Nitrogen Bonded Directly To Ring Carbon Of The Purine Ring System (e.g., Adenine, Etc.) Patents (Class 514/263.4)
  • Publication number: 20100172993
    Abstract: The present invention discloses compositions having particles comprising, inorganic element; one or more active ingredient and optionally a release rate modulating agent, suitable for the delivery of active ingredients to human and animal tissues. The particles are nanoparticles or microparticles or mixtures thereof, made preferably by sol-gel method. The compositions are useful for application to the topical or mucosal surfaces preferably in the form of creams, gels, lotions, dry powders, spray, foam and other suitable forms.
    Type: Application
    Filed: August 10, 2007
    Publication date: July 8, 2010
    Inventors: Amarjit Singh, Sarabjit Singh, Paramjit Singh, Rajesh Jain
  • Publication number: 20100166798
    Abstract: The method includes the steps of cleansing of the scalp sufficiently to remove material which would otherwise block antiviral medication from reaching hair follicles, heating the scalp to increase the absorption of the antiviral medication and applying the antiviral medication to the scalp in effective amount to suppress viral replication or viral activation present in the nerves leading to the scalp.
    Type: Application
    Filed: November 4, 2009
    Publication date: July 1, 2010
    Applicant: Pacific Bioscience Laboratories, Inc.
    Inventor: Robert E. Akridge
  • Publication number: 20100152210
    Abstract: This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.
    Type: Application
    Filed: March 27, 2008
    Publication date: June 17, 2010
    Applicant: NEURO SEARCH A/S/
    Inventors: Birgitte L. Eriksen, Ulrik Svane Sørensen, Charlotte Hougaard, Dan Peters, Tina Holm Johansen, Palle Christophersen
  • Patent number: 7736636
    Abstract: Disclosed are methods of treating subjects having conditions related to angiogenesis including administering an effective amount of a polymeric form of Nicotine, nicotinic acid analogs thereof, their combination with or without other pro-angiogenesis factors, vasodilator, or other therapeutic modalities to promote angiogenesis in the subject. This is composition and combination thereof is applicable to improving wound healing, erectile dysfunction, improving collateral or blood supply in patients with myocardial infarction, stroke, peripheral artery diseases, and other vascular disorders as disclosed.
    Type: Grant
    Filed: February 11, 2004
    Date of Patent: June 15, 2010
    Inventors: Shaker Mousa, Sarah Mousa
  • Patent number: 7737127
    Abstract: The invention provides compounds having the following general formula (I): wherein X, R1, R2, R7 and Z are as described here.
    Type: Grant
    Filed: March 26, 2007
    Date of Patent: June 15, 2010
    Assignee: University of Virginia Patent Foundation
    Inventors: Joel M. Linden, Jayson M. Rieger, Timothy L. Macdonald, Gail W. Sullivan, Lauren Jean Murphree, Robert Alan Figler
  • Publication number: 20100136106
    Abstract: The invention relates to a multiparticulate modified release composition that, upon administration to a patient, delivers famciclovir in a bimodal, multimodal or continuous manner. The multiparticulate modified release composition comprises a first component and at least one subsequent component, the first component comprising a first population of active ingredient containing particles and the at least one subsequent component comprising a second population of active ingredient containing particles. The invention also relates to a solid oral dosage form containing such a multiparticulate modified release composition, and to a method for the treatment or suppression of viral infections.
    Type: Application
    Filed: June 7, 2006
    Publication date: June 3, 2010
    Inventors: Gary Liversidge, Scott Jenkins, John G. Devane, Paul Stark, Niall Fanning, Gurvinder Singh Rekhi
  • Publication number: 20100129321
    Abstract: The present invention relates to pharmaceutical compositions for treating virus infections and/or diseases caused thereby comprising 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide optionally combined with at least one additional therapeutic agent.
    Type: Application
    Filed: December 6, 2006
    Publication date: May 27, 2010
    Applicant: BAYER HEALTHCARE LLC
    Inventors: Olaf Weber, Bernd Riedl
  • Publication number: 20100130476
    Abstract: The present invention relates to compounds and compositions for inducing the expansion of pancreatic ?-cells. The invention further relates to a use of these expanded pancreatic ?-cells to reversibly expand pancreatic ?-cells and other quiescent cells to overcome deficits associated with degenerative and/or autoimmune diseases.
