Nitrogen Attached Directly Or Indirectly To The Purine Ring System By Nonionic Bonding Patents (Class 544/276)
-
Patent number: 8569491Abstract: Disclosed are a novel, high-yield method for preparing entecavir and intermediates used therein.Type: GrantFiled: September 15, 2010Date of Patent: October 29, 2013Assignee: Hanmi Science Co., LtdInventors: Jae Heon Lee, Gha Seung Park, Jin Hee Kim, Tae Jin Choi, Ji Eun Lee, Jung Hee Han, Hyo Jeong Bang, Sun Young Jung, Young Kil Chang, Gwan Sun Lee, Maeng Sup Kim
-
Publication number: 20130281517Abstract: Cyclopropanecarboxylate esters of purine analogues, method of making and using the same for treating herpes virus infections and tumors are disclosed.Type: ApplicationFiled: April 2, 2013Publication date: October 24, 2013Inventors: Ji-Wang CHERN, Shin-yu LAI, Pei-Teh CHANG
-
Patent number: 8563717Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, or C1-6alkoxy; R2 is a group having the structure: n is an integer having a value of 1 to 6; Het is a 6-membered saturated heterocycle containing one nitrogen atom wherein Het is attached to the ā(CH2)nā moiety at any carbon atom of the heterocycle; R3 is hydrogen, C1-8alkyl, or C3-7cycloalkylC0-6alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.Type: GrantFiled: August 7, 2009Date of Patent: October 22, 2013Assignee: GlaxoSmithKline LLCInventors: Helene Bazin-Lee, Diane Mary Coe, Linos Lazarides, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
-
Publication number: 20130236504Abstract: Disclosed are delivery systems that can be used for treating cancer. The delivery systems include a delivery vehicle in conjunction with a chemo-adjuvant. The chemo-adjuvant can enhance the efficacy of a therapeutic agent that can be delivered in conjunction with the delivery vehicle or can be delivered independently of the delivery vehicle.Type: ApplicationFiled: March 5, 2013Publication date: September 12, 2013Applicants: Medical University of South Carolina, Clemson UniversityInventors: Frank Alexis, Bruce Frankel
-
Publication number: 20130231480Abstract: The present invention provides specific double-stranded DNA/RNA binding compounds having a polymeric structure, which are in fact, triplex forming molecules capable of binding tightly and specifically to predetermined sequences in the major groove of double stranded nucleic acid molecules; as well as pharmaceutical compositions comprising thereof. The triplex forming molecules and the pharmaceutical compositions of the invention can be used for various therapeutic applications such as site-specific modulation of gene expression, targeting of DNA or RNA damage, and gene knockout, as well as for diagnostic applications in vitro.Type: ApplicationFiled: July 21, 2011Publication date: September 5, 2013Applicant: GENEARREST LTDInventors: Anwar Rayan, Mizied Falah
-
Publication number: 20130217879Abstract: 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: ApplicationFiled: July 15, 2011Publication date: August 22, 2013Applicant: AUSUN PHARMATECH. CO., LTD.Inventor: Zhiguo Zheng
-
Publication number: 20130217880Abstract: Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.Type: ApplicationFiled: March 15, 2013Publication date: August 22, 2013Applicant: ONO PHARMACEUTICAL CO., LTD.Inventor: Ono Pharmaceutical Co., Ltd.
-
Patent number: 8507507Abstract: The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.Type: GrantFiled: October 15, 2010Date of Patent: August 13, 2013Assignee: Gilead Sciences, Inc.Inventors: Randall L. Halcomb, Paul A. Roethle
-
Publication number: 20130203986Abstract: Arylamino purine derivatives represented by formula I and their preparation method are disclosed, wherein each substituent is defined as in the description. The derivatives have an inhibitory effect on non-small cell lung cancer with deletion mutation of exon 19 or L858R point mutation of exon 21 in epidermal growth factor receptor (EGFR).Type: ApplicationFiled: December 23, 2010Publication date: August 8, 2013Applicants: SI Chuaan University, CSPC Zhongqi Pharmaceutical Technology (Shijazhuan Co., Ltd.Inventors: Shengyong Yang, Yuquan Wei
-
Publication number: 20130203785Abstract: 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: February 27, 2013Publication date: August 8, 2013Applicant: EPIPHANY BIOSCIENCES, INC.Inventor: EPIPHANY BIOSCIENCES, INC.
