CAS: 169148-63-4; Levemir (Tn)

该化合物是用于糖尿病患者血糖控制的长期活性巴沙尔胰岛素类比,它来自人类胰岛素,在位置B29的淋巴残留物中添加了14碳脂肪酸链(糖酸),这增加了可逆的蛋白结合,延长了作用时间.这一修改产生了稳定且可预测的药用植物基因特征,提供了24小时的连续葡萄糖低耗效应,与传统的中间作用胰岛素相比,变异性较小.Insulin Detemir显示低血糖和体重增重风险,使之适合1型和2型糖尿病管理.其机制涉及由于蛋白结合而从亚皮质组织中延迟吸收,确保稳定释放到流通.该化合物通常每天管理一至两次,提供施用疗法的灵活性.

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      专利信息


      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-2011152295-A1
      优先权日:2008-09-08
      标 题:Heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
      发明人:LECLERC JEAN-PHILIPPE; LI CHUN SING; RAMTOHUL YEEMAN K
      权利人:LECLERC JEAN-PHILIPPE; LI CHUN SING; RAMTOHUL YEEMAN K
      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-2011166152-A1
      优先权日:2008-10-02
      标题 :Heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
      发明人:LECLERC JEAN-PHILIPPE; LI CHUN SING; RAMTOHUL YEEMAN K
      权利人:LECLERC JEAN-PHILIPPE; LI CHUN SING; RAMTOHUL YEEMAN K
      摘要:Heteroaromatic 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, such as atherosclerosis; obesity; Type 2 diabetes; insulin resistance; hyperglycemia; Metabolic Syndrome; neurological disease; cancer; and liver steatosis.

      专利号:AU-2020409711-A1
      优先权日:2019-12-20
      标题 :Synthesis of lactone derivatives and their use in the modification of proteins

      专利号:BR-112014026077-B1
      优先权日:2012-04-20
      标 题 :METHOD OF SOLID PHASE SYNTHESIS OF A PROTECTED, PARTIALLY PROTECTED OR UNPROTECTED INSULIN B CHAIN OR AN INSULIN B CHAIN DERIVATIVE, AND METHOD FOR PREPARING AN INSULIN B CHAIN PEPTIDE

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      ✅ COA系统入驻 | 共享模式

      合成参考文献


      参考文献:10.1111/j.1463-1326.2011.01474.x
      摘要:Dungan K, Hall C, Schuster D, Osei K. Differential response between diabetes and stress‐induced hyperglycaemia to algorithmic use of detemir and flexible mealtime aspart among stable postcardiac surgery patients requiring intravenous insulin. Diabetes Obesity Metabolism. 2011 Oct 27;13(12):1130–5. doi: 10.1111/j.1463-1326.2011.01474.x.
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