CAS: 916072-89-4; Naldemedine

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      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:JP-5714490-B2
      优先权日:2008-09-06
      标题:Methods for preparing oligonucleotides by RNA synthesis, phosphoramidites for synthetic RNA in the reverse direction, and bond formation in the 5 'to 3' direction for synthesis of RNA oligomers

      专利号:WO-2025038406-A1
      优先权日:2023-08-11
      标 题 :Design, synthesis, and biological evaluation of nitrogen-walk derivatives of nan as mu opioid receptor selective modulators
      发明人:ZHANG YAN
      权利人:UNIV VIRGINIA COMMONWEALTH
      摘要:A series of non-peptide mu opioid receptor (MOR) selective modulators is provided. The compounds have the general formula (I) where R is (II) and where one of a, b, c, d, e or f is the point of attachment of indole ring R to the epoxymorphinan skeleton; at least one of the atoms at positions a, b, c, d, e and f is N; the remaining atoms at positions at a, b, c, d, e and f are CH; and * is a chiral carbon. The compounds are generally MOR antagonists and are used to treat disorders related to opioid receptor functions such as opioid addiction and opioid overdose, for the treatment of neurological diseases and for the treatment of pain, without causing constipation.

      专利号:US-2007179100-A1
      优先权日:2003-04-09
      标 题:Protected monomers
      发明人:MANOHARAN MUTHIAH
      权利人:MANOHARAN MUTHIAH
      摘要:This invention relates to protected monomers for the synthesis of iRNA agents.

      专利号:KR-102337328-B1
      优先权日:2015-12-21
      标 题 :Systems and Methods for Synthesis of GAP Peptides in Solution Phase

      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

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      主要参考文献


      1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548373/ doi: 10.1136/esmoopen-2019-000527. eCollection 2019.
      4: Blair HA. Naldemedine: A Review in Opioid-Induced Constipation. Drugs. 2019 Jul;79(11):1241-1247. doi: 10.1007/s40265-019-01160-7. Review. doi: 10.1097/j.pain.0000000000001629.
      7: Fukumura K, Yamada T, Yokota T, Kawasaki A. The Influence of Renal or Hepatic Impairment on the Pharmacokinetics, Safety, and Tolerability of Naldemedine. Clin Pharmacol Drug Dev. 2019 Apr 12. doi: 10.1002/cpdd.690. [Epub ahead of print] doi: 10.15403/jgld.2014.1121.281.any. doi: 10.1111/nmo.13563. Epub 2019 Feb 28.

      合成参考文献


      参考文献:10.1007/s11912-015-0481-x
      摘要:Davis M, Gamier P. New Options in Constipation Management. Curr Oncol Rep. 2015 Dec;17(12):55. doi: 10.1007/s11912-015-0481-x.
      参考文献:10.1136/gutjnl-2018-316001
      摘要:Luthra P, Burr NE, Brenner DM, Ford AC. Efficacy of pharmacological therapies for the treatment of opioid-induced constipation: systematic review and network meta-analysis. Gut. 2019 Mar;68(3):434–44. doi: 10.1136/gutjnl-2018-316001.
      参考文献:10.1007/s11605-020-04671-x
      摘要:Chamie K, Golla V, Lenis AT, Lec PM, Rahman S, Viscusi ER. Peripherally Acting μ-Opioid Receptor Antagonists in the Management of Postoperative Ileus: a Clinical Review. Journal of Gastrointestinal Surgery. 2020 Aug 10;25(1):293–302. doi: 10.1007/s11605-020-04671-x.
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