-
Patent number: 8501724Abstract: 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: GrantFiled: April 30, 2012Date of Patent: August 6, 2013Assignee: Pharmacyclics, Inc.Inventors: Wei Chen, David J. Loury
-
Publication number: 20130197014Abstract: 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: April 30, 2012Publication date: August 1, 2013Applicant: Pharmacyclics, Inc.Inventors: Wei CHEN, David J. LOURY
-
Publication number: 20130190494Abstract: The present invention provides a new patentable class of purine analog compounds, as well as compositions and methods of using them, for example, to prevent or treat various diseases and disorders inhuman and non-human animals.Type: ApplicationFiled: March 8, 2013Publication date: July 25, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventor: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
-
Publication number: 20130190320Abstract: The present disclosure provides pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.Type: ApplicationFiled: January 12, 2013Publication date: July 25, 2013Applicant: ACEA BIOSCIENCES, INC.Inventor: ACEA Biosciences, Inc.
-
Publication number: 20130184447Abstract: A metal coordination complex of a biologically active moiety and a metal is disclosed. The complex confers to the biologically active moiety an improved performance which can include potency, stability, absorbability, targeted delivery, and combinations thereof.Type: ApplicationFiled: March 5, 2013Publication date: July 18, 2013Applicant: SYNTHONICS, INC.Inventor: SYNTHONICS, INC.
-
Patent number: 8481728Abstract: A process of making entecavir comprising converting a compound of formula (M5) to entecavir, wherein the two PGs on the formula (M5) are taken together to form an optionally substituted six- or seven-member cyclic ring.Type: GrantFiled: February 15, 2011Date of Patent: July 9, 2013Assignee: Scinopharm Taiwan, Ltd.Inventors: Tsung-Cheng Hu, Hung-Tsung Huang
-
Publication number: 20130172249Abstract: 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.Type: ApplicationFiled: September 9, 2011Publication date: July 4, 2013Applicant: ADVINUS THERAPEUTICS PRIVATE LIMITEDInventors: Dinesh Barawkar, Sujay Basu, Vidya Ramdas, Venkata Poornapragnacharyulu Palle, Yogesh Waman, Meena Patel, Anil Panmand
-
Publication number: 20130172328Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia or so on represented by the formula (I):Type: ApplicationFiled: June 22, 2011Publication date: July 4, 2013Applicant: CROSSWING INC.Inventors: Takahiko Taniguchi, Masato Yoshikawa, Kasei Miura, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Makoto Kamata, Haruhi Kamisaki, John F. Quinn, Joseph Raker, Fatoumata Camara, Yi Wang
-
Publication number: 20130172340Abstract: In one aspect, the invention relates to substituted purine analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 22, 2011Publication date: July 4, 2013Applicant: University of Central Flordia Research Foundation,Inventors: James Turkson, Patrick Gunning
-
Publication number: 20130165455Abstract: The present invention provides for TLR agonist conjugates (compounds) and compositions, as well as methods of using them. The compounds of the invention are broad-spectrum, long-lasting, and non-toxic combination of synthetic immunostimulatory agents, which are useful for activating the immune system of a mammal, preferably a human and can help direct the pharmacophore to the receptor within the endosomes of target cells and enhance the signal transduction induced by the pharmacophore.Type: ApplicationFiled: November 20, 2012Publication date: June 27, 2013Applicant: The Regents of The University of CaliforniaInventors: Dennis A. Carson, Howard B. Cottam, Michael Chan, Christina C.N. Wu, Suzanne Grimshaw
-
Publication number: 20130165426Abstract: Disclosed is a compound of Formula I or a salt thereof, in which X, X1, X2, R1, R2, and R3 are described herein. Also disclosed are pharmaceutical compositions and methods of using the compounds of Formula I to treat disorders mediated by melanocortin-4 receptors.Type: ApplicationFiled: July 5, 2011Publication date: June 27, 2013Applicant: UNIVERSITĆ DE MONTRĆALInventors: RĆ©jean Ruel, Yves Chantigny, Anne Marinier, Patricia Rene, Michel Bouvier
-
