Benzene Ring Bonded Directly To The Hetero Ring (e.g., Flavones, Etc.) Patents (Class 549/403)
  • Publication number: 20080261898
    Abstract: 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: Application
    Filed: April 17, 2008
    Publication date: October 23, 2008
    Inventors: Heather H. Liao, Li Zhan
  • Publication number: 20080254149
    Abstract: 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: Application
    Filed: December 18, 2006
    Publication date: October 16, 2008
    Applicant: BAKTO NATURAL PRESERVATIVES, LLC.
    Inventor: Daphna Havkin-Frenkel
  • Publication number: 20080233242
    Abstract: 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: Application
    Filed: October 8, 2004
    Publication date: September 25, 2008
    Inventors: Ying Zhang, Xiaoqin Wu, Zhuoyu Yu, Dingding Luo, Boyi Lu, Yu Zhang
  • Publication number: 20080194522
    Abstract: 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: Application
    Filed: August 25, 2005
    Publication date: August 14, 2008
    Inventors: Gong Chen, Dominic J. Yee, Niko Gubernator
  • Publication number: 20080188549
    Abstract: 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: Application
    Filed: February 8, 2006
    Publication date: August 7, 2008
    Applicant: Kaneka Corporation
    Inventors: Hozumi Tanaka, Shinichi Yokota, Misuzu Tsukagawa, Tatsumasa Mae, Minpei Kuroda, Yoshihiro Mimaki
  • Publication number: 20080114056
    Abstract: 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: Application
    Filed: June 8, 2005
    Publication date: May 15, 2008
    Inventors: Timothy John Ritchie, Andrew James Culshaw, Terance William Hart, Christopher Thomas Brain, Edward Karol Dziadulewicz
  • Patent number: 7371775
    Abstract: 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: Grant
    Filed: September 4, 2004
    Date of Patent: May 13, 2008
    Assignee: Dong-A Pharmaceuticals Co., Ltd
    Inventors: Moohi Yoo, Dong Sung Kim, Yong Duck Kim, Wonbae Kim
  • Patent number: 7368434
    Abstract: 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: Grant
    Filed: June 27, 2003
    Date of Patent: May 6, 2008
    Assignee: The Endowment for Research in Human Biology, Inc.
    Inventors: Wing Ming Keung, Bert L. Vallee, Guangyao Gao
  • Patent number: 7345090
    Abstract: 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: Grant
    Filed: April 28, 2004
    Date of Patent: March 18, 2008
    Assignee: Merck Patent Gesellschaft mit Beschraenkter Haftung
    Inventors: Frank Pfluecker, Joachim Buenger, Hans-Juergen Driller, Herwig Buchholz, Ralf Rosskopf
  • Patent number: 7329687
    Abstract: 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: Grant
    Filed: April 18, 2003
    Date of Patent: February 12, 2008
    Assignee: SRI International
    Inventors: Nurulain Zaveri, Wan-Ru Chao
  • Patent number: 7326797
    Abstract: 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: Grant
    Filed: July 14, 2003
    Date of Patent: February 5, 2008
    Assignee: DSM IP Assets B.V.
    Inventors: Bruno Burdet, August Ruettimann
  • Publication number: 20080026087
    Abstract: 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: Application
    Filed: June 15, 2004
    Publication date: January 31, 2008
    Inventors: Santiago Rull Prous, Small Alaoui Ismaili, Bernd Fabry
  • Patent number: 7306815
    Abstract: 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: Grant
    Filed: January 23, 2004
    Date of Patent: December 11, 2007
    Assignee: Phenolics, LLC
    Inventors: Gerald T. Gourdin, Steven L. Richheimer, Michael S. Tempesta, David T. Bailey, Rebecca L. Nichols, F. Joseph Daugherty, Delano R. Freeberg
  • Patent number: 7256214
    Abstract: 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: Grant
    Filed: June 18, 2004
    Date of Patent: August 14, 2007
    Assignee: Pokka Corporation
    Inventors: Shigenori Kumazawa, Tsutomu Nakayama, Kayoko Shimoi, Takaki Goto, Syuichi Fukumoto, Tsutomu Arakaki
  • Patent number: 7226644
    Abstract: 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: Grant
    Filed: June 25, 2004
    Date of Patent: June 5, 2007
    Assignee: Dainippon Ink and Chemicals, Inc.
    Inventors: Takashi Matsumoto, Tetsuo Kusumoto, Shotaro Kawakami
  • Patent number: 7129269
    Abstract: 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: Grant
    Filed: December 20, 2002
    Date of Patent: October 31, 2006
    Assignee: Sterix Ltd.
    Inventors: Michael John Reed, Barry Victor Lloyd Potter
  • Patent number: 7109358
    Abstract: 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: Grant
    Filed: April 19, 2002
    Date of Patent: September 19, 2006
    Assignee: DSM IP Assets B.V.
