Benzene Ring Bonded Directly To The Hetero Ring (e.g., Flavones, Etc.) Patents (Class 549/403)
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Publication number: 20080261898Abstract: Compounds, compositions, methods and kits are provided for treating, reducing the risk of, or preventing diseases and/or conditions, such as diseases associated with angiogenesis and/or abnormal cell proliferation, such as cancer. Compounds of the present invention have antiangiogenic and anti-cancer activity with minimum toxic effects on normal cells. Methods for preparing and manufacturing the compounds and pharmaceutical compositions are also provided.Type: ApplicationFiled: April 17, 2008Publication date: October 23, 2008Inventors: Heather H. Liao, Li Zhan
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Publication number: 20080254149Abstract: Methods for recovering valuable compounds and substances from plants after distillation of oils are disclosed. The methods involve various aqueous and non-aqueous solvent extraction of plant material from which oils have been distilled previously.Type: ApplicationFiled: December 18, 2006Publication date: October 16, 2008Applicant: BAKTO NATURAL PRESERVATIVES, LLC.Inventor: Daphna Havkin-Frenkel
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Publication number: 20080233242Abstract: The present invention discloses the composition of antioxidant of bamboo leaves (AOB) and its use. The purpose of present invention is to provide a new food additive which is natural, nutritional, and muti-functional, and which is of rich resources, safety, good effect, and low cost. AOB is yellow or brown powders or particles obtained from bamboo leaves, wherein the main antioxidative components include flavones, lactones, phenolic acids. AOB can either inhibit lipid autoxidation chain reaction, or chelate transitional metal ions, and can be used as primary and second antioxidant. AOB can eliminate nitrite and inhibit the synthesis of N-nitrosamine, and has anti-bacteria, bacteriostatic, deodorizing, aroma enhancing etc. functions. AOB can be commonly used in oil-containing food, meat product, fishery product, expanded food etc. food systems.Type: ApplicationFiled: October 8, 2004Publication date: September 25, 2008Inventors: Ying Zhang, Xiaoqin Wu, Zhuoyu Yu, Dingding Luo, Boyi Lu, Yu Zhang
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Publication number: 20080194522Abstract: The present invention relates to compounds useful for detecting the activity of monoamine oxidases, compounds useful for competitively inhibiting monoamine oxidases, for determining inhibitors of monoamine oxidases and compounds useful for treating monoamine oxidase-related nervous system pathologies, as well as pharmaceutical compositions and methods of manufacture thereof.Type: ApplicationFiled: August 25, 2005Publication date: August 14, 2008Inventors: Gong Chen, Dominic J. Yee, Niko Gubernator
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Publication number: 20080188549Abstract: The present invention has its object to provide a specific compound derived from a naturally occurring substance, and a composition for the prevention and/or treatment of metabolic syndrome and insulin resistance syndrome which comprises that as an active ingredient, easily and efficiently. The present invention relates to a composition for the prevention and/or treatment of metabolic syndrome and a composition for the prevention and/or treatment of insulin resistance syndrome, each of which comprises, as an active ingredient, at least one compound selected from among the compound represented by the formula (1), compounds represented by the formula (4) and compounds represented by the formula (5), or a salt or ester thereof.Type: ApplicationFiled: February 8, 2006Publication date: August 7, 2008Applicant: Kaneka CorporationInventors: Hozumi Tanaka, Shinichi Yokota, Misuzu Tsukagawa, Tatsumasa Mae, Minpei Kuroda, Yoshihiro Mimaki
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Publication number: 20080114056Abstract: The present invention relates to the use of a chromone compound of the formula wherein R1, R2, R3, R4, R5 and m are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in acid addition salt form, as a vanilloid antagonist.Type: ApplicationFiled: June 8, 2005Publication date: May 15, 2008Inventors: Timothy John Ritchie, Andrew James Culshaw, Terance William Hart, Christopher Thomas Brain, Edward Karol Dziadulewicz
