Patents Examined by John Mabry
  • Compounds for inhibiting KSP kinesin activity
    Patent number: 8796460
    Abstract: The present invention relates to compounds of Formula (I), below, (wherein X, R1, R2, R3, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity.
    Type: Grant
    Filed: October 16, 2008
    Date of Patent: August 5, 2014
    Assignee: Mercky Sharp & Dohme Corp.
    Inventors: M. Arshad Siddiqui, Chaoyang Dai, Umar Faruk Mansoor, Liping Yang, Lalalnthi Dilrukshi Vitharana, Angie R. Angeles
  • Preparation method of copolymerizable photoinitiators
    Patent number: 8791289
    Abstract: An intermediate for preparing (meth)acrylated photoinitiators according to Formula (I): wherein: R1 is selected from the group consisting of hydrogen and a methyl group; A represents a group including at least one photoinitiating moiety; L represents a n+o-valent linking group including at least one carbon atom; n and o each independently represent an integer from 1 to 4; p is equal to 0 or 1; X represents a group selected from the group consisting of Cl, Br, I, and R2SO3; and R2 represents an optionally substituted group selected from the group consisting of an alkyl group, an alkenyl group, an alkynyl group, an alkaryl group, an aralkyl group, an aryl group and a heteroaryl group. Also, a method for the preparation of (meth)acrylated photoinitiators by ?-elimination of HX from the intermediate according to Formula (I).
    Type: Grant
    Filed: September 11, 2013
    Date of Patent: July 29, 2014
    Assignee: Agfa Graphics NV
    Inventor: Johan Loccufier
  • Cortistatin A analog and use thereof
    Patent number: 8791263
    Abstract: A compound represented by the general formula (M): (wherein R1 represents a substituted or unsubstituted aromatic heterocyclic group, R2 represents a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 3 carbon atoms, OR3, N(R3)2, C(?O)OR3 or C(?O)N(R3)2, R3 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, or an acyl group having 1 to 4 carbon atoms, R4 represents a hydrogen atom, an oxygen atom or OR5, and R5 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, or an acyl group having 1 to 3 carbon atoms); or a pharmaceutically acceptable salt thereof is a cortistatin A analog which is useful as an active ingredient of medicaments for cancer prevention or treatment in that the analog can be mass-produced by chemical synthesis due to its simple chemical structure and retains the same biological activities as those of cortistatin A.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: July 29, 2014
    Assignee: Osaka University
    Inventors: Motomasa Kobayashi, Naoyuki Kotoku, Masayoshi Arai, Satoru Tamura
  • Functionalized pyridine N-oxides and processes for the preparation of the same
    Patent number: 8785480
    Abstract: In one embodiment, processes for the preparation of certain functionalized pyridine N-oxides are provided. In one form, the functionalized pyridine N-oxides include 2-substituted-5-(1-alkylthio)alkyl-pyridine N-oxides. Further embodiments, forms, objects, features, advantages, aspects, and benefits shall become apparent from the description.
    Type: Grant
    Filed: June 13, 2013
    Date of Patent: July 22, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Douglas C. Bland, Ronald Ross, Jr., Peter L. Johnson, Timothy C. Johnson
  • Compound, novel ligand, novel transition metal complex, and catalyst including novel transition metal complex
    Patent number: 8779133
    Abstract: Provided are novel ligands for transition metal complexes which exhibit high coordination power with respect to metals by being free of substituents at the positions ortho to phosphorus or arsenic and which have electron-withdrawing power comparable to the highest level known in conventional ligands. One ligand includes a compound represented by General Formula (1): R1R2R3A or General Formula (2): R1R2A-Y-AR3R4 and having a total of 15 to 110 carbon atoms. In the formulae, A is phosphorus or arsenic; R1, R2, R3 and R4 are each independently a substituted pyridyl group having optionally different electron-withdrawing groups bonded to the positions meta to the atom A as well as hydrogen atoms bonded to the positions ortho to the atom A; and Y is a divalent group derived from a C2-20, optionally substituted and optionally heteroatom-containing, aliphatic, alicyclic or aromatic compound or from ferrocene.
