Abstract: Camptothecin derivatives of camptothecin of formula (I):
wherein the groups R1, R2 and R3 are as defined in the description are disclosed.
The compounds of formula (I) are endowed with antitumor activity and show a good therapeutic index.
Processes for the preparation of the compounds of formula (I) and their use in the preparation of medicaments useful in the treatment of tumors, viral infections and antiplasmodium falciparum are also disclosed.
Abstract: Compositions comprising an effective amount of a curcuminoid species and an effective amount of a diterpene lactone species, a triterpene species or derivatives thereof that have a synergistic effect on specific inhibition of inducible COX-2 activity and have minimal effect on COX-1 activity are disclosed. Methods of using the compositions for providing synergistic anti-inflammatory effects are also disclosed.
Type:
Application
Filed:
July 16, 2002
Publication date:
June 12, 2003
Inventors:
John G. Babish, Terrence Howell, Linda Pacioretty
Abstract: The present invention relates to an oil in water emulsion vaccine composition. In particular, the present invention relates to a vaccine adjuvant formulation based on oil in water emulsion comprising a metabolisable oil and a saponin, wherein the oil and a saponin are present in a ratio of between 1:1 and 200:1. The invention further relates to methods for preparing the emulsion and its use in medicine.
Type:
Application
Filed:
May 6, 2002
Publication date:
May 22, 2003
Applicant:
SmithKline Beecham Biologicals S.A.
Inventors:
Nathalie Garcon, Patricia Marie Christine Aline Francoise Momin
Abstract: The present invention relates to combinations of xylose compounds with other pharmaceutically active compounds, to pharmaceutical compositions comprising said combinations, as well as to use of these combinations for the manufacture of a medicament for treatment of proliferative disorders. In another aspect, the present invention relates to novel xylose compounds, to pharmaceutical compositions comprising said compounds, and to use of these compounds for the manufacture of a medicament or the treatment of proliferative disorders.
Type:
Application
Filed:
October 15, 2002
Publication date:
May 15, 2003
Inventors:
Goran Magnusson, Pia Magnusson Hall, Mattias Belting, Niklas Falk, Lars-Ake Fransson, Katrin Mani
Abstract: Administration of a pharmaceutical composition in the form of a suppository comprising:
(a) a prostaglandin vasodilator;
(b) 15-hydroxyprostaglandindehydrogenase inhibitor: and
(c) a base material that is solid at room temperature and releases components (a) and (b) when inserted in the urethra,
is effective for the treatment of male erectile dysfunction.
Abstract: A composition is prepared by extracting phytochemicals from plant matter. This composition is enriched preferably in isoflavones, lignans, saponins, catechins and phenolic acids. Soy is the preferred source of these chemicals: however, other plants may also be used, such as red clover, kudzu, flax, and cocoa. The composition is a dietary supplement for treatment of various cancers, pre- and post-menstrual syndromes, and various other disorders.
Abstract: Cytotoxic tumor therapy in a patient is enhanced by co-administration of sphingomyelin. The invention most likely enhances a tumor cell's ability to undergo ceramide-induced apoptosis by increasing the levels of sphingomyelin in all cellular compartments, thereby providing sufficient substrate for activated sphingomyelinase. A method of treating rheumatoid arthritis also is provided.
Type:
Grant
Filed:
March 24, 2000
Date of Patent:
April 1, 2003
Assignee:
Center for Molecular Medicine and Immunology
Abstract: A substance including the chemical structures of bicyclo [3.2.1]octan or the chemical structures of kaurene for the use in a dietary supplementation or as a constituent in a medicament for the treatment of non-insulin dependent diabetes mellitus, hypertension and/or the metabolic syndrome. The unique chemical structures of bicyclo [3.2.1]octan alone or in a kaurene structure provides the substances, such as e.g. steviol, isosteviol and stevioside with the capability of enhancing or potentiating the secretion of insulin in a plasma glucose dependent manner. The substances including these unique chemical structures also have the capability of reducing the glucagon concentration in the blood and/or lowering the blood pressure thereby providing a self-regulatory treatment system for non-insulin dependent diabetes mellitus and/or hypertension.
