Nitrogen Attached Indirectly To The Purine Ring System By Acyclic Nonionic Bonding Patents (Class 514/263.35)
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Patent number: 7589075Abstract: The present invention concerns the use of an active ingredient selected from the group consisting of agonists of the adenosine receptor system, for inhibiting viral replication in cells. In particular, the invention provides a composition and method for inhibiting viral replication in cells, the method comprising presenting to the cells an effective amount of the active ingredient. According to one embodiment, the adenosine agonist is an A3 receptor agonist (A3RAg). The invention is particularly useful, for although not limited to, inhibiting the replication of HIV virus in human cells.Type: GrantFiled: January 13, 2002Date of Patent: September 15, 2009Assignee: Can-Fite Biopharma Ltd.Inventors: Pnina Fishman, Kamel Khalili
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Patent number: 7579354Abstract: The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be useful in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable.Type: GrantFiled: July 10, 2006Date of Patent: August 25, 2009Inventors: William F. Kiesman, Carol L. Ensinger, Russell C. Petter, James E. Dowling, Gnanasambandam Kumaravel, He Xi Chang, Ko Chung Lin
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Patent number: 7560450Abstract: The present invention relates to substituted xanthines of general formula the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: November 18, 2003Date of Patent: July 14, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Roland Maier, Michael Mark, Mohammad Tadayyon
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Publication number: 20090143377Abstract: Compounds and compositions for treating disorders related to TRPA1 are described herein.Type: ApplicationFiled: June 23, 2008Publication date: June 4, 2009Inventors: Howard Ng, Manfred Weigele, Magdalene Moran, Jayhong Chong, Christopher Fanger, Glenn R. Larsen, Donato Del Camino, Neil Hayward, Steven P. Adams, Amy Ripka
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Publication number: 20090137613Abstract: The present invention is concerned with new pharmaceutically acceptable salts of valacyclovir, polymorphic forms, processes for preparing the new pharmaceutically acceptable salts and new polymorphic forms, pharmaceutical compositions containing the same, therapeutic uses thereof and methods of treatment employing the same.Type: ApplicationFiled: March 6, 2007Publication date: May 28, 2009Inventors: Helena Ceric, Zvonimir Siljkovic, Iva Tunjic, Aleksandar Danilovski, Ernest Mestrovic
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Patent number: 7495004Abstract: The invention relates to methods for the treatment or prevention of an LXR mediated disease or condition, including cardiovascular disease and atherosclerosis, novel compounds of formula (I) for use in such methods and pharmaceutical compositions comprising compounds for use in such methods.Type: GrantFiled: May 20, 2003Date of Patent: February 24, 2009Assignee: Glaxo Group LimitedInventors: Sharon Davis Boggs, Jon Loren Collins, Adam Fivush, Eugene Lee Stewart, Timothy Mark Willson
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Patent number: 7495002Abstract: The present invention relates to new substituted xanthines of general formula wherein R1, R2 and X are defined as in the claims, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: September 1, 2005Date of Patent: February 24, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Elke Langkopf, Matthias Eckhardt, Frank Himmelsbach, Mohammad Tadayyon, Leo Thomas, Ralf R. H. Lotz
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Patent number: 7495003Abstract: The application relates to new substituted xanthines of general formula wherein R1 and R2 are defined as in claims 1 to 11, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: September 1, 2005Date of Patent: February 24, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Mohammad Tadayyon, Leo Thomas
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Publication number: 20090035313Abstract: This invention relates to nicotinamide derivatives of general formula (I): in which R1, Z and R2 have the meanings defined herein, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of such derivatives.Type: ApplicationFiled: July 13, 2004Publication date: February 5, 2009Inventors: Christohper Gordon Barber, Mark Edward Bunnage, John Wilson Harvey, John Paul Mathias
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Patent number: 7482337Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: October 28, 2003Date of Patent: January 27, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
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Publication number: 20080293705Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.Type: ApplicationFiled: August 6, 2008Publication date: November 27, 2008Applicant: Endacea, Inc.Inventors: Constance Neely Wilson, John J. Partridge
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Patent number: 7423041Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.Type: GrantFiled: March 23, 2007Date of Patent: September 9, 2008Assignee: Endacea, Inc.Inventors: Constance Wilson, John J. Partridge
