Patents Examined by Oluwafemi Masha
  • Methods of synthesis and purification of heteroaryl compounds
    Patent number: 8686135
    Abstract: Provided herein are methods to prepare Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein. The Heteroaryl compounds are useful for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions.
    Type: Grant
    Filed: April 30, 2013
    Date of Patent: April 1, 2014
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Patrick Anthony Jokiel, Juan Antonio Gamboa, Philip Pye, William Wei-Hwa Leong, Anusuya Choudhury
  • 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
  • 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
  • 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
  • Hydrobenzamide derivatives as inhibitors of Hsp90
    Patent number: 8653084
    Abstract: The invention provides an acid addition salt of a compound of the formula (1) Also provided by the invention are processes for preparing the compound of formula (1) and alkyl analogues thereof, novel intermediates for use in the process and methods for preparing the intermediates. The invention also provides new medical uses of compounds of the formula (1) and its ethyl analogue.
    Type: Grant
    Filed: October 12, 2007
    Date of Patent: February 18, 2014
    Assignee: Astex Therapeutics Ltd.
    Inventors: Martyn Frederickson, Mladen Vinkovic, Andrew James Woodhead, Alison Jo-Anne Woolford, Marian Williams
  • Cyclohexyloxy substituted heterocycles, pharmaceutical compositions containing these compounds and processes for preparing them
    Patent number: 8648191
    Abstract: The present invention relates to cyclohexyloxy-substituted heterocycles of general formula (I) the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways and the preparation thereof.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: February 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Birgit Jung, Ralf Lotz
  • 4-methylpyridopyrimidinone compounds
    Patent number: 8633204
    Abstract: The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I), and to salts thereof, their synthesis, and their use as inhibitors of phosphoinositide 3-kinase alpha (PI3-K?).
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: January 21, 2014
    Assignee: Pfizer Inc.
    Inventors: Hengmiao Cheng, Dilip Bhumralkar, Klaus Ruprecht Dress, Jacqui Elizabeth Hoffman, Mary Catherine Johnson, Robert Steven Kania, Phuong Thi Quy Le, Mitchell David Nambu, Mason Alan Pairish, Michael Bruno Plewe, Khanh Tuan Tran
  • 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
  • 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
  • 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
  • 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
  • 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
  • 3-aryl-substituted quinazolones, and uses thereof
    Patent number: 8575143
    Abstract: Compounds represented by Structural Formula (I): are useful, for example, in the effective killing or reducing the rate of proliferation of cancer cells, such as in patients suffering from cancer. In addition to the compounds themselves, the invention provides pharmaceutical compositions of the compounds and method of treatment using the compounds.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: November 5, 2013
    Assignee: Prolexys Pharmaceuticals, Inc.
    Inventors: Longwu Qi, Raj Gopal Venkat, Michael Pierce, Paul B. Robbins, Sudhir R. Sahasrabudhe, Robert Selliah
  • Derivatives of erlotinib
    Patent number: 8575339
    Abstract: This invention relates to novel compounds and hydrochloric acid salts thereof. More specifically, this invention relates to novel compounds and hydrochloric acid salts thereof derived from erlotinib. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an epidermal growth factor receptor tyrosine kinase (EGFR) inhibitor, such as erlotinib.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: November 5, 2013
    Inventor: Xueheng Cheng
  • Quinazolinamide derivatives
    Patent number: 8546565
    Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R5 and X have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: November 12, 2009
    Date of Patent: October 1, 2013
    Assignee: Merck Patent Gesellschaft
    Inventors: Hans-Michael Eggenweiler, Christian Sirrenberg, Hans-Peter Buchstaller
  • 3,4-diarylpyrazoles as protein kinase inhibitors
    Patent number: 8541575
    Abstract: 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, 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 disregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: September 24, 2013
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maurizio Pulici, Fabio Zuccotto, Alessandra Badari, Stefano Nuvoloni, Giovanni Cervi, Gabriella Traquandi, Sonia Biondaro, Paolo Trifiro', Chiara Marchionni, Michele Modugno
  • Enzyme inhibiting compounds
    Patent number: 8530653
    Abstract: The present invention is directed to compounds that are specifically structured to provide enzyme inhibition. In specific embodiments, the enzyme inhibiting compounds exhibit antifolate activity. Particularly, the inventive compounds are formed of an antifolate residue that is active in inhibiting one or more of TS, DHFR, GAR, FPGS, and AICAR Tfase. The enzyme inhibiting compounds are useful in a variety of methods of treatment, including treating abnormal cell proliferation and treating inflammation.
    Type: Grant
    Filed: November 4, 2010
    Date of Patent: September 10, 2013
    Assignee: Chelsea Therapeutics, Inc.
    Inventor: Michael J. Roberts
  • Compositions and methods for biological sample storage
    Patent number: 8519125
    Abstract: Compositions and methods are disclosed for substantially dry storage at ambient or elevated temperatures of biological samples such as nucleic acids, proteins and cells in a form from which the samples can be substantially recovered, using a dissolvable or dissociable dry storage matrix comprising a borate composition and a stabilizer as disclosed, such as any of a number of zwitterionic stabilizers.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: August 27, 2013
    Assignee: Biomatrica, Inc.
    Inventors: Scott E. Whitney, Sohela De Rozieres, Rolf Muller
  • Tetrahydrocinnoline derivatives
    Patent number: 8501940
    Abstract: Provided herein are compounds of formula (I): as well as pharmaceutically acceptable salts and esters thereof, which are useful as pharmaceutical compositions for the treatment of metabolic diseases and disorders.
    Type: Grant
    Filed: June 25, 2009
    Date of Patent: August 6, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Kurt Amrein, Bernd Kuhn, Alexander V. Mayweg, Werner Neidhart
  • Spirocyclic heterocycles medicaments containing said compounds, use thereof and method for their production
    Patent number: 8497369
    Abstract: The present invention relates to spirocyclic heterocycles of general formula (I) the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways, and the preparation thereof.
    Type: Grant
    Filed: February 5, 2009
    Date of Patent: July 30, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Birgit Jung, Ralf Lotz