Patents Examined by Kahsay T. Habte
  • Xinafoate salt of N4-(2,2-difluoro-4H-benzo[1,4]oxazin-3-one)-6-yl]-5-fluoro-N2-[3-(methylaminocarbonylmethyleneoxy) phenyl]2,4-pyrimidinediamine
    Patent number: 8193181
    Abstract: The present invention relates to the xinafoate salt of N4-[(2,2-difluoro-4H-benzo[1,4]oxazin-3-one)-6-yl]-5-fluoro-N2-[3-(methylaminocarbonylmethyleneoxy)phenyl]-2,4-pyrimidinediamine. This compound is a suitable drug substance and is useful in the treatment of conditions including asthma.
    Type: Grant
    Filed: August 27, 2008
    Date of Patent: June 5, 2012
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventor: Stefan Colin John Taylor
  • Discodermolide analogues and methods of their use
    Patent number: 8193241
    Abstract: 6- and 7-substituted coumarin and related 6- and 7-substituted 1H-quinolin-2-one compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the 7-substituted coumarin and related 7-substituted 1H-quinolin-2-one compounds mimic or exceed the high level of pharmacological activity of discodermolide. In other embodiments, their preparation involves more readily available materials, higher yield processes and/or simpler synthetic sequences. In yet other embodiments, the compounds of the invention represent structurally simpler, therapeutically active analogues of discodermolide than heretofore known and may be useful as microtubule stabilizers and, inter alia, for treating and/or preventing cancer and other diseases, disorders, and/or conditions mediated by the stabilization of microtubules.
    Type: Grant
    Filed: November 15, 2010
    Date of Patent: June 5, 2012
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Amos B. Smith, III, Simon J. Shaw, David C. Myles
  • N-amino tetrahydrothiazine derivatives, method of manufacture and use
    Patent number: 8193180
    Abstract: This invention comprises the innovative synthesis of N-amino tetrahydrothiazine free bases and their salts. This invention further comprises the use of the derivatives and their therapeutic application as anticancer agents. Further this invention comprises their manufacture and use.
    Type: Grant
    Filed: January 23, 2008
    Date of Patent: June 5, 2012
    Assignee: Women & Infants Hospital
    Inventors: Laurent Brard, Rakesh Kumar Singh, Kyu Kwang Kim, Giselle Saulnier-Sholler
  • Compositions, synthesis, and methods of utilizing arylpiperazine derivatives
    Patent number: 8188076
    Abstract: The present invention provides arylpiperazine derivatives having Formula I which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.
    Type: Grant
    Filed: February 26, 2010
    Date of Patent: May 29, 2012
    Assignee: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Kouacou Adiey
  • Benzoxazines and related nitrogen-containing heterobicyclic compounds useful as mineralocorticoid receptor modulating agents
    Patent number: 8188073
    Abstract: The present invention relates to a compound, useful as a mineralocorticoid receptor-modulating agent, of the following formula [I]: wherein Ring A is a benzene ring optionally having a substituent(s) other than R1 etc, R1 is a group of the formula: RaSO2NH— etc, Ra is an alkyl group etc, R2 and R3 are each a hydrogen atom, a phenyl group, an optionally substituted alkyl group etc, X is an oxygen atom etc, Y is a group of the formula: —C(?O)— etc, Ar is an optionally substituted aryl group or an optionally substituted heteroaryl group, Q is a single bond, an alkylene group etc, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: May 29, 2012
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Toru Iijima, Yasuo Yamamoto, Hidenori Akatsuka, Takayuki Kawaguchi
  • Compounds and compositions as ITPKb inhibitors
    Patent number: 8178526
    Abstract: The invention provides a novel class of compounds of formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or dysregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb).
    Type: Grant
    Filed: June 12, 2008
    Date of Patent: May 15, 2012
    Assignee: IRM LLC
    Inventors: Badry Bursulaya, Dai Cheng, Jiqing Jiang, Donald S. Karanewsky, Yi Liu, Shifeng Pan, Yongqin Wan, Xia Wang, Yun Feng Xie, Yang Yang
  • FXA inhibitors with cyclic amidoxime or cyclic amidrazone as P4 subunit, processes for their preparations, and pharmaceutical compositions and derivatives thereof
    Patent number: 8178525
    Abstract: Disclosed are novel oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group, pharmaceutically acceptable salts thereof, methods for preparing the same and pharmaceutical compositions containing the same. The oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group or the pharmaceutically acceptable salts thereof can be effectively used for the treatment of thromboembolism and tumor as an anticoagulant based on the inhibition of factor Xa.
