The Additional Hetero Ring Consists Of Carbon And Chalcogen As The Only Ring Members Patents (Class 514/263.23)
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Publication number: 20120165288Abstract: This invention relates to novel compounds that are azapeptides, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel azapeptide compounds that are derivatives of the HIV protease inhibitor atazanavir sulfate. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering HIV protease inhibitors. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving atazanavir.Type: ApplicationFiled: March 2, 2012Publication date: June 28, 2012Inventors: Scott L. Harbeson, Roger D. Tung
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Publication number: 20120165350Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.Type: ApplicationFiled: December 21, 2011Publication date: June 28, 2012Inventors: Jeff Zablocki, Elfatih Elzein
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Publication number: 20120141491Abstract: The subject application provides small compounds that are able to increase/enhance autophagy in various cells. These compounds are useful in augmenting existing treatments of various cancers, microbial/viral infections, and neurodegenerative diseases. Thus, the subject application also provides methods of treating various types of cancers, microbial/viral infections, and neurodegenerative diseases.Type: ApplicationFiled: August 9, 2010Publication date: June 7, 2012Applicant: University of Florida Research Foundation Inc.Inventors: William A. Dunn, Debra Everton Akin, Brian Keith Law
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Publication number: 20120129807Abstract: 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 scleroderma, keloids, UV injury, or sunburn, and methods for improving or preventing scar formation.Type: ApplicationFiled: October 20, 2011Publication date: May 24, 2012Inventors: Brydon L. Bennett, Brian Edwin Cathers, Kristen Lee Jensen-Pergakes, Heather Raymon, Weilin Xie, Jaman May Maroni
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Publication number: 20120115890Abstract: Solid forms comprising 4-[9-(tetrahydro-furan-3-yl)-8-(2,4,6-trifluoro-phenylamino)-9H-purin-2-ylamino]-cyclohexan-1-ol, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders are disclosed.Type: ApplicationFiled: January 12, 2012Publication date: May 10, 2012Inventors: Marie G. Beauchamps, Louise Michelle Cameron, Robert Hilgraf, Mohit Atul Kothare, Manohar T. Saindane, Jean Xu
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Patent number: 8173618Abstract: Nutriceutical and pharmaceutical formulations for treating neurodegenerative disorders such as Alzheimer's disease are provided. Nutriceutical formulations include two or more of folate, vitamin E, and acetyl-L-carnitine (ALCAR). Pharmaceutical formulations include two or more of 3-deaza-adenosine (DZA), N-acetyl-L-cysteine (NAC), and S-adenosylmethionine (SAM).Type: GrantFiled: July 23, 2004Date of Patent: May 8, 2012Assignee: University of MassachusettsInventors: Thomas B. Shea, Robert J. Nicolosi, Eugene Rogers
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Publication number: 20120108614Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: ApplicationFiled: May 14, 2009Publication date: May 3, 2012Inventor: Jayhong A. Chong
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Publication number: 20120100213Abstract: Provided herein are pharmaceutical formulations, comprising 4-((9-((3S)-tetrahydro-3-furanyl)-8-((2,4,6-trifluorophenyl)amino)-9H-purin-2-yl)amino)-trans-cyclohexanol, including pharmaceutically acceptable salts, solvates, isomers, isotopologues, tautomers and racemic mixtures thereof, and a pharmaceutically acceptable excipient; and their use for treating or preventing disease.Type: ApplicationFiled: October 20, 2011Publication date: April 26, 2012Inventors: Sreenivas S. Bhat, Xiaozhong Liang, Anthony Tutino, Anthony Joseph Frank
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Patent number: 8163754Abstract: Compounds of formula I in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: GrantFiled: October 21, 2005Date of Patent: April 24, 2012Assignee: Novartis AGInventors: Robin Alec Fairhurst, Roger John Taylor, Harinder Pal Singh
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Patent number: 8158635Abstract: Solid forms comprising 4-[9-(tetrahydro-furan-3-yl)-8-(2,4,6-trifluoro-phenylamino)-9H-purin-2-ylamino]-cyclohexan-1-ol, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders are disclosed.Type: GrantFiled: August 28, 2008Date of Patent: April 17, 2012Assignee: Signal Pharmaceuticals, LLCInventors: Marie G. Beauchamps, Louise Michelle Cameron, Robert Hilgraf, Mohit Atul Kothare, Manohar T. Saindane, Jean Xu
