Patents Issued in April 8, 2014
  • Patent number: 8691795
    Abstract: A process for preparing an oligosaccharide derivative from an oligosaccharide mixture, the process being characterized in that the process comprises the steps of (a) introducing a lipophilic group into oligosaccharides of the mixture to obtain a mixture of oligosaccharide derivatives, and (b) treating the oligosaccharide derivative mixture by serotonin affinity column chromatography.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: April 8, 2014
    Assignee: Glytech, Inc.
    Inventors: Kazuaki Kakehi, Mitsuhiro Kinoshita, Yuki Matsuno
  • Patent number: 8691796
    Abstract: A pharmaceutical composition for inhibiting inflammation, comprising (a) hyaluronic acid, (b) a 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor, and (c) a pharmaceutically acceptable carrier, is provided. Also provided is a method for inhibiting inflammation in a mammal, comprising administrating to the mammal an effective amount of a composition comprising (a) hyaluronic acid and (b) an HMG-CoA reductase inhibitor.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: April 8, 2014
    Assignee: China Medical University
    Inventors: Feng-Huei Lin, Teng-Le Huang, Horng-Chaung Hsu
  • Patent number: 8691797
    Abstract: Disclosed is a method for chlorinating a carbohydrate or a derivative thereof to produce a polychlorinated carbohydrate or a derivative thereof, such as sucralose, the method involves (i) reacting the carbohydrate or derivative thereof with a chlorinating agent to obtain a reaction mixture comprising said polychlorinated carbohydrate or derivative thereof and at least one under-chlorinated carbohydrate or derivative thereof, (ii) returning the at least one under-chlorinated carbohydrate or derivative thereof to a chlorinating step and further chlorinating the at least one under-chlorinated carbohydrate or derivative thereof to obtain the desired polychlorinated carbohydrate or derivative thereof; and (iii) optionally repeating steps (i) and (ii) “n” times where n?1. The polychlorinated carbohydrate or a derivative thereof is obtained in high yields.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: April 8, 2014
    Assignee: Lexington Pharmaceuticals Laboratories, LLC
    Inventors: William Randal Erickson, Stephen Craig Fields
  • Patent number: 8691798
    Abstract: Disclosed herein are methods for synthesizing 2,4-pyrimidinediamines as well as intermediates used therein.
    Type: Grant
    Filed: June 7, 2013
    Date of Patent: April 8, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Ulfried Feifer, Karl-Heinz Giselbrecht, Michael Wolberg
  • Patent number: 8691799
    Abstract: The subject invention pertains to the treatment of tumors and cancerous tissues and the prevention of tumorigenesis and malignant transformation through the modulation of JAK/STAT3 intracellular signaling. The subject invention concerns pharmaceutical compositions containing cucurbitacin I, or a pharmaceutically acceptable salt or analog thereof. Another aspect of the invention concerns methods of inhibiting the growth of a tumor by administering a cucurbitacin I, or a pharmaceutically acceptable salt or analog thereof, to a patient, wherein the tumor is characterized by the constitutive activation of the JAK/STAT3 intracellular signaling pathway. The present invention further pertains to methods of moderating the JAK and/or STAT3 signaling pathways in vitro or in vivo using cucurbitacin I, or a pharmaceutically acceptable salt or analog thereof. Another aspect of the present invention concerns a method for screening candidate compounds for JAK and/or STAT3 inhibition and anti-tumor activity.
