Chalcogen Attached Indirectly To The 9- Position Of The Purine Ring System By Acyclic Nonionic Bonding Patents (Class 514/263.38)
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Publication number: 20100124543Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.Type: ApplicationFiled: July 16, 2009Publication date: May 20, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
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Publication number: 20100119580Abstract: A method and device for treating a mammalian organism to obtain a desired local or systemic physiological or pharmacological effect is provided. The method includes administering a sustained release drug delivery system to a mammalian organism in need of such treatment at an area wherein release of an effective agent is desired and allowing the effective agent to pass through the device in a controlled manner. The device includes an inner core or reservoir including the effective agent, an impermeable tube which encloses portions of the reservoir, and a permeable member at an end of the tube.Type: ApplicationFiled: January 19, 2010Publication date: May 13, 2010Applicant: pSivida Inc.Inventors: Hong Guo, Paul Ashton
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Publication number: 20100080830Abstract: The systems and methods disclosed herein provide sustained delivery of a therapeutic agent for treating a patient, e.g., human, to obtain a desired local or systemic physiological or pharmacological effect. Method includes positioning the sustained released drug delivery system at an area wherein release of the agent is desired and allowing the agent to pass through the device to the desired area of treatment. In some embodiments, the method is for treating or reducing the risk of retroviral or lentiviral infection. In certain embodiments, the method is for preventing or reducing the risk of mother-to-child transmission of HIV, wherein the therapeutic agent is an antiviral agent.Type: ApplicationFiled: December 3, 2009Publication date: April 1, 2010Applicant: pSivida Inc.Inventors: Paul Ashton, Jianbing Chen, Thomas J. Smith
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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: 20100069410Abstract: The present invention relates to acyclovir formulations having improved bioavailability resulting in better efficacy and/or requiring less frequent administration.Type: ApplicationFiled: November 30, 2007Publication date: March 18, 2010Applicant: Emisphere Technologies Inc.Inventors: Shingai Majuru, Moses Oyewumi
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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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Publication number: 20090324709Abstract: The invention relates to formulations of hydrophilic substances encapsulated in liposomes, to the method of encapsulation of the hydrophilic substances in the liposomes and the use of said formulations in the prevention and/or treatment of diseases and/or disorders in humans and animals.Type: ApplicationFiled: September 4, 2009Publication date: December 31, 2009Applicant: Italfarmaco, S.A.Inventors: Jaime Moscoso Del Prado, José Ramón Chantres Antoranz, María Ángeles Elorza Barroeta, Begoña Elorza Barroeta, Manuel Cordoba Diaz
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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: 20090270428Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, methods of using the same, processes for preparing the same, and intermediates thereof.Type: ApplicationFiled: May 4, 2006Publication date: October 29, 2009Inventors: David Michael Bender, James Ray McCarthy
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Publication number: 20090270429Abstract: A topical antiviral composition comprising acyclovir, penciclovir and/or omaciclovir in a glucocorticoid-free pharmaceutical carrier comprising 15 to 25 weight % propylene glycol and 10 to 25 weight % isopropyl C12-C22 alkanoic ester. The compositions have utility in the treatment or prophylaxis of herpesvirus infections. Clinical results demonstrate that treatment commencing at the prodromal stage can prevent the development of a classic cold sore lesion in a large proportion of patients.Type: ApplicationFiled: March 13, 2009Publication date: October 29, 2009Applicant: Medivir ABInventor: Torbjorn LARSON
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Publication number: 20090258843Abstract: The present invention is directed to compositions and methods for the treatment of various diseases, pathological disorders, and medical conditions such as viral infections and cancer. The compositions include (A) an antiviral compound or a pharmaceutically acceptable salt thereof; and (B) an agent selected from the group consisting of a substituted or unsubstituted imidazole or a pharmaceutically acceptable salt thereof; a non-steroidal anti-inflammatory agent or a pharmaceutically acceptable salt thereof; an amino acid or a pharmaceutically acceptable salt thereof; a carboxylic acid or a pharmaceutically acceptable salt thereof; a sulfonic acid or a pharmaceutically acceptable salt thereof; and a combination thereof.Type: ApplicationFiled: April 8, 2009Publication date: October 15, 2009Applicant: Mallinckrodt Inc.Inventors: Gary L. Cantrell, Robert E. Halvachs, Narayanasamy Gurusamy, Dawn M. Kyle, Frank W. Moser
