Thiocarboxamides, (i.e., C(=s)-n) Patents (Class 514/599)
  • Patent number: 9603833
    Abstract: The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 25, 2015
    Date of Patent: March 28, 2017
    Assignee: R-Tech Ueno, Ltd.
    Inventors: Tatsuya Matsukawa, Kazuhiro Masuzaki, Akiko Kawasaki, Akiko Akasaka, Yosuke Kawai
  • Patent number: 9107955
    Abstract: Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C?Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ?O or ?S.
    Type: Grant
    Filed: January 25, 2010
    Date of Patent: August 18, 2015
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono
  • Patent number: 9090546
    Abstract: The present invention provides methods and processes for producing ?-fluoroalkyl ketones from non-fluoro ?-haloalkyl ketones using a fluorohydrogenate compound. In some embodiments, the fluorohydrogenate compound is an ionic liquid. One particular method of the invention utilizes a fluorohydrogenate ionic liquid compound of the formula: Q+[F.(HF)n], wherein Q+ is an onium cation and n is a number from 0 to 3.
    Type: Grant
    Filed: July 3, 2014
    Date of Patent: July 28, 2015
    Assignee: CoorsTek FluoroChemicals, Inc.
    Inventors: Rajendra P. Singh, Jerry Lynn Martin
  • Publication number: 20150080386
    Abstract: Disclosed are compounds and pharmaceutical compositions that are useful for treating a subject with a proliferative disorder, such as cancer. The disclosed compounds and pharmaceutical compositions are also useful for treating disorders responsive to Hsp70 induction and/or natural killer induction.
    Type: Application
    Filed: July 21, 2014
    Publication date: March 19, 2015
    Inventors: Keizo Koya, Teresa Kowalczyk Przewloka, Shoujun Chen, Jun Jiang
  • Publication number: 20150057357
    Abstract: Methods of treating a subject with cancer characterized by an impaired ability to repair oxidative DNA damage, comprising administering to the subject an effective amount of a bis(thiohydrazide amide) compound are provided.
    Type: Application
    Filed: January 4, 2013
    Publication date: February 26, 2015
    Inventors: Elizabeth Alli, James Ford
  • Publication number: 20150025042
    Abstract: Disclosed are compounds of formulae (I), (III), (IV), (VII), (X), (XI), (XII), (XIII) and (XIV), wherein the variables are as defined in the claims, and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: December 16, 2013
    Publication date: January 22, 2015
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Shoujun Chen, Keizo Koya, Zachary Demko, Lijun Sun
  • Patent number: 8916604
    Abstract: Provided herein are pharmaceutical compositions and methods for treating disorders characterized by reduced expression of anti-oxidative stress enzymes in a subject. In one aspect, the present invention provides a method for inducing expression of anti-oxidative stress enzymes in a subject in need thereof. The method includes administering to the subject a therapeutically effective amount of a demethylating agent. The demethylating agent includes a phytochemical that induces expression of Nrf2 and Nrf2-mediated genes expressing anti-oxidative stress. Such phytochemicals include indoles, such as 3,3?-diindolylmethane (DIM) and indole-3-carbinol (I3C), and isothiocyanates, such as phenethyl isothiocyanate (PEITC) and sulforaphane (SFN).
    Type: Grant
    Filed: May 31, 2012
    Date of Patent: December 23, 2014
    Assignee: Rutgers, The State University of New Jersey
    Inventor: Ah-Ng T. Kong
  • Publication number: 20140350115
    Abstract: At least 70% by weight of Compound 1 is the single crystalline form, Form A, Form C, or Form D, of the compound. A pharmaceutical composition comprises a pharmaceutically acceptable carrier or diluent, and compound 1, wherein at least 70% by weight of the compound is the single crystalline form, Form A, Form C, or Form D, of the compound. A method of treating a subject with cancer comprises administering to the subject an effective amount of compound 1 or the pharmaceutical composition.
