Patents Examined by Brian McDowell
  • Process for preparation of erlotinib and its pharmaceutically acceptable salts
    Patent number: 8642758
    Abstract: A process for the preparation of a salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine comprising reacting a 4-halo-6,7-bis(2-methoxyethoxy) quinazoline with 3-aminophenyl acetylene or an acid salt thereof under acidic conditions to form the corresponding acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine, the process optionally further comprising converting the acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine to N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine.
    Type: Grant
    Filed: April 3, 2008
    Date of Patent: February 4, 2014
    Assignee: Cipla Limited
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan
  • Pyrazinone derivatives as insulin secretion stimulators, methods for obtaining them and use thereof for the treatment of diabetes
    Patent number: 8637522
    Abstract: The present invention relates to pyrazinone derivatives of formula (I), wherein n, R1, R2, R3 and R4 are as defined in claim 1, as insulin secretion stimulators. The invention also relates to the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.
    Type: Grant
    Filed: January 15, 2009
    Date of Patent: January 28, 2014
    Assignee: Merck Patent GmbH
    Inventors: Gérard Botton, Micheline Kergoat, Christine Charon, Samer Elbawab
  • Dye for a dye-sensitised solar cell, and a solar cell comprising the same
    Patent number: 8629269
    Abstract: The present invention relates to a dye for a dye-sensitized solar cell. The dye according to the present invention has a high degree of light absorbency and can improve the photoelectric current conversion efficiency when employed in a light-absorbing layer for a solar cell. Chemical Formula 1 illustrates the present invention. wherein X1, X2, N, Z1, and A1 are described herein.
    Type: Grant
    Filed: February 5, 2009
    Date of Patent: January 14, 2014
    Assignee: Solarsys Co., Ltd.
    Inventors: Kwang-Yol Kay, Kang-Jin Kim, Jong-Hyung Kim, Young-Jin Kwon
  • Compounds
    Patent number: 8629271
    Abstract: The present invention relates to spirocyclic amide derivatives of the formula I, pharmaceutically acceptable salts thereof, a process for their preparation, pharmaceutical compositions containing them, and their use in therapy.
    Type: Grant
    Filed: April 2, 2012
    Date of Patent: January 14, 2014
    Assignee: AstraZeneca AB
    Inventors: Lilian Alcaraz, Nicholas David Kindon
  • Benzoxazines, benzothiazines, and related compounds having NOS inhibitory activity
    Patent number: 8618286
    Abstract: The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. Exemplary compounds are of the formula: The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: December 31, 2013
    Assignee: NeurAxon, Inc.
    Inventors: Jailall Ramnauth, Subhash C. Annedi, Sarah Silverman, Peter Dove, Shawn Maddaford, Suman Rakhit
  • Analogs of dehydrophenylahistins and their therapeutic use
    Patent number: 8618292
    Abstract: Compounds represented by the following structure (II) are disclosed: as are methods for making such compounds. Compositions and methods for treating various disease conditions including cancer and non-cancer diseases associated with vascular proliferation are also disclosed.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: December 31, 2013
    Assignee: Beyondspring Pharmaceuticals, Inc.
    Inventors: Michael Palladino, George Kenneth Lloyd, Yoshio Hayashi
  • Heterocyclic compounds and uses thereof in the treatment of sexual disorders
    Patent number: 8614319
    Abstract: Novel heterocyclic compounds having the Formula I: wherein A, B, D, E, G, K, L, M, Q, T, X, Y and Z are as defined herein, which exhibit a dopamine receptor (preferably a D4 receptor) agonistic activity, and/or a PDE5 inhibitory activity, processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of sexual disorders such as decreased libido, orgasm disorder and erectile dysfunction are disclosed.
    Type: Grant
    Filed: November 13, 2012
    Date of Patent: December 24, 2013
    Assignee: ATIR Holding S.A.
