Plural Chalcogens Bonded Directly To The Hetero Ring Patents (Class 549/400)
-
Publication number: 20090054518Abstract: 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: ApplicationFiled: March 31, 2006Publication date: February 26, 2009Inventor: Fulin Fan
-
Publication number: 20090007292Abstract: A maize inbred line having the characteristics selected from those of FAR045, including plant parts, tissue, and pigments of the inbred is disclosed.Type: ApplicationFiled: June 20, 2008Publication date: January 1, 2009Inventor: Lee K. French
-
Publication number: 20080286360Abstract: 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: ApplicationFiled: April 7, 2008Publication date: November 20, 2008Inventors: Molly Shoichet, Jordan Wosnick, Ryan Wylie
-
Publication number: 20080280335Abstract: 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: ApplicationFiled: May 30, 2005Publication date: November 13, 2008Applicant: AMOREPACIFIC CORPORATIONInventors: 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: 20080214844Abstract: 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: ApplicationFiled: January 23, 2007Publication date: September 4, 2008Inventors: Nan Zhang, Stuart K. Calderwood
-
Patent number: 7396856Abstract: 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: GrantFiled: May 6, 2005Date of Patent: July 8, 2008Assignee: Alcon, Inc.Inventors: Mark R. Hellberg, Abdelmoula Namil
-
Publication number: 20080153872Abstract: 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: ApplicationFiled: January 13, 2006Publication date: June 26, 2008Inventors: 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: 20080146657Abstract: 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: ApplicationFiled: November 4, 2004Publication date: June 19, 2008Inventors: Hiroshi Tsuboi, Shuji Ikegami, Tomonori Kamiyama, Zai-si Ji, Yukio Asami, Hiroyuki Itou, Munehiro Oda, Kazuo Shin
-
Patent number: 7345090Abstract: The invention relates to compounds of the formula I where R1, R2, R3, R4 and R5 have the meanings given in claim 1. The compound is suitable in particular for use in skin care compositions. They protect, firstly, against harmful oxidation reactions and, secondly, also act as UV filters.Type: GrantFiled: April 28, 2004Date of Patent: March 18, 2008Assignee: Merck Patent Gesellschaft mit Beschraenkter HaftungInventors: Frank Pfluecker, Joachim Buenger, Hans-Juergen Driller, Herwig Buchholz, Ralf Rosskopf
-
Patent number: 7226644Abstract: The present invention relates to a liquid crystal compound which has negative dielectric anisotropy and a large absolute value thereof; and a liquid crystal display element which contains the compound as a constituent element and has a negative value of dielectric anisotropy in the vertical alignment mode, IPS, or the like. The liquid-crystal display element has a structure including a pair of substrates and a liquid crystal sandwiched therebetween, and includes at least an alignment control layer, a transparent electrode, and a polarizing plate, in which the liquid crystal includes at least one compound having a partial structure represented by general formula (A): (wherein W1 and W2 each independently represents fluorine, chlorine, —CF3, —CF2H, —OCF3, or —OCF2H) and has negative dielectric anistropy.Type: GrantFiled: June 25, 2004Date of Patent: June 5, 2007Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Takashi Matsumoto, Tetsuo Kusumoto, Shotaro Kawakami
-
Patent number: 7067679Abstract: 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: GrantFiled: September 9, 2003Date of Patent: June 27, 2006Inventors: Alan P. Kozikowski, Werner Tückmantel, Leo J. Romanczyk, Jr.
