Plural Isoquinoline Ring Systems Attached Directly Or Indirectly To Each Other By Nonionic Bonding Patents (Class 514/308)
  • Patent number: 11074737
    Abstract: A system including a non-transitory computer readable medium configured to store instructions thereon; and a processor. The processor is configured to execute the instructions for defining a virtual space associated with a first user, wherein the virtual space comprises a first region and a first avatar. The processor is configured to execute the instructions for causing the first avatar to enter the first region based on received first input; and moving the first avatar within the first region in response to a received second input. The processor is configured to execute the instructions for registering charging information the received second input; and removing the first avatar from the first region in response to a received third input. The processor is configured to execute the instructions for performing charging-related processing, in accordance with the registered charging information, in response to removing the first avatar from the first region.
    Type: Grant
    Filed: April 16, 2020
    Date of Patent: July 27, 2021
    Assignee: COLOPL, INC.
    Inventor: Kento Nakashima
  • Patent number: 10618885
    Abstract: One embodiment provides a compound of Formula I that activates autophagy, a pharmaceutical composition and use thereof:
    Type: Grant
    Filed: January 3, 2018
    Date of Patent: April 14, 2020
    Inventors: Zhi-Hong Jiang, Li-Ping Bai, Xiaobo Zhou, Kam Wai Vincent Wong, Zhiyuan Zheng, Yuen Kwan Betty Law
  • Patent number: 10376498
    Abstract: Method for treating a viral infection in a patient, comprising administering to the patient a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt thereof, comprising a moiety represented by figure (I), wherein R1 is a saturated or unsaturated bivalent hydrocarbon group. Viruses subject to treatment can include HIV and flaviviruses such as west nile, dengue, or hepatitis C virus. Compositions and methods of isolation and purification are also described including from the Red Sea sponge.
    Type: Grant
    Filed: October 29, 2015
    Date of Patent: August 13, 2019
    Assignee: King Abdullah University of Science and Technology
    Inventors: Christian R. Voolstra, Aubrie O'Rourke, Stephan Kremb
  • Patent number: 10259798
    Abstract: The present invention relates to a method for preparing magnesium lithospermate B. The method is characterized in that: magnesium lithospermate B is extracted or purified from a Salvia miltiorrhiza plant material or a Salvia miltiorrhiza extract in the presence of an added magnesium salt. The present invention also relates to a high-purity magnesium lithospermate B product prepared by the method of the present invention, wherein the content of magnesium lithospermate B is more than 95% by weight.
    Type: Grant
    Filed: February 9, 2015
    Date of Patent: April 16, 2019
    Assignees: SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES, SHANGHAI GREEN VALLEY PHARMACEUTICAL CO., LTD.
    Inventors: Lijiang Xuan, Yiping Wang, Weibin Song, Chunguang Chen, Dingxiang Li, Xiaoyu Zhou, Yunlong Gu, Liang Hu, Jing Zhao, Wenwei Xu, Shumei Wang
  • Patent number: 9675608
    Abstract: The present invention discloses a method of treating cancer and/or multidrug-resistant cancer, comprising administering an effective amount of hernandezine or thalidezine. A pharmaceutical composition comprising hernandezine or thalidezine admixed with a pharmaceutical carrier for treating cancers and/or multidrug-resistant cancer is also disclosed.
    Type: Grant
    Filed: October 28, 2015
    Date of Patent: June 13, 2017
    Assignee: Macau University of Science and Technology
    Inventors: Kam Wai Wong, Yuen Kwan Law, Liang Liu
  • Patent number: 9670181
    Abstract: The invention relates to compounds of the formula wherein R?, R1 through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
    Type: Grant
    Filed: June 25, 2014
    Date of Patent: June 6, 2017
    Assignees: ALLERGAN, INC., EXONHIT THERAPEUTICS SA
    Inventors: Bertrand Leblond, Cedric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Desire, Matthew P. Pando, John E. Donello, Rong Yang
  • Patent number: 9499518
    Abstract: Provided are methods for using bis-quaternary ammonium compounds to treat inflammatory pain, neuropathic pain and nociceptive pain.