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Patent number: 7407955Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: August 12, 2003Date of Patent: August 5, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R. H. Lotz, Mohammad Tadayyon
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Publication number: 20080139585Abstract: The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR.Type: ApplicationFiled: September 21, 2007Publication date: June 12, 2008Applicant: NOVA SOUTHEASTERN UNIVERSITYInventors: Appu Rathinavelu, Sivanesan Dakshanamurthy, Nagarajan Pattabiraman
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Patent number: 7312223Abstract: The present invention is directed to a metabolite of a xanthine Phosphodiesterase type 5 inhibitor having the following structure derivatives, and formulations thereof, and processes for preparing the same.Type: GrantFiled: July 29, 2004Date of Patent: December 25, 2007Assignee: Schering CorporationInventors: Anima Ghosal, Wei Tong, Swapan K. Chowdhury, Shmuel Zbaida, Mark A. Wirth, Kevin B. Alton, James E. Patrick, Craig D. Boyle, Andrew Stamford
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Patent number: 7247639Abstract: The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists of formula (I). Pharmaceutical compositions comprising an A1 adenosine receptor antagonist of formula (I) and a pharmaceutically acceptable carrier are further provided. Compositions also include diagnostic assay-type probes comprising a novel A1 adenosine receptor antagonist of formula (I) that is labeled or conjugated with radioactive or non-radioactive material. Methods for treating A1 adenosine receptor related disorders comprising administering an A1 adenosine receptor antagonist of formula (I) are also disclosed. The novel A1 adenosine receptor antagonist compositions of formula (I) find further use in diagnostic and imaging methods. wherein R3 is Alk14ArR16, and wherein Alk14 is C1-8 straight or branched alkylene or alkenylene.Type: GrantFiled: June 4, 2004Date of Patent: July 24, 2007Assignee: Endacea, Inc.Inventors: Constance N. Wilson, John J. Partridge
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Patent number: 7202252Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.Type: GrantFiled: February 17, 2004Date of Patent: April 10, 2007Assignee: Endacea, Inc.Inventors: Constance Neely Wilson, John J. Partridge
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Patent number: 7098217Abstract: 3,7-Dihydro-purine-2,6-dione derivatives of Formula (I) are provided wherein R1, R2, R3 and R4 are herein defined for use as CRF receptor ligands in the treatment of disorders characterized by overexpression of corticotropin releasing factor (CRF), such as anxiety, depression, and irritable bowel syndrome.Type: GrantFiled: September 8, 2004Date of Patent: August 29, 2006Assignee: Bristol-Myers Squibb CompanyInventor: Richard A. Hartz
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Patent number: 7053096Abstract: Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in biologic systems.Type: GrantFiled: May 5, 2004Date of Patent: May 30, 2006Assignee: Cell Therapeutics Inc.Inventors: David Porubek, Anil M. Kumar, Charles R. Bredl, J. Peter Klein
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Patent number: 6878715Abstract: Novel heterocyclic compounds having a six membered ring structure fused to a five membered ring structure are found to be useful for the treatment and prevention of symptoms or manifestations associated with disorders affected by Interleukin-12 (“IL-12”) intracellular signaling, such as, for example, Th1 cell-mediated disorders. The therapeutic compounds, pharmaceutically acceptable derivatives (e.g., resolved enantiomers, diastereomers, tautomers, salts and solvates thereof) or prodrugs thereof, have the following general formula: Each X, Y and Z are independently selected from a member of the group consisting of C(R3), N, N(R3) and S.Type: GrantFiled: April 7, 2000Date of Patent: April 12, 2005Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Stephen J. Klaus, Anil M. Kumar, Baoqing Gong
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Patent number: 6869974Abstract: Compounds or their salts having general formulas (I) and (II): wherein s is an integer equal to 1 or 2, A is the radical of a drug that satisfies certain pharmacological tests, C and C1 are bivalent radicals, and precursors of the radicals B and B1 satisfy certain pharmacological tests.Type: GrantFiled: April 11, 2000Date of Patent: March 22, 2005Assignee: Nicox S.A.Inventor: Piero Del Soldato
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Publication number: 20040229836Abstract: Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in biologic systems.Type: ApplicationFiled: May 5, 2004Publication date: November 18, 2004Applicant: CELL THERAPEUTICS, INC.Inventors: David Porubek, Anil M. Kumar, Charles R. Bredl, J. Peter Klein
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Publication number: 20040167137Abstract: A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders: 1Type: ApplicationFiled: February 12, 2004Publication date: August 26, 2004Inventors: Samuel Chackalamannil, Yuguang Wang, Craig D. Boyle, Andrew W. Stamford
