Sulfoxy Patents (Class 562/429)
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Publication number: 20080249137Abstract: Compounds are described that are active on at least one of PPAR?, PPAR?, and PPAR?, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPAR?, PPAR?, and PPAR?.Type: ApplicationFiled: September 6, 2006Publication date: October 9, 2008Inventors: Jack Lin, Patrick Womack, Byunghun Lee, Shenghua Shi, Chao Zhang, Dean R. Artis, Prabha N. Ibrahim, Weiru Wang, Rebecca Zuckerman
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Patent number: 7423176Abstract: The present invention provides compounds of the structure: wherein the constituent members are defined herein, including pharmaceutical compositions thereof and methods of treating diseases therewith.Type: GrantFiled: April 12, 2005Date of Patent: September 9, 2008Assignees: Cephalon, Inc., Cephalon FranceInventors: Edward R. Bacon, Sankar Chatterjee, Mohamed Iqbal, Brigitte Lesur, Philippe Louvet
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Publication number: 20080214862Abstract: The present invention encompasses processes for preparing intermediates of armodafinil, and the conversion of the intermediates to armodafinil.Type: ApplicationFiled: December 5, 2007Publication date: September 4, 2008Inventors: Ben-Zion Dolitzky, Kobi Chen
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Patent number: 7411088Abstract: There is provided stereoselective route to a compound of formula I: wherein R represents H or an alkali metal, Ar1 represents 4-chlorophenyl and Ar2 represents 2,5-difluorophenyl.Type: GrantFiled: February 16, 2005Date of Patent: August 12, 2008Assignees: Merck & Co., Inc., Merck Sharp & Dohme Ltd.Inventors: Karel Marie Joseph Brands, Sarah Elizabeth Brewer, Antony John Davies, Ulf H. Dolling, Deborah Camille Hammond, David Ross Lieberman, Jeremy Peter Scott
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Publication number: 20080146632Abstract: The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl zing substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the Fc?RIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.Type: ApplicationFiled: February 1, 2008Publication date: June 19, 2008Applicant: TRILLIUM THERAPEUTICS, INC.Inventors: Mark Phillip Hogarth, Geoffrey Allan Pietersz, Gerard Peter Moloney
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Publication number: 20080132480Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: August 22, 2005Publication date: June 5, 2008Applicant: AstraZeneca ABInventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
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Patent number: 7309720Abstract: A compound of formula (I) wherein T represents O, S or NR and wherein R represents a H, a C1-6alkyl group or a phenyl C1-6alkyl group and pharmaceutically acceptable salts thereof, processes for preparing such compounds, their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, methods for their therapeutic use and and pharmaceutical compositions containing themType: GrantFiled: June 16, 2004Date of Patent: December 18, 2007Assignee: AstraZeneca ABInventor: Eva-Lotte Lindstedt-Alstermark
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Patent number: 7285678Abstract: A method for removing impurities from 2-nitro-4-methylsulfonylbenzoic acid which comprises at least two of the following steps, in any order, (a) dissolving 2-nitro-4-methylsulfonylbenzoic acid in water at a pH of about 2 to 10, followed by filtration; (b) contacting an aqueous solution of 2-nitro-4-methylsulfonylbenizoic acid with activated carbon at a pH of about 2 to 10; (c) treating an aqueous solution of 2-nitro-4-methylsulfonylbenzoic acid with sufficient base to hydrolyze undesired nitro and dinitro substituted impurities; followed by maintaining the resulting aqueous solution comprising 2-nitro-4-methylsulfonylbenzoic acid at a temperature of up to about 95° C., and adjusting the pH of said solution to about a pH which is sufficient to effect crystallization of 2-nitro-4-methylsulfonylbenzoic acid upon cooling.Type: GrantFiled: March 25, 2002Date of Patent: October 23, 2007Assignee: Syngenta LimitedInventors: Kambiz Javdani, Gilbert Rodriguez, James Peter Muxworthy
