Abstract: This invention provides a process for the preparation of a Eleutherobin derivative of the formula:
wherein R1 is a hydrogen, ester, nitrile or C2H4—R wherein R4 is a carbohydrate, an alcohol an amine, an amide, an alkyne, or, R2 is a linear or branched alkyl moiety, R3 is an ester, an amide, a carbamate, an acetal compound,an ether or a urethane, R4 is a hydrogen or CH2,position C2 and C3 is cis or trans,position C8 is &agr; or &bgr; and a compound is produced having the structures:
Additionally, this experiment provides a method for inhibiting growth of cancerous cells comprising contracting an amount of Eleutherobin derivative effective to inhibit the growth of said cells. Further provided is a method for treating cancer in a subject which comprises administering to the subject a therapeutically effective amount of the Eleutherobin derivative.
Type:
Grant
Filed:
December 11, 1998
Date of Patent:
January 9, 2001
Assignee:
The Trustees of Columbia in the City of New York
Inventors:
Samuel J. Danishefsky, Xiao-Tao Chen, Clare E. Gutteridge, Samit K. Bhattacharya, Bishan Zhou
Abstract: The present invention relates to cyclodextrin derivatives, and methods for the preparation thereof, which cyclodextrin derivatives have at least one but no more than N-1 "higher" alkyl groups and at least one but no more than N-1 sulfate groups, wherein the total combined number of "higher" alkyl groups and sulfate groups does not exceed N, and further wherein N is the number of hydroxyl groups of the cyclodextrin from which the derivative was derived. The "higher" alkyl groups are lipids and, more particularly, aliphatic or aromatic carbon chains, especially linear carbon chains having a general structure of --O--C(.dbd.O)--(CH.sub.2).sub.n --CH.sub.3, wherein n is between 6 and 24 and/or --OC(.dbd.O)--(CH.sub.2).sub.m --CH.dbd.CH--(CH.sub.2).sub.m --CH.sub.3, wherein m is at least 6. The sulfate groups disclosed herein are sulfate groups having the formula --OSO.sub.3 R, wherein R may be H, Na, K, Li, NH.sub.4 and/or other atoms/molecules that form monovalent cations.
Abstract: The present invention describes isolated Fagopyritol A1, isolated Fagopyritol A2, and isolated Fagopyritol B3. Compositions which include two or more of Fagopyritol A1, Fagopyritol A2, Fagopyritol B1, Fagopyritol B2, Fagopyritol B3, and D-chiro-inositol, at least one of which is an isolated Fagopyritol A1, isolated Fagopyritol A2, or isolated Fagopyritol B3, are also disclosed. Methods for preparing substantially pure Fagopyritol A1, Fagopyritol A2, Fagopyritol B1, Fagopyritol B2, Fagopyritol B3, or mixtures thereof from buckwheat are also described. The fagopyritols can be used to prepare pharmaceutical compositions, the administration of which can be used to treat diabetes.
Abstract: A Parenteral Water-miscible non-intensely colored injectable composition of Non-steroidal anti-inflammatory drugs is disclosed. The invention utilizes solubilization techniques to achieve sufficiently high concentrations of Nimesulide suitable to deliver therapeutic doses in conveniently small volumes using water and without any salt form or complexing agent of Nimesulide. In the composition of the invention all the ingredients of the base are hydrophillic. The hydrophillic base serves the advantage of better miscibility with body fluids, faster drug disposition and better compatibility with the tissue environment.
Abstract: A water-soluble or water-dispersible amino acid copolymer having pendent polysaccharide moieties. The invention also provides a method for cleaning an article and a method of providing soil resistance to an article using the amino acid copolymer having pendent polysaccharide moieties. The amino acid copolymers are useful in cleaning compositions such as laundry detergents, dishwashing detergents, prespotters, fabric softeners, and hard surface cleaners.
Type:
Grant
Filed:
June 16, 1999
Date of Patent:
December 12, 2000
Assignee:
National Starch and Chemical Investment Holding Corporation
Inventors:
John S. Thomaides, Klein A. Rodrigues, Paul M. Petersen
Abstract: 14-Aza analogs of PGF.sub.2.alpha., PGD.sub.2, and PGE.sub.2 and methods of their use in treating glaucoma and ocular hypertension are disclosed.
