Carbocyclic Ring Bonded Directly To The Hetero Ring Of The Bicyclo Ring System (e.g., Flavanes, Etc.) Patents (Class 549/406)
  • Publication number: 20110033564
    Abstract: The present invention relates to an extract obtained by extracting useful components containing equol from an equol-containing fermented soybean hypocotyl, and to a method for producing the same. The present invention makes it possible to efficiently obtain useful components containing equol from the fermented soybean hypocotyl by subjecting an equol-containing fermented soybean hypocotyl to extraction using an ethanol aqueous solution as an extractant. The present invention reduces the content of saponin, which causes an unpleasant taste, by sequentially subjecting the equol-containing fermented soybean hypocotyl to extraction using an ethanol aqueous solution and ethanol, while efficiently extracting equol and glycitein.
    Type: Application
    Filed: June 13, 2008
    Publication date: February 10, 2011
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD
    Inventors: Michiaki Tominaga, Takao Taki, Toshiaki Matsumoto, Izumi Hanya, Takuma Imada, Kunihiko Matsuoka, Takuya Kishimoto, Yuko Uchiyama, Hiromasa Tsuneishi, Machiko Tsuji, Tania Valdes-Gonzalez, Kentaro Tadano, Kyoko Kameda
  • Patent number: 7875736
    Abstract: Disclosed herein is a compound of formula (I): wherein: Bn represents benzyl; Me represents methyl; and Y represents an oxygen atom or a CH2 group. The compound of formula (I) can be used in the preparation of 7-benzyloxy-3-(4-methoxyphenyl)-2H-1-benzopyran, Preparation processes of said compound of formula (I) are also disclosed herein.
    Type: Grant
    Filed: May 19, 2009
    Date of Patent: January 25, 2011
    Assignee: KaoHsiung Medical University
    Inventors: Eng-Chi Wang, Sie-Rong Li
  • Patent number: 7875735
    Abstract: Disclosed herein are processes for the preparation of isoflavonoids, in particular haginin E, equol, daidzein, formononetin and the like, in which 7-benzyloxy-3-(4-methoxyphenyl)-2H-1-benzopyran is used as a common starting material.
    Type: Grant
    Filed: May 19, 2009
    Date of Patent: January 25, 2011
    Assignee: KaoHsiung Medical University
    Inventors: Eng-Chi Wang, Sie-Rong Li
  • Patent number: 7872042
    Abstract: The present invention provides methods for elevating IKBKAP gene expression and the level of functional IKAP protein in cells, which are beneficial to human individual, such as an individual suffering from Familial Dysautonomia, by providing one or more tocotrienols alone or in combination with one or more tocopherols to the cells. The present invention also provides methods for treating Familial Dysautonomia by providing tocotrienols alone or in combination with one or more tocopherols to a patient having Familial Dysautonomia. Related therapeutic kits are also provided.
    Type: Grant
    Filed: May 13, 2005
    Date of Patent: January 18, 2011
    Inventors: Berish Y. Rubin, Sylvia L. Anderson
  • Publication number: 20100305313
    Abstract: The present invention relates to a process for the extraction of plant ingredients, which comprises a) comminuting plant material b) adding a solvent to the comminuted plant material c) subjecting the mixture of comminuted plant material and solvent to an ultrahigh temperature treatment at 95-150° C. over a period of 5-300 seconds.
    Type: Application
    Filed: December 16, 2008
    Publication date: December 2, 2010
    Applicant: Bayer CropScience AG
    Inventors: Michael Baeuerlein, Joseph Miller
  • Publication number: 20100297272
    Abstract: The invention relates to a cosmetic composition containing lingonberry extract and its use on skin cosmetology thereof. The present invention has provided a lingonberry extract wherein containing polyphenols components including anthocyanidin, procyanidin, resveratrol, catechin and so on. The present invention also relates to the application of lingonberry extract on skin cosmetology, including without limitation whitening, diminishing visible pigmentation, anti-wrinkle, moisturizing, smoothing and improving skin sensitivity. The invention also has revealed drugs, cosmetic composition and food prepared by using lingonberry extract. Comparing with the prior art cosmetic compositions, the said lingonberry extract of the present invention has higher effects and safe.
