Abstract: A process for extracting oleanolic acid from plant material is disclosed. Dried plant material is provided and an extraction process is carried out with a non-halogenated polar to medium polar solvent. The resulting solution that contains oleanolic acid is separated from the plant material and the solvent is removed using cooling, vacuum-evaporation or other techniques. A precipitate is formed that contains mostly oleanolic acid. Subsequent purification steps to provide highly purified oleanolic acid include washing techniques, re-crystallization techniques or the use of chromatography.
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:
January 28, 2002
Date of Patent:
March 2, 2004
Assignee:
Beacon Laboratories, Inc.
Inventors:
Hsuan-Yin Lan-Hargest, Norbert L. Wiech
Abstract: The present invention provides methods of making 21-[4′-(nitrooxyalkyl)benzoate] corticosteroid derivatives according to the following general reaction scheme:
The invention also provides intermediates useful in making such 21-[4′-(nitrooxyalkyl)benzoate] corticosteroid derivatives as well as methods for making such intermediates.
Abstract: The present invention relates to a new microbial process for the preparation of the compound formula (I)
from a compound of general formula (II)
wherein R stands for an alkali metal or ammonium ion, by the submerged cultivation of a mold strain able to 6&bgr;-hydroxylate a compound of the Formula (II) in aerobic fermentation and by the separation and purification of the product of Formula (I) formed in the course of the bioconversion. The process comprises cultivating a strain of Mortierella maculata filamentous mold species that is able to 6&bgr;-hydroxylate a compound of the general Formula (II), on a nutrient medium containing assimilable carbon and nitrogen sources and mineral salts and separating the product formed from the fermentation broth, then isolating the compound of formula (I) and purifying the same. Novel strains of Mortierella maculata are also disclosed.
Type:
Grant
Filed:
May 14, 2003
Date of Patent:
February 24, 2004
Assignee:
Institute for Drug Research, Ltd.
Inventors:
Antonia Jekkel, Attila Konya, Istvan Barta, Eva Ilkoy, Gyorgy Somogyi, Gabor Ambrus, Gyula Horvath, Karoly Albrecht, Istvan Szabo, Julianna Mozes Nee Suto, Janso Salat, Attila Andor, Laszlo Birincsik, Sandor Boros, Ildiko Lang, Margit Bidlo Nee Igloy
Abstract: The present invention relates to metathesis syntheses for insect sex-attractant pheromones or their components, such as E-5-decenyl acetate, the major component of the Peach Twig Borer pheromone; (5R,6S)-6-acetoxy-5-hexadecanolide, the mosquito oviposition attractant pheromone; E9,Z11-hexadecadienal, the pecan nut casebearer moth pheromone; 9-tetradecenyl formate, an analog of the Diamondback Moth (DBM) pheromone; 11-tetradecenyl acetate, the Omnivorous Leafroller (OLR) pheromone; E-4-tridecenyl acetate, the major component of the Tomato Pinworm (TPW) pheromone; E,E-8,10-dodecadienol, the Codling Moth (CM) pheromone. The syntheses preferably employ a Class I-IV metathesis catalyst, entail few reaction steps, use generally commercially available starting materials, and have relatively short process times. These syntheses produce good yields without the need for expensive or sophisticated equipment.
Abstract: The present invention relates to calcium double salts having good preservative properties. Said salts can be used in foods, feeds, pet food, cosmetics and pharmaceuticals, food-contact items, silage, brewers' spent grains, pomace, food wastes, brewers' yeast, distillation residues and other wastes from the food industry or for leather treatment. These substances exhibit a considerably extended shelf life after addition of, or treatment with, one of the calcium double salts.
Abstract: The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.
Type:
Grant
Filed:
April 19, 2002
Date of Patent:
February 10, 2004
Assignee:
Warner-Lambert Company
Inventors:
Justin Stephen Bryans, David Clive Blakemore, Simon Andrew Osborne, Jean-Marie Receveur
Abstract: This invention provides processes for preparing a group of novel bridged tricyclic compounds having the formula:
wherein X is (CH2)n, O, S, SO, SO2 or CR1R2; n is 1 or 2; and R1 and R2 are, independently, hydrogen, halogen, hydroxy, alkyl of one to six carbon atoms, alkoxy of one to six carbon atoms, or R1 and R2, taken together with the carbon to which they are attached, form cycloalkyl of three to six carbon atoms, an alkylidene of up to six carbon atoms or a carbonyl.
