Nitrogen Bonded Directly To Ring Carbon Of The Purine Ring System (e.g., Adenine, Etc.) Patents (Class 514/263.4)
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Publication number: 20100172993Abstract: 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: ApplicationFiled: August 10, 2007Publication date: July 8, 2010Inventors: Amarjit Singh, Sarabjit Singh, Paramjit Singh, Rajesh Jain
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Publication number: 20100166798Abstract: 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: ApplicationFiled: November 4, 2009Publication date: July 1, 2010Applicant: Pacific Bioscience Laboratories, Inc.Inventor: Robert E. Akridge
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Publication number: 20100152210Abstract: 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: ApplicationFiled: March 27, 2008Publication date: June 17, 2010Applicant: NEURO SEARCH A/S/Inventors: Birgitte L. Eriksen, Ulrik Svane Sørensen, Charlotte Hougaard, Dan Peters, Tina Holm Johansen, Palle Christophersen
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Patent number: 7736636Abstract: 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: GrantFiled: February 11, 2004Date of Patent: June 15, 2010Inventors: Shaker Mousa, Sarah Mousa
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Patent number: 7737127Abstract: The invention provides compounds having the following general formula (I): wherein X, R1, R2, R7 and Z are as described here.Type: GrantFiled: March 26, 2007Date of Patent: June 15, 2010Assignee: University of Virginia Patent FoundationInventors: Joel M. Linden, Jayson M. Rieger, Timothy L. Macdonald, Gail W. Sullivan, Lauren Jean Murphree, Robert Alan Figler
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Publication number: 20100136106Abstract: 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: ApplicationFiled: June 7, 2006Publication date: June 3, 2010Inventors: Gary Liversidge, Scott Jenkins, John G. Devane, Paul Stark, Niall Fanning, Gurvinder Singh Rekhi
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Publication number: 20100129321Abstract: 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: ApplicationFiled: December 6, 2006Publication date: May 27, 2010Applicant: BAYER HEALTHCARE LLCInventors: Olaf Weber, Bernd Riedl
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Publication number: 20100130476Abstract: 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: ApplicationFiled: November 12, 2009Publication date: May 27, 2010Applicant: The Scripps Research InstituteInventors: Weidong Wang, Peter G. Schultz
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Patent number: 7723340Abstract: 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: GrantFiled: January 12, 2006Date of Patent: May 25, 2010Assignees: 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
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Publication number: 20100119479Abstract: Disclosed herein are compounds represented by a formula: Therapeutic methods, compositions, medicaments, and dosage forms related thereto are also disclosed.Type: ApplicationFiled: October 14, 2009Publication date: May 13, 2010Applicant: INTERMUNE, INC.Inventors: BRAD BUCKMAN, VLADIMIR SEREBRYANY, SCOTT SEIWERT, LEONID BEIGELMAN, ANTITSA STOYCHEVA
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Publication number: 20100105631Abstract: 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: ApplicationFiled: November 11, 2009Publication date: April 29, 2010Inventors: Antonio Curz, Linda Kurdydyk
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Publication number: 20100105652Abstract: 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: ApplicationFiled: February 28, 2008Publication date: April 29, 2010Inventors: Jose Miguel Coteron-Lopez, Beatriz Diaz-Hernandez, Jose Maria Fiandor-Roman, Maria Marco-Martin
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Patent number: 7704530Abstract: 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: GrantFiled: September 10, 2002Date of Patent: April 27, 2010Inventors: Kenji Nakamura, Koji Nakamura
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Publication number: 20100093769Abstract: 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: ApplicationFiled: October 5, 2009Publication date: April 15, 2010Applicants: CYCLACEL LIMITED, CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Peter William SHELDRAKE, Butrus ATRASH, Simon GREEN, Edward MCDONALD, Sheelagh FRAME
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Publication number: 20100075915Abstract: 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: ApplicationFiled: November 15, 2006Publication date: March 25, 2010Applicant: Agency for Science, Technology and ResearchInventors: Qiang Yu, Jing Tan, Xiao Jing Yang
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Publication number: 20100075914Abstract: 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: ApplicationFiled: April 17, 2009Publication date: March 25, 2010Inventors: Mary R. FLACK, Susan Marie CIOTTI, Tarek HAMOUDA, Joyce A. SUTCLIFFE, James R. Baker, JR.
