Plural Chalcogens Bonded Directly To The Hetero Ring Patents (Class 549/400)
  • Publication number: 20090054518
    Abstract: A ampelopsin salt, its derivatives preparation and application are new. The ampelopsin salt being formed by substituting a monovalent cation for hydrogen atom on the ampelopsin, and the said substitution is a unsaturated substitution, is prepared by the reaction of ampelopsin with salify agent, and which is used for preparing antitumour medicine, and combined with other antitumour medicine thus reduce side effect of other antitumour medicine.
    Type: Application
    Filed: March 31, 2006
    Publication date: February 26, 2009
    Inventor: Fulin Fan
  • Publication number: 20090007292
    Abstract: A maize inbred line having the characteristics selected from those of FAR045, including plant parts, tissue, and pigments of the inbred is disclosed.
    Type: Application
    Filed: June 20, 2008
    Publication date: January 1, 2009
    Inventor: Lee K. French
  • Publication number: 20080286360
    Abstract: A chemically patterned modified hydrogel formed from a modified hydrogel is provided. The hydrogel is conjugated with a multiphoton photocleavable molecule. The molecule has a multiphoton-labile protective group and a protected group. The protective group is cleavable upon multiphoton excitation to deprotect the protected group, without substantial polymerization of the hydrogel. The chemically patterned modified hydrogel is formed by exposing the modified hydrogel to multiphoton excitation to deprotect a portion of the protected groups.
    Type: Application
    Filed: April 7, 2008
    Publication date: November 20, 2008
    Inventors: Molly Shoichet, Jordan Wosnick, Ryan Wylie
  • Publication number: 20080280335
    Abstract: Disclosed is a kaempferol preparing method comprising isolating kaempferol from kaempferol glucosides using an acid, a base, an enzyme or a microbe producing the enzyme. More specifically, the method comprises obtaining a plant extract containing kaempferol glycosides from a plant using water or an organic solvent; and hydrolyzing the plant extract using an acid, a base, an enzyme or a microbe producing the enzyme to isolate kaempferol. The kaempferol glycosides comprise camelliaside A or camelliaside B. The plant extract is derived from a seed or leaf of green tea. When using the method of the invention, it is possible to mass-produce kaempferol, which is one of main physiological activating ingredients, from a plant, particularly a seed or leaf of green tea.
    Type: Application
    Filed: May 30, 2005
    Publication date: November 13, 2008
    Applicant: AMOREPACIFIC CORPORATION
    Inventors: Myeong Hoon Yeom, Jun-seong Park, Won-Seok Park, Kyungmi Joo, Ho Sik Rho, Duck Hee Kim, Ih Seop Jang, Ok-Sub Lee
  • Publication number: 20080214844
    Abstract: The antiproliferative effects of Icaritin or Desmethylicaritin on cancer cell lines, both in vitro, and in vivo, are disclosed. Experimental data show that Icaritin and Desmethylicaritin dramatically inhibit the growth of most malignant cells. In addition, both Icaritin and Desmethylicaritin have significant Anti-agiogenesis properties, inhibiting or eliminating entirely the development of new malignant cells. Further, no obvious side effects including nausea, hair loss or body weight loss were found in the animals treated with Icaritin or Desmethylicaritin, making both highly effective anti cancer drugs.
    Type: Application
    Filed: January 23, 2007
    Publication date: September 4, 2008
    Inventors: Nan Zhang, Stuart K. Calderwood
  • Patent number: 7396856
    Abstract: Novel benzopyran analogs are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.
    Type: Grant
    Filed: May 6, 2005
    Date of Patent: July 8, 2008
    Assignee: Alcon, Inc.
    Inventors: Mark R. Hellberg, Abdelmoula Namil
  • Publication number: 20080153872
    Abstract: Certain bis-(coumarin) compounds as well as the products of their intramolecular cyclization including pharmaceutically acceptable salts, hydrates, solvates, clathrates, prodrugs, tautomers and stereoisomers thereof are disclosed. Certain processes and intermediates for the preparation of certain bis-(coumarin) compounds, as well as for the use of these compounds as therapeutically active agents in the prophylaxis and treatment of asthma and other inflammatory diseases and conditions in mammals, especially humans are also disclosed.
