Chalcogen Bonded Directly To Ring Carbon Of The Five-membered Hetero Ring Patents (Class 514/418)
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Publication number: 20030181507Abstract: The present invention relates to a novel method of treating of pain or anxiety, using compounds that modulate KCNQ potassium channels and currents.Type: ApplicationFiled: February 24, 2003Publication date: September 25, 2003Inventors: Bo Skaaning Jensen, Rikke Schroder, Dorte Strobaek, Soren Peter Olesen
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Patent number: 6624171Abstract: Substituted aza-oxindole derivatives useful as cyclin dependent kinase 11 inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy.Type: GrantFiled: August 28, 2001Date of Patent: September 23, 2003Assignee: SmithKline Beecham CorporationInventors: Philip Anthony Harris, Lee Frederick Kuyper, Karen Elizabeth Lackey, James Marvin Veal
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Publication number: 20030176487Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: August 26, 2002Publication date: September 18, 2003Applicant: SUGEN, INC.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Publication number: 20030162817Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, vascular restenosis, microbial infections, and psoriasis, or as lead compounds for the development of such agents.Type: ApplicationFiled: October 11, 2002Publication date: August 28, 2003Applicant: Tularik Inc.Inventors: John A. Flygare, Julio Cesar Medina, Bei Shan, David Louis Clark, Terry J. Rosen
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Publication number: 20030153612Abstract: The present invention provides a method of treating Restless Legs Syndrome in human or animal patient, which method comprises administering to said patient an effective amount of ropinirole or a pharmaceutically acceptable salt or solvate thereof. Preferably, a dose of ropinirole or a pharmaceutically acceptable salt or solvate thereof is administered to the patient 1 to 3 hours before the patient goes to bed. A typical dose comprises 0.1 mg -5 mg of ropinirole. The invention also provides a pharmaceutical composition for use in the treatment of Restless Legs Syndrome which comprises an effective amount of ropinirole or a pharmaceutically acceptable salt or solvate thereof and a pharmaceutically acceptable carrier.Type: ApplicationFiled: February 10, 2003Publication date: August 14, 2003Applicant: SmithKline Beecham CorporationInventor: Kapil Dev Sethi
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Publication number: 20030153604Abstract: This invention is directed to an (aminoiminomethyl or aminomethyl)benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.Type: ApplicationFiled: February 24, 2003Publication date: August 14, 2003Applicant: Aventis Pharmaceuticals Inc.Inventors: William P. Dankulich, Daniel G. McGarry, Christopher Burns, Timothy F. Gallagher, Francis A. Volz
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Patent number: 6596732Abstract: The invention relates to compounds of formula: and their solvates and/or hydrates exhibiting an affinity and a selectivity for arginine-vasopressin V1b receptors or for both V1b and V1a receptors.Type: GrantFiled: August 12, 2002Date of Patent: July 22, 2003Assignee: Sanofi-SynthelaboInventors: Claudine Serradeil-Le Gal, Bernard Tonnerre, Jean Wagnon
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Patent number: 6576636Abstract: The invention provides conjugates of fatty acids and antiviral agents useful in treating liver disorders.Type: GrantFiled: December 5, 2000Date of Patent: June 10, 2003Assignee: Protarga, Inc.Inventors: Nigel L. Webb, Matthews O. Bradley, Charles S. Swindell, Victor E. Shashoua
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Patent number: 6576656Abstract: An oxindole of Formula 1 or a prodrug thereof, or a pharmaceutically acceptable salt thereof is useful for growth hormone releaser: wherein R1, R2, R3 and R4 are independently hydrogen, optionally substituted alkyl etc; R5 is optionally substituted aryl or optionally substituted heteroaryl; Z is —O— or —NH—; one of W1 and W2 is hydrogen, alkyl or —Y—CON(R10)R11; the other of W1 and W2 is n is 1, 2 or 3; m is 0, 1, 2 or 3; Y is single bond or C1-C3 alkylene; R6 and R7 are independently hydrogen, optionally substituted alkyl etc; R8 and R9 are independently hydrogen, optionally substituted alkyl etc; R10 and R11 are independently hydrogen, alkyl etc.Type: GrantFiled: March 22, 2001Date of Patent: June 10, 2003Assignee: Sumitomo Pharmaceuticals Co., Ltd.Inventors: Teruhisa Tokunaga, Takashi Umezome, W. Ewan Hume, Ryu Nagata, Kazuhiko Okazaki, Yasuyuki Ueki, Kazuo Kumagai
