CAS: 141642-82-2; 1-Tert-Butyl 4-Ethyl 5-Oxoazepane-1,4-Dicarboxylate

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31696-09-0 141642-82-2 912444-87-2

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二碳酸二叔丁酯置于三氟化硼乙醚,三乙胺体系中,用 乙醚,二氯甲烷 用作溶剂,化学反应 17.0H,反应生成1-Boc-5-氧代氮杂环庚烷-甲酸乙酯
参考文献:作为潜在抗惊厥药的 3-[(2,4-Dioxo-1,3,8-Triazaspiro[4.6]Undec-3-yl)Methyl] 苄腈衍生物的合成与评价
标题:作为潜在抗惊厥药的 3-[(2,4-Dioxo-1,3,8-Triazaspiro[4.6]Undec-3-yl)Methyl] 苄腈衍生物的合成与评价
摘要:合成了新的 3-[(2,4-Dioxo-1,3,8-Triazaspiro[4.6]Undec-3-yl)Methyl] 苄腈衍生物 8-37 并测定了它们的药理活性,目的是更好地了解它们的结构-抗惊厥活性的活性关系 (Sar).通过最大电休克发作(mes)和戊四唑(ptz)试验评估所有化合物可能的抗惊厥活性.与标准药物丙戊酸盐相比,化合物 11,18,31 和 32 对癫痫发作具有显着的保护作用.发现相同的化合物表现出先进的抗惊厥活性以及比参考药物更低的神经毒性.从这项研究中可以很明显地看出,抗惊厥药物的活性至少有三个参数,即亲脂结构域,疏水中心,
Doi:10.1002/ardp.201200400

专利信息

专利号:US-2024082435-A1
优先权日:2021-02-26
标 题 :Solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates and their use as precursors for therapeutic and/or diagnostic agents
发明人：PINTO ARTUR; BONTEMPS ALEXIS; LEMAIRE LUCAS
权利人:TELIX INT INNOVATIONS PTY LTD
摘要:The disclosure provides methods for the solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates. The disclosure also relates to key intermediates of this process and methods for their preparation such as a method of preparing a compound of formula (V). Also disclosed are use of the conjugates as precursors for therapeutic and/or diagnostic agents, including treating and diagnosing prostate cancer.

专利号:US-2024400552-A1
优先权日:2016-11-11
标题 :Heterocyclic modulators of lipid synthesis
发明人：BUCKLEY DOUGLAS I; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S
权利人:SAGIMET BIOSCIENCES INC
摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by dysregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).

专利号:US-11622968-B2
优先权日:2011-03-08
标 题:Heterocyclic modulators of lipid synthesis
发明人：BUCKLEY DOUGLAS; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S
权利人:SAGIMET BIOSCIENCES INC
摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).

专利号:US-10226449-B2
优先权日:2013-12-20
标 题:Heterocyclic modulators of lipid synthesis and combinations thereof
发明人：HEUER TIMOTHY SEAN; OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; DUKE GREGORY; OHOL-GUPTA YAMINI; O'FARRELL MARIE
权利人:3 V BIOSCIENCES INC
摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by dysregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.

专利号:US-11034690-B2
优先权日:2016-11-11
标 题:Heterocyclic modulators of lipid synthesis
发明人：BUCKLEY DOUGLAS I; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S
权利人:SAGIMET BIOSCIENCES INC; SAGINIET BIOSCIENCES INC
摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).

专利号:US-9428502-B2
优先权日:2012-07-03
标题:Heterocyclic modulators of lipid synthesis
发明人：OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; WAGMAN ALLAN S
权利人:3-V BIOSCIENCES INC
摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.