    Type: Application
    Filed: January 13, 2006
    Publication date: June 26, 2008
    Inventors: Mladen Mercep, Ivica Malnar, Boska Hrvacic, Stribor Markovic, Anita Filipovic Sucic, Berislav Bosnjak, Andreja Cempuh Klonkay, Renata Rupcic, Antun Hutinec, Ivaylo Jivkov Elenkov, Milan Mesic
  • Publication number: 20080146657
    Abstract: The present inventors produced lotus leaf extracts, and discovered that quercetin is one of the active ingredients. As a result of treating ?3-adrenergic receptor-expressing cells and feeding diabetes model mice with quercetin and evaluating its effects, the present inventors discovered specifically that quercetin produces obesity-improving effects and antidiabetic effects by acting as a ?3-adrenergic receptor agonist.
    Type: Application
    Filed: November 4, 2004
    Publication date: June 19, 2008
    Inventors: Hiroshi Tsuboi, Shuji Ikegami, Tomonori Kamiyama, Zai-si Ji, Yukio Asami, Hiroyuki Itou, Munehiro Oda, Kazuo Shin
  • 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: 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: 7067679
    Abstract: Various processes are disclosed for preparing protected epicatechin oligomers having (4?,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: Grant
    Filed: September 9, 2003
    Date of Patent: June 27, 2006
    Inventors: Alan P. Kozikowski, Werner Tückmantel, Leo J. Romanczyk, Jr.
  • Patent number: 7056952
    Abstract: There are disclosed compounds of formulae (I) or (II) in which A is selected from the group consisting of (1), (2), (3) and (4); OH, and one of R1 and R2 is selected from H, OH and OCH3, and the other of R1 and R2 is selected from OH and OCH3; one of R3 and R4 is selected from H, OH and OCH3, and the other of R3 and R4 is selected from OH and OCH3; provided that at least one of the pairs R1, R2 and R3, R4 are both OH; R5 is selected from OH and OCH3; and denotes a single or double bond; and pharmaceutically acceptable salts and prodrugs thereof. The compounds of the invention are useful for the treatment of hormone-dependent conditions and cancers.
    Type: Grant
    Filed: May 1, 2000
    Date of Patent: June 6, 2006
    Assignee: G.J. Consultants Pty. Ltd.
    Inventor: George Eustace Joannou
  • 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: 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: 6908942
    Abstract: The present invention provides (i) 6-amino-2,2-dimethyl-3,4,6-trisubstituted benzopyran derivatives; (ii) a process for synthesizing benzopyran derivatives with high efficiency by parallel synthesis on a solid-phase as one of combinatorial chemical synthesis technologies; and (iii) a use of the benzopyran derivatives for preventing and treating diseases or disorders induced by promotion of lipid peroxidation or accumulation of oxidized products.
    Type: Grant
    Filed: June 16, 2003
    Date of Patent: June 21, 2005
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Young-Dae Gong, Jin-Soo Seo, Jong Yeon Hwang, Sung-eun Yoo
  • 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: 20040256743
    Abstract: A method for producing an organic compound having Q, the method including a step of reacting a compound represented by general formula (2) with an organic starting material having at least one halogen atom bonded to a carbon atom having four &sgr; bonds so as to replace the halogen atom in the organic starting material with Q:
    Type: Application
    Filed: June 10, 2004
    Publication date: December 23, 2004
    Applicant: Mitsui Chemicals, Inc.
    Inventors: Setsuko Funaki, Yoshiteru Taniguchi, Tadahito Nobori, Yoshihiro Yamamoto, Isao Hara, Takaomi Hayashi, Kazumi Mizutani, Shinji Kiyono
  • Patent number: 6803129
    Abstract: The present invention relates to an organic light emitting diode (OLED) device, comprising an anode disposed on a substrate, an organic EL layer disposed on the anode and a cathode disposed on the organic EL layer.
    Type: Grant
    Filed: April 25, 2003
    Date of Patent: October 12, 2004
    Assignee: RiTdisplay Corporation
    Inventors: Hsien-Chang Lin, Chih-Hao Kung, Chung-Cheng Pai, Shwu-Ju Shieh, Tzu-Chin Tang
  • Patent number: 6790967
    Abstract: The invention concerns a novel method for preparing vitamin E. More particularly, it concerns a novel method for the condensation of trimethylhydroquinone and isophytol.
    Type: Grant
    Filed: December 19, 2002
    Date of Patent: September 14, 2004
    Assignee: Adisseo France S.A.S.