Abstract: A keratan sulfate oligosaccharide which comprises from two to five sugar units and has sulfated N-acetylglucosamine at the reducing end and in a molecule of which at least two hydroxyl groups are sulfated, preferably, which contains at least disaccharide represented by the formula Gal(6S)-GlcNAc(6S) (in the formula, Gal, GlcN, Ac, and 6S represent a galactose, a glucosamine, an acetyl group, and a 6-O-sulfate ester, respectively) as a constitutional ingredient, and/or pharmaceutically acceptable salt thereof are used as active ingredients of anti-inflammatory agents, antiallergic agents, immunomodulators, cell differentiation inducers, and apoptosis inducers.
Abstract: The invention provides a process for the recovery of purified lactic acid values from an aqueous feed solution containing lactic acid, lactic acid salt, or mixtures thereof, comprising: bringing the feed solution into contact with a substantially immiscible anion exchanger to form a substantially water-immiscible phase comprising an anion exchanger-lactic acid adduct; effecting a condensation reaction in the substantially water-immiscible phase between a carboxylic moiety of the lactic acid adduct and a moiety selected from a hydroxyl moiety and a primary or secondary amine moiety to respectively form a lactic acid ester or amine product; and separating the formed lactic acid product from the anion exchanger.
Type:
Grant
Filed:
October 26, 1999
Date of Patent:
December 12, 2000
Assignee:
Cargill Incorporated
Inventors:
Aharon Meir Eyal, Patrick R. Gruber, Paul McWilliams, David R. Witzke
Abstract: A three-stage process for removing mercury contaminants from alcoholic alkali metal alkoxide solutions is provided, in which mercury is depleted in a first filtration through inert fibrous material, followed by a second filtration through pulverized coal, and then by concentration by distillation, to preferably provide a mercury content below 0.1 ppm.
Type:
Grant
Filed:
February 10, 1998
Date of Patent:
December 5, 2000
Assignee:
Huels Aktiengesellschaft
Inventors:
Marcus Bongen, Marcel Feld, Guenter Zoche
Abstract: Sulfoalkyl ether cyclodextrins are produced by a process of treating an unsubstituted cyclodextrin starting material with an alkyl sultone in the presence of a base. The base is added in a stepwise, pH controlled manner so that substantially the entire initial charge of cyclodextrin starting material is at least partially reacted. Additional base is then added to complete the reaction, and residual alkyl suftone is destroyed. The product advantageously contains low levels of both residual cyclodextrin and residual alkyl sultone.
Abstract: This invention provides lipids having: 1) a glycerol backbone; 2) a hydrocarbon chain, preferably saturated and containing 16 or 18 carbon atoms, attached to C-1 of the backbone by an ether linkage; 3) a methyl group attached to C-2 of the backbone, preferably by an ether linkage; and, 4) a sugar attached to C-3 of the glycerol backbone in either the alpha or beta anomeric configuration, the sugar being altered by modification of, or substitution for, one or more of its hydroxyl groups. Also provided herein are ether-lipid-containing compositions, as well as methods of administering such compositions to animals, for example, those afflicted with cancers, as well as various other diseases and disorders.
Type:
Grant
Filed:
September 26, 1996
Date of Patent:
November 28, 2000
Assignee:
The Liposome Company, Inc.
Inventors:
Robert Bittman, Ravi K. Erukulla, Andrew C. Peters, Eric G. Mayhew
Abstract: The invention relates to certain steroidal glycoside derivatives useful as hypocholesterolemic agents and anti-atherosclerosis agents. The present invention is also directed to pharmaceutical compositions comprising such derivatives and use of such derivatives in treating hypercholesterolemia or atherosclerosis.
Abstract: Certain retinoids with CH.sub.2 OH at the side chain terminal position, preferably 4-oxoretinol, inhibit growth of estrogen-receptor positive and estrogen-receptor negative breast cancer tumor cell lines and have utility for adjuvant therapy and treatment of metastatic disease.
