Nitrogen Attached Directly Or Indirectly To The Purine Ring System By Nonionic Bonding Patents (Class 544/276)
-
Patent number: 12059462Abstract: The present invention provides a composition comprising a universal influenza vaccine antigen and a vaccine adjuvant.Type: GrantFiled: July 22, 2019Date of Patent: August 13, 2024Assignees: JAPAN as represented by DIRECTOR GENERAL of National Institute of Infectious Diseases, Sumitomo Pharma Co., Ltd.Inventors: Yoshimasa Takahashi, Yu Adachi, Manabu Ato, Akihisa Fukushima
-
Patent number: 11897885Abstract: 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: GrantFiled: February 24, 2022Date of Patent: February 13, 2024Assignee: ONO PHARMACEUTICAL CO., LTD.Inventors: Shingo Yamamoto, Toshio Yoshizawa
-
Patent number: 11680067Abstract: Certain embodiments are directed to adenosine receptor antagonists that inhibit migration and growth of cancer cells.Type: GrantFiled: March 19, 2021Date of Patent: June 20, 2023Assignee: Board of Regents, The University of Texas SystemInventor: Jean X. Jiang
-
Patent number: 11649259Abstract: Polymorphic forms of deoxycytidine and methods for preparing the same are provided herein. Also provided are compositions comprising polymorphic forms of deoxycytidine and at least one residual solvent, as well as methods of treating mitochondrial diseases using said compositions.Type: GrantFiled: August 19, 2020Date of Patent: May 16, 2023Assignee: ZOGENIX MDS, INC.Inventor: Paul Glidden
-
Patent number: 11292795Abstract: 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: GrantFiled: September 16, 2020Date of Patent: April 5, 2022Assignee: ONO PHARMACEUTICAL CO., LTD.Inventors: Shingo Yamamoto, Toshio Yoshizawa
-
Patent number: 11267816Abstract: The disclosure relates to novel selective Grp94 inhibitors, compositions comprising an effective amount of such compounds, and methods to treat or prevent a condition, such as cancer, comprising administering to an animal in need thereof an effective amount of such compounds.Type: GrantFiled: April 5, 2019Date of Patent: March 8, 2022Assignee: Memorial Sloan-Kettering Cancer CenterInventors: Gabriela Chiosis, Pengrong Yan, Pallav Patel, Hardik J. Patel, Tony Taldone, Chenghua Yang, Weilin Sun, Stefan O. Ochiana
-
Patent number: 10836765Abstract: The present invention relates to an improved process for the preparation of Valacyclovir or pharmaceutically acceptable salts thereof, which comprises reaction of amine-protected Valacyclovir or its salt with deprotecting agent in a continuous flow reactor.Type: GrantFiled: February 24, 2017Date of Patent: November 17, 2020Assignee: Aurobindo Pharma LtdInventors: Sandeep Jain, Komel Ansari, Subramanyam Maddala, Sivakumaran Meenakshisundaram
-
Patent number: 10807981Abstract: 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: GrantFiled: June 25, 2019Date of Patent: October 20, 2020Assignee: ONO PHARMACEUTICAL CO., LTD.Inventors: Shingo Yamamoto, Toshio Yoshizawa
-
Patent number: 10421758Abstract: The disclosure relates to novel selective Grp94 inhibitors, compositions comprising an effective amount of such compounds, and methods to treat or prevent a condition, such as cancer, comprising administering to an animal in need thereof an effective amount of such compounds.Type: GrantFiled: August 15, 2014Date of Patent: September 24, 2019Assignee: Memorial Sloan-Kettering Cancer CenterInventors: Gabriela Chiosis, Pengrong Yan, Pallav Patel, Hardik J. Patel, Tony Taldone, Chenghua Yang, Weilin Sun, Stefan O. Ochiana
-
Patent number: 10125153Abstract: 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: GrantFiled: November 6, 2017Date of Patent: November 13, 2018Assignee: California Institute of TechnologyInventors: Anton Toutov, Kerry Betz, Alexey Fedorov, Brian M. Stoltz, Wenbo Liu, Robert H. Grubbs
-
Patent number: 9994573Abstract: 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: GrantFiled: December 23, 2014Date of Patent: June 12, 2018Assignee: Memorial Sloan-Kettering Cancer CenterInventors: Stefan O. Ochiana, NagaVaraKishore Pillarsetty, Tony Taldone, Gabriela Chiosis
-
Patent number: 9981966Abstract: 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: GrantFiled: July 19, 2017Date of Patent: May 29, 2018Assignee: ONO PHARMACEUTICAL CO., LTD.Inventors: Shingo Yamamoto, Toshio Yoshizawa
-
Patent number: 9896453Abstract: 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: GrantFiled: May 19, 2016Date of Patent: February 20, 2018Assignee: ONO PHARMACEUTICAL CO., LTD.Inventors: Shingo Yamamoto, Toshio Yoshizawa
-
Patent number: 9809607Abstract: 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: GrantFiled: August 5, 2015Date of Patent: November 7, 2017Assignee: California Institute of TechnologyInventors: Anton Toutov, Kerry Betz, Alexey Fedorov, Brian M. Stoltz, Wenbo Liu, Robert H. Grubbs
-