    Type: Application
    Filed: November 12, 2009
    Publication date: May 27, 2010
    Applicant: The Scripps Research Institute
    Inventors: Weidong Wang, Peter G. Schultz
  • Patent number: 7723340
    Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
    Type: Grant
    Filed: January 12, 2006
    Date of Patent: May 25, 2010
    Assignees: Signal Pharmaceuticals, LLC, Pharmacopeia Drug Discovery, Inc.
    Inventors: Ronald J. Albers, Leticia Ayala, Steven S. Clareen, Maria Mercedes Delgado Mederos, Robert Hilgraf, Sayee G. Hegde, Kevin Hughes, Adam Kois, Veronique Plantevin-Krenitsky, Meg McCarrick, Lisa Nadolny, Moorthy S. S. Palanki, Kiran Sahasrabudhe, John Sapienza, Yoshitaka Satoh, Marianne K. Sloss, Elise Sudbeck, Jonathan Wright, Ian Henderson, Andrew G. Cole
  • Publication number: 20100119479
    Abstract: Disclosed herein are compounds represented by a formula: Therapeutic methods, compositions, medicaments, and dosage forms related thereto are also disclosed.
    Type: Application
    Filed: October 14, 2009
    Publication date: May 13, 2010
    Applicant: INTERMUNE, INC.
    Inventors: BRAD BUCKMAN, VLADIMIR SEREBRYANY, SCOTT SEIWERT, LEONID BEIGELMAN, ANTITSA STOYCHEVA
  • Publication number: 20100105631
    Abstract: Inositol derivatives are described that are represented by the structural formula I wherein X is a radical of scyllo-inositol wherein one or more of R1, R2, R3, R4, R5, and R6 are independently alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfoxide, sulfate, sulfonyl, sulfenyl, sulfonate, sulfinyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, seleno, silyl, silyloxy, silylthio, carboxyl, carbonyl, carbamoyl, or carboxamide and the other of R1, R2, R3, R4, R5, or R6 are hydroxyl, or pharmaceutically acceptable salts thereof. The compounds, compositions comprising same and methods using same are described for use in the prevention and/or treatment of diseases characterized by abnormal protein folding or aggregation or amyloid formation, desposition, accumulation or persistence.
    Type: Application
    Filed: November 11, 2009
    Publication date: April 29, 2010
    Inventors: Antonio Curz, Linda Kurdydyk
  • Publication number: 20100105652
    Abstract: Substituted heteroaryl nitrile salt of Formula I, processes for their preparation, pharmaceutical compositions comprising such compounds and use of the compounds as cysteine protease inhibitors are provided.
    Type: Application
    Filed: February 28, 2008
    Publication date: April 29, 2010
    Inventors: Jose Miguel Coteron-Lopez, Beatriz Diaz-Hernandez, Jose Maria Fiandor-Roman, Maria Marco-Martin
  • Patent number: 7704530
    Abstract: The present invention is an antimicrobially-treated material which has a coloring preventing function and is in contact with water or moisture or contains water, comprising (A) a silver-based antimicrobial agent which dissociates silver ions in the water system and (B) a silver ion trapping agent for trapping silver ions comprising one or more kinds of compounds selected from the group consisting of purine bases, pyrimidine bases, thiabendazole, and potassium iodide, wherein a ratio of (A)/(B) is 1/1 to 100/1 by weight.
    Type: Grant
    Filed: September 10, 2002
    Date of Patent: April 27, 2010
    Inventors: Kenji Nakamura, Koji Nakamura
  • Publication number: 20100093769
    Abstract: The present invention relates to compounds of formula (I) wherein: R1 and R2 are each independently H, alkyl or haloalkyl; R3 and R4 are each independently H, alkyl, haloalkyl or aryl; R5 is alkyl or cycloalkyl or cycloalkyl-alkyl, each of which may be optionally substituted with one or more OH groups; R6 is selected from cyclopropylamino, cyclopropylmethylamino, cyclobutylamino, cyclobutylmethylamino and where one of X, Y and Z is N and the remainder are CR9; R7, R8 and each R9 are independently H, alkyl or haloalkyl, wherein at least one of R7, R8 and each R9 is other than H. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula (I), and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.