    Type: Application
    Filed: April 10, 2008
    Publication date: November 25, 2010
    Applicant: Beijing Gingko Group Biological Technology Co., Ltd.
    Inventors: Chunhua Li, Yanmei Li
  • Publication number: 20100298581
    Abstract: Disclosed herein are processes for the preparation of isoflavonoids, in particular haginin E, equol, daidzein, formononetin and the like, in which 7-benzyloxy-3-(4-methoxyphenyl)-2H-1-benzopyran is used as a common starting material.
    Type: Application
    Filed: May 19, 2009
    Publication date: November 25, 2010
    Applicant: KaoHsiung Medical University
    Inventors: Eng-Chi Wang, Sie-Rong Li
  • Publication number: 20100280231
    Abstract: An object of the present invention is to provide a whitening agent containing a novel whitening substance as an effective ingredient. The above object is attained by providing a whitening agent containing equol and/or equol glycoside, in which one or more glycosyl groups bind to the hydroxyl group(s) of equol, as an effective ingredient.
    Type: Application
    Filed: April 3, 2008
    Publication date: November 4, 2010
    Inventors: Masayuki Nakano, Takashi Shibuya, Masaki Miyake, Norie Arai
  • Publication number: 20100151379
    Abstract: The present invention provides a compound represented by the formula (I): wherein P1, P2, P3, P4 and P5 each independently represents a hydrogen atom etc., and at least one selected from the group consisting of R1, R2, R3, R4, R5, R6, R7, R8 and R9 is the group represented by the formula (II): wherein X1 and X2 each independently represent a hydrogen atom etc., n represents an integer of 1 to 4, Z1 represents a C1-C6 alkyl group etc., and ring Y represents an alicyclic hydrocarbon group, and the others each independently represent a hydrogen atom, a C1-C6 alkyl group or a hydroxyl group, and a chemically amplified resist composition containing the same.
    Type: Application
    Filed: December 4, 2009
    Publication date: June 17, 2010
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Ichiki Takemoto, Nobuo Ando
  • Publication number: 20100152284
    Abstract: Provided herein are methods for treating or preventing neuropathy, neuropathy-related conditions, wherein the neuropathy or neuropathy-related conditions are induced by, or otherwise associated with, treatment of the subject with at least one chemotherapeutic agent, the methods comprising administering an effective amount of an isoflavonoid compound of formula (I). Also provided are methods for the treatment of nerve damage. Also provided are uses of isoflavonoid compounds of formula (I) in the treatment of neuropathy, neuropathy-related conditions and nerve damage.
    Type: Application
    Filed: October 30, 2007
    Publication date: June 17, 2010
    Applicant: NOVOGEN RESEARCH PTY LTD
    Inventors: David Brown, Alan James Husband, Ann M. Turnley
  • Publication number: 20100121084
    Abstract: The present invention relates to a coloring food composition containing modified colorings of the anthocyanin family and to a process for the bathochromic modification of these colorings. This coloring composition can be used as additive or ingredient in food preparations.
    Type: Application
    Filed: March 17, 2008
    Publication date: May 13, 2010
    Applicant: DIANA NATURALS
    Inventors: Claude Inisan, Matthieu Besnard, Cecile Bahu, Denis Megard
  • Patent number: 7696363
    Abstract: Disclosed is an improved method for preparing the isoflavonoid compound (+/?)-equol, the method comprising reducing an organic diester of the isoflavone daidzein under hydrogen-transfer conditions using palladium hydroxide catalyst.
    Type: Grant
    Filed: December 4, 2006
    Date of Patent: April 13, 2010
    Assignee: Yasoo Health Inc.
    Inventor: John A. Hyatt
  • Publication number: 20100069653
    Abstract: A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.
    Type: Application
    Filed: May 4, 2009
    Publication date: March 18, 2010
    Applicants: CHILDREN HOSPITAL MEDICAL CENTER, GIRINDUS AMERICA, INC.