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Patent number: 7569574Abstract: The invention relates to new purine derivatives of general formula wherein R1 to R4 are defined as in the claims, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV), the preparation thereof, the use thereof for the prevention or treatment of diseases or conditions associated with an increased DPP-IV activity or capable of being prevented or alleviated by reducing the DPP-IV activity, particularly type I or type II diabetes mellitus, the pharmaceutical compositions containing a compound of general formula (I) or a physiologically acceptable salt thereof as well as processes for the preparation thereof.Type: GrantFiled: August 4, 2003Date of Patent: August 4, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Roland Maier, Frank Himmelsbach, Matthias Eckhardt, Elke Langkopf, Michael Mark, Ralf R. H. Lotz
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Publication number: 20090180980Abstract: Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by hemorrhagic fever viruses, such as Arenaviruses.Type: ApplicationFiled: January 31, 2007Publication date: July 16, 2009Applicant: SIGA TECHNOLOGIES, INC.Inventors: Dennis E. Hruby, Tove C. Bolken, Dongcheng Dai
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Publication number: 20090175928Abstract: The invention relates to a self-adhesive lip plaster which comprises at least one single-layered matrix and which contains at least one antiviral active medical substance for using in the event of Herpes labialis. Said matrix is arranged on a flexible carrier film which is hydrophobic and also permeable to vapor.Type: ApplicationFiled: October 9, 2006Publication date: July 9, 2009Inventors: Stephan Maier, Ulrike Vollmer
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Publication number: 20090169511Abstract: A mucosal bioadhesive slow release carrier comprising an active principle and devoid of starch, lactose, which can release the active principal for a duration of longer than 20 hours. This bioadhesive carrier contains a diluent, an alkali metal alkylsulfate, a binding agent, at least one bioadhesive polymer and at least one sustained release polymer, as well as a method for its preparation.Type: ApplicationFiled: March 23, 2007Publication date: July 2, 2009Applicant: BIOALLIANCE PHARMAInventors: Dominique Costantini, Caroline Lemarchand
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Publication number: 20090130214Abstract: The invention concerns a 2?,2?-difluoro-2?-deoxycytidine derivative of general formula (I), wherein: R1, R2 and R3, identical or different, represent independently of one another, a hydrogen atom or an at least C18 hydrocarbon acyl radical and of such conformation that it is capable of providing the compound of general formula (I), a compacted form in a polar solvent medium, at least one of groups R1, R2 and R3 being other than a hydrogen atom.Type: ApplicationFiled: June 23, 2005Publication date: May 21, 2009Inventors: Patrick Couvreur, Barbara Stella, Luigi Cattel, Flavio Rocco, Jack-Michel Renoir, Veronique Rosilio
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Publication number: 20090124639Abstract: The present invention relates to valacyclovir formulations having improved bioavailability resulting in better efficacy and/or requiring less frequent administration.Type: ApplicationFiled: November 6, 2008Publication date: May 14, 2009Applicant: Emisphere Technologies Inc.Inventors: Moses Oyewumi, Shingai Majuru, Lewis Bender, Akm Nasir Uddin
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Publication number: 20090118168Abstract: The present invention provides a topical composition comprising (a) at least one delivery agent compound and (b) a acyclovir compound. Methods of treatment, and methods of preparing the topical composition are also provided.Type: ApplicationFiled: May 2, 2007Publication date: May 7, 2009Applicant: Emsiphere Technologies Inc.Inventors: Steven Dinh, Puchun Liu, Ihor Shevchuk
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Publication number: 20090099216Abstract: A novel adenine compound represented by the formula (1): wherein Z represents (un)substituted alkylene, a single bond, etc.; R1 represents an (un)substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heteroaryl group; R2 represents hydrogen or (un)substituted alkyl; R3, R4 and R5 each independently represents an (un)substituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl group, provided that R3 and R5 may be bonded to each other to form a 3- to 7-membered, saturated carbocycle or heterocycle in cooperation with the adjacent carbon atom; and X represents oxygen, sulfur, SO2, NR6 (R6 represents hydrogen or alkyl), or a single bond, or a pharmaceutically acceptable salt of the compound. The compound and salt are useful as a medicine.Type: ApplicationFiled: September 22, 2006Publication date: April 16, 2009Applicant: AstraZeneca Aktiebolag A corporation of SwedenInventors: Ian Millichip, Thomas McInally, Roger Bonnert
