Chalcogen Or Nitrogen Attached Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/407)
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Patent number: 7932254Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1 and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: February 20, 2009Date of Patent: April 26, 2011Assignee: Roche Palo AltoInventors: Daisy Joe DuBois, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Yan Lou, Timothy D. Owens, Calvin Wesley Yee
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Publication number: 20110021793Abstract: The present invention relates to a process for reducing a compound of formula (I) wherein X is halogen, a hydroxy group, an alkylsulfoniloxy group or an arylsulfonyloxy group; to give a compound of formula (II) as a di-astereoisomerically pure compound of RS/SR configuration characterized in that said reduction is carried out by the use of (+)-B-chlorodiisopinocampheylborane or (?)-B-chlorodiisopinocampheylborane. The compounds of formula (II) are useful as intermediates for the preparation of Nebivolol.Type: ApplicationFiled: March 16, 2009Publication date: January 27, 2011Applicant: ZACH SYSTEM S.P.A.Inventors: Raffaella Volpicelli, Paolo Maragni, Franco Massaccesi, Ilaria Munari, Livius Cotarca, Johnny Foletto
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Patent number: 7858812Abstract: The present invention relates to a simple and commercially viable process for separation of desired isomers of nebivolol intermediates from a mixture containing undesired isomers of nebivolol intermediates. Thus, (+)-[2R*[1S*,5S*(S*)]]+[2R*[1S*,5R*(R*)]]-?,??-[phenylmethyliminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol] is dissolved in diisopropyl ether at reflux temperature and cooled to below about 30° C. to obtain the desired (+)-[2R*[1S*,5S*(S*)]]-?,??-[phenylmethyliminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol].Type: GrantFiled: January 18, 2006Date of Patent: December 28, 2010Assignee: Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Itiyala Srinivas Reddy
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Publication number: 20100298582Abstract: Disclosed herein is a compound of formula (I): wherein: Bn represents benzyl; Me represents methyl; and Y represents an oxygen atom or a CH2 group. The compound of formula (I) can be used in the preparation of 7-benzyloxy-3-(4-methoxyphenyl)-2H-1-benzopyran, Preparation processes of said compound of formula (I) are also disclosed herein.Type: ApplicationFiled: May 19, 2009Publication date: November 25, 2010Applicant: KaoHsiung Medical UniversityInventors: Eng-Chi Wang, Sie-Rong Li
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Publication number: 20100298580Abstract: Compounds of formula I, V, VI and II, and processes for their preparation, wherein R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl. There is also provided a process for preparing a compound of formula B from the compounds of formula V and I.Type: ApplicationFiled: November 13, 2008Publication date: November 25, 2010Applicant: BIAL - PORTELA & CA, S.A.Inventors: Brian Broadbelt, Alexander Beliaev, David Alexander Learmonth
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Publication number: 20100273869Abstract: Compounds are disclosed relating to the treatment of cancer that include tocotrienols and derivatives of tocotrienols including 2,5,7,8-tetramethyl-2-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)chroman-6-ylphenylsulfonylcarbamate; (R)-2,8-dimethyl-2-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)chroman-6-yl tosylcarbamate; and (R)-2,5,7,8-tetramethyl-2-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-trienyl)chroman-6-yl benzylcarbamate. Therapeutic uses of these types of compounds are also taught.Type: ApplicationFiled: April 23, 2010Publication date: October 28, 2010Applicant: FIRST TECH INTERNATIONAL LIMITEDInventors: Paul W. Sylvester, Khalid A. El Sayed
