Chalcogen Bonded Directly To The Ring Carbon Para To The Ring Oxygen (e.g., Chromones, Etc.) Patents (Class 549/401)
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Patent number: 7714150Abstract: Compounds corresponding to formula I, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n have the meanings given in the description, and also a process for the preparation of these compounds and intermediate products of this process. Furthermore, pharmaceutical compositions comprising the compounds of Formula I and related methods of treatment.Type: GrantFiled: April 10, 2006Date of Patent: May 11, 2010Assignee: Solvay Pharmaceuticals GmbHInventors: Brian Moloney, Lester Marrison, Dieter Ziegler, Michael Mlinaric, Christiane Boecker, Reinhard Brueckner, Michael Weske, Klaus Witte, Yvan Fischer
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Publication number: 20100076206Abstract: The present invention relates to a process for preparing Nebivolol and, more particularly, to an improved process for synthesizing enantiomerically enriched 6-fluoro chroman alcohol or epoxide derivatives of formula, wherein R and X is defined in the description; as useful intermediates in the preparation of Nebivolol.Type: ApplicationFiled: November 23, 2007Publication date: March 25, 2010Applicant: ZACH SYSTEM S.P.A.Inventors: Elio Ullucci, Paolo Maragni, Livius Cotarca, Johnny Foletto
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Patent number: 7671220Abstract: The present invention relates to methods for the preparation of 3,3-dialky 4-chromanones, and particularly to the preparation of 6-fluoro-3,3-dimethyl-2,3-dihydro-4H-chromen-4-one and 3,3-dimethyl-2,3-dihydro-4H-chromen-4-one. In some embodiments, the processes include reaction of a 4-chromanone compound with an alkyl halide in the presence of a metal alkoxide at low temperature.Type: GrantFiled: February 15, 2006Date of Patent: March 2, 2010Assignee: WyethInventors: Ayako Yamashita, Emily B. Norton, Jaechul Shim, Cilien S. Hanna
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Patent number: 7662977Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.Type: GrantFiled: December 21, 2007Date of Patent: February 16, 2010Assignee: Semafore Pharmaceuticals, Inc.Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
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Patent number: 7642283Abstract: Methods of utilizing compounds of general formulas I and II as modulators and affinity labels of the MPTP complex are elucidated. Furthermore, methods for modulating the activity of the MPTP complex, methods for determining the presence of a component of the MPTP complex, and methods for identifying an active agent that modulates the activity of the MPTP complex, specifically methods for identifying an active agent that modulates the activity of the MPTP complex by interacting with the VDAC1 component are identified. Moreover, novel compounds of general formulas I and II are disclosed.Type: GrantFiled: July 14, 2006Date of Patent: January 5, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Andrea Cesura, Emmanuel Pinard
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Publication number: 20090325900Abstract: The present invention provides a compound useful as an agent for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides a fused heterocyclic derivative represented by the following general formula (I), a pharmaceutical composition containing the same, a medicinal use thereof and the like. In the formula (I), ring A represents 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA represents halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; ring B represents aryl or heteroaryl; RB represents halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; E1 and E2 represent an oxygen atom or the like; U represents a single bond or alkylene; X represents a group represented by Y, —SO2—Y, —O— (alkylene)-Y, —O-Z in which Y represents Z, amino or the like; Z represents cycloalkyl, heterocycloalkyl, aryl, heteroaryl or the like; or the like.Type: ApplicationFiled: October 17, 2006Publication date: December 31, 2009Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kohsuke Ohno, Takashi Miyagi, Tomonaga Ozawa, Nobuhiko Fushimi