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Patent number: 8138172Abstract: The present invention provides 8-oxoadenine derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The 8-oxoadenine derivatives act as modulators of Toll-like Receptor (TLR) 7 and thus may be used in the treatment of asthma, hepatitis, allergic diseases, viral and bacterial infection as well as cancer.Type: GrantFiled: July 3, 2007Date of Patent: March 20, 2012Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co Ltd.Inventors: Anthony Cook, Tom McInally, Stephen Thom, Hiroki Wada
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Patent number: 8084458Abstract: Methods are described for the synthesis of Locked Nucleic Acid (LNA) derivatives using certain nitrogen-containing nucleophiles.Type: GrantFiled: August 3, 2009Date of Patent: December 27, 2011Assignee: Santaris Pharma A/SInventors: Mads Detlef Sørensen, Jesper Wengel, Troels Koch, Signe M. Christensen, Christoph Rosenbohm, Daniel Sejer Pedersen
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Publication number: 20110288053Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, 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: ApplicationFiled: July 20, 2011Publication date: November 24, 2011Applicant: Gilead Sciences, Inc.Inventors: Constantine G. Boojamra, Carina Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Heolun Jin, Ralph F. Hirschmann, Alan X. Huang, Choung U. Kim, Thorsten Kirschberg, Christopher P. Lee, William A. Lee, Richard L. Mackman, David Y. Markevitch, David A. Oare, Vidya K. Prasad, Hyung-Jung Pyun, Adrian S. Ray, Rosemarie Sherlock, Sundaramoothi Swaninathan, William J. Watkins, Jenneifer Zhang
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Publication number: 20110269781Abstract: 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: June 7, 2011Publication date: November 3, 2011Applicant: GLAXOSMITHKLINE LLCInventors: Linos Lazarides, Stephen Allan Smith, Richard Stocker, Colin Jack Theobald
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Publication number: 20110269675Abstract: A method for the treatment and/or prophylaxis of an osteonecrotic bone disease in a mammal in need thereof, such as, e.g., idiopathic or secondary osteonecrosis, avascular bone necrosis, glucocorticoid induced bone ischemia/osteonecrosis, Legg-Calve-Perthes disease and femoral head necrosis, the method comprising administering an effective dose of a strontium-containing compound (a) to the mammal. A method for the treatment and/or prophylaxis of an osteonecrotic bone disease, such as, e.g., idiopathic or secondary osteonecrosis, avascular hone necrosis, glucocorticoid induced bone ischemia/osteonecrosis and femoral head necrosis, in a mammal who is to be or is treated with a therapeutic agent (b) known to or suspected of inducing apoptosis and/or necrosis of bone cells, the method comprising administering a strontium-containing compound (a) in combination with (b).Type: ApplicationFiled: July 14, 2011Publication date: November 3, 2011Inventors: Christian HANSEN, Henrik NILSSON, Stephan CHRISTGAU, Henry G. BONE, III
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Patent number: 8044061Abstract: Disclosed are novel compounds of the general formula (Ia), and pharmaceutically acceptable salts, isomers, diastereomers or enantiomers thereof and their use as medicines, for example in the treatment of dopamine-related movement disorders.Type: GrantFiled: December 21, 2007Date of Patent: October 25, 2011Assignee: UCB Pharma GmbHInventors: Christa E. Müller, Jörg Hockemeyer, Nikolay T. Tzvetkov, Joachim C. Burbiel
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Publication number: 20110257167Abstract: Provided herein are methods for treating and/or preventing a cancer or a tumor syndrome in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having cancer or a tumor syndrome, characterized by a LKB1 and/or AMPK gene or protein loss or mutation.Type: ApplicationFiled: February 3, 2011Publication date: October 20, 2011Inventors: Rajesh Chopra, Yuhong Ning, Sabita Sankar, Shuichan Xu, Weiming Xu
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Publication number: 20110257206Abstract: The invention relates to a combination comprising a microtubule active agent; and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; methods of treatment comprising said combination; processes for making said combination; and a commercial package comprising said combination.Type: ApplicationFiled: April 26, 2011Publication date: October 20, 2011Inventors: Gregory Burke, Ronald Richard Linnartz, Paul M.J. McSheehy, Richard William Versace, Markus Wartmann
