filed: May 21, 2012
    Publication date: November 6, 2014
    Applicant: ORYZON GENOMICS, S.A
    Inventors: Tamara Maes, Marc Martinell Pedemonte, Julio Castro-Palomino Laria
  • Publication number: 20140296255
    Abstract: The invention relates to methods and compositions for the treatment or prevention of thrombosis, thrombus formation, a thrombotic event or complication, or a cardiovascular disease or event. In particular, the invention relates to an LSD inhibitor such as a 2-cyclylcyclopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing thrombosis, thrombus formation, a thrombotic event or complication, or a cardiovascular disease or event.
    Type: Application
    Filed: May 21, 2012
    Publication date: October 2, 2014
    Applicant: ORYZONG GENOMICS, S.A.
    Inventors: Tamara Maes, Marc Martinell Pedemonte
  • Patent number: 8846742
    Abstract: The present invention relates to compounds that may be used to inhibit activation of protein kinase G (“PKG”). It is based, at least in part, on the discovery of the tertiary structure of PKG and the identification of molecules that either bind to the active site of PKG and/or are analogs of balanol.
    Type: Grant
    Filed: February 14, 2007
    Date of Patent: September 30, 2014
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Richard Ambron, Ying-Ju Sung, Jeremy Greenwood, Leah Frye, Shi-Xian Deng, Yuli Xie, Donald W. Landry
  • Publication number: 20140288065
    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: Application
    Filed: June 10, 2014
    Publication date: September 25, 2014
    Applicant: 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
  • Patent number: 8835480
    Abstract: The present invention relates to polyamides capable of inhibiting ARE-, GRE- and ERE-mediated gene regulation in cells. The invention also relates to methods to treat diseases related to ARE-, GRE- and ERE-mediated gene regulation.
    Type: Grant
    Filed: April 22, 2008
    Date of Patent: September 16, 2014
    Assignee: California Institute of Technology
    Inventors: Peter B. Dervan, Nicholas G. Nickols
  • Publication number: 20140256729
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.
    Type: Application
    Filed: October 22, 2012
    Publication date: September 11, 2014
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Laria
  • 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
  • Patent number: 8802719
    Abstract: Methods of preparing (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid are disclosed. Also provided are pharmaceutical compositions comprising (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, and methods of treatment using such compositions.
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: August 12, 2014
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Anantha Sudhakar, Tamilarasan Subramani, Mohamed Shiek Mohamed Mujeebur Rahuman, Ramar Subbiah
  • Patent number: 8778628
    Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: July 15, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Okabe, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • Patent number: 8759387
    Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: June 24, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Okabe, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • Publication number: 20140163041
    Abstract: The present invention relates to methods and compositions for the treatment or prevention of diseases and disorder associated with myeloproliferative and lymphoproliferative disorders. In particular, the invention relates to an LSD1 inhibitor for use in treating or preventing diseases and disorder associated with myeloproliferative and lymphoproliferative disorders.
    Type: Application
    Filed: February 8, 2012
    Publication date: June 12, 2014
    Applicant: ORYZON GENOMICS S.A.
    Inventors: Matthew Colin Thor Fyfe, Tamara Maes, Marc Martinell Pedemonte
  • Patent number: 8710049
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.
    Type: Grant
    Filed: July 16, 2012
    Date of Patent: April 29, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu
  • Patent number: 8703721
    Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: April 22, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • Publication number: 20140080770
    Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 17, 2013
    Publication date: March 20, 2014
    Applicant: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi MIYAZAKI, Junko OKABE, Kosuke YASUDA, Iwao TAKAMURO, Osamu SAKURAI, Tetsuya YANAGIDA, Yutaka HISADA
  • Publication number: 20140080833
    Abstract: Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.
    Type: Application
    Filed: November 11, 2013
    Publication date: March 20, 2014
    Applicant: MannKind Corporation
    Inventors: Gary A. Flynn, Sandra A. Lee, Mary Faris, David W. Brandt, Subrata Chakravarty
  • Publication number: 20140045910
    Abstract: Novel amino-pyrrolinic derivatives, their pharmacologically acceptable salts and use thereof in the prevention and/or treatment of metabolic syndrome.
    Type: Application
    Filed: April 17, 2012
    Publication date: February 13, 2014
    Applicant: UNIVERSITE DE STRASBOURG
    Inventors: Pascal Bousquet, Jean Daniel Ehrhardt, Lyne Fellmann, Vincent Gasparik, Hugues Greney, Mohamed Hadjeri, Andre Mann, Nathalie Niederhoffer, Stephan Schann
  • Patent number: 8604021
    Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.