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Patent number: 7186854Abstract: Bicalutamide and/or its intermediates are made by the use of p-fluorobenzenesulfinic acid salt as a reagent.Type: GrantFiled: October 10, 2003Date of Patent: March 6, 2007Assignee: Synthon IP Inc.Inventors: Lambertus Thijs, Rolf Keltjens, Gerrit J. B. Ettema
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Patent number: 7153993Abstract: Process for making a pharmaceutical composition, comprising: a compound of formula (1) in crystalline form: together with a pharmaceutically acceptable carrier or excipient, wherein the compound of formula (1) is present in polymorphic crystal form A substantially free of other polymorphs, and methods for making this polymorph.Type: GrantFiled: December 22, 2005Date of Patent: December 26, 2006Assignee: Medicinova, Inc.Inventors: Kenneth Walter Locke, David Gregory Roe
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Patent number: 7084177Abstract: The present invention relates to a reduced particle size form of the compound (S)-2-ethoxy-3-[4-(2-{4-methanesulfonyloxyphenyl}ethoxy)phenyl]propanoic acid, as shown in formula (I), or a pharmaceutically acceptable salt thereof or a solvate of either thereof. The invention also concerns methods of treating one or more conditions associated with Insulin Resistance Syndrome using the reduced particle size form of the compound, or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in one or more of said conditions. The invention further concerns pharmaceutical compositions containing the reduced particle size form of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof, as an active ingredient, as well as processes for the manufacture of the reduced particle size form of the compound, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 29, 2000Date of Patent: August 1, 2006Assignee: Astrazeneca ABInventors: Agneta Hallgren, Kristina Roos
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Patent number: 6992215Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-? activity, inhibiting angiogenesis, and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.Type: GrantFiled: October 7, 2004Date of Patent: January 31, 2006Assignee: Guildford Pharmaceuticals Inc.Inventors: Takashi Tsukamoto, Pavel Majer, Doris Stoermer, Barbara S. Slusher
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Patent number: 6984663Abstract: Novel sulphones of formula I are disclosed: The compounds modulate the processing of amyloid precursor protein by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.Type: GrantFiled: August 20, 2002Date of Patent: January 10, 2006Assignee: Merck Sharp & Dohme LimitedInventors: Ian Churcher, Kevin Dinnell, Timothy Harrison, Sonia Kerrad, Alan John Nadin, Paul Joseph Oakley, Duncan Edward Shaw, Martin Richard Teall, Susannah Williams, Brian John Williams
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Patent number: 6884907Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-? activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.Type: GrantFiled: May 10, 2002Date of Patent: April 26, 2005Assignee: Guilford Pharmaceuticals Inc.Inventors: Takashi Tsukamoto, Pavel Majer, Bunda Hin, Weizheng Xu, Qun Liu, Doris Stoermer
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Publication number: 20040236146Abstract: A process is described for preparing 3-bromomethylbenzoic acids of the formula II 1Type: ApplicationFiled: March 10, 2004Publication date: November 25, 2004Inventor: Hansjorg Lehmann
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Patent number: 6818766Abstract: Bicalutamide and/or its intermediates are made by the use of p-fluorobenzenesulfinic acid salt as a reagent.Type: GrantFiled: October 2, 2002Date of Patent: November 16, 2004Assignee: Synthon BVInventors: Lambertus Thijs, Rolf Keltjens, Gerrit Jan Bouke Ettema
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Patent number: 6806365Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: April 5, 2002Date of Patent: October 19, 2004Assignee: Hoffmann-La Rocher Inc.Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achytharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
