Abstract: The present invention relates to a method of modulating retinoid X receptor activity in a mammal, novel compounds and pharmaceutical compositions for modulating retinoid X receptor activity in a mammal, and methods of making compounds that modulate retinoid X receptor activity in a mammal. The compounds are represented by Structural Formula 1: The compounds of Structural Formual 1 are efficacious insulin sensitizers and do not have the undesirable side effects of increasing triglycerides or suppressing the thyroid hormone axis.
Type:
Application
Filed:
April 15, 2004
Publication date:
December 9, 2004
Inventors:
Michael Gregory Bell, Timothy Alan Grese, Douglas Linn Gernett, Nathan P. Yumibe, Marcus F. Boehm, Pierre-Yves Michellys, Robert J. Ardecky, Christopher M Mapes, Jyun-Hung Chen, John S. Tyhonas, Lawrence G. Hamann
Abstract: 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:
Application
Filed:
October 2, 2003
Publication date:
November 18, 2004
Inventors:
Kjell Andersson, Maria Boije, Johan Gottfries, Tord Inghardt, Lanna Li, Eva-Lotte Lindstedt Alstermark
Abstract: The present invention provides a phthalate-free plasticizer for polymer resins. The phthalate-free plasticizer according to the invention includes a mixture of different triesters of glycerin, at least one of which meets the formula:
CH2(OOR1)CH(OOR2)CH2(OOR3)
wherein at least two of R1, R2, and R3 are different alkyl or aryl groups. Phthalate-free plasticizers according to the invention can be made by esterifying glycerin with a mixture of acids in the presence of a catalyst. Preferably, the mixture of acids includes at least two selected from the group consisting of alkyl acids and aryl acids, with each acid in the mixture containing up to about 11 carbon atoms, and more preferably from about 4 to about 9 carbon atoms each. The plasticizer according to the invention can be used to modify the properties of a wide variety of polymers including vinyl polymers, rubbers, polyurethanes, and acrylics, and has superb thermostability and low volatility.
Type:
Grant
Filed:
October 10, 2003
Date of Patent:
November 2, 2004
Assignee:
Ferro Corporation
Inventors:
Lei Zhou, George Schaefer, William W. Knickmeyer, David Paul
Abstract: This invention relates to preparation of enantio-enriched compounds, and more particularly to enantio-enriched kavalactone compounds and derivatives thereof. The methods provide compounds that are useful as reagents, or building blocks, in the construction of other enantio-enriched compounds.
Abstract: The present invention provides a process for the preparation of homophthlate esters useful in the preparation of homophthalic anhydride reactants.
Type:
Grant
Filed:
July 28, 2003
Date of Patent:
September 28, 2004
Assignee:
Ilex Products, Inc.
Inventors:
William E. Bauta, William R. Cantrell, Jr., Dennis P. Lovett
Abstract: The present invention relates to production of 2-cyclohexyl-2-hydroxy-2-phenylacetic acid useful as an intermediate for pharmaceutical products, by an industrial means, economically, safely in a good yield. Novel 2-(2′-cyclohexen-1′-yl)-2-hydroxy-2-phenylacetic acid ester obtained by reacting cyclohexene and benzoylformic acid ester in the presence of a Lewis acid is hydrolyzed and reduced to give 2-cyclohexyl-2-hydroxy-2-phenylacetic acid.
Abstract: A ferulic acid derivative represented by the general formula (1); a process for preparing a ferulic acid derivative represented by the general formula (1), comprising reacting ferulic acid or an ester thereof represented by the general formula (2) with a dihalomethane represented by the general formula CH2X2, wherein X is a halogen atom; and an ultraviolet light-absorbent composition comprising the ferulic acid derivative. Since the ultraviolet light absorbent composition is not only excellent in the ultraviolet light absorption but also very stable against heat, the ultraviolet light absorbent composition can be suitably used as cosmetics which especially require long-term stability.
Abstract: Compounds of the formula
where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effect of reducing serum thyroxine levels.