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Publication number: 20090099154Abstract: Pharmaceutical sustained release composition comprising at least one active agent(s), or its tautomeric forms, analogues, isomers, polymorphs, solvates, or salts thereof; preferably an antiviral active agent is provided. Also provided is a process of preparation of such composition and method of using them. The sustained release compositions of the present invention are able to deliver the active agent in a desired manner for an extended period of time.Type: ApplicationFiled: June 29, 2006Publication date: April 16, 2009Applicant: PANACEA BIOTEC LTD.Inventors: Rajesh Jain, Kour Chand Jindal, Sukhjeet Singh, Sanjay Boldhane
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Publication number: 20090099060Abstract: A reverse transcriptase encoded by L-1 (LINE-1) has been identified as a target molecule for treating or preventing cancers induced or mediated by this molecule. Method of treating or preventing such cancers in patients involves administration of a therapeutically effective amount of a composition having an inhibitor or antagonist of the reverse transcriptase in cells of the patients. The inhibitor or antagonist blocks lengthening of telomeres in telomerase negative cells. Methods and kits for detecting pathologically proliferating cells expressing L1RT are also disclosed.Type: ApplicationFiled: January 18, 2005Publication date: April 16, 2009Inventors: Igor E. Bondarev, John S. Bertram
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Publication number: 20090076040Abstract: The present application describes deuterium-enriched valganciclovir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 11, 2008Publication date: March 19, 2009Applicant: Protia, LLCInventor: Anthony W. Czarnik
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Publication number: 20090076041Abstract: Methods and novel intermediates for the preparation of and the treatment with acyclic nucleoside derivatives of the formula: where one of R1 and R2 is an amino acid acyl group and the other of R1 and R2 is a —C(O)C3-C21 saturated or monounsaturated, optionally substituted alkyl and R3 is OH or H.Type: ApplicationFiled: October 3, 2008Publication date: March 19, 2009Applicant: Medivir ABInventors: Per ENGELHARDT, Marita HOGBERG, Xiao-Xiong ZHOU, Nils-Gunnar JOHANSSON, Bjorn LINDBORG
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Publication number: 20090074707Abstract: Water-dispersible or water-soluble polymers, particularly those of the family of compounds comprising the poloxamers or the polyesters or amphiphilic agents (emulsifiers), and also lipophilic materials are dispersed by melting the components at suitable temperatures with admixture of pharmaceutically active substances by mechanical procedures, i.e. a lipophilic dispers phase is distributed in a hydrophilic continuous polymer phase to form a stable dispersion. By controlled cooling, curing, and storage followed by high-pressure molding at defined temperatures and operating pressures there are produced, in addition to other types of shaped bodies, dispersed polymeric fatty sticks distinguished by particularly good fracture strength, flexibility, and variable time-specific dimensional stability.Type: ApplicationFiled: November 17, 2008Publication date: March 19, 2009Inventors: Rainer Rogasch, Friedrich Fisseler, Marc Schmieding
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Publication number: 20090076039Abstract: The present application describes deuterium-enriched valacyclovir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 8, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090062315Abstract: A pharmaceutical acceptable composition is provided. The composition comprises an effective amount of a non-steroidal anti-inflammatory drug (NSAID), a local anesthetic, and an antiviral drug.Type: ApplicationFiled: August 28, 2008Publication date: March 5, 2009Applicant: Yung Shin Pharmaceutical Industrial Co., Ltd.Inventors: Fangchen Lee, Hui-Ling Shieh, Chiung-Ju Tsai, Shin-Hong Jang