    Inventors: Dmitry Tworowski, Ron Matsievitch, Vladimir Kogan
  • Quinazoline based EGFR inhibitors containing a zinc binding moiety
    Patent number: 8604044
    Abstract: The present invention relates to quinazoline containing zinc-binding moiety based derivatives of Formula (IV) below. These compounds have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and are useful in the treatment of EGFR-TK related diseases and disorders such as cancer. These compounds may further act as HDAC inhibitors.
    Type: Grant
    Filed: September 10, 2007
    Date of Patent: December 10, 2013
    Assignee: Curis, Inc.
    Inventors: Changgeng Qian, Xiong Cai, Stephen Gould, Haixiao Zhai
  • Heterocyclic sulfonamides
    Patent number: 8604025
    Abstract: Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Grant
    Filed: February 5, 2013
    Date of Patent: December 10, 2013
    Assignee: Cytokinetics, Inc.
    Inventors: Bradley Paul Morgan, Fady Malik, Erica Anne Kraynack, Alexander Ramon Muci, Xiangping Qian, David J. Morgans, Jr.
  • Acetyl pyrrolidinyl indole derivative
    Patent number: 8592428
    Abstract: The present invention relates to compounds, which are useful for treatment and/or prevention of diabetes mellitus, diabetes mellitus complications or obesity, since the compounds have glucokinase-activating effects, and are presented in Formula (I): wherein R1 represents a lower alkylsulfonyl group; R2 represents a hydrogen atom; R20 represents, e.g., a hydrogen atom; m represents an integer of from 1 to 3; and n represents zero or 1, or relates to a pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 3, 2009
    Date of Patent: November 26, 2013
    Assignee: MSD K. K.
    Inventors: Hideaki Imamura, Takuya Suga, Hiroyuki Takahashi, Hideki Jona, Etsuko Hirose, Norikazu Ohtake
  • Substituted pyrrolo[2,3-b]-pyridines and -pyrazines
    Patent number: 8592448
    Abstract: Compounds of Formula I, as shown below and defined herein: (I) pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by Ron and/or Met.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: November 26, 2013
    Assignee: OSI Pharmaceuticals, LLC
    Inventors: Xin Chen, Melzhong Jin, Andrew Kleinberg, An-Hu Li, Mark J. Mulvihill, Arno G. Steinig, Jing Wang
  • Method for producing dichloropyrazine derivative
    Patent number: 8586741
    Abstract: A method for producing a hydroxypyrazine derivative represented by formula (I) (wherein R1 represents a halogen atom), the method including reacting a pyrazine derivative represented by formula (III) (wherein R2 represents a nitrile group, an N-unsubstituted or N-substituted carbamoyl group, an ester group or a carboxyl group, M represents a cation capable of forming a salt, and n represents a number corresponding with the valence of M) with a halogenating agent. Also, a method for producing a dichloropyrazine derivative represented by formula (II) (wherein R21 represents a nitrile group, an N-unsubstituted or N-substituted carbamoyl group, an ester group, a carboxyl group, or a group formed as a result of a change in the functional group of R2 during chlorination), the method including reacting the hydroxypyrazine derivative (I) with a chlorinating agent.
    Type: Grant
    Filed: January 14, 2010
    Date of Patent: November 19, 2013
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Tamio Hara, Naoki Norimatsu, Hiroaki Kurushima, Takuya Kano
  • Substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives useful in the treatment of autoimmune and inflammatory disorders
    Patent number: 8580841
    Abstract: The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia): and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: November 12, 2013
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Robert M Jones, Daniel J Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Brett Ullman, Jeanne V Moody, Xiuwen Zhu, Scott Stirn
  • Functionalized expanded porphyrins
    Patent number: 8580845
    Abstract: Disclosed are functionalized expanded porphyrins that can be used as spectrometric sensors for high-valent actinide cations. The disclosed functionalized expanded porphyrins have the advantage over unfunctionalized systems in that they can be immobilized via covalent attachment to a solid support comprising an inorganic or organic polymer or other common substrates. Substrates comprising the disclosed functionalized expanded porphyrins are also disclosed. Further, disclosed are methods of making the disclosed compounds (immobilized and free), methods of using them as sensors to detect high valent actinides, devices that comprise the disclosed compounds, and kits.