    Type: Application
    Filed: October 5, 2009
    Publication date: April 15, 2010
    Applicants: CYCLACEL LIMITED, CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Peter William SHELDRAKE, Butrus ATRASH, Simon GREEN, Edward MCDONALD, Sheelagh FRAME
  • Publication number: 20100075915
    Abstract: The present invention relates to a method of inducing apoptosis in a tumour cell as well as modulating pluripotency and/or self-renewing characteristics of a stem/progenitor cell. The method comprises administering to the respective cell a compound of general formula (I). In general formula A is C or N. R1, R4 and R5 are, independently selected, H or aliphatic, cycloaliphatic aromatic, arylaliphatic, or arylcycloaliphatic hydrocarbyl groups, that comprise 0-3 heteroatoms being N, O, S, or Si. R4 and R5 may optionally be linked so as to define an aliphatic hydrocarbyl bridge. R2 is H or a halogen, such as F or Cl. R3 is H, or an aliphatic or arylaliphatic hydrocarbyl group comprising 1-8 main chain carbon atoms and 0-3 heteroatoms being N, O, S, Si, or a halogen such as Cl or F. Also provided is a pharmaceutical composition for inducing apoptosis in a tumour cell and/or modulating pluripotency and/or self-renewing characteristics of a stem/progenitor cell.
    Type: Application
    Filed: November 15, 2006
    Publication date: March 25, 2010
    Applicant: Agency for Science, Technology and Research
    Inventors: Qiang Yu, Jing Tan, Xiao Jing Yang
  • Publication number: 20100075914
    Abstract: The present invention relates to methods for treating, killing, and/or inhibiting the growth of Herpes viruses in human subjects comprising topically administering to a human subject in need thereof a nanoemulsion composition having antiviral properties.
    Type: Application
    Filed: April 17, 2009
    Publication date: March 25, 2010
    Inventors: Mary R. FLACK, Susan Marie CIOTTI, Tarek HAMOUDA, Joyce A. SUTCLIFFE, James R. Baker, JR.
  • Publication number: 20100069383
    Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
    Type: Application
    Filed: July 10, 2009
    Publication date: March 18, 2010
    Applicant: Myriad Pharmaceuticals, Incorporated
    Inventors: MARK B. ANDERSON, J. Adam Willardsen, Warren S. Weiner, Ashantai Yungai, Robert J. Halter, Yevgeniya Klimova, Kazuyuki Suzuki, Matthew Reeder
  • Publication number: 20100069369
    Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.
    Type: Application
    Filed: September 1, 2009
    Publication date: March 18, 2010
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Pingyu Ding, Ankush Argade, Dane Goff, Rajinder Singh, Esteban Masuda, Vanessa Taylor, Sacha Holland
  • Publication number: 20100063004
    Abstract: This invention relates to a novel topical pharmaceutical composition. In particular, this invention is an overnight topical composition for treating cold sores.
    Type: Application
    Filed: December 3, 2007
    Publication date: March 11, 2010
    Inventors: Ranjan Ray Chaudhuri, Satish Ramchandra Dipali, Phillip E. West
  • Patent number: 7671036
    Abstract: The present invention relates to novel types of peptide nucleic acids (PNAS) with improved properties. In particular, it relates to positively charged PNA units having an ethylene linker between the backbone and the nucleobase, to oligonucleotide analogs comprising these units, to oligomers comprising these units, and to the use of positively charged PNAs as novel delivery agents with therapeutic and diagnostic applications including for antisense therapy.
    Type: Grant
    Filed: June 22, 2001
    Date of Patent: March 2, 2010
    Assignee: Yissum Research Development Company of The Hebrew University of Jerusalem
    Inventors: Jehoshua Katzhendler, Ada Schlossman, Yousuf Najajreh, Dan Gibson
  • Publication number: 20100022562
    Abstract: The present invention describes methods for maintaining ABA-induced drought tolerance while reducing ABA-induced leaf yellowing through the combination of ABA with selected plant growth regulators. The present invention also describes a method of using selected ABA analogs to reduce water use with minimal leaf yellowing.