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Publication number: 20040176638Abstract: The present invention relates to a new process for the synthesis of racemic and optically active bicalutamide starting from ethyl pyruvate and methyl methacrylate. The present invention discloses processes of preparing bicalutamide intermediates including ethyl-[2-{4-fluorophenyl sulfone}]-2-hydroxy propionate, 1,2-epoxy-2-methyl propionate and 2-hydrox-2-methyl-3-(4-fluorophenylthio)propionic acid. The present invention further discloses micronized rac-bicalutamide and the preparation thereof.Type: ApplicationFiled: March 8, 2004Publication date: September 9, 2004Inventors: Ben-Zion Dolitzky, Ofer Reany, Jenny Shammai
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Patent number: 6787667Abstract: (E)-styryl benzylsulfones of formula I are useful as anticancer agents: wherein R1, R2, R3, and R4 are independently selected from the group consisting of hydrogen, fluoro, chloro, iodo, bromo, C1-C6 alkyl, C1-C4 alkoxy, nitro, cyano and trifluoromethyl, with the proviso that (a) R1, R2 , and R3 not all hydrogen when R4 is 2-chloro or 4-chloro; (b) when R1 and R3 are hydrogen and R2 is 4-bromo or 4-chloro, then R4 may not be 4-chloro, 4-fluoro or 4-bromo; (c) when R1 and R3 are hydrogen and R2 is 4-fluoro, then R4 may not be 4-fluoro or 4-bromo, (d) when R1 is hydrogen, and R4 is 2-fluoro, the R2 and R3 may not be 4-fluoro; and (e) when R1 is hydrogen and R3 is 4-hydrogen, 4-chloro, 4-bromo, 4-methyl or 4-methoxy, and R4 is 2-hydrogen, 2-chloro, or 2-fluoro; then R2 may not be 4-hydrogen, 4-chloro, 4-fluoro, or 4-bromo.Type: GrantFiled: June 16, 2003Date of Patent: September 7, 2004Assignee: Temple University - of the Commonwealth System of Higher EducationInventors: E. Premkumar Reddy, M. V. Ramana Reddy
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Publication number: 20040171872Abstract: A method for removing impurities from 2-nitro-4-methylsulfonylbenzoic acid which comprises at least two of the following steps, in any order, (a) dissolving 2-nitro-4-methylsulfonylbenzoic acid in water at a pH of about 2 to 10, followed by filtration; (b) contacting an aqueous solution of 2-nitro-4-methylsulfonylberizoic acid with activated carbon at a pH of about 2 to 10; (c) treating an aqueous solution of 2-nitro-4-methylsulfonylbenzoic acid with sufficient base to hydrolyze undesired nitro and dinitro substituted impurities; followed by maintaining the resulting aqueous solution comprising 2-nitro-4-methylsulfonylbenzoic acid at a temperature of up to about 95° C., and adjusting the pH of said solution to about a pH which is sufficient to effect crystallization of 2-nitro-4-methylsulfonylbenzoic acid upon cooling.Type: ApplicationFiled: April 9, 2004Publication date: September 2, 2004Inventors: Kambiz Javdani, Gilbert Rodriguez, James Peter Muxworthy
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Patent number: 6777442Abstract: The present invention relates to compounds of the general formula (I) in which X represents O, S, SO, SO2, CH2, CHF, CF2 or NR8, and Z represents a group of the formula in which A represents O or S, the subscript “a” is 0 or 1, group D represents a straight-chain (C1-C4)-alkylene group, and R36 represents OR37 or NR38R39. It also relates to processes for preparation of such compounds and to their use in medicaments for the treatment of depression, goiter, cancer of the thyroid gland, arteriosclerosis, hypercholesterolaemia, dyslipidaemia, obesity, cardiac insufficiency, pulmonary emphysema, pain, migraine, Alzheimer's disease, osteoporosis, cardiac arrhythmias, hypothyroidism, skin disorders or diabetes.Type: GrantFiled: February 26, 2002Date of Patent: August 17, 2004Assignee: Bayer AktiengesellschaftInventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Christiane Faeste, Hilmar Bischoff, Axel Kretschmer, Verena Vöhringer, Peter Ellinghaus
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Patent number: 6750252Abstract: The present invention relates to certain tri-substituted phenyl derivatives and analogues of formula (I), to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: November 13, 2002Date of Patent: June 15, 2004Assignee: AstraZeneca ABInventors: Maria Boije, Jonas Fägerhag, Eva-Lotte Lindstedt Alstermark, Bengt Ohlsson