    Type: Application
    Filed: January 27, 2014
    Publication date: November 27, 2014
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Elena Kostik, Lijun Sun, Joanna Dziewiszek, Jun Y. Choi
  • Publication number: 20140342999
    Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: May 19, 2014
    Publication date: November 20, 2014
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Lijun Sun, Jun Jiang
  • Patent number: 8859798
    Abstract: Provided herein are compositions of matter and pharmaceutical compositions thereof, for use in inhibiting the growth of various microbial pathogens, including bacteria, fungi, protozoa, and viral pathogens. Also provided herein are methods of treating microbial diseases/infections and cancer with the compositions. The compositions are additionally useful in wood preservation and food preservation by inhibition of microbial growth.
    Type: Grant
    Filed: July 6, 2007
    Date of Patent: October 14, 2014
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Arkady Mustaev, Natalia Kurepina
  • Patent number: 8853437
    Abstract: An object of the present invention is to provide a compound having a novel structure for overcoming the defects of conventional steroid agents and NSAIDs. It is found that the particular dihydroxy bodies of eicosapentaenoic acid and docosahexaenoic acid, which have not conventionally been known (11,18-dihydroxy eicosapentaenoic acid (11,18-diHEPE), 17,18-dihydroxy eicosapentaenoic acid (17,18-diHEPE) etc.), have activity of inhibiting neutrophil, thereby solving the object. The present invention unexpectedly remarkably inhibits infiltration into a tissue of, and activation of neutrophil found out at acute inflammation. The compound of the present invention is a compound which has not conventionally been known. Therefore, utility as a new therapeutic is provided.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: October 7, 2014
    Assignee: The University of Tokyo
    Inventors: Makoto Arita, Hiroyuki Arai, Yousuke Isobe, Ryo Taguchi
  • Publication number: 20140296343
    Abstract: Methods and compounds for treating neurological and other disorders are provided. Included is the administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for a TrkB receptor molecule.
    Type: Application
    Filed: March 31, 2014
    Publication date: October 2, 2014
    Inventors: Frank M. LONGO, Stephen M. MASSA, Sandeep GUPTA
  • Patent number: 8802725
    Abstract: The present invention is directed to a compound comprising a bis[thiohydrazide amide] or a deprotonated form thereof, complexed to a transition metal cation, wherein the bis[thiohydrazide amide] is represented by Structural Formula (I): or a prodrug, isomer, ester, salt, hydrate, solvate, polymorph or a deprotonated form thereof. The present invention also provides a pharmaceutical composition comprising a compound of the invention and method of use thereof.
    Type: Grant
    Filed: May 24, 2013
    Date of Patent: August 12, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Masazumi Nagai, Jianhua Shen
  • Patent number: 8785451
    Abstract: Disclosed are compounds of formula (IA), formula (IV) or formula (V), wherein the variables are as defined herein, and pharmaceutical compositions containing them which are useful for treating a subject with a proliferative disorder, such as cancer. The disclosed compounds and pharmaceutical compositions are also useful for treating disorders responsive to Hsp70 induction and/or natural killer induction.
    Type: Grant
    Filed: August 20, 2007
    Date of Patent: July 22, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Jun Jiang
  • Publication number: 20140113972
    Abstract: The present invention provides methods for the preselection of a subject for therapeutic treatment with elesclomol based on modulated levels of hypoxia in the subject. In one embodiment, the invention provides methods for the preselection of a subject for therapeutic treatment with elesclomol based on modulated levels of lactate dehydrogenase (LDH). The invention also provides methods for treating cancer in a subject by administering an effective amount of elesclomol to the subject, wherein the subject has a modulated level of hypoxia. The invention further provides kits to practice the methods of the invention.
    Type: Application
    Filed: December 27, 2013
    Publication date: April 24, 2014
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Ronald K. Blackman, Vojo Vukovic
  • Patent number: 8680100
    Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.