    Type: Grant
    Filed: June 5, 2009
    Date of Patent: May 15, 2012
    Assignee: Legochem Bioscience Ltd.
    Inventors: Ho Young Song, Young Lag Cho, Dae Yon Lee, Hee Sock Park, Sung Yoon Baek, Sang Eun Chae, Sang Hui Jo, Yeon Ok Kim, Hyang Sook Lee, Ju Hyun Park, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
  • Cefazolin sodium pentahydrate crystal and its molecular assembly preparation method
    Patent number: 8178521
    Abstract: The present invention relates to cefazolin sodium pentahydrate crystal and a method for assembly and preparation of the crystal molecule. The cefazolin sodium pentahydrate crystal molecule contains five water molecules, orthorhombic system, space group of C222(1), in which sodium ion is bonded to the cefazolin molecule with a coordinate bond. The method for assembly and preparation of cefazolin sodium pentahydrate crystal molecule are: adding a solvent to a reactor equipped with a jacket, adding cefazolin acid and a sodium salt, heating until the reaction solution is clear, stirring continuously, adjusting pH, upon the completion of the reaction, transferring the liquid into a jacketed crystallizer, adding crystal seeds or nucleating spontaneously, controlling cooling, slowly adding a antisolvent.
    Type: Grant
    Filed: September 15, 2006
    Date of Patent: May 15, 2012
    Assignees: Tianjin University, Shenzhen Gosun Pharmaceutical Co., Ltd.
    Inventors: Jingkang Wang, Yuxin Qian, Meijing Zhang, Jiehua Wu, Zhan'ao Yang
  • Method of preparing cyclic carbonates, cyclic carbamates, cyclic ureas, cyclic thiocarbonates, cyclic thiocarbamates, and cyclic dithiocarbonates
    Patent number: 8178700
    Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl) carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.
    Type: Grant
    Filed: May 4, 2009
    Date of Patent: May 15, 2012
    Assignee: International Business Machines Corporation
    Inventors: James L. Hedrick, Alshakim Nelson, Daniel P. Sanders
  • 4-amino-1,2,3-benzoxathiazine-derivatives as pesticides
    Patent number: 8173641
    Abstract: The present invention relates to novel benzoxathiazine derivatives of the formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to several processes for preparation thereof and to the use thereof as insecticides and/or acaricides in combination with further compositions such as penetrants and/or ammonium or phosphonium salts.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: May 8, 2012
    Assignee: Bayer CropScience AG
    Inventors: Bernd Alig, Klaus-Helmut Müller, Eva-Maria Franken, Ulrich Görgens, Arnd Voerste
  • Aminodihydrothiazine derivatives
    Patent number: 8173642
    Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the general formula (I): wherein ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; E is lower alkylene; X is S, O, or NR1; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; its pharmaceutically acceptable salt, or a solvate thereof.
    Type: Grant
    Filed: October 23, 2006
    Date of Patent: May 8, 2012
    Assignee: Shionogi & Co., Ltd.
    Inventors: Naotake Kobayashi, Kazuo Ueda, Naohiro Itoh, Shinji Suzuki, Gaku Sakaguchi, Akira Kato, Akira Yukimasa, Akihiro Hori, Yuji Koriyama, Hidekazu Haraguchi, Ken Yasui, Yasuhiko Kanda
  • Hydroxylthienoquinolones and related compounds as anti-infective agents
    Patent number: 8173636
    Abstract: Disclosed herein are hydroxylthienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula in which the variables R2, R6, and R7 are defined herein. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity and are particularly efficacious for the treatment of MRSA infections. The invention also provides pharmaceutical compositions, pharmaceutical compositions containing a hydroxylthienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a hydroxylthienoquinolone or related compound to an animal suffering from a microbial infection.
    Type: Grant
    Filed: April 5, 2010
    Date of Patent: May 8, 2012
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Barton James Bradbury, Milind Deshpande, Akihiro Hashimoto, Ha Young Kim, Edlaine Lucien, Godwin Pais, Michael Pucci, Qiuping Wang, Jason Allan Wiles, Avinash Phadke
  • 3-substituted-[1,2,3]-benzotriazinone compound for enhancing glutamatergic synaptic responses
    Patent number: 8173644
    Abstract: This invention relates to the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for higher order behaviors. These brain networks are involved in cognitive abilities related to memory impairment, such as is observed in a variety of dementias, an in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia and affective disorders. In a particular aspect, the present invention relates to a compound useful for treatment of such conditions, and methods of using this compound for such treatment.