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Publication number: 20110251172Abstract: The invention encompasses purine derivatives as gamma secretase modulators, useful for treating diseases associated with the deposition of beta-amyloid peptide in the brain, such as Alzheimer's disease, or of preventing or delaying the onset of dementia associated with such diseases. Pharmaceutical compositions and methods of use are included.Type: ApplicationFiled: July 31, 2009Publication date: October 13, 2011Inventors: Alexey A. Rivkin, Sean P. Ahearn, Stephanie M. Chichetti, Christohpher L. Hamblett, Yudith Garcia, Michelle Martinez, Benito Munoz
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Publication number: 20110236348Abstract: The present invention includes therapeutic methods that include the administration of a compound of Formula I or II: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, to a subject in need of such, and therapeutic methods that include the administration of such compounds with at least one additional active agent.Type: ApplicationFiled: June 3, 2011Publication date: September 29, 2011Applicant: Gilead Sciences, Inc.Inventors: Michael Graupe, Randall L. Halcomb
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Publication number: 20110230503Abstract: 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: May 26, 2011Publication date: September 22, 2011Inventors: Lucie Szucova, Marek Zatloukal, Lukas Spichal, Jiri Voller, Karel Dolezal, Miroslav Strnad, Frank J. Massino
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Publication number: 20110224217Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1, R3, R4, L, X, Y, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.Type: ApplicationFiled: May 23, 2011Publication date: September 15, 2011Inventors: Deborah Sue Mortensen, Maria Mercedes Delgado Mederos, John Joseph Sapienza, Ronald J. Albers, Steven Spencer Clareen, Kimberly Lyn Schwarz, Jason Simon Parnes, Jennifer R. Riggs, Patrick William Papa, Sayee Gajanan Hegde, Jeffrey Mark McKenna
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Publication number: 20110224238Abstract: The present invention provides methods and compositions for countering the adverse effects of aging on mammalian cells in vitro and in vivo, especially human skin cells and human skin, and treatment of hyperproliferative and related skin diseases in mammals by administering compositions containing 6,9-disubstituted purine derivatives.Type: ApplicationFiled: May 26, 2011Publication date: September 15, 2011Inventors: Lucie Szucova, Marek Zatloukal, Lukas Spichal, Ludek Frolich, Karel Dolezal, Miroslav Strnad, Frank J. Massino
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Publication number: 20110195066Abstract: The present invention relates to new quinoline inhibitors of tyrosine kinases, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: February 3, 2011Publication date: August 11, 2011Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Chengzhi Zhang
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Patent number: 7989459Abstract: A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKC?. inhibitors, and their methods of use are disclosed. The genus is represented by the formula I: wherein R1 is chosen from nitrogen-attached heterocyclyl, nitrogen-attached substituted heterocyclyl wherein the point of attachment is a nitrogen heteroatom, and R2 is chosen from aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, hetroarylalkyl, and substituted heteroarylalkyl.Type: GrantFiled: February 2, 2007Date of Patent: August 2, 2011Assignee: Pharmacopeia, LLCInventors: Andrew Roughton, Yajing Rong, Koc Kan Ho, Michael Ohlmeyer, David Diller
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Publication number: 20110182973Abstract: The invention relates to polymerase inhibitors, particularly polymerase alpha inhibitors, and the use thereof in the treatment of cell growth disorders, particularly tumor disorders, preferably actinic keratoses, basal cell carcinomas, and/or spinocellular carcinomas.Type: ApplicationFiled: May 13, 2008Publication date: July 28, 2011Applicants: FREIE UNIVERSITAET BERLIN, HEINRICH-HEINE-UNIVERSITAET DUESSELDORFInventors: Monika Schaefer-Korting, Hans-Dieter Hoeltje
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Patent number: 7977345Abstract: A compound for modulating kinase activity according to Formula I, or a pharmaceutically acceptable salt thereof, Wherein J1, J2, J3, R2, J4, Z, Ar and R3 are as defined in the specification, compositions thereof, and methods of use thereof.Type: GrantFiled: July 1, 2005Date of Patent: July 12, 2011Assignee: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Lisa Esther Dalrymple, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrisson B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Yong Wang, Wie Xu