    Type: Grant
    Filed: May 10, 2011
    Date of Patent: December 10, 2013
    Inventors: Oren Becker, Rosa Melendez, Yael Marantz, Anurag Sharadendu, Merav Fichman, Mercedes Lobera, Hanoch Senderowitz, Srinivasa Rao Cheruku, Sharon Shacham, Laurence Wu, Ashis Saha, Pini Orbach, Dale S. Dhanoa
  • Publication number: 20130310379
    Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
    Type: Application
    Filed: November 21, 2011
    Publication date: November 21, 2013
    Applicant: CONSTELLATION PHARMACEUTICALS
    Inventors: Brian K. Albrecht, James Edmund Audia, Alexandre Gagnon, Jean-Christophe Harmange, Christopher G. Naveschuk
  • Publication number: 20130274267
    Abstract: The present invention relates to the use of potent selective LSD1 inhibitors and LSD1/MAO-B iithibitors for treating or preventing viral infections. Furthermore, the present invention relates to the new use of cyclopropylamine acetamide derivatives or cyclopropylamine derivatives, as defmed herein, for treating or preventing viral infection and treating or preventing reacti - vation of a virus after latency.
    Type: Application
    Filed: February 24, 2011
    Publication date: October 17, 2013
    Inventors: Julio Cesar Castro Palomino Laria, Alberto Ortega Munoz, Nathalie Guibourt, Jonathan Alleman Baker
  • Publication number: 20130231332
    Abstract: The present invention relates to compositions and methods for the treatment of infection by enveloped viruses, such as Ebola and Lassa fever viruses.
    Type: Application
    Filed: September 1, 2011
    Publication date: September 5, 2013
    Inventors: James Cunningham, Kyungae Lee, Tao Ren, Kartik Chandran
  • Patent number: 8497383
    Abstract: Compounds of Formula (I) are disclosed; wherein XA, k, A, B, R3A, R3B, R4 and R5 are defined herein. The compounds of Formula (I) are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: July 30, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, M. Katharine Holloway, Joseph P. Vacca
  • Patent number: 8497282
    Abstract: Methods of preparing (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid are disclosed. Also provided are pharmaceutical compositions comprising (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, and methods of treatment using such compositions.
    Type: Grant
    Filed: December 30, 2009
    Date of Patent: July 30, 2013
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Anantha Sudhakar, Tamilarasan Subramani, Mohamed Sheik Mohamed Mujeebur Rahuman, Ramar Subbiah
  • Patent number: 8492111
    Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
    Type: Grant
    Filed: May 7, 2010
    Date of Patent: July 23, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakural, Tetsuya Yanagida, Yataka Hisada
  • Publication number: 20130184262
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.
    Type: Application
    Filed: July 16, 2012
    Publication date: July 18, 2013
    Inventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu
  • Patent number: 8466182
    Abstract: The present invention relates to compounds of Formula I below and their tautomers or pharmaceutically acceptable salts, compositions and methods of uses thereof.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: June 18, 2013
    Assignees: The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone, University of Maryland, Baltimore
    Inventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
  • Publication number: 20130150374
    Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
    Type: Application
    Filed: December 17, 2012
    Publication date: June 13, 2013
    Applicant: Mitsubishi Tanabe Pharma Corporation
    Inventor: Mitsubishi Tanabe Pharma Corporation
  • Patent number: 8450345
    Abstract: Provided are methods of treating or preventing viral infections caused by or associated with a Dengue virus using iminosugars.
    Type: Grant
    Filed: February 22, 2010
    Date of Patent: May 28, 2013
    Assignees: The Chancellor, Masters and Scholars of the University of Oxford, United Therapeutics Corporation
    Inventors: Urban Ramstedt, Brennan Klose, Nicole Zitzmann, Raymond A. Dwek, Terry D. Butters
  • Patent number: 8410150
    Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: April 2, 2013
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
  • Patent number: 8404738
    Abstract: The present invention provides compounds of formula or pharmaceutically acceptable salts, esters or stereoisomers thereof, wherein R1 to R4, A and Y have the meanings given herein, as well as methods for making those compounds and their use as medicament, in particular as medicament for the treatment of cancer.
    Type: Grant
    Filed: January 17, 2012
    Date of Patent: March 26, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Jason Christopher Wong, Zhenshan Zhang
  • Patent number: 8383668
    Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, of the general formula I. Their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: February 26, 2013
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Soren Ebdrup, Henrik Sune Andersen
  • Publication number: 20130035325
    Abstract: Methods of inhibiting kinases using kinase inhibitors having olefin moieties are disclosed.
    Type: Application
    Filed: November 16, 2010
    Publication date: February 7, 2013
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: John William Taunton, JR., Rebecca Maglathlin, Iana Serafimova, Michael S. Cohen, Rand Miller, Ville Paavilainen, Jesse McFarland, Shyam Krishnan
  • Patent number: 8362003
    Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: January 29, 2013
    Assignee: Incyte Corporation
    Inventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taisheng Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
  • Patent number: 8362274
    Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.
    Type: Grant
    Filed: May 27, 2005
    Date of Patent: January 29, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
  • Publication number: 20130023503
    Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
    Type: Application
    Filed: September 24, 2012
    Publication date: January 24, 2013
    Applicant: OPKO Health, Inc.
    Inventor: OPKO Health, Inc.