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Patent number: 7820837Abstract: The present invention aims at providing a novel fused ring compound having a GPR40 receptor function modulating action and being useful as an insulin secretagogue or a pharmaceutical agent for the prophylaxis or treatment of diabetes, more particularly, a compound represented by the formula: wherein Ar is an optionally substituted cyclic group, ring A is a ring optionally further substituted (provided that the ring is not thiazole, oxazole, imidazole and pyrazole), Xa and Xb are each independently a bond or a spacer having a main chain of 1 to 5 atom(s), Xc is O, S, SO or SO2, ring B is a 5- to 7-membered ring, Xd is a bond, CH or CH2, is a single bond when Xd is a bond or CH2, or a double bond when Xd is CH, and R1 is an optionally substituted hydroxy group, and a salt thereof.Type: GrantFiled: May 28, 2004Date of Patent: October 26, 2010Assignee: Takeda Pharmaceutical Company LimitedInventors: Tsuneo Yasuma, Nobuyuki Negoro
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Publication number: 20100267820Abstract: Vitamin E succinate derivatives according to formula I: are described. These compounds can be included in pharmaceutical compositions, and can be used for the treatment of cancers such as metastatic cancer and as antiadhesive agents.Type: ApplicationFiled: April 16, 2010Publication date: October 21, 2010Applicant: THE OHIO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: Ching-Shih Chen, Dasheng Wang, Samuel K. Kulp
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Publication number: 20100197684Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: February 9, 2010Publication date: August 5, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Matthew Abelman, Robert Jiang, Jeff Zablocki
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Patent number: 7759389Abstract: 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: July 20, 2010Assignee: Roche Palo Alto LLCInventors: Nancy Elisabeth Krauss, Shu-Hai Zhao
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Patent number: 7754759Abstract: Compounds of the formula I: wherein m, n, p, X, Ar, R1, R2, R3, R4 and R5 are as defined herein. Methods of making the compounds and using the compounds for treatment of 5-HT6 receptor-mediated diseases are disclosed.Type: GrantFiled: November 3, 2006Date of Patent: July 13, 2010Assignee: Roche Palo Alto LLCInventors: Jacob Berger, Joan Marie Caroon, Francisco Javier Lopez-Tapia, Lee Edwin Lowrie, Jr., Dov Nitzan, Shu-Hai Zhao
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Publication number: 20100168448Abstract: The invention relates to methods of preparing cannabinoids in substantially pure form starting from plant material. Also described are substantially pure preparations of various cannabinoids and cannabinoid acids, and also extracts enriched in cannabinoids and cannabinoid acids.Type: ApplicationFiled: March 1, 2010Publication date: July 1, 2010Applicant: GW Pharma LimitedInventors: Ian Flockhart, Gary William Wheatley, Su Dring, Leslie Archer
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Publication number: 20100056813Abstract: The present invention relates to a process for preparing nebivolol and, more particularly, to a process for preparing d-nebivolol and its enantiomer l-nebivolol or acid addition salts thereof starting from commercially available or easily obtainable 2,2-dimethyl-1,3 dioxolane-4-carbaldehyde and a vinyl Grignard reagent.Type: ApplicationFiled: November 23, 2007Publication date: March 4, 2010Applicant: ZACH SYSTEM S.P.A.Inventors: Raffaella Volpicelli, Paolo Maragni, Livius Cotarca, Johnny Foletto, Franco Massaccesi
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Publication number: 20100048512Abstract: Administration of either a tocopherol represented by the general formula (1) or a tocotrienol compound ester derivative before or after exposure to radiation is effective in preventing or treating health disorders caused by the radiation exposure.Type: ApplicationFiled: November 14, 2007Publication date: February 25, 2010Applicants: National Institute of Radiological Sciences, Fukuoka UniversityInventors: Kazunori Anzai, Megumi Ueno, Haruko Yakumaru, Junichi Ueda, Makoto Akashi, Shizuko Kobayashi, Jiro Takata, Nobuo Ikota
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Patent number: 7632861Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.Type: GrantFiled: November 7, 2008Date of Patent: December 15, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Joanne J. Bronson, Andrew P. Degnan, William D. Schmitz