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Publication number: 20080299220Abstract: A waterless composition suitable for delivery of an active agent to a body surface or cavity includes a vehicle having about 70% to about 99% by weight of a hydrophilic polar solvent, said hydrophilic solvent selected from the group consisting of (i) a mixture of two or more different polyethylene glycols (PEGs), wherein at least one PEG is a high molecular weight PEG having a melting point greater than 25° C.; and (ii) propylene glycol (PG); about 0% to about 10% of at least one surface active agent; about 0% to about 5% of a polymeric agent; about 0% to about 30% of a secondary hydrophilic solvent; and about 0% to about 5% of a silicone oil; and about 3% to about 25% hydrophobic propellant. The composition is otherwise substantially free of a hydrophobic solvent and includes at least one of a surface active agent and a polymeric agent. The vehicle and the propellant are sufficiently miscible that the components may be homogeneously distributed with mild shaking.Type: ApplicationFiled: January 14, 2008Publication date: December 4, 2008Inventors: Dov Tamarkin, Meir Eini, Doron Friedman, Alex Besonov, David Schuz, Tal Berman, Jorge Danziger, Rita Keynan, Ella Zlatkis
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Publication number: 20080274164Abstract: The invention relates to a plaster composition for administering active agents in and to bodily orifices, such as e.g. the buccal cavity, lips or genitalia.Type: ApplicationFiled: September 1, 2005Publication date: November 6, 2008Inventor: Ulrike Vollmer
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Publication number: 20080260844Abstract: The invention relates to the field of solid, oral, microparticulate dosage forms having a composition that prevents the misuse of the active pharmaceutical ingredient contained therein. The aim of the invention is to prevent the improper use of solid oral medicaments for any use other than the therapeutic use(s) officially approved by the appropriate public health authorities. More specifically, the invention relates to a solid, oral drug form which is characterised in that at least one part of the active pharmaceutical ingredient is contained in the microparticles thereof and in that the inventive form comprises anti-crushing means which are intended to impede or completely prevent the crushing of the microparticles of the active pharmaceutical ingredient, such as to preclude the misuse thereof.Type: ApplicationFiled: November 21, 2005Publication date: October 23, 2008Applicant: Flamel TechnologiesInventors: Gerard Soula, Florence Guimberteau
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Patent number: 7432274Abstract: Methods and novel intermediates for the preparation of and the treatment with acyclic nucleoside derivatives of the formula: where one of R1 and R2 is an amino acid acyl group and the other of R1 and R2 is a —C(O)C3-C21 saturated or monounsaturated, optionally substituted alkyl and R3 is OH or H.Type: GrantFiled: December 19, 2003Date of Patent: October 7, 2008Assignee: Medivir ABInventors: Per Engelhardt, Marita Hogberg, Nils-Gunnar Johansson, Xiao-Xiong Zhou, Bjorn Lindborg
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Publication number: 20080220079Abstract: Sustained release spherical or non-spherical pellets comprising (a) an active ingredient (b) a wax-like agent, and (c) a spheronizing agent are provided. Oral dosage forms comprising said pellets and methods for preparing and using such pellets and dosage forms are also provided.Type: ApplicationFiled: February 29, 2008Publication date: September 11, 2008Applicant: FARNAM COMPANIES, INC.Inventors: Andrew Xian Chen, Patricia D. Kigin
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Publication number: 20080213403Abstract: The present invention provides a method for treating a pulmonary disease state in mammals by protecting indigenous in vivo levels of nitric oxide in mammalian cells comprising contacting the mammalian cells with a therapeutically effective amount of a nitric oxide mediator, wherein the nitric oxide mediator is selected from the group consisting of ?-keto acids having four or more carbon atoms, precursors of ?-keto acids having four or more carbon atoms, and the salts thereof.Type: ApplicationFiled: January 22, 2008Publication date: September 4, 2008Inventor: Alain Martin
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Patent number: 7419967Abstract: 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: GrantFiled: August 25, 2005Date of Patent: September 2, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R Hale, Clarence W Andrews, III, Eric S Furfine, Ronald G Sherrill, Andrew Spaltenstein, Gregory T Lowen
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Publication number: 20080181944Abstract: A dosage form is disclosed comprising a semipermeable walled container that houses a capsule, which capsule comprises a drug formulation, a piston, and an osmotic composition. The dosage form delivers the drug formulation through a passageway at a controlled rate over a sustained-release period of time up to 24 hours.Type: ApplicationFiled: April 2, 2008Publication date: July 31, 2008Applicant: ALZA CORPORATIONInventors: Liang-Chang Dong, Patrick S.L. Wong, Vincent Joseph Ferrari, Steven Espinal