Abstract: The present invention relates to compounds of the formula ##STR1## in which R.sup.1 is defined in the specification, and non-toxic metabolically labile esters and amides thereof are useful as modulators of metabotropic glutamate receptor function.
Abstract: The invention relates to a process for the preparation of methoxyacetic acid esters in which a chloroacetic acid ester is reacted with an alkali metal methoxide to give the methoxyacetic acid ester.
Type:
Grant
Filed:
October 27, 1998
Date of Patent:
November 7, 2000
Assignee:
Huels Aktiengesellschaft
Inventors:
Wolfgang Kleemiss, Klaus-Dieter Steffen, Marcel Feld
Abstract: A manufacturing process of cellulose solution with low viscosity includes the step of dissolving a cellulose in a mixture solvent which is produced by mixing an additional solvent mixture, N-methylol caprolactom, with a main solvent, N-methyl morpholine oxide. The present invention not only can increase the swelling of the pulp during the dissolving process, but also can lower the viscosity of the cellulose solution that enables the manufacturing process to process at lower temperature and the cellulose solution produced to spin in higher spinning speed. Therefore, the physical property and the quality of the final fiber product are improved by eliminating the problem of cellulose polymerization decay.
Abstract: The present application describes total or partial butyric esters of polysaccharides as novel compounds; the number of hydroxyl groups esterified with butyric residues per each glycosidic monomer is preferably higher than 0.001; the application also describes the process of preparation of said esters, their use in therapy as antiproliferative agents, and pharmaceutical compositions containing them.
Abstract: Novel compounds which are a glucocorticosteroid (GCS) chemically bound to a sugar, having the general formulaGCS.sup.1 --O--Sugar.sup.1for colon- or ileum-specific delivery of the GCS to inflamed bowel mucosa, as well as processes for their preparation, pharmaceutical preparations containing the compounds and the use of said compounds in therapy.
Type:
Grant
Filed:
March 3, 1999
Date of Patent:
October 31, 2000
Assignee:
Aktiebolaget Astra
Inventors:
Ralph Lennart Brattsand, Peter Edman, Thomas Hogberg, Stinabritt Nilsson, Bror Arne Thalen, Jan Erik Ulmius
Abstract: A process of preparing a L-ribose fraction having greater than 97% purity starting from an aqueous solution of L-arabinose is provided by utilizing an epimerization reaction conducted in the presence of a Mo compound and eluting the product formed by said epimerization reaction through a separation zone containing a strong acid cation exchange resin. A process of crystallized said L-ribose fraction under conditions effective to form monohydrate L-ribose crystals is also disclosed.
Type:
Grant
Filed:
November 17, 1998
Date of Patent:
October 31, 2000
Assignee:
Xyrofin Oy
Inventors:
Juho Jumppanen, Juha Nurmi, Ossi Pastinen
Abstract: A spinnable, isotropic solution containing cellulose, phosphoric acid and/or anhydrides of phosphoric acid and water is prepared by dissolving cellulose in a solvent, the solvent being a homogeneous mixture of water and at least one of phosphoric acid and anhydrides of phosphoric acid such that the solvent contains 72-85 wt. % of phosphorous pentoxide, P.sub.2 O.sub.5. The cellulose is mixed with the solvent in a mixing apparatus, the mixing apparatus having mixers, kneaders or the like, and capable of generating high shearing forces. The solution is converted from anisotropic phase to isotropic phase by the addition of water. The water required to convert the solution to the isotropic phase is added either just prior to, during or after the mixing step. The solvent preferably contains 72-80 wt. % P.sub.2 O.sub.5 and 7-20 wt. % of cellulose, and is used to make hollow fibers, membranes, non-woven films, and other articles requiring the use of cellulose-containing solutions.
Type:
Grant
Filed:
August 6, 1998
Date of Patent:
October 31, 2000
Assignee:
Akzo Nobel N.V.
Inventors:
Jan Barend Westerink, Marco Ypma, Hendrik Maatman, Hanueke Boerstoel