    Type: Grant
    Filed: August 15, 2011
    Date of Patent: April 8, 2014
    Assignee: University of South Florida
    Inventors: Said M. Sebti, Richard Jove
  • Patent number: 8691800
    Abstract: Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of Formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a quaternary amine thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof, wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; R2 is hydrogen, hydroxy, thio, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; R4 is hydrogen, alkyl or benzyl; R5 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R5 radicals may be taken together to form together with the phenyl ring to which they
    Type: Grant
    Filed: July 31, 2006
    Date of Patent: April 8, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Koenraad Jozef Lodewijk Marcel Andries, Anil Koul, Jérôme Emile Georges Guillemont, Elisabeth Thérèse Jeanne Pasquier
  • Patent number: 8691801
    Abstract: Manzamine compounds have been discovered to decrease cell dissociation and cell migration associated with the metastatic potential of cancer cells and a restoration of cancer cell susceptibility to agents, such as TRAIL, which can induce apoptosis. Specifically, Manzamine A has a formerly unrecognized utility in both blocking tumor cell invasion and tumor metastasis as well in restoring cancer cell susceptibility to standard chemotherapeutic agents which induce apoptosis and, therefore, has utility in treating cancer.
    Type: Grant
    Filed: July 17, 2012
    Date of Patent: April 8, 2014
    Assignee: Florida Atlantic University Board of Trustees
    Inventors: Esther A. Guzman, Jacob D. Johnson, Amy E. Wright
  • Patent number: 8691802
    Abstract: Citric acid and conjugate bases thereof are useful for stabilizing stabilized chlorine dioxide in the presence of therapeutically active agents and excipients in a composition. Ophthalmic compositions and methods related thereto are also disclosed herein.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: April 8, 2014
    Assignee: Allergan, Inc.
    Inventors: Robert T. Lyons, Robert S. Jordan
  • Patent number: 8691803
    Abstract: The present invention relates to a process for the preparation of carbapenem antibiotic compounds, which are useful for intravenous and intramuscular administration.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: April 8, 2014
    Assignee: Savior Lifetec Corporation
    Inventors: Wei-Hong Tseng, Wen-Hsin Chang, Shiuan-Ting Chuang
  • Patent number: 8691804
    Abstract: The invention relates to compounds of formula (I) wherein R, R0, R1, m, n and X1 to X4 have the meaning as cited in the description and the claims. These compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
    Type: Grant
    Filed: May 5, 2009
    Date of Patent: April 8, 2014
    Assignee: Evotec AG
    Inventors: Adam James Davenport, David James Hallett, Massimo Corsi
  • Patent number: 8691805
    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 Y, Z, R1, and s are defined herein.
    Type: Grant
    Filed: May 1, 2013
    Date of Patent: April 8, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Patent number: 8691806
    Abstract: The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
    Type: Grant
    Filed: June 28, 2012
    Date of Patent: April 8, 2014
    Assignees: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology Limited
    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
  • Patent number: 8691807
    Abstract: The present invention provides azetidinyl phenyl, pyridyl, or pyrazinyl carboxamide derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAKs) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: April 8, 2014
    Assignee: Incyte Corporation
    Inventors: Wenqing Yao, David M. Burns, Jincong Zhuo
  • Patent number: 8691808
    Abstract: The present disclosure provides compounds having affinity for the M2 proton channel, useful for the treatment of viral infections such as influenza, which are of the Formula (I): wherein R1, R2, and Y are as defined herein. Methods of preparing the compounds, pharmaceutical compositions containing the compounds, and methods of using the compounds in the treatment of viral infections such as influenza are also provided.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: April 8, 2014
    Assignee: Influmedix, Inc.
    Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
  • Patent number: 8691809
    Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.
    Type: Grant
    Filed: August 18, 2010
    Date of Patent: April 8, 2014
    Assignees: VentiRx Pharmaceuticals, Inc., Array BioPharma, Inc.
    Inventors: James Jeffry Howbert, Gregory Dietsch, Robert Hershberg, Laurence E. Burgess, Joseph P. Lyssikatos, Brad Newhouse, Hong Woon Yang
  • Patent number: 8691810
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, B, R1, R2, R3, R4a, R5, and Z are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: April 8, 2014
    Assignee: AbbVie Inc.