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Publication number: 20100069383Abstract: 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: ApplicationFiled: July 10, 2009Publication date: March 18, 2010Applicant: Myriad Pharmaceuticals, IncorporatedInventors: MARK B. ANDERSON, J. Adam Willardsen, Warren S. Weiner, Ashantai Yungai, Robert J. Halter, Yevgeniya Klimova, Kazuyuki Suzuki, Matthew Reeder
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Publication number: 20100069369Abstract: 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: ApplicationFiled: September 1, 2009Publication date: March 18, 2010Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Pingyu Ding, Ankush Argade, Dane Goff, Rajinder Singh, Esteban Masuda, Vanessa Taylor, Sacha Holland
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Publication number: 20100063004Abstract: This invention relates to a novel topical pharmaceutical composition. In particular, this invention is an overnight topical composition for treating cold sores.Type: ApplicationFiled: December 3, 2007Publication date: March 11, 2010Inventors: Ranjan Ray Chaudhuri, Satish Ramchandra Dipali, Phillip E. West
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Patent number: 7671036Abstract: 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: GrantFiled: June 22, 2001Date of Patent: March 2, 2010Assignee: Yissum Research Development Company of The Hebrew University of JerusalemInventors: Jehoshua Katzhendler, Ada Schlossman, Yousuf Najajreh, Dan Gibson
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Publication number: 20100022562Abstract: 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: ApplicationFiled: July 23, 2009Publication date: January 28, 2010Inventors: Xiaozhong Liu, Derek D. Woolard, Peter D. Petracek
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Publication number: 20100010020Abstract: PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.Type: ApplicationFiled: September 22, 2009Publication date: January 14, 2010Inventors: Ruiping LIU, Hans-Jurgen Ernst Hess, Allen Hopper, Ashok Tehim, Yujing Rong
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Publication number: 20100008927Abstract: 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: ApplicationFiled: March 30, 2007Publication date: January 14, 2010Applicant: NEUROKIN INMEDInventors: Serge Timsit, Bénédicte Menn, Laurent Meijer
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Publication number: 20100004236Abstract: PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.Type: ApplicationFiled: February 26, 2009Publication date: January 7, 2010Inventors: Ashok Tehim, Allen T. Hopper, Ruiping Liu, Hans-Juregen Ernst Hess, Yajing Rong
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Publication number: 20090325931Abstract: 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: ApplicationFiled: July 30, 2007Publication date: December 31, 2009Applicant: University Court of the University of EdinburghInventors: Adriano Rossi, Christopher Haslett
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Publication number: 20090312320Abstract: 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: ApplicationFiled: August 12, 2009Publication date: December 17, 2009Inventors: 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
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Publication number: 20090306098Abstract: 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: ApplicationFiled: November 13, 2006Publication date: December 10, 2009Applicant: Cyclacel LimitedInventors: Simon Green, Sheelagh Frame, Ian Fleming
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Publication number: 20090306099Abstract: 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: ApplicationFiled: April 22, 2009Publication date: December 10, 2009Inventors: Seth HETHERINGTON, Arlene R. HUGHES, Eric H. LAI, Michael MOSTELLER, JR., Denise D. SHORTINO
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Publication number: 20090281126Abstract: A compound of formula (I) and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.Type: ApplicationFiled: April 19, 2007Publication date: November 12, 2009Inventors: Robin Alec Fairhurst, Roger John Taylor
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Publication number: 20090281127Abstract: A compound of formula (I) and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.Type: ApplicationFiled: April 19, 2007Publication date: November 12, 2009Inventors: Robin Alec Fairhurst, Roger John Taylor
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Publication number: 20090274650Abstract: 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: ApplicationFiled: February 12, 2009Publication date: November 5, 2009Inventors: 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
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Publication number: 20090275564Abstract: 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: ApplicationFiled: March 16, 2009Publication date: November 5, 2009Inventors: 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
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Patent number: 7612079Abstract: 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: GrantFiled: December 18, 2003Date of Patent: November 3, 2009Assignees: Cyclacel Limited, Cancer Research Technology LimitedInventors: Peter Martin Fischer, Mike Jarman, Ted McDonald, Bernard Nutley, Florence Raynaud, Stuart Wilson, Paul Workman