Type:
Application
Filed:
July 31, 2002
Publication date:
March 27, 2003
Inventors:
Kjeld Hermansen, Soren Gregersen, Per Jeppesen
Abstract: This invention provides compositions for repelling insects, particularly biting insects, such as mosquitoes, ticks, and biting flies comprising ratite oil, active fractions of ratite oil obtained by flash chromatography or compositions comprising mixtures of fatty acids found in ratite oil. Also provided are compositions for repelling insects comprising ratite oil, active fractions of ratite oil or compositions comprising mixtures of fatty acids found in ratite oil further comprising at least one additional insect repellent. Methods of repelling insects, particularly biting insects, are provided comprising topically applying ratite oil, active fractions of ratite oil, or compositions comprising mixtures of fatty acids found in ratite oil; or ratite oil, active fractions thereof, or compositions comprising fatty acids found in ratite oil and further comprising at least one additional insect repellent.
Type:
Grant
Filed:
February 15, 2001
Date of Patent:
March 25, 2003
Assignee:
AgraQuest, Inc.
Inventors:
Denise C. Manker, Pamela Gail Marrone, Stephen Judd
Abstract: Art adjuvant composition for stimulating an effective immune resposne to an antigenic substance when co-administered to an animal with said antigenic substance, comprising: (a) a saponin with immune stimulating activity; (b) a polycationic polyelectrolyte with immune stimulating activity; and (c) an immunoadjuvant oil.
Type:
Grant
Filed:
November 30, 2000
Date of Patent:
March 4, 2003
Assignee:
Commonwealth Scientific and Industrial Research
Organisation
Abstract: This invention provides methods that are useful for inhibiting a MXR transporter in a cell overexpressing a MXR gene but not overexpressing a Pgp gene by contacting the cell with an acridine derivative. The invention also provides for a method of treating a mammal suffering from a cancer, which overexpressing a MXR gene but not overexpress a Pgp gene, by the co-administration of a chemotherapeutic and an acridine derivative.
Type:
Grant
Filed:
January 22, 2001
Date of Patent:
February 18, 2003
Assignee:
The United States of America as represented by the Department
of Health and Human Services
Abstract: Described herein are methods for ablation, i.e., elimination or reduction, of unwanted tissue, particularly tissue which is normal to be present in the body but is unwanted for either health or cosmetic reasons. In particular embodiments, there are described methods for elimination of fat tissue from the body. According to the methods described herein, a drug which acts to eliminate the undesired tissue is provided in a carrier which is biocompatible, capable of being administered by injection, and which effects a controlled release of the drug over time. The drug with carrier is administered by injection locally in the area of the unwanted tissue, resulting in elimination of the tissue in that local area.
Type:
Application
Filed:
January 30, 2002
Publication date:
January 30, 2003
Applicant:
The Regents Of The University of Michigan
Abstract: Activated carbon, as well as compositions and kits comprising the same, are effective for preventing pregnancy and sexually transmitted diseases including HIV.
Type:
Application
Filed:
August 8, 2002
Publication date:
January 2, 2003
Applicant:
The Procter & Gamble Company
Inventors:
Richard Joseph Sunberg, Sheri Anne Hunt
Abstract: A composition is prepared by extracting phytochemicals from plant matter. This composition is enriched preferably in isoflavones, lignans, saponins, catechins and phenolic acids. Soy is the preferred source of these chemicals: however, other plants may also be used, such as red clover, kudzu, flax, and cocoa. The composition is a dietary supplement for treatment of various cancers, pre- and post-menstrual syndromes, and various other disorders.
Abstract: The invention discloses the use of a number of saponins and sapogenins, notably those of steroidal structure, in the treatment of cognitive disfunction and similar conditions. Methods of treatment, and pharmaceutical compositions are also disclosed.
Type:
Application
Filed:
February 15, 2002
Publication date:
December 19, 2002
Inventors:
Zongqin Xia, Yaer Hu, Ian Rubin, Jonathan Brostoff, Brian Whittle, Weijun Wang, Phil Gunning
Abstract: A physiologically acceptable aqueous solution, and water-soluble compositions suitable for obtaining it, comprising a first physiologically acceptable compound of an acidic nature and a second physiologically acceptable compound of a basic nature that are able to give rise to a precipitate in water, characterized in that it also contains a trisubstituted salt of glycyrrhizic acid in a sufficient quantity to form a clear solution in water.
Abstract: Compositions and methods for promoting a healthy cardiovascular system and enhancing healthy blood flow by gently removing toxic buildup from the arterial walls and dilating and strengthening the arterial walls, in a mammal. The compositions comprise calcium; magnesium; selenium; manganese; zinc; potassium; vitamin E; vitamin A; alpha-lipoic acid; Allium sativum extract; Afecicago satiia extract; Chondrus crispus extract; L-cysteine; L-glutamic acid; glycine; and glutathione.