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Publication number: 20090306197Abstract: The present invention relates to substituted chromanol derivatives, to processes for their preparation, to their use on their own or in combination for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: March 7, 2007Publication date: December 10, 2009Applicant: Bayer Healthcare AGInventors: Carsten Schmeck, Hilmar Bischoff, Volkhart Li, Klemens Lustig, Michael Thutewohl, Alexandros Vakalopoulos, Olaf Weber
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Patent number: 7629477Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: June 19, 2008Date of Patent: December 8, 2009Assignees: Cytokinetics, Inc., SmithKline Beecham CorporationInventors: Andrew McDonald, Gustave Bergnes, Bainian Feng, David J. Morgans, Jr., Steven David Knight, Kenneth A. Newlander, Dashyant Dhanak, Christopher A. Brook
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Publication number: 20090259055Abstract: Various chromanone, flavanone and abyssinone compounds as can be prepared enantioselectively using a chiral thiourea catalyst.Type: ApplicationFiled: March 2, 2009Publication date: October 15, 2009Inventors: Karl Scheidt, Margaret Biddle
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Patent number: 7601754Abstract: Novel flavonoid compounds having anti-oxidant activity are described. Formula 1. The compounds have been shown to exhibit anti-oxidative properties in biological systems and their utility in a sunscreen or skincare composition or to treat conditions involving oxidative damage, especially curative or prophylactic treatment of Alzheimer's disease or ischaemia-reperfusion injury, is described.Type: GrantFiled: July 14, 2003Date of Patent: October 13, 2009Assignee: Antoxis LimitedInventors: Stuart Thomas Caldwell, Christopher James Bennett, Richard Charles Hartley, Donald Barton McPhail, Garry Graeme Duthie
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Publication number: 20090253919Abstract: Chiral thioureas are effective catalysts for the borane reduction of prochiral ketones to optically active alcohols. A prochiral ketone may be reduced to an optically active alcohol in the presence of a substantially sub-stoichiometric amount of chiral thiourea. The asymmetric thiourea compound of the present invention may be produced according to a production method described herein.Type: ApplicationFiled: April 3, 2008Publication date: October 8, 2009Applicant: Board of RegentsInventors: Derun Li, John R. Falck
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Patent number: 7598403Abstract: Processes for the preparation of biologically active chromanones are disclosed, including processes for the preparation of intermediates useful in the preparation of the biologically active chromanones. The chromanones and the intermediates disclosed herein may be useful for a variety of therapies, including the treatment of various cancers and the treatment of inflammation and inflammation related disorders.Type: GrantFiled: May 17, 2004Date of Patent: October 6, 2009Assignee: The University of South Carolina Research FoundationInventors: Brian A. Salvatore, Ferdinand C. Solis
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Publication number: 20090220438Abstract: The invention relates to the use of compounds of the formula (I), where R1 and R2 may be identical or different and stand for H, OH, OCH3, CH3, CH2OH or CH2OCH3, R3 stands for H or straight-chain or branched C1- to C20-alkyl groups, R4 stands for H or OR8, R5 and R6 may be identical or different and are selected from —H, —OH, straight-chain or branched C1 to C20-alkyl groups, straight-chain or branched C3- to C20-alkenyl groups, straight-chain or branched C1- to C20-hydroxyalkyl groups, where the hydroxyl group may be bonded to a primary or secondary carbon atom of the chain, and furthermore the allyl chain may also be interrupted by oxygen, and R8 stands for H or straight-chain or branched C1- to C20-alkyl groups, with the proviso that R2 does not denote H if R1 denotes CH3, as self-tanning agents, and to compounds and the preparation thereof.Type: ApplicationFiled: January 9, 2007Publication date: September 3, 2009Applicant: MERCK PATENT GMBHInventors: Christophe Carola, Anne Toullec, Herwig Buchholz
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Patent number: 7582675Abstract: A preparation process is provided for preparing a novel flavonoid compound having a high level of antioxidative action. The flavonoid compound is obtained by subjecting hesperidin to microbial fermentation treatment with Aspergillus saitoi.Type: GrantFiled: August 4, 2006Date of Patent: September 1, 2009Assignees: Pokka Corporation, National University Corp. Nagoya UniversityInventors: Toshihiko Osawa, Kenichiro Minato, Yoshiaki Miyake