    Inventors: Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
  • Publication number: 20100041746
    Abstract: The present invention refers to compounds of the general formulae Ia to Ie as defined above for use as/in a composition (especially foods and dietary supplements, cosmetic, as well as pharmaceutical compositions) for the prevention and improvement of muscular disorders and for the improvement of muscle function.
    Type: Application
    Filed: May 24, 2007
    Publication date: February 18, 2010
    Inventors: Daniel D'Orazio, Daniel Raederstorff, Goede Schueler, Ying Wang-Schmidt, Karin Wertz, Swen Wolfram
  • Patent number: 7648742
    Abstract: The invention relates to compounds of formula (I), wherein a, b, c, d, e, R1, R2, A1, A2, A3, A4, Y1, Y2, Y3, Z1, Z2, Z3, Z4 and are such as defined in claim 1, to a method for the production thereof, intermediates for the production and the thereof in the form of components in liquid crystalline media and to electrooptic display elements containing said liquid crystalline media.
    Type: Grant
    Filed: July 5, 2005
    Date of Patent: January 19, 2010
    Assignee: Merck Patent GmbH
    Inventors: Andreas Taugerbeck, Melanie Klasen-Memmer
  • Publication number: 20090263509
    Abstract: The problems to be solved by the invention are to provide antibacterial agents originated from natural products that are safe for regular use with potent antibacterial activity, and antibacterial compositions containing said antibacterial agents. Antibacterial agents containing Eysenhardtia adenostylis extract or isoflavan compounds are a solution to the problem. Also antibacterial agents containing Eysenhardtia adenostylis extract or isoflavan compounds as active ingredients. The antibacterial agents can be applied to products such as cosmetics, including quasi-drugs, pharmaceuticals and foods. Further, antibacterial compositions containing these antibacterial agents, Eysenhardtia adenostylis extract or isoflavan compounds, and other compositions such as cosmetics, including quasi-drugs, pharmaceuticals and foods.
    Type: Application
    Filed: February 25, 2005
    Publication date: October 22, 2009
    Applicant: SAKAMOTO BIO CO., LTD
    Inventors: Kenji Sakamoto, Toshiyuki Mukaiyama, Kazuyuki Hori, Saori Takahashi
  • Publication number: 20090233913
    Abstract: The present invention relates to dihydro-2,3-benzodiazepine compounds of high enantiomeric purity according to the general formula (I), which contain an asymmetric centre at the position 4 of the dihydro-2,3-benzodiazepine compound, and the preparation thereof and the used intermediates as well. These compounds have anti-convulsiveA muscle relaxant and neuroprotective effect due their non-competitive AMPA antagonistic properties.
    Type: Application
    Filed: December 29, 2006
    Publication date: September 17, 2009
    Inventors: Istvan Ling, Jozsef Barkoczy, Zoltan Greff, Gabor Szenasi, Gabor Gigler, Szabolcs Kertesz, Gyula Szucs, Mihaly Albert, Gabor Kapus, Geza Szabo, Miklos Vegh, Marta Agoston, Gyorgy Levay, Krisztina Moricz, Laszlo Gabor Harsing
  • Patent number: 7531646
    Abstract: This invention provides a method of detecting enzyme activity on a solid medium. The enzyme substrate has a chromogenic portion comprising a catechol residue, in which a derivitising moiety is linked to the aromatic ring of the catechol via a bond, and an enzyme cleavable group which is attached via an ester or ether linkage to the oxygen atom derived from a hydroxyl group of the catechol residue. If the enzyme substrate contacts an enzyme capable of cleaving the enzyme cleavable groups and the cleaved compound contacts a chelatable metal ion, a substantially non-diffusable coloured precipitate is formed.
    Type: Grant
    Filed: October 24, 2002
    Date of Patent: May 12, 2009
    Inventor: Michael Burton
  • Patent number: 7528267
    Abstract: A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.