Type:
Grant
Filed:
February 4, 2003
Date of Patent:
July 6, 2004
Assignee:
Allergan, Inc.
Inventors:
Jayasree Vasudevan, Richard L. Beard, Haiqing Yuan, Roshantha A. Chandratratna
Abstract: Compounds of formula I:
wherein the variables are defined as explained in the disclosure. The invention also provides liquid crystalline mixtures and optical or electro-optical devices including compounds of formula (I).
Type:
Grant
Filed:
October 17, 2001
Date of Patent:
June 8, 2004
Assignee:
Rolic AG
Inventors:
Zoubair Mohammed Cherkaoui, Carsten Benecke, Klaus Schmitt
Abstract: The present invention provides a phthalate-free plasticizer for polymer resins. The phthalate-free plasticizer according to the invention includes a mixture of different triesters of glycerin, at least one of which meets the formula:
CH2(OOR1)CH(OOR2)CH2(OOR3)
wherein at least two of R1, R2, and R3 are different alkyl or aryl groups. Phthalate-free plasticizers according to the invention can be made by esterifying glycerin with a mixture of acids in the presence of a catalyst. In the presently most preferred embodiment of the invention, the mixture of acids includes benzoic acid and butanoic acid. The plasticizer according to the invention can be used to modify the properties of a wide variety of polymers including vinyl polymers, rubbers, polyurethanes, and acrylics, and has superb thermostability and low volatility.
Abstract: Polysubstituted indan-1-ol compounds of formula I, its physiologically acceptable salts and physiologically functional derivatives are disclosed 1
Type:
Application
Filed:
October 27, 2003
Publication date:
May 13, 2004
Applicant:
Aventis Pharma Deutschland GmBH
Inventors:
Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
Abstract: Novel acetyloxymethyl esters are disclosed. Methods of treating an illness, including cancer, hemological disorders and inherited metabolic disorders, and treating or ameliorating other conditions using these compounds are also disclosed. The compounds are effective in the inhibition of histone deacetylase.
Type:
Grant
Filed:
December 21, 2000
Date of Patent:
April 13, 2004
Assignee:
Beacon Laboratories, Inc.
Inventors:
Hsuan-Yin Lan-Hargest, Norbert L. Wiech
Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
Type:
Application
Filed:
July 29, 2003
Publication date:
February 12, 2004
Inventors:
Douglas Wade Beight, Trelia Joyce Craft, Carl Penman Denny, Jeffry Bernard Franciskovich, Theodore Goodson, Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milet, Marta Maria Pinelro-Nunez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
Abstract: The present invention provides a novel diamine and a novel acid anhydride which are applicable for a polyimide and includes a cinnamoyl group or a derived cinnamoyl group. The novel diamines and acid anhydrides have photo-reactivity and heat-reactivity inherent to the cinnamoyl group.
Abstract: The invention relates to a method of producing alkoxycinnamic acid ester (alkoxy cinnamate) by condensing C5-C8 acetic acid esters with C1-C4 alkoxybenzaldehyde in the presence of an alkaline and/or alkaline earth C1-C4 alcohalate and removing the C1-C4 alcohol that is produced by this reaction from the reaction mixture.
Type:
Grant
Filed:
November 16, 2001
Date of Patent:
January 20, 2004
Assignee:
Symrise GmbH & Co. KG
Inventors:
Walter Kuhn, Werner Marks, Klaus Zahlmann
Abstract: The present invention relates to novel antiobesity and hypocholesterolemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel &bgr;-aryl-&agr;-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereosomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.
Type:
Grant
Filed:
March 27, 2001
Date of Patent:
December 16, 2003
Assignees:
Dr. Reddy's Laboratories Limited, Reddy-Cheminor Inc.
Abstract: O-medium alkyl esters of diflunisal and related compounds are disclosed having anti-platelet activity, hydroxy radical scavenging properties, enhanced hepatic clearance and low ulcerogenic potential. These compounds have general formula (I) wherein n equals 3-13.
