(2S)-1-ethylpyrrolidine-2-carbaldehyde | 919482-06-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: (2S)-1-ethylpyrrolidine-2-carbaldehyde
• CAS: 919482-06-7
• 化学式: C₇H₁₃NO
• 分子量: 127.18
• InChiKey: JZTDQNCGEQOQLX-ZETCQYMHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  9
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• Arylalkanoic Acid Derivative
  申请人：Maekawa Tsuyoshi

  公开号：US20080051418A1

  公开（公告）日：2008-02-28

  A compound represented by the formula (I): wherein Ar is an optionally substituted aromatic ring; Xa, Xc, Ya, Yc, Z 1 and Z 2 are each a bond, O, S, —CO—, —CS—, —CR 3 (OR 4 )—, —NR 5 —, —SO—, —SO 2 —, —CONR 6 — or —NR 6 CO— (wherein R 3 , R 4 , R 5 and R 6 are as defined in the specification); Xb and Yb are each a bond or a divalent hydrocarbon group having 1 to 20 carbon atoms; R 1 is an optionally substituted hydrocarbon group; ring A is an optionally further substituted aromatic ring, provided that the ring should not be benzimidazole; n is an integer of 1 to 8; ring B is an optionally further substituted aromatic ring, provided that the ring should not be oxazole; W is a divalent saturated hydrocarbon group having 1 to 20 carbon atoms; and R 2 is —OR 8 or —NR 9 R 10 (wherein R 8 , R 9 and R 10 are as defined in the specification) or a salt thereof, is useful as an agent for the prophylaxis or treatment of diabetes and the like.

  化合物式(I)所代表的复合物，其中Ar是一个可选择性取代的芳香环；Xa、Xc、Ya、Yc、Z1和Z2分别是键合、O、S、—CO—、—CS—、—CR3(OR4)—、—NR5—、—SO—、—SO2—、—CONR6—或—NR6CO—（其中R3、R4、R5和R6如规范中所定义）；Xb和Yb分别是一个键合或具有1到20个碳原子的二价碳氢基团；R1是一个可选择性取代的碳氢基团；环A是一个可选择性进一步取代的芳香环，但不应为苯并咪唑；n是1到8的整数；环B是一个可选择性进一步取代的芳香环，但不应为噁唑；W是一个具有1到20个碳原子的二价饱和碳氢基团；和R2是—OR8或—NR9R10（其中R8、R9和R10如规范中所定义）或其盐，用作预防或治疗糖尿病等疾病的药剂。
• BIOREACTIVE AGENTS
  申请人：Rothschild Kenneth J.

  公开号：US20090075253A1

  公开（公告）日：2009-03-19

  This invention relates to agents and conjugates that can be used to detect and isolate target components from complex mixtures such as nucleic acids from biological samples, cells from bodily fluids, and nascent proteins from translation reactions. Agents comprise a detectable moiety bound to a photoreactive moiety. Conjugates comprise agents coupled to substrates by covalent bounds which can be selectively cleaved with the administration of electromagnetic radiation. Targets substances labeled with detectable molecules can be easily identified and separated from a heterologous mixture of substances. Exposure of the conjugate to radiation releases the target in a functional form and completely unaltered. Using photocleavable molecular precursors as the conjugates, label can be incorporated into macromolecules, the nascent macromolecules isolated and the label completely removed. The invention also relates to targets isolated with these conjugates which may be useful as pharmaceutical agents or compositions that can be administered to humans and other mammals. Useful compositions include biological agents such as nucleic acids, proteins, lipids and cytokines. Conjugates can also be used to monitor the pathway and half-life of pharmaceutical composition in vivo and for diagnostic, therapeutic and prophylactic purposes. The invention also relates to kits comprised of agents and conjugates that can be used for the detection of diseases, disorders and nearly any individual substance in a complex background of substances.

