Patents Examined by Kristin Bianchi
  • Bicyclo-pyrazoles and pharmaceutical compositions comprising them
    Patent number: 8273765
    Abstract: Bicyclo-pyrazole compounds of formula (I), as herein defined, are useful for treating diseases linked to disregulated protein kinases.
    Type: Grant
    Filed: May 13, 2009
    Date of Patent: September 25, 2012
    Assignee: Pfizer Italia S.R.L.
    Inventors: Daniele Fancelli, Valeria Pittala′, Mario Varasi
  • Substituted 2-indolinone as PTK inhibitors containing a zinc binding moiety
    Patent number: 8273785
    Abstract: The present invention relates to substituted 2-indolinone containing zinc-binding moiety based derivatives that have enhanced or unique properties as inhibitors of protein tyrosine kinase (PTK) receptors and their use in the treatment of PTK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.
    Type: Grant
    Filed: March 28, 2011
    Date of Patent: September 25, 2012
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Changgeng Qian, Stephen Gould
  • Compounds and methods for kinase modulation, and indications therefor
    Patent number: 8268858
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Grant
    Filed: December 20, 2007
    Date of Patent: September 18, 2012
    Assignee: Plexxikon Inc.
    Inventors: Guoxian Wu, Wayne Spevak, Songyuan Shi, Hanna Cho, Prabha N. Ibrahim, Chao Zhang, Shenghua Shi, Yong Zhou, Dean Artis, Jiazhong Zhang
  • Compounds derived from 2-(3-methylenedioxy)-benzoyl indol
    Patent number: 8268831
    Abstract: The present invention describes a series of derivatives of 2-(3-methylenedioxy)-benzoyl indol, their mixtures, their pharmaceutically acceptable salts, their enantiomers, pharmaceutical compositions comprising them, processes for preparing them, use in the prophylactic and/or curative treatment of sexual dysfunction. More specifically, the invention describes derivatives (R)-3-((2-(benzo[d][1,3]dioxol-5-carbonyl)-1H-indol-3-yl)methyl)-1-methylpiperazine-2,5-dione, and S)-3-((2-(benzo[d][1,3]dioxol-5-carbonyl)-1H-indol-3-yl)methyl)-1-methylpiperazine-2,5-dione.
    Type: Grant
    Filed: September 30, 2009
    Date of Patent: September 18, 2012
    Assignee: Biolab Sanus Farmaceutica Ltda.
    Inventors: Sérgio Luiz Sacurai, Carlos Eduardo Da Costa Touzarim, Marcio Henrique Zaim
  • Triptolide C-ring derivatives as anticancer agents and immune modulators
    Patent number: 8268882
    Abstract: Disclosed are compounds based on C- and D-ring modifications of triptolide and hydroxylated triptolide, for use in therapy, such as antiproliferative, anticancer, and immunosuppressive therapy.
    Type: Grant
    Filed: February 4, 2010
    Date of Patent: September 18, 2012
    Assignee: Pharmagenesis, Inc.
    Inventor: John H. Musser
  • 3-3-di-substituted-oxindoles as inhibitors of translation initiation
    Patent number: 8268879
    Abstract: Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.
    Type: Grant
    Filed: June 9, 2010
    Date of Patent: September 18, 2012
    Assignee: President and Fellows of Harvard College
    Inventors: José A. Halperin, Amarnath Natarajan, Huseyin Aktas, Yun-Hua Fan, Han Chen
  • Anti-cancer compounds, synthesis thereof, and methods of using same
    Patent number: 8268874
    Abstract: Embodiments relate to the field of chemistry and biochemistry, and, more specifically, to anti-cancer compounds, synthesis thereof, and methods of using same. Disclosed herein are various heterocyclic compounds and methods of using the novel anti-cancer compounds to inhibit the growth of a cancer cell, for instance a leukemia, non-small cell lung, central nervous system (CNS), skin, ovarian, renal, prostate, breast, or colon cancer cell. Other embodiments include methods of treating cancer in a subject, such as using the disclosed heterocyclic anti-cancer agents.
    Type: Grant
    Filed: March 3, 2009
    Date of Patent: September 18, 2012
    Assignee: University of Notre Dame du Lac
    Inventors: Marvin J. Miller, Garrett C. Moraski, Jonathan Stefely
  • Substituted N-phenyl-bipyrrolidine carboxamides and therapeutic use thereof
    Patent number: 8252824
    Abstract: The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: August 28, 2012
    Assignee: SANOFI
    Inventors: Werngard Czechtizky, Zhongli Gao, William Joseph Hurst, Lothar Schwink, Siegfried Stengelin
  • Process for the preparation of imatinib base
    Patent number: 8252926
    Abstract: Provided is an environmentally-friendly process for preparing imatinib base in high yield, without the use of an organic solvent.
    Type: Grant
    Filed: May 27, 2011
    Date of Patent: August 28, 2012
    Assignee: Mustafa Nevzat llaç Sanayii A.S.