    Type: Grant
    Filed: December 28, 2007
    Date of Patent: May 8, 2012
    Assignee: Les Laboratoires Servier
    Inventors: Alexis Cordi, Gary Rogers, Rudolf Mueller
  • N-substituted thiomorpholine derivatives as the inhibitors of dipeptidyl peptidase IV and the pharmaceutical uses thereof
    Patent number: 8173643
    Abstract: The present invention relates to N-Substituted thiomorpholine compounds of formula I, the possible isomers, the pharmaceutically acceptable salts, the solvates, the hydrates or the prodrugs thereof as inhibitors of dipeptidyl peptidase IV (DPP-IV); and to a method for preparing the compounds of formula I, pharmaceutical compositions comprising the compounds of formula I and use of the compounds of formula II in medical field, particularly in the preparation of medicaments for treating and preventing diabetes (in particular type II diabetes), hyperglycemia, X syndrome, hyperinsulinemia, obesity, atherosclerosis and all kinds of diseases modulated by immune system.
    Type: Grant
    Filed: June 1, 2007
    Date of Patent: May 8, 2012
    Assignee: Beijing Molecule Science and Technology Co., Ltd.
    Inventors: Song Li, Wu Zhong, Junhai Xiao, Xinghai Ma, Lili Wang, Hongying Liu, Zhibing Zheng
  • Aminodihydrothiazine derivatives substituted with a cyclic group
    Patent number: 8168630
    Abstract: This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid ? protein.
    Type: Grant
    Filed: April 23, 2008
    Date of Patent: May 1, 2012
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yuusuke Tamura, Shinji Suzuki, Yukio Tada, Shuji Yonezawa, Chiaki Fujikoshi, Sae Matsumoto, Yuuji Kooriyama, Tatsuhiko Ueno
  • Conjugated psychotropic drugs and uses thereof
    Patent number: 8168628
    Abstract: Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.
    Type: Grant
    Filed: April 21, 2010
    Date of Patent: May 1, 2012
    Assignees: Ramot at Tel-Aviv University Ltd., Bar-Ilan University
    Inventors: Abraham Nudelman, Ada Rephaeli, Irit Gil-Ad, Abraham Weizman
  • Fluorene derivatives, compositions containing the same and use thereof as inhibitors of the protein chaperone HSP 90
    Patent number: 8163750
    Abstract: The present invention relates to compounds of formula (I): wherein R1, R2, R2?, L, Het, p and p? are as defined herein, compositions containing them, and their use as medicinal products.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: April 24, 2012
    Assignee: Sanofi-Aventis
    Inventors: Fabienne Thompson, Patrick Mailliet, Jean-Marie Ruxer, Helene Goulaouic, Francois Vallee, Herve Minoux, Fabienne Pilorge, Luc Bertin, Stephane Hourcade, Maria Mendez-Perez, Peter Hamley
  • 6-substituted benzoxazines
    Patent number: 8163740
    Abstract: The present invention is concerned with 6-substituted benzoxazine derivatives of formula (I) wherein X, Y, R1 and R2 are as described herein, their manufacture, and pharmaceutical compositions containing them. The active compounds of the present invention are 5-HT5A receptor antagonists, useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders, Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: April 24, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Fused aminodihydrothiazine derivatives
    Patent number: 8158620
    Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Grant
    Filed: January 16, 2009
    Date of Patent: April 17, 2012
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Yuichi Suzuki, Takafumi Motoki, Toshihiko Kaneko, Mamoru Takaishi, Tasuku Ishida, Kunitoshi Takeda, Yoichi Kita, Noboru Yamamoto, Afzal Khan, Paschalis Dimopoulos
  • Quinuclidine derivative useful in the preparation of mequitazine
    Patent number: 8158784
    Abstract: The invention relates to a 1-aza-bicyclo[2.2.2]oct-2-en-3-ylmethyl acetate of the formula (I), wherein said compound is useful as a synthesis intermediate for the production of mequitazine.
    Type: Grant
    Filed: January 17, 2008
    Date of Patent: April 17, 2012
    Assignee: Pierre Fabre Medicament
    Inventors: Charles Mioskowski, Vanessa Gonnot, Rachid Baati, Marc Nicolas