专利号:US-10336703-B2 优先权日:2015-05-12 标题 :Process for the synthesis of ivacaftor and related compounds 发明人:REDDY DUMBALA SRINIVASA; NATARAJAN VASUDEVAN; JACHAK GORAKHNATH RAJARAM 权利人:COUNCIL SCIENT IND RES 摘要:The present patent discloses a novel one pot two-step process for the synthesis of ivacaftor and related compounds of [Formula (I)], wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and Ar 1 are as described above; its tautomers or pharmaceutically acceptable salts thereof starting from indole acetic acid amides.
专利号:US-12024731-B2 优先权日:2017-05-03 标 题 :Methods and enzyme catalysts for the synthesis of non-canonical amino acids 发明人:BOVILLE CHRISTINA E; BRINKMANN-CHEN SABINE; BULLER ANDREW R; ROMNEY DAVID K; PRIER CHRISTOPHER K; KOCH PHILIPP; SCHEELE REMKES A 权利人:CALIFORNIA INST OF TECHN 摘要:The present disclosure provides methods for preparing β-substituted tryptophan compounds. The methods include: combining i) an unsubstituted indole or a substituted indole, ii) a β-substituted serine, and iii) a tryptophan synthase β-subunit (i.e., a TrpB); and maintaining the resulting mixture under conditions sufficient to form the β-substituted tryptophan. The TrpB contains at least one amino acid mutation which promotes formation of an amino-acrylate intermediate. New TrpB variants and new β-substituted tryptophan analogs are also described.
专利号:US-6057465-A 优先权日:1997-05-22 标 题:Arene-transition metal linkers for solid phase synthesis 发明人:GALLOP MARK A 权利人:GLAXO WELLCOME INC 摘要:Compositions and methods for the solid phase synthesis of organic compounds are provided. The compositions are solid supports having an attached traceless linker precursor and are represented by the formula: ##STR1## In this formula, S 0 is a solid support; B is a connecting group; M is a transition metal, for example ruthenium, chromium, iron, molybdenum and manganese; each L is independently a transition metal ligand; the letter n represents an integer of from 1 to 4, such that M has a sufficient number of ligands to fill the available valences; and X - represents an anion which is typically a non-nucleophilic anion.
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-9573939-B2 优先权日:2011-09-08 标题:Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases 发明人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; DANG QUN 权利人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; DANG QUN; MERCK SHARP & DOHME; MSD ITALIA SRL 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:WO-2020240272-A1 优先权日:2019-05-31 标题:Preparation of novel 1 h-pyrazolo[4,3-d]pyrimidines, their compositions, synthesis and methods of using them for treating tuberculosis 发明人:PAL MANOJIT; MISRA PARIMAL; SRIKANTAM APARNA; AHMAD FARHAN JALEES; EHTESHAM NASREEN ZAFAR; HASNAIN SEYED EHTESHAM 权利人:DR REDDYS INST OF LIFE SCIENCES; JAMIA HAMDARD UNIV 摘要:The present invention provides novel heterocyclic compounds of Formula (I): their derivatives, analogs, tautomeric forms, stereoisomers, bioisosters, diastereomers, polymorphs, enantiomers, prodrugs and their pharmaceutically acceptable salts for the treatment of tuberculosis. Also disclosed is the process for preparing compounds of Formula (I), and intermediates useful for preparing compounds of Formula (I).
[参考文献]: Amy S Newman, Et Al. 5-Chloroindole: A Potent Allosteric Modulator Of The 5-Ht Receptor. Br J Pharmacol. 2013 Jul;169(6):1228-38. [参考文献]: Douglas R Davies, Et Al. Discovery Of Leukotriene A4 Hydrolase Inhibitors Using Metabolomics Biased Fragment Crystallography. J Med Chem. 2009 Aug 13;52(15):4694-715.
合成参考文献
摘要:Wu, X.-F., Science of Synthesis Knowledge Updates, (2014) 1, 284. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 270. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 340. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 315. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 345.