Nitrogen Attached Directly Or Indirectly To The Purine Ring System By Nonionic Bonding Patents (Class 544/276)
  • Patent number: 10125153
    Abstract: The present invention describes chemical systems and methods for silylating N—H bonds of aliphatic amines, said system or method comprising or consisting essentially of a mixture of (a) at least one organosilane and (b) at least one hydroxide, especially KOH, said system being preferably, but not necessarily substantially free of a transition-metal compound, and said methods comprising contacting a quantity of the organic substrate with a mixture of (a) at least one organosilane and (b) at least one strong base, under conditions sufficient to replace an N—H bond with a silyl N—Si bond.
    Type: Grant
    Filed: November 6, 2017
    Date of Patent: November 13, 2018
    Assignee: California Institute of Technology
    Inventors: Anton Toutov, Kerry Betz, Alexey Fedorov, Brian M. Stoltz, Wenbo Liu, Robert H. Grubbs
  • Patent number: 9994573
    Abstract: The present invention provides methods for radiolabeling compounds useful as Hsp90 inhibitors. The present invention also provides intermediates useful in such methods, and compositions of radiolabeled compounds. The present invention provides, among other things, novel methods for the synthesis of radiolabeled compounds. In certain embodiments, the present invention provides compounds of formula I.
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: June 12, 2018
    Assignee: Memorial Sloan-Kettering Cancer Center
    Inventors: Stefan O. Ochiana, NagaVaraKishore Pillarsetty, Tony Taldone, Gabriela Chiosis
  • Patent number: 9981966
    Abstract: The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.
    Type: Grant
    Filed: July 19, 2017
    Date of Patent: May 29, 2018
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shingo Yamamoto, Toshio Yoshizawa
  • Patent number: 9896453
    Abstract: The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.
    Type: Grant
    Filed: May 19, 2016
    Date of Patent: February 20, 2018
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shingo Yamamoto, Toshio Yoshizawa
  • Patent number: 9809607
    Abstract: The present invention describes chemical systems and methods for silylating aromatic organic substrates, said system or method comprising or consisting essentially of a mixture of (a) at least one organosilane and (b) at least one strong base, the definition of strong base now also including KOH, said system being preferably, but not necessarily substantially free of a transition-metal compound, and said methods comprising contacting a quantity of the organic substrate with a mixture of (a) at least one organosilane and (b) at least one strong base, under conditions sufficient to silylate the aromatic substrate.
    Type: Grant
    Filed: August 5, 2015
    Date of Patent: November 7, 2017
    Assignee: California Institute of Technology
    Inventors: Anton Toutov, Kerry Betz, Alexey Fedorov, Brian M. Stoltz, Wenbo Liu, Robert H. Grubbs
  • Patent number: 9403864
    Abstract: Disclosed is a process for preparing a carbonucleoside of formula (1) and intermediates for use therein. The process involves the step of reacting a compound of formula (2) with a compound of formula (3) under Mitsunobu-type reaction conditions to obtain a compound of formula (4), wherein PG1, PG2, PG3 and PG4 are protecting groups. The compound of formula (4) is deprotected to form the compound of formula (1), as shown below.
    Type: Grant
    Filed: May 30, 2011
    Date of Patent: August 2, 2016
    Assignee: Alphora Research Inc.
    Inventors: Dino Alberico, Joshua Clayton, Craig Dixon, Boris Gorin
  • Patent number: 9403828
    Abstract: Purine scaffold Hsp90 inhibitors are useful in therapeutic applications and as radioimaging ligands.
    Type: Grant
    Filed: July 6, 2011
    Date of Patent: August 2, 2016
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventor: Gabriela Chiosis
  • Patent number: 9371325
    Abstract: The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.