Patent number: 9403828Abstract: Purine scaffold Hsp90 inhibitors are useful in therapeutic applications and as radioimaging ligands.Type: GrantFiled: July 6, 2011Date of Patent: August 2, 2016Assignee: Sloan-Kettering Institute for Cancer ResearchInventor: Gabriela Chiosis
-
Patent number: 9403864Abstract: 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: GrantFiled: May 30, 2011Date of Patent: August 2, 2016Assignee: Alphora Research Inc.Inventors: Dino Alberico, Joshua Clayton, Craig Dixon, Boris Gorin
-
Patent number: 9371325Abstract: 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: GrantFiled: June 12, 2015Date of Patent: June 21, 2016Assignee: ONO PHARMACEUTICAL CO., LTD.Inventors: Shingo Yamamoto, Toshio Yoshizawa
-
Patent number: 9309249Abstract: 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: GrantFiled: July 15, 2011Date of Patent: April 12, 2016Assignee: Zhejiang Ausun Pharmaceutical Co., LtdInventor: Zhiguo Zheng
-
Patent number: 9273050Abstract: 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: GrantFiled: November 27, 2009Date of Patent: March 1, 2016Assignee: National University Corporation Kagawa UniversityInventors: Ikuko Tsukamoto, Ryoji Konishi, Masaaki Tokuda, Yasuo Kubota, Tokumi Maruyama, Hiroaki Kosaka, Junsuke Igarashi
-
Patent number: 9200278Abstract: 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: GrantFiled: December 19, 2013Date of Patent: December 1, 2015Assignee: BONAC CorporationInventors: Tadaaki Ohgi, Hirotake Hayashi, Hisao Shirohzu, Tomohiro Hamasaki, Akihiro Itoh, Hiroshi Suzuki
-
Patent number: 9187480Abstract: 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: GrantFiled: February 15, 2013Date of Patent: November 17, 2015Assignee: Research Triangle InstituteInventors: Rangan Maitra, Alan Bradley Fulp, Yanan Zhang, Herbert H. Seltzman
-
Patent number: 9187507Abstract: 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: GrantFiled: June 21, 2010Date of Patent: November 17, 2015Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. ChinaInventors: Bohua Zhong, Xinhua He, Yongguang Wang, He Liu
-
Patent number: 9084792Abstract: 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: GrantFiled: March 17, 2010Date of Patent: July 21, 2015Assignee: Zhejiang Charioteer Pharmaceutical Co., Ltd.Inventors: Tong Pu, Yi Fan, Tian Chen, Ming Lei, Naixing Wang, Zhen Yang, Jianming Yang
-
Publication number: 20150133457Abstract: 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: ApplicationFiled: July 11, 2014Publication date: May 14, 2015Inventors: Xiao XU, Xiaobo WANG, Long MAO, Li ZHAO, Biao XI
-
Patent number: 9024022Abstract: 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: GrantFiled: September 22, 2009Date of Patent: May 5, 2015Assignee: Cis Bio InternationalInventors: Emmanuel Bourrier, Michel Laget, Laurent Lamarque, Norbert Tinel, Eric Trinquet, Hervé Bazin
-
Patent number: 8993755Abstract: 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: GrantFiled: January 17, 2014Date of Patent: March 31, 2015Assignee: Gilead Sciences, Inc.Inventors: Michael Graupe, Randall L. Halcomb
-
Publication number: 20150087643Abstract: 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: ApplicationFiled: October 10, 2014Publication date: March 26, 2015Applicant: Advinus Therapeutics Private LimitedInventors: Venkata Palle, Vidya Ramdas, Dinesh Barawkar, Sujay Basu, Summon Koul, Yogesh Waman, Meena Patel, Anil Panmand
-
Publication number: 20150079157Abstract: 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: ApplicationFiled: April 12, 2013Publication date: March 19, 2015Applicant: DAEWOONG CO., LTD.Inventors: Gyeong-Sug Nam, Se-Joon Yoon, Ok-Gyung Choi, Jin-Pyo Kim, Soo-Jin Choi, Hyong-Jin Park
-
Patent number: 8969362Abstract: 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: GrantFiled: October 21, 2013Date of Patent: March 3, 2015Assignees: 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: 20150051229Abstract: 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: ApplicationFiled: June 19, 2014Publication date: February 19, 2015Inventors: Mike H. O'NEILL, Gregory P. BUTKE
-
Publication number: 20150051394Abstract: 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: ApplicationFiled: November 10, 2011Publication date: February 19, 2015Applicant: ARATANA THERAPEUTICS NVInventors: Eleonora Kiss, Erwin Blomsma, Serge De Bruijn, E.J.N. Remy Litjens
-
Publication number: 20150038494Abstract: 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: ApplicationFiled: October 20, 2014Publication date: February 5, 2015Applicant: Katholieke Universiteit Leuven, K.U.Leuven R&DInventors: 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: 8946243Abstract: 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: GrantFiled: March 27, 2009Date of Patent: February 3, 2015Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, Katholieke Universiteit LeuvenInventors: Leonid Margolis, Jan Balzarini, Christopher McGuigan, Andrea Lisco, Christophe Vanpouille, Marco Derudas