    Inventors: Jildaz Dhainaut, Thierry Durand
  • Publication number: 20040176616
    Abstract: A highly efficient process is provided for producing an optically active compound having high optical purity by an asymmetric reaction using as a catalyst a transition metal complex having an optically active nitrogen-containing compound as an asymmetric ligand.
    Type: Application
    Filed: December 31, 2003
    Publication date: September 9, 2004
    Applicant: KANTO KAGAKU KABUSHIKI KAISHA
    Inventors: Masahito Watanabe, Kunihiko Murata, Takao Ikariya
  • Patent number: 6737439
    Abstract: A composition and method of cancer treatment is disclosed. The composition and method utilized the extract of B. papyrifera, or compounds included therein having aromatase inhibition properties, as active cancer chemopreventative and treating agents in mammals, including humans.
    Type: Grant
    Filed: July 25, 2002
    Date of Patent: May 18, 2004
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Alan Douglas Kinghorn, John M. Pezzuto, Dongho Lee, Krishna P. L. Bhat
  • Patent number: 6720353
    Abstract: The present invention is directed to isolation and identification of plant proanthocyanidin extracts and particular proanthocyanidin compounds for prevention and treatment of urinary tract infections caused by P-type Escherichia coli. These extracts can be obtained from any proanthocyanidin-containing plants, including plants of the families Ericaceae, Rosaceae, Pinaceae, Vitaceae and the like. Preferably the extracts are from cranberry plants (especially, Vaccinium macrocarpon) and other plants, particularly fruit and berry plants from the Vaccinium spp. The extracts and compounds are also provided as pharmaceutical compositions, food additives and food compositions, especially beverages, ground meat preparations and cranberry-containing food products. The invention also relates to methods of reducing pathogenicity of P-type E. coli in the digestive tracts of cattle and reducing P-type E. coli contamination in ground meat as well as methods of detecting P-type bacteria.
    Type: Grant
    Filed: April 30, 2003
    Date of Patent: April 13, 2004
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Amy B. Howell, Nicholi Vorsa
  • Patent number: 6677371
    Abstract: This invention relates to a 4-oxybenzopyran derivative of formula (I) wherein, R1 and R2 represent each independently a hydrogen atom, a C1-6 alkyl group or a phenyl group; R3 represents a hydroxyl group or C1-6 alkylcarbonyloxy group; R4 represents a hydrogen atom, a C3-6 cycloalkyl group, a C1-6 alkyl group, a C1-6 alkylcarbonyl group, a C1-6 alkylaminocarbonyl group, a di-C1-6 alkylaminocarbonyl group, an aryl group or a heteroaryl group; R5 represents a hydrogen atom or a C1-6 alkyl group; X is absent or represents C═O or SO2; R6 represents a hydrogen atom, a C1-6 alkyl group or a C3-6 cycloalkyl group; R7 represents a hydrogen atom, a halogen atom, a nitro group or a cyano group; or a pharmaceutically acceptable salt thereof. And this invention also relates to a drug for treating arrhytmia having the prolongation effect on the functional refractory period comprising said compound or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: March 29, 2002
    Date of Patent: January 13, 2004
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Keizo Tanikawa, Kazuhiko Ohrai, Kazufumi Yanagihara, Yukihiro Shigeta, Toru Tsukagoshi, Toru Yamashita
  • Patent number: 6670390
    Abstract: Disclosed and claimed are cocoa extracts, compounds, combinations thereof and compositions containing the same, such as polyphenols or procyanidins, methods for preparing such extracts, compounds and compositions, as well as uses for them, especially a polymeric compound of the formula An, wherein A is a monomer of the formula: wherein n is an integer from 2 to 18, such that there is at least one terminal monomeric unit A, and one or a plurality of additional monomeric units; R is 3-(&agr;)-OH, 3-(&bgr;)-OH, 3-(&agr;)-O-sugar, or 3-(&bgr;)-O-sugar.
    Type: Grant
    Filed: November 21, 2000
    Date of Patent: December 30, 2003
    Assignee: Mars Incorporated
    Inventors: Leo J. Romanczyk, Jr., John F. Hammerstone, Jr., Margaret M. Buck, Laurie S. Post, Giovanni G. Cipolla, Craig A. McClelland, Jeff A. Mundt, Harold H. Schmitz
  • Patent number: 6645997
    Abstract: A class of benzopyrancarboxylic acid derivatives comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.