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: July 15, 2014
    Assignee: National University Corporation Okayama University
    Inventors: Toshinobu Korenaga, Takashi Sakai, Aram Ko
  • Optically active 2-hydroxy tetrahydrothienopyridine derivatives, preparation method and use in manufacture of medicament thereof
    Patent number: 8772489
    Abstract: Optically active 2-hydroxytetrahydrothienopyridine derivatives represented by Formula I and pharmaceutically acceptable salts, preparation method and use in the manufacture of a medicament thereof are disclosed. The pharmacodynamic experiment results show that the present compounds of Formula I are useful for inhibiting platelet aggregation. The pharmacokinetic experiment results show that the present compound of Formula I can be converted in vivo into pharmacologically active metabolites and are therefore useful for inhibiting platelet aggregation. Therefore, the present compounds are useful for the manufacture of a medicament for preventing or treating thrombosis and embolism related diseases.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: July 8, 2014
    Assignee: Jiangsu Vcare PharmaTech Co. Ltd.
    Inventors: Hongbin Sun, Jiaqi Shan, Boyu Zhang, Fang Yuan
  • TRPV3 modulators
    Patent number: 8772500
    Abstract: Disclosed herein are modulators of TRPV3 of formula (II): wherein G1, X1, X2, X3, X4, X5, G2, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: July 8, 2014
    Assignee: AbbVie Inc.
    Inventors: Erol K. Bayburt, Bruce Clapham, Phil B. Cox, Jerome F. Daanen, Michael J. Dart, Gregory A. Gfesser, Arthur Gomtsyan, Michael E. Kort, Philip R. Kym, Robert G. Schmidt
  • Compounds having auditory protective effect
    Patent number: 8772493
    Abstract: The present invention relates to a compound represented by formula 1 in the present specification or a pharmaceutically acceptable thereof, which inhibits an apoptosis mechanism of auditory hair cells for various ototoxicities leading to deafness, and protects the auditory organ and hearing, a method for preparation thereof, and a composition containing the same.
    Type: Grant
    Filed: December 11, 2012
    Date of Patent: July 8, 2014
    Assignees: Ajou University Industry-Academic Cooperation Foundation, Korea Research Institute of Chemical Technology
    Inventors: Chul Ho Kim, Young Sik Jung
  • Cannabinoid receptor 2 (CB2) inverse agonists and therapeutic potential for multiple myeloma and osteoporosis bone diseases
    Patent number: 8772541
    Abstract: Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: July 8, 2014
    Assignee: University of Pittsburgh—Of the Commonwealth System of Higher Education
    Inventors: Xiang-qun Xie, Peng Yang, Rentian Feng
  • TRPV3 modulators
    Patent number: 8772499
    Abstract: Disclosed herein are modulators of TRPV3 of Formula (I) wherein p is 1, 2, 3, or 4, and G1, X1, X2, X3, X4, X5, G2, Z1, Ra, Rb, and u are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: July 8, 2014
    Assignee: AbbVie Inc.
    Inventors: Erol K. Bayburt, Bruce Clapham, Phil B. Cox, Jerome F. Daanen, Michael J. Dart, Gregory A. Gfesser, Arthur Gomtsyan, Michael E. Kort, Philip R. Kym, Robert G. Schmidt, Eric A. Voight
  • Piperidine derivatives, pharmaceutical compositions and uses thereof
    Patent number: 8759528
    Abstract: The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: June 24, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Martin Fleck, Thorsten Lehmann-Lintz, Bernd Nosse
  • Piperidinyl-substituted lactams as GPR119 modulators
    Patent number: 8754226
    Abstract: Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which X1, X2, L, R3, R4, R5, R6, R6a, R7, R9, R9a, and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.
    Type: Grant
    Filed: May 13, 2011
    Date of Patent: June 17, 2014
    Assignee: Array BioPharma Inc.
