Patents Examined by James O. Wilson
  • Inhibitors of human phosphatidylinositol 3-kinase delta
    Patent number: 8653077
    Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.
    Type: Grant
    Filed: September 28, 2011
    Date of Patent: February 18, 2014
    Assignee: ICOS Corporation
    Inventors: Chanchal Sadhu, Kennith O. Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
  • 6-phenyl-2-[((piperidin-4-ylmethyl)-piperazin-1YL) or piperazin 1-ylmethyl)-piperidin-1-yl)]-imidazo[2,1-B][1,3,4]thiadiazole derivatives and their use
    Patent number: 8653082
    Abstract: Heterocyclic compounds of formula (I), (II), (III) or a pharmaceutically acceptable salt thereof: wherein R1, R2 and R3 are each independently selected from hydrogen, halogen, C1-6alkyl, C2-6alkenyl, N—(C1-6alkyl)2, and N—(C2-6alkenyl)2, the C1-6alkyl and C2-6alkenyl being straight or branched; and Y1 and Y2 are selected from N and CH where one of Y1 and Y2 is N and the other is CH, are provided. Also provided are the synthesis of and pharmaceutical compositions including these compounds. These compounds and pharmaceutical compositions thereof can be used for the treatment of disorders, and in particular, cancer.
    Type: Grant
    Filed: February 25, 2010
    Date of Patent: February 18, 2014
    Assignee: Urifer Ltd.
    Inventors: Uri Nir, Sally Shpungin, Etai Yaffe, Moshe Cohen
  • Methods for screening and compounds that protect against amyloid diseases
    Patent number: 8653080
    Abstract: The disclosure provides methods and compositions useful for screening inhibitors of aggregation mediated proteotoxicity. The disclosure provides transgenic animals and cell useful for such screening. Also provided are compounds useful for inhibiting aggregation mediated proteotoxicity in a subject.
    Type: Grant
    Filed: January 14, 2010
    Date of Patent: February 18, 2014
    Assignee: Salk Institute for Biological Studies
    Inventors: Andrew Dillin, Thomas J. Baiga, Erik Kapernick, Joseph P. Noel
  • Solid forms of (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)-pyrimidin-4-yl)phenyl)propanoate and methods of their use
    Patent number: 8653094
    Abstract: Solid forms of (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate and salts thereof are disclosed.
    Type: Grant
    Filed: June 1, 2012
    Date of Patent: February 18, 2014
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Mark S. Bednarz, Susan De Paul, Ramanaiah C. Kanamarlapudi, Anett Perlberg, Haiming Zhang
  • 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
  • Preparation method of rosuvastatin calcium and its intermediates
    Patent number: 8653265
    Abstract: A preparation method of rosuvastatin calcium (Formula 1), which can be used for the production of medicament lowering the levels of LDL-cholesterol and triglycerides in vivo, is provided. Such preparation method is suitable for industrial production. Furthermore, the intermediate crystallines used in the preparation method are provided.
    Type: Grant
    Filed: May 27, 2009
    Date of Patent: February 18, 2014
    Assignee: Changzhou Pharmaceutical Factory
    Inventors: Benshun Chen, Bing Wang, Xiaofeng Jin, Lin Zou
  • Co-crystal compound of optical device
    Patent number: 8653267
    Abstract: The present invention discloses a co-crystal compound of optical devices. The co-crystal compound is crystallized out with hydrogen bonding by a temperature fluctuation method after mixing small organic molecules without optoelectronic properties and organic molecules having heterocyclic rings with optoelectronic properties. The photoluminescence (PL) intensity of this hydrogen-bonded co-crystal compound according to the present invention can vary with a variety of the small organic molecules without optoelectronic properties, so as to modulate the PL intensity.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: February 18, 2014
    Assignee: National Central University
    Inventors: Tu Lee, Pu-Yun Wang
  • Ethynyl nitrogen containing heteroaryl pyrazolidin-3-one derivatives
    Patent number: 8648088
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein G, X, R1, R2, R3, R3?, R4, and R4? are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Grant
    Filed: April 24, 2012
    Date of Patent: February 11, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • 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
  • Certain dipeptidyl peptidase inhibitors
    Patent number: 8648073
    Abstract: Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
    Type: Grant
    Filed: December 28, 2010
    Date of Patent: February 11, 2014
    Assignee: Fochon Pharma, Inc.