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Patent number: 7371775Abstract: The present invention relates to 7-carboxymethyloxy-3?,4?,5-trimethoxy flavone.monohydrate which is a non hygroscopic product suitable for the preparation of metered dose of 7-carboxymethyloxy-3?,4?,5-trimethoxy flavone having protective activity for gastrointestinal tract including the colon, and a preparation method and uses thereof. 7-carboxymethyloxy-3?,4?,5-trimethoxy flavone.monohydrate of the present invention has advantages such as mucus protecting activity for gastrointestinal tract including the colon, convenience for handling and storage under ordinary humidity owing to its non-hygroscopicity, and ability to contain an active compound consistently for the formulation production of a medicine. In addition, the preparation method of 7-carboxymethyloxy-3?,4?,5-trimethoxy flavone.Type: GrantFiled: September 4, 2004Date of Patent: May 13, 2008Assignee: Dong-A Pharmaceuticals Co., LtdInventors: Moohi Yoo, Dong Sung Kim, Yong Duck Kim, Wonbae Kim
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Patent number: 7368434Abstract: The present invention provides novel antidipsotropic compounds. The invention further provides methods of inhibiting ALDH-2 using the compounds described herein. Methods for modulating alcohol consumption, alcohol dependence and/or alcohol abuse by administering the compounds of the invention to an individual are also provided. The present invention further provides a rationale for designing additional novel antidipsotropic compounds.Type: GrantFiled: June 27, 2003Date of Patent: May 6, 2008Assignee: The Endowment for Research in Human Biology, Inc.Inventors: Wing Ming Keung, Bert L. Vallee, Guangyao Gao
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Patent number: 7345090Abstract: The invention relates to compounds of the formula I where R1, R2, R3, R4 and R5 have the meanings given in claim 1. The compound is suitable in particular for use in skin care compositions. They protect, firstly, against harmful oxidation reactions and, secondly, also act as UV filters.Type: GrantFiled: April 28, 2004Date of Patent: March 18, 2008Assignee: Merck Patent Gesellschaft mit Beschraenkter HaftungInventors: Frank Pfluecker, Joachim Buenger, Hans-Juergen Driller, Herwig Buchholz, Ralf Rosskopf
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Patent number: 7329687Abstract: Compounds useful as chemotherapeutic, chemopreventive, and antiangiogenic agents are provided. The compounds are flavanoids, including flavanones, flavanols, and chalcones. The compounds have the structure of formula (I) wherein R1 through R3 and R5 through R11 are defined herein, and ?, ?, and ? are optional bonds, providing that when ? is absent, ? is present, and when ? is absent, ? is present. When ? is present, preferred R4 moieties are selected from O, S, NH and CH2, and when ? is absent, preferred R4 groups are selected from OH, SH, NH2 and CH3. When ? is present, the preferred R5 substituent is O, while when ? is absent, the preferred R5 substituent is OH. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.Type: GrantFiled: April 18, 2003Date of Patent: February 12, 2008Assignee: SRI InternationalInventors: Nurulain Zaveri, Wan-Ru Chao
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Patent number: 7326797Abstract: A process for manufacturing a hydroxylated isoflavone of the formula (I) given in the description comprises re-acting an appropriately substituted 2-hydroxydeoxybenzoin of the formula (II), also given in the description, with a formic acid anhydride of the formula HCOOCOR3, wherein R3 signifies C2-20-alkyl or various other groups as given in the description, in presence of a base or in a solvent which acts as a base, and if necessary promoting the ensuing hydrolysis of the so-produced acylated form of the hydroxylated isoflavone of the formula I by acidification. Of particular interest as products of this process are the 5,7dihydroxyisoflavones, e.g. genistein (5,7,4?-trihydroxyisoflavone). Isoflavones display many useful biochemical effects.Type: GrantFiled: July 14, 2003Date of Patent: February 5, 2008Assignee: DSM IP Assets B.V.Inventors: Bruno Burdet, August Ruettimann
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Publication number: 20080026087Abstract: A botanic extract of Litchi sinensis containing, based on active substance content, at least 15% by weight of an oligomeric proanthocyanidin of the OPC A2 type is disclosed. Processes of making such extracts containing at least 15% by weight of OPC A2 are also disclosed.Type: ApplicationFiled: June 15, 2004Publication date: January 31, 2008Inventors: Santiago Rull Prous, Small Alaoui Ismaili, Bernd Fabry