    Type: Grant
    Filed: September 13, 2010
    Date of Patent: November 22, 2016
    Assignees: University of Kentucky Research Foundation, University of Utah
    Inventors: Joseph R. Holtman, Peter A. Crooks, Linda P. Dwoskin, J. Michael McIntosh, Elzbieta Pogonowska Wala
  • Patent number: 9345257
    Abstract: Enhancing the bioavailability of a drug or dietary supplement by administering it concurrently with one or more members of the d-tetrandrine family.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: May 24, 2016
    Assignee: CBA Pharma, Inc.
    Inventor: Daryl L. Barnett
  • Patent number: 9169268
    Abstract: The present invention provides a method of preventing, alleviating and/or treating depression, comprising the step of administering to a subject in need thereof a therapeutically effective amount of a 7-alkoxy fangchinoline compound or a pharmaceutically acceptable derivative thereof.
    Type: Grant
    Filed: October 6, 2014
    Date of Patent: October 27, 2015
    Assignee: Peking University
    Inventors: Yonghe Zhang, Xueqiong Zhang, Zhaofu Sheng
  • Patent number: 9133158
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, A1, A2, A3, A4, A5 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful, for example, as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: September 15, 2015
    Assignee: HOFFMAN-LA ROCHE INC.
    Inventors: Johannes Aebi, Kurt Amrein, Wenming Chen, Benoit Hornsperger, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Xuefei Tan, Zhanguo Wang, Mingwei Zhou
  • Patent number: 9119847
    Abstract: The present invention discloses a method of treating neurodegenerative disorder comprising administering an effective amount of an alkaloid which is a bisbenzylisoquinline alkaloid isolated from the traditional Chinese medicinal herb Nelumbo nucifera. The pharmaceutical composition thereof for treating Huntington's disease is also disclosed.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: September 1, 2015
    Assignee: Macau University of Science and Technology
    Inventors: Yuen Kwan Law, Kam Wai Wong, Liang Liu
  • Publication number: 20150133492
    Abstract: This invention is directed to the use of N-desmethyldauricine, a novel autophagy enhancer, in treating cancers or neurodegenerative conditions.
    Type: Application
    Filed: October 29, 2014
    Publication date: May 14, 2015
    Inventors: Kam Wai WONG, Yuen Kwan LAW, Zhi Hong JIANG, Liang LIU, Wai Kit CHAN, Xiao Jun YAO
  • Publication number: 20150133427
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: October 15, 2014
    Publication date: May 14, 2015
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
  • Patent number: 8940774
    Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and/or gastrointestinal tract disorders.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: January 27, 2015
    Inventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
  • Publication number: 20150018352
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: March 7, 2013
    Publication date: January 15, 2015
    Inventors: Thomas Dineen, Charles Kreiman, Matthew Weiss, Stephanie Geuns-Meyer
  • Publication number: 20150004134
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention.
    Type: Application
    Filed: December 3, 2013
    Publication date: January 1, 2015
    Applicant: CALITHERA BIOSCIENCES, INC.
    Inventors: Mark K. Bennett, Matthew I. Gross, Susan D. Bromley, Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren
  • Publication number: 20140309253
    Abstract: The invention relates to compounds of the formula wherein R?, R1 through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
    Type: Application
    Filed: June 25, 2014
    Publication date: October 16, 2014
    Inventors: Bertrand Leblond, Cedric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Desire, Matthew P. Pando, John E. Donello, Rong Yang
  • Publication number: 20140275061
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 18, 2014
    Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, James R. Corte, Shefali Srivastava
  • Publication number: 20140275157
    Abstract: Enhancing the cellular uptake of a drug or dietary supplement by administering it concurrently with one or more members of the d-tetrandrine family.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: CBA Pharma, Inc.
    Inventor: Daryl L. Barnett
  • Publication number: 20140228343
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: August 14, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
  • Publication number: 20140221345
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: August 7, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
  • Patent number: 8772316
    Abstract: The invention relates to compounds of the formula wherein R?, R1, through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
    Type: Grant
    Filed: February 17, 2012
    Date of Patent: July 8, 2014
    Assignees: Allergan, Inc., Exonhit Therapeutics SA
    Inventors: Bertrand Leblond, John E. Donello, Cédric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Désiré, Matthew P. Pando, Rong Yang
  • Patent number: 8703803
    Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: April 22, 2014
    Inventors: Peter A. Crooks, Linda P. Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
  • Publication number: 20140080866
    Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and/or gastrointestinal tract disorders.
