Plural Isoquinoline Ring Systems Attached Directly Or Indirectly To Each Other By Nonionic Bonding Patents (Class 546/140)
  • Patent number: 10840453
    Abstract: The present specification provides a di-polycyclic compound, and a polymer chain consisting of alternating electron donor compounds and electron acceptor compounds, which include the di-polycyclic compound.
    Type: Grant
    Filed: January 7, 2019
    Date of Patent: November 17, 2020
    Assignee: International Business Machines Corporation
    Inventors: Brandon M. Kobilka, Joseph Kuczynski, Jacob T. Porter, Jason T. Wertz
  • 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
  • Publication number: 20150034938
    Abstract: A compound for an organic optoelectronic device, an organic light emitting diode including the same, and a display device including the organic light emitting diode are disclosed and the compound for an organic optoelectronic device represented by the following Chemical Formula 1 or 2 provides an organic light emitting diode having life-span characteristics due to excellent electrochemical and thermal stability, and high luminous efficiency at a low driving voltage.
    Type: Application
    Filed: September 12, 2014
    Publication date: February 5, 2015
    Inventors: Dong-Min KANG, Hyun-Jung KIM, Chang-Ju SHIN, Jong-Woo WON, Nam-Heon LEE, Soo-Young JEONG, Ho-Kuk JUNG, Mi-Young CHAE
  • 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: 20150021197
    Abstract: The invention relates to novel metal complexes useful as catalysts in redox reactions (such as, hydrogen (H2) production). In particular, the invention provides novel transition metal (e.g., cobalt (Co) or nickel (Ni)) complexes, in which the transition metal is coupled with N,N-Bis(2-pyridinylmethyl)-2,2?-Bipyridine-6-methanamine (DPA-Bpy), 6?-((bis(pyridin-2-ylmethyl)amino)methyl)-N,N-dimethyl-2,2?-bipyridin-6-amine (DPA-ABpy), N,N-bis((isoquinolin-1-yl)methyl)(6-(pyridin-2-yl)pyridin-2-yl)methanamine (DIQ-Bpy), or a derivative thereof. The invention also relates to a method of producing H2 from an aqueous solution by using the metal complex as a catalyst. In certain embodiments, the invention provides a metal complex of the formulae as described herein.
    Type: Application
    Filed: July 31, 2014
    Publication date: January 22, 2015
    Inventors: Xuan Zhao, Charles E. Webster
  • 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: 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: 20140238900
    Abstract: The present invention is related to formulations consisting by block copolymers ?,?-di-aryl or alkyl sulfonates of poly(ethylene oxide)w-poly(propylene oxide)-poly(ethylene oxide)w of bis-ammonium and block copolymers ?,?-di-amine of poly(ethylene oxide)w-poly(propylene oxide)-poly(ethylene oxide)w, that are effective in the dewatering and desalting crude whose specific gravities are within the range of 14 to 23° API.
    Type: Application
    Filed: February 25, 2014
    Publication date: August 28, 2014
    Inventors: Eugenio Alejandro FLORES OROPEZA, Cesar Andres FLORES SANDOVAL, Reyna REYES MARTINEZ, Jose Gonzalo HERNANDEZ CORTEZ, Alfonso LOPEZ ORTEGA, Laura Veronica CASTRO SOTELO, Fernando ALVAREZ RAMIREZ, Arquimedes ESTRADA MARTINEZ, Flavio Salvador VAZQUEZ MORENO
  • 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: 8785641
    Abstract: The present invention describes tripodal catechol derivatives with an adamantyl basic framework for the functionalization of surfaces, methods for their production and use. The remaining fourth bridgehead position is easily suitable to be further functionalised via so-called click reactions, by way of example with biomolecules, dyes, radiomarkers, polyethylene glycol or active agents.
    Type: Grant
    Filed: September 7, 2011
    Date of Patent: July 22, 2014
    Assignee: Justus-Liebig-Universitat Giessen
    Inventors: Wolfgang Maison, Faiza Khalil, Elisa Franzmann
  • 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: 8741924
    Abstract: Small molecule compounds are provided for treating lupus as are methods of treating lupus using these compounds.
    Type: Grant
    Filed: May 6, 2011
    Date of Patent: June 3, 2014
    Assignee: The Feinstein Institute for Medical Research
    Inventors: Yousef Al-Abed, Betty A. Diamond
  • 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: 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
  • 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: 20130245269
    Abstract: The present invention describes tripodal catechol derivatives with an adamantyl basic framework for the functionalisation of surfaces, methods for their production and use. The remaining fourth bridgehead position is easily suitable to be further functionalised via so-called click reactions, by way of example with biomolecules, dyes, radiomarkers, polyethylene glycol or active agents.
    Type: Application
    Filed: September 7, 2011
    Publication date: September 19, 2013
    Applicant: JUSTUS-LIEBIG-UNIVERSITA GIESSEN
    Inventors: Wolfgang Maison, Faiza Khalil, Elisa Franzmann
  • 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
  • Patent number: 8461338
    Abstract: The present invention provides an improved method of chromatographically separating the isomers of (1R,rR)-atracurium salts by high-performance liquid chromatography (HPLC), in the absence of a strong acid. The separation is preferably performed on a silica gel HPLC column using an eluent containing an organic solvent, a polar aprotic co-solvent and a weak organic acid.
    Type: Grant
    Filed: March 5, 2008
    Date of Patent: June 11, 2013
    Assignee: Chemagis Ltd.
    Inventors: Oded Arad, Elena Ostrovsky
  • Patent number: 8461329
    Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.
