CAS: 866460-33-5; 2-(2-(1-Naphthoyl)-8-Fluoro-3,4-Dihydro-1H-Pyrido[4,3-B]Indol-5(2H)-yl)Acetic Acid

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Tert-Butyl 5-(2-Ethoxy-2-Oxoethyl)-8-Fluoro-3,4-Dihydro-1H-Pyrido[4,3-B]Indole-2(5H)-Carboxylate 1060979-22-7
Tert-Butyl 8-Fluoro-3,4-Dihydro-1H-Pyrido[4,3-B]Indole-2(5H)-Carboxylate 870471-42-4
8-氟-2,3,4,5-四氢-1H-吡啶并[4,3-B]吲哚 8-Fluoro-2,3,4,5-Tetrahydro-1H-Pyrido[4,3-B]Indole 39876-39-6

📜8-氟-2,3,4,5-四氢-1H-吡啶并[4,3-B]吲哚置于盐酸,Caesium Carbonate,N,N-二异丙基乙胺,Sodium Hydroxide体系中,用 四氢呋喃,1,4-二氧六环,二氯甲烷,丙酮 作为反应溶剂,化学反应 5.5H,反应生成 塞替匹仑
参考文献:Identification Of 2-(2-(1-Naphthoyl)-8-Fluoro-3,4-Dihydro-1H-Pyrido[4,3-B]Indol-5(2H)-yl)Acetic Acid (Setipiprant/act-129968),A Potent,Selective,And Orally Bioavailable Chemoattractant Receptor-Homologous Molecule Expressed On Th2 Cells (Crth2) Antagonist
标题:Identification Of 2-(2-(1-Naphthoyl)-8-Fluoro-3,4-Dihydro-1H-Pyrido[4,3-B]Indol-5(2H)-yl)Acetic Acid (Setipiprant/act-129968),A Potent,Selective,And Orally Bioavailable Chemoattractant Receptor-Homologous Molecule Expressed On Th2 Cells (Crth2) Antagonist
摘要:Herein We Describe The Discovery Of The Novel Crth2 Antagonist 2-(2-(1-Naphthoyl)-8-Fluoro-3,4-Dihydro-1H-Pyrido[4,3-B]Indol-5(2H)-yl)Acetic Acid 28 (Setipiprant/act-129968),A Clinical Development Candidate For The Treatment Of Asthma And Seasonal Allergic Rhinitis. A Lead Optimization Program Was Started Based On The Discovery Of The Recently Disclosed Crth2 Antagonist 2-(2-Benzoyl-3,4-Dihydro-1H-Pyrido[4,3-B]Indol-5(2H)-yl)Acetic Acid 5. An Already Favorable And Druglike Profile Could Be Assessed For Lead Compound 5. Therefore,The Lead Optimization Program Mainly Focused On The Improvement In Potency And Oral Bioavailability. Data Of Newly Synthesized Analogs Were Collected From In Vitro Pharmacological,Physicochemical,In Vitro Adme,And In Vivo Pharmacokinetic Studies In The Rat And The Dog. The Data Were Then Analyzed Using A Traffic Light Selection Tool As A Visualization Device In Order To Evaluate And Prioritize Candidates Displaying A Balanced Overall Profile. This Data-Driven Process And The Excellent Results Of The Pk Study In The Rat (F = 44%) And The Dog (F = 55%) Facilitated The Identification Of 28 As A Potent (Ic50 = 6 Nm),Selective,And Orally Available Crth2 Antagonist.
DOI:10.1021/jm400122F