The Nitrogen Is Bonded Directly At 4- Or 6-position Patents (Class 544/317)
  • Patent number: 10385089
    Abstract: Disclosed are a compound and a pharmaceutical composition that exhibit an excellent drug efficacy against a tumor, in particular a tumor which has acquired resistance to gemcitabine. Specifically, provided is a thionucleoside derivative represented by General (in the formula, R1 represents a hydroxyl group which may be protected, a C1-20 alkoxy group which may be substituted, or the like; R2 represents a C1-20 alkoxy group which may be substituted, a C3-8 cycloalkoxy group which may be substituted, or the like; and R3 represents a hydrogen atom or the like); or a salt thereof. Further, provided is a pharmaceutical composition containing such a thionucleoside derivative or a salt thereof.
    Type: Grant
    Filed: July 17, 2018
    Date of Patent: August 20, 2019
    Assignee: FUJIFILM Corporation
    Inventors: Hidenobu Kuniyoshi, Daisuke Nakagawa, Takuya Matsumoto, Yuji Yoshimitsu
  • Patent number: 9981961
    Abstract: Provided herein are compounds that bind to dCK and methods for treating cancer.
    Type: Grant
    Filed: January 31, 2017
    Date of Patent: May 29, 2018
    Assignees: The Regents of the University of California, The Board of Trustees of the University of Illinois
    Inventors: Caius G. Radu, Zheng Li, Raymond M. Gipson, Jue Wang, Nagichettiar Satyamurthy, Arnon Lavie, Jennifer M. Murphy, David A. Nathanson, Michael E. Jung
  • Patent number: 9598404
    Abstract: Provided herein are compounds that bind to dCK and methods for treating cancer.
    Type: Grant
    Filed: January 11, 2016
    Date of Patent: March 21, 2017
    Assignees: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Caius G. Radu, Zheng Li, Raymond M. Gipson, Jue Wang, Nagichettiar Satyamurthy, Arnon Lavie, Jennifer M. Murphy, David A. Nathanson, Michael E. Jung
  • Patent number: 9505720
    Abstract: The present invention relates to novel compounds of general formula: and to the cosmetic or pharmaceutical use thereof.
    Type: Grant
    Filed: May 8, 2015
    Date of Patent: November 29, 2016
    Assignee: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Cédric Poinsard, Pascal Collette, Jean-Michel Linget, Sandrine Rethore, Pascale Mauvais
  • Patent number: 9447051
    Abstract: This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit RSV infection and/or replication; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: September 20, 2016
    Assignee: AbbVie Inc.
    Inventors: Tatyana Dekhtyar, Arthur Gomtsyan, M-Akhteruzzaman Molla, Anil Vasudevan, Iok Chan Ng, Mikhail Chafeev
  • Patent number: 9321734
    Abstract: This present disclosure is related to the field of to N-(substituted)-5-fluoro-4-imino-3-methyl-2-oxo-3,4-dihydropyrimidine-1(2H)-carboxamide compounds and their derivatives and to the use of these compounds as fungicides. This application claims the benefit of U.S. Provisional Patent Application Ser. No. 61/746,837 filed Dec. 28, 2012, which is expressly incorporated by reference herein. Background and Summary of the Invention Fungicides are compounds, of natural or synthetic origin, which act to protect and/or cure plants against damage caused by agriculturally relevant fungi. Generally, no single fungicide is useful in all situations. Consequently, research is ongoing to produce fungicides that may have better performance, are easier to use, and cost less.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: April 26, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Beth Lorsbach, W. John Owen, Lindsay Stelzer, Chenglin Yao
  • Patent number: 9067929
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: June 30, 2015
    Assignee: CELGENE AVILOMICS RESEARCH, INC.
    Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter
  • Publication number: 20150139905
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Application
    Filed: October 9, 2014
    Publication date: May 21, 2015
    Inventors: Dinesh Chimmanamada, Weiwen Ying
  • Patent number: 9024022
    Abstract: The invention relates to compounds of formula (I?): in which A, L2, M and B are as defined in the description. These compounds are substrates of O6-alkylguanine-DNA alkyltransferase and mutants thereof.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: May 5, 2015
    Assignee: Cis Bio International
    Inventors: Emmanuel Bourrier, Michel Laget, Laurent Lamarque, Norbert Tinel, Eric Trinquet, Hervé Bazin
  • Publication number: 20150111851
    Abstract: This present disclosure is related to the field of 5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Inventors: Timothy Boebel, Kristy Bryan, Peter Lee Johnson, Beth Lorsbach, Kevin G. Meyer, W. John Owen, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao
  • Patent number: 9006259
    Abstract: This present disclosure is related to the field of N1-sulfonyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: April 14, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Timothy A. Boebel, Kristy Bryan, Beth Lorsbach, Timothy P. Martin, W. John Owen, Mark A. Pobanz, Scott Thornburgh, Jeffery D. Webster, Chenglin Yao
  • Publication number: 20150099743
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: Hui LI, Seiji NUKUI, Stephanie Anne SCALES, Min TENG, Chunfeng YIN
  • Patent number: 9000160
    Abstract: 2-Amino-5,8-dialkoxy[1,2,4]-triazolo[1,5-c]pyrimidines are manufactured from 4-chloro-2,5-dialkoxypyrimidines in a process that avoids hydrazine and cyanogen halide.
    Type: Grant
    Filed: September 10, 2013
    Date of Patent: April 7, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Douglas C. Bland, Gary Roth, Craig Bott, Christopher T. Hamilton, Joseph Neuman
  • Patent number: 9000002
    Abstract: This present disclosure is related to the field of N1-substituted-5-fluoro-2-oxopyrimidinone-1-(2H)-carboxamides and their derivatives and to the use of these compounds as fungicides.
    Type: Grant
    Filed: September 12, 2013
    Date of Patent: April 7, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Timothy A. Boebel, Kristy Bryan, Beth Lorsbach, Timothy P. Martin, W. John Owen, Mark A. Pobanz, Scott Thornburgh, Jeffery D. Webster, Chenglin Yao
  • Patent number: 8975250
    Abstract: The present invention relates to 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives having Formula (I) as defined herein, their preparation and their therapeutic use.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: March 10, 2015
    Assignee: SANOFI
    Inventors: Philippe Beauverger, Guillaume Begis, Sandrine Biscarrat, Olivier Duclos, Gary McCort
  • Patent number: 8952028
    Abstract: Methods of treating or preventing chemoresistance or relapse growth of cancer cells are provided. Methods of treating or preventing resistance to tyrosine kinase based chemotherapeutic treatment in hematologic and solid tumors are provided. BCR-ABL drug resistance in chronic myelogenous leukemia (CML) and models for conducting further study on the same are presented. The methods comprise administering a therapeutically effective amount of one or more SIRT1 modulators to the cells or subject in need thereof. The methods may be administered in combination with, prior to or subsequent to chemotherapy or may be administered to counteract the effect of a spontaneous genetic mutation. Methods of using SIRT1 inhibitors to treat or prevent insulin and transferrin-induced resistance are also presented. A novel cell model to study mechanisms of acquired chemoresistance is also provided.
    Type: Grant
    Filed: February 5, 2008
    Date of Patent: February 10, 2015
    Assignee: City of Hope
    Inventor: Wenyong Chen
  • Patent number: 8952018
    Abstract: A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl; -2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, with a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf is beneficial, eg. cancer.
    Type: Grant
    Filed: March 5, 2014
    Date of Patent: February 10, 2015
    Assignee: GlaxosmithKline LLC
    Inventors: Melissa Dumble, Rakesh Kumar, Sylvie Laquerre, Peter Lebowitz
  • Patent number: 8946242
    Abstract: Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an effective amount of a spiro[2.4]heptane as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier, are provided. The spiro[2.4]heptane compounds either possess antiviral activity, or are metabolized to a compound that exhibits such activity.
    Type: Grant
    Filed: January 23, 2014
    Date of Patent: February 3, 2015
    Assignee: University of Georgia Research Foundation, Inc.
    Inventor: Chung K. Chu
  • Patent number: 8933090
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I); wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them. Formula (I), wherein A represents O or N(R1); Y represents a group of formula, or wherein the left bond is attached to the A group and the right bond is attached to the R group; R represents a substituted or unsubstituted C5-C10aryl, substituted or unsubstituted hetero-C5-C10aryl, a group N(R1)(R4), or a group N(R2)(CHP3R4); R represent a hydrogen, C1-C4alkyl, or CF3; R2 represents hydrogen, C1-C4alkyl, or CF3; R3 represents hydrogen, C1-C4alkyl, or CF3; R4 represents a substituted or unsubstituted C5-C10 aryl or a substituted or unsubstituted C5-C10heteroaryl; in free base or acid addition salt form.