    Type: Grant
    Filed: August 1, 2005
    Date of Patent: May 5, 2009
    Assignees: Girindus America, Inc., Children's Hospital Medical Center
    Inventors: Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
  • Patent number: 7524975
    Abstract: The present invention easily and efficiently provides a peroxisome proliferator-activated receptor ligand, and a composition for amelioration of insulin resistance or for prevention and/or amelioration of the insulin resistance syndrome containing the same, as an active ingredient. The present invention relates to a peroxisome proliferator-activated receptor ligand which comprises a prenylflavonoid, a chalcone derivative exclusive of prenylflavonoids, a flavonol derivative exclusive of prenylflavonoids, and a salt, a glycoside and/or an esterified substance thereof acceptable as a pharmaceutical preparation or a food or a beverage; a composition containing the above ligand; a plant-derived extract containing the above ligand; and a process for producing the above extract.
    Type: Grant
    Filed: October 11, 2002
    Date of Patent: April 28, 2009
    Assignee: Kaneka Corporation
    Inventors: Tatsumasa Mae, Misuzu Tsukagawa, Mikio Kitahara, Kaku Nakagawa, Shiro Kitamura, Yasuyoshi Ueda, Minpei Kuroda, Yoshihiro Mimaki, Yutaka Sashida
  • Patent number: 7514461
    Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondrial disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.
    Type: Grant
    Filed: September 15, 2004
    Date of Patent: April 7, 2009
    Assignee: Edison Pharmaceuticals, Inc.
    Inventors: Bing Wang, Gail Walkinshaw, Sekhar Boddupalli, Arkadij M. Elizarov, Xianming Jin, Xianfeng Li, Donald R. James, Jiangao Song, Jian Chen, Wei Zhang
  • Patent number: 7488494
    Abstract: Isoflavone compounds are described and recommended as therapeutic agents. Exemplified and preferred compounds are (a). Indications show compounds have good competitive binding to estrogen receptors.
    Type: Grant
    Filed: November 7, 2003
    Date of Patent: February 10, 2009
    Assignee: Novogen Research Pty Ltd.
    Inventors: Andrew Heaton, Naresh Kumar, Graham Edmund Kelly, Alan Husband
  • Patent number: 7485735
    Abstract: A process is described for selectively extracting cocoa procyanidins from an aqueous mixture of cocoa polyphenols by using a particular sequence of solvents to extract selected procyanidin monomers and/or oligomers. The solvents are n-butyl acetate, ethyl acetate, methyl acetate, diethyl ether, or mixtures of methyl acetate and diethyl ether. Preferably, the aqueous mixture of cocoa polyphenols is first extracted with n-butyl acetate. The mixtures of methyl acetate and diethyl ether are between 25:75 and 75:25 (v/v).
    Type: Grant
    Filed: October 3, 2005
    Date of Patent: February 3, 2009
    Assignee: Mars, Inc.
    Inventors: Rebecca J. Robbins, John P. Munafo, Mark A. Kelm
  • Patent number: 7435722
    Abstract: A method of improving the resistance of collagenous tissue to mechanical degradation in accordance with the present invention comprises the step of contacting at least a portion of a collagenous tissue with an effective amount of a crosslinking reagent. Methods and devices for enhancing the body's own efforts to stabilize discs in scoliotic spines by increasing collagen crosslinks. This stability enhancement is caused by reducing the bending hysteresis and increasing the bending stiffness of scoliotic spines, by injecting non-toxic crosslinking reagents into the convex side of discs involved in the scoliotic curve. Alternatively, contact between the tissue and the crosslinking reagent is affected by placement of a time-release delivery system directly into or onto the target tissue.
    Type: Grant
    Filed: February 24, 2004
    Date of Patent: October 14, 2008
    Assignee: University of Southern California
    Inventor: Thomas P. Hedman
  • Patent number: 7432297
    Abstract: A compound of the following formula (I) or (II) (in the formula (I), n represents an integer of 0 to 2) (in the formula (II), m represents an integer of 0 to 2).