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Patent number: 7306815Abstract: Provided are processes for the preparation of compositions enriched in phenolic compounds from a crude plant extract. One process includes a novel column purification step using a polymer resin that releasably adsorbs the phenolic compounds but does not retain polar non-phenolic compounds, wherein the resin comprises aromatic rings substituted with one or more electron-withdrawing groups. This invention also includes compositions enriched in phenolic compounds. This invention encompasses methods of using the phenolic-enriched compositions for treating warm-blooded animals, including humans, infected with paramyxovaridae such as respiratory syncytial virus, orthomyoxovaridae such as influenza A, B, and C, parainfluenza, Herpes viruses such as HSV-1 and HSV-2, and Flaviviruses such as West Nile Virus, and for treating inflammation such as caused by arthritis, stress and digestive disease. The compositions are also useful as meat additives to inhibit food-borne pathogens.Type: GrantFiled: January 23, 2004Date of Patent: December 11, 2007Assignee: Phenolics, LLCInventors: Gerald T. Gourdin, Steven L. Richheimer, Michael S. Tempesta, David T. Bailey, Rebecca L. Nichols, F. Joseph Daugherty, Delano R. Freeberg
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Patent number: 7256214Abstract: Each of an antioxidant, an antimicrobial agent, an antitumor agent, a food and beverage product, cosmetics, a quasi-drug and a pharmaceutical of the present invention contains a new flavanone compound represented by the following structural formula: Alternatively, each of an antioxidant, an antimicrobial agent, an antitumor agent, a food and beverage product, cosmetics, a quasi-drug and a pharmaceutical of the present invention contains at least one flavanone compound selected from the group consisting of nymphaeol-A, nymphaeol-B, and nymphaeol-C.Type: GrantFiled: June 18, 2004Date of Patent: August 14, 2007Assignee: Pokka CorporationInventors: Shigenori Kumazawa, Tsutomu Nakayama, Kayoko Shimoi, Takaki Goto, Syuichi Fukumoto, Tsutomu Arakaki
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Patent number: 7226644Abstract: The present invention relates to a liquid crystal compound which has negative dielectric anisotropy and a large absolute value thereof; and a liquid crystal display element which contains the compound as a constituent element and has a negative value of dielectric anisotropy in the vertical alignment mode, IPS, or the like. The liquid-crystal display element has a structure including a pair of substrates and a liquid crystal sandwiched therebetween, and includes at least an alignment control layer, a transparent electrode, and a polarizing plate, in which the liquid crystal includes at least one compound having a partial structure represented by general formula (A): (wherein W1 and W2 each independently represents fluorine, chlorine, —CF3, —CF2H, —OCF3, or —OCF2H) and has negative dielectric anistropy.Type: GrantFiled: June 25, 2004Date of Patent: June 5, 2007Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Takashi Matsumoto, Tetsuo Kusumoto, Shotaro Kawakami
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Patent number: 7129269Abstract: The instant invention relates to sulphamate compounds of formula I, wherein A represents a ring structure, B represents a ring structure, D a ring structure, C is a bond, E is a link joining ring structure B to the ring structure D, X represents a suitable first group, and Y represents a suitable second group; wherein one ring of the compound is a phenolic ring; and wherein any one of ring structures A, B and D has bound thereto a sulphamate group.Type: GrantFiled: December 20, 2002Date of Patent: October 31, 2006Assignee: Sterix Ltd.Inventors: Michael John Reed, Barry Victor Lloyd Potter
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Patent number: 7109358Abstract: The invention relates to a process for the preparation of 2H-isoflavones which process comprises the reaction of a 2-hydroxyaryl alkyl ketone in the presence of a base with a formic-sulfuric anhydride salt which reaction is followed by neutralization. The procedure is especially suitable for the preparation of genistein.Type: GrantFiled: April 19, 2002Date of Patent: September 19, 2006Assignee: DSM IP Assets B.V.Inventor: David Carl Burdick