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Patent number: 6747170Abstract: A thermosensitive recording material has a support and a thermosensitive coloring layer formed thereon containing a leuco dye and a color developer capable of inducing color formation in the leuco dye upon application of heat thereto, with the color developer including at least one compound (A) having in a molecule thereof at least two aromatic ring moieties with specific structures, selected from the group consisting of an aromatic ring moiety having at least one carboxyl group and electron-attracting functional group, an aromatic ring moiety having at least one carboxyl group and electron-donating functional group, and an aromatic ring moiety having at least one carboxyl group, free of the electron-attracting and electron-donating functional groups. An aromatic carboxylic acid compound serving as the above-mentioned compound (A) and the producing method thereof are also disclosed.Type: GrantFiled: May 23, 2002Date of Patent: June 8, 2004Assignee: Ricoh Company, Ltd.Inventors: Kunio Hayakawa, Mitsunobu Morita
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Publication number: 20040029963Abstract: The use of pamoic acid or of one of its derivatives is described with general formula (I), in which groups R1 and R5 are as indicated in the description, or of one of their pharmaceutically acceptable salts, for the preparation of a medicament for the treatment of diseases characterised by deposits of amyloid aggregates.Type: ApplicationFiled: January 31, 2003Publication date: February 12, 2004Inventors: Maria Grazia Gallo, Maria Grazia Cima, Fabrizio Giorgi, Maria Ornella Tinti, Paola Piovesan, Orlando Ghirardi
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Patent number: 6677473Abstract: Compounds and pharmaceutical compositions useful as plasminogen activator inhibitor (PAI) antagonists are provided. In particular, methods of antagonizing PAI with substituted and unsubstituted aryl and heteroaryl ethers and thioethers, benzils, benzyl ethers, benzoate esters, sulfones and benzophenones are provided.Type: GrantFiled: November 17, 2000Date of Patent: January 13, 2004Assignee: Corvas International INCInventors: Edwin L. Madison, Terence K. Brunck, Joseph Edward Semple, Marguerita Lim-Wilby, Kent E. Pryor, Ronald D. Lewis, II, David F. Duncan, C. Maxwell Lawrence
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Publication number: 20030220517Abstract: A novel process affords &ohgr;-ketocarboxylic acid derivatives of the formula (I) 1Type: ApplicationFiled: March 14, 2003Publication date: November 27, 2003Inventor: Albrecht Marhold
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Publication number: 20030216535Abstract: (E)-styryl benzylsulfones of formula I are useful as anticancer agents: 1Type: ApplicationFiled: June 16, 2003Publication date: November 20, 2003Applicant: Temple University - Of The Commonwealth System of Higher EducationInventors: E. Premkumar Reddy, M.V. Ramana Reddy
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Patent number: 6630600Abstract: Novel 3-aryl propionic acid derivatives and analogs, process and intermediate for their manufacture, pharmaceutical preparations containing them and the use of the compounds in clinical conditions associated with insulin resistance.Type: GrantFiled: July 20, 1999Date of Patent: October 7, 2003Assignee: AstraZeneca ABInventors: Kjell Andersson, Maria Boije, Johan Gottfries, Tord Inghardt, Lanna Li, Eva-Lotte Lindstedt Alstermark
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Publication number: 20030187033Abstract: The present invention is related to anthranilamides of formula I, 1Type: ApplicationFiled: April 26, 2002Publication date: October 2, 2003Inventors: Joachim Brendel, Bernard Pirard, Stefan Peukert, Heinz-Werner Kleemann, Horst Hemmerle
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Patent number: 6624152Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.Type: GrantFiled: August 22, 2001Date of Patent: September 23, 2003Assignee: Biogen, Inc.Inventors: Steven P. Adams, Ko-Chung Lin, Wen-Cherng Lee, Alfredo C. Castro, Craig N. Zimmerman, Charles E. Hammond, Yu-Sheng Liao
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Publication number: 20030149109Abstract: Pre-treatment with &agr;,&bgr; unsaturated aryl sulfones protects normal cells from the cytotoxic side effects of two classes of anticancer chemotherapeutics. Administration of a cytoprotective sulfone compound to a patient prior to anticancer chemotherapy with a mitotic phase cell cycle inhibitor or topoisomerase inhibitor reduces or eliminates the cytotoxic side effects of the anticancer agent on normal cells. The cytoprotective effect of the &agr;,&bgr; unsaturated aryl sulfone allows the clinician to safely increasing the dosage of the anticancer chemotherapeutic.Type: ApplicationFiled: November 27, 2002Publication date: August 7, 2003Inventors: Stephen C. Cosenza, M. V. Ramana Reddy, E. Premkumar Reddy