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Patent number: 7608601Abstract: 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: GrantFiled: July 15, 2004Date of Patent: October 27, 2009Assignee: Roche Palo Alto LLCInventors: Rene Robert Devos, Christopher John Hobbs, Wen Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda
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Patent number: 7601713Abstract: 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: GrantFiled: December 15, 2006Date of Patent: October 13, 2009Assignee: Rigel Pharmaceuticals, Inc.Inventors: Pingyu Ding, Ankush Argade, Dane Goff, Rajinder Singh, Esteban Masuda, Vanessa Taylor, Sacha Holland
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Publication number: 20090253718Abstract: 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 saturType: ApplicationFiled: April 25, 2007Publication date: October 8, 2009Applicants: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology LimitedInventors: Thomas Glanmor Davies, Michelle Dawn Garrett, Robert George Boyle, Ian Collins
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Publication number: 20090247487Abstract: 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: ApplicationFiled: June 12, 2009Publication date: October 1, 2009Applicant: GILEAD SCIENCES, INC.Inventors: Phillip A. Furman, George R. Painter, III, David W. Barry, Franck Rousseau
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Publication number: 20090233922Abstract: 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: ApplicationFiled: October 13, 2006Publication date: September 17, 2009Inventor: Min Zhuo
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Publication number: 20090233872Abstract: [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: ApplicationFiled: November 17, 2006Publication date: September 17, 2009Applicant: National University Corporation Hokkaido UniversityInventor: Hiroyoshi Ariga
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Publication number: 20090209557Abstract: 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: ApplicationFiled: December 19, 2008Publication date: August 20, 2009Inventors: Margaret PHILLIPS, Pradipsinh K. Rathod, Ramesh Gujjar, Alka Marwaha, Susan A. Charman
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Publication number: 20090203636Abstract: 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: ApplicationFiled: March 14, 2007Publication date: August 13, 2009Inventor: Igor E. Bondarev
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Publication number: 20090203638Abstract: 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: ApplicationFiled: April 7, 2009Publication date: August 13, 2009Applicant: VDF FUTURECEUTICALS, INC.Inventors: Dusan Miljkovic, Jovan Hranisavljevic, Zbigniew Pietrzkowski
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Patent number: 7572800Abstract: 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: GrantFiled: February 25, 2003Date of Patent: August 11, 2009Assignee: Gilead Sciences, Inc.Inventors: Phillip A. Furman, George R. Painter, III, David W. Barry, Franck Rousseau
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Publication number: 20090181988Abstract: 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: ApplicationFiled: August 19, 2008Publication date: July 16, 2009Applicant: The Regents of the University of CaliforniaInventors: Masahiro Tanaka, Chao Zhang, Kevan M. Shokat, Alma L. Burlingame, Kirk Hansen, Raynard L. Bateman, Stephen G. DiMagno
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Patent number: 7560483Abstract: 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: GrantFiled: June 21, 2005Date of Patent: July 14, 2009Assignee: XenoPort, Inc.Inventors: Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat, Cindy X. Zhou
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Publication number: 20090170879Abstract: 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: ApplicationFiled: December 28, 2007Publication date: July 2, 2009Inventors: Lucie Szucova, Marek Zatloukal, Lukas Spichal, Jiri Voller, Karel Dolezal, Miroslav Strnad, Frank J. Massino
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Publication number: 20090162319Abstract: 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: December 12, 2008Publication date: June 25, 2009Applicant: Ardea BiosciencesInventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
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Publication number: 20090156598Abstract: 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: ApplicationFiled: December 16, 2008Publication date: June 18, 2009Inventor: Alec D. Lebsack
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Publication number: 20090149479Abstract: 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: ApplicationFiled: September 12, 2008Publication date: June 11, 2009Applicant: Elan Pharma International LimitedInventors: Scott Jenkins, Gary Liversidge
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Publication number: 20090118309Abstract: 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: ApplicationFiled: July 16, 2007Publication date: May 7, 2009Inventors: Anthony Beauglehole, Jayson M. Rieger, Robert D. Thompson