    Type: Grant
    Filed: October 19, 2010
    Date of Patent: January 13, 2015
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Werner Müller, Bernard Lucien Roy, Thomas J. Troxler, Konstanze Hurth, Mathias Frederiksen
  • Publication number: 20150011512
    Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.
    Type: Application
    Filed: September 12, 2014
    Publication date: January 8, 2015
    Inventors: Steven Albert Everett, Saraj Ulhaq
  • Publication number: 20150005498
    Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific triazolopyrimidine compounds and intermediates thereof as well as related derivatives, suitable for the preparation of Ticagrelor (TCG).
    Type: Application
    Filed: September 14, 2012
    Publication date: January 1, 2015
    Applicant: Lek Pharmaceuticals d.d.
    Inventors: Nened Maras, Borut Zupancic
  • Patent number: 8921384
    Abstract: Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an effective amount of a spiro[2.4]heptane as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier, are provided. The spiro[2.4]heptane compounds either possess antiviral activity, or are metabolized to a compound that exhibits such activity.
    Type: Grant
    Filed: January 23, 2014
    Date of Patent: December 30, 2014
    Assignee: Unversity of Georgia Research Foundation, Inc.
    Inventor: Chung K. Chu
  • Publication number: 20140378305
    Abstract: Compounds of formula wherein the substituents are as defined in claim 1, and related compositions, methods of use and processes of preparation.
    Type: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Applicant: SYNGENTA LIMITED
    Inventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
  • Patent number: 8916579
    Abstract: This present disclosure is related to the field of 5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: December 23, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Timothy A. Boebel, Kristy Bryan, Peter L. Johnson, Beth Lorsbach, Timothy P. Martin, Kevin G. Meyer, W. John Owen, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao
  • Publication number: 20140371449
    Abstract: The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor.
    Type: Application
    Filed: December 20, 2012
    Publication date: December 18, 2014
    Applicant: Lek Pharmaceuticals d.d.
    Inventors: Nenad Maras, Ivana Gazic Smilovic, Damjan Sterk
  • Patent number: 8912207
    Abstract: This present disclosure is related to the field of 2-aldoximino-5-fluoropyrimidines and their derivatives and to the use of these compounds as fungicides.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: December 16, 2014
    Assignee: Dow AgroSciences, LLP.
    Inventors: Timothy A. Boebel, Beth Lorsbach, Timothy P. Martin, W. John Owen, Michael T. Sullenberger, Chenglin Yao
  • Patent number: 8889860
    Abstract: The present invention relates generally to 3?-OH unblocked, labeled and unlabeled nucleotides and nucleosides with 5-methoxy-substituted nitrobenzyl-based photocleavable terminating groups for use in methods and systems related to DNA and RNA sequencing and analysis. These compounds, which may be represented by the following formulas: wherein the variables are defined herein, may be used as reversible terminators as they exhibit fast nucleotide incorporation kinetics, single-base termination, high nucleotide selectivity, and rapid terminating group cleavage that results in a naturally occurring nucleotide.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: November 18, 2014
    Assignee: Lasergen, Inc.
    Inventors: Brian Stupi, Hong Li, Weidong Wu, Megan N. Hersh, David Hertzog, Sidney E. Morris, Michael L. Metzker
  • Patent number: 8889741
    Abstract: Disclosed herein are therapeutic agents and/or preventive agents for pain or therapeutic agents and/or preventive agents for a sodium channel associated disease.
    Type: Grant
    Filed: January 31, 2013
    Date of Patent: November 18, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Tsuyoshi Shinozuka, Hiroyuki Kobayashi, Sayaka Suzuki, Kyosuke Tanaka, Hiroko Kimoto, Yuki Domon
  • Patent number: 8865731
    Abstract: Provided are: an agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), which comprises a compound having adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof as an active ingredient; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance or constipation; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance; and the like.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: October 21, 2014
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Jun Ouchi, Shunji Kunori, Yozo Kojima, Katsumi Shinoda, Katsutoshi Sasaki, Shiro Shirakura
  • Publication number: 20140303137
    Abstract: The present invention relates to compounds useful as inhibitors of Aurora 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: Application
    Filed: April 5, 2013
    Publication date: October 9, 2014
    Inventors: Michael Mortimore, Julian Golec, Daniel Robinson, John Studley
  • Publication number: 20140303139
    Abstract: The present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A1, X, A2, W1, W2, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
    Type: Application
    Filed: August 31, 2012
    Publication date: October 9, 2014
    Inventors: Chiyou Ni, Laykea Tafesse, Jiangcho Yao, Mark Youngman, Minnie Park, Bin Shao
  • Publication number: 20140275536
    Abstract: The use of compounds in the treatment of skin disorders is described. In particular, use of a compound of formula (I): or one of its pharmaceutically acceptable salts, solvates or hydrates in the preparation of a medicament to treat skin pathologies is described.