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Patent number: 7060470Abstract: The present invention relates to low and medium molecular weight isoflavone-?-D-glucan produced by submerged liquid culture of Agaricus blazei, a method of producing the isoflavone-?-D-glucan using autolysis enzyme of Agaricus blazei mycelia, and use of the isoflavone-?-D-glucan for anti-cancer and immunoenhancing effect.Type: GrantFiled: July 12, 2004Date of Patent: June 13, 2006Assignee: HK Biotech Co., Ltd.Inventors: Jeong Ok Kim, Yeong Lae Ha, Young Suk Kim, Cherl Woo Park
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Patent number: 7045155Abstract: Compositions enriched with natural phyto-oestrogens or analogues thereof selected from Genistein, Daidzein, Formononetin and Biochanin A. These may be used as food additives, tablets or capsules for promoting health in cases of cancer, pre-menstrual syndrome, menopause or hypercholesterolaemia.Type: GrantFiled: October 21, 2002Date of Patent: May 16, 2006Assignee: Novogen Research Pty Ltd.Inventor: Graham Edmund Kelly
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Patent number: 7012149Abstract: A process is provided for making (?)-epigallocatechin gallate (EGCG) by subjecting a green tea extract to chromatography on a macroporous polar resin, eluting EGCG from the resin with a polar elution solvent, optionally concentrating the eluate, optionally regenerating the resin by desorbing the remaining catechins, and optionally concentrating the desorbed catechins.Type: GrantFiled: September 18, 2002Date of Patent: March 14, 2006Assignee: DSM IP Assets B.V.Inventors: David Carl Burdick, Heinz Egger, Andrew George Gum, Ingo Koschinski, Elena Muelchi, Isabelle Prevot-Halter
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Patent number: 6987098Abstract: Compositions enriched with natural phyto-oestrogens or analogues thereof selected from Genistein, Daidzein, Formononetin and Biochanin A. These may be used as food additives, tablets or capsules for promoting health in cases of cancer, pre-menstrual syndrome, menopause or hypercholesterolaemia.Type: GrantFiled: July 2, 2003Date of Patent: January 17, 2006Assignee: Novogen Research Pty. Ltd.Inventor: Graham Edmund Kelly
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Patent number: 6987125Abstract: Compositions and methods for the treatment, reduction and/or prevention of cardiovascular diseases and disorders are described. Individuals at high risk for developing or having cardiovascular disease or disorder may be treated with an effective dose of a polymethoxyflavone including limocitrin derivatives, quercetin derivatives, naturally occurring polymethoxyflavones, tocotrienols, and mixtures of these compounds.Type: GrantFiled: March 17, 2000Date of Patent: January 17, 2006Assignee: The United States of America as represented by the Secretary of AgricultureInventors: Najla Guthrie, Elzbieta Maria Kurowska, John A. Manthey, Sylvia Horowitz, Robert M. Horowitz
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Patent number: 6987126Abstract: Disclosed is a neutralizing agent for a clostridium bacterial neurotoxin and a preparation method thereof. The neutralizing agent contains a flavonol glycoside (A) or a flavonol glycoside (B). The flavonol glycoside (A) has a flavone skelton which has two hydroxyl groups at the 5 and 7 positions, at least one hydroxyl group bonding at either one of the 3?, 4? and 5? positions, and an ether linkage forming glycoside at the 3 position with a carbohydrate chain containing a rutinose skelton. The flavonol glycoside (B) has also another ether linkage at the 4? position with a carbohydrate chain containing rhamnose. The neutralizing agent is prepared by separating the thearubigin fraction of black tea extract by elution with methanol/water solvent using a reverse phase liquid chromatography. A fraction eluted with methanol/water solvent containing 40% methanol and a fraction eluted with methanol/water solvent containing 60% methanol have high neutralizing activity, and at least one of them is collected.Type: GrantFiled: November 7, 2003Date of Patent: January 17, 2006Assignee: Ito En, Ltd.Inventors: Shin-ichi Sawamura, Masakazu Nishimura, Iwao Sakane
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Patent number: 6977294Abstract: The present invention relates to a process of isolation of bioactive eupalitin (3-O-O-D-galactopyranoside) of formula 1 possessing anti-osteoporosis activity by extraction of powdered leaves of Boerhaavia diffusa, with better yield:Type: GrantFiled: March 13, 2002Date of Patent: December 20, 2005Assignee: Council of Scientific and Industrial ResearchInventors: Deepak Mundkinajeddu, Lila Ram Manahas, Rakesh Maurya, Sukhdev Swami Handa