    Type: Grant
    Filed: December 1, 2009
    Date of Patent: March 25, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
  • Patent number: 8673980
    Abstract: This invention relates to the field of biologically active compounds and specifically to closthioamides, pharmaceutical compositions comprising these compounds, and their use as antibiotic, antifungal, and/or cytotoxic agent.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: March 18, 2014
    Assignee: Leibniz-Institut fuer Naturstoff-Forschung und Infektionsbiologie
    Inventors: Swantje Behnken, Hans-Martin Dahse, Christian Hertweck, Keishi Ishida, Thorger Lincke, Martin Roth, Florian Kloss
  • Patent number: 8637575
    Abstract: The present invention provides new tyrphostin derivatives acting as protein kinase (PK) and receptor kinase (RK) signaling modulators. The invention further provides methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for preventions and treatments of PK and RK related disorders such as metabolic, inflammatory, fibrotic, and cell proliferative disorders, in particular cancer.
    Type: Grant
    Filed: June 7, 2009
    Date of Patent: January 28, 2014
    Assignee: Novotyr Therapeutics Ltd.
    Inventors: Hadas Reuveni, Alexander Levitzki, Revital Sasson, Andre C. B. Lucassen
  • Patent number: 8637704
    Abstract: At least 70% by weight of Compound 1 is the single crystalline form, Form A, Form C, or Form D, of the compound. A pharmaceutical composition comprises a pharmaceutically acceptable carrier or diluent, and compound 1, wherein at least 70% by weight of the compound is the single crystalline form, Form A, Form C, or Form D, of the compound. A method of treating a subject with cancer comprises administering to the subject an effective amount of compound 1 or the pharmaceutical composition.
    Type: Grant
    Filed: November 28, 2008
    Date of Patent: January 28, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Elena Kostik, Lijun Sun, Joanna Dziewiszek, Jun Y. Choi
  • Publication number: 20140018422
    Abstract: Disclosed herein are derivatives of tetracaine that, among other things, block cyclic nucleotide gated (CNG) channels and are useful in the treatment of diseases characterized by overactive CNG channels such as retinal degeneration diseases.
    Type: Application
    Filed: December 14, 2012
    Publication date: January 16, 2014
    Inventors: Jeffrey Karpen, Sarah Kirk, Adriana Andrade, Michelle Schaffer, Kenneth Melich
  • Patent number: 8623921
    Abstract: Disclosed herein are compositions comprising a compound represented by structural formula (I): 2 g of which is reconstitutable in 10 mL of a water in less than 10 minutes, and methods for preparing these compositions. Also disclosed are compositions comprising a compound represented by structural formula (I) and a pharmaceutically acceptable excipient, wherein the molar ratio of said compound to said excipient is from 1:20 to 1:1, and methods for preparing these compositions.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: January 7, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Walter J. Lunsmann, Ninad Deshpanday
  • Patent number: 8609730
    Abstract: This invention provides REL inhibitors which interfere with the DNA binding capacity of a REL protein. Additionally this invention provides methods of treating, abrogating, or preventing diseases which respond with a positive clinical score to a REL inhibitor. Methods of identifying REL inhibitor based on a REL protein three dimensional model are described.
    Type: Grant
    Filed: January 7, 2009
    Date of Patent: December 17, 2013
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Youhai H. Chen, Ramachandran Murali, Jing Sun
  • Patent number: 8581004
    Abstract: Disclosed are compounds of Formula (I) and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: November 12, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Teresa Kowalczyk-Przewloka, Lijun Sun
  • Publication number: 20130289122
    Abstract: Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly useful for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases.
    Type: Application
    Filed: March 11, 2013
    Publication date: October 31, 2013
    Inventor: Newron Pharmaceuticals S.P.A.
  • Patent number: 8563533
    Abstract: The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: October 22, 2013
    Assignee: Trustees of Tufts College
    Inventors: William W. Bachovchin, Hung-sen Lai, Wengen Wu
  • Patent number: 8536227
    Abstract: The present invention provides new tyrphostin derivatives acting as protein kinase (PK) and receptor kinase (RK) signaling modulators. The invention further provides methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for preventions and treatments of PK and RK related disorders such as metabolic, inflammatory, fibrotic, and cell proliferative disorders, in particular cancer.