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Patent number: 6590119Abstract: The invention relates to improved methods of producing aryl dioxoalkanoic acid compounds and derivatives useful as intermediates for diarylpyrrole therapeutic agents by the alcoholysis of benzoylcyclohexanone ketal compounds.Type: GrantFiled: November 7, 2001Date of Patent: July 8, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Michael P. Ferro, Kathleen A. McCoy
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Patent number: 6586623Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.Type: GrantFiled: January 17, 2002Date of Patent: July 1, 2003Assignee: Guilford Pharmaceuticals Inc.Inventors: Takashi Tsukamoto, Pavel Majer, Doris Stoermer, Barbara S. Slusher
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Patent number: 6562807Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism, such as dyslipidemia, and obesity.Type: GrantFiled: June 22, 2001Date of Patent: May 13, 2003Assignee: Novo Nordisk A/SInventors: Anker Steen Jorgensen, Inge Thoger Christensen, Janos Tibor Kodra, Christian Sams, Carsten Behrens, Peter Madsen, Jesper Lau
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Publication number: 20030045741Abstract: The present invention relates to a new process for the synthesis of racemic and optically active bicalutamide starting from ethyl pyruvate and methyl methacrylate. The present invention discloses processes of preparing bicalutamide intermediates including ethyl-[2-{4-fluorophenyl sulfone}]-2-hydroxy propionate, 1,2-epoxy-2-methyl propionate and 2-hydrox-2-methyl-3-(4-fluorophenylthio)propionic acid. The present invention further discloses micronized rac-bicalutamide and the preparation thereof.Type: ApplicationFiled: June 13, 2002Publication date: March 6, 2003Inventors: Ben-Zion Dolitzky, Ofer Reany, Jenny Shammai
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Patent number: 6525093Abstract: Compounds are provided that lower blood glucose concentrations, lower serum triglyceride concentrations, lower systolic blood pressure, and increase glucose uptake by adipose tissue, but do not affect the expression of PPAR-&ggr; by adipose tissue.Type: GrantFiled: November 8, 1999Date of Patent: February 25, 2003Assignee: Calyx Therapeutics Inc.Inventors: Partha Neogi, Bishwajit Nag, Frederick J. Lakner, Debendranath Dey, Satyanarayana Medicherla
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Publication number: 20030036536Abstract: Styryl benzylsulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: 1Type: ApplicationFiled: July 29, 2002Publication date: February 20, 2003Inventors: E. Premkumar Reddy, M.V. Ramana Reddy
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Patent number: 6495546Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.Type: GrantFiled: November 22, 2000Date of Patent: December 17, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Publication number: 20020133030Abstract: This invention provides processes for the preparation of a compound of Formula I:Type: ApplicationFiled: May 8, 2002Publication date: September 19, 2002Applicant: Syntex USA, LLCInventors: Jeffrey Allen Campbell, Lawrence Emerson Fisher, Charles Alois Dvorak, Paul Leo McGrane
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Publication number: 20020115643Abstract: Styryl benzylsulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: 1Type: ApplicationFiled: April 12, 2001Publication date: August 22, 2002Inventors: E. Premkumar Reddy, M. V. Ramana Reddy
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Patent number: 6376546Abstract: Compounds represented by general formula I or salts thereof, wherein n is an integer of 2 or 3; R represents a straight-chain or branched saturated alkyl group having 4 or 4 carbon atoms, a cyclopentyl group, a cyclohexyl group or the like, Y represents a hydroxyl or amino group, A represents a hydrogen atom, a hydroxyl, methoxy, nitro group or the like, Q represents a hydrogen atom or a hydroxyl or methoxy group. They can be formulated to give pharmaceutical compositions that are effective as prophylactic or therapeutic agents for allergic diseases associated with IgE production inhibitors or IgE antibodies.Type: GrantFiled: June 8, 2000Date of Patent: April 23, 2002Assignee: Asahi Kasei Kabushiki KaishaInventors: Motoshi Shoda, Hiromichi Itoh