    Type: Grant
    Filed: December 25, 2009
    Date of Patent: June 11, 2013
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Tetsuo Takayama, Hajime Asanuma, Daisuke Wakasugi, Rie Nishikawa, Yoshinori Sekiguchi, Madoka Kawamura, Naoya Ono, Tetsuya Yabuuchi, Takahiro Oi, Yusuke Oka, Shoichi Kuroda, Fumito Uneuchi, Takeshi Koami
  • Publication number: 20130112946
    Abstract: A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the heterocyclic compound: wherein X1 and X2, X1 and R1 to R10 are defined as in the specification.
    Type: Application
    Filed: February 29, 2012
    Publication date: May 9, 2013
    Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.
    Inventors: Bum-Woo Park, Yoon-Hyun Kwak, Sun-Young Lee, Chang-Ho Lee, Se-Jin Cho
  • 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
  • Patent number: 8435648
    Abstract: A compound for an organic photoelectric device, the compound being represented by the following Chemical Formula 1:
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: May 7, 2013
    Assignee: Cheil Industries, Inc.
    Inventors: Kyu-Yeol In, Myeong-Soon Kang, Ho-Kuk Jung, Nam-Soo Kim, Eui-Su Kang, Mi-Young Chae
  • 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
  • Publication number: 20130041154
    Abstract: The present invention provides a process of producing cisatracurium compounds, e.g., cisatracurium besylate, from isoquinolinium salts of the structural formula (VIIA) wherein X? is an anion and R is H or a C1-C6 alkyl, or an activated form of the carboxylic acid with 1,5-pentanediol to form a cisatracurium salt, optionally via an intermediate compound (VIII). The cisatracurium compounds can be purified using simple techniques to afford pure cisatracurium besylate without the need for HPLC purification.
    Type: Application
    Filed: October 10, 2012
    Publication date: February 14, 2013
    Applicant: CHEMAGIS LTD.
    Inventor: CHEMAGIS LTD.
  • 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: 8354537
    Abstract: The present invention provides R,R?-atracurium salts, processes for producing and purifying such salts, and methods of using such salts to produce highly pure cisatracurium besylate.
    Type: Grant
    Filed: October 7, 2008
    Date of Patent: January 15, 2013
    Assignee: CHEMAGIS Ltd.
    Inventors: Oded Arad, Ofer Sharon, 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
  • Patent number: 8222634
    Abstract: The present invention relates to a novel anthracene derivative and an organic electronic device using the same. The organic electronic device according to the present invention shows excellent characteristics in efficiency, driving voltage, and life time.
    Type: Grant
    Filed: May 16, 2008
    Date of Patent: July 17, 2012
    Assignee: LG Chem, Ltd.
    Inventors: Dong-Hoon Lee, Jae-Chol Lee, Jae-Soon Bae, Jun-Gi Jang, Kong-Kyeom Kim, Dae-Woong Lee
  • Publication number: 20120153266
    Abstract: The present invention provides a new class of excited state intramolecular charge transfer (ESIPT) dye compounds based on mono or dihydroxy substituted 1,3-bisiminoisoindole motif and metal complexes containing such compounds as ligands. The present invention also provides OLEDs containing the compound and/or metal complex as the emissive material.
    Type: Application
    Filed: December 12, 2011
    Publication date: June 21, 2012
    Inventors: Mark E. THOMPSON, Kenneth HANSON, Peter DJUROVICH
  • Patent number: 8178678
    Abstract: Provided are bis-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: May 14, 2007
    Date of Patent: May 15, 2012
    Assignee: University of Kentucky Research Foundation
    Inventors: Peter Crooks, Linda P. Dwoskin, Guangrong Zheng, Zhenfa Zhang, Sangeetha Sumithran, Marharyta Pivavarchyk
  • 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: 8158795
    Abstract: A process for the preparation of neuromuscular blocking agents with isoquinoline structure, such as atracurium besylate, doxacurium chloride, mivacurium chloride and gantacurium chloride, by chromatographic purification of their mixtures of isomers using a silica modified by treatment with a tertiary amine of formula NR1R2R3 or a corresponding quaternary ammonium compound N+R1R2R3R4X? wherein R1, R2, R3 and R4, the same or different, are linear or branched C1-C4 alkyl groups or —CH2—Ar groups or two among R1, R2, R3 and R4 form a 5- or 6-membered cycle, optionally substituted with a —CH2—Ar group or condensed with an Ar group, Ar being an aryl optionally substituted with one or more electrodonating groups, and X? being a suitable anion, is described.
    Type: Grant
    Filed: July 10, 2009
    Date of Patent: April 17, 2012
    Assignee: Farmabios S.p.A.
    Inventors: Claudio Gianluca Pozzoli, Franco Malanga, Vincenzo Redaelli
  • 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
  • Patent number: 8143257
    Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.
    Type: Grant
    Filed: November 23, 2005
    Date of Patent: March 27, 2012
    Assignee: PTC Therapeutics, Inc.
    Inventors: Soongyu Choi, Young-Choon Moon, Nadarajan Tamilarasu
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    Abstract: The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type I (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration.
    Type: Application
    Filed: June 4, 2010
    Publication date: March 22, 2012
    Inventors: Juan Lorenzo Catena Ruiz, Carme Serra Comas, Oscar Rey Puiggros, Albert Antolin Hernandez, Esther Monlleomas
  • Publication number: 20110284832
    Abstract: A compound for an organic photoelectric device, the compound being represented by the following Chemical Formula 1:
    Type: Application
    Filed: June 30, 2011
    Publication date: November 24, 2011
    Inventors: Kyu-Yeol In, Myeong-Soon Kang, Ho-Kuk Jung, Nam-Soo Kim, Eui-Su Kang, Mi-Young Chae