    Type: Grant
    Filed: June 7, 2009
    Date of Patent: September 17, 2013
    Assignee: Novotyr Therapeutics Ltd.
    Inventors: Hadas Reuveni, Alexander Levitzki, Revital Sasson, Andre C. B. Lucassen
  • Patent number: 8507493
    Abstract: The present invention relates to inhibitors of 11-?-hydroxysteroid dehydrogenase type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.
    Type: Grant
    Filed: April 20, 2010
    Date of Patent: August 13, 2013
    Assignee: AbbVie Inc.
    Inventors: Sridhar Peddi, Meena V. Patel, Jeffrey J. Rohde
  • Patent number: 8481599
    Abstract: Compositions and methods for treating, preventing, or reducing alcoholism, in particular methods for increasing patient compliance with therapies that require the intake of an ALDH inhibitor comprising the step of administering a monoamine oxidase B inhibitor.
    Type: Grant
    Filed: December 30, 2011
    Date of Patent: July 9, 2013
    Assignee: Tonix Pharmaceuticals Inc.
    Inventor: Seth Lederman
  • Publication number: 20130150440
    Abstract: Improved cancer treatments with bis[thiohydrazide amide] compounds such as elesclomol, in particular for identifying patient populations that would benefit from such treatments.
    Type: Application
    Filed: April 20, 2011
    Publication date: June 13, 2013
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Masazumi Nagai, Ronald K. Blackman, Patricia E. Rao, Yumiko Wada, Keizo Koya
  • Publication number: 20130149392
    Abstract: The present invention is a method for treating non-small cell lung cancer in a subject in need thereof, comprising administering to the subject an effective amount of a bis(thiohydrazideamide) compound of formula (I): wherein the variables are defined herein. Furthermore, pharmaceutical compositions, combination therapies, and uses thereof are also provided in the present application.
    Type: Application
    Filed: December 12, 2011
    Publication date: June 13, 2013
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Wei Guo, Vojo Vukovic
  • Patent number: 8461199
    Abstract: The present invention is directed to a compound comprising a bis[thiohydrazide amide] or a deprotonated form thereof, complexed to a transition metal cation, wherein the bis[thiohydrazide amide] is represented by Structural Formula (I): or a prodrug, isomer, ester, salt, hydrate, solvate, polymorph or a deprotonated form thereof. The present invention also provides a pharmaceutical composition comprising a compound of the invention and method of use thereof.
    Type: Grant
    Filed: October 21, 2009
    Date of Patent: June 11, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Nagai Masazumi, Jianhua Shen
  • Patent number: 8461208
    Abstract: Disclosed are bis(thio-hydrazide amide) disalts and pharmaceutical compositions thereof. Also disclosed are methods of using bis(thio-hydrazide amide) disalts to treat cancer.
    Type: Grant
    Filed: October 14, 2011
    Date of Patent: June 11, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Keizo Koya, Lijun Sun, Elena Kostik, Farid Vaghefi, Shoujun Chen, Noriaki Tatsuta, Guiqing Liang, Takayo Inoue, Zhi-Qiang Xia
  • Patent number: 8394858
    Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: November 30, 2010
    Date of Patent: March 12, 2013
    Assignee: Novartis AG
    Inventors: David Barnes, Gregory Raymond Bebernitz, Scott Louis Cohen, Robert Edson Damon, Robert Francis Day, Monish Jain, Rajeshri Ganesh Karki, Louise Clare Kirman, Tajesh Jayprakash Patel, Brian Kenneth Raymer, Herbert Franz Schuster, Wei Zhang
  • Publication number: 20120270940
    Abstract: This invention relates to the field of biologically active compounds and specifically to closthioamides, pharmaceutical compositions comprising these compounds, and their use as antibiotic, antifungal, and/or cytotoxic agent.