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Patent number: 6965039Abstract: The invention concerns novel flavone and isoflavone derivatives of formulae (Ia) and (Ib) wherein: X represents a group of formula —COOR, or —PO(OR)2; R represents a hydrogen atom or an alkaline or alkaline-earth metal, or a lower alkyl group; R1 represents a hydroxy group, a lower alkoxy group or an acyloxy group; R2 and R3, identical or different, represent a hydrogen or halogen atom, or a trifluoromethyl group, a trichloromethyl group, a hydroxy group, an alkoxy group or an acyloxy group comprising 1 to 5 carbon atoms, or R2 and R3 can combine to form an alkylene dioxy group. The invention is useful for rheumatic diseases.Type: GrantFiled: October 5, 2001Date of Patent: November 15, 2005Assignee: Negma-LeradsInventors: Jean-Pierre Gesson, Nadia Fonteneau, Martine Mondon, Suzy Charbit, Hervé Ficheux, Francois Schutze
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Patent number: 6960360Abstract: This invention provides a process for the preparation of compositions enriched in total phenols from a crude plant extract. The process includes a novel column purification step using a brominated polystyrene resin. This invention also includes compositions enriched in total phenols. The enriched compositions are characterized as containing monomeric, oligomeric and polymeric phenols and having HPLC chromatograms substantially as set forth in FIGS. 10-13. This invention encompasses methods of using the total phenol-enriched compositions for treating warm-blooded animals, including humans, infected with paramyxovaridae such as respiratory syncytial virus, orthomyoxovaridae such as influenza A, B, and C, parainfluenza, Herpes viruses such as HSV-1 and HSV-2, and Flaviviruses such as West Nile Virus, and for treating inflammation such as caused by arthritis, stress and digestive disease.Type: GrantFiled: November 22, 2002Date of Patent: November 1, 2005Assignee: Phenolics, LLCInventors: Gerald T. Gourdin, Steven L. Richheimer, Michael S. Tempesta, David T. Bailey, Rebecca L. Nichols, F. Joseph Daugherty, Delano R. Freeberg
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Patent number: 6949537Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.Type: GrantFiled: April 5, 2004Date of Patent: September 27, 2005Assignee: Semafore Pharmaceuticals, Inc.Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
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Patent number: 6924376Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: April 11, 2003Date of Patent: August 2, 2005Assignees: Cytokinetics, Inc., Smithkline Beecham CorporationInventors: Andrew McDonald, Gustave Bergnes, Bainian Feng, David J. Morgans, Jr., Steven David Knight, Kenneth A. Newlander, Dashyant Dhanak, Christopher A. Brook
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Patent number: 6916831Abstract: Compounds are described having a structure according to Formula I or Formula II: wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O and S; m is from 1 to 3; n is from 1 to 5; R1 and R3 are each independently selected from the group consisting of H, hydroxy, lower alky, lower alkoxy, halo, amino, aminoalkyl, nitro, heteroaryl, —OC(?O)R6, —O(C?O)OR6; and —O(C?O)N(R6)2; and R2 is side chain such as an acetic acid side chain, where p is O to 4, R5 is hydroxy, alkoxy or amino, and R6 is H or lower alkyl, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer.Type: GrantFiled: February 24, 2003Date of Patent: July 12, 2005Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Yi Xia, Zheng-Yu Yang, Kenneth F. Bastow, Sheng-Chu Kuo
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Patent number: 6849746Abstract: A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.Type: GrantFiled: January 31, 2003Date of Patent: February 1, 2005Assignee: Mars, Inc.Inventors: Leo J. Romanczyk, Jr., Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
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Publication number: 20040266999Abstract: A method for extracting a hydrophobic group-containing water-soluble organic compound, comprising the step of bringing an aqueous solution containing the hydrophobic group-containing water-soluble organic compound and a saccharide into contact with a polar organic solvent to obtain an aqueous phase and an organic phase, whereby the hydrophobic group-containing water-soluble organic compound is transferred to the organic phase. The saccharide concentration of the aqueous solution may be at least 12 g per 100 ml of the aqueous solution. The aqueous solution may further contain a phase separation assisting agent. The phase separation assisting agent may be selected from the group consisting of sodium chloride, sodium citrate, magnesium sulfate, and ammonium sulfate.Type: ApplicationFiled: August 19, 2004Publication date: December 30, 2004Inventors: Takashi Kuriki, Takahisa Nishimura, Kazuhisa Sugimoto
