专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:US-4201869-A 优先权日:1970-12-21 标 题:Intermediates for steroid total synthesis process utilizing asymmetric induction 发明人:COHEN NOAL; SAUCY GABRIEL 权利人:HOFFMANN LA ROCHE 摘要:A multi-step, stereospecific total synthesis of steroids is disclosed. The starting materials for this process are the relatively inexpensive and readily available m-alkoxy acetophenones. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly A-ring aromatic steroids. This process features an early optical resolution and a unique asymmetric induction which insures the correct stereochemistry of the final steroidal product.
专利号:US-4092483-A 优先权日:1973-10-16 标题 :Intermediates for steroid total synthesis process utilizing asymmetric induction 发明人:COHEN NOAL; SAUCY GABRIEL 权利人:HOFFMANN LA ROCHE 摘要:A multi-step, stereospecific total synthesis of steroids is disclosed. The starting materials for this process are the relatively inexpensive and readily available m-alkoxy acetophenones. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly A-ring aromatic steroids. This process features an early optical resolution and a unique asymmetric induction which insures the correct stereochemistry of the final steroidal product.
专利号:US-4102925-A 优先权日:1970-12-21 标题:Steroid total synthesis process utilizing asymmetric induction 发明人:COHEN NOAL; SAUCY GABRIEL 权利人:HOFFMANN LA ROCHE 摘要:A multi-step, stereospecific total synthesis of steroids is disclosed. The starting materials for this process are the relatively inexpensive and readily available m-alkoxy acetophenones. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly A-ring aromatic steroids. This process features an early optical resolution and a unique asymmetric induction which insures the correct stereochemistry of the final steroidal product.
专利号:US-4011211-A 优先权日:1973-10-16 标题:Steroid total synthesis process utilizing asymmetric induction 发明人:COHEN NOAL; SAUCY GABRIEL 权利人:HOFFMANN LA ROCHE 摘要:A multi-step, stereospecific total synthesis of steroids is disclosed. The starting materials for this process are the relatively inexpensive and readily available m-alkoxy aceto-phenones. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly A-ring aromatic steroids. This process features an early optical resolution and a unique asymmetric induction which insures the correct stereochemistry of the final steroidal product.
专利号:US-2008300418-A1 优先权日:2004-11-08 标 题:Synthesis of Cardiolipin Analogues and Uses Thereof 发明人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 权利人:AHMAD MOGHIS U; UKKALAM MURALI K; ALI SHOUKATH M; AHMAD IMRAN 摘要:The invention provides novel synthetic methodologies for preparing cardiolipin, migrated caridiolipin (1,2-positional isomer of cardiolipin) and their analogues having varying fatty acids and/or alkyl chains with varying length and degrees of saturation/unsaturation. The method comprises (a) reacting an optically pure 1,2-O-dialkyl-sn-glycerol or 1,2-O-dialkyl-sn-glycerol with one or more phosphoramidite reagent(s), wherein a phosphite triester is produced; (b) coupling the product of (a) with glycerol, wherein a protected cardiolipin is produced; and (c) deprotecting the protected cardiolipin, such that cardiolipin is prepared. The cardiolipins and analogues thereof, prepared by the present methods, can be incorporated into liposomes, which can also include active agents such as hydrophobic or hydrophilic drugs, antisense nucleotides or diagnostic agents. Such liposomes can be used to treat diseases or can be used in diagnostic and/or analytical assays.
1: Hu JH, Wang L, Li WS, Dai DP, Cai JP, Hu GX. Effect of CYP2C9 Genetic Polymorphism in a Chinese Population on the Metabolism of Mestranol in vitro. Pharmacology. 2015;95(5-6):218-23. doi: 10.1159/000381189. Epub 2015 Apr 25. Polish. Japanese. 10: Coezy E, Auzan C, Lonigro A, Philippe M, Menard J, Corvol P. Effect of mestranol on cell proliferation and angiotensinogen production in HepG2 cells: relation with the cell cycle and action of tamoxifen. Endocrinology. 1987 Jan;120(1):133-41. German. German.
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