    Type: Application
    Filed: November 2, 2010
    Publication date: October 25, 2012
    Applicant: LELBUIZ-INSTITUT FUR NATURSTOFF-FORSCHUNG UND INFE
    Inventors: Swantje Behnken, Hans-Martin Dahse, Christian Hertweck, Keishi Ishida, Thorger Lincke, Martin Roth, Florian Kloss
  • Publication number: 20120128580
    Abstract: The present invention provides methods for the preselection of a subject for therapeutic treatment with elesclomol based on modulated levels of hypoxia in the subject. In one embodiment, the invention provides methods for the preselection of a subject for therapeutic treatment with elesclomol based on modulated levels of lactate dehydrogenase (LDH). The invention also provides methods for treating cancer in a subject by administering an effective amount of elesclomol to the subject, wherein the subject has a modulated level of hypoxia. The invention further provides kits to practice the methods of the invention.
    Type: Application
    Filed: November 18, 2011
    Publication date: May 24, 2012
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Ronald K. Blackman, Vojo Vukovic
  • Publication number: 20120083528
    Abstract: The present invention provides new tyrphostin derivatives acting as protein tyrosine kinase (PTK) inhibitors and receptor tyrosine kinase (RTK) inhibitors, and/or which directly or indirectly affect proteins in the PTK-mediated signal transduction pathway, methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for preventions and treatments of PTK and RTK related disorders such as metabolic, fibrotic, and cell proliferative disorders, in particular psoriasis and cancer.
    Type: Application
    Filed: November 10, 2011
    Publication date: April 5, 2012
    Applicant: NOVOTYR THERAPEUTICS LTD.
    Inventors: Hadas Reuveni, Alexander Levitzki, Lilach Steiner, Revital Sasson, Iris Ben-David, Avi Weissberg
  • Patent number: 8148426
    Abstract: A method of treating a Hsp70-responsive disorder in a subject includes administering to the subject an effective amount of a compound represented by Structural Formula I, or a pharmaceutically acceptable salt or solvate thereof. Y is a covalent bond or an optionally substituted straight chained hydrocarbyl group, or, Y, taken together with both >C?Z groups to which it is bonded, is an optionally substituted aromatic group. R1-R4 are independently —H, an optionally substituted aliphatic group, an optionally substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. R7-R8 are independently —H, an optionally substituted aliphatic group, or an optionally substituted aryl group. Z is O or S.
    Type: Grant
    Filed: November 17, 2005
    Date of Patent: April 3, 2012
    Assignee: Synta Pharmaceuticals Corp.
    Inventor: James Barsoum
  • Publication number: 20120065206
    Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.
    Type: Application
    Filed: December 1, 2009
    Publication date: March 15, 2012
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
  • Publication number: 20120035266
    Abstract: Disclosed are bis(thio-hydrazide amide) disalts and pharmaceutical compositions thereof. Also disclosed are methods of using bis(thio-hydrazide amide) disalts to treat cancer.
    Type: Application
    Filed: October 14, 2011
    Publication date: February 9, 2012
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Keizo KOYA, Lijun Sun, Elena Kostik, Farid Vaghefi, Shoujun Chen, Noriaki Tatsuta, Guiqing Liang, Takayo Inoue, Zhi-Qiang Xia
  • Publication number: 20120030779
    Abstract: Disclosed herein is a non-human animal model of protein aggregation cardiomyopathy. Also disclosed are compo-sitions and methods of treating or preventing a condition in a subject caused or exacerbated by reductive stress. Also disclosed are compositions and methods of predicting, detecting, or monitoring reductive stress in a subject.
    Type: Application
    Filed: January 18, 2008
    Publication date: February 2, 2012
    Applicant: UNIVERSITY OF UTAH RESEARCH FOUNDTION
    Inventors: Ivor J. Benjamin, Namakkal S. Rajasekaran, Thomas P. Kennedy
  • Patent number: 8093300
    Abstract: Compositions and methods for treating, preventing, or reducing alcoholism, in particular methods for increasing patient compliance with therapies that require the intake of an ALDH inhibitor comprising the step of administering a monoamine oxidase B inhibitor.