    Type: Grant
    Filed: June 12, 2015
    Date of Patent: June 21, 2016
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Shingo Yamamoto, Toshio Yoshizawa
  • Patent number: 9309249
    Abstract: The present invention relates to a preparation method for a medicine and an intermediate compound thereof, specifically, relates to a preparation method for entecavir, an intermediate compound thereof, and a synthesis method for the intermediate compound.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: April 12, 2016
    Assignee: Zhejiang Ausun Pharmaceutical Co., Ltd
    Inventor: Zhiguo Zheng
  • Patent number: 9273050
    Abstract: Provided is a compound having at least one selected from the group consisting of cell growth promoting activity, angiogenesis promoting activity, lumen formation promoting activity, cell migration promoting activity, and neurocyte growth promoting activity, which is a chemically stable low-molecular-weight substance that has high absorbability and can be supplied stably at a low cost because of its low molecular weight. A cyclobutyl purine derivative, a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof according to the present invention is a cyclobutyl purine derivative represented by the following general formula (1), a tautomer or stereoisomer thereof, or a salt, solvate, or hydrate thereof.
    Type: Grant
    Filed: November 27, 2009
    Date of Patent: March 1, 2016
    Assignee: National University Corporation Kagawa University
    Inventors: Ikuko Tsukamoto, Ryoji Konishi, Masaaki Tokuda, Yasuo Kubota, Tokumi Maruyama, Hiroaki Kosaka, Junsuke Igarashi
  • Patent number: 9200278
    Abstract: Provided is a novel nucleic acid molecule that can be produced easily and efficiently and can inhibit the expression of a gene. The nucleic acid molecule is a single-stranded nucleic acid molecule including an expression inhibitory sequence that inhibits expression of a target gene. The single-stranded nucleic acid molecule includes: a region (X); a linker region (Lx); and a region (Xc). The linker region (Lx) is linked between the regions (Xc) and (Xc). The region (Xc) is complementary to the region (X). At least one of the regions (X) and (Xc) includes the expression inhibitory sequence. The linker region (Lx) has a non-nucleotide structure including at least one of a pyrrolidine skeleton and a piperidine skeleton. According to this single-stranded nucleic acid molecule, it is possible to inhibit the expression of the target gene.
    Type: Grant
    Filed: December 19, 2013
    Date of Patent: December 1, 2015
    Assignee: BONAC Corporation
    Inventors: Tadaaki Ohgi, Hirotake Hayashi, Hisao Shirohzu, Tomohiro Hamasaki, Akihiro Itoh, Hiroshi Suzuki
  • Patent number: 9187480
    Abstract: The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: Such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: November 17, 2015
    Assignee: Research Triangle Institute
    Inventors: Rangan Maitra, Alan Bradley Fulp, Yanan Zhang, Herbert H. Seltzman
  • Patent number: 9187507
    Abstract: The present invention relates to an acyclic nucleoside phosphonate derivative and medical uses thereof. Specifically, the present invention relates to an acyclic nucleoside phosphonate derivative of Formula I having strong potency against viruses, such as hepatitis B virus, and low cytotoxicity, or a pharmaceutically acceptable salt, isomer, hydrate or solvate thereof, wherein R1 is H or methyl; each R2 is independently —R3 or —OR3, each R3 is independently C1-C8 alkyl, C3-C8 cycloalkyl. The present invention further relates to a process for preparing the compounds of Formula I, a pharmaceutical composition comprising the compound, and the medical uses of the compound. The acyclic nucleoside phosphonate derivative of the present invention has activity against virus such as hepatitis B virus and good in vivo behavioral traits.
    Type: Grant
    Filed: June 21, 2010
    Date of Patent: November 17, 2015
    Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Bohua Zhong, Xinhua He, Yongguang Wang, He Liu
  • Patent number: 9084792
    Abstract: Preparation of acyclovir 2/3 hydrate comprises mixing acyclovir with water at weight ratio of 1:5˜50, dissolving at 50˜100° C., filtering, cooling filtrate at 0˜30° C. to precipitate crystal, collecting the crystal by filtration, and drying the crystal at 0˜150° C. for 0.5˜24 hours to obtain acyclovir 2/3 hydrate. The preparation process is simple and suitable for industrial production. The prepared product has good and stable crystal form.
    Type: Grant
    Filed: March 17, 2010
    Date of Patent: July 21, 2015
    Assignee: Zhejiang Charioteer Pharmaceutical Co., Ltd.