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Publication number: 20040260076Abstract: Methods for the synthesis, isolation, and purification of procyanidin B2 are disclosed. The synthetic methods utilize epicatechin as a starting material and produce procyanidin B2 in high yields. The isolation methods extract procyanidin B2 from a sample of bark powder from plant matter of the genus Uncaria. The isolated and/or synthesized procyanidin B2 is used to treat amyloid disease, such as Alzheimer's disease and Parkinson's disease. Pharmaceutical compositions containing the synthesized and/or isolated procyanidin B2 are also disclosed.Type: ApplicationFiled: October 10, 2003Publication date: December 23, 2004Inventors: Gerardo M. Castillo, Beth P. Nguyen, Paula Y. Choi, Lesley Larsen, Stephen D. Lorimer, Alan D. Snow
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Publication number: 20040254357Abstract: This invention relates to a biologically active formulation containing a conjugate of a fatty acid and a complex phenol. The fatty acid can be selected from a variety of fatty acids including acids have between 12 and 24 carbon atoms. The phenol can be a polynuclear phenol, a polyphenol or a polyfunctional phenol having a variety of substituents. The formulation can include pharmaceutically acceptable carrier, including diluent. The formulation can be provided in an active dosage form suitable to inhibit mammalian cell growth and/or metastasis of malignant cells. The formulation can be used to induce cytotoxicity in mammalian cells particularly tumor cells or to treat and prevent cellular injury or dysfunction.Type: ApplicationFiled: December 19, 2003Publication date: December 16, 2004Inventors: Gary P. Zaloga, Rafat Siddiqui, William Stillwell
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Patent number: 6831098Abstract: A hesperitin pro-form is provided. The invention provides both a hydrophilic and lipophilic hesperetin pro-form. A pharmaceutical composition is provided which is suitable for topical or oral administration in an individual, the composition comprising a hydrophilic hesperetin pro-form and a pharmaceutically acceptable carrier. A pharmaceutical composition is also provided which is suitable for topical or oral administration in an individual, the composition including a lipophilic hesperetin pro-form and a pharmaceutically acceptable carrier. A method is provided for treating a subject having or at risk of having a cell proliferative disorder, including administering to the subject a therapeutically effective amount of a hesperetin pro-form.Type: GrantFiled: February 8, 2002Date of Patent: December 14, 2004Assignee: Zielinski LaboratoryInventor: Jan E. Zielinski
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Publication number: 20040242870Abstract: The invention provides a method, compounds, and compositions for inhibiting the replication or proliferation of a virus. In accordance with the invention, at least one cannabichromene derivative is exposed to the virus, a host cell, or an infected cell under conditions sufficient to inhibit the replication or proliferation of the virus.Type: ApplicationFiled: April 5, 2004Publication date: December 2, 2004Applicant: Immugen Pharmaceuticals, Inc.Inventor: Craig R. Travis
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Publication number: 20040242907Abstract: Simple and efficient total syntheses of flavonoids including baicalein, oroxylin A and wogonin are described herein. Simultaneous syntheses of oroxylin A and wogonin are also described.Type: ApplicationFiled: May 28, 2004Publication date: December 2, 2004Applicant: Unitech Pharmaceuticals, Inc.Inventors: Jiajiu Shaw, An-Rong Lee, Wen-Hsin Huang