    Type: Grant
    Filed: January 12, 2006
    Date of Patent: October 7, 2008
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Tatsumi Nuno, Tomokazu Nakamura
  • Patent number: 7429411
    Abstract: The compound (1) according to the invention has general solid-state properties necessary for a compound, stability against heat, light and the like, a suitable optical anisotropy, a suitable dielectric anisotropy, and excellent compatibility with other liquid crystalline compounds. The liquid crystal composition according to the invention contains at least one compound represented by formula (1). The liquid crystal display element according to the invention contains the composition. The compound (1) is represented by formula (1): wherein Ra, Rb, A1, A2, A3, A4, A5, A6, Z11, Z12, Z13, Z14, Z15, Z16, Y1, Y2, k, l, m, n, p and q are as defined in the specification.
    Type: Grant
    Filed: June 23, 2004
    Date of Patent: September 30, 2008
    Assignees: Chisso Petrochemical Corporation, Chisso Corporation
    Inventors: Teruyo Sugiura, Makoto Ushioda
  • Patent number: 7427686
    Abstract: The present invention relates to compounds of the formula I in which substituents R2 and R3 are arranged in trans-configuration: wherein: R1 is H or C1-C6 alkyl; C3-C7 cycloalkyl; R2 is phenyl, optionally substituted with 1 to 5 substituents independently selected from the group comprising OH, C1-C6-alkyl, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkoxy and phenyl, wherein R4 is C1-C6 alkyl; R3 is phenyl substituted with OR5 wherein R5 has the formula (II), (III) or (IV) wherein Y is chosen from NHR4, NR42, NHCOR4, NHSO2R4, CONHR4, CONR4, CONR42, COOH, COOR4, SO2R4, SOR4, SONHR4, SONR42, a C3-C7 heterocyclic ring, saturated or unsaturated, containing one or two heteroatoms independently selected from the group consisting of O, S and N, optionally being substituted with 1 to 3 substituents independently selected from the group comprising H, OH, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkyl and C1-C6-alkoxy, preferably NHR4, NR24, or a nitrogen heterocycle, wh
    Type: Grant
    Filed: September 30, 2003
    Date of Patent: September 23, 2008
    Assignee: Counsel of Scientific and Industrial Research
    Inventors: Sangita, Atul Kumar, Man Mohan Singh, Suprabhat Ray, Girish Kumar Jain
  • Patent number: 7365113
    Abstract: Flavan-based and spirodichroman compound-based phosphate esters prepared by reacting flavans and spirodichroman compounds with phosphorus oxychloride, monophenyl dichlorophosphate, or diphenyl chlorophosphate compounds are described. The flavans and spirodichroman compounds can be synthesized by the reaction of resorcinol with aliphatic acetone. Such phosphate esters can be used as flame retardants.
    Type: Grant
    Filed: September 21, 2005
    Date of Patent: April 29, 2008
    Inventors: Raj B. Durairaj, Gary A. Jesionowski
  • Publication number: 20080085263
    Abstract: the present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.
    Type: Application
    Filed: June 6, 2005
    Publication date: April 10, 2008
    Inventors: Krister Thuresson, Fredrik Tiberg, Markus Johansson, Ian Harwigsson, Fredrik Joabsson
  • Patent number: 7332260
    Abstract: The present invention relates to novel compounds of the naphthopyran type which have an annelated carbocycle in position 5,6. These compounds are of formula (I) given below: in which A is an alicyclic ring which is optionally annelated with an aromatic ring and in which two adjacent R3 can together form at least one ring, for example a benzo group. These compounds (I) possess interesting photochromic properties. The invention also relates to the method of preparing these compounds (I), as well as their applications as photochromes and compositions and (co)polymer matrices comprising them.