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Publication number: 20090306413Abstract: The contemplated invention relates to the field of synthesis of biologically active substances, namely to the synthesis of an acetate derivative of the main water-soluble ?-tocopherol metabolite known under the name of ?-CEHC, which is prepared by the acid-catalyzed reaction of condensation of trimethyl hydroquinone with linalool in boiling octane, using n-toluenesulfonic acid or (+)-camphor-10-sulfonic acid as the catalyst. The reaction is carried out for 3 hours at the trimethyl hydroquinone:linalool:catalyst mole ratio of 1:1:0.1. The forming product is acetylated with acetic anhydride in pyridine at room temperature for 0.5 hour, and then ozonized in acetone in the presence of Ba(OH)2, oxidized with Jones' reagent in acetone, and isolated on silica gel column chromatography. Said compound is an acetate derivative of the main ?-tocopherol metabolite—?-CEHC, for which high efficiency has been noted in treating disorders of the central nervous system.Type: ApplicationFiled: June 15, 2006Publication date: December 10, 2009Inventors: Anna Yulievna Spivak, Viktor Nikolaevich Odinokov, Oxana Valerievna Knyshenko
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Patent number: 7615650Abstract: The invention provides a process for producing a chroman compound represented by formula (1), characterized in that the process includes allowing a phenol, an unsaturated compound, and a formaldehyde to react in the absence of catalyst and in the presence of water in an amount by mole 1 to 10 times that of the phenol. According to the present invention, a high-purity chroman compound can be produced in the absence of catalyst and under mild conditions. In addition, the invention provides an industrial means for producing the compound, without using a large amount of an acid or a base serving as a reaction promoter or a catalyst, which would otherwise cause side reactions, apparatus corrosion, etc.Type: GrantFiled: January 28, 2005Date of Patent: November 10, 2009Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Kazuo Tanaka, Youichi Kyuuko, Toshio Hidaka
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Publication number: 20090198050Abstract: The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.Type: ApplicationFiled: October 31, 2008Publication date: August 6, 2009Inventors: Eric Marsault, Luc Ouellet, Carl St-Louis, Sylvie Beaubien, Kamel Benakli, Hamid R. Hoveyda, Mark L. Peterson, Shridhar Bhat
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Patent number: 7560575Abstract: A process of making racemic [2S*[R*[R*[R*]]]] and [2R*[S*[S*[S*]]]]-(±)?,??-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol] of the compound of the formula (I) and its pure [2S*[R*[R*[R*]]]]- and [2R*[S*[S*[S*]]]]-enantiomer compounds and pharmaceutically acceptable salts thereof.Type: GrantFiled: December 28, 2005Date of Patent: July 14, 2009Assignee: Acino Pharma AGInventors: Thomas Bader, Alfred Stutz, Harald Hofmeier, Hans-Ulrich Bichsel
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Publication number: 20090124613Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.Type: ApplicationFiled: November 7, 2008Publication date: May 14, 2009Inventors: Joanne J. Bronson, Andrew P. Degnan, William D. Schmitz
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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: 20090104118Abstract: The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.Type: ApplicationFiled: December 19, 2008Publication date: April 23, 2009Inventors: Heike S. Radeke, David S. Casebier, Michael T. Azure, Douglas D. Dischino
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Publication number: 20090076288Abstract: The present invention relates to a simple and commercially viable process for separation of desired isomers of nebivolol intermediates from a mixture containing undesired isomers of nebivolol intermediates. Thus, (+)-[2R*[1S*,5S*(S*)]]+[2R*[1S*,5R*(R*)]]-?,??-[phenylmethyliminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol] is dissolved in diisopropyl ether at reflux temperature and cooled to below about 30° C. to obtain the desired (+)-[2R*[1S*,5S*(S*)]]-?,??-[phenylmethyliminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol].Type: ApplicationFiled: January 18, 2006Publication date: March 19, 2009Applicant: HETERO DRUGS LIMITEDInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Itiyala Srinivas Reddy