    Inventors: Michael R. Michaelides, Andrew S. Judd, Shannon R. Fix-Stenzel, Richard F. Clark, Bryan K. Sorensen, Zhiqin Ji
  • Patent number: 8691811
    Abstract: The present invention provides a compound of general formulae 5a-r, 9a-i to 13a-i and 17a-i to 22a-i, useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]benzodiazepine hybrids of general formulae 5a-r, 9a-i to 13a-i and 17a-i to 22a-i.
    Type: Grant
    Filed: July 13, 2009
    Date of Patent: April 8, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: Kamal Ahmed, Earla V. Bharathi, Dudekula Dastagiri, Jonnala S. Reddy, Arutla Viswanath
  • Patent number: 8691812
    Abstract: A composition comprising a carboxamide compound represented by following formula (I), wherein R1 represents a hydrogen atom or a methyl group, and R2 represents a methyl group, a difluoromethyl group or a trifiuoromethyl group, and one or more neonicotinoid compound selected from group (A) consisting of acetamiprid, clothianidin, dinotefuran, imidacloprid, nitenpyram thiacloprid and thiamethoxam possesses an excellent pesticidal effect.
    Type: Grant
    Filed: April 25, 2011
    Date of Patent: April 8, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Yuichi Matsuzaki
  • Patent number: 8691813
    Abstract: The present invention relates to novel indole and benzoxazine derivatives which are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”) and which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds and to the use of such compounds and compositions for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: April 8, 2014
    Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma SA
    Inventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez, Gregor James MacDonald
  • Patent number: 8691814
    Abstract: The present invention provides compounds having formula (I): wherein R1, R2, R3 and n are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of inflammatory or autoimmune and proliferative disorders and as inhibitors of cell adhesion molecule expression and inflammatory cytokine signal transduction generally.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: April 8, 2014
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Jane Daun, Heather A. Davis, Bruce DeCosta, Fabian Gusovsky, Ieharu Hishinuma, Yimin Jiang, Toshihiko Kaneko, Kouichi Kikuchi, Seiichi Kobayashi, André Lescarbeau, Xiang-Yi Li, Kenzo Muramoto, Norihito Ohi, Marc Pesant, Boris M. Seletsky, Motohiro Soejima, Mark Spyvee, Lynda Tremblay, Ye Yao, Hiromitsu Yokohama, Yan (Janet) Zhao, Wanjun Zheng
  • Patent number: 8691815
    Abstract: The invention relates to novel oxindol derivative of general formula (I), wherein substituents R1, R2, A, B and Y are such as defined in a claim 1. Drugs containing said derivatives and the use thereof for preventing and/or treating vassopress-and/or oxytocin-dependent-diseases are also disclosed.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: April 8, 2014
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Thorsten Oost, Wilfried Lubisch, Wilfried Hornberger, Liliane Unger, Andrea Hager-Wernet
  • Patent number: 8691816
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: April 8, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Patent number: 8691817
    Abstract: The present application relates to novel sulfonamide- or sulfoximine-substituted 1,4-diaryldihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: April 8, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig, Dirk Schneider
  • Patent number: 8691818
    Abstract: Compounds of general structure in which X and Y are each N or C with at least one of X and Y being N; Z is a single bond or an optionally substituted linking group R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when RI is hydrogen or ?NH when R1 is a substituent group; or N* is a group NRaRb where Ra and Rb are independently H or an alkyl group; or N* is an optionally substituted piperazinyl ring; and A is an optionally substituted heterocyclic or carbocyclic ring system which may be linked to the triazo/diazo ring through R2 to form a fused multicyclic ring; are indicated as suitable for treatment of disorders in mammals that are susceptible to sodium channel blockers and antifolates, and particularly disorders such epilepsy, multiple sclerosis, glaucoma and uevitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motorneurone disease, Alzheimer's disease, Parkinson's disease, chronic infl
    Type: Grant
    Filed: January 16, 2009
    Date of Patent: April 8, 2014
    Assignee: University Of Greenwich
    Inventors: Michael Leach, Laurence Harbige, Dieter Riddall, Karl Franzmann
  • Patent number: 8691819
    Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.