    Type: Application
    Filed: July 23, 2009
    Publication date: January 28, 2010
    Inventors: Xiaozhong Liu, Derek D. Woolard, Peter D. Petracek
  • Publication number: 20100010020
    Abstract: PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.
    Type: Application
    Filed: September 22, 2009
    Publication date: January 14, 2010
    Inventors: Ruiping LIU, Hans-Jurgen Ernst Hess, Allen Hopper, Ashok Tehim, Yujing Rong
  • Publication number: 20100008927
    Abstract: The present invention relates to the use of 6-(benzyl-amino)-2(S)-[[1-(hydroxymethyl) propyl]amino]-9-isopropylpurine) or at least one of its pharmaceutical acceptable salts for manufacturing a medication intended for the prevention and/or treatment of neurological diseases, in particular associated with neurological lesions.
    Type: Application
    Filed: March 30, 2007
    Publication date: January 14, 2010
    Applicant: NEUROKIN INMED
    Inventors: Serge Timsit, Bénédicte Menn, Laurent Meijer
  • Publication number: 20100004236
    Abstract: PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.
    Type: Application
    Filed: February 26, 2009
    Publication date: January 7, 2010
    Inventors: Ashok Tehim, Allen T. Hopper, Ruiping Liu, Hans-Juregen Ernst Hess, Yajing Rong
  • Publication number: 20090325931
    Abstract: Described herein is the use of CDK inhibitors such as roscovitine for inducing apoptosis of granulocytes, for example neutrophils. Their use for treating inflammatory diseases is also provided.
    Type: Application
    Filed: July 30, 2007
    Publication date: December 31, 2009
    Applicant: University Court of the University of Edinburgh
    Inventors: Adriano Rossi, Christopher Haslett
  • Publication number: 20090312320
    Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
    Type: Application
    Filed: August 12, 2009
    Publication date: December 17, 2009
    Inventors: Ronald J. Albers, Leticia Ayala, Steven S. Clareen, Maria Mercedes Delgado Mederos, Robert Hilgraf, Sayee G. Hegde, Kevin Hughes, Adam Kois, Veronique Plantevin-Krenitsky, Meg McCarrick, Lisa Nadolny, Moorthy S.S. Palanki, Kiran Sahasrabudhe, John Sapienza, Yoshitaka Satoh, Marianne K. Sloss, Elise Sudbeck, Jonathan Wright, Ian Henderson, Andrew G. Cole
  • Publication number: 20090306098
    Abstract: A first aspect of the invention relates to a combination comprising roscovitine, or a pharmaceutically acceptable salt thereof, and a HDAC inhibitor selected from sodium butyrate, or a prodrug thereof, suberoylanilide hydroxamic acid (SAHA), sodium valproate and trichostatin A (TSA). A second aspect of the invention relates to a pharmaceutical product comprising roscovitine, or a pharmaceutically acceptable salt thereof, and a HDAC inhibitor selected from sodium butyrate, or a prodrug thereof, suberoylanilide hydroxamic acid (SAHA), sodium valproate and trichostatin A (TSA) as a combined preparation for simultaneous, sequential or separate use in therapy.
    Type: Application
    Filed: November 13, 2006
    Publication date: December 10, 2009
    Applicant: Cyclacel Limited
    Inventors: Simon Green, Sheelagh Frame, Ian Fleming
  • Publication number: 20090306099
    Abstract: Methods of assessing the risk of clinical signs of hypersensitivity reaction to nucleoside antiviral compounds, including abacavir, are described. The methods include genotyping subjects for polymorphisms in the TNF? gene, the class 1 HLA genes, or a combination of both the TNF? and HLA genes.
    Type: Application
    Filed: April 22, 2009
    Publication date: December 10, 2009
    Inventors: Seth HETHERINGTON, Arlene R. HUGHES, Eric H. LAI, Michael MOSTELLER, JR., Denise D. SHORTINO
  • Publication number: 20090281126
    Abstract: A compound of formula (I) and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.