    Inventors: Tong Pu, Yi Fan, Tian Chen, Ming Lei, Naixing Wang, Zhen Yang, Jianming Yang
  • Publication number: 20150133457
    Abstract: The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye or an immunologically related disease, and in some embodiments diseases or disorders related to the dysregulation of kinase such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, FLT3(D835Y), ITK, TEC, TXK, BTK, or JAK, and the respective pathways.
    Type: Application
    Filed: July 11, 2014
    Publication date: May 14, 2015
    Inventors: Xiao XU, Xiaobo WANG, Long MAO, Li ZHAO, Biao XI
  • 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
  • Patent number: 8993755
    Abstract: The present application includes a compound of Formula I or II: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: March 31, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Randall L. Halcomb
  • 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: 20150079157
    Abstract: The present invention provides a pharmaceutical composition for preventing or treating atopic dermatitis comprising 2-amino-1,9-dimethylpurin-6-one or its pharmaceutically acceptable salt as an active ingredient. And also, the present invention provides a cosmetic composition for improving atopic dermatitis comprising 2-amino-1,9-dimethylpurin-6-one or its pharmaceutically acceptable salt; and a food (i.e., a functional food) for preventing or improving atopic dermatitis comprising 2-amino-1,9-dimethylpurin-6-one or its pharmaceutically acceptable salt.
    Type: Application
    Filed: April 12, 2013
    Publication date: March 19, 2015
    Applicant: DAEWOONG CO., LTD.
    Inventors: Gyeong-Sug Nam, Se-Joon Yoon, Ok-Gyung Choi, Jin-Pyo Kim, Soo-Jin Choi, Hyong-Jin Park
  • Patent number: 8969362
    Abstract: The present invention provides an 8-oxoadenine compound having immunomodulating activities such as an interferon inducing activity and useful as an antiviral agent and antiallergic agent, which is represented by the following formula (1): [wherein the ring A represents a 6-10 membered aromatic carbocyclic ring and the like, R represents a halogen atom, an alkyl group and the like, n represents an integer of 0-2, Z1 represents alkylene, X2 represents oxygen atom, sulfur atom, SO2, NR5, CO, CONR5, NR5CO and the like, Y1, Y2 and Y3 represent independently a single bond or an alkylene group, X1 represents oxygen atom, sulfur atom, NR4 (R4 is hydrogen atom or an alkyl group) or a single bond, R2 represents a substituted or unsubstituted alkyl group, R1 represents hydrogen atom, hydroxy group, an alkoxy group, an alkoxycarbonyl group or a haloalkyl group] or its pharmaceutically acceptable salt.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: March 3, 2015
    Assignees: AstraZeneca Aktiebolag, Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Ayumu Kurimoto, Kazuki Hashimoto, Yoshiaki Isobe, Stephen Brough, Ian Millichip, Hiroki Wada, Roger Bonnert, Thomas Mcinally
  • Publication number: 20150051229
    Abstract: The present invention relates to crystalline forms of valomaciclovir, processes for preparing crystalline forms of valomaciclovir, pharmaceutical compositions thereof and methods of using thereof.
    Type: Application
    Filed: June 19, 2014
    Publication date: February 19, 2015
    Inventors: Mike H. O'NEILL, Gregory P. BUTKE
  • Publication number: 20150051394
    Abstract: The present invention relates to the preparation of cyclopropane derivatives, in particular 2-amino-9-[[(1S,2R)-1,2-bis(hydroxymethyl)cyclopropyl]methyl]-4,8-dihydro-1H-purin-6-one, especially via the [(1S,7R)-4-phenyl-3,5-dioxabicyclo[5.1.0]octan-1-yl]methanol intermediate.