    Type: Grant
    Filed: October 14, 2009
    Date of Patent: April 8, 2014
    Assignee: PRISM BioLab Corporation
    Inventors: Hiroyuki Kouji, Yuji Kogami, Takenao Odagami
  • Patent number: 8691820
    Abstract: The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer.
    Type: Grant
    Filed: June 23, 2011
    Date of Patent: April 8, 2014
    Assignee: Curis, Inc.
    Inventors: Changgeng Qian, Xiong Cai, Haixiao Zhai
  • Patent number: 8691821
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: April 8, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Andrew P. Degnan, Hong Huang, Lawrence B. Snyder, Fukang Yang, Kevin W. Gillman, Michael F. Parker
  • Patent number: 8691822
    Abstract: Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed.
    Type: Grant
    Filed: September 14, 2010
    Date of Patent: April 8, 2014
    Assignees: Jiangsu Hengrui Medicine Co., Ltd., Shanghai Hengrui Pharmaceutical Co., Ltd.
    Inventors: Peng Cho Tang, Nong Zhang, Baolei Zhang, Weimin Wang, Hao Zheng, Lin Wu
  • Patent number: 8691823
    Abstract: The present invention features compounds of formula (I) for the treatment or prevention of HIV infection and for the treatment of AIDS and ARC.
    Type: Grant
    Filed: February 19, 2013
    Date of Patent: April 8, 2014
    Assignees: Shionogi & Co., Ltd., ViiV Healthcare Company
    Inventors: Brian A. Johns, Jason G. Weatherhead, Yasunori Aoyama, Hiroshi Yoshida, Yoshiyuki Taoda
  • Patent number: 8691824
    Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
    Type: Grant
    Filed: August 3, 2009
    Date of Patent: April 8, 2014
    Assignee: CHDI Foundation, Inc.
    Inventors: John Wityak, Leticia M. Toledo-Sherman, Celia Dominguez, Stephen Martin Courtney, Christopher John Yarnold, Paula C. De Aguiar Pena, Andreas Scheel, Dirk Winkler
  • Patent number: 8691825
    Abstract: The instant invention provides for substituted fused pyrimidine compounds of Formula A that inhibit Akt activity: In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: April 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Qi Chen, Mingxiang Cui, Bin Hu, Shuangxi Hu, Zhifa Pu, Philip E. Sanderson, Richard Soll, Xue Tang, Jiabing Wang, Yongjin Yan, Jinfeng Yao, Hongjie Zhang
  • Patent number: 8691826
    Abstract: Compounds of formula (I): are useful as inhibitors of human neutrophil elastase.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: April 8, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Toby Jonathan Blench, Christine Edwards, Robert Andrew Heald, Janusz Jozef Kulagowski, Jonathan Mark Sutton, Carmelida Capaldi
  • Patent number: 8691827
    Abstract: The present invention is directed to amino tetrahydro-pyridopyrimidine 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: Grant
    Filed: August 5, 2010
    Date of Patent: April 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, John D. Schreier
  • Patent number: 8691828
    Abstract: 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, or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
    Type: Grant
    Filed: March 4, 2010
    Date of Patent: April 8, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Yuya Oguro, Osamu Kurasawa
  • Patent number: 8691829
    Abstract: The invention provides methods to treat certain liver disorders by administering a compound that inhibits PD K isoforms, particularly the delta isoform. It further provides specific compounds useful for these methods and ways to identify subjects who are particularly suitable for receiving these treatments.
    Type: Grant
    Filed: July 21, 2010
    Date of Patent: April 8, 2014
    Assignee: Gilead Calistoga LLC
    Inventor: Roger G. Ulrich
  • Patent number: 8691830
    Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: April 8, 2014
    Assignee: G1 Therapeutics, Inc.
