Patents Examined by James O. Wilson
  • Kinase inhibitors
    Patent number: 8629132
    Abstract: The present invention provides a new group of protein kinase inhibitors, pyrropyrimidine and pyrazolopyrimidine derivatives, and pharmaceutically acceptable salts and prodrugs thereof that are useful for treating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrropyrimidine and pyrazolopyrimidine derivatives.
    Type: Grant
    Filed: November 12, 2010
    Date of Patent: January 14, 2014
    Assignees: Genosco, Oscotec, Inc.
    Inventors: Jaekyoo Lee, Ho-Juhn Song, Jong Sung Koh, Hee Kyu Lee, Youngsam Kim, Hong Woo Kim, Sunhwa Chang, Sun-Hee Lim, Jang-Sik Choi, Jung-Ho Kim, Se-Won Kim
  • Method for stereoselective synthesis of bicyclic heterocyclic compounds
    Patent number: 8629146
    Abstract: The invention relates to a method for the stereoselective preparation of a compound of formula (5), optionally in the form of the tautomers thereof,
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: January 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Juergen Schnaubelt, Wenjun Tang
  • Aspartyl protease inhibitors
    Patent number: 8629155
    Abstract: Disclosed are compounds of formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: January 14, 2014
    Assignee: Merck Sharp & Dohme, Corp.
    Inventors: Yusheng Wu, Ulrich Iserloh, Jared N. Cumming, Xiaoxiang Liu, Robert D. Mazzola, Zhong-Yue Sun, Ying Huang, Andrew Stamford, Brian McKittrick, Zhaoning Zhu
  • Pyridazinone derivatives
    Patent number: 8623870
    Abstract: Compounds of the formula (I), in which D, R1, R2, R3, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: December 10, 2009
    Date of Patent: January 7, 2014
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
  • Nitrogen containing heteroaryl compounds
    Patent number: 8623866
    Abstract: The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: January 7, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Felix Gruber, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento
  • Derivatives of N-[(1-pyrazol-1-yl)aryl]-1-indole or 1-indazole-3-carboxamide, preparation thereof and applications thereof in therapeutics
    Patent number: 8623862
    Abstract: The present invention relates to compounds corresponding to formula (I): X represents a —CH— group or a nitrogen atom; R1 represents a (C1-C4)alkyl or a (C1-C4)alkoxy; R2 represents a group Alk; R5 represents a hydrogen atom, a halogen atom or a group Alk; R6 represents a hydrogen atom, a halogen atom, a cyano, a group —COOAlk or a —CONH2 group.
    Type: Grant
    Filed: September 13, 2011
    Date of Patent: January 7, 2014
    Assignee: Sanofi
    Inventors: Alain Badorc, Christophe Boldron, Nathalie Delesque, Valérie Fossey, Gilbert Lassalle, Xavier Yvon
  • 5-alkynyl-pyrimidines
    Patent number: 8618111
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: January 24, 2011
    Date of Patent: December 31, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Siegfried Schneider, Dirk Kessler, Lars van der Veen, Tobias Wunberg
  • RAF kinase modulator compounds and methods of use thereof
    Patent number: 8618289
    Abstract: Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.
    Type: Grant
    Filed: March 17, 2009
    Date of Patent: December 31, 2013
    Assignee: Ambit Biosciences Corporation
    Inventors: Sunny Abraham, Shripad S. Bhagwat, Brian T. Campbell, Qi Chao, Raffaella Faraoni, Mark W. Holladay, Andiliy G. Lai, Martin W. Rowbottom, Eduardo Setti, Kelly G. Sprankle
  • Pyrenyloxysulfonic acid fluorescent agents
    Patent number: 8614294
    Abstract: The invention provides a novel class of reactive fluorescent agents that are based on a pyrene sulfonic acid nucleus. The agents are readily incorporated into conjugates with other species by reacting the reactive group with a group of complementary reactivity on the other species of the conjugate. Also provided are methods of using the compounds of the invention to detect and/or quantify an analyte in a sample. In an exemplary embodiment, the invention provides multi-color assays incorporating the compounds of the invention.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: December 24, 2013
    Assignee: Life Technologies Corporation
    Inventors: Richard Haugland, Wai-Yee Leung, Jixiang Liu
  • Pyrimidine hydroxy amide compounds as protein deacetylase inhibitors and methods of use thereof
    Patent number: 8614223
    Abstract: The present invention relates to novel pyrimidine hydroxy amide compounds, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.