Publication number: 20130156826Abstract: The present invention relates to respiratory formulations comprising a compound of formula (I): and use of said compounds and compositions in treatment, for example in the treatment of an inflammatory disease or a respiratory disorder, in particular an inflammatory mediated and/or virally mediated respiratory disorder such as asthma and COPD or the treatment or prevention of viral infection, for example infection by influenza virus, rhinovirus or RSV. The invention also extends to certain novel compounds of formula (I).Type: ApplicationFiled: June 17, 2011Publication date: June 20, 2013Applicant: Respivert LimitedInventors: Peter John Murray, Stuart Thomas Onions, Jonathan Gareth Williams, Kevin Joly
-
Publication number: 20130144058Abstract: 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: ApplicationFiled: May 30, 2011Publication date: June 6, 2013Applicant: ALPHORA RESEARCH INC.Inventors: Dino Alberico, Joshua Clayton, Craig Dixon, Boris Gorin
-
Publication number: 20130137694Abstract: There is provided modulators of Nrf2 protein which comprises a compound which binds at least one of the BTB domain, IVR domain and Kelch domain of Keap1 protein, activating or inhibiting Nrf2. There is also provided pharmaceutical compositions containing the modulators, as well as uses and method of use of the modulators for the treatment of conditions.Type: ApplicationFiled: May 31, 2011Publication date: May 30, 2013Inventors: Gerald Batist, Jian Hui Wu
-
Publication number: 20130133289Abstract: Amorphous valgancyclovir hydrochloride has a median particle size of below 100 ?m. A process for the preparation of the compound includes dissolving valgancyclovir hydrochloride in at least one solvent, removing the solvents under moisture controlled conditions, and drying the wet mass.Type: ApplicationFiled: May 24, 2012Publication date: May 30, 2013Inventors: Madhuresh Kumar Sethi, Vijendra Singh Ravat, Raja Krishna Yerramalla, Lakshminarayana Vemula, Jagan Mohana Rao Bontalakoti, Kartikeyan Ayyaran, Debashish Datta
-
Publication number: 20130136764Abstract: The present invention refers to the preparation of adenine derivative active esters of formula (I) and use thereof for the preparation of stable conjugates between adenine derivative and allergenic proteins having general structure (II) for the modulation of TH2 response in allergic diseases.(I, II).Type: ApplicationFiled: August 4, 2011Publication date: May 30, 2013Applicant: UNIVERSITA ' DEGLI STUDI DI FIRENZEInventors: Sergio Romagnani, Enrico Maggi, Paola Parronchi, Antonio Guarna, Ernesto Giovanni Occhiato
-
Publication number: 20130131038Abstract: N-containing heteroaryl derivatives of formula I or II, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK, particularly JAK3, kinase inhibitors.Type: ApplicationFiled: October 29, 2010Publication date: May 23, 2013Inventors: Carmen Almansa Rosales, Jorge Salas Solana, Robert Soliva Soliva, Sergio RodrĆguez Escrich, Maria Cristina Sicre GonzĆ„les
-
Publication number: 20130129651Abstract: The present invention has objects to provide an agent for enhancing the effect of skin-whitening ingredients which enhances the skin-whitening action of skin-whitening ingredients and has an improved safeness, and to provide a skin-whitening agent, which contains the above agent and a skin-whitening ingredient(s) and has an improved and enhanced skin-whitening action. The present invention solves the above objects by providing an agent for enhancing the effect of skin-whitening ingredients, which contains one or more members selected from the group consisting of guanine and derivatives thereof as an effective ingredient(s); and a skin-whitening agent which contains the above agent along with a skin-whitening ingredient(s) particularly, members derivatives thereof and/or equol including derivatives thereof.Type: ApplicationFiled: July 28, 2011Publication date: May 23, 2013Applicant: HAYASHIBARA CO., LTD.Inventors: Masaki Miyake, Osamu Sano, Kanso Iwaki, Takanori Okura, Shigeharu Fukuda
-
Publication number: 20130089512Abstract: New heteroaryl imidazolone derivatives having the chemical structure of formula (I) are disclosed, as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: ApplicationFiled: June 14, 2011Publication date: April 11, 2013Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Elena Gomez Castillo, Jordi Bach TaƱa
-
Publication number: 20130079327Abstract: Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.Type: ApplicationFiled: May 30, 2011Publication date: March 28, 2013Inventors: Shingo Yamamoto, Toshio Yoshizawa
-
