CAS: 203866-15-3; (S)-1-(Tert-Butoxycarbonyl)-4,4-Difluoropyrrolidine-2-Carboxylic Acid

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N-Boc-反式-4-羟基-L-脯氨酸甲酯置于2,2,6,6-四甲基哌啶氧化物,二乙胺基三氟化硫,三氯异氰尿酸,Potassium Hydroxide体系中,用 甲醇,乙醇,二氯甲烷 用作溶剂,化学反应 34.0H,反应生成N-Boc-4,4-二氟-L-脯氨酸
参考文献:成纤维细胞活化蛋白(fap)的(4-喹啉基)糖基-2-氰基吡咯烷酮抑制剂的扩展结构-活性关系和药代动力学研究
标题:成纤维细胞活化蛋白(fap)的(4-喹啉基)糖基-2-氰基吡咯烷酮抑制剂的扩展结构-活性关系和药代动力学研究
摘要:成纤维细胞活化蛋白(fap)是一种与二肽基肽酶iv(dppiv)相关的丝氨酸蛋白酶.它已令人信服地与涉及细胞外基质重塑的多种疾病状态联系在一起.Fap抑制已被研究作为这些疾病中的几种的治疗选择,迄今为止,大多数注意力都集中在肿瘤学应用上.我们之前发现了n-4-喹啉基-Gly-(2 S)-Cyanopro支架可能是高效和选择性fap抑制剂的一种可能.在本研究中,我们将详细探讨围绕该核心支架的结构与活性之间的关系.我们报告了广泛优化的化合物,这些化合物对相关的二肽基肽酶(dpps)dppiv,Dpp9,Dppii和脯氨酰寡肽酶(prep)表现出低纳摩尔抑制力和高选择性.发现所选化合物的log D值,血浆稳定性和微粒体稳定性非常令人满意.选定抑制剂在小鼠体内的药代动力学评估表明,其口服生物利用度高,血浆半衰期高,并且具有体内选择性和完全抑制fap的潜力.
Doi:10.1021/jm500031W

专利信息

专利号:US-7179918-B2
优先权日:2001-06-11
标 题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
发明人：CANAN KOCH STACIE S; ALEXANDER THERESE N; BURKE BENJAMIN J; JEWELL TANYA M; KUCERA DAVID J; LINTON MARIA ANGELICA; MITCHELL JR LENNERT J; REICH SIEGFRIED H; SKALITZKY DONALD J; TATLOCK JOHN H; VARNEY MICHAEL D; VIRGIL SCOTT C; WEBBER STEPHEN E; WORLAND STEPHEN T; BARVIAN MARK; BOLTON GARY; BOYER JR FREDERICK EARL; MACHAK JEFFREY J; HOLLER TOD; MURPHY SEAN T; MELNICK MICHAEL; JOSYULA VARA PRASAD
权利人:AGOURON PHARMA
摘要:Compounds of the formula: n nwhere the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.

专利号:US-7094909-B2
优先权日:2001-06-11
标 题 :HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
发明人：KUCERA DAVID JOHN; SCOTT ROBERT WILLIAM
权利人:AGOURON PHARMA
摘要:The present invention concerns processes for preparing compounds of formula (I-H), or a prodrug, pharmaceutically active metabolite, or pharmaceutically active salt or solvate thereof, n nwhich are useful as inhibitors of the HIV protease enzyme.