    Type: Application
    Filed: November 10, 2011
    Publication date: February 19, 2015
    Applicant: ARATANA THERAPEUTICS NV
    Inventors: Eleonora Kiss, Erwin Blomsma, Serge De Bruijn, E.J.N. Remy Litjens
  • Publication number: 20150038494
    Abstract: The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Applicant: Katholieke Universiteit Leuven, K.U.Leuven R&D
    Inventors: Piet Herdewijn, Steven De Jonghe, Ling-Jie Gao, Mi-Yeon Jang, Bart Vanderhoydonck, Mark Jozef Albert Waer, Yuan Lin, Jean Ferdinand Herman, Thierry Andre Michel Louat
  • Patent number: 8946243
    Abstract: The invention relates to compounds and methods for treating or preventing a viral infection, by administering a monophosphorylated prodrug of acyclovir or monophosphorylated derivative of an acyclovir prodrug to a subject suffering from or susceptible (to a viral infection, such as HIV infection.
    Type: Grant
    Filed: March 27, 2009
    Date of Patent: February 3, 2015
    Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, Katholieke Universiteit Leuven
    Inventors: Leonid Margolis, Jan Balzarini, Christopher McGuigan, Andrea Lisco, Christophe Vanpouille, Marco Derudas
  • Patent number: 8940751
    Abstract: The present disclosure relates to purine compounds of formula (I) or formula (II) or its tautomers, polymorphs, stereoisomers, solvates or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2B adenosine receptor antagonists. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2B receptor. The present disclosure also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: September 9, 2011
    Date of Patent: January 27, 2015
    Assignee: Advinus Therapeutics Private Limited
    Inventors: Dinesh Barawkar, Sujay Basu, Vidya Ramdas, Venkata Poornapragnacharyulu Palle, Yogesh Waman, Meena Patel, Anil Panmand
  • Publication number: 20150025090
    Abstract: The present application relates to novel substituted azabicycles, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: March 5, 2013
    Publication date: January 22, 2015
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Alexandros Vakalopoulos, Dieter Lang, Frank Wunder, Walter Hübsch, Michael Hahn
  • Patent number: 8937076
    Abstract: The present invention relates to a crystalline form of entecavir and its process for preparation, and provides a pharmaceutical composition comprising a therapeutically effective amount of the crystalline form of entecavir. Furthermore, the present invention also provides a use of the crystalline form of entecavir in preparation for a medicament for the treatment of hepatitis B viral infections. The present invention is beneficial toe preparations for pharmaceutical formulations and enhancements of its bioavailability.
    Type: Grant
    Filed: January 31, 2008
    Date of Patent: January 20, 2015
    Assignee: Zhejiang Medicine Co., Ltd. Xinchang Pharaceutical Factory
    Inventors: Weidong Ye, Jianyong Yuan, Jingjing Nie, Duanjun Xu, Chaotian Chen
  • Publication number: 20150011545
    Abstract: The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.
    Type: Application
    Filed: July 15, 2014
    Publication date: January 8, 2015
    Applicant: AstraZeneca AB
    Inventors: Audrey DAVIES, Stephanos IOANNIDIS, Michelle Laurae LAMB, Mei SU, Tao WANG, Hai-Jun ZHANG
  • Publication number: 20150011731
    Abstract: Dye compounds of the formula (1) wherein A is a protective agent group that has a characteristic of modifying the singlet-triplet occupancy of the shown cyanine moiety, and M is a reactive crosslinking group or a group that can be converted to a reactive crosslinking group. Methods for synthesizing the dye compounds and applications for their use are also described.
    Type: Application
    Filed: January 18, 2013
    Publication date: January 8, 2015
    Applicant: CORNELL UNIVERSITY
    Inventors: Scott C. Blanchard, Roger Altman, J. David Warren, Zhou Zhou
  • 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: 20140371245
    Abstract: Novel N-acylated, O-acylated and (bis or tris)-N,O-acylated derivatives of purinic and pyrimidinic nucleoside analogs, pharmaceutical compositions containing same, and uses thereof for treating proliferative diseases or disorders are disclosed.
    Type: Application
    Filed: July 24, 2014
    Publication date: December 18, 2014
    Inventors: Abraham NUDELMAN, Ada REPHAELI
  • 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
  • Patent number: 8895570
    Abstract: The invention provides the compound of formula (I) and pharmaceutically acceptable salt thereof, pharmaceutical compositions containing the compound and the use of the compound in therapy.