    Type: Grant
    Filed: July 16, 2002
    Date of Patent: February 19, 2008
    Assignee: Corning Incorporated
    Inventors: Olivier Breyne, You-Ping Chan, Patrick Jean
  • Patent number: 7312344
    Abstract: A compound of the general formula (I) or (II) wherein X is O, NR4 or S and R1-R8 are as defined in the specification
    Type: Grant
    Filed: March 8, 2002
    Date of Patent: December 25, 2007
    Assignee: Novogen Research Pty Limited
    Inventors: Andrew Heaton, Graham Edmund Kelly, Naresh Kumar
  • Patent number: 7282598
    Abstract: Processes are disclosed for the production of linear and branched procyanidin oligomers having “n” procyanidin monomeric units where n is 2 to 18. The processes include coupling protected, activated monomers with an unprotected monomer to produce a partially protected (4?8) dimer. The dimer is optionally blocked, coupled with an activated protected monomer to produce a partially protected, optionally blocked trimer, and deprotected. The steps can be repeated to produce higher oligomers. Processes are also provided for producing (8?8), (8?6), and (6?6) dimers and doubly branched oligomers. Crystalline 8-bromo tetra-O-benzyl (?)-epicatechin is produced under certain conditions.
    Type: Grant
    Filed: March 11, 2004
    Date of Patent: October 16, 2007
    Inventors: Leo J. Romanczyk, Jr., Amit Basak, Craig A. Townsend
  • Patent number: 7250120
    Abstract: Disclosed are novel benzo-, naphtho- and phenanthrochromenes substituted by carbamated or ureated phenyls having the following general formula (I): wherein R1 represents a group their preparation, photochromic compositions and articles containing them. This family of compounds have interesting and useful photochromic properties, especially in terms of absorption band and discoloration speed.
    Type: Grant
    Filed: June 14, 2004
    Date of Patent: July 31, 2007
    Assignee: Corning Inc.
    Inventors: You-Ping Chan, Olivier Breyne
  • Patent number: 7247355
    Abstract: The present invention relates to a compound having a chroman ring, which has good thermal and optical stability, adequate optical anisotropy, adequate dielectric anisotropy and superior compatibility with other liquid crystal compounds, a liquid crystal composition comprising the compound, and a liquid crystal device comprising the composition.
    Type: Grant
    Filed: December 16, 2005
    Date of Patent: July 24, 2007
    Assignees: Chisso Corporation, Chisso Petrochemical Corporation
    Inventors: Kouki Sagou, Atsuko Fujita
  • 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: 7202247
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.
    Type: Grant
    Filed: December 19, 2002
    Date of Patent: April 10, 2007
    Assignee: AtheroGenics, Inc.
    Inventors: James A. Sikorski, Charles Q. Meng, M. David Weingarten
  • Patent number: 7126014
    Abstract: Oligomeric procyanidins containing 4?-linked epicatechin units are rare in nature and have hitherto not been accessible through stereoselective synthesis. Provided herein is the preparation of the prototypical dimer, epicatechin-4?,8-epicatechin, by reaction of the protected 4-ketones with aryllithium reagents derived by halogen/metal exchange from the aryl bromides. Removal of the 4-hydroxyl group from the resulting tertiary benzylic alcohols is effected by tri-n-butyltin hydride and trifluoroacetic acid in a completely stereoselective manner, resulting in hydride delivery exclusively from the ? face.
    Type: Grant
    Filed: February 20, 2004
    Date of Patent: October 24, 2006
    Inventors: Alan P. Kozikowski, Leo J. Romanczyk, Jr., Werner Tückmantel
  • Patent number: 7102020
    Abstract: The present invention provides a method to prepare 2H-benzo[6]pyrans, such as the anti-HIV natural product daurichromenic acid (1a), by microwave-assisted tandem aldol reaction of a phenolic enolate followed by intramolecular SN2? type cyclization to form the 2H-benzo[6]pyran core structure.
    Type: Grant
    Filed: December 18, 2003
    Date of Patent: September 5, 2006
    Inventors: Zhendong Jin, Ying Kang
  • Patent number: 7045514
    Abstract: Provided herein is a compound having the formula (I): Wherein said compounds are useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B and 5HT1D antagonists.
