CAS: 135632-53-0; Tert-Butyl (Piperidin-4-Ylmethyl)Carbamate

相似化合物

144222-22-0 7144-05-0 157023-34-2

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((1-苄基哌啶-4-基)甲基)氨基甲酸叔丁酯 Tert-Butyl ((1-Benzylpiperidin-4-yl)Methyl)Carbamate 173340-23-3

哌啶-4-甲酰胺置于lithium Aluminium Tetrahydride,Palladium Hydroxide,20 Wt% On Carbon,三乙胺,环己烯体系中,用 四氢呋喃,甲醇,二氯甲烷 用作溶剂,化学反应 51.0H,反应生成4-Boc-氨甲基哌啶
参考文献:基于晶体结构的抑制剂优化的魔力:具有皮摩尔亲和力和体内活性的丁酰胆碱酯酶抑制剂的开发
标题:基于晶体结构的抑制剂优化的魔力:具有皮摩尔亲和力和体内活性的丁酰胆碱酯酶抑制剂的开发
摘要:大脑中丁酰胆碱酯酶(bche)的酶活性随阿尔茨海默氏病的发展而增加,因此将bche归类为晚期阿尔茨海默氏病的有希望的药物靶标.我们使用基于结构的药物发现方法来开发有效的,选择性的和可逆的人类bche抑制剂.最有效的化合物3由于与阳离子b相互作用强,因此与bche具有皮摩尔的抑制常数,这是由其与人bche的复合物的晶体结构解析得出的.另外,化合物3离体抑制bche并且是无细胞毒性的.体外药代动力学实验表明,化合物3具有高蛋白结合性,高渗透性和代谢稳定性.最后,化合物3跨越血脑屏障,并且在东pol碱痴呆模型中改善了小鼠的记忆,认知功能和学习能力.因此,化合物3是用于开发减轻晚期阿尔茨海默氏病患者的胆碱能功能减退症状的药物的有希望的先进先导化合物.
Doi:10.1021/acs.Jmedchem.7B01086

专利信息

专利号:US-12150934-B2
优先权日:2016-11-30
标 题 :Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases
发明人：SIDDIQUI ARSHAD M; CIBLAT STEPHANE; CONSTANTINEAU-FORGET LEA; GRAND-MAITRE CHANTAL; GUO XIANGYU; SRIVASTAVA SANJAY; SHIPPS GERALD W; COOPER ALAN B; OZA VIBHA; KOSTURA MATTHEW W; LUTHER MICHAEL; LEVINE JEDD
权利人:BANTAM PHARMACEUTICAL LLC
摘要:Disclosed are methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formula (I), in which X1, X2, Z1, Z2, the ring system denoted by “aâ€?, R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.

专利号:US-5939392-A
优先权日:1993-06-03
标 题 :Method of thrombin inhibition
发明人：ANTONSSON KARL THOMAS; BYLUND RUTH ELVY; GUSTAFSSON NILS DAVID; NILSSON NILS OLOV INGEMAR
权利人:ASTRA AB
摘要:The invention relates to new competitive tripeptide inhibitors of trypsin-like serine proteases, their synthesis, pharmaceutical compositions containing the compounds as active ingredients, and the use of the compounds as thrombin inhibitors, anticoagulants and antiinflammatory inhibitors for prophylaxis and treatment of related diseases.

专利号:WO-2025068371-A1
优先权日:2023-09-28
标 题:Inhibitors of the proprotein convertase furin, methods of production thereof and use
发明人：STEINMETZER TORSTEN; LANGE ROMAN WERNER; BOLLER CHARLOTTE; FRIEBERTSHÄUSER EVA; BLOCH KONSTANTIN
权利人:PHILIPPS UNIV MARBURG
摘要:The invention relates to novel inhibitors of the serine protease furin and to related furin-like proprotein convertases according to claim 1, and to methods of synthesis thereof and to use for production of medicaments for treatment of furin-dependent viral and bacterial infection diseases, and other disorders involving furin, such as cystic fibrosis, cancer, osteoarthritis, hypertension, and neurodegenerative disorders.

专利号:US-5723444-A
优先权日:1993-06-03
标 题:Starting materials in the synthesis of thrombin and kinogenase inhibitors

专利号:LT-3768-B
优先权日:1993-06-03
标题 :Novel peptides derivatives, process for their preparation, pharmaceutical compositions and use starting materials in synthesis of a serine protease inhibitors

专利号:US-5780631-A
优先权日:1993-06-03
标题 :Starting materials in the synthesis of thrombin and kininogenase inhibitors