专利号:WO-2017137895-A1 优先权日:2016-02-09 标题 :New dendrimeric pyrrolidines, their synthesis and medical use 发明人:CARDONA FRANCESCA; PARMEGGIANI CAMILLA; MATASSINI CAMILLA; GOTI ANDREA; MORRONE AMELIA; CATARZI SERENA; D'ADAMIO GIAMPIERO 权利人:UNIVERSITA' DEGLI STUDI DI FIRENZE; AZIENDA OSPEDALIERO UNIV MEYER 摘要:The subject-matter of the present invention relates to the synthesis of new dendrimeric molecules based on polyhydroxylated pyrrolidines obtained by means of Click Chemistry reactions. The proposed molecules inhibit the enzymes N-acetylgalactosamine-6-sulfatase (GALNS), iduronate-2-sulfatase (IDS), a-mannosidase and β-glucosidase, deficient in lysosomal storage diseases. The presentation of multivalent iminosugars on a scaffold is a prerequisite for the inhibitory activity as the corresponding monomers are not active. The inhibitory activity reported is the basis for the development of the first-ASSC pharmacological chaperones proposed for the treatment of the above mentioned pathologies. Formula (I)
专利号:US-5419966-A 优先权日:1991-06-10 标 题 :Solid support for synthesis of 3'-tailed oligonucleotides 发明人:REED MICHAEL W; MEYER JR RICH B; PETRIE CHARLES R; TABONE JOHN C 权利人:MICROPROBE CORP 摘要:A solid support for oligonucleotide synthesis has the structure where CPG represents a controlled pore glass matrix, the wavy line represents a carbon chain covalently linking the NH group with the controlled pore glass matrix, X is 2,2'-dimethoxytrityl or H, and R is alkyl, aryl, arylalkyl, heteroalkyl, or heteroaryl. The dimethoxytrityl group is removed from the solid support by treatment with acid, and the oligonucleotide is built, step-by-step in a conventional synthesizer after attachment of the 3' end of the first oligonucleotide unit to the hydroxyl function connected to the R group.
专利号:WO-9318787-A1 优先权日:1992-03-25 标 题 :Trans-sialidase and methods of use and making thereof 发明人:NUSSENZWEIG VICTOR; SCHENKMAN SERGIO; EICHINGER DAN; VANDEKERCKHOVE FLIP 权利人:UNIV NEW YORK 摘要:Polypeptides are provided having trans-sialidase enzymatic activity in substantially pure form, nucleic acids coding therefor, antibodies specific for such polypeptides, processes for producing the enzyme and methods of use of the enzyme, in particular for the synthesis of sialyl α(2â†?3)-linked saccharides, glycoproteins and glycolipids. Such enzymes are isolatable as nucleic acid or amino acid sequences from parasites of the genus Trypanosoma.
专利号:WO-2005040371-A1 优先权日:2003-10-29 标题 :Engineered enzymes and their use for synthesis of thioglycosides 发明人:WITHERS STEPHEN G; JAHN MICHAEL 权利人:UNIV BRITISH COLUMBIA; WITHERS STEPHEN G; JAHN MICHAEL 摘要:Mutant glycosidases that are the subject of this invention (Fig. 1 D) have both the amino acids in the active site that serve as the acid, base, or acid/base catalyst, and the amino acid in the active site that serves as the catalytic nucleophile converted to some other amino acid (for example to a simple alkyl, as in alanine, or H, as in glycine) different from the wild-type amino acid. These double mutant enzymes, acting in the fashion of a scaffold, can catalyze the reaction of a thiosugar acceptor and a glycosyl donor (that has a good leaving group in the 1-position) to form a thioglycoside. The 'thioglycosynthases' represent a novel class of mutant enzymes and represent a first aspect of the invention. Thioglycosynthases can be used in accordance with the method of the invention to couple a thiosugar acceptor and an activated donor to form a thioglycoside. By selection of the donor and acceptor species, as well as the specific enzyme employed, thioglycosides of different structure and stereochemistry can be obtained.
专利号:US-6150403-A 优先权日:1997-10-14 标 题 :Topical compositions for regulating the oily/shiny appearance of skin 发明人:BIEDERMANN KIMBERLY A; SCHUBERT HARRY L; PARRAN JR JOHN J 权利人:PROCTER & GAMBLE 摘要:The present invention relates to methods for inhibiting sebaceous gland activity in mammalian skin comprising administration of a topical composition comprising dehydroacetic acid or pharmaceutically acceptable salts thereof, and a dermatologically-acceptable carrier. The present invention also relates to methods and topical compositions further comprising agents which regulate the oily and/or shiny appearance of skin, and agents which treat acne and related skin disorders in mammalian skin and scalp. Methods of reducing sebum synthesis with the use of dehydroacetic acid, methods of regulating the oily and/or shiny appearance of skin, and methods of treating acne and other skin disorders are also encompassed by the present invention.
专利号:US-2007232495-A1 优先权日:2006-03-24 标题:Compositions and methods to add value to plant products, increasing the commercial quality, resistance to external factors and polyphenol content thereof 发明人:NAPPA ALVARO O; LORENZINI FELIPE C; SANHUEZA ANDRES L 权利人:NAPPA ALVARO O; LORENZINI FELIPE C; SANHUEZA ANDRES L 摘要:The invention is related to compositions and methods that naturally protect plant tissues against ultraviolet radiation and temperature, thus giving protection against sunburn to plants, plant parts, fruits and/or flowers during their development. The invention is also related to compositions and methods to naturally improve the color of plants, plant parts, fruits and/or flowers by inducing the natural synthesis of flavonoids and anthocyanins present in plants. Likewise, the present invention is directed to improving the nutritional value of plants, plant parts, fruits and/or flowers by increasing the normal levels of polyphenolic compounds, especially flavonoids, present therein. Additionally, the present invention is related to compositions and methods that give more resistance to plants, plant parts, fruits and/or flowers against pathogens as bacteria and fungi. Finally, the present invention is related to plants, plant parts, fruits, flowers and/or propagating material treated with the compositions described in the present document.