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Publication number: 20090209637Abstract: The invention relates to the use of chromen-4-one derivatives of the formula I where R1 and R2 may be identical or different and are selected from H, —C(?O)—R7, —C(?O)—OR7, alkyl groups, alkenyl groups, hydroxyalkyl groups and/or cycloalkyl groups and/or cycloalkenyl groups, R3 is H or alkyl groups, R4 is H or OR8, R5 and R6 are selected from —H, —OH, alkyl groups, alkenyl groups and hydroxyalkyl groups, and R7 is H, alkyl groups, a polyhydroxyl compound, such as, preferably, an ascorbic acid radical or glycosidic radicals, and R8 is H or alkyl groups, where at least two of the substituents R1, R2 and R4-R6 are different from H or at least one substituent from R1 and R2 is —C(?O)—R7 or —C(?O)—OR7, to prevent, reduce or combat signs of cellulite and/or reduce localized fatty excesses.Type: ApplicationFiled: August 30, 2006Publication date: August 20, 2009Inventors: Christophe Carola, Herwig Buchholz
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Patent number: 7572919Abstract: Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I: wherein X is selected from O, N, S, SO, SO2, and S(CH2)n, wherein n=1-10; R1 and R2 may be the same or different and are selected from H, OH, OCH3, OCH2CH3, OCH2C6H5, NH2, NHCH3, N(CH3)2, CH3, CH2CH3, CH2CH2CH3, CH(CH3)2, C(CH3)3, NO2, F, Cl, Br, CF3, SH, SCH3, SCH2CH3, OCOCH3, OCOC(CH3)3, OCOCH2COOH, and CN; and R3 is a nitrogen-containing heterocyclic ring. Also provided are method for treating or preventing cancer in a subject by administering a therapeutically effective amount of a heteroaryl-containing isoflavone, or a pharmaceutically acceptable salt or prodrug thereof, to a subject in need of treatment.Type: GrantFiled: August 26, 2005Date of Patent: August 11, 2009Assignee: The Ohio State University Research FoundationInventors: Robert W. Brueggemeier, Young-Woo Kim, John C. Hackett
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Patent number: 7544711Abstract: The present invention relates to the use of the following compounds, their compositions, and their salts for the preparation of medicaments for the treatment of urinary incontinence and other diseases, the compounds having the general formula: A-X1—NO2 wherein: A=RCO(X)t, wherein t is the integer 0 or 1; X?O, NH, NR1C, wherein R1C is a linear or branched C1 to C10 alkyl group; when t=1, R= and X1=—YO—, wherein Y is a C1 to C20 alkylene, C5 to C7 cycloalkyl or oxyalkyl derivative.Type: GrantFiled: December 22, 2004Date of Patent: June 9, 2009Assignee: Nicox S.A.Inventors: Piero Del Soldato, Francesco Sannicolo'
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Patent number: 7528250Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1, R2, R3 and R4 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.Type: GrantFiled: December 21, 2005Date of Patent: May 5, 2009Assignee: Roche Palo Alto LLCInventors: Nancy Elisabeth Krauss, Shu-Hai Zhao
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Patent number: 7528267Abstract: 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: GrantFiled: August 1, 2005Date of Patent: May 5, 2009Assignees: Girindus America, Inc., Children's Hospital Medical CenterInventors: Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
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Publication number: 20090053641Abstract: [PROBLEMS] Providing a charge control agent that has a negative charge providing property at a practical level, is colorless to light-colored and usable in color toners, produces static charges stable to environmental changes by electrifying the resin powder of a toner and the like, is excellent in storage stability and durability, and is highly safe, as well as a method of controlling the charge of resin powder using the charge control agent, and a toner. [MEANS OF SOLVING THE PROBLEMS] A charge control agent having a compound represented by the formula shown below as the active ingredient, as well as a method of controlling the charge of resin powder using the charge control agent, and a toner.Type: ApplicationFiled: March 22, 2006Publication date: February 26, 2009Inventors: Kazuyoshi Kuroda, Masashi Yasumatsu
