专利号:US-2009099061-A1 优先权日:2006-01-27 标 题:Synthesis of carotenoid analogs or derivatives with improved antioxidant characteristics 发明人:FOSS BENTE J; NADOLSKI GEOFFRY T; LOCKWOOD SAMUEL F 权利人:FOSS BENTE J; NADOLSKI GEOFFRY T; LOCKWOOD SAMUEL F 摘要:A method is described for synthesizing and administering carotenoid compounds with improved antioxidant characteristics. In some embodiments, extension or improvement of conjugation may be employed in structural modification of carotenoids. In other embodiments, reduction of ring/chain steric hindrance may improve the lambda max, and hence, the overall antioxidant capability, of particular compounds. In other embodiments, introduction and/or increase in synthetic handles for conjugation may improve the stoichiometric ratios of conjugating moieties to the polyene backbone. The methods may be used to improve natural and/or synthetic compounds for medicinal application in the treatment of disease.
专利号:US-2005124683-A1 优先权日:2003-09-17 标 题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis 发明人:ALEGRIA LARRY A; CANAN-KOCH STACIE S; DRESS KLAUS R; HUANG BUWEN; KUMPF ROBERT A; LEWIS KATHLEEN K; MATTHEWS JEAN J; SAKATA SYLVIE K; VIRGIL SCOTT C 权利人:AGOURON PHARMA 摘要:The present invention relates to a series of chemical compounds useful as Human Immunodeficiency Virus (HIV) protease inhibitors and to the use of such compounds as antiviral agents. The invention further relates to pharmaceutical compositions containing such antiviral agents, and their uses and materials for their synthesis
专利号:US-7179918-B2 优先权日:2001-06-11 标 题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis 发明人:CANAN KOCH STACIE S; ALEXANDER THERESE N; BURKE BENJAMIN J; JEWELL TANYA M; KUCERA DAVID J; LINTON MARIA ANGELICA; MITCHELL JR LENNERT J; REICH SIEGFRIED H; SKALITZKY DONALD J; TATLOCK JOHN H; VARNEY MICHAEL D; VIRGIL SCOTT C; WEBBER STEPHEN E; WORLAND STEPHEN T; BARVIAN MARK; BOLTON GARY; BOYER JR FREDERICK EARL; MACHAK JEFFREY J; HOLLER TOD; MURPHY SEAN T; MELNICK MICHAEL; JOSYULA VARA PRASAD 权利人:AGOURON PHARMA 摘要:Compounds of the formula: n nwhere the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.
专利号:US-2008004415-A1 优先权日:2004-05-03 标题 :Non-linear optically active molecules, their synthesis, and use 发明人:MCGINNISS VINCENT D; RISSER STEVEN M; DROTLEFF ELIZABETH; JIANG EDWARD; SPAHR KEVIN B 权利人:OPTIMER PHOTONICS INC 摘要:In one aspect, the present invention provides a hyperpolarizable organic chromophore. The chromophore is a nonlinear optically active compound that includes a Ï€-donor conjugated to a Ï€-acceptor through a Ï€-electron conjugated bridge. In other aspects of the invention, donor structures and acceptor structures are provided. In another aspect of the invention, a chromophore-containing polymer is provided. In one embodiment, the chromophore is physically incorporated into the polymer to provide a composite. In another embodiment, the chromophore is covalently bonded to the polymer, either as a side chain polymer or through crosslinking into the polymer. In other aspects, the present invention also provides a method for making the chromophore, a method for making the chromophore-containing polymer, and methods for using the chromophore and chromophore-containing polymer.
专利号:EP-1836163-B1 优先权日:2004-12-23 标题 :Pyrrolidine derivatives for the treatment of a disease depending on the activity of renin 发明人:BREITENSTEIN WERNER; COTTENS SYLVAIN; EHRHARDT CLAUS; JACOBY EDGAR; LORTHIOIS EDWIGE LILIANE JEANNE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER; SIMIC OLIVER 权利人:NOVARTIS AG 摘要:Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.
专利号:US-7723498-B2 优先权日:2004-06-04 标题:Directed evolution of recombinant monooxygenase nucleic acids and related polypeptides and methods of use 发明人:WOOD THOMAS K; VARDAR GONUL 权利人:UNIV CONNECTICUT 摘要:The present invention relates to novel monooxygenase nucleic acids and polypeptides created using mutagenesis, DNA shuffling, or both, in a single iteration or multiple iterations, and methods for their creation and use. The monooxygenase enzymes of the present disclosure have particular utility as biocatalysts in industrial chemical redox reactions, such as the oxidation of aromatic hydrocarbons, for example, toluene, benzene, or nitrobenzene, into industrially desirable products. The systems and processes of the present invention are especially useful for the coupled synthesis and recovery of catechols, methylcatechols, resorcinols, methylresorcinols, hydroquinones, methylhydroquinones, hydroxybenzenes, cresols, nitrobenzenes, and nitrohydroxyquinones.
[参考文献]: Cristina Alfaro, Et Al. Screening For Metabolites From Penicillium Novae-Zeelandiae Displaying Radical-Scavenging Activity And Oxidative Mutagenicity: Isolation Of Gentisyl Alcohol. Mutat Res. 2003 Aug 5;539(1-2):187-94. [参考文献]: M Bruze, Et Al. Contact Allergy To 3-Methylol Phenol, 2,4-Dimethylol Phenol And 2,6-Dimethylol Phenol. Acta Derm Venereol. 1985;65(6):548-51.
合成参考文献
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