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Publication number: 20040235905Abstract: Therapeutically active compounds of formula (I): wherein X is —O—, —CH2— or —C(O)—; Z is —CHR9— or valence bond; Y is —CH2—, —C(O)—, CH(OR10)—, —CH(NR11R12)—, —O—, —S—, —S(O)— or —S(O2)—, provided that in case Z is a valence bond, Y is not C(O); the dashed line represents an optional double bond in which case Z is —CR9— and Y is —CH—, C(OR10)— or —C(NR11R12)—; R1 is —(CH2)nNR4R7 or one of the following groups: n is 1-4; R2 and R3 are independently H, lower alkyl, lower alkoxy, —NO2, halogen, —CF3, —OH, —NHR8 or —COOH, R4 and R7 are independently H, lower alkyl or lower hydroxyalkyl; R5 is H, lower alkoxy, —CF3, —NH2 or —CN; R6 is —NO2, —NR14R19, —CF3 or R8 and R16 are independently H or acyl; R9 is H or lower alkyl; R10 is H, alkylsulfonyl or acyl; R11 and R12 aType: ApplicationFiled: June 8, 2004Publication date: November 25, 2004Inventors: Tuula Koskelainen, Leena Otsomaa, Arto Karjalainen, Pekka Kotovuori, Jukka Tenhunen, Sirpa Rasku, Pentti Nore, Eija Tiainen, Olli Tormakangas
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Publication number: 20040235941Abstract: A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.Type: ApplicationFiled: June 14, 2004Publication date: November 25, 2004Applicant: Mars, IncorporatedInventors: Leo J. Romanczyk, Marc E. Lippman
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Publication number: 20040235902Abstract: A compound represented by the following general formula (I) or a salt thereof: 1Type: ApplicationFiled: June 15, 2004Publication date: November 25, 2004Inventors: Tetsuo Nagano, Kazuya Kikuchi, Tomoya Hirano, Satoko Maruyama
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Patent number: 6818668Abstract: A compound is provided for increasing the concentration of a parent isoflavone in a subject in vivo. The parent isoflavone has a skeletal structure including a 5 position and a 7 position, a 5 alkyl group, and a 7-hydroxy group with a 7-hydroxy oxygen appended to the 7 position and a 7-hydroxy hydrogen appended to the 7-hydroxy oxygen. The compound includes a substrate having the skeletal structure of the parent isoflavone, with a 5 position and a 7 position corresponding to the 5 and 7 positions respectively of the parent isoflavone. An alkyl group is appended to the 5 position. A promoiety is appended to the 7-hydroxy oxygen of the substrate as a substitute for the 7-hydroxy hydrogen of the parent isoflavone, the promoiety and the 7-hydroxy oxygen establishing an alkylcarbonate ester. A related method also is provided.Type: GrantFiled: April 12, 2002Date of Patent: November 16, 2004Assignee: Biotest Laboratories, LLCInventor: William J. Roberts
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Patent number: 6812246Abstract: The invention provides an aminoflavone having formula (I), wherein each of R1 and R2 is H, COCH2—R7, wherein R7 is amino alkylamino, dialkylamino, or alkyl- or dialkylaminoalkyl, or an &agr;-amino acid residue, provided that at least one of R1 or R2 is other than H, and R3 is H, branched or straight-chain alkyl, hydroxyalkyl, alkanoyloxyalkyl, alkanoyloxy, alkoxy, or alkoxyalkyl, or pharmaceutically acceptable salts thereof. The present invention also provides a pharmaceutical composition comprising an aminoflavone as described above, and a method of inhibiting the growth of a tumor in a host by administering a tumor growth-inhibiting amount of an aminoflavone compound having the formula as described above.Type: GrantFiled: June 12, 2003Date of Patent: November 2, 2004Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth M. Snader, B. Rao Vishnuvajjala, Tsutomu Akama
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Publication number: 20040209825Abstract: 3-Deoxyflavonoid compounds and methods for inhibiting T-cell activity and treating diseases and disorders (e.g., autoimmune disorders, inflammatory disorders, diabetes, ALS, MS, rheumatoid arthritis, etc.). In some cases the efficacy and/or duration of action of luteolin and/or other 3-dioxyflavinoid compounds may be increased by administering such compounds along with Rutin, a Rutin congener and/or a Rutin derivative. Also, in some cases, first pass metabolism of luteolin or other 3-deoxyflavinoids may be avoided by administering such compounds by parenteral routes (e.g., sublingual, buccal, intranasal, injection, etc.).Type: ApplicationFiled: May 4, 2004Publication date: October 21, 2004Inventors: Thomas P. Lahey, V.J. Rajadhyaksha
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Publication number: 20040198750Abstract: The present invention relates to compounds useful as inhibitors of protein kinasas. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: March 25, 2004Publication date: October 7, 2004Inventors: Jeremy Green, Alex Aronov, Albert C. Pierce