    Type: Application
    Filed: November 26, 2013
    Publication date: March 20, 2014
    Applicant: University of Kentucky Research Foundation
    Inventors: Peter Crooks, Linda DWOSKIN, Roger Papke, Guangrong ZHENG, Sangeetha SUMITHRAN
  • Publication number: 20140073591
    Abstract: Multidrug resistance reversers of the d-tetrandrine family are used in conjunction with penicillins and other principle drugs used to treat MRSA.
    Type: Application
    Filed: September 12, 2013
    Publication date: March 13, 2014
    Applicant: CBA Pharma, Inc.
    Inventors: Wayne Michael Putnam, Beth D. Gudeman
  • Publication number: 20140045872
    Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.
    Type: Application
    Filed: September 14, 2011
    Publication date: February 13, 2014
    Applicant: NOVARTIS AG
    Inventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Henrik Moebitz, Saumitra Sengupta
  • Publication number: 20140011836
    Abstract: Provided are methods for using bis-quaternary ammonium compounds to treat inflammatory pain, neuropathic pain and nociceptive pain.
    Type: Application
    Filed: September 6, 2013
    Publication date: January 9, 2014
    Applicant: University of Kentucky Research Foundation
    Inventors: Joseph R. HOLTMAN, Peter Anthony CROOKS, Linda P. DWOSKIN, J. Michael MCINTOSH, Elzbieta Pogonowska WALA
  • Patent number: 8623877
    Abstract: The present disclosure relates to a series of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I). wherein R, R1, R2, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: January 7, 2014
    Assignee: Sanofi
    Inventors: Zhongli Gao, Ryan Hartung
  • Patent number: 8592451
    Abstract: The invention provides neuromuscular blockade agents of the non-depolarizing type with few if any circulatory effects. Compounds of the invention include bis(isoquinolylalkanol) diesters of fumaric, maleic, succinic, and acetylenedicarboxylic acids; compositions suitable for parenteral administration of these compounds as a surgical adjunct to anesthesia, and methods of preparation of the compounds. Compounds of the invention can produce neuromuscular blockade of short or intermediate duration, which for various compounds can be reversed by administration of a thiol compound such as L-cysteine, D-cysteine or glutathione. For various compounds of the invention, the neuromuscular blockade effect can be reversed quickly, efficiently, and without notable side-effects.
    Type: Grant
    Filed: March 17, 2010
    Date of Patent: November 26, 2013
    Assignee: Cornell University
    Inventor: John J. Savarese
  • Publication number: 20130296333
    Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).
    Type: Application
    Filed: July 9, 2013
    Publication date: November 7, 2013
    Inventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
  • Publication number: 20130289027
    Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).
    Type: Application
    Filed: January 23, 2012
    Publication date: October 31, 2013
    Applicant: ViiV Healthcare UK Limited
    Inventors: Martha Alicia De La Rosa, Simon Haydar, Brian Alvin Johns, Emile Johann Velthuisen
  • Patent number: 8557812
    Abstract: The invention relates to small molecules which function as inhibitors of anti-apoptotic Bcl-2 family member proteins (e.g., Bcl-2 and Bcl-xL). The invention also relates to the use of these compounds for inducing apoptotic cell death and sensitizing cells to the induction of apoptotic cell death.
    Type: Grant
    Filed: August 22, 2005
    Date of Patent: October 15, 2013
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Guoping Wang, Guozhi Tang, Renxiao Wang, Zaneta Nikolovska-Coleska, Dajun Yang, Liang Xu
  • Publication number: 20130231366
    Abstract: This application provides a method for the use of select quaternary ammonium antagonists to alpha-7 nAChR for the treatment of cancer and HIV and AIDS.
