CAS: 147269-67-8; Benzyl (2-Oxo-1,2-Dihydropyridin-3-yl)Carbamate

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3-amino-2-pyridone benzyl chloroformate 3-nitropyridone 1,4-dioxaneamino>-5-iodopyrid-2-one3-(benzyloxy)carbonylamino-5-iodopyrid-2-one Methyl [3-benzyloxycarbonylamino-1,2-dihydro-2-oxo-1-pyridyl]-acetate methyl (2S)-2-(3-{[(benzyloxy)carbonyl]amino}-2-oxo-1,2-dihydropyridin-1-yl)propanoate (3-Amino-2-oxo-2H-pyridin-1-yl)-acetic acid methyl ester

📜2-羟基-3-硝基吡啶置于palladium On Activated Charcoal 氢气,Sodium Carbonate体系中,用 四氢呋喃,乙醇 用作溶剂,25.0 °C,101.33 Kpa 条件下,反应 8.0H,反应生成2-氧代-1,2-二氢吡啶-3-基氨基甲酸苄酯
参考文献:人白细胞弹性蛋白酶的非肽抑制剂.1.含吡啶酮的抑制剂的设计与合成.
标题:人白细胞弹性蛋白酶的非肽抑制剂.1.含吡啶酮的抑制剂的设计与合成.
摘要:人白细胞弹性蛋白酶(hle)是嗜中性粒细胞产生的一种丝氨酸蛋白酶,与肺气肿和囊性纤维化等疾病有关.Hle抑制剂在这些疾病中可能具有治疗价值.结合三肽三氟甲基酮(tfmk)抑制剂2的hle活性位点模型是由hle和猪胰弹性蛋白酶的x射线结构创建的.对模型的分析表明,三肽具有较好的结合构象,并且可能与酶发生重要的相互作用.该信息用于辅助设计一系列新颖的含吡啶酮的非肽类hle抑制剂,例如2-[3-[[((苄氧基)羰基]氨基]-2-氧-1,2-二氢-1-吡啶基]-N-(3,3,3-三氟-1-异丙基-2-氧丙基)乙酰氨基化物(5B)(ki = 280 +/-78 Nm).活性位点模型的检查表明,在吡啶酮环的5位上的苄基取代基可能通过与酶s2口袋形成亲脂性相互作用而提高效能.一系列5-苄基吡啶酮tfmk的合成和生物学评估为这一主张提供了证据.对模型的进一步分析表明,在吡啶酮环的3-氨基上被氢键受
Doi:10.1021/jm00045A014

专利信息

专利号:US-6514997-B2
优先权日:1999-12-03
标题:Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
发明人：DRAGOVICH PETER S; PRINS THOMAS J; ZHOU RU; JOHNNSON JR THEODORE O
权利人:AGOURON PHARMA
摘要:Compounds of the formula: n where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the picornaviral 3C protease. Also disclosed are compounds of the formula: n where the formula variables are as defined herein that advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as rhinovirus 3C proteases. Intermediates and synthetic methods for preparing such compounds are also described.

专利号:US-5521179-A
优先权日:1991-04-18
标题 :Heterocyclic amides
发明人：BERNSTEIN PETER R; SHAW ANDREW; THOMAS ROYSTON M; WARNER PETER; WOLANIN DONALD J
权利人:ZENECA LTD
摘要:The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.