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Patent number: 6780865Abstract: Disclosed are compounds having selective hydrolytic potential. The disclosed compounds are useful as compounds having selective stability and are capable of undergoing programmed hydrolysis in biologic systems.Type: GrantFiled: September 18, 1997Date of Patent: August 24, 2004Assignee: Cell Therapeutics, Inc.Inventors: David Porubek, Anil M. Kumar, Charles R. Bredl, J. Peter Klein
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Publication number: 20040132820Abstract: The present invention relates to the use of the antiviral activity of exogenous leukotriene B4 (LTB4), variants and derivatives thereof as a therapeutic agent in viral infections caused by human and animal viruses. The present invention also relates to the use of LTB4 as an anti-neoplastic agent in the prophylaxis and treatment of cancers induced by tumor viruses and in other neoplasic diseases. The human and animal viruses are DNA viruses, such as parvoviridae, papovaviridae, adenoviridae, herpesviridae, poxyviridae and hepadnaviridae; RNA viruses, such as picornaviridae, togaviridae, orthomyxoviridae, paramyxoviridae, coronaviridae, reoviridae, and filoviridae in general, and Retroviridae such as HIV-1 and HIV-2.Type: ApplicationFiled: October 10, 2003Publication date: July 8, 2004Inventors: Jean Gosselin, Pierre Borgeat
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Publication number: 20040110776Abstract: Methods for controlling intraocular pressure with propentofylline are disclosed.Type: ApplicationFiled: June 30, 2003Publication date: June 10, 2004Inventors: Iok-hou Pang, Mark R Hellberg, Abbott F Clark, Peggy E Hellberg, Debra L Fleenor
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Publication number: 20040106572Abstract: The present invention concerns the use of an active ingredient selected from the group consisting of agonists of the adenosine receptor system, for inhibiting viral replication in cells. In particular, the invention provides a composition and method for inhibiting viral replication in cells, the method comprising presenting to the cells an effective amount of the active ingredient. According to one embodiment, the adenosine agonist is an A3 receptor agonist (A3RAg). The invention is particularly useful, for although not limited to, inhibiting the replication of HIV virus in human cells.Type: ApplicationFiled: January 15, 2004Publication date: June 3, 2004Inventors: Pnina Fishman, Kamel Khalili
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Publication number: 20040092536Abstract: This invention provides pharmacologically active compounds having neurological and other bio-active capability. These active compounds comprise the derivatives of guanidino, aminoguanidino, 2-imadazolino, 2-hydrazinoimidazolino or 2-guanidinobenzimidazolino groups.Type: ApplicationFiled: July 1, 2002Publication date: May 13, 2004Inventor: N. Eric Naftchi
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Patent number: 6734187Abstract: Purine derivatives represented by the following formula and salts thereof: wherein R1 represents a C1-C4 alkyl group or difluoromethyl group; R2 represents tetrahydrofuranyl group, a C1-C7 alkyl group and the like; X represents hydrogen atom, a halogen atom or nitro group; and A represents a group represented by the following formula: wherein R3 represents hydrogen atom, a halogen atom and the like; R4 and R5 represent hydrogen atom, a halogen atom, a C1-C4 alkyl group, a C1-C4 alkoxyl group and the like, which are useful as active ingredients of medicaments such as antiasthmatic agents.Type: GrantFiled: July 23, 2002Date of Patent: May 11, 2004Assignee: Mitsubishi Chemical CorporationInventors: Toshihiko Tanaka, Eiichirou Iwashita, Akiko Tarao, Akira Amenomori, Yuya Ono
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Publication number: 20040087587Abstract: The present invention relates to substituted xanthines of general formula 1Type: ApplicationFiled: October 24, 2003Publication date: May 6, 2004Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Michael Mark, Matthias Eckhardt, Elke Langkopf, Roland Maier, Ralf Lotz
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Publication number: 20040072848Abstract: The present invention relates to the use of certain glycol derivatives of xanthines for the treatment of irritable bowel syndrome and functional dyspepsia.Type: ApplicationFiled: August 7, 2003Publication date: April 15, 2004Inventors: Brian E Huber, Allen Wayne Mangel
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Publication number: 20040014766Abstract: The present invention is a 1,3,8 substituted xanthine derivative of formula I 1Type: ApplicationFiled: June 12, 2003Publication date: January 22, 2004Inventors: Peter W. Dunten, Louise H. Foley, Nicholas J.S. Huby, Sherrie L. Pietranico-Cole, Weiya Yun
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Publication number: 20030236260Abstract: Methods of treating IL-6 involved diseases with EP4 receptor ligands, including EP4 receptor antagonists. Assays to determine the effect of test compounds on PGE2-induced whole blood cells activation.Type: ApplicationFiled: April 10, 2003Publication date: December 25, 2003Inventors: Masato Shimojo, Kana Taniguchi