Publication number: 20130079324Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, T, V, W, X, Y, Z, ring A, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and m are defined herein. There novel pyrrolopyrimidine and purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.Type: ApplicationFiled: September 14, 2012Publication date: March 28, 2013Inventors: Hengmiao Cheng, Theodore Otto Johnson, JR., John Charles Kath, Kevin Kun-Chin Liu, Elizabeth Ann Lunney, Asako Nagata, Sajiv Krishnan Nair, Simon Paul Planken, Scott Channing Sutton
-
Publication number: 20130072506Abstract: 6,8-Disubstituted purines which can be used in drug and cosmetic compositions and/or applications are provided. These 6,8-disubstituted purines have a wide range of biological activities, including for example anti-inflammatory, anti-senescent, as well as well as other activities which are especially useful in pharmaceutical and cosmetic applications. The 6,8-disubstituted purine compounds and compositions containing such 6,8-disubstituted purines provide growth-regulatory, differentiating, antisenescent and antiaging properties with improved selectivities and efficiencies and lower toxicities than analogues known heretofore.Type: ApplicationFiled: September 12, 2012Publication date: March 21, 2013Inventors: Lenka ZAHAJSKA, Jan Hanus, Lukas Spichal, Jiri Voller, Miroslav Strnad
-
Publication number: 20130066071Abstract: Anti-virally active carbanucleosides such as entecavir are prepared by a process which utilizes, throughout the synthesis, an aromatic protectant group for the hydroxyl and the alkyl hydroxy groups of the starting material, removed as the final step of a multi-step synthesis. Such protectant groups yield intermediates which are solid and therefore easily purified at various stages of the process, for an economical and relatively fast process for synthesizing the final product.Type: ApplicationFiled: May 30, 2011Publication date: March 14, 2013Applicant: ALPHORA RESEARCH INC.Inventors: Dino Alberico, Boris Gorin, Ryan Beharrilall, Craig Dixon, Joshua Clayton, Varghese Rexon
-
Publication number: 20130053406Abstract: The invention provides novel therapeutic compounds, pharmaceutical compositions comprising these compounds, and methods for using these compounds and compositions to treat diseases and disorders such as cancer.Type: ApplicationFiled: August 23, 2010Publication date: February 28, 2013Applicant: Myrexis, Inc.Inventors: SE-HO KIM, Herbert L. Ley, III, Ashok Bajji
-
Publication number: 20130040949Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: ApplicationFiled: December 29, 2010Publication date: February 14, 2013Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael S. Gray, Hwan G. Choi, Xianming Deng, Jianming Zhang
-
Patent number: 8372852Abstract: Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders.Type: GrantFiled: May 11, 2012Date of Patent: February 12, 2013Assignee: Ardea Biosciences, Inc.Inventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
-
Patent number: 8357374Abstract: The invention provides TLR agonists and conjugates thereof useful in vaccines and to prevent, inhibit or treat a variety of disorders including pathogen infection and asthma.Type: GrantFiled: February 7, 2008Date of Patent: January 22, 2013Assignee: The Regents of the University of CaliforniaInventors: Dennis A. Carson, Wolfgang Wrasidlo, Christina C. N. Wu
-
Publication number: 20130005749Abstract: The invention relates to extended release compositions and formulations comprising 6-thioguanine (6-TG), and methods for treating diseases or conditions responsive to 6-TG.Type: ApplicationFiled: June 8, 2012Publication date: January 3, 2013Applicant: The University of QueenslandInventors: Timothy Henri Jeremy Florin, Yunmei Song, Xianling Luo
-
Publication number: 20130005687Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: ApplicationFiled: September 12, 2012Publication date: January 3, 2013Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C. Rech, Wei Xiao
-
Patent number: 8338593Abstract: The present application provides for 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: July 6, 2007Date of Patent: December 25, 2012Assignee: Gilead Sciences, Inc.Inventors: Lee S. Chong, Manoj C. Desai, Brian Gallagher, Michael Graupe, Randall L. Halcomb, Hong Yang, Jennifer R. Zhang
-