    Type: Application
    Filed: December 22, 2010
    Publication date: September 18, 2014
    Applicant: Galderma Research & Development
    Inventor: Cédric Poinsard
  • Publication number: 20140275537
    Abstract: Processes for the preparation of 4-amino-1-((1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-hydroxymethyl-cyclopent-2-enyl)-1H-pyrimidin-2-one (13, RX-3117) and its intermediates are described.
    Type: Application
    Filed: March 17, 2014
    Publication date: September 18, 2014
    Applicant: Rexahn Pharmaceuticals, Inc.
    Inventors: Haifeng YIN, Deog Joong KIM, Eliezer FALB, Leigh Andre PEARCEY, Jonathan CUMMINS, Petra DIETERICH, Jean-Francois CARNIAUX
  • Patent number: 8835450
    Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-furancarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: September 16, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Melissa Dumble, Tona Gilmer, Rakesh Kumar, Peter F. Lebowitz, Shannon Renae Morris, Sylvie Laquerre
  • Publication number: 20140256708
    Abstract: The present invention is directed to substituted azetidinecompounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: October 1, 2012
    Publication date: September 11, 2014
    Inventors: Christopher D. Cox, Douglas C. Beshore, June J. Kim, Scott D. Kuduk, Carol A. McVean, Thomas Reger, Justin T. Sheen
  • Publication number: 20140249135
    Abstract: New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
    Type: Application
    Filed: May 9, 2014
    Publication date: September 4, 2014
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Mika Lindvall, Wooseok Han, Jiong Lan, Gisele Nishiguchi, Cynthia Shafer, Cornelia Bellamacina, Kay Huh, Gordana Atallah, Christopher McBride, William Antonios-McCrea, JR., Tatiana Zavorotinskaya, Annette Walter, Pablo Dominguez Garcia
  • Publication number: 20140249134
    Abstract: The present invention is directed to substituted triazolyl compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: October 3, 2012
    Publication date: September 4, 2014
    Inventors: Christopher D. Cox, Vadim Y. Dudkin, June J. Kim, Scott D. Kuduk, Carol A. McVean, Thomas Reger, Justin T. Sheen, Thomas Steele
  • Patent number: 8816074
    Abstract: The present invention relates to 2?-Fluoro-6?-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number of viral infections and secondary disease states and conditions thereof, especially including Hepatitis B virus (HBV) and secondary disease states and conditions thereof (cirrhosis and liver cancer), Heptatitis C virus (HCV), Herpes Simplex virus I and II (HSV-1 and HSV-2), cytomegalovirus (CMV), Varicella-Zoster Virus (VZV) and Epstein Barr virus (EBV) and secondary cancers which occur thereof (lymphoma, nasopharyngeal cancer, including drug resistant (especially including lamivudine and/or adefovir resistant) and other mutant forms of these viruses.
    Type: Grant
    Filed: May 13, 2011
    Date of Patent: August 26, 2014
    Assignee: University of Georgia Foundation, Inc.