    Type: Grant
    Filed: September 24, 2001
    Date of Patent: November 11, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Soumya P. Sahoo, Hiroo Koyama, Daniel J. Miller, Julia K. Boueres, Ranjit C. Desai
  • Patent number: 6608102
    Abstract: The present invention is directed to isolation and identification of plant proanthocyanidin extracts and particular proanthocyanidin compounds for prevention and treatment of urinary tract infections caused by P-type Escherichia coli. These extracts can be obtained from any proanthocyanidin-containing plants, including plants of the families Ericaceae, Rosaceae, Pinaceae, Vitaceae and the like. Preferably the extracts are from cranberry plants (especially, Vaccinium macrocarpon) and other plants, particularly fruit and berry plants from the Vaccinium spp. The extracts and compounds are also provided as pharmaceutical compositions, food additives and food compositions, especially beverages, ground meat preparations and cranberry-containing food products. The invention also relates to methods of reducing pathogenicity of P-type E. coli in the digestive tracts of cattle and reducing P-type E. coli contamination in ground meat as well as methods of detecting P-type bacteria.
    Type: Grant
    Filed: September 2, 1998
    Date of Patent: August 19, 2003
    Assignee: Rutgers, the State University of New Jersey
    Inventors: Amy B. Howell, Nicholi Vorsa
  • Publication number: 20030125356
    Abstract: The present invention relates to a novel 3-hydroxychromen-4-one derivative of formula (1), pharmaceutically acceptable salt, hydrate, solvate or isomer thereof which is useful as an inhibitor for Cyclin Dependent Kinase (“CDK”); to a process for preparing the compound of formula (1); and to a composition for suppression or treatment of cancer and diseases induced by cell proliferation such as inflammation, angiostenosis, angiogenesis, etc. comprising the compound of formula (1) as an active component together with pharmaceutically acceptable carriers.
    Type: Application
    Filed: November 1, 2002
    Publication date: July 3, 2003
    Inventors: Chang-Yong Hong, Jin-Ho Lee, Tae-Sik Park, Jong-Hyun Kim, Sei-Hyun Choi, Sook-Kyung Yoon, Hyun-Ho Chung, Ho-Sun Son, Eunie Eun-Kyeong Kim, Seong-Gu Ro, Shin-Wu Jeong, Dong-Myung Kim
  • Patent number: 6555574
    Abstract: This invention relates to a 4-oxybenzopyran derivative of formula (I) wherein, R1 and R2 represent each independently a hydrogen atom, a C1-6 alkyl group or a phenyl group; R3 represents a hydroxyl group or a C1-6 alkylcarbonyloxy group; R4 represents a hydrogen atom, a C3-6 cycloalkyl group, a C1-6 alkyl group, a C1-6 alkylcarbonyl group, a C1-6 alkylaminocarbonyl group, a di-C1-6 alkylaminocarbonyl group, an aryl group or a heteroaryl group; n represents an integer of 0-4; X represents —C(═O)NR7—, —NR8—, —NHC(═O)NH— or —S(O)2NH—; R5 represents a hydrogen atom or (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), or (l); R6 represents a hydrogen atom, a halogen atom, a nitro group or a cyano group; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 29, 2002
    Date of Patent: April 29, 2003
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Keizo Tanikawa, Kazuhiko Ohrai, Kazufumi Yanagihara, Yukihiro Shigeta, Toru Tsukagoshi, Toru Yamashita
  • Patent number: 6531617
    Abstract: Enantiomerically enriched hydroxychromanones are obtained by the AlCl3-catalyzed intramolecular Friedel-Crafts acylation of the corresponding 3-phenoxy-2-alkylcarbonyloxy-propionic acid followed by cleavage of the carboxylate in the presence of an alkali metal peroxide or hydroperoxide. Enantiomerically enriched cis-aminochromanols can then be prepared by treating the hydroxychromanones with a hydroxylamine and hydrogenating the resulting oxime. The cis-aminochromanols can be employed as intermediates in the production of HIV protease inhibitors which are useful for treating HIV infection and AIDS.
