CAS: 35120-18-4; Ethyl 1-Bromocyclobutanecarboxylate

相似化合物

32122-23-9 51175-79-2 14924-53-9

上下游产品

CAS号14924-53-9 环丁烷甲酸乙酯 | CAS号64-17-5 乙醇 | CAS号3721-95-7 环丁基甲酸 | CAS号120728-10-1 B°C-1-氨基环丁烷羧酸 | CAS号32122-23-9 1-溴环丁烷甲酸 | CAS号2987-17-9 环丁基甲醛 | CAS号49640-66-6 1-(羟甲基)环丙烷羧酸

环丁烷甲酸乙酯置于n-溴代丁二酰亚胺(Nbs),偶氮二异丁腈体系中,用 四氯化碳 作为反应溶剂,化学反应 16.0H,以40%的收率获得产物乙基1-溴环丁烷甲酸酯
参考文献:连接物的献血作用决定了二硫键连接的吡咯并苯并二氮杂卓抗体-药物结合物的细胞杀伤活性
标题:连接物的献血作用决定了二硫键连接的吡咯并苯并二氮杂卓抗体-药物结合物的细胞杀伤活性
摘要:对于需要在分子的两个部分之间进行可调裂解的各种治疗应用,二硫键可能是有价值的连接子(例如抗体-药物偶联物).研究了β-巯基乙基-氨基甲酸酯二硫化物的体外接头消灭和相关有效负载的dna烷基化特性,以了解抗cd22连接的吡咯并苯并二氮杂(pbd-二聚体)缀合物对细胞杀伤力的决定性作用.在甲基和环丁基取代的二硫键被二硫键裂解后,观测到具有强大的dna烷基化特性的pbd-二聚体的有效分解和释放.但是,类似的含环丙基的连接基并没有被烧毁,并且相关的含硫醇的产物是一个不良的dna烷基化剂.正如这些体外评估所预测的那样,相关的抗cd22 Adc在wsu-Dlcl2和bjab细胞系中显示出不同的靶标依赖性细胞杀伤活性.这些结果证明了体外献血模型如何可用于帮助设计有效的adc.
DOI:10.1021/acsmedchemlett.6B00233

专利信息

专利号:WO-0010565-A1
优先权日:1998-08-18
标 题 :Growth hormone secretagogues
发明人：DODGE JEFFREY ALAN; HAUSER KENNETH LEE; HEIMAN MARK LOUIS; JONES SCOTT ALAN; ALT CHARLES ARTHUR; BRYANT HENRY UHLMAN; COHEN JEFFREY DANIEL; COPP JAMES DENSMORE; FAHEY KENNAN JOSEPH; GRITTON WILLIAM HARLAN; JUNGHEIM LOUIS NICKOLAUS; KENNEDY JOSEPH HENRY; LUGAR CHARLES WILLIS III; MUEHL BRIAN STEPHEN; PALKOWITZ ALAN DAVID; RATZ ANDREW MICHAEL; RHODES GARY ANTHONY; ROBEY ROBERT LEWIS; SEYLER DAVID EDWARD; SHEPHERD TIMOTHY ALAN; THRASHER KENNETH JEFF; TRANKLE WILLIAM GEORGE
权利人:LILLY CO ELI; DODGE JEFFREY ALAN; HAUSER KENNETH LEE; HEIMAN MARK LOUIS; JONES SCOTT ALAN; ALT CHARLES ARTHUR; BRYANT HENRY UHLMAN; COHEN JEFFREY DANIEL; COPP JAMES DENSMORE; FAHEY KENNAN JOSEPH; GRITTON WILLIAM HARLAN; JUNGHEIM LOUIS NICKOLAUS; KENNEDY JOSEPH HENRY; LUGAR CHARLES WILLIS III; MUEHL BRIAN STEPHEN; PALKOWITZ ALAN DAVID; RATZ ANDREW MICHAEL; RHODES GARY ANTHONY; ROBEY ROBERT LEWIS; SEYLER DAVID EDWARD; SHEPHERD TIMOTHY ALAN; THRASHER KENNETH JEFF; TRANKLE WILLIAM GEORGE
摘要:This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.

专利号:US-6992097-B2
优先权日:1998-08-18
标 题 :Growth hormone secretagogues
发明人：HAUSER KENNETH LEE; DODGE JEFFREY ALAN; HEIMAN MARK LOUIS; JONES SCOTT ALAN; ALT CHARLES ARTHUR; BRYANT HENRY UHLMAN; COHEN JEFFREY DANIEL; COPP JAMES DENSMORE; FAHEY KENNAN JOSEPH; GRITTON WILLIAM HARLAN; JUNGHEIM LOUIS NICKOLAUS; KENNEDY JOSEPH HENRY; LUGAR III CHARLES WILLIS; MUEHL BRIAN STEPHEN; PALKOWITZ ALAN DAVID; RATZ ANDREW MICHAEL; RHODES GARY ANTHONY; ROBEY ROGER LEWIS; SEYLER DAVID EDWARD; SHEPHERD TIMOTHY ALAN; THRASHER KENNETH JEFF; TRANKLE WILLIAM GEORGE
权利人:LILLY CO ELI
摘要:This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.