  本发明涉及用于检测和分离复杂混合物中的目标成分的试剂和共轭物。这些混合物包括来自生物样本的核酸、来自体液的细胞和来自翻译反应的新生蛋白质。试剂包括与光反应基团结合的可检测基团。共轭物由试剂通过共价键耦合到底物上，这些键可以通过电磁辐射的给予而被选择性地断裂。标记有可检测分子的目标物质可以轻松地从异源物质混合物中识别和分离。将光解分子前体作为共轭物，标签可以被并入大分子中，新生大分子可以被分离并完全去除标签。本发明还涉及使用这些共轭物分离的目标物质，这些目标物质可能作为药物或组成物在人类和其他哺乳动物中使用。有用的组成物包括核酸、蛋白质、脂质和细胞因子等生物制剂。共轭物还可用于监测体内药物组成物的途径和半衰期，以及用于诊断、治疗和预防目的。本发明还涉及试剂和共轭物组成的试剂盒，可用于检测疾病、疾病和几乎任何复杂物质背景中的个体物质。
• COVALENT TETHERING OF FUNCTIONAL GROUPS TO PROTEINS AND SUBSTRATES THEREFOR
  申请人：Promega Corporation

  公开号：US20150125924A1

  公开（公告）日：2015-05-07

  A mutant hydrolase optionally fused to a protein of interest is provided. The mutant hydrolase is capable of forming a bond with a substrate for the corresponding nonmutant (wild-type) hydrolase which is more stable than the bond formed between the wild-type hydrolase and the substrate and has at least two amino acid substitutions relative to the wild-type hydrolase. Substrates for hydrolases comprising one or more functional groups are also provided, as well as methods of using the mutant hydrolase and the substrates of the invention. Also provided is a fusion protein capable of forming a stable bond with a substrate and cells which express the fusion protein.

  本发明提供了一种可选地与感兴趣的蛋白质融合的突变水解酶。该突变水解酶能够与相应的非突变（野生型）水解酶的底物形成比野生型水解酶与底物形成的键更加稳定的键，并且相对于野生型水解酶至少有两个氨基酸替换。本发明还提供了一种具有一种或多种功能基团的水解酶的底物，以及使用突变水解酶和本发明的底物的方法。还提供了一种能够与底物形成稳定键的融合蛋白和表达该融合蛋白的细胞。
• FUSED HETEROCYCLIC DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, AND MEDICINAL USE THEREOF
  申请人：Kissei Pharmaceutical Co., Ltd.

  公开号：EP1609798A9

  公开（公告）日：2012-01-11

  The present invention provides fused heterocyclic derivatives represented by the general formula: wherein R1 represents H, halogen, OH, etc.; R2 represents H, halogen or an alkyl group; R3 and R4 represent H, OH, halogen, etc.; Q represents alkylene, etc.; ring A represents aryl or heteroaryl; and G represents or     or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.

  本发明提供了由通式表示的融合杂环衍生物： 其中 R1 代表 H、卤素、OH 等；R2 代表 H、卤素或烷基；R3 和 R4 代表 H、OH、卤素等；Q 代表亚烷基等；环 A 代表芳基或杂芳基；以及 G 代表 或 或其药学上可接受的盐，或其原药，它们对人类 SGLT 具有优异的抑制活性，可用作预防或治疗与高血糖有关的疾病（如糖尿病、餐后高血糖、糖耐量受损、糖尿病并发症或肥胖）的制剂、包含这些制剂的药物组合物及其药物用途。
• Small peptides for the treatment of Alzheimer's disease and other beta-amyloid protein fibrillogenesis disorders
  申请人：Proteotech Inc.

  公开号：EP2380583A1

  公开（公告）日：2011-10-26

  A composition of matter that includes the peptide sequence Arg-Val-Ala-Val-Ile-Met-Gly-amide (Dp-068). A pharmaceutical composition that includes peptide Arg-Val-Ala-Val-Ile-Met-Gly-amide (Dp-068). Use of the peptide for preparation of a medicament for the treatment of a diseases characterized by Aβ fibrillogenesis. Use of an aantibody directed against a peptide comprising Arg-Val-Ala-Val-Ile-Met-Gly-amide in the manufacture of a medicament for the treatment of a disease characterized by Aβ fibrillogenesis. Preferably where at least one amino acid of the peptide sequence is a D-amino acid.

  一种包括肽序列Arg-Val-Ala-Val-Ile-Met-Gly-amide (Dp-068)的物质组合物。一种药物组合物，它包括肽 Arg-Val-Ala-Val-Ile-Met-Gly-amide (Dp-068)。该肽用于制备治疗以Aβ纤丝化为特征的疾病的药物。将针对包含Arg-Val-Ala-Val-Ile-Met-Gly-amide的多肽的抗体用于制造治疗以Aβ纤溶为特征的疾病的药物。最好肽序列中至少有一个氨基酸是D-氨基酸。