    Type: Grant
    Filed: October 24, 2001
    Date of Patent: March 11, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Karl Hansen, Paul Devine, Philippe M. Rabbat
  • Patent number: 6528664
    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: December 14, 2001
    Date of Patent: March 4, 2003
    Assignee: Mars, Incorporated
    Inventors: Leo J. Romanczyk, Jr., Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
  • Patent number: 6479671
    Abstract: A process for producing a compound of the formula (II): (wherein R1, R2, R3 and R4 are each independently hydrogen, alkyl, alkoxy or the like, R5 is alkyl or alkoxyalkyl, A is O or S, Ar is aryl or the like, * represents the position of an asymmetric carbon atom and that the compound is the (R) or (S) isomer and Q is an optical resolution reagent) comprising isolating the compound as crystals from a solution or suspension containing the compound of the formula (II) (wherein * represents that the compound is the (R) or (S) isomer or a mixture thereof and the other symbols are the same as the above).
    Type: Grant
    Filed: August 15, 2000
    Date of Patent: November 12, 2002
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshiro Konoike, Tadahiko Yorifuji, Shoji Shinomoto, Yutaka Ide, Takashi Ohya, Ken-ichi Matsumura
  • Publication number: 20020128493
    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: December 14, 2001
    Publication date: September 12, 2002
    Applicant: Mars, Incorporated
    Inventors: Leo J. Romanczyk, Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
  • Publication number: 20020095047
    Abstract: Enantiomerically enriched hydroxychromanones are obtained by the AlCl3-catalyzed intramolecular Friedel-Crafts acylation of the corresponding 3-phenoxy-2-alkylcarbonyloxy-propionic acid followed by cleavage of the carboxylate in the presence of an alkali metal peroxide or hydroperoxide. Enantiomerically enriched cis-aminochromanols can then be prepared by treating the hydroxychromanones with a hydroxylamine and hydrogenating the resulting oxime. The cis-aminochromanols can be employed as intermediates in the production of HIV protease inhibitors which are useful for treating HIV infection and AIDS.
    Type: Application
    Filed: October 24, 2001
    Publication date: July 18, 2002
    Inventors: Karl Hansen, Paul Devine, Philippe M. Rabbat
  • Patent number: 6420572
    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: October 9, 1998
    Date of Patent: July 16, 2002
    Assignee: Mars, Incorporated
    Inventors: Leo J. Romanczyk, Jr., Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
  • Patent number: 6291518
    Abstract: The present invention relates to novel hydroxy and polyhydroxy derivatives of coumarin fused with dialdehydes and aldehyde acids of the general formulae I, II, III and IV: wherein R1=R2=4-hydroxycoumarin; R1=R2=4,7-dihydroxycoumarin; R1=R2=4,5,7-trihydroxycoumarin; R1=4-hydroxycoumarin, R2=—CH(OH)CH3. An object of the invention are also processes for the preparation of hydroxy and polyhydroxy derivatives of coumarin fused with dialdehydes and aldehyde acids, and the antiviral action thereof. Novel hydroxy and polyhydroxy derivatives of coumarin according to the present invention exhibit antiviral action against HIV-1 virus.
    Type: Grant
    Filed: January 3, 2000
    Date of Patent: September 18, 2001
    Assignee: Pliva farmaceutska, kemijska, prehrambena i kozmeticka industrija, dionicko drustvo
    Inventors: Mladen Trkovnik, Zrinka Ivezić
  • Patent number: 6215007
    Abstract: Novel polyketides and novel methods of efficiently producing both new and known polyketides, using recombinant technology, are disclosed. In particular, a novel host-vector system is described which is used to produce polyketide synthases which in turn catalyze the production of a variety of polyketides.
    Type: Grant
    Filed: March 5, 1999
    Date of Patent: April 10, 2001
    Assignees: The Leland Stanford Junior Univ., The John Innes Institute
    Inventors: Chaitan Khosla, David A. Hopwood, Suzanne Ebert-Khosla, Robert McDaniel, Hong Fu
  • Patent number: 6207842
    Abstract: A process is disclosed for the production of polyphenol oligomers having n polyphenol monomers, 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 monomers. Advantageously, polyphenol monomers forming the polyphenol oligomers may be the same or different.