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Publication number: 20090005436Abstract: This invention is related to novel aminoalkyl- and amidoalkyl-benzopyran derivatives of the following general formula (I) wherein: the group ?is a substituent in position 6 or 7 wherein: R is an aromatic mono- or bi-cyclic carbocyclic ring or a mono- or bi-cyclic heterocyclic ring radical, said rings being optionally substituted by one or two substituents selected from (C1-C5) straight or branched alkyl, (C1-C5) straight or branched alkoxy, hydroxy, halogen and trifluoromethyl; m is zero or an integer from 1 to 3; n, p, R1 and R2 are as herein indicated and R3 and R4 are both hydrogen or taken together represent an oxygen atom, and the pharmaceutically acceptable salts thereof. The compounds that are active as selective and reversible MAO-B inhibitors in vitro and in vivo, are useful as medicaments for the prevention and the treatment of CNS degenerative disorders.Type: ApplicationFiled: February 22, 2006Publication date: January 1, 2009Applicant: NEWRON PHARMACEUTICALS S.p.A.Inventors: Angelo Carotti, Piero Melloni, Florian Thaler, Carla Caccia, Sara Maestroni, Patricia Salvati
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Publication number: 20080234363Abstract: Compounds of general formula (I), wherein R1, R2, R3, R4, R5, R6 and Y are as defined, and X group is O, S(O)m or NR; are of use in the treatment of cancer.Type: ApplicationFiled: August 1, 2006Publication date: September 25, 2008Applicant: PHARMA MAR, S.A.Inventors: Jose Fernando Reyes Benitez, Jose Antonio Jimenez Guerrero, Andres Manuel Francesch Solloso, Maria Del Carmen Cuev As Marchante
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Publication number: 20080207610Abstract: Disclosed are novel isoflavone derivatives having the structure of Formula I which are useful as ALDH-2 inhibitors for treating mammals for dependence upon drugs of addiction, for example addiction to dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and alcohol.Type: ApplicationFiled: January 24, 2008Publication date: August 28, 2008Inventors: Jeff Zablocki, Matthew Abelman, Michael Organ, Yaroslav Bilokin, Robert Jiang, Elfatih Elzein, Tetsuya Kobayashi, Rao Kalla, Thao Perry, Xiaofen Li, Ivan Diamond, Lina Yao, Peidong Fan, Maria Pia Arolfo, Zhan Jiang
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Substituted Benzo-Condensed Cycloheptanone Derivatives and the Use Thereof for Medicament Production
Publication number: 20080161352Abstract: The invention relates to substituted benzo-condensed cyclohexanone derivatives, to a method for the production thereof, to medicaments containing said derivatives and to the use of the inventive compounds for producing medicaments.Type: ApplicationFiled: May 17, 2006Publication date: July 3, 2008Applicant: Gruenenthal GmbHInventors: Robert Frank, Michael Przewosny, Ruth Jostock -
Patent number: 7384976Abstract: The invention describes novel compositions comprising nebivolol and/or at least one metabolite of nebivolol and at least one nitric oxide donor, and, optionally, at least one antioxidant or a pharmaceutically acceptable salt thereof, and/or at least one compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof, and/or at least one nitrosated compound used to treat cardiovascular diseases. The compounds and compositions of the invention can also be bound to a matrix. The nitric oxide donor is a compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and may preferably be isosorbide dinitrate and/or isosorbide mononitrate. The antioxidant may preferably be a hydralazine compound or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 13, 2005Date of Patent: June 10, 2008Assignee: Nitromed, Inc.Inventor: David S. Garvey
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Publication number: 20080125481Abstract: 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: ApplicationFiled: January 31, 2008Publication date: May 29, 2008Inventor: George Eustace Joannou
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Patent number: 7345090Abstract: The invention relates to compounds of the formula I where R1, R2, R3, R4 and R5 have the meanings given in claim 1. The compound is suitable in particular for use in skin care compositions. They protect, firstly, against harmful oxidation reactions and, secondly, also act as UV filters.Type: GrantFiled: April 28, 2004Date of Patent: March 18, 2008Assignee: Merck Patent Gesellschaft mit Beschraenkter HaftungInventors: Frank Pfluecker, Joachim Buenger, Hans-Juergen Driller, Herwig Buchholz, Ralf Rosskopf