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Patent number: 6649600Abstract: The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be usefull in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable. In one embodiment, the invention features a compound of formula I: wherein: R3 is an optionally substituted bicyclic, tricylic, or pentacyclic group selected from: and wherein R1, R2, R6, X1, X2, and Z are as described in the specification.Type: GrantFiled: November 13, 2000Date of Patent: November 18, 2003Assignee: Biogen, Inc.Inventors: William F. Kiesman, Carol L. Ensinger, Russell C. Petter, James E. Dowling, Gnanasambandam Kumaravel, He Xi Chang, Ko Chung Lin
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Publication number: 20030211156Abstract: A novel oral dosage to be delivered to the stomach comprising a safe and effective amount of an active ingredient selected from the group consisting of emepronium bromidebromide, doxycycline, and other tetracyclines/antibiotics, iron preparations, quinidine, nonsteroidal anti-inflammatory drugs, alprenolol, ascorbic acid, captopril, theophylline, zidovoudine (AZT), bisphosphonates and mixtures thereof and pharmaceutically-acceptable excipients, wherein said oral dosage form is a generally oval form and film coated to facilitate rapid esophageal transit and avoid irritation in the mouth, buccal cavity, pharynx, and esophagus.Type: ApplicationFiled: March 28, 2003Publication date: November 13, 2003Applicant: The Procter & Gamble CompanyInventors: Richard John Dansereau, Petrus Jakobus Bekker
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Publication number: 20030199528Abstract: The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity. The present inhibitors are novel purine derivatives, attached at position 8 of the purine skeleton to a diamine.Type: ApplicationFiled: January 28, 2003Publication date: October 23, 2003Inventors: Anders B. Kanstrup, Christian Klarner Sams, Jane Marie Lundbeck, Lise Brown Christiansen, Andrew Neil Bowler
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Publication number: 20030199529Abstract: Disclosed are (i) compounds of a steroid, a &bgr;-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, &bgr;-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.Type: ApplicationFiled: May 5, 2003Publication date: October 23, 2003Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Stewart K. Richardson
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Publication number: 20030171383Abstract: The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine A2 receptor antagonism, preferably an adenosine A2b receptor antagonism, or a salt thereof.Type: ApplicationFiled: October 9, 2002Publication date: September 11, 2003Inventors: Masahiro Yasuda, Hitoshi Harada, Shuhei Miyazawa, Seiichi Kobayashi, Kokichi Harada, Takayuki Hida, Hisashi Shibata, Nobuyuki Yasuda, Osamu Asano, Yoshihiko Kotake
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Patent number: 6608069Abstract: The present invention relates to novel compounds of formula (I): wherein Z represents a 5 or 6 membered cycloalkyl, aryl, substituted cycloalkyl, or substituted aryl, said cycloalkyl, aryl, substituted cycloalkyl or substituted aryl optionally containing one or more heteroatoms selected from 0, N or S; k represents 0 or 1; n represents an integer of 1 to 50; X represents —O—, —N(H)—, —N(C1-6alkyl)-, —N(C3-8cycloalkyl)-, —N(C1-8alkyl)(C3-8 cycloalkyl), —N[(CH2CH2O)m(C1-12 alkyl, aryl, or aralkyl)]-, —CH2O—, —CH2NH—, —CH2N(C1-6alkyl)-, —CH2N(C3-8cycloalkyl)-, or —C1-12alkyl-; Q represents (—CH2)p, (—CH═CH—)p, (—C≡C—)p, (—(O)p1CH2—)p or (—CH2(O)p1)p R6 and R7 independently represent O or S; and all other variables are as defined herein; processes for their preparation, pharmaceutical formulations containing them, and their use in meType: GrantFiled: February 9, 2001Date of Patent: August 19, 2003Assignee: SmithKline Beecham CorporationInventors: Susan Mary Daluge, Michael Tolar Martin, Martin Howard Osterhout
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Patent number: 6605600Abstract: The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be useful in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable. In one embodiment, the invention features a compound of formula I: R3 is an optionally substituted group selected from: and wherein X1, X2, Z, R1, R2, and R6 are as described in the specification.Type: GrantFiled: November 13, 2000Date of Patent: August 12, 2003Assignee: Biogen, IncorporatedInventors: Carol L. Ensinger, James E. Dowling, Russell C. Petter, Gnanasambandam Kumaravel
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Publication number: 20030143199Abstract: The present invention provides A therapeutic method to enhance the efficacy of interferon treatment comprising administering to a mammal subject to interferon treatment a compound which is an antagonist of the IL-4 or IL-13 signal transduction pathway in an amount effective to enhance said efficacy. The method includes treatment of diseases such as cancer, proliferative fibrotic diseases, viral diseases, or autoimmune diseases. The invention also includes the use of chemotherapeutic agents, radiation or other treatments in conjunction with the method of the invention.Type: ApplicationFiled: October 9, 2002Publication date: July 31, 2003Inventors: Dennis A. Carson, Howard B. Cottam, Lorenzo M. Leoni, Sylvie Barchechath