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Publication number: 20090069415Abstract: The present application describes deuterium-enriched nebivolol, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 3, 2008Publication date: March 12, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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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: 20090005437Abstract: The present invention relates generally to the field of pharmaceuticals and medicine. More particularly, the present invention relates to certain compounds (e.g., ?-ketoglutarate compounds; compounds that activate HIF? hydroxylase; compounds that increases the level of ?-ketoglutarate, etc.) and their use in medicine, for example, in the treatment of cancer (e.g., cancer in which the activity of one of the enzymes in the tricarboxylic acid (TCA) cycle is down regulated), in the treatment of angiogenesis (e.g., hypoxia-induced angiogenesis). One preferred class of compounds are ?-ketoglutarate compounds having a hydrophobic moiety that is, or is part of, an ester group formed from one of the acid groups of ?-ketogluartic acid; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof.Type: ApplicationFiled: August 9, 2005Publication date: January 1, 2009Inventors: Eyal Gottlieb, Mary A. Selak, Elaine D. MacKenzie, David G. Watson
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Patent number: 7429411Abstract: The compound (1) according to the invention has general solid-state properties necessary for a compound, stability against heat, light and the like, a suitable optical anisotropy, a suitable dielectric anisotropy, and excellent compatibility with other liquid crystalline compounds. The liquid crystal composition according to the invention contains at least one compound represented by formula (1). The liquid crystal display element according to the invention contains the composition. The compound (1) is represented by formula (1): wherein Ra, Rb, A1, A2, A3, A4, A5, A6, Z11, Z12, Z13, Z14, Z15, Z16, Y1, Y2, k, l, m, n, p and q are as defined in the specification.Type: GrantFiled: June 23, 2004Date of Patent: September 30, 2008Assignees: Chisso Petrochemical Corporation, Chisso CorporationInventors: Teruyo Sugiura, Makoto Ushioda
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Patent number: 7427693Abstract: Compounds that are useful in compositions for flat panel displays, for example, are provided. The compounds provided are polar, and are useful in low threshold voltage mixtures. The compounds provided have the general structure: CpCOCH2[A]nZ1[B]mZ2PhX1X2Y, where CpCOCH2 is the structure: A and B are independently in each instance selected from the group consisting of 1,4-cyclohexane, 1,4-phenyl, 1,3-dioxan-5,2-diyl; pyridine-5,2-diyl; and pyrimidin-5,2-diyl; n and m are independently in each instance 0, 1 or 2; Z1 and Z2 are independently a single bond, —(CH2)2—, CF2O, OCF2, CH2O, OCH2, —C?C—, COO, OOC; and Y is selected from the group consisting of: F, Cl, CN, OCH2F, CHF2, OCF3, and CF3.Type: GrantFiled: April 3, 2007Date of Patent: September 23, 2008Assignee: Daily Polymer CorporationInventor: Xinhua Chen
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Publication number: 20080221340Abstract: The subject of the invention is a process for the production of the racemic active ingredient nebivolol, in which diastereomeric cyanohydrins are produced, separated, and the separated diastereomers are coupled to one another after a transformation, preferably a partial or complete reduction of the cyano group or a Pinner saponification.Type: ApplicationFiled: July 17, 2006Publication date: September 11, 2008Applicant: Pharmacon Forschung und Bearatung GmbHInventors: Christian R. Noe, Muhamed Jasic, Hermann Kollmann, Bodo Lachmann
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Patent number: 7410998Abstract: Benzopyran-based inhibitors of NADH:ubiquinone oxidoreductase for inhibiting the growth of cancer cells.Type: GrantFiled: September 6, 2001Date of Patent: August 12, 2008Assignee: The Scripps Research InstituteInventors: Kyriacos C. Nicolaou, Jeffrey Pfefferkorn, Guo-Qiang Cao, Anthony Roecker
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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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Patent number: 7365095Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R2, R3, R4, y, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.Type: GrantFiled: April 21, 2006Date of Patent: April 29, 2008Assignee: WyethInventors: Gavin David Heffernan, Gary Paul Stack, Jonathan Laird Gross, Dahui Zhou, Hong Gao