    Type: Grant
    Filed: December 14, 2011
    Date of Patent: November 25, 2014
    Assignee: AstraZeneca AB
    Inventors: Phillip Abbott, Roger Victor Bonnert, Thomas McInally, Stephen Thom, Hiroki Wada, Satoshi Onuma
  • Publication number: 20140330015
    Abstract: The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.
    Type: Application
    Filed: November 28, 2012
    Publication date: November 6, 2014
    Applicant: ONO Pharmaceutical CO., Ltd
    Inventors: Shingo Yamamoto, Toshio Yoshizawa
  • Publication number: 20140323728
    Abstract: The present invention provides a novel class of peptide nucleic acid derivatives, which show good cell penetration and strong binding affinity for nucleic acid.
    Type: Application
    Filed: December 19, 2013
    Publication date: October 30, 2014
    Applicant: CTI BIO
    Inventors: Shin CHUNG, Heui-Yeon KIM, Hyun-Jin PARK, Mi-Ran KIM, Jong-Ook LEE
  • 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
  • Patent number: 8865896
    Abstract: A method for producing adenine compound (1): wherein m and n are independently an integer of 2 to 5, R1 is C1-6 alkyl group, R2 and R3 are the same or different, and hydrogen atom, or C1-6 alkyl group, or R2 and R3 are combined with an adjacent nitrogen atom to form pyrrolidine, morpholine, piperidine, piperazine, etc., and R4 is C1-3 alkyl group, which comprises a step of reacting compound (2): and compound (3): in the presence of a boron-containing reducing agent.
    Type: Grant
    Filed: January 16, 2009
    Date of Patent: October 21, 2014
    Assignees: Astrazeneca Aktiebolag, Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Kazuki Hashimoto, Wataru Katoda, Kazuhiko Takahashi, Ayumu Kurimoto
  • Publication number: 20140309419
    Abstract: This invention relates to a method for enhancing the thermal stability of ionic compounds including ionic liquids, by immobilization on porous solid support materials having a pore diameter of between about 20-200 ?, wherein the solid support does not have a pore size of 90 ?.
    Type: Application
    Filed: August 30, 2012
    Publication date: October 16, 2014
    Applicants: Danmarks Tekniske Universite, The Board of Trustees of the University of Alabama for and on behalf of the University of Alabama
    Inventors: Anders Riisager, Rasmus Fermann, Robin D. Rogers, Gabriela Gurau
  • Publication number: 20140303151
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Application
    Filed: September 14, 2011
    Publication date: October 9, 2014
    Applicant: Exelixis, Inc.
    Inventor: James William Leahy
  • Publication number: 20140303193
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Application
    Filed: June 6, 2013
    Publication date: October 9, 2014
    Applicant: MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: Christopher F. Claiborne, Stephen Critchley, Courtney A. Cullis, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
  • Publication number: 20140296520
    Abstract: The present invention provides a process for the preparation of 2-[(2-amino-1,6-dihydro-6-oxo-9H-yl)]ethyl L-valine ester hydrochloride (valacyclovir hydrochloride) of formula I comprising deprotection of N-[(benzyloxy)carbonyl]-L-valine-2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy]ethyl ester, of formula II using 5% palladium on carbon as a catalyst and mineral acid in the presence of water, avoiding use of organic solvents under hydrogen pressure to yield valacyclovir hydrochloride having yield of ?90% and purity of ?99.5%, pharmaceutically acceptable grade. The valacyclovir hydrochloride obtained using the process of the present invention is valacyclovir hydrochloride polymorphic Form I.
    Type: Application
    Filed: November 23, 2012
    Publication date: October 2, 2014
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Mita Roy, Ashutosh Jagtap, Nitin Pawar
  • Patent number: 8846697
    Abstract: The present invention provides purine analog compounds, as well as compositions and methods of using them, for example, to prevent or treat various diseases and disorders in human and non-human animals.