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Patent number: 6566389Abstract: A method for treating or preventing symptoms of tardive dyskensia comprises administering melatonin to patient exhibiting or liable to develop such symptoms. The melatonin is administered in an amount effective to ameliorate or prevent symptoms of tardive dyskensia developing in the patient.Type: GrantFiled: November 26, 2001Date of Patent: May 20, 2003Assignee: Neurim Pharmaceuticals (1991) Ltd.Inventors: Nava Zisapel, Moshe Laudon
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Patent number: 6562858Abstract: The present invention discloses a method for the treatment of depression in a human being identified as having depression. This method comprises the administration of a therapeutically effective depression treatment amount of M-3 agonists, 5-MCA-NAT or an analog, to said human being. The 5-MCA-NAT, or an analog, thereof may be administered alone or in combination with other agents, as Ca++ antagonists.Type: GrantFiled: April 12, 2001Date of Patent: May 13, 2003Assignee: St. Elizabeth's Medical Center of Boston, Inc.Inventor: Gregory Oxenkrug
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Patent number: 6559176Abstract: The invention provides autoinducer-2 analogs that regulate the activity of autoinducer-2 and methods of using such analogs for regulating bacterial growth and pathogenesis.Type: GrantFiled: May 10, 2001Date of Patent: May 6, 2003Assignees: Princeton University, Quorex Pharmaceuticals, Inc., University Technologies International, Inc.Inventors: Bonnie L. Bassler, Carol Dammel, Stephan Schauder, Kevan Shokat, Jeffrey Stein, Michael G. Surette
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Patent number: 6544970Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings, in combination with progestins, estrogens, or both. These methods of treatment may be used for contraception, for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, or prostate, minimization of side effects, cyclic menstrual bleeding, or stimulation of food intake.Type: GrantFiled: May 22, 2002Date of Patent: April 8, 2003Assignees: WYETH, Ligand Pharmaceuticals, Inc.Inventors: Gary S. Grubb, Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H. W. Bender, Puwen Zhang, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Patent number: 6531502Abstract: The present invention relates to novel 3-methylidenyl-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: February 5, 2001Date of Patent: March 11, 2003Assignee: Sugen, Inc.Inventors: Pen Cho Tang, Li Sun, Todd Anthony Miller, Congxin Liang, Ngoc My Tran, Anh Thi Nguyen, Asaad Nematalla
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Patent number: 6525072Abstract: The present invention relates to novel geometrically restricted 2-indolinones and physiologically acceptable salts thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: August 30, 1999Date of Patent: February 25, 2003Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Todd Anthony Miller, Li Sun, Ngoc My Tran, Asaad Nematalla, Anh Thi Nguyen
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Patent number: 6521657Abstract: This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.Type: GrantFiled: October 30, 2001Date of Patent: February 18, 2003Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Andrew Fensome, Puwen Zhang, Marci C. Koko, Lin Zhi, Todd K. Jones, Jay E. Wrobel, Christopher M. Tegley, James P. Edwards, Edward G. Melenski
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Patent number: 6514992Abstract: The present invention is to novel compounds of Formula (I), their pharmaceutical compositions, and to the novel inhibition of Caspases for use in the treatment of apoptosis, and disease states caused by excessive or inappropriate cell death.Type: GrantFiled: December 14, 2000Date of Patent: February 4, 2003Assignee: SmithKline Beecham CorporationInventors: Dennis Lee, Scott A. Long
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Patent number: 6506763Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.Type: GrantFiled: July 30, 2001Date of Patent: January 14, 2003Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 6498176Abstract: Compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, D, X, Y and Z have the meaning as defined in the claims exhibit protein tyrosine kinase and protein serin/threonine kinase inhibitory activity.Type: GrantFiled: August 22, 2001Date of Patent: December 24, 2002Assignee: SmithKlineBeecham CorporationInventors: Karen Elizabeth Lackey, Robert Walton McNutt, Jr.