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Patent number: 7312232Abstract: The present invention provides an antiproliferative compound having the structural formula wherein X is oxygen, nitrogen or sulfur; Y is selected from the group consisting of oxygen, nitrogen and sulfur wherein when Y is oxygen or nitrogen, n is 1 and when Y is sulfur, n is 0. Also provided is a method for inducing apoptosis in a cell comprising administering a composition comprising a compound having said structural formula.Type: GrantFiled: August 20, 2003Date of Patent: December 25, 2007Assignee: Research Development FoundationInventors: Bob G. Sanders, Kimberly Kline, Laurence Hurley, Robb Gardner, Marla Menchaca, Weiping Yu, Puthucode N. Ramanan, Shenquan Liu, Karen Israel
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Patent number: 7297715Abstract: A class of chromane and chromene compounds having the structure shown below and pharmaceutically acceptable salts thereof are useful as therapeutic compounds, particularly in the treatment and control of hyperlipidemia, hypercholesterolemia, dyslipidemia, and other lipid disorders, and in delaying the onset of or reducing the risk of conditions and sequelae that are associated with these diseases, such as atherosclerosisType: GrantFiled: July 25, 2003Date of Patent: November 20, 2007Assignee: Merck & Co., Inc.Inventors: Ranjit C. Desai, Soumya Sahoo
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Patent number: 7217706Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: May 15, 2007Assignee: Astellas Pharma Inc.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 7148240Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.Type: GrantFiled: August 23, 2001Date of Patent: December 12, 2006Assignee: Sanofi-AventisInventors: Jean-Louis Assens, Claude Bernhart, Frédérique Cabanel-Haudricourt, Dino Nisato
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Patent number: 7144919Abstract: The present invention relates to polyoxyethylene-polyoxypropylene (POE-POP) vitamin E, which is prepared from vitamin E by polyethoxylation and polypropoxylation, and a method for preparing the same. The POE-POP vitamin E has a high surface activity and an excellent safety for the skin, so that the POE-POP vitamin E can be advantageously used in the cosmetic industry, the food industry and the medical industry.Type: GrantFiled: August 23, 2000Date of Patent: December 5, 2006Inventors: Youngdae Kim, Keunja Park, Jungsoo Kim, Jisoo Kim
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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: 7045514Abstract: Provided herein is a compound having the formula (I): Wherein said compounds are useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B and 5HT1D antagonists.Type: GrantFiled: July 12, 2004Date of Patent: May 16, 2006Assignee: AstraZeneca ABInventors: Edward Pierson, Daniel Sohn, Markus Haeberlein, Timothy Davenport, Marc Chapdelaine, Carey Horchler, John P. McCauley
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Patent number: 6890952Abstract: Cyclic substituted aminomethyl compounds of general formula IA and IB, methods for production thereof, intermediates in said production methods, a medicament containing at least one of said cyclic substituted aminomethyl compounds, the use of said cyclic substituted aminomethyl compounds for the production of a medicament, pharmaceutical compositions containing said compounds, and methods for the treatment of pain, incontinence, pruritis, tinnitus aurium and/or diarrhea using said pharmaceutical compositions.Type: GrantFiled: January 10, 2003Date of Patent: May 10, 2005Assignee: Gruenenthal GmbHInventors: Oswald Karl Zimmer, Babette-Yvonne Koegel, Wolfgang Werner Alfred Strassburger
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Patent number: 6855833Abstract: 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: GrantFiled: June 1, 2001Date of Patent: February 15, 2005Assignee: Millennium Pharmaceuticals, Inc.Inventors: James Kanter, John J. G. Mullins, Robert Scarborough, Derek Walker, Thomas Hense