    Type: Application
    Filed: February 20, 2013
    Publication date: September 5, 2013
    Applicant: UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION
    Inventors: Roger L. PAPKE, Peter A. CROOKS, Linda P. DWOSKIN, Gretchen Lopez HERNANDEZ, Zhenfa ZHANG, Jeffrey S. THINSCHMIDT, Guangrong ZHENG
  • Patent number: 8513280
    Abstract: The present invention is about the use of at least one epothilone or derivative thereof as an active ingredient for manufacturing a medicament for use in the treatment of disease(s) involving a neuronal connectivity defect.
    Type: Grant
    Filed: September 9, 2010
    Date of Patent: August 20, 2013
    Assignees: Institut National de la Sante et de la Recherche Medicale, Commissariat a l'Energie Atomique, Gesellschaft fur Biotechnologische Forschung mbH (GBF)
    Inventors: Annie Andrieux, Didier Job, Annie Schweitzer, Gerhard Höfle
  • Patent number: 8507491
    Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).
    Type: Grant
    Filed: August 24, 2009
    Date of Patent: August 13, 2013
    Assignee: IRM LLC
    Inventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
  • Publication number: 20130203709
    Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.
    Type: Application
    Filed: August 9, 2011
    Publication date: August 8, 2013
    Applicants: THE PENN STATE RESEARCH FOUNDATION, UNIVERSITY OF SOUTH FLORIDA
    Inventors: Roman Manetsch, Sameer Kulkarni, Iredia D. Iyamu, Hong-Gang Wang, Kenichiro Doi, Wayne Guida, Daniel Santiago, Courtney du Boulay
  • Publication number: 20130158068
    Abstract: The present invention relates to a novel dicarboximide derivative of berbamine represented by formula I, including, but not limited to, a phthalimide derivative of berbamine and an aromatic heterocyclic dicarboximide derivative of berbamine, or a pharmaceutically acceptable salt thereof, to a process for preparation of the same, to a pharmaceutical composition comprising said compound and to use thereof in manufacture of an antitumor medicament.
    Type: Application
    Filed: August 25, 2011
    Publication date: June 20, 2013
    Applicant: HANGZHOU BENSHENG PHARMACEUTICAL CO., LTD.
    Inventors: Rongzhen Xu, Frank Rong, Fuwen Xie, Hongxi Lai
  • Publication number: 20130116276
    Abstract: The present invention reveals a new use of neferine. Neferine regulates M8 and V1 subtype of transient receptor potential ion channel (TRPM8 and TRPV1), respectively, in mammalians, including humans, and can be used for preparing medicaments for treating disease related to said ion channel (such as hyperalgesia, Parkinson's disease, painful bladder syndrome, chronic obstructive pulmonary disease, and tumor of skin, prostate, mammary gland, lung, colon, etc). The potency of neferine in the present invention is higher than that of hexahydrothymol.
    Type: Application
    Filed: April 13, 2010
    Publication date: May 9, 2013
    Applicant: Institute of Chinese Materia Medica, Chinese Academy of Medical Sciences
    Inventors: Tingliang Jiang, Feng Sui, Hairu Huo, Lanfang Li, Shuying Guo
  • Publication number: 20130059838
    Abstract: The present disclosure relates to a series of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I). wherein R, R1, R2, X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.
    Type: Application
    Filed: November 6, 2012
    Publication date: March 7, 2013
    Applicant: SANOFI
    Inventor: Sanofi
  • Patent number: 8362020
    Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: January 29, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
  • Patent number: 8357805
    Abstract: The present invention provides an improved method for obtaining cisatracurium besylate, which preferably chromatographically separating cisatracurium besylate from a mixture of (1R,1?R)-atracurium isomers via flash chromatography.
    Type: Grant
    Filed: March 5, 2008
    Date of Patent: January 22, 2013
    Assignee: CHEMAGIS Ltd.
    Inventors: Oded Arad, Elena Ostrovsky
  • Patent number: 8338455
    Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as VEGF mediated diseases. The invention encompasses novel compounds, 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: December 19, 2007
    Date of Patent: December 25, 2012
    Assignee: Amgen Inc.