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Publication number: 20080039640Abstract: A process for the preparation of a compound of formula (I) or a salt thereof wherein R is an amino, nitro or —NHCOR1 group, wherein R1 is C1-C6 alkyl or phenyl optionally substituted by a —O—(CH2)n-phenyl group, wherein n is an integer of 1 to 6; comprising reacting a compound of formula (II) or a salt thereof, both as the individual isomer and as an isomeric mixture, wherein R is as defined above; with a dehydrating agent, if necessary in the presence of an organic solvent, and optionally in the presence of a basic agent; and, if desired, converting a compound of formula (I) to another compound of formula (I) or a salt thereof.Type: ApplicationFiled: August 8, 2007Publication date: February 14, 2008Applicant: DIPHARMA FRANCIS S.R.L.Inventors: Lino COLOMBO, Pietro ALLEGRINI, Alessandra AMOROSI, Gabriele RAZZETTI, Roberto ROSSI
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Patent number: 7326797Abstract: A process for manufacturing a hydroxylated isoflavone of the formula (I) given in the description comprises re-acting an appropriately substituted 2-hydroxydeoxybenzoin of the formula (II), also given in the description, with a formic acid anhydride of the formula HCOOCOR3, wherein R3 signifies C2-20-alkyl or various other groups as given in the description, in presence of a base or in a solvent which acts as a base, and if necessary promoting the ensuing hydrolysis of the so-produced acylated form of the hydroxylated isoflavone of the formula I by acidification. Of particular interest as products of this process are the 5,7dihydroxyisoflavones, e.g. genistein (5,7,4?-trihydroxyisoflavone). Isoflavones display many useful biochemical effects.Type: GrantFiled: July 14, 2003Date of Patent: February 5, 2008Assignee: DSM IP Assets B.V.Inventors: Bruno Burdet, August Ruettimann
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Patent number: 7285671Abstract: The subject invention provides anticoagulant compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R3, n and Ar are as defined herein. The compounds of the subject invention can be used to treat at-risk populations thereby bringing relief of symptoms, improving the quality of life, preventing acute and long-term complications, reducing mortality and treating accompanying disorders. The invention further comprises pharmaceutical compositions comprising the compounds and salts of the invention, as well as methods of using the compounds, salts, and compositions of the invention.Type: GrantFiled: August 28, 2006Date of Patent: October 23, 2007Assignee: ARYx TherapeuticsInventors: Pascal Druzgala, Cyrus Becker
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Patent number: 7226644Abstract: The present invention relates to a liquid crystal compound which has negative dielectric anisotropy and a large absolute value thereof; and a liquid crystal display element which contains the compound as a constituent element and has a negative value of dielectric anisotropy in the vertical alignment mode, IPS, or the like. The liquid-crystal display element has a structure including a pair of substrates and a liquid crystal sandwiched therebetween, and includes at least an alignment control layer, a transparent electrode, and a polarizing plate, in which the liquid crystal includes at least one compound having a partial structure represented by general formula (A): (wherein W1 and W2 each independently represents fluorine, chlorine, —CF3, —CF2H, —OCF3, or —OCF2H) and has negative dielectric anistropy.Type: GrantFiled: June 25, 2004Date of Patent: June 5, 2007Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Takashi Matsumoto, Tetsuo Kusumoto, Shotaro Kawakami
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Patent number: 7138429Abstract: A preparation process is provided for preparing a novel flavonoid compound having a high level of antioxidative action. The flavonoid compound is obtained by subjecting hesperidin to microbial fermentation treatment with Aspergillus saitoi.Type: GrantFiled: March 14, 2002Date of Patent: November 21, 2006Assignee: Japan Sci. Tech. Corp.Inventors: Toshihiko Osawa, Kenichiro Minato, Yoshiaki Miyake