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Publication number: 20020193415Abstract: The invention as disclosed herein is a method and composition for the treatment of HIV in humans and other host animals, that includes the administration of an effective HIV treatment amount of a phenylindole as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier. The compounds of this invention either possess antiviral (i.e., anti-HIV) activity, or are metabolized to a compound that exhibits such activity.Type: ApplicationFiled: April 11, 2002Publication date: December 19, 2002Inventors: Paulo LaColla, Marino Artico, Jean-Pierre Sommadossi
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Patent number: 6486192Abstract: This invention relates to the use of certain indole compounds, which are active as inhibitors of the fatty acid synthase FabH, for the treatment of bacterial infections.Type: GrantFiled: November 28, 2001Date of Patent: November 26, 2002Assignee: SmithKline Beecham CorporationInventors: Robert A. Daines, Pamela A. Chambers
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Patent number: 6482848Abstract: The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.Type: GrantFiled: May 24, 2001Date of Patent: November 19, 2002Assignee: Sugen IncorporatedInventors: Malcolm Wilson Moon, Walter Morozowich, Ping Gao, Marcel Koenig
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Patent number: 6479528Abstract: Methods for inhibiting and/or reversing tau filament formation or polymerization are provided. These methods can be used for treating certain neurological disorders in vivo by administering pharmaceutical compositions which inhibit and/or reverse tau filament formation or polymerization. An especially preferred pharmaceutical composition contains an inhibitor of the general formula I wherein R1 is an aliphatic radical having one to six carbon atoms and wherein R2 and R3 independently are a second aliphatic radical having one to six carbon atoms, a hydroxyl-substituted aliphatic radical having one to six carbon atoms, or a pheny radical or a pharmaceutically acceptable salt of the inhibitor.Type: GrantFiled: July 31, 2001Date of Patent: November 12, 2002Assignee: Neuronautics, Inc.Inventors: Jeff Kuret, Sam Khatami
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Patent number: 6472406Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: July 5, 2000Date of Patent: October 29, 2002Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
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Patent number: 6469042Abstract: There is provided novel 3-fluoro-3-phenyl oxindole derivatives of Formula I wherein R1, R2, R3 and R4 each are independently hydrogen, C1-4 alkyl, halogen, fluoromethyl, trifluoromethyl, phenyl, 4-methylphenyl or 4-trifluoromethylphenyl; R5 is C1-6 alkyl optionally substituted with one to three same or different groups selected from fluoro and chloro, provided R5 is not C1-6 alkyl when Y is O; Y is O or S; and R6 and R7 each are independently hydrogen, chloro, bromo or trifluoromethy; which are openers of the KCNQ potassium channels and are useful in the treatment of disorders which are responsive to the opening of the KCNQ potassium channels.Type: GrantFiled: February 14, 2002Date of Patent: October 22, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Piyasena Hewawasam, Pierre Dextraze, Valentin K. Gribkoff, Gene G. Kinney, Steven I. Dworetzky
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Patent number: 6465507Abstract: The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds of the invention. The invention also relates to methods of modulating the function of protein kinases using indolinone compounds of the invention and methods of treating diseases by modulating the function of protein kinases and related signal transduction pathways.Type: GrantFiled: February 28, 2001Date of Patent: October 15, 2002Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Todd A. Miller, Xiaoyuan Li, Ruofei Zhang, Jinrong Cui, Ping Huang, Chung Chun Wei
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Patent number: 6462032Abstract: This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings, in combination with progestins, estrogens, or both. These methods of treatment may be used for contraception or for the treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.Type: GrantFiled: April 19, 2000Date of Patent: October 8, 2002Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: Gary S. Grubb, Andrew Fensome, Lori L. Miller, John W. Ullrich, Reinhold H. W. Bender, Puwen Zhang, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Patent number: 6455541Abstract: The present invention focuses upon a method for inhibiting bone resorption. This method involves administering a 5-lipoxygenase inhibitor to a subject in an amount inhibiting the effects of an osteoclast-stimulating factor. When the production of the osteoclast-stimulating factors such as PTH, PTHrp, IL-1, TNF, LT, 1,25(OH)2D3 or other factors which may stimulate the production of 5-LO metabolites via the 5-lipoxygenase pathway is inhibited, bone resorption markedly declines. The direct osteoclast-stimulating factors include leukotriene, peptidoleukotriene and 5-hydroxyeicosatetraenoic acid. Other factors yet to be identified or previously known may also be 5-lipoxygenase metabolites that stimulate bone resorption. While 5-lipoxygenase inhibitors may be substrate analogs or allosteric inhibitors, a substance which inhibits the activity of this enzyme may utilize other mechanisms (e.g., inhibition of 5-LO biosynthesis) and nevertheless function to inhibit bone resorption.Type: GrantFiled: May 8, 2000Date of Patent: September 24, 2002Assignee: Board of Regents, The University of Texas SystemInventors: Lynda F. Bonewald, G. R. Mundy, Wolf E. Gallwitz