    Inventors: Chung K. Chu, Jianing Wang
  • Patent number: 8796298
    Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: August 5, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Melissa Dumble, Tona Gilmer, Rakesh Kumar, Peter F. Lebowitz, Shannon Renae Morris, Sylvie Laquerre
  • Patent number: 8796452
    Abstract: A thermodynamically controlled process for preparing Form I polymorph of lamivudine is described, wherein the process involves crystallizing Form I at a temperature of from about 0° C. to about 50° C. from a mixture which comprises (a) lamivudine or an acid salt thereof or both, (b) a solvent system comprising water and at least one organic solvent, and optionally (c) Form I seed; wherein, when a lamivudine acid salt is employed in the mixture, the crystallizing step is conducted in the presence of a base; and wherein the water activity of the solvent system is maintained in a range in which Form I is thermodynamically the most stable form of lamivudine.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: August 5, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Benjamin Cohen, Christopher Wahl, Itzia Z. Arroyo, Aaron S. Cote
  • Patent number: 8785444
    Abstract: The present invention relates to compounds useful as inhibitors of Aurora 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: August 2, 2012
    Date of Patent: July 22, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Mortimore, Julian Golec, Christopher Davis, Daniel Robinson, John Studley
  • Patent number: 8785467
    Abstract: The present invention is directed to 2-alkoxy pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: September 26, 2011
    Date of Patent: July 22, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher D. Cox, Izzat T. Raheem, William D. Shipe, Cory R. Theberge
  • Patent number: 8779127
    Abstract: The present invention provides a facile process for the preparation of tri- and tetra—substituted pyrimidines. The process is useful for preparing inhibitors of protein kinases, especially Aurora kinase. These inhibitors are useful for treating or lessening the severity of Aurora—mediated diseases or conditions.
    Type: Grant
    Filed: August 15, 2012
    Date of Patent: July 15, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Francesca Mazzei, David Kay, Andrew Miller
  • Publication number: 20140187777
    Abstract: Disclosed herein are some methods for synthesizing the base-assisted coupling of aromatic alcohols with substituted aromatic compounds including some substituted heteroaromatic compounds such as pyrimidines or pyridines to form esters. The reactions may include inexpensive bases such as potassium hydroxide and take place in a solvent mixture comprised primarily of hindered tertiary alcohols that are at least partially immiscible with water. In some embodiments the tertiary alcohol solvents forms azeotropes with water which stabilize the formation of an alkoxide intermediate when the alkoxide formation step is heated to the boiling point of the azeotrope and water is withdrawn from the reaction mixture.
    Type: Application
    Filed: March 22, 2013
    Publication date: July 3, 2014
    Applicant: Dow Agrosciences LLC
    Inventor: Dow Agrosciences LLC
  • Publication number: 20140187540
    Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
    Type: Application
    Filed: February 15, 2012
    Publication date: July 3, 2014
    Applicant: The Johns Hopkins University
    Inventors: Donald J. Zack, Cynthia Berlinicke, Laszlo Hackler, Zhiyong Yang, Joseph P. Steiner, Tomas Vojkovsky, Dana Ferraris, Barbara S. Slusher, James Inglese
  • Patent number: 8754078
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: June 17, 2014
    Assignee: ArQule, Inc.
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi M. Moussa, Neru Munshi
  • Patent number: 8748411
    Abstract: Chemical compounds derived by in silico molecular modelling, having a well defined structure suitable for the blocking of the phosphorylation event, through the specific interaction of the chemical with the Casein Kinase 2 enzyme substrate phosphorylation domain or it's neighbourhood. This invention comprises also the pharmaceutical compositions containing such compounds, and their use in the preparation of medicines or agents for the treatment of diseases or conditions related with neoplasic processes.
    Type: Grant
    Filed: May 5, 2006
    Date of Patent: June 10, 2014
    Assignee: Centro de Ingenieria Genetica y Biotechnologia
    Inventors: Rolando Eduardo Rodriguez Fernandez, Roberto Vera Alvarez, Ania De La Nuez Veulens, Yuliet Mazola Reyes, Silvio Ernesto Perea Rodriguez, Boris Ernesto Acevedo Castro, Alexis Musacchio Lasa, Raimundo Ubieta Gómez
  • Patent number: 8748604
    Abstract: The present invention provides an improved process for stereoselective preparation of 5-fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: June 10, 2014
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Prakash Bhimaji Kshirsagar, Satish Manohar Bhoge, Santosh Richhariya, Kaptan Singh
  • Patent number: 8748603
    Abstract: There is provided crystalline forms of N-[2-[[(2,3-difluorophenyl)methyl]thio]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]1-azetidinesulfon-amide anhydrate. Such compounds/forms may be useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.
    Type: Grant
    Filed: July 12, 2011
    Date of Patent: June 10, 2014
    Assignee: AstraZeneca AB
    Inventors: Britt Anne Ingela Gullberg, Thomas Peter Larsson, Jeffrey Paul Stonehouse
  • Publication number: 20140148430
    Abstract: Certain imidazopyridines (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Application
    Filed: November 26, 2012
    Publication date: May 29, 2014
    Applicant: Gilead Connecticut, Inc.
    Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Aaron C. Schmitt, Jianjun Xu, Zhongdong Zhao