    Type: Grant
    Filed: June 25, 2008
    Date of Patent: January 10, 2012
    Assignee: Krele Pharmaceuticals, Inc.
    Inventor: Seth Lederman
  • Publication number: 20120004310
    Abstract: Methods and compounds for treating neurological and other disorders are provided. Included is the administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for a TrkB receptor molecule.
    Type: Application
    Filed: May 27, 2011
    Publication date: January 5, 2012
    Inventors: Frank M. LONGO, Stephen M. Massa, Sandeep Gupta
  • Publication number: 20110286927
    Abstract: In one aspect, the invention relates to a method for identifying a drug candidate with activity as a neuroprotective agent. The method includes determining whether a compound reduces ATF4 activity; and identifying the compound that reduces ATF4 activity as a drug candidate.
    Type: Application
    Filed: August 4, 2008
    Publication date: November 24, 2011
    Applicant: CORNELL UNIVERSITY
    Inventor: Rajiv R. Ratan
  • Publication number: 20110288162
    Abstract: The present invention is directed to a compound comprising a bis[thiohydrazide amide] or a deprotonated form thereof, complexed to a transition metal cation, wherein the bis[thio-hydrazide amide] is represented by Structural Formula (I): or a prodrug, isomer, ester, salt, hydrate, solvate, polymorph or a deprotonated form thereof. The present invention also provides a pharmaceutical composition comprising a compound of the invention and method of use thereof.
    Type: Application
    Filed: October 21, 2009
    Publication date: November 24, 2011
    Applicant: SYNTA PHARMACEUTICAL CORP
    Inventors: Nagai Masazumi, Jianhua Shen
  • Patent number: 8048925
    Abstract: Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R1-R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Z is —O or —S. M+ is a pharmaceutically acceptable monovalent cation and M2+ is a pharmaceutically acceptable divalent cation. Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.
    Type: Grant
    Filed: August 30, 2010
    Date of Patent: November 1, 2011
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Keizo Koya, Lijun Sun, Elena Kostik, Farid Vaghefi, Shoujun Chen, Noriaki Tatsuta, Guiqing Liang, Takayo Inoue, Zhi-Qiang Xia
  • Publication number: 20110245262
    Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: August 20, 2007
    Publication date: October 6, 2011
    Inventors: Lijun Sun, Keizo Koya, Shoujun Chen, Zachary Demko, Zhi-Qiang Xia
  • Publication number: 20110196025
    Abstract: At least 70% by weight of Compound 1 is the single crystalline form, Form A, Form C, or Form D, of the compound. A pharmaceutical composition comprises a pharmaceutically acceptable carrier or diluent, and compound 1, wherein at least 70% by weight of the compound is the single crystalline form, Form A, Form C, or Form D, of the compound. A method of treating a subject with cancer comprises administering to the subject an effective amount of compound 1 or the pharmaceutical composition.
    Type: Application
    Filed: November 28, 2008
    Publication date: August 11, 2011
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Elena I. Kostik, Lijun Sun, Joanna Dziewiszek, Jun Y. Choi
  • Publication number: 20110177085
    Abstract: The present invention relates to bitter-taste receptors and their role in bitter taste transduction. The invention also relates to assays for screening molecules that modulate, e.g. suppress or block, bitter taste transduction, or enhance bitter taste response.
    Type: Application
    Filed: March 25, 2011
    Publication date: July 21, 2011
    Inventors: Bernd Bufe, Thomas Hofmann, Dietmar Krautwurst, Christina Kuhn, Wolfgang Meyerhof
  • Patent number: RE42889
    Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: April 23, 2007
    Date of Patent: November 1, 2011
    Assignee: G.D. Searle LLC
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
  • Patent number: RE43802
    Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: September 21, 2011
    Date of Patent: November 13, 2012
    Assignee: G.D. Searle LLC
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz