Patents Examined by James O. Wilson
  • Imidazo pyrazines
    Patent number: 8673905
    Abstract: Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of AML.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: March 18, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kin-Chun Luk, Michael Soth
  • Substituted indazole derivatives active as kinase inhibitors
    Patent number: 8673893
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: March 18, 2014
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • 2-heteroaryl-pyrrolo [3,4-C]pyrrole derivatives, and use thereof as SCD inhibitors
    Patent number: 8673917
    Abstract: The invention relates to compounds of the formula (I), where the groups R1, M, A, B, D, L, and R have the specified meanings, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treating metabolic syndrome, insulin resistance, obesity, and diabetes.
    Type: Grant
    Filed: September 2, 2009
    Date of Patent: March 18, 2014
    Assignee: Sanofi
    Inventors: Gerhard Zoller, Marc Dietrich Voss, Hans Matter, Andreas Herling
  • Pyridine, pyridazine, pyrimidine or pyrazine carboxamides as HDL-cholesterol raising agents
    Patent number: 8669254
    Abstract: The present invention relates to compounds of the formula wherein A1 to A3 and R1 to R9 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: March 11, 2014
    Assignee: Hoffman-La Roche Inc.
    Inventors: Paul Hebeisen, Stephan Roever
  • Heterocyclic compounds as pesticides
    Patent number: 8664229
    Abstract: The present application relates to novel amides and thioamides, to processes for preparation thereof and to the use thereof for controlling animal pests, in particular arthropods and especially insects.
    Type: Grant
    Filed: April 15, 2011
    Date of Patent: March 4, 2014
    Assignee: Bayer CropScience AG
    Inventors: Thomas Bretschneider, Adeline Köhler, Reiner Fischer, Martin Füβlein, Peter Jeschke, Joachim Kluth, Friedrich August Mühlthau, Arnd Voerste, Olga Malsam, Ulrich Görgens, Yoshitaka Sato
  • 1H-pyrrolo[2,3 b]-pyridine derivatives
    Patent number: 8664236
    Abstract: 1H-Pyrrolo[2,3-b]pyridine compounds are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumors.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: March 4, 2014
    Assignee: Merck Patent GmbH
    Inventors: Timo Heinrich, Margarita Wucherer-Plietker, Hans-Peter Buchstaller
  • Phosphorus-containing prodrugs
    Patent number: 8664195
    Abstract: Novel cyclic phosphoramidate prodrugs of drugs of formula I their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.
    Type: Grant
    Filed: December 19, 2011
    Date of Patent: March 4, 2014
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Mark D. Erion, K. Raja Reddy, Serge H. Boyer
  • Process for the introduction of hydroxyethoxy side chain in bosentan
    Patent number: 8664390
    Abstract: The present invention relates to an improved process for the preparation of bosentan. In particular it relates to a process for preparing bosentan substantially free from the dimer impurity of formula (II) and the 6-hydroxy impurity of formula (III). The invention also relates to a pharmaceutical composition comprising bosentan and its use in the treatment of endothelin-receptor mediated disorders.
    Type: Grant
    Filed: June 27, 2008
    Date of Patent: March 4, 2014
    Assignee: Generics (UK) Limited
    Inventors: Abhay Gaitonde, Bindu Manojkumar, Sandeep Sonawane, Dattatrey Kokane, Sandeep Mekde, Dattatraya Shinde, Prakash Bansode
  • Specific salt, anhydrous and crystalline form of a dihydropteridione derivative
    Patent number: 8664222
    Abstract: The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide, to its crystallization in the form of an hydrate with water, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: March 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Guenter Linz, Peter Sieger, Matthias Grauert, Rolf Schmid
  • Bridged bicyclic heteroaryl substituted triazoles useful as inhibitors
    Patent number: 8658669
    Abstract: Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: February 25, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Sacha Holland, Joane Litvak, Dane Goff, Jing Zhang, Thilo J. Heckrodt
  • Pyridazine derivatives, processes for their preparation and their use as fungicides
    Patent number: 8658644
    Abstract: The present invention relates to novel pyridazine derivatives of formula (I) wherein R1 is methyl or ethyl; R2 is H or chloro; R3 is fluoro or chloro; R4 is fluoro or methoxy; and R5 is chloro or methoxy or an agrochemically usable salt from thereof, as active ingredients which have microbiodidal activity, in particular fungicidal activity.