    Inventor: David Carl Burdick
  • Patent number: 7060470
    Abstract: 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: Grant
    Filed: July 12, 2004
    Date of Patent: June 13, 2006
    Assignee: HK Biotech Co., Ltd.
    Inventors: Jeong Ok Kim, Yeong Lae Ha, Young Suk Kim, Cherl Woo Park
  • Patent number: 7045155
    Abstract: 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: Grant
    Filed: October 21, 2002
    Date of Patent: May 16, 2006
    Assignee: Novogen Research Pty Ltd.
    Inventor: Graham Edmund Kelly
  • Patent number: 7012149
    Abstract: 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: Grant
    Filed: September 18, 2002
    Date of Patent: March 14, 2006
    Assignee: DSM IP Assets B.V.
    Inventors: David Carl Burdick, Heinz Egger, Andrew George Gum, Ingo Koschinski, Elena Muelchi, Isabelle Prevot-Halter
  • Patent number: 6987098
    Abstract: 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: Grant
    Filed: July 2, 2003
    Date of Patent: January 17, 2006
    Assignee: Novogen Research Pty. Ltd.
    Inventor: Graham Edmund Kelly
  • Patent number: 6987125
    Abstract: 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: Grant
    Filed: March 17, 2000
    Date of Patent: January 17, 2006
    Assignee: The United States of America as represented by the Secretary of Agriculture
    Inventors: Najla Guthrie, Elzbieta Maria Kurowska, John A. Manthey, Sylvia Horowitz, Robert M. Horowitz
  • Patent number: 6987126
    Abstract: 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: Grant
    Filed: November 7, 2003
    Date of Patent: January 17, 2006
    Assignee: Ito En, Ltd.
    Inventors: Shin-ichi Sawamura, Masakazu Nishimura, Iwao Sakane
  • Patent number: 6977294
    Abstract: 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: Grant
    Filed: March 13, 2002
    Date of Patent: December 20, 2005
    Assignee: Council of Scientific and Industrial Research
    Inventors: Deepak Mundkinajeddu, Lila Ram Manahas, Rakesh Maurya, Sukhdev Swami Handa
  • Patent number: 6965039
    Abstract: 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: Grant
    Filed: October 5, 2001
    Date of Patent: November 15, 2005
    Assignee: Negma-Lerads
    Inventors: Jean-Pierre Gesson, Nadia Fonteneau, Martine Mondon, Suzy Charbit, Hervé Ficheux, Francois Schutze
  • Patent number: 6960360
    Abstract: 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: Grant
    Filed: November 22, 2002
    Date of Patent: November 1, 2005
    Assignee: Phenolics, LLC
    Inventors: Gerald T. Gourdin, Steven L. Richheimer, Michael S. Tempesta, David T. Bailey, Rebecca L. Nichols, F. Joseph Daugherty, Delano R. Freeberg
  • Patent number: 6949537
    Abstract: 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: Grant
    Filed: April 5, 2004
    Date of Patent: September 27, 2005
    Assignee: Semafore Pharmaceuticals, Inc.
    Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
  • Patent number: 6924376
    Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
    Type: Grant
    Filed: April 11, 2003
    Date of Patent: August 2, 2005
    Assignees: Cytokinetics, Inc., Smithkline Beecham Corporation
    Inventors: Andrew McDonald, Gustave Bergnes, Bainian Feng, David J. Morgans, Jr., Steven David Knight, Kenneth A. Newlander, Dashyant Dhanak, Christopher A. Brook
  • Patent number: 6916831
    Abstract: 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: Grant
    Filed: February 24, 2003
    Date of Patent: July 12, 2005
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Kuo-Hsiung Lee, Yi Xia, Zheng-Yu Yang, Kenneth F. Bastow, Sheng-Chu Kuo
  • Patent number: 6849746
    Abstract: 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: Grant
    Filed: January 31, 2003
    Date of Patent: February 1, 2005
    Assignee: Mars, Inc.
    Inventors: Leo J. Romanczyk, Jr., Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
  • Publication number: 20040266999
    Abstract: 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: Application
    Filed: August 19, 2004
    Publication date: December 30, 2004
    Inventors: Takashi Kuriki, Takahisa Nishimura, Kazuhisa Sugimoto
  • Publication number: 20040260076
    Abstract: 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: Application
    Filed: October 10, 2003
    Publication date: December 23, 2004
    Inventors: Gerardo M. Castillo, Beth P. Nguyen, Paula Y. Choi, Lesley Larsen, Stephen D. Lorimer, Alan D. Snow
  • Publication number: 20040254357
    Abstract: 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: Application
    Filed: December 19, 2003
    Publication date: December 16, 2004
    Inventors: Gary P. Zaloga, Rafat Siddiqui, William Stillwell
  • Patent number: 6831098
    Abstract: 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: Grant
    Filed: February 8, 2002
    Date of Patent: December 14, 2004
    Assignee: Zielinski Laboratory
    Inventor: Jan E. Zielinski
  • Publication number: 20040242870
    Abstract: 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: Application
    Filed: April 5, 2004
    Publication date: December 2, 2004
    Applicant: Immugen Pharmaceuticals, Inc.