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Patent number: 6441004Abstract: The invention concerns the use of a compound of the formula (I) in which Z, X, T, A, R1, R2, p and q have any of the meanings defined herein, and their pharmaceutically acceptable salts or in vivo hydrolysable esters, in the treatment of a disease or condition mediated by monocyte chemoattractant protein-1 (MCP-1). Certain of the components of formula (I) are novel and are provided, together with pharmaceutical compositions thereof, as further features of the invention.Type: GrantFiled: February 3, 2000Date of Patent: August 27, 2002Assignee: Zeneca LimitedInventors: Alan Wellington Faull, Andrew John Barker, Jason Grant Kettle
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Patent number: 6436949Abstract: Heterocyclically substituted benzamides of the formula I are described, where R1, R2, R3, R4, R5, X, m and n have the meanings given in the description. The novel compounds are useful for controlling diseases.Type: GrantFiled: September 21, 2000Date of Patent: August 20, 2002Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber
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Patent number: 6436965Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts and hydrates thereof are disclosed as useful for treating or preventing diseases and conditions mediated by PDE-IV. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: March 1, 2001Date of Patent: August 20, 2002Assignee: Merck Frosst Canada & Co.Inventors: Marc Labelle, Claudio Sturino, Nicolas Lachance, Dwight Macdonald
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Publication number: 20020103248Abstract: This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: 1Type: ApplicationFiled: October 30, 2001Publication date: August 1, 2002Inventors: Andrew Fensome, Puwen Zhang, Marci C. Koko, Lin Zhi, Todd K. Jones, Jay E. Wrobel, Christopher M. Tegley, James P. Edwards, Edward G. Melenski
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Patent number: 6423738Abstract: A method for treating circadian rhythm phase disorders is described. The invention provides methods to specifically advance or delay the phase of certain circadian rhythms in humans. The disclosed methods relate to the administration of melatonin at times determined with relation to the time of dim light endogenous melatonin onset. Embodiments capable of alleviating the effects of jet lag, winter depression and shift-work sleep disturbance are provided.Type: GrantFiled: May 30, 2000Date of Patent: July 23, 2002Assignee: Oregon Health & Sciences UniversityInventors: Alfred J. Lewy, Robert L. Sack
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Publication number: 20020091133Abstract: The present invention is directed to a method of inducing neurogenesis by administering to a mammal an effective quantity of a compound that induces neurogenesis, where neurogenesis includes proliferation of neural stem and progenitor cells, differentiation of these cells into neurons, and/or survival of these new neurons. In general, the compound comprises three moieties, A, L, and B, covalently linked. A can be a purine, tetrahydroindolone, or pyrimidine; L is a linker, while B is a moiety that promotes absorption of the compound. A particularly preferred compound is N4-[[3-(6-oxo-1,6-dihydropurin-9-yl)-1-oxopropyl] amino] benzoic acid (also known as AIT-082 or leteprinim potassium). Another aspect of the invention is pharmaceutical compositions for inducing neurogenesis.Type: ApplicationFiled: December 12, 2001Publication date: July 11, 2002Applicant: Eve M. TaylorInventor: Eve M. Taylor
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Publication number: 20020086895Abstract: A method for treating a fungal infection is disclosed. The method includes contacting a fungus with a substituted aurone derivative.Type: ApplicationFiled: September 20, 2001Publication date: July 4, 2002Inventors: Wai-Lam Alex Chu, Flemming R. Jensen, Thomas B. Jensen, James B. McAlpine, Brigitte Sokilde, Alexandra M. SantAna-Sorensen, Sunil Ratnayake, Jack B. Jiang, Catharine Noble, Angela M. Stafford