-
Patent number: 7056952Abstract: 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: GrantFiled: May 1, 2000Date of Patent: June 6, 2006Assignee: G.J. Consultants Pty. Ltd.Inventor: George Eustace Joannou
-
Patent number: 7012149Abstract: A process is provided for making (?)-epigallocatechin gallate (EGCG) by subjecting a green tea extract to chromatography on a macroporous polar resin, eluting EGCG from the resin with a polar elution solvent, optionally concentrating the eluate, optionally regenerating the resin by desorbing the remaining catechins, and optionally concentrating the desorbed catechins.Type: GrantFiled: September 18, 2002Date of Patent: March 14, 2006Assignee: DSM IP Assets B.V.Inventors: David Carl Burdick, Heinz Egger, Andrew George Gum, Ingo Koschinski, Elena Muelchi, Isabelle Prevot-Halter
-
Patent number: 6916831Abstract: Compounds are described having a structure according to Formula I or Formula II: wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O and S; m is from 1 to 3; n is from 1 to 5; R1 and R3 are each independently selected from the group consisting of H, hydroxy, lower alky, lower alkoxy, halo, amino, aminoalkyl, nitro, heteroaryl, —OC(?O)R6, —O(C?O)OR6; and —O(C?O)N(R6)2; and R2 is side chain such as an acetic acid side chain, where p is O to 4, R5 is hydroxy, alkoxy or amino, and R6 is H or lower alkyl, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer.Type: GrantFiled: February 24, 2003Date of Patent: July 12, 2005Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Yi Xia, Zheng-Yu Yang, Kenneth F. Bastow, Sheng-Chu Kuo
-
Patent number: 6908942Abstract: 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: GrantFiled: June 16, 2003Date of Patent: June 21, 2005Assignee: Korea Research Institute of Chemical TechnologyInventors: Young-Dae Gong, Jin-Soo Seo, Jong Yeon Hwang, Sung-eun Yoo
-
Patent number: 6849746Abstract: A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.Type: GrantFiled: January 31, 2003Date of Patent: February 1, 2005Assignee: Mars, Inc.Inventors: Leo J. Romanczyk, Jr., Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
-
Publication number: 20040256743Abstract: 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: ApplicationFiled: June 10, 2004Publication date: December 23, 2004Applicant: Mitsui Chemicals, Inc.Inventors: Setsuko Funaki, Yoshiteru Taniguchi, Tadahito Nobori, Yoshihiro Yamamoto, Isao Hara, Takaomi Hayashi, Kazumi Mizutani, Shinji Kiyono
-
Patent number: 6803129Abstract: 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: GrantFiled: April 25, 2003Date of Patent: October 12, 2004Assignee: RiTdisplay CorporationInventors: Hsien-Chang Lin, Chih-Hao Kung, Chung-Cheng Pai, Shwu-Ju Shieh, Tzu-Chin Tang
-
Patent number: 6790967Abstract: 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: GrantFiled: December 19, 2002Date of Patent: September 14, 2004Assignee: Adisseo France S.A.S.Inventors: Jildaz Dhainaut, Thierry Durand
-
Publication number: 20040176616Abstract: 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: ApplicationFiled: December 31, 2003Publication date: September 9, 2004Applicant: KANTO KAGAKU KABUSHIKI KAISHAInventors: Masahito Watanabe, Kunihiko Murata, Takao Ikariya
-
Patent number: 6737439Abstract: 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: GrantFiled: July 25, 2002Date of Patent: May 18, 2004Assignee: The Board of Trustees of the University of IllinoisInventors: Alan Douglas Kinghorn, John M. Pezzuto, Dongho Lee, Krishna P. L. Bhat
-
Patent number: 6720353Abstract: 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: GrantFiled: April 30, 2003Date of Patent: April 13, 2004Assignee: Rutgers, The State University of New JerseyInventors: Amy B. Howell, Nicholi Vorsa
-
Patent number: 6677371Abstract: 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: GrantFiled: March 29, 2002Date of Patent: January 13, 2004Assignee: Nissan Chemical Industries, Ltd.Inventors: Keizo Tanikawa, Kazuhiko Ohrai, Kazufumi Yanagihara, Yukihiro Shigeta, Toru Tsukagoshi, Toru Yamashita
-
Patent number: 6670390Abstract: 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: GrantFiled: November 21, 2000Date of Patent: December 30, 2003Assignee: Mars IncorporatedInventors: 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: 6645997Abstract: 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: GrantFiled: September 24, 2001Date of Patent: November 11, 2003Assignee: Merck & Co., Inc.Inventors: Soumya P. Sahoo, Hiroo Koyama, Daniel J. Miller, Julia K. Boueres, Ranjit C. Desai
-
Patent number: 6608102Abstract: 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: GrantFiled: September 2, 1998Date of Patent: August 19, 2003Assignee: Rutgers, the State University of New JerseyInventors: Amy B. Howell, Nicholi Vorsa
-
Publication number: 20030125356Abstract: 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: ApplicationFiled: November 1, 2002Publication date: July 3, 2003Inventors: 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: 6555574Abstract: 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: GrantFiled: March 29, 2002Date of Patent: April 29, 2003Assignee: Nissan Chemical Industries, Ltd.Inventors: Keizo Tanikawa, Kazuhiko Ohrai, Kazufumi Yanagihara, Yukihiro Shigeta, Toru Tsukagoshi, Toru Yamashita
-
Patent number: 6531617Abstract: 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: GrantFiled: October 24, 2001Date of Patent: March 11, 2003Assignee: Merck & Co., Inc.Inventors: Karl Hansen, Paul Devine, Philippe M. Rabbat