Type:
Application
Filed:
December 27, 2002
Publication date:
November 27, 2003
Applicant:
The University of Queensland
Inventors:
Daniel Yung-Yu Hung, Michael Stephen Roberts
Abstract: The present invention provides a phthalate-free plasticizer for polymer resins. The phthalate-free plasticizer according to the invention includes a mixture of different triesters of glycerin, at least one of which meets the formula:
CH2(OOR1)CH(OOR2)CH2(OOR3)
wherein at least two of R1, R2, and R3 are different alkyl or aryl groups. Phthalate-free plasticizers according to the invention can be made by esterifying glycerin with a mixture of acids in the presence of a catalyst. Preferably, the mixture of acids includes at least two selected from the group consisting of alkyl acids and aryl acids, with each acid in the mixture containing up to about 11 carbon atoms, and more preferably from about 4 to about 9 carbon atoms each. The plasticizer according to the invention can be used to modify the properties of a wide variety of polymers including vinyl polymers, rubbers, polyurethanes, and acrylics, and has superb thermostability and low volatility.
Type:
Grant
Filed:
December 20, 2001
Date of Patent:
November 25, 2003
Assignee:
Ferro Corporation
Inventors:
Lei Zhou, George Schaefer, William W. Knickmeyer, David Paul
Abstract: A method for transferring amino acid into ketone acid (ester) may obtain ketone acid (ester) at low cost. The method uses sodium hypochlorous acid as oxidizing agent and proceeds oxidation reaction with amino acid or its derivatives so as to obtain ketone acid and its derivatives. The sodium hypochlorous acid is easily to get with low cost and the conditions of the reaction are mild so that the method meets the needs of the industry.
Abstract: 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 are provided.
Type:
Grant
Filed:
November 19, 1999
Date of Patent:
October 28, 2003
Assignee:
Corvas International, Inc.
Inventors:
Edwin L. Madison, Terence K. Brunck, Joseph Edward Semple, Marguerita Lim-Wilby, Kent E. Pryor
Abstract: The present invention provides a process for preparing optically active &agr;-hydroxy acids and derivatives thereof by subjecting the alkylated 1,3-dioxolanones of formula (IV) wherein R1 and R2 are the same or different and are each independently H or C1-6 alkyl; R5 is H, C1-16 alkyl, or unsubstituted or substituted phenyl; and R6 is C1-8 alkyl, C2-7 alkenyl or unsubstituted or substituted benzyl, to either alcoholysis or hydrolysis, in which the alkylated 1,3-dioxolanones are obtained by using 10-camphorsulfonamide as a chiral auxiliary.
Type:
Grant
Filed:
October 8, 2002
Date of Patent:
October 28, 2003
Inventors:
Biing-Jiun Uang, Jia-Wen Chang, Der-Pin Jang
Abstract: 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:
Grant
Filed:
July 20, 1999
Date of Patent:
October 7, 2003
Assignee:
AstraZeneca AB
Inventors:
Kjell Andersson, Maria Boije, Johan Gottfries, Tord Inghardt, Lanna Li, Eva-Lotte Lindstedt Alstermark
Abstract: This invention encompasses a method for the treatment or prevention of prostaglandin mediated diseases comprising administering to a mammalian patient a compound of formula I:
in an amount that is effective to treat or prevent said prostaglandin mediated disease. Novel compounds are also disclosed.
Type:
Grant
Filed:
April 24, 2001
Date of Patent:
September 30, 2003
Inventors:
Michel Gallant, Nicolas Lachance, Marc Labelle, Robert Zamboni, Helene Juteau, Yves Gareau, Patrick Lacombe
Abstract: Disclosed is a novel process for the preparation of the anti-glaucoma drug Latanoprost, in good yield, in large amounts and with desired purity. Also disclosed are novel intermediates for the above process.
Type:
Application
Filed:
October 25, 2002
Publication date:
August 7, 2003
Inventors:
Arie Gutman, Gennadiy Nisnevich, Marina Etinger, Igor Zaltzman, Lev Judovich, Boris Pertsikov
Abstract: A compound of formula I
wherein
A is a moiety which provides UV absorbing activity to the compound of formula I that comprises 1 divalent group or 2 monovalent groups, with at least one group having carbonyl (C═O) functionality, and each R is independently linear or branched C1-C8 alkyl. Sunscreen formulations which contain these compounds and methods using these compounds to prepare formulations are also provided.
Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR&dgr; suptype.
Type:
Application
Filed:
July 19, 2002
Publication date:
July 24, 2003
Inventors:
Lone Jeppesen, Paul Stanley Bury, John Patrick Mogensen, Ingrid Pettersson, Per Sauerberg
Abstract: Chiral diphosphines constituted by an aromatic pentatomic biheterocyclic system, suitable to act as chiral ligands, complexes between said diphosophines and transition metals, and their utilization as chiral catalysts in sterocontrolled reactions, such as diastereo- and enantioselective reduction reactions. Process for the preparation of said chiral diphosophines and process for the preparation of said complexes and for their utilization as chiral catalysts in sterocontrolled reactions.
Abstract: The present invention relates to compounds of formula (I)
The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
Type:
Grant
Filed:
January 26, 2001
Date of Patent:
May 27, 2003
Assignee:
Novo Nordisk A/S
Inventors:
John Patrick Mogensen, Per Sauerberg, Paul Stanley Bury, Lone Jeppesen, Ingrid Pettersson
Abstract: This invention relates to derivatives of acrylic acid useful as fungicides, to processes for preparing them, to fungicidal compositions containing them, and to methods of combating fungi, especially fungal infections in plants, using them.
Type:
Grant
Filed:
October 11, 1985
Date of Patent:
May 20, 2003
Assignee:
Zeneca Limited
Inventors:
Michael J Bushell, Kevin Beautement, John M Clough, Vivienne M Anthony, Paul deFraine, Christopher R Godfrey
Abstract: The present invention relates to an improved process for the preparation of 3-aryl-2-hydroxy propanoic acid derivatives of the formula (1)
useful as an intermediate for the preparation of many pharmaceutically active compounds.
Abstract: An improved light attenuating compound for use in the production of microdevices is provided. Broadly, the light attenuating compound is difunctional and can be directly incorporated (either physically or chemically) into photolithographic compositions such as anti-reflective coatings (ARC) and contact or via hole fill materials. The preferred light attenuating compound comprises functional groups electronically isolated from the light absorbing moieties of the compound. As a result, the spectral properties of the compound are not negatively affected when the functional groups form bonds with other compounds during polymerization or crosslinking.
Abstract: An accelerated process for preparing an O-methyl phenol comprising reacting a phenol with dimethyl carbonate in the presence of a catalyst selected from 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and dimethylaminopyridine. According to another aspect, the invention provides an accelerated process for preparing an N-methyl heteroaromatic compound comprising reacting an NH-containing heteroaromatic compound with dimethyl carbonate in the presence of a catalyst selected from 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and dimethylaminopyridine. According to an additional aspect, the invention provides an accelerated process for preparing a methylated aminophenol comprising reacting an aminophenol having at least one N—H with dimethyl carbonate in the presence of a catalyst selected from 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and dimethylaminopyridine.
Abstract: 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:
Grant
Filed:
November 8, 1999
Date of Patent:
February 25, 2003
Assignee:
Calyx Therapeutics Inc.
Inventors:
Partha Neogi, Bishwajit Nag, Frederick J. Lakner, Debendranath Dey, Satyanarayana Medicherla
Abstract: Compounds of the formula (I) and their physiologically acceptable salts and solvates are useful as integrin-inhibiting substances. They are especially useful in the prophylaxis and treatment of cardiovascular disorders, of thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, osteoporosis, in pathological conditions that are caused or propagated by angiogenesis and in tumor therapy.
Type:
Grant
Filed:
October 15, 2001
Date of Patent:
February 18, 2003
Assignee:
Merck Patent GmbH
Inventors:
Wolfgang Stähle, Rudolf Gottschlich, Simon Goodman
Abstract: HIV protease inhibitors inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds can be prepared by the novel methods of the present invention using the novel inventive compounds and intermediates.