    Type: Grant
    Filed: November 15, 2011
    Date of Patent: December 24, 2013
    Assignee: Acetylon Pharmaceuticals, Inc.
    Inventors: John H. van Duzer, Ralph Mazitschek, Yanbing Ding, Nan Yu, Yun Cao, Yong Liu
  • 3-(heteroaryl-oxy)-2-alkyl-1-aza-bicycloalkyl derivatives as alpha. 7-nachr ligands for the treatment of CNS diseases
    Patent number: 8609662
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula (I) wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals in the prevention and treatment of psychotic and neurodegenerative disorders. The claimed compounds act as nicotinic acetylcholine receptors (NACHR) ligands.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: December 17, 2013
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy
  • 4, 5, 6-trisubstituted pyrimidine derivatives as factor IXa inhibitors
    Patent number: 8609676
    Abstract: The present invention relates to novel heterocyclic compounds of Formulae (I): (Chemical formula should be inserted here as it appears on abstract in paper form) Formula (I) as disclosed herein, or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: December 17, 2013
    Assignee: Merck Sharp & Dohme, Corp.
    Inventors: Mariappan V. Chelliah, Samuel Chackalamannil, William J. Greenlee, Keith Eagan, Zhuyan Guo, Martin C. Clasby, Yan Xia, Charles L. Jayne, Michael Dwyer, Kartik M. Keertikar, Tin-Yau Chan, Li Wang
  • Therapeutic agents useful for treating pain
    Patent number: 8604037
    Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.
    Type: Grant
    Filed: August 18, 2011
    Date of Patent: December 10, 2013
    Assignee: Purdue Pharma, L.P.
    Inventors: Qun Sun, Laykea Tafesse, Sam Victory
  • Pyrrolidine derived beta 3 adrenergic receptor agonists
    Patent number: 8604038
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: December 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Edmondson, Lehua Chang, Nam Fung Kar, Gergori J. Morriello, Christopher R. Moyes, Dong-Ming Shen, Cheng Zhu, Neville J. Anthony, Philip Jones, Graham F. Smith, Mark E. Scott, Christopher F. Thompson, Joon Jung, Carolyn Cammarano, Dawn Marie Hoffman
  • Fluoroergoline analogs
    Patent number: 8604035
    Abstract: Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and/or the 5-HT1B receptor, without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alpha2A and/or the alpha2B receptors using the compounds and compositions disclosed herein.
    Type: Grant
    Filed: June 22, 2012
    Date of Patent: December 10, 2013
    Assignee: Map Pharmaceuticals, Inc.
    Inventors: Robert O. Cook, Jian Zhang, Thomas A. Armer
  • Pyridazinone derivatives
    Patent number: 8604036
    Abstract: Compounds of the formula (I), in which R1, R2, R3, W and D have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: March 24, 2009
    Date of Patent: December 10, 2013
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
  • Therapeutic pyrazoloquinoline derivatives
    Patent number: 8598159
    Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below and can exist in tautomeric forms: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
    Type: Grant
    Filed: November 18, 2010
    Date of Patent: December 3, 2013
    Assignee: Dart Neuroscience (Cayman) Ltd.
    Inventors: Alan P. Kaplan, Varsha Gupta, Jan W. F. Wasley
  • Process for etravirine intermediate and polymorphs of etravirine
    Patent number: 8598341
    Abstract: 4-[[6-chloro-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-benzonitrile is a key intermediate for the preparation of etravirine. The present invention provides a process for preparation of 4-[[6-chloro-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethylbenzonitrile. The present invention also provides a novel process for the preparation of etravirine crystalline form I. The present invention further provides novel crystalline forms of etravirine, processes for their preparation and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: December 3, 2013
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Bandi Vamsi Krishna, Adulla Venkat Narsimha Reddy
  • CDK inhibitors
    Patent number: 8598186
    Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: December 3, 2013
    Assignee: G1 Therapeutics, Inc.
    Inventors: Francis X. Tavares, Jay C. Strum
  • CDK inhibitors
    Patent number: 8598197
    Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: December 3, 2013
    Assignee: G1 Therapeutics, Inc.
    Inventors: Francis X. Tavares, Jay C. Strum