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Patent number: 7388002Abstract: Compounds represented by the formula: A is (CH2)nR2, —CH?CH2, CH2—CH?CH2, O(CH2)nR2, CH(OH)CH3, CH(OH)CH2OH, CH2—CH(OH)CH3, CH2CH(OH)CH2OH, or CH(OH)CH(OH)CH3, R,R1 individually is H, NH2OH, Cl, Br, I, aryl, substituted aryl, heterocycle, NR3R4, OR3 or SR3, R2 is H, OH, F, N3, NH2, CO2H, SH, alkyl, substituted alkyl, S-alkyl, O-acyl, CONH2, or CONH-alkyl, n is 1-3, y is O, S or NH, W is O or S, Z, Z? individually is OR3, OR4, O(CH2)m—O—(CH2)xCH3, NH—CH(alkyl)CO2R3, alkyl, substituted alkyl, OCH2CH2S—C(O)CH3, OCH2CH2S—C(O)CH(CH3)2, OCH2CH2S—C(O)C(CH3)3, OCH2CH2—SC(O)aryl, OCH2CH2—S—S—OCH2CH2OH, OCH2OC(O)C(CH3)3, OCH2—O—C(O)OCH(CH3)2, or OCH2—O—C(O)CH(CH3)2 R3, R4 individually is H, alkyl, substituted alkyl, aryl, or substituted aryl; Both R3 and R4 can form a monocyclic ring of 4-7 atoms with N or optionally a further heteroatom in the ring; m is 1-3, x is 0-19; and pharmaceutically acceptable salts thereof and prodrugs thereof are provided.Type: GrantFiled: November 9, 2005Date of Patent: June 17, 2008Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, Yahya El-Kattan, Minwan Wu
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Publication number: 20080132527Abstract: The present invention relates to an acyclovir formulation having improved bioavailability resulting in better efficacy and/or requiring less frequent administration.Type: ApplicationFiled: May 19, 2005Publication date: June 5, 2008Applicant: Emisphere Technologies, Inc.Inventors: Amy C. Adams, Brahma N. Singh, Nikhil Dhoot, Shingai Majuru
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Publication number: 20080063673Abstract: 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: September 13, 2006Publication date: March 13, 2008Inventor: Robert E. Akridge
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Patent number: 7273864Abstract: The present invention provides compositions and methods for differentiating and transdifferentiating mammalian cells into cells of an osteoblast lineage, using compounds of the following formula: wherein R4 is a functional group including, for example, C1-4alkyl, C3-8cycloalkyl, hydroxyl-C1-4alkyl, aryl-C0-3alkyl, substituted with 0-2 R4a groups, and heterocyclo-C0-2alkyl, optionally substituted with C1-4alkyl; R5 is hydrogen and R6 is a functional group including, for example, halogen, C1-4alkyl, —C(O)—C1-4alkyl, —SO2—N(R2b R2b), halo—C1-4alkyl, —O-aryl and —N(R7 R8), or when R5 and R6 are on adjacent ring atoms they are optionally taken together to form —O—(CH2)1-2—O—; and all pharmaceutically acceptable salts and hydrates thereof.Type: GrantFiled: October 15, 2003Date of Patent: September 25, 2007Assignee: The Scripps Research InstituteInventors: Xu Wu, Sheng Ding, Nathanael S. Gray
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Patent number: 7256196Abstract: The present invention relates to 2,8,9-substituted purines which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions comprising said 2,8,9-substituted purines and methods for preventing, abating, or otherwise controlling enzymes which are understood to be the active components responsible for the herein described disease states.Type: GrantFiled: December 7, 2004Date of Patent: August 14, 2007Assignee: The Procter & Gamble CompanyInventors: Mark Sabat, Michael Philip Clark, Todd Andrew Brugel, Adam Golebiowski, John Charles Van Rens, Biswanath De
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Patent number: 7238700Abstract: Disclosed are novel A2B adenosine receptor antagonists of Formula I: A compound of the formula: wherein: R1 is optionally substituted alkyl or a group —Y-Z, in which Y is a covalent bond or optionally substituted alkylene, and Z is optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted alkenyl or optionally substituted alkynyl, with the proviso that when Y is a covalent bond Z cannot be alkenyl or alkynyl; and X is oxygen, sulfur, or NH—, or a pharmaceutically acceptable salt, ester, or prodrug thereof. The compounds are particularly useful for treating asthma and diabetic retinopathy.Type: GrantFiled: April 30, 2004Date of Patent: July 3, 2007Assignee: CV Therapeutics, Inc.Inventors: Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki, Dengming Xiao
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Patent number: 7229961Abstract: This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including into and across ocular tissues and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length (SEQ ID NO:86).Type: GrantFiled: February 25, 2002Date of Patent: June 12, 2007Assignee: Cellgate, Inc.Inventors: Jonathan B. Rothbard, Paul A. Wender, P. Leo McGrane, Lalitha V. S. Sista, Thorsten A. Kirschberg