-
Patent number: 6528664Abstract: A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.Type: GrantFiled: December 14, 2001Date of Patent: March 4, 2003Assignee: Mars, IncorporatedInventors: Leo J. Romanczyk, Jr., Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
-
Patent number: 6479671Abstract: 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: GrantFiled: August 15, 2000Date of Patent: November 12, 2002Assignee: Shionogi & Co., Ltd.Inventors: Toshiro Konoike, Tadahiko Yorifuji, Shoji Shinomoto, Yutaka Ide, Takashi Ohya, Ken-ichi Matsumura
-
Publication number: 20020128493Abstract: A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.Type: ApplicationFiled: December 14, 2001Publication date: September 12, 2002Applicant: Mars, IncorporatedInventors: Leo J. Romanczyk, Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
-
Publication number: 20020095047Abstract: 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: ApplicationFiled: October 24, 2001Publication date: July 18, 2002Inventors: Karl Hansen, Paul Devine, Philippe M. Rabbat
-
Patent number: 6420572Abstract: A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.Type: GrantFiled: October 9, 1998Date of Patent: July 16, 2002Assignee: Mars, IncorporatedInventors: Leo J. Romanczyk, Jr., Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
-
Patent number: 6291518Abstract: 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: GrantFiled: January 3, 2000Date of Patent: September 18, 2001Assignee: Pliva farmaceutska, kemijska, prehrambena i kozmeticka industrija, dionicko drustvoInventors: Mladen Trkovnik, Zrinka Ivezić
-
Patent number: 6215007Abstract: 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: GrantFiled: March 5, 1999Date of Patent: April 10, 2001Assignees: The Leland Stanford Junior Univ., The John Innes InstituteInventors: Chaitan Khosla, David A. Hopwood, Suzanne Ebert-Khosla, Robert McDaniel, Hong Fu
-
Patent number: 6207842Abstract: 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: GrantFiled: October 9, 1997Date of Patent: March 27, 2001Assignee: Mars IncorporatedInventors: Leo J. Romanczyk, Jr., Alan P. Kozikowski, Werner Tueckmantel
-
Patent number: 6194450Abstract: 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: GrantFiled: July 23, 1998Date of Patent: February 27, 2001Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Bruno Charpentier, Philippe Diaz, Philippe Nedoncelle
-
Patent number: 6130342Abstract: 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: GrantFiled: July 12, 1999Date of Patent: October 10, 2000Assignee: Gentest CorporationInventors: Vaughn P. Miller, Charles L. Crespi
-
Patent number: 6080780Abstract: 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: GrantFiled: July 8, 1998Date of Patent: June 27, 2000Assignee: University of StrathclydeInventors: Alejandro Constantino Paladini, Jorge Horacio Medina
-
Patent number: 6071938Abstract: 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: GrantFiled: April 9, 1999Date of Patent: June 6, 2000Assignee: Pfizer Inc.Inventors: Alexander Roderick MacKenzie, Sandra Marina Monaghan
-
Patent number: 6051601Abstract: 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: GrantFiled: April 9, 1997Date of Patent: April 18, 2000Assignee: Pfizer Inc.Inventors: Mark Anthony Dombroski, Kevin Koch, Anthony Daniel Piscopio
-
Patent number: 6034121Abstract: 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: GrantFiled: April 1, 1998Date of Patent: March 7, 2000Assignee: Agrevo UK LimitedInventors: Mary Josephine O'Mahony, Peter John West, Jacqueline Anne MacRitchie, Stephen David Lindell, Peter Millward
-
Patent number: 6004998Abstract: 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: GrantFiled: September 29, 1997Date of Patent: December 21, 1999Assignee: University of StrathclydeInventors: Bruce Kennedy Cassels, Federico Jose Dajas, Jorge Horacio Medina, Alejandro Constantino Paladini, Rodolfo Horacio Silveira
-
Patent number: 6001821Abstract: The preparation of compositions containing cyclodextrin moieties which are modified by fusing 1,4 dioxane rights to glucopyranosyl residues is described.Type: GrantFiled: June 17, 1998Date of Patent: December 14, 1999Inventor: Josef Pitha
-
Patent number: 5977167Abstract: 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: GrantFiled: February 19, 1998Date of Patent: November 2, 1999Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroshi Koga, Haruhiko Sato, Takenori Ishizawa, Hiroyuki Nabata
-
Patent number: 5939452Abstract: 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: GrantFiled: April 9, 1997Date of Patent: August 17, 1999Assignee: Pfizer IncInventors: Mark Anthony Dombroski, Kevin Koch, Anthony Daniel Piscopio
-
Patent number: 5861430Abstract: 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: GrantFiled: June 7, 1995Date of Patent: January 19, 1999Assignees: Jasmine Fockerman, Michel FockermanInventor: Maria Markonius
-
Patent number: 5849798Abstract: 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: GrantFiled: March 14, 1996Date of Patent: December 15, 1998Assignee: Centre International De Recherches Dermatologiques GaldermaInventors: Bruno Charpentier, Philippe Diaz, Philippe Nedoncelle
-
Patent number: 5801179Abstract: 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: GrantFiled: June 2, 1997Date of Patent: September 1, 1998Assignee: Janssen Pharmaceutica, NVInventors: Guy Rosalia Eugene Van Lommen, Marcel Frans Leopold De Bruyn, Piet Tom Bert Paul Wigerinck