The Additional Hetero Ring Consists Of Carbon And Chalcogen As The Only Ring Members Patents (Class 514/263.23)
  • Patent number: 10166235
    Abstract: The solubility of kinetin and/or of zeatin is increased when either or both are combined in a formulation that includes a polyoxyalkylene-n-glycerol dicarboxylate component and a fatty acid component. These two components provide a synergistic increase in the solubility of kinetin and/or zeatin that is greater than that which would be expected based on the solubility of kinetin and zeatin in the individual components.
    Type: Grant
    Filed: March 26, 2018
    Date of Patent: January 1, 2019
    Assignee: Dow Pharmaceutical Sciences, Inc.
    Inventors: Pramod P. Sarpotdar, Sarmistha Basu, Varsha D. Bhatt, Yunik Chang, Gordon J. Dow
  • Patent number: 9649315
    Abstract: Compounds and compositions for treating disorders related to TRPA1 are described herein.
    Type: Grant
    Filed: March 9, 2015
    Date of Patent: May 16, 2017
    Assignee: Hydra Biosciences, Inc.
    Inventors: Howard Ng, Jianfeng Hang
  • Patent number: 9132130
    Abstract: Disclosed are: a novel purine derivative, a composition thereof, a method for treating tumor using the purine derivative, and an antitumor agent using the purine derivative. Specifically disclosed is a compound represented by formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof, or a prodrug thereof.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: September 15, 2015
    Assignee: ZENYAKU KOGYO KABUSHIKI KAISHA
    Inventors: Toshiaki Suzuki, Hideki Satoh, Toshiyuki Matsuno, Kenichi Saitoh, Soichi Ohta, Manami Masuda, Shinichi Yaguchi, Ichiro Koshimizu, Yuriko Watanabe, Yoshie Minowa, Masayuki Takahashi, Tomoyoshi Kayou
  • Patent number: 9096601
    Abstract: Arylamino purine derivatives represented by formula I and their preparation method are disclosed, wherein each substituent is defined as in the description. The derivatives have an inhibitory effect on non-small cell lung cancer with deletion mutation of exon 19 or L858R point mutation of exon 21 in epidermal growth factor receptor (EGFR).
    Type: Grant
    Filed: December 23, 2010
    Date of Patent: August 4, 2015
    Assignees: CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd., Sichuan University
    Inventors: Shengyong Yang, Yuquan Wei
  • Publication number: 20150105351
    Abstract: The present invention is directed to novel nanomolar and picomolar inhibitors of HIV reverse transcriptase, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV-1 and HIV-2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.
    Type: Application
    Filed: October 8, 2014
    Publication date: April 16, 2015
    Inventors: William L. Jorgensen, Karen S. Anderson
  • Patent number: 9006207
    Abstract: Compounds and compositions for treating disorders related to TRPA1 are described herein.
    Type: Grant
    Filed: January 8, 2013
    Date of Patent: April 14, 2015
    Assignee: Hydra Biosciences, Inc.
    Inventors: Howard Ng, Jianfeng Hang
  • Publication number: 20150087643
    Abstract: The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity; the compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.
    Type: Application
    Filed: October 10, 2014
    Publication date: March 26, 2015
    Applicant: Advinus Therapeutics Private Limited
    Inventors: Venkata Palle, Vidya Ramdas, Dinesh Barawkar, Sujay Basu, Summon Koul, Yogesh Waman, Meena Patel, Anil Panmand
  • Publication number: 20140378446
    Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Application
    Filed: January 30, 2013
    Publication date: December 25, 2014
    Applicant: Pharmacyclics, Inc.
    Inventors: Wei Chen, David J. Loury, Yan Shunqi, Longcheng Wang, Leah Lynn Frye
  • Publication number: 20140371244
    Abstract: The present invention relates to a method by use of a pharmaceutical composition for preventing or treating inflammatory disease, colorectal cancer and prostate cancer, which contains an A3 adenosine receptor agonist, 2-chloro-N6-(3-iodobenzyl)-4?-thioadenosine-5?-N-methyluronamide (thio-Cl-IB-MECA), N6-(3-iodobenzyl)-4?-thioadenosine-5?-N-methyluronamide (thio-IB-MECA), or a pharmaceutically acceptable salt thereof. The pharmaceutical composition of the invention is significantly less toxic than conventional A3 adenosine agonists, and thus is useful for prevention or treatment of inflammatory disease. In addition, it more selectively inhibits the growth of androgen receptor-dependent or independent prostate cancer cells than other A3 adenosine receptor agonists and thus is useful for prevention or treatment of colorectal cancer or prostate cancer.