    Type: Grant
    Filed: July 12, 2004
    Date of Patent: May 16, 2006
    Assignee: AstraZeneca AB
    Inventors: Edward Pierson, Daniel Sohn, Markus Haeberlein, Timothy Davenport, Marc Chapdelaine, Carey Horchler, John P. McCauley
  • 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: 7009062
    Abstract: The invention relates to a process for the preparation of flavone derivatives in which a 2-hydroxyacetophenone compound is metallated using a lithium compound at low temperatures and subsequently reacted with a keto compound, and where the ratio of the molar equivalents of lithium compound to the 2-hydroxyacetophenone compound functional groups to be metallated is from 1 to 1.2. The resultant ?-diketone compound is subsequently cyclized with warming in an acidic medium.
    Type: Grant
    Filed: January 12, 2002
    Date of Patent: March 7, 2006
    Assignee: Merck Patent GmbH
    Inventors: Herwig Buchholz, Sophie Perruchon
  • 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: 6951883
    Abstract: 2H-1-Benzopyran derivatives, processes for their preparation and use thereof for the preparation of pharmaceutical compositions for the prevention and treatment of postmenopausal pathologies.
    Type: Grant
    Filed: January 21, 2002
    Date of Patent: October 4, 2005
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Maurizio Delcanale, Gabriele Amari, Elisabetta Armani, Maurizio Civelli, Elisabetta Galbiati
  • Patent number: 6849649
    Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.
    Type: Grant
    Filed: October 28, 2003
    Date of Patent: February 1, 2005
    Assignee: Pfizer Inc.
    Inventors: Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
  • 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
  • Patent number: 6849646
    Abstract: The invention relates to compounds having formula (I), wherein R1, R2, R3, R4, R5, R7, R8, R11, Z, m and n have the meaning cited in claim 1, and to the physiologically acceptable salts and solvates which can be used as integrin inhibitors, especially in the prophylaxis and treatment of circulatory diseases, in case of thrombosis, myocardial infarction, coronary heart diseases, arteriosclerosis, osteoporosis, pathologic processes caused or propagated by angiogenesis and in tumor therapy.
    Type: Grant
    Filed: October 14, 1999
    Date of Patent: February 1, 2005
    Assignee: Merck Patent GmbH
    Inventors: Claus Fittschen, Simon Goodman, Joachim März, Peter Raddatz, Matthias Wiesner
  • Patent number: 6844336
    Abstract: This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I, in which Z is a straight-chain or branched-chain alkyl group with up to 5 carbon atoms that is fluorinated in at least one place, preferably a trifluoromethyl group, and R1, R2, X, Y and n have the meanings that are indicated in the description. The new compounds have at their disposal strong antiestrogenic action. In addition, they can have at their disposal estrogenic action that occurs in a tissue-selective manner. They can be used for the production of pharmaceutical agents, especially for the treatment of estrogen-dependent diseases and tumors and pharmaceutical agents for hormone replacement therapy (HRT) as well as for the prevention and treatment of osteoporosis.
    Type: Grant
    Filed: March 15, 2001
    Date of Patent: January 18, 2005
    Assignee: Schering AG
    Inventors: Hermann Kuenzer, Rolf Jautelat, Ludwig Zorn, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier
  • Publication number: 20040236123
    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: May 28, 2004
    Publication date: November 25, 2004
    Applicant: M&M/Mars Inc.
    Inventors: Leo J. Romanczyk, Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
  • Publication number: 20040224906
    Abstract: Water soluble antioxidant composition derived from natural sources having less than 10 ppm chlorinated hydrocarbons, less than 0.5% by weight fat, at least 15% by weight in total polyphenolic antioxidants, less than 5% by weight purine components, less than 0.5% by weight caffeine, and a Trolox Equivalent Antioxidant Capacity value of at least 0.4. The composition is suitable for use in pharmaceuticals, cosmetic, and nutritional compositions.
    Type: Application
    Filed: June 7, 2004
    Publication date: November 11, 2004
    Inventors: Hendrik Derk Hoving, Hans Robert Kattenberg, Dick Antonius Johannes Starmans
  • Patent number: RE40792
    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: May 19, 1993
    Date of Patent: June 23, 2009
    Assignee: Novogen Research Pty Ltd
    Inventor: Graham Edmund Kelly