Abstract: A composition is prepared by extracting phytochemicals from plant matter. This composition is enriched preferably in isoflavones, lignans. saponins. catechins and phenolic acids. Soy is the preferred source of these chemicals: however other plants may also be used, such as red clover, kudzu, flax, and cocoa. The composition is a dietary supplement for treatment of various cancers, pre- and post-menstrual syndromes, and various other disorders.
Abstract: The present invention relates to a new and safe pharmaceutical composition for treating and preventing infertilities and increasing immune function.
Specifically, this invention provides a new and safe composition, which is Icariin (ICN) extracted from Epimedium sagittatum Maxim, E. brevicornum Maxim and E. macranthum Morr. The chemical structure of Icariin is indicated. ICN also inhibits peroxidation significantly.
Abstract: The present invention describes the use of fumitremorgin A, B and C and a series of diketopiperazines of Formula (I) to resensitize multidrug resistant (MDR) cancer cells to the cytotoxic effects of chemotherapeutic drugs.
Type:
Application
Filed:
February 28, 2002
Publication date:
October 24, 2002
Applicant:
American Cyanamid Company
Inventors:
Sridhar Krishna Rabindran, Haiyin He, Maya Prakash Singh, Lee Martin Greenberger
Abstract: The products and methods of the present invention provide a means for increasing the solubility and bioavailability of active agents. More particularly the invention provides compositions containing active agents as water-soluble complexes with glycyrrhizin, and methods of preparing such complexes. The invention further provides methods for the preparation of highly water soluble complex dosage forms.
Abstract: An ingestible mollusc poison contains a simple metal compound, an activity enhancing additive such as ethylene diamine disuccinic acid (EDDS) and derivatives thereof, and a carrier material edible to molluscs. In one embodiment the active agent of the mollusc poison may be in the form of a metal complex of EDDS. The composition may be used alone or in conjunction with molluscicidal co-active agents and/or fertilizers.
Abstract: Novel compositions comprising a potassium channel opener, such as minoxidil, and a protein kinase C inhibitor, such as procyanidin B2 are presented, as are kits containing a first composition comprising a potassium channel opener and a second composition comprising a protein kinase C inhibitor. Also presented are methods for using the novel compositions for treating and preventing hair loss in a region of a patient.
Abstract: A method is provided for therapeutic use of a class of compounds that are effective in protecting nerve cells from deterioration and cell death arising from degenerative disease, trauma or aging and may be used to achieve a similar effect in male and female subjects with minimal adverse side effects. The method comprises administering a therapeutically effective dose of a natural or synthetic bioflavonoid that acts as an MAPK cascade antagonist. Examples of bioflavonoids that may be used in the present method are apigenin and 2-(2′-amino-3′ methoxyphenyl)-oxanaphthalen-4-one (PD098059).
Abstract: The present invention provides a therapeutic agent and therapeutic method for treatment of mastitis in livestock comprising glycyrrhizin and pharmaceutically acceptable salts thereof as effective ingredients.
Abstract: The invention provides the use of the saponin derivatives, which is of the general formula (I) or the pharmaceutically acceptable salts and esters thereof: 1
Abstract: A novel formulation is provided that serves to synergistically inhibit the generation of free radicals and oxidative stress in animals. The formulation comprises as a first component a carotenoid species, and, as a second component, at least one member selected from the group consisting of lipoic acid, dihydrolipoic acid (DHLA), a stilbene species, ergothioneine, a flavone species, a triterpene species, ascorbic acid and derivatives thereof.
Abstract: Food composition in the form of a flour comprising at least 50% of protein, less than 15% of carbohydrates and 35 to 50% of plant fibers; preferably the carbohydrate content is less than 10%, advantageously less than 5%; this composition may be used as a substitute for wheat flour in the preparation of foods such as pasta, bread, bread sticks, bakery products and pastries and constitutes the basis of a method for improving the appearance of a person by achieving a loss of weight which is beneficial from the aesthetic point of view.
Abstract: Methods for treating, preventing, or inhibiting diseases and disorders associated with inflammation, cell-proliferation, and pain comprising the administration of a compound having the structural formula 1
Abstract: A novel formulation is provided that serves to inhibit the inflammatory response in animals. The formulation comprises, as a first component an effective amount of a sesquiterpene lactone species and an effective amount of a second component selected from the group consisting of a diterpene lactone species and a triterpene species or derivatives thereof, and provides synergistic anti-inflammatory effects in response to physical or chemical injury or abnormal immune stimulation due to a biological agent or unknown etiology.