    Type: Application
    Filed: April 19, 2007
    Publication date: November 12, 2009
    Inventors: Robin Alec Fairhurst, Roger John Taylor
  • Publication number: 20090281127
    Abstract: A compound of formula (I) and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.
    Type: Application
    Filed: April 19, 2007
    Publication date: November 12, 2009
    Inventors: Robin Alec Fairhurst, Roger John Taylor
  • Publication number: 20090274650
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Application
    Filed: February 12, 2009
    Publication date: November 5, 2009
    Inventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
  • Publication number: 20090275564
    Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
    Type: Application
    Filed: March 16, 2009
    Publication date: November 5, 2009
    Inventors: Ronald J. Albers, Leticia Ayala, Steven S. Clareen, Maria Mercedes Delgado Mederos, Robert Hilgraf, Sayee G. Hegde, Kevin Hughes, Adam Kois, Veronique Plantevin-Krenitsky, Meg McCarrick, Lisa Nadolny, Moorthy S.S. Palanki, Kiran Sahasrabudhe, John Sapienza, Yoshitaka Satoh, Marianne K. Sloss, Elise Sudbeck, Jonathan Wright
  • Patent number: 7612079
    Abstract: The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof wherein R2 is 2-hydroxymethylpyrrolidin-1-yl, or NHCH(R4)CH(R3)OH, wherein R3 is hydrogen or methyl and R4 is methyl, ethyl or isopropyl; R6 is 3-nitrophenylamino, 3,4-dimethoxybenzylamino, 3-iodobenzyl-amino, pyrid-2-yl-methylamino, pyrid-4-yl-methylamino or indan-5-amino; R9 is isopropyl or cyclopentanyl. In a further aspect, the invention relates to pharmaceutical compositions comprising said compounds, and the use thereof in treating antiproliferative disorders and or viral disorders.
    Type: Grant
    Filed: December 18, 2003
    Date of Patent: November 3, 2009
    Assignees: Cyclacel Limited, Cancer Research Technology Limited
    Inventors: Peter Martin Fischer, Mike Jarman, Ted McDonald, Bernard Nutley, Florence Raynaud, Stuart Wilson, Paul Workman
  • Patent number: 7608601
    Abstract: The present invention relates to the use of nucleoside derivatives of formula I wherein B signifies a 9-purinyl residue B1 of formula or a 1-pyrimidyl residue B2 of formula wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof; for the treatment of diseases mediated by the Hepatitis C Virus (HCV), for the preparation of a medicament for such treatment and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: July 15, 2004
    Date of Patent: October 27, 2009
    Assignee: Roche Palo Alto LLC
    Inventors: Rene Robert Devos, Christopher John Hobbs, Wen Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda
  • Patent number: 7601713
    Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.
    Type: Grant
    Filed: December 15, 2006
    Date of Patent: October 13, 2009
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Pingyu Ding, Ankush Argade, Dane Goff, Rajinder Singh, Esteban Masuda, Vanessa Taylor, Sacha Holland
  • Publication number: 20090253718
    Abstract: The invention provides a compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N?C(R6), (R7)C?N, (R8)N—C(O), (R8)2C—C(O), N?N or (R7)C?C(R6); A is an optionally substituted saturated C1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, one of the carbon atoms in the linker group being optionally replaced by oxygen or nitrogen; E is a monocyclic or bicyclic carbocyclic or heterocyclic group or an acyclic group X-G wherein X is CH2, O, S or NH and G is a C1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R1 is hydrogen or an aryl or heteroaryl group; R2 and R3 are each hydrogen, optionally substituted C1-4 hydrocarbyl or optionally substituted C1-4 acyl; or NR2R3 forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR2R3 and A together form a satur
    Type: Application
    Filed: April 25, 2007
    Publication date: October 8, 2009
    Applicants: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology Limited
    Inventors: Thomas Glanmor Davies, Michelle Dawn Garrett, Robert George Boyle, Ian Collins
  • Publication number: 20090247487
    Abstract: The present invention is directed to a method for treating hepatitis B virus infection in humans comprising administering a synergistically effective amount of agents having known anti-hepatitis B virus activity in combination or alternation. Specifically, the invention is directed to a method for treating hepatitis B virus infection comprising administering FTC in combination or alternation with penciclovir, famciclovir or Bis-POM-PMEA. Additionally, the invention is directed to a method for treating hepatitis B virus infection comprising administering L-FMAU in combination or alternation with DAPD, penciclovir or Bis-POM-PMEA. The invention is further directed to a method for treating hepatitis B virus infection comprising administering DAPD in combination or alternation with Bis-POM-PMEA.