    Type: Application
    Filed: February 28, 2014
    Publication date: December 18, 2014
    Applicant: Ewha University - Industry Collaboration Foundation
    Inventors: Lak Shin JEONG, Sang Kook LEE, Hwa Jin CHUNG, Hyuk Woo LEE
  • Publication number: 20140364446
    Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 1?,4?-thio nucleoside compounds which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human. In certain embodiments, the compounds are of Formula 3001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof; wherein Base, RA, RB, W, X, Y, and Z are as described herein.
    Type: Application
    Filed: June 4, 2014
    Publication date: December 11, 2014
    Inventors: David DUKHAN, Gilles GOSSELIN, Cyril B. DOUSSON
  • Publication number: 20140323441
    Abstract: The present invention relates to purine derivatives of formula (I), processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
    Type: Application
    Filed: November 8, 2012
    Publication date: October 30, 2014
    Inventors: Jean-François Bonfanti, Frédéric Marc Maurice Doublet, Werner Embrechts, Jérôme Michel Claude Fortin, David Craig Mc Gowan, Philippe Muller, Piere Jean-Marie Bernand Raboisson
  • Publication number: 20140271826
    Abstract: The solubility of kinetin and/or of zeatin is increased when either or both are combined in a formulation that includes a polyoxyalkylene-n-glycerol dicarboxylate component and a fatty acid component. These two components provide a synergistic increase in the solubility of kinetin and/or zeatin that is greater than that which would be expected based on the solubility of kinetin and zeatin in the individual components.
    Type: Application
    Filed: March 17, 2014
    Publication date: September 18, 2014
    Applicant: Dow Pharmaceutical Sciences, Inc.
    Inventors: Pramod Sarpotdar, Sarmistha Basu, Varsha D. Bhatt, Yunik Chang, Gordon J. Dow
  • Publication number: 20140275128
    Abstract: Provided herein are compounds of Formula I, compositions comprising an effective amount of a compound of Formula I, and methods for preventing, reducing or treating retinal ganglion cell damage comprising administering an effective amount of a purine derivative to a subject in need thereof.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: INOTEK PHARMACEUTICALS CORPORATION
    Inventor: William K. MCVICAR
  • Publication number: 20140275013
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite, such as Leishmaniasis, Human African Trypanosomiasis and Chagas disease.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicants: UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR COMMERCIALIZATION, IRM LLC
    Inventors: Arnab Kumar CHATTERJEE, Fang LIANG, Casey Jacob Nelson MATHISON, Pranab Kumar MISHRA, Valentina MOLTENI, Advait Suresh Nagle, Frantisek SUPEK, Liying Jocelyn TAN, Agnes VIDAL, Michael Herman GELB, Frederick Simmons BUCKNER, Hari Babu TATIPAKA, Neil Richard NORCROSS, John Robert GILLESPIE
  • Publication number: 20140243359
    Abstract: The compound 2-[1-(6-aminopurin-9-yl)-2-oxoethoxy]prop-2-enal of formula (I), its monohydrate of formula (II), or its corresponding cyclic monohydrate of formula (III), in which the stereochemical chiral center indicated with an asterisk can be R (Rectus), S (Sinister) or racemic, including the tautomers of the adenine ring and the pharmaceutically acceptable salts, are used in the treatment of inflammatory disorders or of pain disorders.
    Type: Application
    Filed: July 20, 2012
    Publication date: August 28, 2014
    Applicant: MEDESTEA RESEARCH & PRODUCTION S.P.A.
    Inventors: Giulia Federica Merizzi, Fabio Grassi, Antonio Soleti
  • Publication number: 20140235562
    Abstract: A method of treating an ocular disorder in a subject includes administering to the subject a therapeutically effective amount of an agent that modulates at least one target in a signaling cascade associated with light induced retinal degeneration, aberrant all-trans-retinal accumulation, and/or generation of reactive oxygen species (ROS).
    Type: Application
    Filed: April 25, 2014
    Publication date: August 21, 2014
    Inventors: Krzysztof Palczewski, Yu Chen
  • Patent number: 8791126
    Abstract: In the present invention, a novel 2-alkynyl-N9-propargyladenine represented by formula (I) wherein R1 represents a halogen atom, a furyl group, or a triazolyl group; R2 and R3 each represents a hydrogen atom or a C1-8 alkyl group, or form a cycloalkyl group by bonding to each other; and X represents a hydrogen atom or a hydroxyl group, or a pharmaceutically acceptable salt thereof, has a stronger and longer-lasting effect as a therapeutic agent for Parkinsonian syndromes.