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Patent number: 7977344Abstract: 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: GrantFiled: February 15, 2008Date of Patent: July 12, 2011Assignee: GlaxoSmithKline LLCInventors: Linos Lazarides, Stephen Allan Smith, Richard Stocker, Colin Jack Theobald
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Patent number: 7968556Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1, R3, R4, L, X, Y, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.Type: GrantFiled: October 18, 2007Date of Patent: June 28, 2011Assignee: Signal Pharmaceuticals, LLCInventors: Deborah Sue Mortensen, Maria Mercedes Delgado Mederos, John Joseph Sapienza, Ronald J. Albers, Steven Spencer Clareen, Kimberly Lyn Schwarz, Jason Simon Parnes, Jennifer R. Riggs, Patrick William Papa, Sayee Gajanan Hegde, Jeffrey Mark McKenna
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Publication number: 20110151018Abstract: The present invention is directed towards methods of inhibiting thermo- and chemo-sensing in insects and pests by inhibiting TRPA1 ion gated channel or family members. The present invention is also directed towards methods of insect control by modulating the TRPA1 ion gated channel or family members. The methods are applicable to a wide variety of insects and pests including agricultural and horticultural pests.Type: ApplicationFiled: December 10, 2010Publication date: June 23, 2011Applicant: BRANDEIS UNIVERSITYInventors: Paul Garrity, KyeongJin Kang
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Patent number: 7960397Abstract: Certain 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts of the following general formula are provided wherein R6 and R9 are as defined in the specification. These 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts are useful in compositions for application to mammalian cells, and especially human skin cells, in order to improve the cosmetic appearance of the mammalian cells, especially human skin.Type: GrantFiled: December 28, 2007Date of Patent: June 14, 2011Assignee: Institute of Experimental Botany, Academy of Sciences of the Czech RepublicInventors: Lucie Szucova, Marek Zatloukal, Lukas Spichal, Jiri Voller, Karel Dolezal, Miroslav Strnad, Frank J. Massino
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Publication number: 20110135670Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, or C1-6alkoxy; m is an integer having a value of 3, 4, or 5; n is an integer having a value of 0 to 3; p is an integer having a value of 1 or 2 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: ApplicationFiled: August 7, 2009Publication date: June 9, 2011Applicant: GLAXOSMITHKLINE LLCInventors: Sebastien Andre Campos, Diane Mary Coe, Naimisha Trivedi
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Publication number: 20110130397Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.Type: ApplicationFiled: September 21, 2007Publication date: June 2, 2011Inventors: Soongyu Choi, Arthur Branstrom, Scott A. Gothe, Richard Lipman, Tamil Arasu, Richard G. Wilde
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Publication number: 20110130381Abstract: Inhibitors of dihydroorotate dehydrogenase (DHODH) for the Plasmodium enzyme have been identified and characterized. The inhibitors have high specificity, submicromolar efficacy against cultured parasite strains, exhibit drug-like properties, and are not overtly cytotoxic.Type: ApplicationFiled: May 7, 2009Publication date: June 2, 2011Inventors: Cecilia Bastos, Michael L. Booker, Cassandra A. Celatka, Jon C. Clardy, Joseph Cortese, Vishal P. Patel, Renato Skerlj, Roger C. Wiegand, Dyann F. Wirth
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Patent number: 7951803Abstract: Compounds of the formula wherein R1 represents optionally substituted C1-C10 alkyl, aryl or heteroaryl, and R3 represents alkoxy-substituted aryl or optionally substituted heteroaryl, are disclosed as Mnk2 inhibitors which are useful for the treatment and prevention of metabolic disorders such as obesity and diabetes.Type: GrantFiled: March 9, 2007Date of Patent: May 31, 2011Assignee: Pharmacopeia, LLCInventors: Andrew G. Cole, Marc-Raleigh Brescia, Joan J. Zhang, Zahid Hussain, David J. Diller, Axel Metzger, Gulzar Ahmed, Ian Henderson
