CAS: 41731-83-3; Ethyl 2-Bromothiazole-5-Carboxylate

上下游产品

CAS号32955-21-8 2-氨基噻唑-5-羧酸酯 | CAS号3034-53-5 2-溴噻唑 | CAS号623-49-4 氰基甲酸乙酯 | CAS号216867-46-8 2-(4-吡啶)噻唑-5-羧酸 | CAS号54045-76-0 2-溴噻唑-5-甲酸 | CAS号687636-93-7 2-溴噻唑-5-甲醇 | CAS号848499-31-0 2-溴噻唑-5-甲酰胺

📜2-氨基噻唑-5-羧酸乙酯置于亚硝酸特丁酯,Copper(Ll) Bromide体系中,用 乙腈 作为反应溶剂,以4.4 %的收率获得产物2-溴噻唑-5-甲酸乙酯
参考文献:基于片段的药物发现活动中的片段大小的噻唑:朋友还是敌人
标题:基于片段的药物发现活动中的片段大小的噻唑:朋友还是敌人
摘要:噻唑具有广泛的生物活性,因此代表了有用且有吸引力的结构单元.为了评估它们的用途并确定它们在片段筛选活动中的责任,我们组装了一个包含 49 个片段大小的噻唑和噻二唑的重点库,这些化合物具有各种取代基,即胺,溴化物,羧酸和腈.该文库在一系列生化抑制测定,氧化还原活性,硫醇反应性和稳定性测定中进行了分析.我们的研究表明,当噻唑衍生物被确定为筛选命中时,应仔细处理它们的反应性并将其与特定的靶向参与相关联.重要的是,应使用实验方法和计算机排除非特异性抑制预测.为了帮助验证在片段筛选活动中确定的命中,我们可以应用我们的高通量分析工作流程来专注于具有明确作用机制的最易处理的化合物.
DOI:10.1021/acsmedchemlett.2C00429

专利信息

专利号:US-2009170828-A1
优先权日:2006-06-12
标题:Azetidine Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase
发明人：ISABEL ELISE; OBALLA RENATA; POWELL DAVID; ROBICHAUD JOEL
权利人:ISABEL ELISE; OBALLA RENATA; POWELL DAVID; ROBICHAUD JOEL
摘要:Azetidine derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis. (I)

专利号:US-2011301143-A1
优先权日:2009-02-23
标题 :Heterocyclic derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：ISABEL ELISE; LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; RAMTOHUL YEEMAN K; ROY PATRICK; TRANMER GEOFFREY K; ASPIOTIS RENEE; LI LIANHAI; MARTINS EVELYN
权利人:ISABEL ELISE; LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; RAMTOHUL YEEMAN K; ROY PATRICK; TRANMER GEOFFREY K; ASPIOTIS RENEE; LI LIANHAI; MARTINS EVELYN
摘要:Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R1— substituted heteroaryl, R1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N—CR5R6, Câ•?CR5 or CR13—CR5R6, Y is a bond or —C(O)—, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis, obesity, diabetes, neurological disease, Metabolic Syndrome, insulin resistance, cancer, liver steatosis, and non-alcoholic steatohepatitis.

专利号:US-2012010186-A1
优先权日:2009-03-23
标题:Heterocyclic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：LACHANCE NICOLAS; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; TRANMER GEOFFREY K; MARTINS EVELYN; GAREAU YVES
权利人:LACHANCE NICOLAS; LEGER SERGE; OBALLA RENATA M; POWELL DAVID; TRANMER GEOFFREY K; MARTINS EVELYN; GAREAU YVES; MERCK FROSST CANADA LTD
摘要:Heterocyclic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer, liver steatosis; and non-alcoholic steatohepatitis.

专利号:US-9168248-B2
优先权日:2009-02-17
标 题:Spiro compounds useful as inhibitors of stearoyl-coenzyme A delta-9 desaturase
发明人：LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LI CHUN SING; MORADEI OSCAR MIGUEL
权利人:LACHANCE NICOLAS; LECLERC JEAN-PHILIPPE; LI CHUN SING; MORADEI OSCAR MIGUEL; MERCK CANADA INC
摘要:Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.

专利号:US-8383643-B2
优先权日:2009-07-28
标题 :Spiro compounds useful as inhibitors of stearoyl-coenzyme A delta-9 desaturase
发明人：LECLERC JEAN-PHILIPPE; LI CHUN-SING; MORADEI OSCAR MIGUEL
权利人:MERCK CANADA INC; LECLERC JEAN-PHILIPPE; LI CHUN-SING; MORADEI OSCAR MIGUEL
摘要:Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.

专利号:WO-2010065383-A1
优先权日:2008-11-25
标 题 :Calcilytic compounds
发明人：CASILLAS LINDA N; CHARNLEY ADAM KENNETH; HARRIS PHILIP ANTHONY; JEONG JAE U; MARQUIS ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT
权利人:GLAXOSMITHKLINE LLC; CASILLAS LINDA N; CHARNLEY ADAM KENNETH; HARRIS PHILIP ANTHONY; JEONG JAE U; MARQUIS ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT
摘要:Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.