    Type: Grant
    Filed: November 24, 2011
    Date of Patent: July 29, 2014
    Assignee: Yamasa Corporation
    Inventors: Kazuki Endo, Kohei Yamada, Kazuki Deguchi
  • Publication number: 20140100174
    Abstract: Treatment for Cancer Using A Preparation containing a combination of one or more Natural or Synthetic or a Combination of Natural and Synthetic Boswellic Acids and one or more Natural or Synthetic or a Combination of Natural and Synthetic Cytokinins such as Kinetin, Kinetin Riboside and other Cytokinins and (the Preparation) could also contain one or more Natural or Synthetic or a Combination of Natural and Synthetic plant growth hormones such as Auxins in any percentage ratio for Treating Cancer. The said Components of the said Preperation works by Inducing Apoptosis of the Cancerous cells, by “executing” them by Inducing Caspases-8 and other mechanisms.
    Type: Application
    Filed: October 4, 2012
    Publication date: April 10, 2014
    Inventor: Kingsley Yianomah Quartey
  • Publication number: 20140093566
    Abstract: Provided herein are pharmaceutical formulations, comprising 4-((9-((3S)-tetrahydro-3-furanyl)-8-((2,4,6-trifluorophenyl)amino)-9H-purin-2-yl)amino)-trans-cyclohexanol, including pharmaceutically acceptable salts, solvates, isomers, isotopologues, tautomers and racemic mixtures thereof, and a pharmaceutically acceptable excipient; and their use for treating or preventing disease.
    Type: Application
    Filed: November 8, 2013
    Publication date: April 3, 2014
    Applicant: Signal Pharmaceuticals, LLC
    Inventors: Sreenivas S. Bhat, Xiaozhong Liang, Anthony Tutino, Anthony Joseph Frank
  • Patent number: 8680076
    Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing scleroderma, keloids, UV injury, or sunburn, and methods for improving or preventing scar formation.
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: March 25, 2014
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Brydon L. Bennett, Brian Edwin Cathers, Kristen Lee Jensen-Pergakes, Heather Raymon, Weilin Xie, Jaman May Maroni
  • Publication number: 20140080846
    Abstract: A method of treating orphan respiratory disease.
    Type: Application
    Filed: September 14, 2012
    Publication date: March 20, 2014
    Inventors: William Wayne Howard, Russell Francis Somma
  • Publication number: 20140056922
    Abstract: A method is provided herein to increase an immune response to an antigen. The method includes administering an agent that inhibits extracellular adenosine or inhibits adenosine receptors. Also disclosed are methods to increase the efficacy of a vaccine and to increase an immune response to a tumor antigen or immune cell-mediated tumor destruction.
    Type: Application
    Filed: October 30, 2013
    Publication date: February 27, 2014
    Applicant: The United States of America,as represented by the Secretary, Department of Health and Human Service
    Inventors: Michail V. Sitkovsky, Akio Ohta
  • Patent number: 8623408
    Abstract: Provided are compositions of cladribine and cyclodextrin which are especially suited for the oral and buccal administration of cladribine.
    Type: Grant
    Filed: September 27, 2010
    Date of Patent: January 7, 2014
    Assignee: Ares Trading S.A.
    Inventor: Nicholas S Bodor
  • Patent number: 8603527
    Abstract: Provided herein are pharmaceutical formulations, comprising 4-((9-((3S)-tetrahydro-3-furanyl)-8-((2,4,6-trifluorophenyl)amino)-9H-purin-2-yl)amino)-trans-cyclohexanol, including pharmaceutically acceptable salts, solvates, isomers, isotopologues, tautomers and racemic mixtures thereof, and a pharmaceutically acceptable excipient; and their use for treating or preventing disease.