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Publication number: 20040181068Abstract: The present invention discloses the identification of the novel inhibitors of farnesyl protein transferase and ras protein farnesylation. The compounds and pharmaceutical compositions disclosed herein are useful in treating diseases associated with farnesyl protein transferase, such as cancer.Type: ApplicationFiled: February 10, 2004Publication date: September 16, 2004Inventor: Rajeev S. Bhide
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Patent number: 6780442Abstract: This invention includes both a one-column process and a two-column process for the preparation of compositions enriched for anthocyanins from a crude plant extract. Both processes include a novel column purification step using a brominated polystyrene resin. This invention also includes extracts enriched for anthocyanins.Type: GrantFiled: August 30, 2001Date of Patent: August 24, 2004Assignee: Hauser, Inc.Inventors: David T. Bailey, Delano R. Freeberg, Dennis Gertenbach, Gerald T. Gourdin, Steven L. Richheimer, Michael S. Tempesta, F. Joseph Daugherty
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Patent number: 6774142Abstract: 3-Deoxyflavonoid compounds and methods for inhibiting T-cell activity and treating diseases and disorders (e.g., autoimmune disorders, inflammatory disorders, diabetes, ALS, MS, rheumatoid arthritis, etc.). In some cases the efficacy and/or duration of action of luteolin and/or other 3-dioxyflavinoid compounds may be increased by administering such compounds along with Rutin, a Rutin congener and/or a Rutin derivative. Also, in some cases, first pass metabolism of luteolin or other 3-deoxyflavinoids may be avoided by administering such compounds by parenteral routes (e.g., sublingual, buccal, intranasal, injection, etc.).Type: GrantFiled: September 6, 2002Date of Patent: August 10, 2004Inventors: Thomas P. Lahey, Vithal J. Rajadhyasksha
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Publication number: 20040152762Abstract: A preparation process is provided for preparing a novel flavonoid compound having a high level of antioxidative action. The flavonoid compound is obtained by subjecting hesperidin to microbial fermentation treatment with Aspergillus saitoi.Type: ApplicationFiled: September 10, 2003Publication date: August 5, 2004Inventors: Toshihiko Osawa, Kenichiro Minato, Yoshiaki Miyake
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Patent number: 6770630Abstract: A naringenin derivative of the general formula I: where R1 and R2 each represents either a hydrogen atom or &bgr;-D-glucosyl group, and but both R1 and R2 are not identical.Type: GrantFiled: May 15, 2002Date of Patent: August 3, 2004Assignees: Japan Science and Technology Corporation, National Institute of Agrobiological Sciences, National Food Research InstituteInventors: Kouichi Kashiwaba, Norihiko Tomooka, Duncan A. Vaughan, Akito Kaga, Hiroshi Ono, Mayumi Kameyama, Mituru Yoshida
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Publication number: 20040116717Abstract: This invention relates to a process for isolating (−)-epicatechin from a new plant source namely Dichrostachys cinerea in significant yield.Type: ApplicationFiled: February 24, 2003Publication date: June 17, 2004Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Janaswamy Madhusudana Rao, Rao Jagadeeshwar Rao, Jhillu Singh Yadav, Kondapuram Vijaya Raghavan
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Publication number: 20040116718Abstract: Various processes are disclosed for preparing protected epicatechin oligomers having (4&bgr;,8)-interflavan linkages. In one process, a tetra-O-protected epicatechin monomer or oligomer is coupled with a protected, C-4 activated epicatechin monomer in the presence of an acidic clay such as a mortmorillonite clay. In another process, a 5,7,3′,4′-benzyl protected or a 3-acetyl-, 5,7,3′,4′-benzyl protected epicatechin or catechin monomer or oligomer is reacted with 3-O-acetyl-4-[(2-benzothiazolyl)thio]-5,7,3′,4′-tetra-O-benzylepicatechin in the presence of silver tetrafluoroborate. In another process, two 5,7,3′,4′-benzyl protected epicatechin monomers activated with 2-(benzothiazolyl)thio groups at the C-4 positions are cross-coupled in the presence of silver tetrofluoroborate. A process is also disclosed for reacting an unprotected epicatechin or catechin monomer with 4-(benzylthio) epicatechin or catechin.Type: ApplicationFiled: September 9, 2003Publication date: June 17, 2004Inventors: Alan P. Kozikowski, Werner Tuckmantel, Leo J. Romanczyk