Type:
Application
Filed:
July 31, 2001
Publication date:
June 20, 2002
Applicant:
Ashni Naturaceuticals, Inc.
Inventors:
John G. Babish, Terrence Howell, Linda Pacioretty
Abstract: Compositions for maintaining normal sexual function and treating sexual dysfunction in males and females comprising at least 15% by weight icariside I or at least 3.5% by weight anhydroicaritin, derived from extracts of plants belonging the Epimedium genus, and methods for preparing the same, are provided. The methods comprise subjecting an Epimedium extract to mild acid hydrolysis. Methods for maintaining normal sexual function and treating sexual dysfunction in both males and females are also provided, comprising oral administration of an effective amount of a novel composition of this invention comprising at least 15% by weight icariside I or at least 3.5% by weight anhydroicaritin.
Type:
Grant
Filed:
August 15, 2000
Date of Patent:
June 4, 2002
Assignee:
Hauser, Inc.
Inventors:
Rod Lenoble, Steven L. Richheimer, David Bailey, Coralee G. Mannila, Rebecca L. Nichols
Abstract: The compound referred to herein as IB-962 12, having structure (I) can be obtained by cultivating the strain of Micromonospora sp. ES25-008, available under the accession number CECT-3333, and can be hydrolyzed to give IB-96212B having structure (II). The sugar substituent which is L-rhodinose, can its elf be derivatized or the sugar can be replaced, in either case, giving further derivatives of IB-96212 having a group other than L-rhodinose at the position of the sugar.
Type:
Grant
Filed:
April 17, 2000
Date of Patent:
May 28, 2002
Assignee:
Instituto Biomar S.A.
Inventors:
Rosa Isabel Fernandez-Chimeno, Francisco Romero, Jose Luis Fernandez-Puentes, Julia Perez-Baz, Librada Maria Canedo, Fernando Espliego
Abstract: The cosmetic topical formulation of this invention is directed toward diminishing skin wrinkling, fine line, improving skin tone, and combinations thereof. Preferably, the topical formulation contains a matrix metalloproteinase inhibitor, MMPI, and advantageously includes a natural estrogen, e.g., a true estrogen compound, such as 17-beta estradiol, or an estrogen-like steroid, (such as various phytoestrogens found in herbal preparations), as opposed to a synthetic estrogen. Other forms of the cosmetic topical formulation of this invention include combinations of synthetic estrogen and MMP inhibitor. Exemplary synthetic estrogens include, but are not limited to, ethinyl estradiol and clomiphine citrate. The cosmetic topical formulation is safe and effective diminishing wrinkling, and improving skin tone.
Abstract: Compositions which comprise, in a physiologically acceptable medium, at least one sapogenin or a derivative or natural extract containing the same, and at least one xanthine base are useful, in particular, for preventing or combating cellulite and/or for refining the figure or the contours of the face. Preferably, the composition comprises diosgenin or an extract of wild yam, combined with caffeine.
Abstract: Improved methods and compositions for protecting plants or seeds from plant diseases are provided. Broadly, the compositions comprise (and preferably consist essentially of) saponin, such as triterpene type saponins extracted from Quinoa or Quillaja. The methods comprise contacting the portion of the plant (e.g., foliage, shoot, etc.) to be treated with a disease-inhibiting or protective amount of the composition. The compositions can also be used to treat plant seeds or tubers prior to planting thereof, as well as soil adjacent a growing plant. The inventive compositions are particularly useful for the treatment, control and/or prevention of fungal diseases. The saponins of the invention can be applied as liquids or dry particulates, and are especially suited for the treatment of potato seed, tubers and plants.
Type:
Application
Filed:
February 13, 2001
Publication date:
January 31, 2002
Inventors:
Joseph M. Dutcheshen, Theodore Anthony Danyluk
Abstract: This invention relates to pharmaceutical compositions of and methods of treating viral infections with a synergistic combination of glycyrrhizic acid and either a lactoferrin or a lysozyme.
Type:
Grant
Filed:
January 18, 2000
Date of Patent:
December 11, 2001
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F.
S.p.A.