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Patent number: 7138430Abstract: The invention describes novel nitrosated and/or nitrosylated nebivolol, novel nitrosated and/or nitrosylated metabolites of nebivolol and novel compositions comprising at least one nitrosated and/or nitrosylated nebivolol and/or at least one nitrosated and/or nitrosylated metabolite of nebivolol, and, optionally, at least one nitric oxide donor and/or at least one antioxidant or a pharmaceutically acceptable salt thereof, and/or at least one compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof, and/or at least one nitrosated compound used to treat cardiovascular diseases.Type: GrantFiled: October 29, 2003Date of Patent: November 21, 2006Assignee: NitroMed, Inc.Inventor: David S. Garvey
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Patent number: 7094914Abstract: A process for producing a dicarboxylic acid compound represented by the formula (4): wherein R1 and R2 are the same or different and each represents lower alkyl and the wavy line indicates that this compound is the E- or Z-isomer or a mixture of them, characterized by reacting a compound represented by the formula (2): wherein R1, R2 and the wavy line have the same meanings as the above, and one of X2 and X3 represents hydrogen and the other represents halogen, with nitrophenol represented by the formula (3): in the presence of a base; a process for producing a nitrochromone compound represented by the formula (5): wherein R1 has the same meaning as the above, characterized by reacting the dicarboxylic acid compound or carboxylic acid thereof with an acid; a process for producing an aminochromone compound which comprises reducing the nitrochromone compound; and a process for producing an amidochromone compound which comprises acylating the aminochromone compound are provided.Type: GrantFiled: February 27, 2003Date of Patent: August 22, 2006Assignees: Sumitomo Chemical Company, Limited, Ono Pharmaceutical Co., Ltd.Inventors: Hiroaki Hibino, Susumu Ohtsuka, Yasunobu Miyamoto, Tomoyasu Yoshida, Itsuo Okumoto
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Patent number: 7012149Abstract: A process is provided for making (?)-epigallocatechin gallate (EGCG) by subjecting a green tea extract to chromatography on a macroporous polar resin, eluting EGCG from the resin with a polar elution solvent, optionally concentrating the eluate, optionally regenerating the resin by desorbing the remaining catechins, and optionally concentrating the desorbed catechins.Type: GrantFiled: September 18, 2002Date of Patent: March 14, 2006Assignee: DSM IP Assets B.V.Inventors: David Carl Burdick, Heinz Egger, Andrew George Gum, Ingo Koschinski, Elena Muelchi, Isabelle Prevot-Halter
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Patent number: 6949537Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.Type: GrantFiled: April 5, 2004Date of Patent: September 27, 2005Assignee: Semafore Pharmaceuticals, Inc.Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
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Patent number: 6936726Abstract: The present invention refers to new products generated by the conjugation of flavanols with molecules that contain the thiol group. New molecules are obtained from polyphenolic plant extracts rich in oligomeric and polymeric procyanidines and prodelfinidins. In this way, new products are generated with antioxidant properties for application as protective agents for the organism against disorders such as cancer, cardiovascular diseases and premature aging. The invention also refers to obtaining these new agents from waste material generated by the agroalimentary industry. Since these waste materials are highly complex mixtures a simple and effective method is described to isolate and purify these, based on the physico-chemical characteristics of the new molecules.Type: GrantFiled: December 14, 2001Date of Patent: August 30, 2005Assignee: Consejo Superior de Investigaciones CientificasInventor: José Luis Torres Simón
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Patent number: 6924376Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: April 11, 2003Date of Patent: August 2, 2005Assignees: Cytokinetics, Inc., Smithkline Beecham CorporationInventors: Andrew McDonald, Gustave Bergnes, Bainian Feng, David J. Morgans, Jr., Steven David Knight, Kenneth A. Newlander, Dashyant Dhanak, Christopher A. Brook