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Publication number: 20110091418Abstract: Methods for treating viral infections using polyamine analogs, including mitoguazone (MGBG), are provided. In these methods, polyamine analogs destroy macrophages that act as viral reservoirs, facilitating the destruction of the viruses that dwell within the macrophages. Examples of viral infections that may be treated with the present methods include, but are not limited to, infections from human immunodeficiency viruses. These methods differ from previous methods of treatment using polyamine analogs, wherein the polyamine analogs were administered only as anti-tumor agents.Type: ApplicationFiled: December 21, 2010Publication date: April 21, 2011Applicant: Pathlogica, LLCInventors: Michael S. McGrath, Kenneth G. Hadlock
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Patent number: 7915268Abstract: The present invention provides novel purines useful for the prevention and treatment of autoimmune diseases, inflammatory diseases, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 4, 2007Date of Patent: March 29, 2011Assignee: Wyeth LLCInventors: Yingchun Lu, Celia Kingsbury, Adolph Bohnstedt, Michael Ohlmeyer, Vidyadhar Paradkar
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Publication number: 20110065721Abstract: Disclosed herein are methods of using metaxalone. In one embodiment, the method comprises determining that a patient in need metaxalone therapy is taking a substance that is a n inhibitor or an inducer of a cytochrome p450 isozyme, wherein the cytochrome P450 is CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4, and adjusting administration to the patient of metaxalone or the substance to avoid an adverse event associated with metaxalone. In another embodiment, the method comprises informing a user that metaxalone is metabolized by a cytochrome p450 isozyme, wherein the cytochrome P450 is CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4. Also included are articles of manufacture comprising a container containing a dosage form of metaxalone, wherein the container is associated with published material informing that metaxalone affects activity of a cytochrome p450 isozyme. Also disclosed are a method of treatment and a method of manufacturing a metaxalone product.Type: ApplicationFiled: May 21, 2010Publication date: March 17, 2011Applicant: MUTUAL PHARMACEUTICAL COMPANY, INC.Inventors: Richard H. ROBERTS, Jie DU, Matthew W. DAVIS
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Publication number: 20110003819Abstract: Methods and compounds for treating neurodegenerative and other disorders. Included is the administering to a subject in need thereof an effective amount of a compound having binding specificity for a p75NTR receptor molecule. Enhanced survival of neural and other cells has been observed.Type: ApplicationFiled: April 19, 2010Publication date: January 6, 2011Inventors: Frank M. Longo, Stephen M. Massa
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Publication number: 20110003806Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: January 28, 2010Publication date: January 6, 2011Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company LimitedInventors: Masaaki Hirose, Steven P. Langston, Hirotake Mizutani, Stepan Vyskocil
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Patent number: 7838508Abstract: Compounds represented by the formula 1: A is selected from the group consisting of wherein each R individually is H or acyl, Y is X, N3, NH2, monoalkylamino, or dialkylamino; Z is O or S; and X is selected from the group consisting of hydrogen, halo, hydroxy, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, thioaryl, thioalkyl, allylamino, cyano and nitro; tautomers thereof; and pharmaceutically acceptable salts thereof are provided along with methods for their fabrication. Various of these compounds can be used as anticancer agents, or antiviral agents or to inhibit DNA replication.Type: GrantFiled: November 7, 2006Date of Patent: November 23, 2010Assignee: Southern Research InstituteInventors: John A. Secrist, III, Kamal N. Tiwari, John A. Montgomery, William L. Hinds, Jr., legal representative
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Patent number: 7825126Abstract: Disclosed are (N)-methanocarba adenine nucleosides of the formula: as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias. The invention also provides compounds that are agonists of both A1 and A3 adenosine receptors for use in cardioprotection.Type: GrantFiled: September 2, 2005Date of Patent: November 2, 2010Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Bhalchandra V. Joshi, Susanna Tchilibon