    Inventors: Weibo Wang, Tongshuang Li
  • 1,3,6-substituted indole derivatives having inhibitory activity for protein kinase
    Patent number: 8648089
    Abstract: Disclosed are a 1,3,6-substituted indole compound having inhibitory activity for protein kinases, a pharmaceutically acceptable thereof, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth including the compound as an active ingredient. Since the novel indole compound exhibits superior inhibitory activity for various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating cancers caused by abnormal cell growth.
    Type: Grant
    Filed: November 24, 2012
    Date of Patent: February 11, 2014
    Assignee: Korea Institute of Science and Technology
    Inventors: Tae Bo Sim, Young Jin Ham, Hwan Geun Choi
  • Low hygroscopic aripiprazole drug substance and processes for the preparation thereof
    Patent number: 8642760
    Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous Aripiprazole crystals is stored for an extended period.
    Type: Grant
    Filed: June 23, 2011
    Date of Patent: February 4, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Takuji Bando, Satoshi Aoki, Junichi Kawasaki, Makoto Ishigami, Youichi Taniguchi, Tsuyoshi Yabuuchi, Kiyoshi Fujimoto, Yoshihiro Nishioka, Noriyuki Kobayashi, Tsutomu Fujimura, Masanori Takahashi, Kaoru Abe, Tomonori Nakagawa, Koichi Shinhama, Naoto Utsumi, Michiaki Tominaga, Yoshihiro Ooi, Shohei Yamada, Kenji Tomikawa
  • Heterocycle phenyl amide T-type calcium channel antagonists
    Patent number: 8637513
    Abstract: The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. 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 T-type calcium channels are involved.
    Type: Grant
    Filed: October 23, 2008
    Date of Patent: January 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Paul J. Coleman, Thomas S. Reger, Kelly-Ann S. Schlegel, Youheng Shu, Zhi-Qiang Yang
  • Serine/threonine kinase inhibitors
    Patent number: 8637537
    Abstract: Compounds having the formula I wherein A, Z, R1a, R1b, R2, R3, R4, R5, R6, R7, R9, R10, Ra, Rb and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: January 28, 2014
    Assignee: Genentech, Inc.
    Inventors: Ignacio Aliagas-Martin, James Crawford, Wendy Lee, Simon Mathieu, Joachim Rudolph
  • Aminopyrimidines useful as kinase inhibitors
    Patent number: 8637511
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.
    Type: Grant
    Filed: June 8, 2010
    Date of Patent: January 28, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Hayley Binch, Michael Mortimore, Chris Davis, Dean Boyall, Simon Everitt, Daniel Robinson, Sham Ramaya, Damien Fraysse, John Studley, Andrew Miller, Michael O'Donnell, Alistair Rutherford, Joanne Pinder
  • Pyridazinone derivatives
    Patent number: 8637518
    Abstract: Compounds of the formula (I), in which Y, R1, R2, R3 and R3? 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 tumours.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: January 28, 2014
    Assignee: MERCK PATENT GmbH
    Inventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
  • AZA spiro alkane derivatives as inhibitors of metalloproteases
    Patent number: 8637497
    Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: January 28, 2014
    Assignee: Incyte Corporation
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian Metcalf
  • 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
  • Bicyclic organic compounds suitable for the treatment of inflammatory or allergic conditions
    Patent number: 8633211
    Abstract: A compound of formula (I): in free or salt form, wherein A, R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.
    Type: Grant
    Filed: March 4, 2008
    Date of Patent: January 21, 2014
    Assignee: Novartis AG
    Inventor: Roger John Taylor
  • Spirolactam derivatives and uses of same
    Patent number: 8633190
    Abstract: The present invention provides spirolactam derivatives of formula (I): wherein R1-R7 are as defined herein; or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and uses of the same.
    Type: Grant
    Filed: October 26, 2010
    Date of Patent: January 21, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Hao Zhou, Guiying Li, Dario Doller, Gil Ma