专利号:EP-0725144-A1 优先权日:1995-02-06 标题 :Process for the preparation of glycosides using glycosidases from ciliates 发明人:KIY THOMAS DR; HOERSCH BRIGITTE DR; MARQUARDT RUEDIGER DR 权利人:HOECHST AG 摘要:The invention relates to a process for the production of glycosides by enzymatic glycosylation by means of α- and β-glycosidases from holotrich ciliates and in particular from Hymenostomatida.n n n Glycosidases from holotrich ciliates are very well suited for the enzymatic synthesis of alkyl glycosides, glycopeptides, di- or oligosaccharides. Preferred glycosyldoren are nitrophenylglycosides, glycosyl fluorides or disaccharides, preferred acceptors are short-chain alcohols, polyhydroxy compounds, in particular monosaccharides, or protected hydroxyamino acids or corresponding peptides.
专利号:US-2025011792-A1 优先权日:2021-12-01 标题:Irap inhibitors for use in the treatment of inflammatory diseases 发明人:HERMINE OLIVIER; WEIMERSHAUS MIRJANA; TROVATI MACIEL THIAGO; VAN ENDERT PETER; DUSSIOT MICHAEL; RIGNAULT-BRICARD RACHEL; CARVALHO CAROLINE 权利人:INST NAT SANTE RECH MED; ASSIST PUBLIQUE HOPITAUX PARIS APHP; FOND IMAGINE; UNIV PARIS CITE; CENTRE NAT RECH SCIENT 摘要:Upon activation, mast cells rapidly release preformed inflammatory mediators from large cytoplasmic granules via regulated exocytosis. This acute degranulation is followed by a late activation phase involving synthesis and secretion of cytokines, growth factors and other inflammatory molecules via the constitutive pathway that remains ill-defined. Here the inventors describe a role for an insulin-responsive vesicle-like endosomal compartment, marked by insulin-regulated aminopeptidase (IRAP), in the secretion of TNF-α and IL-6 in mast cells and macrophages. IRAP-deficient mice are protected from TNF-dependent kidney injury and inflammatory arthritis. In the absence of IRAP, TNF fails to be efficiently exported from the Golgi. Chemical targeting of IRAP+ endosomes reduced pro-inflammatory cytokine secretion thereby highlighting this compartment as a promising target for the therapeutic control of inflammation. Thus the present invention relates to the use of IRAP inhibitors for the treatment of inflammatory diseases
专利号:US-5852005-A 优先权日:1994-07-27 标 题:Tetracyclic triterpenes 发明人:HIESTAND PETER; NAEF RETO; NAEGELI HANS-ULRICH; OBERER LUKAS; REVESZ LASZLO; ROTH HANS-JOERG 权利人:NOVARTIS AG 摘要:The present invention relates to 17 α-dammara compounds having immunosuppressant and antiinflammatory activity and which are useful as pharmaceuticals, particularly for use as immunosuppressant and antiinflammatory agents. Specific 17 α-dammara compounds are included per se, for example the compound of formula IC, i.e. 17 α-23-(E)-dammara-20, 23-dien-3β, 25-diol, which may be obtained from the flour of the shoots of the Palmyrah palm, Borassus flabellifer L. In addition, processes for the synthesis of this and other dammara compounds and intermediates thereof are described.
专利号:US-4918009-A 优先权日:1985-12-11 标 题:Method of controlling the regioselectivity of glycosidic bonds 发明人:NILSSON KURT G I 权利人:SVENSKA SOCKERFABRIKS AB 摘要:A method of controlling the regioselectivity of the glycosidic bond between glycosyl donor and glycosyl acceptor in the enzymatic production of an oligosaccharide compound which either consists of or is a fragment or an analog of the cabohydrate part in a glycoconjugate, by reverse hydrolysis or transglycosidation reactions, is described. The synthesis is carried out in that a donor substance which is a mono- or oligosaccharide or a glycoside thereof, is caused to react, in the presence of a glycosidase, with an acceptor substance which is an O-, N-, C- or S-glycoside consisting of a monosaccharide, oligosaccharide or a saccharide analog and at least one aglycon which is O-, N-, C- or S-glycosidically bonded in 1-position, the alpha or beta -configuration being selected on the glycoside bond between the glycosyl group and the aglycon in the acceptor substance, and the oligosaccharide compound being separated from the reaction mixture.
专利号:US-5433947-A 优先权日:1992-12-15 标 题 :Antifungal synergistic combination of enzyme fungicide and non-enzymatic fungicide and use thereof 发明人:HARMAN GARY E; LORITO MATTEO; PIETRO ANTONIO D; HAYES CHRISTOPHER K 权利人:CORNELL RES FOUNDATION INC 摘要:Antifungal composition comprising synergistic combination of fungal cell wall degrading enzyme selected from the , group consisting of chitinolytic enzymes, glucanolytic enzymes and cellulases and non-enzymatic fungicides selected from the group consisting of sterol synthesis inhibiting fungicides (e.g., flusilazole and miconazole) and thiol group inactivating fungicides which are not specific to fungal cell membranes (e.g., captan) are applied in an antifungal effective amount to fungus to be inhibited or to a locus to be protected from said fungus.
专利号:US-6090944-A 优先权日:1998-08-13 标 题:Alkanoic acid derivatives as αv integrin receptor antagonists 发明人:HUTCHINSON JOHN H 权利人:MERCK & CO INC 摘要:The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3, αvβ5 and/or αvβ6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, and tumor growth and metastasis.
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合成参考文献
参考文献:10.1021/jf9039952 摘要:Xie X, Zhou H, Huang Q, Wei X, Wang Y, Yan J, Chen Q. Inhibitory Kinetics of Betaine on β-N-Acetyl-d-glucosaminidase from Prawn (Litopenaeus vannamei). J. Agric. Food Chem. 2010 Feb 16;58(6):3820–4. doi: 10.1021/jf9039952.