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Publication number: 20100256082Abstract: The present invention is directed to methods for screening for metallohydrolase inhibitors using metal binding moieties in combination with targeting moieties.Type: ApplicationFiled: June 12, 2007Publication date: October 7, 2010Applicant: Viamet Pharmaceuticals, Inc.Inventor: Robert J. Schotzinger
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Publication number: 20100254965Abstract: We disclose a method of treating priapism in a mammal by administering to the mammal a composition containing an effective amount of an inhibitor of adenosine signaling and a pharmaceutically-acceptable carrier, wherein the inhibitor of adenosine signaling has at least one activity selected from the group consisting of decreasing adenosine levels in the mammal, inhibiting adenosine receptor activity in the mammal, and inhibiting signaling pathways downstream of an adenosine receptor in the mammal.Type: ApplicationFiled: October 24, 2007Publication date: October 7, 2010Inventors: Yang Xia, Rodney E. Kellems, Michael Blackburn, Janci Chunn Lindsay
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Patent number: 7807685Abstract: Compounds of formula (I) below are disclosed. Their use as medicaments is described, in particular for the treatment of pain or inflammation: wherein: when X=Y=Z=OH, R1 is OCH2CF2CF3, phenoxy (substituted with 3-(4-trifluoromethylphenyl), 3,4-dichloro, (3-trifluoromethyl,4-fluoro), (3-trifluoromethyl,4-chloro), (3-chloro, 4-cyano), or 3,5-bis(trifluoromethyl)), 1-piperazinyl(4-(3,4-dichlorophenyl)), phenyl (substituted with 3,4-dichloro, 3,5-difluoro, 3,5-bis(trifluoromethyl) or 3,4,5-trifluoro) or 2-benzofuranyl; or when X=Y=OH and Z=OMe, R1 is OCH3, OCH2CHF2, OCH2cyclopentyl, O-(2,5-difluorophenyl) or (S)-sec-butylamino; or when X=H and Y=Z=OH, R1 is n-hexylamino or cyclopentylamino; or when (IV) X=Z=OH and Y=H, R1 is cyclopentylamino; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 26, 2007Date of Patent: October 5, 2010Assignee: CBT Development LimitedInventors: Michael Higginbottom, Edward D. Savory, Giles A. Brown, Viet-Anh A. Horgan, Emma J. Chapman
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Publication number: 20100249122Abstract: The present invention provides compositions and methods of use thereof to prevent and/or treat pathogenic infection. In particular, the present invention provides the use of kinase inhibitors to inhibit kinases that involve in pathogen-host cell interactions that are associated with or cause pathogenic infections, therefore, to effectively prevent and/or treat pathogenic infections with far less likely to engender resistance as compared to conventional antibiotics and anti-viral drugs. The present invention further provides the use of kinase inhibitors for the treatment of acute pathogenic infections for a short period of time to avoid toxicities that may caused by long term use of these kinase inhibitors.Type: ApplicationFiled: September 5, 2007Publication date: September 30, 2010Applicant: Emory UniversityInventor: Daniel Kalman
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Publication number: 20100249066Abstract: 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: May 13, 2010Publication date: September 30, 2010Inventors: Brydon L. Bennett, Kate Blease, Brian Edwin Cathers
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Publication number: 20100249068Abstract: Disclosed herein are nucleotide analogs with protected phosphates, methods of synthesizing nucleotide analogs with protected phosphates and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the nucleotide analogs with protected phosphates.Type: ApplicationFiled: March 19, 2010Publication date: September 30, 2010Applicant: Alios BioPharma, Inc.Inventors: Leonid Beigelman, Lawrence Blatt, Guangyi Wang
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Publication number: 20100240680Abstract: Compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein W, R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: ApplicationFiled: July 11, 2007Publication date: September 23, 2010Inventors: Robin Alec Fairhurst, Roger John Taylor
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Publication number: 20100234401Abstract: The present invention provides methods and compositions for countering the adverse effects of aging on mammalian cells in vitro and in vivo, especially human skin cells and human skin, and treatment of hyperproliferative and related skin diseases in mammals by administering compositions containing 6,9-disubstituted purine derivatives.Type: ApplicationFiled: May 24, 2010Publication date: September 16, 2010Inventors: Lucie Szucova, Marek Zatloukal, Lukas Spichal, Ludek Frohlich, Karel Dolezal, Miroslav Strnad, Frank J. Massino