专利号:US-9969686-B2 优先权日:2014-08-05 标 题 :Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them 发明人:TANG WEIPING; LI XIAOXUN; SHU DONGXU; WINSTON-MCPHERSON GABRIELLE N 权利人:WISCONSIN ALUMNI RES FOUND 摘要:Described is a method to make diindolylmethanes and indolyl/pyrrolylmethanes, The method includes the steps of contacting an ether comprising an arylpropargyl moiety and an amine-protected, substituted or unsubstituted aniline moiety with a substituted or unsubstituted indol or a substituted or unsubstituted pyrrole, in the presence of a metal-containing catalyst, for a time and at a temperature to cause an annulation/arylation cascade reaction that yields a diindolylmethane or a indolyl/pyrrolylmethane. The resulting compounds are effective to modulate activity of arylhydrocarbon receptors, to inhibit activity of PCSK9, and to stimulate secretion of glucagon-like peptide 1 in mammals.
专利号:US-10752927-B2 优先权日:2018-03-01 标 题 :Method for the synthesis of tryptophan analogs in aqueous solvents at reduced temperatures 发明人:BOVILLE CHRISTINA E; ROMNEY DAVID K; ALMHJELL PATRICK J; SIEBEN MICHAELA M 权利人:CALIFORNIA INST OF TECHN 摘要:The present disclosure provides methods for preparing tryptophans and tryptophan derivatives. The methods include: combining i) an indole substrate or azulene substrate, ii) a serine substrate, and iii) an engineered tryptophan synthase β-subunit (TrpB); and maintaining the resulting mixture under conditions sufficient to form the product compound. The engineered TrpB comprises a PLP binding loop mutation, a helix 1 mutation, a strand 7-8 mutation, or a combination thereof. New TrpB variants are also described.
专利号:WO-0053313-A2 优先权日:1999-03-09 标 题:Lanthanide catalysts for synthesis of compounds and combinatorial libraries
专利号:US-2019271016-A1 优先权日:2018-03-01 标题:Method for the synthesis of tryptophan analogs in aqueous solvents at reduced temperatures
专利号:US-2016039754-A1 优先权日:2014-08-05 标题 :Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them
专利号:US-2018222861-A1 优先权日:2014-08-05 标题:Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them
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