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5308-28-1 21867-64-1 33174-08-2欧盟法规
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pivalaldehydee]pyrido[3,2-b][1,4]diazepin-6-one11-{[4-(2,2-dimethyl-propyl)-piperazin-1-yl]-acetyl}-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one 26H32ClN5O2C26H32ClN5O2 📜Tert-Butyl 4-Neopentylpiperazine-1-Carboxylate置于三氟乙酸体系中,用 二氯甲烷 作为反应溶剂,化学反应 18.0H,以60%的收率获得产物1-新戊基哌嗪
参考文献:Novel Vanilloid Receptor-1 Antagonists: 3. The Identification Of A Second-Generation Clinical Candidate With Improved Physicochemical And Pharmacokinetic Properties
标题:Novel Vanilloid Receptor-1 Antagonists: 3. The Identification Of A Second-Generation Clinical Candidate With Improved Physicochemical And Pharmacokinetic Properties
摘要:Based On The Previously Reported Clinical Candidate,Amg 517 (Compound 1),A Series Of Related Piperazinylpyrimidine Analogues Were Synthesized And Evaluated As Antagonists Of The Vanilloid 1 Receptor (Vr1 Or Trpv1). Optimization Of In Vitro Potency And Physicochemical And Pharmacokinetic Properties Led To The Discovery Of (R)-N-(4-(6-(4-(1-(4-Fluorophenyl)Ethyl)Piperazin-1-yl)Pyrimidin-4-Yloxy)Benzo[d]Thiazol-2-yl)Acetamide (16P),A Potent Trpv1 Antagonist [rtrpv1(Cap) Ic50 = 3.7 Nm] With Excellent Aqueous Solubility (>= 200 Mu G/ml In 0.01 N Hcl) And A Reduced Half-Life (Rat T(1/2) = 3.8 H,Dog T(1/2) = 2.7 H,Monkey T(1/2) = 3.2 H) As Compared To Amg 517. In Addition,Compound 16P Was Shown To Be Efficacious At Blocking A Trpv1-Mediated Physiological Response In Vivo (Ed50 = 1.9 Mg/kg,P.O. In The Capsaicin-Induced Flinch Model In Rats) And Was Also Effective At Reducing Thermal Hyperalgesia Induced By Complete Freund'S Adjuvant In Rats (Med = 1 Mg/kg,P.O). Based On Its Improved Overall Profile,Compound 16P (Amg 628) Was Selected As A Second-Generation Candidate For Further Evaluation In Human Clinical Trials As A Potential New Treatment For Chronic Pain.
DOI:10.1021/jm070191H
专利信息
专利号:US-8551435-B2
优先权日:2009-06-30
标 题 :Process for reducing contaminants in an industrial fluid stream
发明人:BLAIR ALAN M; GARSIDE KEITH N; ANDREWS WILLIAM J; SAWANT KAILAS B
权利人:BLAIR ALAN M; GARSIDE KEITH N; ANDREWS WILLIAM J; SAWANT KAILAS B; NALCO CO
摘要:This invention provides novel processes utilizing compositions comprising substituted polyamines as acid gas scrubbing solutions and methods of using the compositions in an industrial system. The invention relates to the use of such polyamine compounds in industrial processes to remove acidic contaminants from natural and industrial fluid streams, such as natural gas, combustion gas, natural gas, synthesis gas, biogas, and other industrial fluid streams. The compositions and methods of the invention are useful for removal, absorption, or sequestration of acidic contaminants and sulfide contaminants including CO 2 , H 2 S, RSH, CS 2 , COS, and SO 2 .