    Inventors: Francis X. Tavares, Jay C. Strum
  • Patent number: 8691831
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula I are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: April 8, 2014
    Assignees: Merck Sharp & Dohme Corp., Pharmacopeia Drug Discovery, Inc.
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voight, Corey O. Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, Jr., John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoxiang Liu, Tao Guo, Thuy X. E. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
  • Patent number: 8691832
    Abstract: The present invention is directed to novel tricyclic heterocycles of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: December 1, 2011
    Date of Patent: April 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Duane A. Burnett, Zhiqiang Zhao, David Cole, Hubert Josien, Dmitri A. Pissarnitski, Thavalakulamgar Sasikumar, Wen-Lian Wu, Martin Domalski
  • Patent number: 8691833
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: April 8, 2014
    Assignees: Merck Sharp & Dohme Corp., Pharmacopeia Inc.
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voight, Corey O. Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, Jr., John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoiang Liu, Tao Guo, Thuy X.E. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
  • Patent number: 8691834
    Abstract: The present invention relates to combinations of pyrimethanil, or a salt thereof, and a monoterpene, or a salt thereof, which provide an improved biocidal effect. More particularly, the present invention relates to compositions comprising a combination of pyrimethanil, or a salt thereof, together with a monoterpene selected from thymol and ?-thujaplicin in respective proportions to provide a synergistic biocidal effect. Compositions comprising these combinations are useful for the protection of any living or non-living material, such as crops, plants, fruits, seeds, objects made of wood, thatch or the like, engineering material, biodegradable material and textiles against deterioration due to the action of microorganisms such as bacteria, fungi, yeasts, algae, virusses, and the like.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: April 8, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Dany Leopold Jozefien Bylemans, Jan Pieter Hendrik Bosselaers
  • Patent number: 8691835
    Abstract: A composition is provided having the formula where R1 in each occurrence is independently H or a C1-C4 hydrocarbon; R3 is H, and R4 is a moiety capable of crossing the blood brain barrier selected from the group consisting of: an amino acid, a peptide, transferrin, gluconate, lactate, citrate, malate, fumarate, benzoate, salicylate, pyruvate and propionate. The composition includes 4-aminopyridine and a transporter species which allows for improved transport of the aminopyridine across the blood brain barrier thereby reducing systemic side effects of aminopyridine administration.
    Type: Grant
    Filed: January 24, 2011
    Date of Patent: April 8, 2014
    Inventor: Landon C. G. Miller
  • Patent number: 8691836
    Abstract: Provided are D2 or D3 antagonist compounds and pharmaceutical compositions of formula I and pharmaceutically acceptable salts thereof, or isomers thereof, wherein R1, R2 and R3 are as defined herein. The invention further comprises methods for making the compounds of the invention and methods for the treatment of conditions mediated by the dopamine D2 or D3 receptor from the compounds of the invention.
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: April 8, 2014
    Assignee: Altos Therapeutics, LLC
    Inventors: Gary W. Luehr, Arathi Sundaram, Priyadarshini Jaishankar, Philip W. Payne, Pascal Druzgala
  • Patent number: 8691837
    Abstract: Imidazo ring systems substituted at the 1-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: November 24, 2004
    Date of Patent: April 8, 2014
    Assignee: 3M Innovative Properties Company
    Inventors: Larry R. Krepski, Joseph F. Dellaria, Jr., Daniel E. Duffy, Matthew R. Radmer, David T. Amos
  • Patent number: 8691838
    Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds of Formula I, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: May 22, 2009
    Date of Patent: April 8, 2014
    Assignee: Amgen Inc.