    Inventors: Halit Gündüz, Yusuf Özlü, Serkan Yalçin
  • 1-butyl-2-hydroxyaralkyl piperazine derivatives and the uses as anti-depression medicine thereof
    Patent number: 8252796
    Abstract: The invention discloses 1-butyl-2-hydroxyl aralkyl piperazine derivatives and their use as antidepressants. The derivatives of the present invention have triple inhibition effect on the reuptake of 5-HT, NA and DA, and can be administrated to the patients in need thereof in form of composition by route of oral administration, injection and the like. Compared with clinically currently used dual targets antidepressants (such as venlafaxine), said derivatives may have stronger antidepression effect, broader indications, faster onset and lower neurotoxicity and side reaction; and said derivatives have stronger antidepression activity, lower toxicity, higher bioavailability, longer half life and better druggablity, compared with aryl alkanol piperazine derivatives and optical isomers thereof disclosed in prior art.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: August 28, 2012
    Assignees: CSPC Zhonggi Pharmaceutical Technology (Shijiazhuang) Co. Ltd., Shanghai Institute of Pharmaceutical Industry
    Inventors: Jianqi Li, Na Lv, Hua Jin, Zhijie Weng, Yongyong Zheng
  • Kinesin inhibitors as cancer therapeutics
    Patent number: 8252832
    Abstract: The invention provides novel compounds having a substituted imidazole ring, and methods of using such compounds for the treatment of certain disorders such as hematological cancers and solid tumors. The compounds of the invention are tri-substituted imidazole derivatives that inhibit KSP. These compounds are also useful for the treatment of drug resistant tumors, such as solid tumors that express elevated levels of P-glycoprotein.
    Type: Grant
    Filed: November 25, 2008
    Date of Patent: August 28, 2012
    Assignee: Novartis AG
    Inventors: Tinya Abrams, Paul Barsanti, David Duhl, Michel Faure, Paul A. Renhowe, Annette Olga Walter
  • IL-12 modulatory compounds
    Patent number: 8236795
    Abstract: The invention relates to heterocyclic compounds, compositions including the compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.
    Type: Grant
    Filed: March 24, 2010
    Date of Patent: August 7, 2012
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Elena Kostik, Teresa Przewloka, Howard P. Ng, Dinesh Chimmanamada, Zachary Demko
  • Substituted aryl-indole compounds and their kynurenine/kynuramine-like metabolites as therapeutic agents
    Patent number: 8236858
    Abstract: This invention is directed to substituted aryl compounds, which are linked to a substituted indole moiety by various linkers, and the kynurenine/kynuramine-like metabolites of these agents, their preparation and pharmaceutical compositions containing these compounds. This invention further is directed to the pharmaceutical use of the compounds for inhibiting GSK3? kinase and/or modulating N-methyl-D-aspartate (NMDA) channel activities for the treatment of neurodegenerative and other disorders.
    Type: Grant
    Filed: August 3, 2011
    Date of Patent: August 7, 2012
    Assignee: Neurim Pharmaceuticals (1991) Ltd.
    Inventors: Tal Peleg-Shulman, Moshe Laudon, Dvorah Daily
  • Insecticidal compounds
    Patent number: 8236828
    Abstract: A compound of formula (I) wherein A1, A2, A3, A4, G1, G2, R1, R2, R3, R4, Q1, Y1, Y2, Y3 and Y4 are as defined in claim 1; or a salt or TV-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests.
    Type: Grant
    Filed: October 13, 2008
    Date of Patent: August 7, 2012
    Assignee: Syngenta Crop Protection LLC
    Inventors: Pierre Joseph Marcel Jung, Peter Renold, Christopher Richard Ayles Godfrey, William Lutz, Peter Maienfisch, Werner Zambach
  • Pyrrolo[2,3-d]pyrimidine derivatives; their intermediates and synthesis
    Patent number: 8232394
    Abstract: This invention relates to methods and intermediates useful for the synthesis of pyrrolo[2,3-d]pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.
    Type: Grant
    Filed: July 17, 2006
    Date of Patent: July 31, 2012
    Assignee: Pfizer Inc.
    Inventors: Sally Gut Ruggeri, Joel M. Hawkins, Teresa M. Makowski, Jennifer L. Rutherford, Frank J. Urban
  • Proteasome inhibitors
    Patent number: 8227503
    Abstract: Disclosed herein are compounds of Formula (I) that include a sulfonate ester, ester or ether group. Compounds of Formula (I) can be included in pharmaceutical compositions, and can be used to treating and/or ameliorating a disease or condition, such as cancer, a microbial disease and/or inflammation.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: July 24, 2012
    Assignee: Nereus Pharmaceuticals, Inc.
    Inventors: Venkat Rami Reddy Macherla, Barbara Christine Potts, Rama Rao Manam, Katherine A. McArthur, Ta-Hsiang Chao, Saskia Theodora Cornelia Neuteboom
  • Isoxazoles
    Patent number: 8227461
    Abstract: The present invention is concerned with novel isoxazole derivatives of formula I wherein X, R1, R2, R3, R4 and R5 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: April 23, 2010
    Date of Patent: July 24, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
  • Organic compounds
    Patent number: 8222248
    Abstract: The present invention provides compounds of the following structure; A-L1-B—C-D that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
    Type: Grant
    Filed: October 17, 2007
    Date of Patent: July 17, 2012
    Assignee: Novartis AG
    Inventors: Moo Je Sung, Gary Mark Coppola, Taeyoung Yoon, Thomas A. Gilmore
  • Isoindoline compounds and methods of their use
    Patent number: 8222249
    Abstract: Provided herein are isoindoline compounds, pharmaceutical compositions comprising one or more of such compounds, and methods of their use for treating, preventing, or managing various diseases.
    Type: Grant
    Filed: January 26, 2012
    Date of Patent: July 17, 2012
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Alexander L. Ruchelman
  • Compounds as lysophosphatidic acid receptor antagonists
    Patent number: 8217066
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Grant
    Filed: October 1, 2010
    Date of Patent: July 10, 2012
    Assignee: Amira Pharmaceuticals, Inc.
    Inventors: Thomas Jon Seiders, Lucy Zhao, Jeannie M. Arruda, Brian Andrew Stearns, Yen Pham Truong, Jill Melissa Scott, John Howard Hutchinson, Nicholas Simon Stock, Deborah Volkots