    Inventors: Thomas Daniel Aicher, Josef Roland Bencsik, Kevin Ronald Condroski, Jay Bradford Fell, John P. Fischer, Ronald Jay Hinklin, Scott Alan Pratt, Ajay Singh, Timothy M. Turner, David A. Mareska, Steven Armen Boyd
  • Vinyl quinuclidine useful as a synthesis intermediate in the preparation of (R)-mequitazine
    Patent number: 8754074
    Abstract: The present invention relates to the use of the vinyl quinuclidine enantiomer (R) of the following formula 2 as a synthesis intermediate in the preparation of (R)-mequitazine.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: June 17, 2014
    Assignees: Pierre Fabre Medicament, Commissariat a l'Energie Atomique et aux Energies Alternatives
    Inventors: Marc Nicolas, Laurent Larquetoux, Sébastien Leroux, Eric Doris
  • Method and substances for preparation of N-substituted pyridinium compounds
    Patent number: 8754111
    Abstract: A method for the synthesis of N-substituted 3-acylated pyridinium compounds by reacting a pentamethine precursor with a primary amine.
    Type: Grant
    Filed: July 18, 2013
    Date of Patent: June 17, 2014
    Assignee: Roche Diagnostics Operations, Inc.
    Inventors: Peter Gebauer, Dieter Heindl, Carina Horn
  • Methods of producing methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate
    Patent number: 8754110
    Abstract: Methods of producing methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate. One method comprises adding methyl isobutyl ketone to an aqueous solution comprising 4-chloro-2-fluoro-3-methoxyphenyl-boronic acid to form an organic phase comprising the 4-chloro-2-fluoro-3-methoxyphenylboronic acid and an aqueous phase. The organic phase and the aqueous phase are separated. The 4-chloro-2-fluoro-3-methoxyphenylboronic acid is reacted with methyl 4-(acetylamino)-3,6-dichloropyridine-2-carboxylate in methyl isobutyl ketone to produce methyl 4-(acetylamino)-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate, which is deacetylated to produce methyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylate.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: June 17, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Jossian Oppenheimer, Mark V. M. Emonds, Christopher W. Derstine, Robert C. Clouse
  • Oligomer-calcium channel blocker conjugates
    Patent number: 8748648
    Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.
    Type: Grant
    Filed: September 3, 2008
    Date of Patent: June 10, 2014
    Assignee: Nektar Therapeutics
    Inventors: Zhongxu Ren, Bo-Liang Deng, Jennifer Riggs-Sauthier, Micah Harvey
  • Quinuclidine esters of 1-azaheterocyclylacetic acid as antimuscarinic agents, process for their preparation and medicinal compositions thereof
    Patent number: 8748613
    Abstract: Compounds of formula (I): wherein A, R1, R2, X, m, and n are as defined in the specification, are selective M3 receptor antagonists and may be used in the treatment of, inter alia, a respiratory disease such as asthma and COPD.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: June 10, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele Amari, Cristina Pesenti, Stefano Bossolo
  • Amide compound or salt thereof, and biofilm inhibitor, biofilm remover and disinfectant containing the same
    Patent number: 8748617
    Abstract: The present invention provides a new amide compound and salt thereof that is capable of inhibiting biofilm formation or removing deposited biofilms. The present invention also provides a biofilm formation inhibitor or a biofilm remover containing the amide compound or salt thereof as an active ingredient. An amide compound or salt thereof according to the present invention is denoted by General Formula (1): wherein R1 is a hydrogen atom or a hydroxyl group, R2 is a C5-12 alkyl group, and Q is a substituent denoted by Formula (Q1) or (Q2), wherein n and m are 0 or 1.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: June 10, 2014
    Assignees: University of Tokyo, Otsuka Chemical Co., Ltd.
    Inventors: Hiroaki Suga, Jun Igarashi
  • Production method of intermediate compound for synthesizing medicament
    Patent number: 8741927
    Abstract: The present invention relates to a novel method for preparing a compound of formula (2) as the intermediate, which can be effectively used for preparation of a compound of formula (1) exhibiting good inhibitory activity against dipeptidyl peptidase IV enzyme.
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: June 3, 2014
    Assignee: LG Life Sciences Ltd.
    Inventors: Bong Chan Kim, Kyu Young Kim, Hee Bong Lee, Ji Eun An, Kyu Woong Lee
  • Glycine transporter inhibiting substances
    Patent number: 8729271
    Abstract: The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: May 20, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd
    Inventors: Minoru Moriya, Akito Yasuhara, Kazunari Sakagami, Hiroshi Ohta, Kumi Abe, Shuji Yamamoto, Yuko Araki, Hiroki Urabe, Xiang-Min Sun