Publication number: 20120315291Abstract: The present invention relates to compounds of formula (I): wherein; R1 represents hydrogen or C1-3alkyl; n is an integer having a value of 1 to 5; X represents O or NH; Y represents C or N; or a pharmaceutically acceptable salt thereof, have been shown to be inducers of human interferon and may possess an improved profile with respect to known inducers of human interferon, for example enhanced potency. The compounds of the invention may therefore be useful in the treatment of various disorders, in particular the treatment of infectious diseases, cancer, allergic diseases and other inflammatory conditions, and their use as vaccine adjuvants.Type: ApplicationFiled: February 8, 2011Publication date: December 13, 2012Applicant: GLAXOSMITHKLINE LLCInventors: Helene Bazin-Lee, Diane Mary Coe, David A. Johnson, Charlotte Jane Mitchell
-
Patent number: 8329926Abstract: The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: July 27, 2005Date of Patent: December 11, 2012Assignee: Gilead Sciences, Inc.Inventors: Constantine G. Boojamra, Kuei-Ying Lin, Richard L. Mackman, David Y. Markevitch, Oleg V. Petrakovsky, Adrian S. Ray, Lijun Zhang
-
Publication number: 20120308652Abstract: The invention relates to pharmaceutical formulations, preferably in the form of an oral dosage form, for the treatment of chronic hepatitis-B virus infections, containing micronised Entecavir, and processes for preparing it. The invention further relates to intermediates containing micronised entecavir, in which the D50 value for the particle size distribution is less than 50 ?m, and processes for preparing them.Type: ApplicationFiled: December 22, 2010Publication date: December 6, 2012Inventors: Daniela Stumm, Jana Paetz
-
Publication number: 20120308609Abstract: The present invention relates to a compound which is 6-amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one: in the form of a maleate salt, may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.Type: ApplicationFiled: February 8, 2011Publication date: December 6, 2012Applicant: GlaxoSmithKline LLCInventors: Robert Hermann Gibbon, Amanda Lucas, Stephen Andrew Hermitage
-
Patent number: 8324381Abstract: A process for the preparation of valganciclovir with triacetyl ganciclovir (V) as a starting material, comprising the following steps: selective hydrolysis, reacting with a coupling agent and CBZ valine and a solvent, followed by hydrolysis under basic conditions and hydrogenolysis in the presence of a catalyst.Type: GrantFiled: March 20, 2007Date of Patent: December 4, 2012Assignee: CIPLA LimitedInventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Vidyadhar Purushottam Pande
-
Patent number: 8309555Abstract: The present invention provides 2,6-disubstituted purine compounds, compositions and methods for dedifferentiating lineage committed mammalian cells into stem cells. The present invention also provides methods of inducing dedifferentiation of lineage committed mammalian cells into stem cells, which can be further differentiated into various lineage committed cells. Methods of identifying additional 2,6-disubstituted purine compounds useful for inducing dedifferentiation of lineage committed cells into stem cells are also provided.Type: GrantFiled: September 21, 2009Date of Patent: November 13, 2012Assignee: The Scripps Research InstituteInventors: Shuibing Chen, Sheng Ding, Peter G. Schultz
-
Publication number: 20120283438Abstract: The present invention includes novel compounds useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants.Type: ApplicationFiled: July 18, 2012Publication date: November 8, 2012Applicant: GLAXOSMITHKLINE LLCInventors: Linos LAZARIDES, Stephen Allan SMITH, Richard STOCKER, Colin Jack THEOBALD
-
Publication number: 20120277206Abstract: Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders.Type: ApplicationFiled: May 11, 2012Publication date: November 1, 2012Applicant: Andrea Boesciences, Inc.Inventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
-
Patent number: 8288397Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: GrantFiled: December 16, 2008Date of Patent: October 16, 2012Assignee: Janssen Pharmaceutica NVInventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C Rech, Wei Xiao
-
Publication number: 20120252791Abstract: The present invention relates to the field of small molecule heterocyclic inhibitors of GTP cyclohydrolase (GCH-I), or a tautomer, prodrug, or pharmaceutically acceptable salt thereof. The invention also features pharmaceutical compositions of the compounds and the medical use of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, or neuropathic pain).Type: ApplicationFiled: September 16, 2010Publication date: October 4, 2012Inventor: Julian Blagg