Type:
Grant
Filed:
June 27, 2002
Date of Patent:
February 10, 2004
Assignee:
Wyeth
Inventors:
Alexander Alexei Greenfield, John Anthony Butera
Abstract: This invention provides a process for the preparation of all four stereoisomers of formula I or a pharmaceutically acceptable salt thereof
which may be represented by the following structures:
Type:
Grant
Filed:
June 27, 2002
Date of Patent:
February 10, 2004
Assignee:
Wyeth
Inventors:
Reinhardt Bernhard Baudy, Jean Yi-ching Sze, Jonathan Laird Gross
Abstract: Polyampholytes including fibronectin and aggrecan are made to aggregate and form fibrillar lattice networks environment free of cells, extraneous proteins and other materials which may be present in an extracellular matrix. A composition having sufficient charge density is utilized to cause aggregation and self-assembly of such polyampholytes and to provide an assay for determining the effects of environmental agents on such aggregation and self-assembly.
Type:
Grant
Filed:
March 21, 2001
Date of Patent:
February 3, 2004
Assignee:
The Research Foundation of the State University of New
York
Inventors:
Kenneth J. McLeod, Nadine Pernodet, Miriam Rafailovich
Abstract: The present invention relates to compounds of formula (I)
wherein U, Y, V, W, L, X, A1, A2, A3, A4, A5 and A6 are as defined in the description and claims and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasite infections, gallstones, tumors and/or hyperproliferative disorders, and/or treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
Type:
Grant
Filed:
July 16, 2001
Date of Patent:
January 27, 2004
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Jean Ackermann, Johannes Aebi, Alexander Chucholowski, Henrietta Dehmlow, Olivier Morand, Sabine Wallbaum, Thomas Weller
Abstract: The present invention relates to a production method of (R)-3-hydroxy-3-(2-phenylethyl)hexanoic acid which comprises optical resolution of racemic 3-hydroxy-3-(2-phenylethyl)hexanoic acid with an optically active amine of the formula (VIII)
wherein R2 is 3,4-dimethoxyphenyl or 2-chlorophenyl. According to the present invention, (R)-3-hydroxy-3-(2-phenylethyl)hexanoic acid useful as a starting material of a pharmaceutical agent can be efficiently produced with a high optical purity and a relatively high total yield.
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 invention relates to a continuous method for producing a cross-linked unsaturated fatty acid-based or fatty acid ester-based bonding agent, an elastic bonding agent produced according to said method and the use of said elastic bonding agent.
Abstract: Novel unsaturated esters for use in dentistry as bonding agents are produced by a reaction of a cyclic dianhydride with unsaturated alcohols. The novel unsaturated ester products have the formula:
wherein R2 is H or CH3.
Abstract: A process for monitoring and controlling reactor conditions during the production of acetic acid by the catalyzed carbonylation of methanol is provided. The process of the present invention comprises measuring the density of the heavy phase of the light ends distillation column in the purification system of the carbonylation process. The density measurement is used to adjust the feed of methanol and/or to regulate the temperature in the reaction zone to optimize reactor conditions. The density measurement may also be used to adjust other parameters in the reactor system. The invention is also directed to the system for manufacturing acetic acid based on the process control procedure described.
Type:
Grant
Filed:
January 28, 2002
Date of Patent:
January 13, 2004
Assignee:
Celanese International Corporation
Inventors:
Michael E. Huckman, G. Paull Torrence, Hung-Cheun Cheung
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, benzils, benzyl ethers, benzoate esters, sulfones and benzophenones are provided.
Type:
Grant
Filed:
November 17, 2000
Date of Patent:
January 13, 2004
Assignee:
Corvas International INC
Inventors:
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
Abstract: A method of synthesis of dinitro-diaza-alkanes and intermediate products thereto from alkylamines and esters, whereby a dialkyl ester of a dicarboxylic acid is reacted with an alkylamine in an aqueous medium to form the corresponding dialkyldiamide of the dicarboxylic acid;
the resulting dialkyldiamide is nitrated by means of conventional nitration agents to form the corresponding dialkyldinitroamide of the dicarboxylic acid and;
the resulting dialkyldinitroamide is reacted with methylamine and/or ethylamine in an aquous medium to yield a corresponding alkylnitroamine and the dimethyldiamide and/or diethyldiamide of the dicarboxylic acid, and the alkylnitroamine is isolated from that, and the isolated alkylnitroamine is condensed in a known manner to form the dinitro-diaza-alkanes.