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Patent number: 6414153Abstract: Novel compounds of the formula I: which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary compounds are: 3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-1,3-dihydroindol-2-one; 3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-3-methyl-1,3-dihydro-indol-2-one; 3-benzyl-1-(3,5-dichlorophenyl)-3-methyl-1,3-dihydroindol-2-one; 3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-4-hydroxy-3-methyl-1,3-dihydroindol-2-one; and, 3-(4-bromobenzyl)-1-(3,5-dichlorophenyl)-5-fluoro-1,3-dihydroindol-2-one.Type: GrantFiled: June 28, 2000Date of Patent: July 2, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Terence Alfred Kelly, Jiang-Ping Wu, Daniel Kuzmich, Yancey David Ward, Leah Lynn Frye
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Publication number: 20020082256Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: ApplicationFiled: September 25, 2001Publication date: June 27, 2002Inventors: Rajashehar Betageri, Steffen Breitfelder, Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, Thomas M. Kirrane, Monica H. Moriak, Neil Moss, Usha R. Patel, John R. Proudfoot, John R. Regan, Rajiv Sharma, Sanxing Sun, Alan D. Swinamer, Hidenori Takahashi
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Patent number: 6410584Abstract: A method for inhibiting neoplastic cells and related conditions by exposing them to substituted indole derivatives.Type: GrantFiled: November 25, 1998Date of Patent: June 25, 2002Assignee: Cell Pathways, Inc.Inventors: Rifat Pamukcu, Gary A. Piazza
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Publication number: 20020068732Abstract: The invention relates to method of preventing or treating a disease related to the 5-HT2C receptor and the 5-HT6 receptor, comprising administering to a human or animal subject in need thereof a 5-HT2C receptor agonist and a 5-HT6 receptor antagonist in sufficient amounts to provide a therapeutic effect. The invention also relates to a pharmaceutical composition comprising an effective amount of a combination of a 5-HT2C receptor agonist and a 5-HT6 receptor antagonist, and optionally a pharmaceutically acceptable carrier.Type: ApplicationFiled: July 20, 2001Publication date: June 6, 2002Inventors: Jossan Sukhwinder, Bjorn M. Nilsson, Kjell S. Sakariassen, Jan Svartengren
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Patent number: 6395768Abstract: The cytotoxic effects of amyloid beta protein on cells are prevented by contacting the cells with an effective amount of an indole-3-propionic acid or a salt or ester thereof. Furthermore, a fibrillogenic disease can be treated in a human subject by administering to the human subject an amount of-an indole-3-propionic acid or a salt or ester thereof effective to prevent or reverse fibrillogenesis. Oxidation in a biological sample can be decreased by contacting the biological sample with an effective amount of an indole-3-propionic acid or a salt or ester thereof. Additionally, diseases or other conditions where free radicals and/or oxidative stress play a role can be treated by administering an effective amount of an indole-3-propionic acid or a salt or ester thereof.Type: GrantFiled: May 30, 2000Date of Patent: May 28, 2002Assignees: South Alabama Medical Science Foundation, New York UniversityInventors: Miguel A. Pappolla, Blas Frangione, Jorge Ghiso, Burkhard Poeggeler
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Patent number: 6395764Abstract: This invention involves compounds having the following structure: wherein: a) R1 is hydrogen; or alkyl; bond (a) is a single or a double bond; b) R2 and R3 are each independently selected from hydrogen; unsubstituted C1-C3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C1-C3 alkylamino or C1-C3 dialkylamino and halo; c) R4, R5 and R6 are each independently selected from hydrogen; unsubstituted C1-C3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C1-C3 alkylamino or C1-C3 dialkylamino; halo; and 2-imidazolinylamino; and wherein one and only one of R4, R5 and R6 is 2-imidazolinylamino; d) R7 is selected from hydrogen; unsubstituted C1-C3 alkanyl, alkenyl or alkynyl; cycloalkanyl, cycloalkenyl; unsubstituted C1-C3 alkylthio or alkoxy; hydroxy; thio; nitro; cyano; amino; C1-C3 alkylamino or C1-C3 dialkylamino and halo;Type: GrantFiled: October 17, 2000Date of Patent: May 28, 2002Assignee: The Procter & Gamble CompanyInventors: Raymond Todd Henry, Russell James Sheldon, William Lee Seibel
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Publication number: 20020061899Abstract: A method of treating drug-induced peripheral neuropathy comprises administering to a patient with drug-induced peripheral neuropathy an effective quantity of a purine derivative or analogue, a tetrahydroindolone derivative or analogue, or a pyrimidine derivative or analogue. If the compound is a purine derivative, the purine moiety can be guanine or hypoxanthine. The compound can induce peripheral nerve sprouting through the action of a neurotrophic factor such as nerve growth factor (NGF) without the occurrence of hyperalgesia. The peripheral nerve sprouting can be nociceptive nerve sprouting. The drug-induced peripheral neuropathy can be drug-induced peripheral neuropathy associated with the administration of oncolytic drugs, such as a vinca alkaloid, cisplatin, paclitaxel, suramin, altretamine, carboplatin, chlorambucil, cytarabine, dacarbazine, docetaxel, etoposide, fludarabine, ifosfamide with mesna, tamoxifen, teniposide, or thioguanine.Type: ApplicationFiled: July 6, 2001Publication date: May 23, 2002Inventors: Jack Diamond, Alvin J. Glasky, Mark M. Foreman