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: December 10, 2013
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Sreenivas S. Bhat, Xiaozhong Liang, Anthony Tutino, Anthony Joseph Frank
  • Patent number: 8575181
    Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, or C1-6alkoxy; m is an integer having a value of 3, 4, or 5; n is an integer having a value of 0 to 3; p is an integer having a value of 1 or 2 and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
    Type: Grant
    Filed: August 7, 2009
    Date of Patent: November 5, 2013
    Assignee: GlaxoSmithKline LLC
    Inventors: Sebastien Andre Campos, Diane Mary Coe, Naimisha Trivedi
  • Patent number: 8575182
    Abstract: Certain 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts of the general formula are provided wherein R6 and R9 are as defined in the specification. These 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts are useful in compositions for treating mammalian cells, and especially human skin cells, in order to ameliorate the adverse effects of aging, treat skin disease states, treat immunological responses resulting from or associated with inflammation, and the like.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: November 5, 2013
    Assignee: Institute of Experimental Botany, Academy of Sciences of the Czeck Republic
    Inventors: Lucie Szucova, Marek Zatloukal, Lukas Spichal, Jiri Voller, Karel Dolezal, Miroslav Strnad, Frank J. Massino
  • Publication number: 20130281517
    Abstract: Cyclopropanecarboxylate esters of purine analogues, method of making and using the same for treating herpes virus infections and tumors are disclosed.
    Type: Application
    Filed: April 2, 2013
    Publication date: October 24, 2013
    Inventors: Ji-Wang CHERN, Shin-yu LAI, Pei-Teh CHANG
  • Publication number: 20130244964
    Abstract: The present invention provides an isolated HIV-1 mutant and isolated nucleic acid molecules comprising HIV-RT coding sequences harboring a novel mutation in the S68 codon, and in particular, deletions of the S68 codon. This novel deletion reduces the sensitivity of HIV to various nucleoside reverse transcriptase inhibitors. Methods of using this mutation for selecting effective antiretroviral agents in vitro and in vivo, methods for monitoring infection progression in HIV-infected individuals and methods for avoiding the emergence of and/or to treat individuals infected with HIV comprising mutations, including deletions, at the S68 codon of HIV-RT are provided.
    Type: Application
    Filed: November 9, 2012
    Publication date: September 19, 2013
    Applicant: EMORY UNIVERSITY
    Inventor: Raymond F. Schinazi
  • Publication number: 20130245046
    Abstract: In the present invention, a novel 2-alkynyl-N9-propargyladenine represented by formula (I) wherein R1 represents a halogen atom, a furyl group, or a triazolyl group; R2 and R3 each represents a hydrogen atom or a C1-8 alkyl group, or form a cycloalkyl group by bonding to each other; and X represents a hydrogen atom or a hydroxyl group, or a pharmaceutically acceptable salt thereof, has a stronger and longer-lasting effect as a therapeutic agent for Parkinsonian syndromes.
    Type: Application
    Filed: November 24, 2011
    Publication date: September 19, 2013
    Applicant: YAMASA CORPORATION
    Inventors: Kazuki Endo, Kohei Yamada, Kazuki Deguchi
  • Patent number: 8492390
    Abstract: The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as ?-L-oxy-LNA, amino-LNA, ?-L-amino-LNA, thio-LNA, ?-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.
    Type: Grant
    Filed: December 23, 2011
    Date of Patent: July 23, 2013
    Assignee: Santaris Pharma A/S
    Inventors: Mads Detlef Sorensen, Jesper Wengel, Troels Koch, Signe M. Christensen, Christoph Rosenbohm, Daniel Sejer Pedersen
  • Publication number: 20130172340
    Abstract: In one aspect, the invention relates to substituted purine analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 22, 2011
    Publication date: July 4, 2013
    Applicant: University of Central Flordia Research Foundation,
    Inventors: James Turkson, Patrick Gunning
  • Publication number: 20130165427
    Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.
    Type: Application
    Filed: August 24, 2012
    Publication date: June 27, 2013
    Applicant: HYDRA BIOSCIENCES, INC.
    Inventor: Jayhong A. Chong
  • Publication number: 20130137694
    Abstract: There is provided modulators of Nrf2 protein which comprises a compound which binds at least one of the BTB domain, IVR domain and Kelch domain of Keap1 protein, activating or inhibiting Nrf2. There is also provided pharmaceutical compositions containing the modulators, as well as uses and method of use of the modulators for the treatment of conditions.
    Type: Application
    Filed: May 31, 2011
    Publication date: May 30, 2013
    Inventors: Gerald Batist, Jian Hui Wu
  • Publication number: 20130123280
    Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
    Type: Application
    Filed: November 1, 2012
    Publication date: May 16, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.
  • Publication number: 20130109704
    Abstract: This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.
    Type: Application
    Filed: December 19, 2012
    Publication date: May 2, 2013
    Applicant: NEUROSEARCH A/S
    Inventor: NeuroSearch A/S
  • Publication number: 20130072505
    Abstract: The present invention provides methods and compositions for countering the adverse effects of aging on mammalian cells in vitro and in vivo, especially human skin cells and human skin, and treatment of hyperproliferative and related skin diseases in mammals by administering compositions containing 6,9-disubstituted purine derivatives.
