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1000339-51-4 115661-37-5 872366-63-7欧盟法规
ECHA物质C&L通报上下游产品
2bromo6fluoronitrobenzenemethyl 5-(3-cyano-2-nitrophenylamino)thiophene-2-carboxylate 📜Copper(L) Cyanide,2-溴-6-氟硝基苯 以 N,N-二甲基甲酰胺 用作溶剂,化学反应 1.0H,以81%的收率获得3-氟-2-硝基苯腈
参考文献:Optimization Of Potent Inhibitors Of P. Falciparum Dihydroorotate Dehydrogenase For The Treatment Of Malaria
标题:Optimization Of Potent Inhibitors Of P. Falciparum Dihydroorotate Dehydrogenase For The Treatment Of Malaria
摘要:Inhibition Of Dihydroorotate Dehydrogenase (Dhodh) For P. Falciparum Potentially Represents A New Treatment Option For Malaria,Since Dhodh Catalyzes The Rate-Limiting Step In The Pyrimidine Biosynthetic Pathway And P. Falciparum Is Unable To Salvage Pyrimidines And Must Rely On De Novo Biosynthesis For Survival. We Report Herein The Synthesis And Structure-Activity Relationship Of A Series Of 5-(2-Methylbenzimidazol-1-yl)-N-Alkylthiophene-2-Carboxamides That Are Potent Inhibitors Against Pfdhodh But Do Not Inhibit The Human Enzyme. On The Basis Of Efficacy Observed In Three Mouse Models Of Malaria,Acceptable Safety Pharmacology Risk Assessment And Safety Toxicology Profile In Rodents,Lack Of Potential Drug-Drug Interactions,Acceptable Adme/pharmacokinetic Profile,And Projected Human Dose,5-(4-Cyano-2-Methyl-1H-Benzo[d]Imidazol-1-yl)-N-Cyclopropylthiophene-2-Carboxamide 2Q Was Identified As A Potential Drug Development Candidate.
Doi:10.1021/ml200143C
专利信息
专利号:US-11548898-B2
优先权日:2017-07-06
标题 :Synthesis of halichondrins
发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI
权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD
摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:US-2023128195-A1
优先权日:2017-07-06
标 题:Synthesis of halichondrins
专利号:KR-20220124279-A
优先权日:2017-07-06
标题 :Synthesis of Halicondrin
专利号:CN-118515685-A
优先权日:2017-07-06
标题 :Synthesis of halichondrin
专利号:CA-3069160-C
优先权日:2017-07-06
标题:Synthesis of halichondrins
专利号:CN-111433211-B
优先权日:2017-07-06
标题 :Synthesis of Halichondrin