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Publication number: 20020052398Abstract: The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, thalidomide and various related compounds such as thalidomide precursors, analogs, metabolites and hydrolysis products have been shown to inhibit angiogenesis and to treat disease states resulting from angiogenesis. Importantly, these compounds can be administered orally.Type: ApplicationFiled: December 12, 2001Publication date: May 2, 2002Inventor: Robert J. D'Amato
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Patent number: 6376531Abstract: The present invention provides organic deuterium compounds which can be therapeutic compounds to treat manic depression. In particular, the present invention relates to deuterated methionine, norepinephrine, pyridoxine-5-phosphate, tryptophan, 5-hydroxytryptophan, serotonin, N-acetyl serotonin and melatonin, which can be used as therapeutic agents.Type: GrantFiled: November 12, 1999Date of Patent: April 23, 2002Inventor: Rupert Charles Bell
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Patent number: 6369109Abstract: The present invention is, generally, directed to the use of betulinic acid and derivatives thereof for the treatment of neuroectodermal tumors. The present invention is based on the discovery that betulinic acid and its derivatives are potent anti-neuroectodermal agents. As disclosed herein, betulinic acid and its derivatives are useful for the treatment of neuroectodermal tumors, including, due to its distinct mechanism of action, neuroectodermal tumors that are resistant to conventional chemotherapeutical agents. In addition to the new use of known compounds, the invention discloses novel compounds and pharmaceutical compositions for the treatment of neuroectodermal tumors.Type: GrantFiled: October 28, 1998Date of Patent: April 9, 2002Assignee: Deutsches Krebsforschungszentrum Stiftung des Offentlichen RechtsInventors: Klaus Michael Debatin, Simone Fulda, Manfred Wiessler, Marek Los, Walter Mier
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Publication number: 20020040047Abstract: The invention relates to the use of 4-aryl-4-hydroxy-tetrahydropyrans and 3-aryl-3-hydroxy-tetrahydrofurans for the treatment or prevention of chronic obstructive pulmonary disease.Type: ApplicationFiled: December 6, 2000Publication date: April 4, 2002Inventors: Edward Raymond Halstead Walker, Roger Metcalf, Stephen John Foster
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Patent number: 6358992Abstract: A method for inhibiting neoplasia, particularly cancerous and precancerous lesions, by exposing the affected cells to indole derivatives.Type: GrantFiled: November 19, 1999Date of Patent: March 19, 2002Assignee: Cell Pathways, Inc.Inventors: Rifat Pamukcu, Gary A. Piazza
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Publication number: 20020028828Abstract: The present invention relates to (2-oxindol-3-ylidenyl)acetic acid derivatives which modulate the activity of protein kinases and are therefore useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: ApplicationFiled: May 2, 2001Publication date: March 7, 2002Inventor: Chung-Chen Wei
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Publication number: 20020025972Abstract: The comprehensive pharmacologic therapy for treatment of obesity is a procedure which involves the administration of a desired therapeutic range of Diethylpropion and/or Phentermine in combination with a SSRI medication and nutritional supplementation for brief and long durations which may be 12 months or more. The preferred procedure involves the administration of drugs in combination which are identified as: Citalopram (Celexa) and Phentermine; Citalopram (Celexa) and Diethylpropion; Citalopram (Celexa), Phentermine, and Diethylpropion. In addition nutritional supplementation such as a multivitamin, 5-Hydroxytryptophan, vitamin B6, vitamin C, Tyrosine, Calcium, and Lysine may be used to enhance the performance of the weight loss treatment program.Type: ApplicationFiled: August 30, 2001Publication date: February 28, 2002Inventor: Martin C. Hinz
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Publication number: 20020025343Abstract: A process is disclosed for the preparation of an essentially tetramerfree, substantially stromafree, polymerized, pyridoxylated hemoglobin. Also disclosed is an essentially tetramerfree, substantially stromafree, polymerized, pyridoxylated hemoglobin product capable of being infused into human patients in an amount of up to about 5 liters.Type: ApplicationFiled: May 10, 1999Publication date: February 28, 2002Inventors: RICHARD E. DE WOSKIN, MARC D. DOUBLEDAY