    Type: Application
    Filed: September 28, 2012
    Publication date: March 21, 2013
    Inventors: Lucie Szucova, Marek Zatioukai, Lukas Spichal, Ludek Frohich, Karel Dolezal, Miroslav Stmad, Frank J. Massino
  • Patent number: 8383634
    Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1, R3, R4, L, X, Y, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
    Type: Grant
    Filed: May 23, 2011
    Date of Patent: February 26, 2013
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Deborah Sue Mortensen, Maria Mercedes Delgado Mederos, John Joseph Sapienza, Ronald J. Albers, Steven Spencer Clareen, Kimberly Lyn Schwarz, Jason Simon Parnes, Jennifer R. Riggs, Patrick William Papa, Sayee Gajanan Hegde, Jeffrey Mark McKenna
  • Publication number: 20130034495
    Abstract: Provided herein are isotopologues of Compound 1, which are enriched with isotopes such as, for example, deuterium. Pharmaceutical compositions comprising the isotope-enriched compounds, and methods of using such compounds are also provided.
    Type: Application
    Filed: December 9, 2009
    Publication date: February 7, 2013
    Inventors: Marie Georges Beauchamps, Louise Michelle Cameron, Mohit Atul Kothare, Manohar T. Saindane
  • Publication number: 20120329816
    Abstract: This invention relates to methods for altering the splicing of mRNA in cells. In particular, this invention also relates to methods for increasing the ratio of wild type to misspliced forms of mRNA and corresponding encoded proteins in cells possessing a mutant gene encoding either the i) misspliced mRNA corresponding to the mutant protein or ii) a component in the splicing machinery responsible for processing the misspliced mRNA. In addition, this invention relates to treating individuals having a disorder associated with a misspliced mRNA, such as Familial Dysautonomia or Neurofibromatosis 1, by administering to such an individual a cytokinin such as kinetin.
    Type: Application
    Filed: August 31, 2012
    Publication date: December 27, 2012
    Applicant: The General Hospital Corporation
    Inventors: Susan A. Slaugenhaupt, James F. Gusella
  • Publication number: 20120329747
    Abstract: A patentable new class of hydrazone derivative compounds is described, as are methods for synthesizing such compounds. The hydrazones of the invention can be used, for example, as potent anti-cancer agents, including to inhibit the growth of cancer cells that exhibit multidrug resistance.
    Type: Application
    Filed: June 21, 2012
    Publication date: December 27, 2012
    Inventors: Hiremagular N. JAYARAM, Praveen KUSUMANCHI, Mario GRIFANTINI, Palmarisa FRANCHETTI, Loredana CAPPELLACCI, Riccardo PETRELLI
  • Publication number: 20120322815
    Abstract: The present invention relates to a pharmaceutical composition for preventing or treating inflammatory disease, colorectal cancer and prostate cancer, which contains an A3 adenosine receptor agonist, 2-chloro-N6-(3-iodobenzyl)-4?-thioadenosine-5?-N-methyluronamide (thio-Cl-IB-MECA), N6-(3-iodobenzyl)-4?-thioadenosine-5?-N-methyluronamide (thio-IB-MECA), or a pharmaceutically acceptable salt thereof. The pharmaceutical composition of the invention is significantly less toxic than conventional A3 adenosine agonists, and thus is useful for prevention or treatment of inflammatory disease. In addition, it more selectively inhibits the growth of androgen receptor-dependent or independent prostate cancer cells than other A3 adenosine receptor agonists and thus is useful for prevention or treatment of colorectal cancer or prostate cancer.
    Type: Application
    Filed: December 16, 2010
    Publication date: December 20, 2012
    Applicant: EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION
    Inventors: Lak Shin Jeong, Sang Kook Lee, Hwa Jin Chung, Hyuk Woo Lee
  • Publication number: 20120270887
    Abstract: Methods for inhibiting myopia are disclosed. A method for inhibiting myopia includes reducing a level of an intraocular cAMP in a subject. The level of the intraocular cAMP is reduced by injecting an adenylyl cyclase inhibitor to achieve the inhibition of myopia in the subject. In one method, the adenylyl cyclase inhibitor is SQ22536.