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Patent number: 6369261Abstract: Compounds having Formula 2 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: April 9, 2002Assignee: Allergan Sales, Inc.Inventors: Alan T. Johnson, Jayasree Vasudevan, Liming Wang, Roshantha A. Chandraratna
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Patent number: 6365625Abstract: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalenesulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.Type: GrantFiled: September 17, 1999Date of Patent: April 2, 2002Assignee: Procept, Inc.Inventors: Shyam K. Singh, Raymond J. Patch, Peter V. Pallai, Edith A. Neidhardt, Gerard P. Palace, Kevin J. Willis, Theresa M. Sampo, Kevin W. McDonald, Zhan Shi
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Publication number: 20020038037Abstract: This invention provides processes for the preparation of a compound of Formula I:Type: ApplicationFiled: November 9, 2001Publication date: March 28, 2002Applicant: Syntex (U.S.A.) Inc.Inventors: Jeffrey Allen Campbell, Lawrence Emerson Fisher, Charles Alois Dvorak, Paul Leo McGrane
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Patent number: 6355836Abstract: An isomerization process of trans-5-fluoro-2-methyl-1-[p-(methylthio)benzyliden]inden-3-acetic acid for the treatment of sodium salt in methanol and in the presence of a base at 70±2° C. is described.Type: GrantFiled: October 3, 2000Date of Patent: March 12, 2002Assignee: Zambon Group S.p.A.Inventors: Giuseppe Barreca, Vincenzo Cannata
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Patent number: 6337306Abstract: Phenoxyacetic acid derivatives of the formula: wherein R1, R2, Xn and A are as defined herein, and a process for preparing the derivatives. The derivatives are used as herbicides.Type: GrantFiled: November 5, 1999Date of Patent: January 8, 2002Assignee: Rhone-Poulenc AgroInventors: Norio Sasaki, Atsushi Go, Hideshi Mukaida, Yukiko Oe
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Publication number: 20010034371Abstract: A novel 3-aryl-2-hydroxypropionic acid derivative, a process and intermediate for its manufacture, pharmaceutical preparations containing it and the use of the compound in clinical conditions associated with insulin resistance.Type: ApplicationFiled: May 18, 2001Publication date: October 25, 2001Inventor: Kjell Andersson
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Patent number: 6306873Abstract: This invention relates to compounds of general formula (I): in which Ar is a group selected from: A1, A2, B, C, D, E, Q1-Q3, R1-R9, Z1 and Z2 are as defined in the disclosure, and Y represents carboxy or an acid bioisostere. These compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.Type: GrantFiled: July 20, 1999Date of Patent: October 23, 2001Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Christopher J. Burns, Richard Labaudiniere, Stephen Condon, Robert D. Groneberg, Rose M. Mathew, Joseph M. Salvino
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Patent number: 6306840Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.Type: GrantFiled: January 23, 1995Date of Patent: October 23, 2001Assignee: Biogen, Inc.Inventors: Steven P. Adams, Ko-Chung Lin, Wen-Cherng Lee, Alfredo C. Castro, Craig N. Zimmerman, Charles E. Hammond, Yu-Sheng Liao
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Patent number: RE38921Abstract: Phenoxyalkylcarboxylic acid derivative represented by the following formula, wherein R1 indicates hydrogen atom, methyl group or ethyl group, m is an integer from 2 to 5, and n is an integer from 3 to 8, X1 and X2 each independently represent sulfur atom, oxygen atom, sulfinyl group or sulfonyl group, proviso X1 and X2 are not simultaneously oxygen atom; their alkali salts and hydrates thereof are useful as antiallergic agents.Type: GrantFiled: July 21, 2003Date of Patent: December 13, 2005Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Mitsuo Ohashi, Katsuya Awano, Toshio Tanaka, Tetsuya Kimura