    Type: Application
    Filed: June 12, 2009
    Publication date: October 1, 2009
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Phillip A. Furman, George R. Painter, III, David W. Barry, Franck Rousseau
  • Publication number: 20090233922
    Abstract: A method for the combined treatment of neuronal and non-neuronal pain in mammals is provided comprising administration of adenylyl cyclase 1 inhibitors having the following general formula (1): (1) wherein: G, H, J and M are each N, or H and J are each C, and G and M are each N, S or O, or H, J and M are each C and G is N, S or O.
    Type: Application
    Filed: October 13, 2006
    Publication date: September 17, 2009
    Inventor: Min Zhuo
  • Publication number: 20090233872
    Abstract: [Problems] To provide a neuronal cell death inhibitor and a therapeutic agent for a neurodegenerative disease, particularly Parkinson's disease. [Means for Solving Problems] It is known that DJ-1 protein is involved in Parkinson's disease and is capable of inhibiting neuronal cell death caused by oxidative stress. Based on this knowledge, screening is made for a low molecular weight molecule capable of binding to an active site of DJ-1 protein (i.e., a region around a cysteine residue at position-106) using an analysis softwear FastDock (Fujitsu Ltd.). When various tests are made using candidate low molecular weight compounds each having a binding energy of ?60 kcal/mol or lower, these compounds show a therapeutic effect on a neurodegenerative disease.
    Type: Application
    Filed: November 17, 2006
    Publication date: September 17, 2009
    Applicant: National University Corporation Hokkaido University
    Inventor: Hiroyoshi Ariga
  • Publication number: 20090209557
    Abstract: Compounds according to Formula I, Formula II, Formula III, Formula V, Formula VI, or to Formula VII, and pharmaceutical compositions of compounds that conform to Formula IV or Formula VIII: where R1 through R33 are prescribed, selectively inhibit P. falciparum dihydroorotate dehydrogenase. Accordingly, a method for preventing and treating malaria attaches to such compounds, as well as to pharmaceutically acceptable salts, solvates, stereoisomers, tautomers, and prodrugs thereof.
    Type: Application
    Filed: December 19, 2008
    Publication date: August 20, 2009
    Inventors: Margaret PHILLIPS, Pradipsinh K. Rathod, Ramesh Gujjar, Alka Marwaha, Susan A. Charman
  • Publication number: 20090203636
    Abstract: Nucleoside chemical compounds, which interact with specific structures of deoxyribonucleic acid (DNA) or ribonucleic acid (RNA) are disclosed. The compounds interfere with the activities of telomerase and reverse transcriptase, and are useful as antivirals, antibacterials and anticancer agents. Methods of treating or preventing cancers in patients involving administration of a therapeutically effective amount of a composition having an inhibitor or antagonist of the reverse transcriptases (RTs) expressed in cells of the patients are also disclosed. Method of using nucleoside analogs and other inhibitors of RTs in conjunction with DNA damaging agents such as genotoxic agents or radiation or photodynamic therapy or combinations these for the treatment of various cancers are also disclosed.
    Type: Application
    Filed: March 14, 2007
    Publication date: August 13, 2009
    Inventor: Igor E. Bondarev
  • Publication number: 20090203638
    Abstract: Pharmaceutical compositions include compounds with cytokinin activity to modulate glucose and/or lipid metabolism in a mammal. Especially preferred compounds include those comprising a purine scaffold, and it is further preferred that contemplated compositions are employed to prevent and/or treat various diseases, including pre-diabetes, insulin resistance, type-2 diabetes, Syndrome X, and dyslipidemia. In still further preferred aspects, compounds with cytokinin activity are used to activate AMPK and/or Akt. Consequently, various diseases associated with dysregulation of AMPK and/or Akt may be treated using the compounds of the present inventive subject matter.