    Type: Application
    Filed: December 21, 2011
    Publication date: October 25, 2012
    Applicant: SCHOOL OF OPHTHALMOLOGY AND OPTOMETRY, WENZHOU MEDICAL COLLEGE
    Inventors: Xiangtian Zhou, Jia Qu, Yijin Tao, Miaozhen Pan
  • Publication number: 20120202785
    Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: February 8, 2012
    Publication date: August 9, 2012
    Inventors: Robert Heald, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Bohdan Waszkowycz
  • Patent number: 8236810
    Abstract: The invention 8-aminothioxanthines and the derivatives of formula I wherein the various R groups and substituents are comprised of a number of different (C1-C10)-alkyl, cycloalkyl, aryl, alkene, alkyne, etc. groups and derivatives thereof which are hereinafter more specifically defined for the treatment of metabolic disorders such as type-2 diabetes, hyperglycemia, arteriosclerotic diseases and the like.
    Type: Grant
    Filed: January 11, 2007
    Date of Patent: August 7, 2012
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Karl Schoenafinger, Gerhard Jaehne, Elisabeth Defossa, Guenter Billen, Christian Buning, Georg Tschank, Ulrich Werner
  • Publication number: 20120190697
    Abstract: HIV replication inhibitors of formula wherein -a1=a2-a3=a4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; -b1=b2-b3=b4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; n and m is 0-4, R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; —S(?O)pR6; C(?NH)R6; R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; —CH?N—NH—C(?O)—R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; —CH?N—NH—C(?O)—R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substituted
    Type: Application
    Filed: March 2, 2012
    Publication date: July 26, 2012
    Inventors: Jerôme Emile Georges GUILLEMONT, Mikaël Paugam, Bruno Francois Marie Delest, Jan Heeres, Paulus Joannes Lewi, Frank Xavier Jozef Herwig Arts
  • Publication number: 20120190666
    Abstract: The present invention provides compounds that are PIKK inhibitors, more specifically, mTOR and/or PI3K? kinase inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of kinases, specifically PI3 kinases, more specifically, mTOR and/or PI3K?, such as cancer. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Application
    Filed: May 12, 2010
    Publication date: July 26, 2012
    Applicant: Amgen Inc.
    Inventors: Christiane Bode, Alessandro Boezio, Alan C. Cheng, Deborah Choquette, James Robert Coats, Katrina Woodin Copeland, Hongbing Huang, Daniel La, Richard Thomas Lewis, Hongyu Liao, Michele Potashman, John Stellwagen, Shuyan Yi, Mark H. Norman, Markian M. Stec, Emily Anne Peterson, Russell Graceffa
  • Publication number: 20120172347
    Abstract: The present invention provides a compound represented by the formula (1) or a pharmaceutically acceptable salt thereof (wherein W represents a hydrogen atom, a halogen atom, or the others; A represents an alkyl group optionally substituted by aryl group or the others, an aryl group, or the others; and one of X and Y represents a di-substituted alkylaminocarbonyl group, or the others, and the other represents a hydrogen atom, an alkyl group, an alkylcarbonyl group, or the others); a medicament or a pharmaceutical composition for treatment or prophylaxis of FAAH-related diseases such as depression, anxiety disorder or pains, comprising the compound or the like as an active ingredient; a use of the compound or the like; and a method for treatment or prophylaxis using the compound or the like.
    Type: Application
    Filed: September 8, 2010
    Publication date: July 5, 2012
    Applicant: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Keiji Aachi, Yoko Nakai, Tomoyuki Furuta, Yuki Fujii
  • Publication number: 20120165288
    Abstract: This invention relates to novel compounds that are azapeptides, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel azapeptide compounds that are derivatives of the HIV protease inhibitor atazanavir sulfate. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering HIV protease inhibitors. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving atazanavir.
    Type: Application
    Filed: March 2, 2012
    Publication date: June 28, 2012
    Inventors: Scott L. Harbeson, Roger D. Tung
  • Publication number: 20120165350
    Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
    Type: Application
    Filed: December 21, 2011
    Publication date: June 28, 2012
    Inventors: Jeff Zablocki, Elfatih Elzein
  • Publication number: 20120141491
    Abstract: The subject application provides small compounds that are able to increase/enhance autophagy in various cells. These compounds are useful in augmenting existing treatments of various cancers, microbial/viral infections, and neurodegenerative diseases. Thus, the subject application also provides methods of treating various types of cancers, microbial/viral infections, and neurodegenerative diseases.
    Type: Application
    Filed: August 9, 2010
    Publication date: June 7, 2012
    Applicant: University of Florida Research Foundation Inc.
    Inventors: William A. Dunn, Debra Everton Akin, Brian Keith Law