Abstract: An object of the present invention is to obtain an oral glycyrrhizin preparation not only manufacturable by a simple method but also having an excellent property of being absorbed from the digestive tract. In the present invention, such oral preparations are made into enteric forms wherein glycyrrhizin is admixed with an effervescent agent in combination with an absorption enhancer such as a medium-chain fatty acid or a salt thereof. In the preparation of the present invention, it is now possible to achieve an excellent absorption of glycyrrhizin from the digestive tract by addition of an effervescent agent and, moreover, the preparation can be manufactured by a simple, convenient method without special steps.
Abstract: Compositions comprising oligonucleotides comprising at least one unmethylated CpG dinucleotide and saponin and the use thereof for stimulating innate immunity and enhancing natural killer cell activity are disclosed.
Abstract: Disclosed are combinations of a taxoid, an alkylating agent and an anthracycline antibiotic, which compositions exhibit therapeutic synergy in the treatment of cancer.
Abstract: Compositions and methods for controlling the population of insects are disclosed. The compositions include a feeding stimulant for a particular insect, an effective amount of a 1-arylpyrazole or nicotinyl insecticide to kill an desired insect, at a concentration which is not typically toxic when applied to a plant in the absence of a feeding stimulant and the insect consumes an ordinary amount of toxin during the course of normal feeding, but is toxic when applied in conjunction with a feeding stimulant which causes the insect to consume more of the toxin than would normally be consumed during normal feeding. The use of normally non-toxic amounts of insecticides allows one to minimize the residual insecticide present on the crops.
Abstract: Water-soluble derivatives of epipodophyllotoxin, process for their preparation and their use for the treatment of rheumatoid arthritis, complaints caused by human papilloma virus and cancer.
Type:
Grant
Filed:
April 21, 1997
Date of Patent:
August 22, 2000
Assignee:
Pierre Fabre Medicament
Inventors:
Thierry Imbert, Yves Guminski, Barbara Monse, Bridget Hill, Jean-Pierre Robin
Abstract: The invention described here concerns the unique utility of fatty acids and their derivatives to eradicate existing fungal and bacterial infections in plants. Also, described herein are combination treatments whereby fatty acids are used to enhance or augment the activity of fungicides, bactericides, and biological control agents.
Type:
Grant
Filed:
September 8, 1997
Date of Patent:
August 15, 2000
Assignee:
Mycogen Corporation
Inventors:
Steven D. Savage, Steven L. Evans, Robert A. Haygood, Paul S. Zorner, Keith Jones
Abstract: Administration of a pharmaceutical composition comprising:(a) a vasodilator; and(b) a 15-hydroxyprostaglandindehydrogenase inhibitor is effective for the treatment of male erectile dysfunction.
Abstract: This invention describes the effect of a means to prevent the sexual transmission of infectious pathogens of the vaginal and uterine wall in women, farm animals and pets. This discovery concerns a means to disrupt the sexual transmission of infectious pathogens which attack the cavity living of the vagina and uterus of women, farm animals and pets which consists of a foam that prevents the docking of pathogens to the cavity lining and which acts as a pathogen-killing substance.
Abstract: Methods of promoting would healing and the growth and proliferation of keratinocytes, fibroblasts and endothelial cells are disclosed. These methods comprise contacting a wound with an effective wound healing amount of a composition comprising a pseudopterosin or pseudopterosin derivative.
Abstract: A method for treating skin conditions, such as rosacea and sensitive skin, that manifest as a tendency towards flushing and blushing is provided. Also provided herein, are compositions for the treatment of rosacea and sensitive skin that are comprised of at least one antioxidant selected from the following groups of antioxidants: (a) phenolic compounds that contain at least one hydroxyl group connected directly to a benzene ring and to another unsaturated chemical grouping, (b) sulfur-containing compounds that contain at least one sulfhydryl groups or sulfur-containing compounds that contain at least one disulfide group, or (c) polyene compounds that have conjugated systems of double bonds.
Abstract: The present invention is directed to deacyl teicoplanin, and to a process for preparing deacyl teicoplanin by reacting teicoplanin with ECB deacylase. Deacyl teicoplanin can be alkylated to produce compounds useful for their antibacterial activity.
Type:
Grant
Filed:
April 1, 1998
Date of Patent:
August 10, 1999
Assignee:
Eli Lilly and Company
Inventors:
Barbara Shreve Briggs, Robin David Grey Cooper, Adam Joseph Kreuzman, Milton Joseph Zmijewski, Jr.