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Publication number: 20030139428Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.Type: ApplicationFiled: November 8, 2002Publication date: July 24, 2003Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
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Publication number: 20030139370Abstract: Compositions are provided, which comprise at least one nucleoside analogue inhibitor, pharmaceutically acceptable salts, solvates, or prodrugs thereof and fusaric acid, derivatives, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising the above compositions are also provided that optionally further include another therapeutically effective compound, such as a carrier. Systemic and topical preparations comprising the above compositions are also provided as well as methods of treating viral diseases by the administration of the above antiviral agents to a patient.Type: ApplicationFiled: December 3, 2002Publication date: July 24, 2003Inventors: Michael G. Douglas, Avinash N. Amin
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Publication number: 20030134865Abstract: A screening method for identifying a drug-like compound or lead compound for the development of a drug-like compound in which (1) a xanthine or related compound is exposed to a histone deacetylase, (2) the binding of the compound to the histone deacetylase is measured or the change in the activity of the histone deacetylase is measured or the change in the binding of the histone deacetylase to activated glucocorticoid receptor (GR) is measured and (3) any compound capable of the required binding to the histone deacetylase or producing the required change in the activity of the histone deacetylase or its binding to activated glucocorticoid receptor is identified. Methods of treatment make use of compounds identifiable by the screening methods.Type: ApplicationFiled: January 13, 2003Publication date: July 17, 2003Inventors: Ian Adcock, Samson Lim, Kazuhiro Ito, Peter John Barnes
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Publication number: 20030124191Abstract: The present invention relates to the use of a powder comprising at least one active substance, at least one surfactant, at least one wetting agent and at least one diluent, for preparing a pharmaceutical or nutraceutical composition, this composition allowing rapid and immediate release of the active substance.Type: ApplicationFiled: March 25, 2002Publication date: July 3, 2003Inventors: Jerome Besse, Laurence Besse
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Publication number: 20030119831Abstract: Compounds provided herein are 3,7-dihydro-purine-2,6-dione derivatives of Formula (I): 1Type: ApplicationFiled: November 7, 2002Publication date: June 26, 2003Inventor: Richard A. Hartz
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Publication number: 20030104371Abstract: The invention relates to methods of evaluating transplant rejection in a host comprising determining a heightened magnitude of gene expression of genes in rejection-associated gene clusters. The disclosed gene clusters include genes that are substantially co-expressed with cytotoxic lymphocyte pro-apoptotic genes, cytoprotective genes and several other cytokine and immune cell genes.Type: ApplicationFiled: February 6, 2001Publication date: June 5, 2003Inventors: Terry B. Strom, Manikkam Suthanthiran, Lauro Vasconcellos
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Publication number: 20030050318Abstract: A water in oil emulsion system and a process for preparing such a emulsion has been provided for topically applying aminophylline for reducing cellulite conditions.Type: ApplicationFiled: August 29, 2002Publication date: March 13, 2003Inventor: Kenneth Shirley
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Publication number: 20030032650Abstract: Adenosine receptor antagonists, especially aminophyllline, are used to treat or prevent acute renal failure. In the preferred embodiment, aminophylline is administered by infusion so that it does not exceed a serum theophylline level of 15-20 micrograms/ml, most preferably the aminophylline is administered to achieve a serum theophylline concentration of 3-10 micrograms/ml, with an infusion rate of 0.1-0.6 mg/kg IBW/hour (IBW=ideal body weight). The adenosine receptor antagonist can also be used to help sustain a kidney for transplant purposes. Preferably, aminophylline is loaded while the kidney is still part of the donor. A dose of aminophylline of 5 mg/kg lean body weight is infused into the donor over a 30-60 min period, with cardiac monitoring. The infusion dose is decreased in the event of supraventricular or ventricular tachycardias. The kidney is removed and placed in the standard “cold” bath, but containing aminophylline at a dose of 5-10 micrograms/ml (5-10 mg/l).Type: ApplicationFiled: August 8, 2002Publication date: February 13, 2003Applicant: GenoMed, LLC DEInventor: David W. Moskowitz
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Publication number: 20020198205Abstract: The present invention relates to substituted xanthines of general formula 1Type: ApplicationFiled: February 22, 2002Publication date: December 26, 2002Inventors: Frank Himmelsbach, Michael Mark, Matthias Eckhardt, Elke Langkopf, Roland Maier, Ralf Lotz