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Patent number: 6849746Abstract: A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.Type: GrantFiled: January 31, 2003Date of Patent: February 1, 2005Assignee: Mars, Inc.Inventors: Leo J. Romanczyk, Jr., Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
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Publication number: 20040225137Abstract: Disclosed are processes for producing chromane compounds, preferably chroman-2-yl acetic acid compounds and 6-amino-chroman-2-yl acetic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors.Type: ApplicationFiled: August 25, 2003Publication date: November 11, 2004Inventors: James Kanter, John J.G. Mullins, Robert Scarborough, Derek Walker, Thomas Hense
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Publication number: 20040202624Abstract: The invention relates to compounds of the formula I 1Type: ApplicationFiled: April 28, 2004Publication date: October 14, 2004Inventors: Frank Pfluecker, Joachim Buenger, Hans-Juergen Driller, Herwig Buchholz, Ralf Rosskopf
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Publication number: 20040192672Abstract: The present invention relates to iodobenzopyran-4-one derivativespossessing fungicidal properties against phytopathogenic organisms, amethod for preparing some of these derivatives. their use for protecting plants, and fungicidal compositions comprising such derivatives incombination with one or more other lungicidal compounds.Type: ApplicationFiled: January 30, 2004Publication date: September 30, 2004Inventors: Thomas Wegmann, Nathalie Huser, Rainer Karl Preuss, Joseph Perez
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Publication number: 20040176440Abstract: Novel compounds of the formula I 1Type: ApplicationFiled: December 2, 2003Publication date: September 9, 2004Inventors: Teresa Mujica-Fernaud, Herwig Buchholz, Christophe Carola, Wilfried Rautenberg, Christian Sirrenberg
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Patent number: 6750248Abstract: Methods for preparing an estrogenic preparation and isolating estrogenic compounds from a plant, such as an Epimedium plant, are provided. Also provided are estrogenic compounds from Epimedium plant that have been isolated and characterized, and methods for their use in modulating estrogen receptors and in treating conditions mediated by estrogen receptors, such as menopause and estrogen-dependent cancers. Also provided are preparations from Epimedium that are enriched for estrogenic compounds, and methods for their use in modulating estrogen receptors and preventing and treating conditions that are mediated by estrogen receptors.Type: GrantFiled: November 5, 2002Date of Patent: June 15, 2004Assignee: National University of SingaporeInventors: Eu Leong Yong, Sook Peng Yap
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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
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Publication number: 20040092579Abstract: Chromanone derivatives of the formula I 1Type: ApplicationFiled: July 29, 2003Publication date: May 13, 2004Inventors: Heinz-Hermann Bokel, Christoph Muermann, Uschi Schmid
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Publication number: 20040087575Abstract: Provided herein is a compound of the formula (I) wherein said compound is 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 antagonists. Also provided herein are processes for making compounds of Formula (I) and intermediate compounds.Type: ApplicationFiled: July 16, 2003Publication date: May 6, 2004Inventors: Marc Chapdelaine, Timothy Davenport, Markus Haeberlein, Carey Horchler, John McCauley, Edward Pierson, Daniel Sohn
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Publication number: 20040082638Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: ApplicationFiled: April 11, 2003Publication date: April 29, 2004Applicant: Cytokinetics, Inc.Inventors: Andrew McDonald, Gustave Bergnes, Bainian Feng, David J. Morgans, Steven David Knight, Kenneth A. Newlander, Dashyant Dhanak, Christopher A. Brook
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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
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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