-
Patent number: 8940751Abstract: 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: GrantFiled: September 9, 2011Date of Patent: January 27, 2015Assignee: Advinus Therapeutics Private LimitedInventors: Dinesh Barawkar, Sujay Basu, Vidya Ramdas, Venkata Poornapragnacharyulu Palle, Yogesh Waman, Meena Patel, Anil Panmand
-
Publication number: 20150025090Abstract: 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: ApplicationFiled: March 5, 2013Publication date: January 22, 2015Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Alexandros Vakalopoulos, Dieter Lang, Frank Wunder, Walter Hübsch, Michael Hahn
-
Patent number: 8937076Abstract: 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: GrantFiled: January 31, 2008Date of Patent: January 20, 2015Assignee: Zhejiang Medicine Co., Ltd. Xinchang Pharaceutical FactoryInventors: Weidong Ye, Jianyong Yuan, Jingjing Nie, Duanjun Xu, Chaotian Chen
-
Publication number: 20150011545Abstract: 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: ApplicationFiled: July 15, 2014Publication date: January 8, 2015Applicant: AstraZeneca ABInventors: Audrey DAVIES, Stephanos IOANNIDIS, Michelle Laurae LAMB, Mei SU, Tao WANG, Hai-Jun ZHANG
-
Publication number: 20150011731Abstract: 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: ApplicationFiled: January 18, 2013Publication date: January 8, 2015Applicant: CORNELL UNIVERSITYInventors: Scott C. Blanchard, Roger Altman, J. David Warren, Zhou Zhou
-
Publication number: 20140378446Abstract: 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: ApplicationFiled: January 30, 2013Publication date: December 25, 2014Applicant: Pharmacyclics, Inc.Inventors: Wei Chen, David J. Loury, Yan Shunqi, Longcheng Wang, Leah Lynn Frye
-
Publication number: 20140371245Abstract: 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: ApplicationFiled: July 24, 2014Publication date: December 18, 2014Inventors: Abraham NUDELMAN, Ada REPHAELI
-
Publication number: 20140364446Abstract: 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: ApplicationFiled: June 4, 2014Publication date: December 11, 2014Inventors: David DUKHAN, Gilles GOSSELIN, Cyril B. DOUSSON
-
Patent number: 8895570Abstract: 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: GrantFiled: December 14, 2011Date of Patent: November 25, 2014Assignee: AstraZeneca ABInventors: Phillip Abbott, Roger Victor Bonnert, Thomas McInally, Stephen Thom, Hiroki Wada, Satoshi Onuma
-
Publication number: 20140330015Abstract: 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: ApplicationFiled: November 28, 2012Publication date: November 6, 2014Applicant: ONO Pharmaceutical CO., LtdInventors: Shingo Yamamoto, Toshio Yoshizawa
-
Publication number: 20140323441Abstract: The present invention relates to purine derivatives of formula (I), processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.Type: ApplicationFiled: November 8, 2012Publication date: October 30, 2014Inventors: Jean-François Bonfanti, Frédéric Marc Maurice Doublet, Werner Embrechts, Jérôme Michel Claude Fortin, David Craig Mc Gowan, Philippe Muller, Piere Jean-Marie Bernand Raboisson
-
Publication number: 20140323728Abstract: 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: ApplicationFiled: December 19, 2013Publication date: October 30, 2014Applicant: CTI BIOInventors: Shin CHUNG, Heui-Yeon KIM, Hyun-Jin PARK, Mi-Ran KIM, Jong-Ook LEE
-
Patent number: 8865896Abstract: 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: GrantFiled: January 16, 2009Date of Patent: October 21, 2014Assignees: Astrazeneca Aktiebolag, Dainippon Sumitomo Pharma Co., Ltd.Inventors: Kazuki Hashimoto, Wataru Katoda, Kazuhiko Takahashi, Ayumu Kurimoto
-
Publication number: 20140309419Abstract: 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: ApplicationFiled: August 30, 2012Publication date: October 16, 2014Applicants: Danmarks Tekniske Universite, The Board of Trustees of the University of Alabama for and on behalf of the University of AlabamaInventors: Anders Riisager, Rasmus Fermann, Robin D. Rogers, Gabriela Gurau
-
Publication number: 20140303151Abstract: 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: ApplicationFiled: September 14, 2011Publication date: October 9, 2014Applicant: Exelixis, Inc.Inventor: James William Leahy
-
Publication number: 20140303193Abstract: 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: ApplicationFiled: June 6, 2013Publication date: October 9, 2014Applicant: 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: 20140296520Abstract: 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: ApplicationFiled: November 23, 2012Publication date: October 2, 2014Applicant: PIRAMAL ENTERPRISES LIMITEDInventors: Mita Roy, Ashutosh Jagtap, Nitin Pawar