    Type: Grant
    Filed: October 9, 1997
    Date of Patent: March 27, 2001
    Assignee: Mars Incorporated
    Inventors: Leo J. Romanczyk, Jr., Alan P. Kozikowski, Werner Tueckmantel
  • Patent number: 6194450
    Abstract: Novel pharmaceutically/cosmetically-active polyaromatic heterocyclic compounds have the structural formula (I): in which Z is a divalent radical selected from among —O—, —S— or —Nr′— and Ar is either a radical having the following structural formula (II): or a radical having the following structural formula (III): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: July 23, 1998
    Date of Patent: February 27, 2001
    Assignee: Centre International de Recherches Dermatologiques Galderma
    Inventors: Bruno Charpentier, Philippe Diaz, Philippe Nedoncelle
  • Patent number: 6130342
    Abstract: Novel fluorescent substrates of the human P450 enzyme CYP2D6 are provided. Also provided are methods for their manufacture and use. These substrates are useful in assessing CYP2D6 enzyme activity and in selecting compounds which inhibit CYP2D6 enzyme activity and, in particular, for identifying potential adverse drug interactions which are mediated by inhibition of CYP2D6 enzyme activity.
    Type: Grant
    Filed: July 12, 1999
    Date of Patent: October 10, 2000
    Assignee: Gentest Corporation
    Inventors: Vaughn P. Miller, Charles L. Crespi
  • Patent number: 6080780
    Abstract: Methods of treating anxiety with flavonoid compounds according to Formula (I) and dimers thereof, compounds of Formula (I) and dimers thereof, use of compounds of Formula (I) and pharmaceutical formulations comprising flavonoids of Formula (I) and dimers thereof.
    Type: Grant
    Filed: July 8, 1998
    Date of Patent: June 27, 2000
    Assignee: University of Strathclyde
    Inventors: Alejandro Constantino Paladini, Jorge Horacio Medina
  • Patent number: 6071938
    Abstract: A compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein X, O R, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are defined in the specification; compositions containing such compounds; intermediates used in the preparation of such compounds; and methods for treating a disease associated with the altered tone and/or motility of smooth muscle, for example chronic obstructive airways disease, asthma, urinary incontinence, irritable bowel syndrome, diverticular disease, oesophageal achalasia, and hypertension.
    Type: Grant
    Filed: April 9, 1999
    Date of Patent: June 6, 2000
    Assignee: Pfizer Inc.
    Inventors: Alexander Roderick MacKenzie, Sandra Marina Monaghan
  • Patent number: 6051601
    Abstract: This invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds or a pharmaceutically acceptable salt thereof, and to methods of using such compounds as LTB.sub.4 antagonists. The compounds and the pharmaceutically acceptable salts of this invention inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruritus and acne, stroke and other forms of reperfuslon injury, graft rejection, autoimmune diseases, asthma, and other conditions where marked neutrophil infiltration occurs.
    Type: Grant
    Filed: April 9, 1997
    Date of Patent: April 18, 2000
    Assignee: Pfizer Inc.
    Inventors: Mark Anthony Dombroski, Kevin Koch, Anthony Daniel Piscopio
  • Patent number: 6034121
    Abstract: Compounds of the formula ##STR1## where one of Z and Y is CO and the other is C--W--R.sup.2 and the dotted line indicates a double bond is present where necessary to meet valency requirements, W is O, S(O).sub.n, N(R.sup.3), N(R.sup.3)(R.sup.4), N(R.sup.3)O or ON(R.sup.3); R.sup.1 is hydrogen, or an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or heterocyclyl group; R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, are as defined above for R.sup.1, or are acyl, or R.sup.2 and R.sup.3 or R.sup.2 and R.sup.4 or R.sup.3 and R.sup.4 together with the nitrogen or oxygen to which they are attached form an optionally substituted ring which may contain other hetero atoms; each X, which may be the same as or different from any other X, is halogen, CN, NO.sub.2, SF.sub.5, B(OH).sub.2, triakylsilyl or a group E, OE or S(O).sub.n E where E is a group as defined hereinbefore for R.sup.
    Type: Grant
    Filed: April 1, 1998
    Date of Patent: March 7, 2000
    Assignee: Agrevo UK Limited
    Inventors: Mary Josephine O'Mahony, Peter John West, Jacqueline Anne MacRitchie, Stephen David Lindell, Peter Millward
  • Patent number: 6004998
    Abstract: Certain flavonoids, notably derivatives of flavone, chrysin and apigenin, together with dimers thereof such as amentoflavone, have been found to possess anxiolytic properties (i.e., anxiety reducing properties) without exhibiting a sedative effect. Novel compounds and pharmaceutical formulations are also described.