    Type: Application
    Filed: April 7, 2009
    Publication date: August 13, 2009
    Applicant: VDF FUTURECEUTICALS, INC.
    Inventors: Dusan Miljkovic, Jovan Hranisavljevic, Zbigniew Pietrzkowski
  • Patent number: 7572800
    Abstract: The present invention is directed to a method for treating hepatitis B virus infection in humans comprising administering a synergistically effective amount of agents having known anti-hepatitis B virus activity in combination or alternation. Specifically, the invention is directed to a method for treating hepatitis B virus infection comprising administering FTC in combination or alternation with penciclovir, famciclovir or Bis-POM-PMEA. Additionally, the invention is directed to a method for treating hepatitis B virus infection comprising administering L-FMAU in combination or alternation with DAPD, penciclovir or Bis-POM-PMEA. The invention is further directed to a method for treating hepatitis B virus infection comprising administering DAPD in combination or alternation with Bis-POM-PMEA.
    Type: Grant
    Filed: February 25, 2003
    Date of Patent: August 11, 2009
    Assignee: Gilead Sciences, Inc.
    Inventors: Phillip A. Furman, George R. Painter, III, David W. Barry, Franck Rousseau
  • Publication number: 20090181988
    Abstract: This invention generally relates to pyrazolo pyrimidine derivatives useful as, inter alia, inhibitors of short chain dehydrogenase/reductase (SDR) family of NAD(P)(H) dependent oxido-reductases. More specifically, the invention relates to pyrazolo pyrimidine derivatives, including derivatives and analogs of SDR inhibitors, pharmaceutical compositions containing derivatives and analogs of SDR inhibitors, methods of making derivatives and analogs of SDR inhibitors and methods of use thereof.
    Type: Application
    Filed: August 19, 2008
    Publication date: July 16, 2009
    Applicant: The Regents of the University of California
    Inventors: Masahiro Tanaka, Chao Zhang, Kevan M. Shokat, Alma L. Burlingame, Kirk Hansen, Raynard L. Bateman, Stephen G. DiMagno
  • Patent number: 7560483
    Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
    Type: Grant
    Filed: June 21, 2005
    Date of Patent: July 14, 2009
    Assignee: XenoPort, Inc.
    Inventors: Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat, Cindy X. Zhou
  • Publication number: 20090170879
    Abstract: Certain 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts are provided. These 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts are useful in compositions for treating mammalian cells, and especially human skin cells, in order to ameliorate the adverse effects of aging, treat skin disease states, treat immunological responses resulting from or associated with inflammation, and the like.
    Type: Application
    Filed: December 28, 2007
    Publication date: July 2, 2009
    Inventors: Lucie Szucova, Marek Zatloukal, Lukas Spichal, Jiri Voller, Karel Dolezal, Miroslav Strnad, Frank J. Massino
  • Publication number: 20090162319
    Abstract: 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: Application
    Filed: December 12, 2008
    Publication date: June 25, 2009
    Applicant: Ardea Biosciences
    Inventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
  • Publication number: 20090156598
    Abstract: Certain TRPV1-modulating imidazolopyrimidine 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: Application
    Filed: December 16, 2008
    Publication date: June 18, 2009
    Inventor: Alec D. Lebsack
  • Publication number: 20090149479
    Abstract: Methods and kits are provided enabling a twice daily dosing regimen that achieves daily patient blood levels of active pharmaceutical ingredient comparable to a dosing regimen requiring the same active ingredient to be administered three times a day.
    Type: Application
    Filed: September 12, 2008
    Publication date: June 11, 2009
    Applicant: Elan Pharma International Limited
    Inventors: Scott Jenkins, Gary Liversidge
  • Publication number: 20090118309
    Abstract: The present invention provides compounds of formulae Ia and Ib: wherein R1-5, Q, X, Y, Z, p, q, and r are as defined herein. The compounds are potent and selective antagonists of A2A adenosine receptors (ARs). The invention further includes pharmaceutical compositions containing these compounds and methods of using the same.
    Type: Application
    Filed: July 16, 2007
    Publication date: May 7, 2009
    Inventors: Anthony Beauglehole, Jayson M. Rieger, Robert D. Thompson