succinimidyl-6-(biotinamido) hexanoate | 1053713-00-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 生物素及其衍生物
• 英文名称: succinimidyl-6-(biotinamido) hexanoate
• 英文别名: 5-[(3aS,4S,6aR)-4-[[6-(2,5-dioxopyrrolidin-1-yl)oxy-6-oxohexyl]carbamoyl]-2-oxo-3,3a,6,6a-tetrahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoic acid
• CAS: 1053713-00-0
• 化学式: C₂₁H₃₀N₄O₈S
• 分子量: 498.557
• InChiKey: OAMHEGLHGYDSMM-FPSMJMQUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  34
• 可旋转键数：
  14
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  197
• 氢给体数：
  4
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  3-amino-N-{4-methyl-5-[2-(4-morpholin-4-yl-phenylamino)-pyrimidin-4-yl]-thiazol-2-yl}-propionamide 、 succinimidyl-6-(biotinamido) hexanoate 以 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 3.0h， 生成 6-[5-(2-oxo-hexahydro-thieno[3,4-d]imidazol-4-yl)-pentanoylamino]-hexanoic acid (2-{4-methyl-5-[2-(4-morpholin-4-yl-phenylamino)-pyrimidin-4-yl]-thiazol-2-ylcarbamoyl}-ethyl)-amide
  参考文献：
  名称：

  [EN] PYRIMIDINE COMPOUNDS
  [FR] COMPOSES DE PYRIMIDINE

  摘要：

  本发明涉及式(I)的取代嘧啶化合物，它们的制备，含有它们的药物组合物，以及它们作为细胞周期依赖性激酶（CDKs）抑制剂的用途，因此可用于治疗增殖性疾病和/或病毒性疾病。

  公开号：

  WO2004043953A1

文献信息

• SUBSTITUTED BRIDGED UREA ANALOGS AS SIRTUIN MODULATORS
  申请人：GLAXOSMITHKLINE LLC

  公开号：US20150152108A1

  公开（公告）日：2015-06-04

  The present invention relates to novel substituted bridged urea compounds, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

  本发明涉及新型取代桥式脲化合物，相应的相关类似物，药物组合物以及其使用方法。本发明的抑制素调节化合物可用于延长细胞寿命，并治疗和/或预防各种疾病和疾病，包括但不限于与衰老或压力、糖尿病、肥胖、神经退行性疾病、心血管疾病、血液凝块疾病、炎症、癌症和/或潮红有关的疾病或疾病，以及那些会受益于增加线粒体活性的疾病或疾病。本发明还涉及包含抑制素调节化合物与另一治疗剂组合的组合物。
• [EN] COMPOUNDS AND METHODS FOR REGULATING INSULIN SECRETION<br/>[FR] COMPOSÉS ET MÉTHODES DE RÉGULATION DE SÉCRÉTION D'INSULINE
  申请人：BROAD INST INC

  公开号：WO2018175324A1

  公开（公告）日：2018-09-27

  Disclosed herein are methods for inducing insulin secretion in a glucose-dependent manner and compounds for use in these methods.

  本文揭示了一种在葡萄糖依赖性方式下诱导胰岛素分泌的方法以及用于这些方法的化合物。
• [EN] BENZOYL AMINO PYRIDYL CARBOXYLIC ACID DERIVATIVES USEFUL AS GLUCOKINASE (GLK) ACTIVATORS<br/>[FR] DERIVES DE L'ACIDE BENZOYL-AMINO-PYRIDYL-CARBOXYLIQUE UTILES EN TANT QU'ACTIVATEURS DE LA GLUCOKINASE (GLK)
  申请人：ASTRAZENECA AB

  公开号：WO2005056530A1

  公开（公告）日：2005-06-23

  A compound of Formula (I): Formula (I) wherein: R1 is selected from hydrogen and C1-4alkyl; R2 is selected from: R4-C(R5aR5b)- , R4=C(R6)- and R7aC(R7b)=C(R6)-; R3 X- is selected from methyl, methoxymethyl and ; R4 is selected from (optionally substituted) C1-4alkyl, phenyl, C3-6cycloalkyl and heteroaryl; R5a and R5b are independently selected from hydrogen, fluoro and C1-4alkyl; R6 is selected from hydrogen and C1-4alkyl; R7a and R7b are optionally substituted C1-4alkyl; or a salt, pro-drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.

  化合物的化学式（I）：化学式（I）其中：R1选择氢和C1-4烷基; R2选择自R4-C（R5aR5b）-，R4=C（R6）-和R7aC（R7b）=C（R6）-; R3X-选择甲基，甲氧甲基和; R4选择（可选取代）C1-4烷基，苯基，C3-6环烷基和杂环芳基; R5a和R5b独立选择氢，氟和C1-4烷基; R6选择氢和C1-4烷基; R7a和R7b是可选取代的C1-4烷基; 或其盐，前药或溶剂。描述了它们作为GLK激活剂的用途，包含它们的制药组合物以及它们的制备方法。
• [EN] BENZOYL AMINO PYRIDYL CARBOXYLIC ACID DERIVATIVES USEFUL AS GLUCOKINASE (GLK) ACTIVATORS<br/>[FR] DERIVES D'ACIDE BENZOYL-AMINO-PYRIDYL-CARBOXYLIQUE UTILISES EN TANT QU'ACTIVATEURS DE LA GLUCOKINASE (GLK)
  申请人：ASTRAZENECA AB

  公开号：WO2005054200A1

  公开（公告）日：2005-06-16

  Compounds of Formula: (I); wherein: R¹ is selected from: fluoro, chloro, C1-3alkyl and C1-3alkoxy; R²-X- is selected from: methyl, methoxymethyl and Formula: (X); n is 0,1 or 2; or a salt, pro-drug or solvate thereof are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.

  式化合物：(I)；其中：R¹选择自：氟、氯、C1-3烷基和C1-3烷氧基；R²-X-选择自：甲基、甲氧甲基和式：(X)；n为0、1或2；或其盐、前药或溶剂化合物。描述了它们作为GLK激活剂的用途，含有它们的药物组合物，以及它们的制备方法。
• [EN] PYRIDINE CARBOXYLIC ACID DERIVATIVES AS GLUCOKINASE MODULATORS<br/>[FR] DERIVES D'ACIDES CARBOXYLIQUE DE PYRIDINE EN TANT QUE MODULATEURS DE LA GLUCOKINASE
  申请人：ASTRAZENECA AB

  公开号：WO2005044801A1

  公开（公告）日：2005-05-19

  A compound of Formula (I): wherein: A is phenyl or a 5- or 6-membered heteroaryl ring, optionally substituted; R1 and R2 are selected from hydrogen and methyl; with the proviso that at least one of R1 and R2 is methyl; or a salt, pro-drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.

  式(I)的化合物：其中：A为苯基或5-或6-成员杂环芳基环，可选择地取代；R1和R2从氢和甲基中选取；条件是R1和R2中至少有一个为甲基；或其盐、前药或溶剂化合物。描述了它们作为GLK激活剂的用途，含有它们的药物组合物以及它们的制备方法。