Abstract: The invention provides LC compositions that exhibit V-shaped switching when aligned in an analog device configuration and exhibit bistability when aligned in a bookshelf-type device configuration. The invention more specifically provides LC compositions of formula 1 and particularly chiral nonracemic compounds of formula 1 which exhibit bistable switching as well as V-shaped switching when aligned in appropriate device configurations. The invention also provides methods of using the compounds of the invention in making LC compositions and electooptical devices comprising an aligned layer of the compositions of this invention.
Abstract: Ibuprofen-aspirin compounds useful in treating aspirin or ibuprofen-treatable conditions, hydroxymethylacylfulvene analogs useful as antitumor drugs, and L-sugar illudin analogs useful as antitumor drugs.
Abstract: A novel fatty polypropoxylate ester which is an ester of an aliphatic or an aromatic monoacid formed by reacting the acid with a stoichiometric excess of a polypropoxylated fatty alcohol.
Type:
Application
Filed:
February 26, 2002
Publication date:
December 19, 2002
Inventors:
Ronald J. Smith, Maria K. Smith, Sayer B. Needelman, G. Frank DeMonico
Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below.
The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
Type:
Grant
Filed:
January 25, 2001
Date of Patent:
December 17, 2002
Assignee:
Warner-Lambert Company
Inventors:
Lain-Yen Hu, Michael Francis Rafferty, Todd Robert Ryder
Abstract: A malic acid or oxalacetic acid derivative is represented by the following formula (1):
wherein ring Z is an alicyclic carbon ring; each of Ra and Rb is independently a hydrogen atom, a metal atom, or an organic group; and Y is a hydroxyl group or an oxygen atom, where ring Z is a bridged carbon ring or a monocyclic carbon ring having eight or more members when Y is an oxygen atom. The alicyclic carbon ring includes, for example, cyclooctane ring and adamantane ring. This compound is a novel malic acid derivative having an alicyclic group bonded to a carbon atom at the 3-position, or a novel oxalacetic acid derivative having a specific alicyclic group bonded to a carbon atom at the 3-position.
Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.
Abstract: Novel thyroid receptor ligands are provided which have the general formula (I)
where R1 is alkyl of 1 to 4 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 3 carbons or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen; n is an integer from 0 to 4; R4 is an aliphatic hydrocarbon, an aromatic hydrocarbon, carboxylic acid ester thereof, alkenyl carboxylic acid or ester thereof, hydroxy, halogen, cyano, or a phosphonic acid or an ester thereof, or a pharmaceutically acceptible salt thereof. A method for treating diseases associated with metabolism dysfunction or which are dependent on the expression of a T3 regulated gene, such as obesity, hypercholesterolemia, osteoporosis, hypothyroidism, and goiter, is also provided.
Type:
Grant
Filed:
March 20, 2000
Date of Patent:
October 15, 2002
Assignee:
Karo Bio AB
Inventors:
Yi-Lin Li, Ye Liu, Asa Hedfors, Johan Malm, Charlotta Mellin, Minsheng Zhang
Abstract: The present invention relates to a process for the production of perfuming compositions, to perfumed products, and to products obtained therefrom. More specifically, the present invention concerns a process for the production of perfuming compositions, perfumed products and substances for perfumery characterized in that they comprise, as an active ingredient with an influence on the scent, an effective quantity of an alkylsalicylic acid ester.
Abstract: The invention relates to substituted cinnamic acids and cinnamic acid esters of formula (I), wherein X represents F, Cl or J and R1 and R2 are the same or different and represent hydrogen, an optionally substituted C1-C10-alkyl radical or an optionally substituted benzyl radical. Substituted indanone carboxylic acid esters are produced using said substituted cinnamic acid and cinnamic acid ester in a technically simple and non-dangerous manner as far as safety is concerned.
Type:
Grant
Filed:
February 13, 2001
Date of Patent:
September 24, 2002
Assignee:
Bayer Aktiengesellschaft
Inventors:
Walter Lange, Joachim Komoschinski, Guido Steffan, Ernst Kysela