CAS: 51173-05-8; 5-Fluoro-2-Hydroxypyridine

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5-氨基-2-甲氧基吡啶置于盐酸,Tetrafluoroboric Acid,Sodium Nitrite体系中,用 乙醇,水,甲苯 作为反应溶剂,化学反应 9.0H,反应生成 2-羟基-5-氟吡啶
参考文献:Inhibitors Of Human Immunodeficiency Virus Type 1 (Hiv-1) Attachment. 12. Structure-activity Relationships Associated With 4-Fluoro-6-Azaindole Derivatives Leading To The Identification Of 1-(4-Benzoylpiperazin-1-yl)-2-(4-Fluoro-7-[1,2,3]Triazol-1-Yl-1H-Pyrrolo[2,3-C]Pyridin-3-yl)Ethane-1,2-Dione (Bms-585248)
标题:Inhibitors Of Human Immunodeficiency Virus Type 1 (Hiv-1) Attachment. 12. Structure-activity Relationships Associated With 4-Fluoro-6-Azaindole Derivatives Leading To The Identification Of 1-(4-Benzoylpiperazin-1-yl)-2-(4-Fluoro-7-[1,2,3]Triazol-1-Yl-1H-Pyrrolo[2,3-C]Pyridin-3-yl)Ethane-1,2-Dione (Bms-585248)
摘要:A Series Of Highly Potent Hiv-1 Attachment Inhibitors With 4-Fluoro-6-Azaindole Core Heterocycles That Target The Viral Envelope Protein Gp120 Has Been Prepared. Substitution In The 7-Position Of The Azaindole Core With Amides (12A,B),C-Linked Heterocycles (12C-I),And N-Linked Heterocycles (12M-U) Provided Compounds With Subnanomolar Potency In A Pseudotype Infectivity Assay And Good Pharmacokinetic Profiles In Vivo. A Predictive Model Was Developed From The Initial Sar In Which The Potency Of The Analogues Correlated With The Ability Of The Substituent In The 7-Position Of The Azaindole To Adopt A Coplanar Conformation By Either Forming Internal Hydrogen Bonds Or Avoiding Repulsive Substitution Patterns. 1-(4-Benzoylpiperazin-1-yl)-2-(4-Fluoro-7-[1,2,3]Triazol-1-Yl-1H-Pyrrolo[2,3-C]Pyridin-3-yl)Ethane-1,2-Dione (Bms-585248,12M) Exhibited Much Improved In Vitro Potency And Pharmacokinetic Properties Than The Previous Clinical Candidate Bms-488043 (1). The Predicted Low Clearance In Humans,Modest Protein Binding,And Good Potency In The Presence Of 40% Human Serum For 12M Led To Its Selection For Human Clinical Studies.
DOI:10.1021/jm3016377

专利信息

专利号:US-7754188-B2
优先权日:2003-06-30
标 题:Radiolabeled cannabinoid-1 receptor modulators
发明人：BURNS H DONALD; CHEN ALEX M; GIBSON RAYMOND E; GOULET MARK T; HAGMANN WILLIAM K; HAMILL TERENCE G; JEWELL JAMES P; LIN LINUS S; LIU PING; PERESYPKIN ANDREY V
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to particular radiolabeled Cannabinoid-1 (CB1) receptor modulators, and methods of using these modulators for labeling and diagnostic imaging of Cannabinoid-1 receptors in mammals, particularly humans. In addition, intermediates useful for the synthesis of the radiolabeled Cannabinoid-1 receptor modulators are also disclosed, as well as the processes for synthesizing the radiolabeled Cannabinoid-1 receptor modulators. Still further, formulations of the radiolabeled Cannabinoid-1 receptor compounds are described.

专利号:US-11286268-B1
优先权日:2019-07-02
标题:EIF4E-inhibiting compounds and methods
发明人：SPERRY SAMUEL; XIANG ALAN X; ERNST JUSTIN T; REICH SIEGFRIED H; SPRENGELER PAUL A; SHAGHAFI MIKE; MICHELS THEO; NILEWSKI CHRISTIAN; TRAN CHINH VIET; PACKARD Garrick Kenneth; GRUBBS ALAN; URKALAN KAVERI; MUKAIYAMA TAKASUKE
权利人:EFFECTOR THERAPEUTICS INC
摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. n n n n n n n n n n For Formula I compounds X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , Q, L 1 , L 2 , Y, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and rings A, B and C are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4e and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.