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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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Patent number: 6835845Abstract: A is a novel methine compound, for example, which is represented by the following formula (I): wherein R1, R2, R3, R4 and R5 each represents a hydrogen atom or a substituent; X represents an oxygen atom, a sulfur atom, or N—R6; Z represents —NR7R8, or —OG; R6, R7 and R8 each represents a hydrogen atom or a substituent; G represents a hydrogen atom, a cation or a substituent; L1, L2 and L3 each represents a substituted or unsubstituted methine group; n represents 1 or 2; and W represents an electron attractive group. Also, a material for organic luminescence element and organic luminescence element using the same are disclosed.Type: GrantFiled: July 26, 2002Date of Patent: December 28, 2004Assignee: Fuji Photo Film Co., Ltd.Inventors: Hisashi Okada, Terukazu Yanagi
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Patent number: 6818666Abstract: Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.Type: GrantFiled: August 9, 2002Date of Patent: November 16, 2004Assignee: Galderma Research & DevelopmentInventors: Jean-Michel Bernardon, Philippe Diaz
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Patent number: 6812225Abstract: Provided herein is a compound having the formula (I): Wherein said compounds are useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B and 5HT1D antagonists.Type: GrantFiled: January 16, 2002Date of Patent: November 2, 2004Assignee: AstraZeneca ABInventors: Edward Pierson, Daniel Sohn, Markus Haeberlein, Timothy Davenport, Marc Chapdelaine, Carey Horchler, John P. McCauley
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Patent number: 6750247Abstract: Compounds that are effective lipoxygenase inhibitors, and methods and pharmaceutical compositions for inhibiting lipoxygenases and for treatment of lipoxygenase-mediated conditions in humans and other subjects. The compounds, methods and pharmaceutical compositions utilize subersic terpenoids, jaspic terpenoids, igernellic terpenoids, hippospongic terpenoids, halicondric terpenoids, dictyodendric terpenoids, and/or heteronemic terpenoids, and synthetic derivatives or analogs thereof. Exemplary compounds include (−)-subersic acid, (+)-subersin, jaspaquinol, (−)-jaspic acid, igernellin, halisufate 7, and hipposulfate C and D, and derivatives thereof.Type: GrantFiled: May 31, 2002Date of Patent: June 15, 2004Assignee: Galileo Laboratories, Inc.Inventors: Phillip Crews, Jennifer Carroll, Theodore Holman, Guy Miller, Steve Bobzin, Lesley Brown
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Patent number: 6716873Abstract: Disclosed are novel tocopherol ester compounds having the formula wherein X is a chain of 2 or 3 carbon atoms, e.g., ethylene and trimethylene, joining the 2 carbonyl groups to which they are bonded; and R1 is a group having the formula —Y—R4 wherein Y is a selenium, tellurium or sulfur atom and R4 is an alkyl, cycloalkyl or aryl radical. The tocopherol ester compounds of formula (I) exhibit antiproliferative and growth inhibitory effects on breast cancer cell lines.Type: GrantFiled: March 20, 2003Date of Patent: April 6, 2004Assignee: Yasoo Health Inc.Inventors: Anastasios Keramidas, Andreani Odysseos, Andreas Michael Papas
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Patent number: 6700001Abstract: A process for the stereoselective synthesis of 2-hydroxymethyl-chromans of formula (II) is provided where R, R1, R2 and R3 are as defined herein. The compound of formula (II) is prepared using an optically active benzene compound of formula (I) where R0 is as defined herein. The 2-hydroxymethyl-chroman compounds of formula (II) are useful as intermediates for preparing a variety of medicinal agents.Type: GrantFiled: October 4, 2002Date of Patent: March 2, 2004Assignee: WyethInventors: Jonathan L. Gross, Gary P. Stack
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Patent number: 6699860Abstract: This invention is related to novel di-substituted aminomethyl chroman derivatives which are useful in the treatment of beta-3 receptor-mediated conditions.Type: GrantFiled: December 7, 2001Date of Patent: March 2, 2004Assignee: Bayer Pharmaceuticals CorporationInventors: Gaetan H. Ladouceur, William H. Bullock, Steven R. Magnuson, Stephen J. O'Connor, Roger A. Smith, Quanrong Shen, Qingjie Liu, Ning Su, Emil J. Velthuisen, Ann-Marie Campbell, Paul P. Ehrlich
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Patent number: 6683115Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.Type: GrantFiled: August 21, 2001Date of Patent: January 27, 2004Assignee: Theravance, Inc.Inventors: Edmund J. Moran, Seok-Ki Choi