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Patent number: 7196093Abstract: 1. The present invention provides compositions and methods for reversibly inhibiting S-adenosyl-L-homocysteine (SAH) hydrolase. The compounds of the present invention can be used as an anti-hemorrhagic viral infection agent, an immunosuppressant, a homocysteine lowering agent, or an anti-neoplasm agent. The compositions and methods of the present invention can be used for the prevention and treatment of hemorrhagic virus infection, autoimmune diseases, autograft rejection, neoplasm, hyperhomocysteineuria, cardiovascular disease, stroke, Alzheimer's disease, multiple sclerosis or diabetes.Type: GrantFiled: April 9, 2003Date of Patent: March 27, 2007Assignee: General AtomicsInventor: Chong-Sheng Yuan
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Patent number: 7189730Abstract: Disclosed are novel A2A adenosine receptor antagonists of the formula: wherein: R1 is optionally substituted aryl or optionally substituted heteroaryl; R2 is optionally substituted lower alkyl or optionally substituted cycloalkyl; R3 is hydrogen, halogen, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocyclyl; X is —O—, —S—, or —NH—; and Y is optionally substituted alkylene; and the pharmaceutically acceptable salts thereof; which are useful for treating various disease states, for example cardiovascular disorders, including tissue damage due to ischemia, CNS diseases, including Parkinson's disease, depression, and the like.Type: GrantFiled: December 18, 2002Date of Patent: March 13, 2007Assignee: CV Therapeutics, Inc.Inventor: Gloria Cristalli
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Patent number: 7045525Abstract: A method of treatment of: i) HIV-1 infections in mammals, including humans; or ii) HBV infections in mammals, including humans; which method comprises the administration to the human in need of such treatment, an effective amount of the (R)-enantiomer of the triphosphate of a compound of formula (A) or a pharmaceutically acceptable salt thereof; and compounds for use in the method.Type: GrantFiled: April 23, 1996Date of Patent: May 16, 2006Assignee: Novartis AGInventors: Richard Anthony Vere Hodge, Raymond F Schinazi
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Patent number: 6958344Abstract: The invention provides certain heterocyclic compounds, processes, and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy; in formula (I), A is a group of formula (a) or (b).Type: GrantFiled: February 7, 2001Date of Patent: October 25, 2005Assignee: AstraZeneca ABInventors: Roger Bonnert, Peter Cage, Fraser Hunt, Iain Walters, Paul Willis
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Patent number: 6855736Abstract: The present invention relates to the fields of biology, genetics and medicine. In particular it concerns new methods for the detection, characterization and/or treatment (or management) of neuro degenerative diseases, particularly amyotrophic lateral sclerosis.Type: GrantFiled: October 25, 2001Date of Patent: February 15, 2005Assignee: Exonhit Therapeutics SAInventors: Ali Ait Ikhlef, Annelies Resink, Fabien Schweighoffer
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Publication number: 20040248910Abstract: Methods and novel intermediates for the preparation of acyclic nucleoside derivatives of the formula: 1Type: ApplicationFiled: June 17, 2004Publication date: December 9, 2004Applicant: Medivir ABInventors: M. Robert Leanna, Steven M. Hannick, Michael Rasmussen, Jien-Heh J. Tien, Lakshmi Bhagavatula, Pulla Reddy Singam, Bradley D. Gates, Lawrence Kolaczkowski, Ramesh R. Patel, Greg Wayne, Greg Lannoye, Weijiang Zhang, Zhenping Tian, Kirill A. Lukin, Bikshandarkoil A. Narayanan, David A. Riley, Howard Morton, Sou-Jen Chang, Cynthia B. Curty, Daniel Plata, John Bellettini, Bhadra Shelat, Tiffany Spitz, Cheng-Xi Yang
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Publication number: 20040242457Abstract: The invention provides a method for treating visual field defects associated with the use of GABAergic drugs in a mammal in need thereof. The method comprises administering an effective amount of a drug that improves retinal perfusion. Novel compositions containing a GABAergic drug and a drug that improves retinal perfusion are also provided.Type: ApplicationFiled: May 27, 2003Publication date: December 2, 2004Inventor: Charles R. Ashby
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Publication number: 20040235869Abstract: Compounds of formula (XXIII), or pharmaceutically acceptable salts or esters thereof, are inhibitors of reverse transcriptase: 1Type: ApplicationFiled: May 19, 2004Publication date: November 25, 2004Inventors: Raven H. Huang, Xianjun Liu
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Publication number: 20040209900Abstract: A pharmaceutical composition for treating lipodystrophy and a method of treating lipodystrophy with the pharmaceutical composition. The composition comprising a therapeutically effective amount, e.g., 400 mg. three times per day, of pentoxifylline and a pharmaceutically acceptable carrier.Type: ApplicationFiled: April 6, 2004Publication date: October 21, 2004Inventor: Stephen P. Hauptman