    Type: Grant
    Filed: April 23, 2007
    Date of Patent: September 30, 2014
    Assignee: The Regents of the University of California
    Inventors: Dennis A. Carson, Howard B. Cottam, Guangyi Jin, Christina C. N. Wu, Suzanne Grimshaw
  • Publication number: 20140288099
    Abstract: Compound (I), and pharmaceutically acceptable salts thereof, are inducers of human interferon. Certain discrete and particular dosages of Compound (I) may be particularly useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and allergic asthma.
    Type: Application
    Filed: July 19, 2012
    Publication date: September 25, 2014
    Applicant: GLAXOSMITHKLINE LLC
    Inventors: Claire Louise Ambery, Christopher David Edwards
  • Publication number: 20140274936
    Abstract: A coordination complex having a physiologically acceptable pKa includes a metal and a biologically active agent. The pKa of the coordination complex is less than the pKa of the biologically active agent. A pharmaceutical solution for treating a patient includes a coordination complex and water, wherein the coordination complex is at least partially soluble in the water at physiological pH and in a therapeutically efficacious concentration. A method for treating a patient includes administering a pharmaceutical solution including a coordination complex and water to a patient in need of a biologically active agent.
    Type: Application
    Filed: May 29, 2014
    Publication date: September 18, 2014
    Applicant: SYNTHONICS, INC.
    Inventors: Thomas Piccariello, John D. Price, Robert A. Oberlender, Michaela E. Mulhare, Mary C. Spencer, Scott B. Palmer
  • Publication number: 20140275508
    Abstract: Artificial nucleosides including 2-methyl-nucleobase-substituted butane-1,3-diol nucleosides are disclosed. Four different stereoisomers of such nucleosides are possible. Oligonucleotides made up of the artificial nucleosides form homoduplexes of greater stability than DNA duplexes and have a reduced ability to hybridize to DNA or RNA.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: Elitech Holding B.V.
    Inventors: Noah Scarr, Eugeny A. Lukhtanov
  • Publication number: 20140275071
    Abstract: Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: HYDRA BIOSCIENCES, INC.
    Inventors: Bertrand L. Chenard, Randall J. Gallaschun
  • Publication number: 20140242108
    Abstract: A conjugated compound of Formula I: Q-Z—R4 wherein Q is a TLR7 and/or TLR8 agonist and Z—R4 is a TLR2 agonist, the conjugated compound being chosen among compounds of Formula II:
    Type: Application
    Filed: February 22, 2013
    Publication date: August 28, 2014
    Applicant: CAYLA
    Inventors: Thierry LIOUX, Daniel DROCOURT, Fabienne VERNEJOUL, Gerard TIRABY, Eric PEROUZEL
  • Publication number: 20140243282
    Abstract: The present invention relates to novel drug conjugates, where in two drugs are linked together through an appropriate linker having at least two functional groups capable of forming covalent bond with drugs D1 and D2. The invention also relates to developing novel compositions, methods for their preparation and their use in treating various disease conditions.
    Type: Application
    Filed: December 12, 2011
    Publication date: August 28, 2014
    Inventor: Satish Reddy Kallam
  • Publication number: 20140242606
    Abstract: The present invention relates to a probe for iFRET and use thereof. Specifically, the present invention relates to a novel probe for iFRET, a method for preparing the probe for iFRET, a method for searching a target protein-specific binding site or a molecule having the binding site using the probe for iFRET, and a method for imaging the target protein using the probe for iFRET. The probe for iFRET according to the present invention utilizes an amino acid in a protein as a fluorescent donor, unlike the conventional FRET method. Therefore, only one fluorescent material is used, and its emission wavelength is distinct from the intrinsic fluorescence of the protein. Thus, high specificity and sensitivity are ensured, and the quantity, activity and mechanism of various proteins can be analyzed in an easy and accurate manner.
    Type: Application
    Filed: June 25, 2012
    Publication date: August 28, 2014
    Applicant: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
    Inventors: Sang Jeon Chung, Ju Hwan Kim, Elena Ruchkina, Hyo Jin Kang
  • 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