    Inventors: Yuan Cheng, Deborah Choquette, Jean-Christophe Harmange, Andrew Tasker
  • Patent number: 8299253
    Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: October 30, 2012
    Assignee: University of Kentucky Research Foundation
    Inventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha P Sumithran
  • Publication number: 20120263670
    Abstract: The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.
    Type: Application
    Filed: June 29, 2011
    Publication date: October 18, 2012
    Applicant: Ardelyx, Inc.
    Inventors: Dominique Charmot, Jeffrey W. Jacobs, Michael Robert Leadbetter, Marc Navre, Christopher Carreras, Noah Bell
  • Publication number: 20120258957
    Abstract: The present invention relates to a heterocyclic derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders or diseases influenced by modulation of orexins, such as sleep disorders.
    Type: Application
    Filed: November 22, 2010
    Publication date: October 11, 2012
    Inventors: Matilda Jane Bingham, Andrew Dunbar, Margaret Jean Laats, Grant Wishart
  • Patent number: 8263607
    Abstract: Provided is a compound useful as an N-type Ca2+ channel blocker. As a result of intensive studies of compounds having an action of blocking N-type Ca2+ channels, the present inventors found that a tetrahydroisoquinoline compound of the present invention having a substituent at the 1-position has an action of blocking the N-type Ca2+ channels, an antinociceptive pain action, an antineuropathic pain action, an abdominal pain-inhibitory action and an opioid-induced constipation-improving action, and the present invention has been completed based on these findings.
    Type: Grant
    Filed: May 20, 2008
    Date of Patent: September 11, 2012
    Assignee: Astellas Pharma Inc.
    Inventors: Jun-ichi Shishikura, Makoto Inoue, Takashi Ogiyama, Koichi Yonezawa, Susumu Yamaki, Kazuhiro Yokoyama, Shuichirou Kakimoto, Hidetsugu Okada
  • Publication number: 20120214837
    Abstract: The invention relates to compounds of the formula wherein R?, R1, through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 23, 2012
    Applicants: ExonHit Therapeutics SA, ALLERGAN, INC.
    Inventors: Bertrand Leblond, Cédric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Désiré, Matthew P. Pando, John E. Donello, Rong Yang
  • Publication number: 20120108629
    Abstract: The present invention reveals a new use of neferine. Neferine regulates M8 and V1 subtype of transient receptor potential ion channel (TRPM8 and TRPV1), respectively, in mammalians, including humans, and can be used for preparing medicaments for treating disease related to said ion channel (such as hyperalgesia, Parkinson's disease, painful bladder syndrome, chronic obstructive pulmonary disease, and tumor of skin, prostate, mammary gland, lung, colon, etc). The potency of neferine in the present invention is higher than that of hexahydrothymol.
    Type: Application
    Filed: April 13, 2010
    Publication date: May 3, 2012
    Applicant: Institute of Chinese Materia Medica, China Academy
    Inventors: Tingliang Jiang, Feng Sui, Hairu Huo, Lanfang Li, Shuying Guo
  • Publication number: 20120095041
    Abstract: The invention provides neuromuscular blockade agents of the non-depolarizing type with few if any circulatory effects. Compounds of the invention include bis(isoquinolylalkanol) diesters of fumaric, maleic, succinic, and acetylenedicarboxylic acids; compositions suitable for parenteral administration of these compounds as a surgical adjunct to anesthesia, and methods of preparation of the compounds. Compounds of the invention can produce neuromuscular blockade of short or intermediate duration, which for various compounds can be reversed by administration of a thiol compound such as L-cysteine, D-cysteine or glutathione. For various compounds of the invention, the neuromuscular blockade effect can be reversed quickly, efficiently, and without notable side-effects.
    Type: Application
    Filed: March 17, 2010
    Publication date: April 19, 2012
    Applicant: Cornell University
    Inventor: John J. Savarese
  • Patent number: 8148398
    Abstract: The invention provides novel neuromuscular blocking agents, methods of using the neuromuscular blocking agents as well as reagents, methods and kits for reversing the effects of the neuromuscular blocking agents.
    Type: Grant
    Filed: December 5, 2007
    Date of Patent: April 3, 2012
    Assignee: Cornell Research Foundation, Inc.
    Inventor: John J. Savarese