    Type: Grant
    Filed: September 29, 1997
    Date of Patent: December 21, 1999
    Assignee: University of Strathclyde
    Inventors: Bruce Kennedy Cassels, Federico Jose Dajas, Jorge Horacio Medina, Alejandro Constantino Paladini, Rodolfo Horacio Silveira
  • Patent number: 6001821
    Abstract: The preparation of compositions containing cyclodextrin moieties which are modified by fusing 1,4 dioxane rights to glucopyranosyl residues is described.
    Type: Grant
    Filed: June 17, 1998
    Date of Patent: December 14, 1999
    Inventor: Josef Pitha
  • Patent number: 5977167
    Abstract: Novel benzopyran and benzoxazine derivatives represented by the general formula: wherein R.sub.1 and R.sub.2 represent a lower haloalkyl group, R.sub.3 represents a hydrogen atom, etc., R.sub.4 represents a heterocyclic group or A--O-- wherein A represents a cyclic structure, etc., R.sub.5 and R.sub.6 represent a lower haloalkyl, X represents .dbd.N--, N.fwdarw.O, etc, are disclosed. These compounds exhibit K.sup.+ channel opening activating and can be widely used as an anti-asthma drug, an anti-epilepsy drug, etc.
    Type: Grant
    Filed: February 19, 1998
    Date of Patent: November 2, 1999
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Hiroshi Koga, Haruhiko Sato, Takenori Ishizawa, Hiroyuki Nabata
  • Patent number: 5939452
    Abstract: The invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists of formula I and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds, and to a method of using such compounds as LBT.sub.4 antagonists. The compounds of the invention inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruitus and acne, stroke and other forms of reperfusion injury, graft rejection, autoimmune diseases, asthma and other conditions where marked neutrophil infiltration occurs.
    Type: Grant
    Filed: April 9, 1997
    Date of Patent: August 17, 1999
    Assignee: Pfizer Inc
    Inventors: Mark Anthony Dombroski, Kevin Koch, Anthony Daniel Piscopio
  • Patent number: 5861430
    Abstract: A method of inhibiting microorganisms, including bacteria, using benzopyran phenol derivates from propolis. Propolis is extracted with an alcohol, and the resulting compounds are effective as antibacterial, antiviral or immunostimulating agents.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 19, 1999
    Assignees: Jasmine Fockerman, Michel Fockerman
    Inventor: Maria Markonius
  • Patent number: 5849798
    Abstract: Novel pharmaceutically/cosmetically-active polyaromatic heterocyclic compounds have the structural formula (I): ##STR1## in which Z is a divalent radical selected from among --O--, --S-- or --Nr'-- and Ar is either a radical having the following structural formula (II): ##STR2## or a radical having the following structural formula (III): ##STR3## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: March 14, 1996
    Date of Patent: December 15, 1998
    Assignee: Centre International De Recherches Dermatologiques Galderma
    Inventors: Bruno Charpentier, Philippe Diaz, Philippe Nedoncelle
  • Patent number: 5801179
    Abstract: The present invention is concerned with compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or C.sub.1--6 alkyl; R.sup.2 is hydrogen or C.sub.1- 6 alkyl; R.sup.3 is C.sub.1-6 alkyl, hydroxy, cyano, halo, C.sub.1-6 alkyloxy, aryloxy, arylmethoxy, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkyl--S--, C.sub.1-6 alkyl(S.dbd.O)--, C.sub.1-6 alkylcarbonyl; R.sup.4 is hydrogen, halo, hydroxy, C.sub.1-6 alkyl, or C.sub.1-6 alkyloxy; or R.sup.3 and R.sup.4 taken together form a bivalent radical; R.sup.5 and R.sup.6 each independently are hydrogen, halo, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, aryloxy or arylmethoxy; R.sup.7 is hydrogen; Alk.sup.1 is C.sub.2-5 alkanediyl; Alk.sup.2 is C.sub.2-15 alkanediyl; Q is a heterocyclic ring containing at least one nitrogen atom or a radical of formula ##STR2## Pharmaceutical compositions, preparations and use as a medicine are described.
    Type: Grant
    Filed: June 2, 1997
    Date of Patent: September 1, 1998
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Guy Rosalia Eugene Van Lommen, Marcel Frans Leopold De Bruyn, Piet Tom Bert Paul Wigerinck