    Inventor: Craig R. Travis
  • Publication number: 20040242907
    Abstract: 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: Application
    Filed: May 28, 2004
    Publication date: December 2, 2004
    Applicant: Unitech Pharmaceuticals, Inc.
    Inventors: Jiajiu Shaw, An-Rong Lee, Wen-Hsin Huang
  • Publication number: 20040235905
    Abstract: 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 a
    Type: Application
    Filed: June 8, 2004
    Publication date: November 25, 2004
    Inventors: Tuula Koskelainen, Leena Otsomaa, Arto Karjalainen, Pekka Kotovuori, Jukka Tenhunen, Sirpa Rasku, Pentti Nore, Eija Tiainen, Olli Tormakangas
  • Publication number: 20040235941
    Abstract: 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: Application
    Filed: June 14, 2004
    Publication date: November 25, 2004
    Applicant: Mars, Incorporated
    Inventors: Leo J. Romanczyk, Marc E. Lippman
  • Publication number: 20040235902
    Abstract: A compound represented by the following general formula (I) or a salt thereof: 1
    Type: Application
    Filed: June 15, 2004
    Publication date: November 25, 2004
    Inventors: Tetsuo Nagano, Kazuya Kikuchi, Tomoya Hirano, Satoko Maruyama
  • Patent number: 6818668
    Abstract: 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: Grant
    Filed: April 12, 2002
    Date of Patent: November 16, 2004
    Assignee: Biotest Laboratories, LLC
    Inventor: William J. Roberts
  • Patent number: 6812246
    Abstract: 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: Grant
    Filed: June 12, 2003
    Date of Patent: November 2, 2004
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Kenneth M. Snader, B. Rao Vishnuvajjala, Tsutomu Akama
  • Publication number: 20040209825
    Abstract: 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: Application
    Filed: May 4, 2004
    Publication date: October 21, 2004
    Inventors: Thomas P. Lahey, V.J. Rajadhyaksha
  • Publication number: 20040198750
    Abstract: 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: Application
    Filed: March 25, 2004
    Publication date: October 7, 2004
    Inventors: Jeremy Green, Alex Aronov, Albert C. Pierce
  • Publication number: 20040181068
    Abstract: 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: Application
    Filed: February 10, 2004
    Publication date: September 16, 2004
    Inventor: Rajeev S. Bhide
  • Patent number: 6780442
    Abstract: 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: Grant
    Filed: August 30, 2001
    Date of Patent: August 24, 2004
    Assignee: Hauser, Inc.
    Inventors: David T. Bailey, Delano R. Freeberg, Dennis Gertenbach, Gerald T. Gourdin, Steven L. Richheimer, Michael S. Tempesta, F. Joseph Daugherty
  • Patent number: 6774142
    Abstract: 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: Grant
    Filed: September 6, 2002
    Date of Patent: August 10, 2004
    Inventors: Thomas P. Lahey, Vithal J. Rajadhyasksha
  • Publication number: 20040152762
    Abstract: 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: Application
    Filed: September 10, 2003
    Publication date: August 5, 2004
    Inventors: Toshihiko Osawa, Kenichiro Minato, Yoshiaki Miyake
  • Patent number: 6770630
    Abstract: 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: Grant
    Filed: May 15, 2002
    Date of Patent: August 3, 2004
    Assignees: Japan Science and Technology Corporation, National Institute of Agrobiological Sciences, National Food Research Institute
    Inventors: Kouichi Kashiwaba, Norihiko Tomooka, Duncan A. Vaughan, Akito Kaga, Hiroshi Ono, Mayumi Kameyama, Mituru Yoshida
  • Publication number: 20040116717
    Abstract: This invention relates to a process for isolating (−)-epicatechin from a new plant source namely Dichrostachys cinerea in significant yield.
    Type: Application
    Filed: February 24, 2003
    Publication date: June 17, 2004
    Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH
    Inventors: Janaswamy Madhusudana Rao, Rao Jagadeeshwar Rao, Jhillu Singh Yadav, Kondapuram Vijaya Raghavan
  • Publication number: 20040116718
    Abstract: 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: Application
    Filed: September 9, 2003
    Publication date: June 17, 2004
    Inventors: Alan P. Kozikowski, Werner Tuckmantel, Leo J. Romanczyk