    Inventors: Brian K. Albrecht, Steven Bellon, Christiane M. Bode, Alessandro Boezio, Deborah Choquette, Jean-Christophe Harmange
  • Patent number: 8691839
    Abstract: The present application relates generally to amino tetraline derivative compounds and methods of use, specifically, embodiments including compounds of formula (I) described herein, pharmaceutically acceptable salts and solvates. More specifically, this application relates to amino tetraline derivative compounds and uses of such compounds producing medicaments for the treatment of various disease and conditions including movement disorders and disorders of the central nervous system.
    Type: Grant
    Filed: August 15, 2013
    Date of Patent: April 8, 2014
    Inventors: Peter Gmeiner, Miriam Ruberg, Harald Huebner
  • Patent number: 8691840
    Abstract: The invention relates to N-biarylamides useful for the prophylaxis and/or treatment of impairments of perception, concentration, learning and/or memory, and to processes for preparing them, and pharmaceutical compositions containing them.
    Type: Grant
    Filed: September 19, 2011
    Date of Patent: April 8, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Timo Flessner, Frank-Gerhard Böss, Frank-Thorsten Hafner, Joachim Luithle, Christoph Methfessel, Leila Telan
  • Patent number: 8691841
    Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the ?7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: April 8, 2014
    Assignee: Memory Pharmaceuticals Corporation
    Inventors: Wenge Xie, Brian Herbert, Richard Schumacher, Truc Nguyen, Jianguo Ma, Carla Gauss, Ashok Tehim
  • Patent number: 8691842
    Abstract: The present invention provides a pharmaceutical composition for preventing or treating rheumatoid arthritis comprising rebamipide as an active ingredient and a pharmaceutically acceptable carrier. The pharmaceutical composition may be for oral administration, for example an oral solid dosage form of a tablet or capsule form. The pharmaceutical composition may be formulated into a unit dosage form suitable for orally administering rebamipide in a dose ranging from 0.5 to 50 mg/kg, preferably from 0.6 to 6 mg/kg.
    Type: Grant
    Filed: October 8, 2009
    Date of Patent: April 8, 2014
    Assignees: Catholic University Industry Academic Cooperation Foundation, Hanlim Pharmaceutical Co., Ltd.
    Inventors: Jun-Ki Min, Mi-La Cho, Yun-Ju Woo, Hye-Jwa Oh, Joo-Yeon Jhun, Geun-Hyeog Lee, Se-Wan Park, Jin-Ha Park, Eun-Young Kwak
  • Patent number: 8691843
    Abstract: The present invention provides a combination of antioxidants that effectively stabilize different types of fats utilized in a ruminant diet. When included in a ruminant feed ration or water source, the antioxidant combination typically increases nutrient digestion, such as fiber and protein, improves rumen fermentation, improves microbial growth, improves microbial efficiency, increases milk production and/or milk fat, improves antioxidant status of the ruminant, and attenuates the negative effects of some fats in the ruminant animal.
    Type: Grant
    Filed: February 14, 2007
    Date of Patent: April 8, 2014
    Assignee: Novus International, Inc.
    Inventors: Mercedes Vazquez-Anon, Gavin R. Bowman
  • Patent number: 8691844
    Abstract: A method for inhibiting coagulation including administering to a patient in need thereof a pharmaceutical composition containing 21-(S)-Argatroban and/or a pharmaceutically acceptable salt thereof. Compared with 21-(R)-Argatroban, 21-(S)-Argatroban significantly prolongs coagulation time of whole blood (CT), recalcification time (RT), kaolin partial thromboplastin time (APTT), pro-time prothrombin time (PT), thrombin time (TT), and reduces platelet adhesion rate and platelet aggregation rate in healthy dogs. Therefore, 21-(S)-Argatroban has a stronger effect for inhibiting coagulation and reducing therapeutically effective dose and is suitable for use in a method for treatment and/or prevention of thrombosis and inhibiting platelet aggregation.
    Type: Grant
    Filed: April 18, 2012
    Date of Patent: April 8, 2014
    Assignee: Tianjin Weijie Technology Co., Ltd.
    Inventor: Honghai Song