    Type: Grant
    Filed: June 23, 2008
    Date of Patent: November 12, 2013
    Assignee: Board of Regents, The University of Texas System
    Inventors: Jonathan L. Sessler, Patricia J. Pantos
  • Compositions, synthesis, and methods of utilizing quinazolinedione derivatives
    Patent number: 8575185
    Abstract: The present invention provides quinazolinedione derivatives of Formulae Ia and Ib, which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, depression and dementia.
    Type: Grant
    Filed: February 26, 2010
    Date of Patent: November 5, 2013
    Assignee: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Sureshbabu Dadiboyena, Kouacou Adiey
  • Heterocyclic compound and use thereof
    Patent number: 8575154
    Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.
    Type: Grant
    Filed: August 9, 2011
    Date of Patent: November 5, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masakuni Kori, Toshihiro Imaeda, Shinji Nakamura, Masashi Toyofuku, Eiji Honda, Yasutomi Asano, Osamu Ujikawa, Michiyo Mochizuki
  • Bicyclic dihydroimidazolone CGRP receptor antagonists
    Patent number: 8569291
    Abstract: Compounds of formula (I): wherein variables B, G1, G2, G3, G4, Ea, Eb, Ec, A1, A2, A3, A4, R6 and RPG and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: September 10, 2009
    Date of Patent: October 29, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Craig A. Stump
  • Nanoparticulate probe for in vivo monitoring of tissue oxygenation
    Patent number: 8569482
    Abstract: A new class of micro- and nano-particulate paramagnetic spin probes useful for magnetic resonance imaging techniques, including electron paramagnetic resonance (EPR) and magnetic resonance imaging (MRI). The probes are lithium phthalocyanine derivative compounds. Also provided are suspensions and emulsions comprising lithium phthalocyanine derivative probes. Also provided are noninvasive methods for measuring noninvasive methods of measuring oxygen concentration, oxygen partial pressure, oxygen metabolism, and nitric oxide concentration in a specific tissue, organ, or cell in vivo or in vitro.
    Type: Grant
    Filed: November 29, 2011
    Date of Patent: October 29, 2013
    Assignee: The Ohio State University Research Foundation
    Inventors: Periannan Kuppusamy, Vijay Kutala, Jay L. Zweier, Pawel Kwiatkowski
  • Organometal complex and light-emitting element using the same
    Patent number: 8569486
    Abstract: An organometallic complex according to the present invention comprises a structure represented by the following general formula (1). In the formula, R1 to R5 are any one selected from the group consisting of hydrogen, a halogen element, an acyl group, an alkyl group, an alkoxy group, an aryl group, a cyano group, and a heterocyclic group, Ar is an aryl group having an electron-withdrawing group or a heterocyclic group having electron-drawing group, and M is an element of Group 9 or an element of Group 10.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: October 29, 2013
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hideko Inoue, Satoshi Seo, Satoko Shitagaki, Hiroko Abe
  • Hydroxy-substituted gold(III) porphyrin complexes as histone deacetylase inhibitors
    Patent number: 8563712
    Abstract: A method for treatment of cancer by inhibiting the activity of histone deacetylase, comprising administering to a human in need of such treatment a composition containing a therapeutically effective amount of a gold(III) complex having the structural formula of or a pharmaceutically acceptable salt thereof, wherein: —R is selected from the group consisting of —OH, —CH2OH, C2H4OH, —C3H6OH or —C4H8OH; and X is independently a pharmaceutically acceptable counter-ion.
    Type: Grant
    Filed: October 27, 2010
    Date of Patent: October 22, 2013
    Assignee: The University of Hong Kong
    Inventors: Chi Ming Che, Yu Wang, Raymond Wai Yin Sun, Kim Hei-Man Chow