专利号:US-4396542-A 优先权日:1980-02-14 标 题 :Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production 发明人:WENGER ROLAND 权利人:SANDOZ LTD 摘要:A method for the total synthesis of cyclosporins, in particular Cyclosporin A, cyclosporins produced in accordance with the method of the invention and novel intermediates, in particular novel [1S, 2R, 3R]- and [1R, 2S, 3S]-1-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes, employed in the method of the invention.
专利号:US-4554351-A 优先权日:1980-02-14 标 题:Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production 发明人:WENGER ROLAND 权利人:SANDOZ LTD 摘要:A method for the total synthesis of cyclosporins, in particular Cyclosporin A, cyclosporins produced in accordance with the method of the invention and novel intermediates, in particular novel [1S, 2R, 3R]- and [1R, 2S, 3S]-1-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes, employed in the method of the invention.
专利号:US-8293290-B2 优先权日:2003-04-08 标题:Annatto extract compositions, including geranyl geraniols and methods of use 发明人:TAN BARRIE 权利人:TAN BARRIE; AMERICAN RIVER NUTRITION INC 摘要:Annatto extract composition (AEC), including cis and trans geranyl geraniols (GG) and tocopherol-free C-5 unsubstituted tocotrienols (T3), increases the de novo synthesis of intermediate isoprenoid and distal protein products, including endogenous coenzyme Q10 (CoQ10), dolichols (DL) and all subsequent GG-prenylated and DL-glycosylated proteins, including GG-porphyrinated hemes. This intermediate and distal product replenishment by AEC reverses maladies of myotoxicity (of both drug and non-drug origins), including maladies that affect the muscle, kidney, eye, GI tract and skin, nerve, blood, and CoQ10-related syndromes of energetics and LDL protection. AEC anabolically increases the endogenous de novo CoQ10 synthesis via GG elongation/prenylation of side-chain and conversely CoQ10 catabolically increases the endogenous de novo GG synthesis via beta-oxidation of CoQ10. Also, such AEC decreases de novo synthesis and increases disposal of triglycerides (TG) in humans via PPAR activation and SREBP deactivation. Such drop in TG by AEC reverses maladies of insulin resistance (IR) and metabolic syndrome (MS), prediabetes, diabetes and diabetes-related cardiovascular diseases (CVD). GG activates PPAR and down regulates SREBP transcription factors. This AEC, containing GG, inhibits cancer growth whether or not GG involvement in protein prenylation is required.
专利号:US-5948693-A 优先权日:1994-09-01 标题:Solid phase synthesis of immunosuppressive agents 发明人:RICH DANIEL H; RAMAN PRAKASH; ANGELL YVONNE M 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The present invention relates generally to cyclosporin analogs, and more paritcularly to methods for the solid-phase synthesis and on-resin cyclization of cyclosporin analogs. Methods are described for the on-resin cyclization of sterically hindered compounds synthesized through solid phase synthesis techniques. The methods utilize solvent, temperature, and washing conditions that allow the efficient on-resin cyclization of compounds like analogs of cyclosporin A.
专利号:US-2009143426-A1 优先权日:2007-12-04 标 题:Synthesis of 1,3,6-trisubstituted-2-carboxyquinol-4-ones as selective ET A antagonists and their use as medicaments 发明人:STEPHANI RALPH ANTHONY; PATEL HARDIK JITENDRA; REZNIK SANDRA EVE; CANTOR JEROME OWEN 权利人:STEPHANI RALPH ANTHONY; PATEL HARDIK JITENDRA; REZNIK SANDRA EVE; CANTOR JEROME OWEN 摘要:The invention discloses the composition and preparation of various 1,3,6-trisubstituted-2-carboxy-quinol-4-ones of the formula 1 where R is H, alkyl, haloalkyl or hydroxyalkyl, R′ is alkyl, nitro, halogen or NR 2 ′″ where R′″ is alkyl or cycloalkyl, and R″ is H or alkyl. The composition of the invented compounds as methods of antagonizing the action of endothelin-1 to treat cardiovascular, pulmonary diseases and obstetric disorders and preterm labor and preeclampsia in mammals is disclosed.
专利号:WO-0031134-A9 优先权日:1998-11-20 标题:Regulation of hair follicle morphogenesis based on beta-catenin 发明人:GAT URI; DASGUPTA RAMANUJ; DEGENSTEIN LINDA; FUCHS ELAINE 权利人:ARCH DEV CORP; GAT URI; DASGUPTA RAMANUJ; DEGENSTEIN LINDA; FUCHS ELAINE 摘要:The present invention provides a method for inducing hair growth by providing beta-catenin activity to a skin cell. This may be achieved by providing a beta-catenin polypeptide, providing a beta-catenin agonist, providing a polynucleotide encoding a beta-catenin polypeptide, enhancing the de novo synthesis of beta-catenin, increasing the stability or decreasing the degradation of beta-catenin polypeptides.