    Type: Grant
    Filed: February 1, 2011
    Date of Patent: February 25, 2014
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Stephan Trah, Clemens Lamberth
  • 6-amino-2-substituted-5-vinylsilylpyrimidine-4-carboxylic acids and esters and 4-amino-6-substituted-3-vinylsilylpyridine-2-carboxylic acids and esters as herbicides
    Patent number: 8658568
    Abstract: 6-Amino-2-substituted-5-vinylsilylpyrimidine-4-carboxylates and 4-amino-6-substituted-3-vinylsilylpyridine-picolinates and their amine and acid derivatives are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: February 25, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Paul R. Schmitzer
  • Crystalline CDC7 inhibitor salts
    Patent number: 8658662
    Abstract: The present invention relates to novel crystalline salts of a CDC7 or CDC7/CDKs inhibitor, to a novel crystal form of the corresponding free base, to a process for their preparation, to hydrates, solvates and polymorphs of such new salt forms, to their use in therapy and to pharmaceutical compositions containing them. Such crystal salts are selected from L-asparate, hemifumarate, hydrochloride, maleate, mesylate, sulfate, L-tartrate or phosphate salts of 5-(2-amino-pyrimidin-4-yl)-2-(2,4-dichloro-phenyl)-1H-pyrrole-3-carboxylic acid amide.
    Type: Grant
    Filed: November 5, 2010
    Date of Patent: February 25, 2014
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Massimo Zampieri, Ermes Vanotti, Paola Civaroli, Maria Gioia Fornaretto
  • TRPV4 antagonists
    Patent number: 8658636
    Abstract: The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
    Type: Grant
    Filed: March 23, 2011
    Date of Patent: February 25, 2014
    Assignee: GlaxoSmithKline, LLC
    Inventors: Carl A. Brooks, Mui Cheung, Hilary S. Eidam, Ryan M. Fox, Mark A. Hilfiker, Eric S. Manas, Guosen Ye
  • Process for the preparation of pyrimidine derivatives
    Patent number: 8658793
    Abstract: A process for the preparation of 5-substituted 4-amino-2-methylpyrimidines of the formula wherein R is CONH2 or CN, and of acid addition salts thereof, characterized in that a compound of formula H2N—CH?C(R) CN (II) is reacted with acetimidic acid methyl ester or an acid addition salt thereof and that, if desired, a compound of formula I is transferred into an acid addition salt, and the transformation of a compound of formula II wherein R is CONH2 into a compound of formula II wherein R is CN by treatment with POCl3.
    Type: Grant
    Filed: May 13, 2013
    Date of Patent: February 25, 2014
    Assignee: DSM IP Assets B.V.
    Inventors: Reinhard Karge, Jan Schultz
  • 2-substituted-6-amino-5-alkyl, alkenyl or alkynyl-4-pyrimidinecarboxylic acids and 6-substituted-4-amino-3-alkyl, alkenyl or alkynyl picolinic acids and their use as herbicides
    Patent number: 8658791
    Abstract: 6-Amino-4-pyrimidinecarboxylic acids having alkyl, alkenyl or alkynyl substituents in the 5-position and 4-aminopicolinic acids having alkyl, alkenyl or alkynyl substituents in the 3-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: February 25, 2014
    Assignee: Dow AgroSciences, LLC
    Inventors: Jeffrey B. Epp, Paul R. Schmitzer, Terry W. Balko, Carla N. Yerkes
  • Oxadiazole inhibitors of leukotriene production
    Patent number: 8658661
    Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: August 12, 2011
    Date of Patent: February 25, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Todd Bosanac, Zhidong Chen, Stephane De Lombaert, John D. Huber, Ho Yin Lo, Pui Leng Loke, Weimin Liu, Tina Marie Morwick, Alan Olague, Doris Riether, Heather Tye, Lifen Wu, Renee M. Zindell
  • Compound, certain novel forms thereof, pharmaceutical compositions thereof and methods for preparation and use
    Patent number: 8658658
    Abstract: Compound of Formula A and pharmaceutically acceptable salts thereof and crystalline Forms I and II of Compound of Formula A! Also, methods for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and methods for their uses.
    Type: Grant
    Filed: November 23, 2010
    Date of Patent: February 25, 2014
    Assignee: Hutchison MediPharma Limited
    Inventors: Wei-Guo Su, Weihan Zhang, Hong Jia, Yumin Cui, Yongxin Ren, Yang Sai, Zhenping Wu, Wenji Li, Jiangyong Shao, Zhenping Tian
  • Pyrid-2yl fused heterocyclic compounds, and compositions and uses thereof
    Patent number: 8653091
    Abstract: Fused heterocyclic compounds are provided according to formula 1a or 1b: where R1, R2, and R3 are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.
    Type: Grant
    Filed: March 31, 2008
    Date of Patent: February 18, 2014
    Assignee: Evotec AG
    Inventors: Zhi-Liang Wei, John Kincaid, Michael G. Kelly, Donogh John Roger O'Mahony, Carl Kaub
  • Oximes for treatment of peripheral and central nervous system exposure to acetyl cholinesterase inhibitors
    Patent number: 8653108
    Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.
    Type: Grant
    Filed: May 17, 2012
    Date of Patent: February 18, 2014
    Assignee: Southwest Research Institute
    Inventors: Stanton F. McHardy, Richard M. Corbett, Donald M. Maxwell, Michael W. Tidwell, Bismarck Campos, Christopher J. Bemben