butyl 4-hydroxypiperidine-1-carboxylate | 1310693-22-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: butyl 4-hydroxypiperidine-1-carboxylate
• 英文别名: butoxycarbonyl-4-hydroxypiperidine；Butyl-4-hydroxypiperidine-1-carboxylate
• CAS: 1310693-22-1
• 化学式: C₁₀H₁₉NO₃
• 分子量: 201.266
• InChiKey: AVKUKFHJQRKPPU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  49.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  butyl 4-hydroxypiperidine-1-carboxylate 、 1-(4-methanesulfonyl-phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-ol 在 三苯基膦 、 偶氮二甲酸二乙酯 作用下， 以 四氢呋喃 为溶剂， 生成 4-[1-(4-methanesulfonyl-phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy]-piperidine-1-carboxylic acid butyl ester
  参考文献：
  名称：

  在葡萄糖控制的啮齿动物模型中发现具有体内活性的孤儿G蛋白偶联受体GPR119的稠合双环激动剂

  摘要：

  我们在此概述了胰腺和GI表达的孤儿G蛋白偶联受体GPR119的新系列激动剂的设计，该激动剂是从原型激动剂AR231453开始的，在代谢领域中最近引起了人们的极大关注。首先通过并入吡唑并嘧啶核以创建新的结构系列，然后通过引入被氨基甲酸酯封端的哌啶醚基，改善了许多关键参数。长期使用该系列化合物中的一种3k进行的长期治疗首次显示，在数周的服药期间，Zucker糖尿病脂肪（ZDF）大鼠的血糖和糖化血红蛋白（HbA1c）水平可能显着降低。由于此处描述的这些数据和其他数据，因此3k （APD668，JNJ-28630368）是第一种具有这种作用机制的化合物，已被开发用于临床治疗糖尿病。

  DOI：

  10.1016/j.bmcl.2011.03.007

文献信息

• 2,3,4,6-TETRA-SUBSTITUTED BENZENE-1,5-DIAMINE DERIVATIVES, PREPARATION METHOD THEREFOR AND MEDICINAL USE THEREOF
  申请人：SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO., LTD.

  公开号：US20170057957A1

  公开（公告）日：2017-03-02

  The present invention relates to 2,3,4,6-tetra-substituted benzene-1,5-diamine derivatives, a preparation method therefor and a medicinal use thereof. Specifically, disclosed are compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs, preparation method therefor and application thereof. Definition of each group in the formula can be found in the specification for details.

  本发明涉及2,3,4,6-四取代苯-1,5-二胺衍生物，其制备方法及药用。具体公开了式(I)化合物或药用可接受的盐、立体异构体、溶剂合物或前药，其制备方法和应用。公式中每个基团的定义详见说明书。
• [EN] ACTIVATORS OF SMALL CONDUCTANCE CALCIUM ACTIVATED POTASSIUM CHANNELS AND USE THEREOF<br/>[FR] ACTIVATEURS DE CANAUX DE POTASSIUM ACTIVES PAR CALCIUM DE CONDUCTANCE FAIBLE ET UTILISATION ASSOCIEE
  申请人：GLAXO GROUP LTD

  公开号：WO2004014425A1

  公开（公告）日：2004-02-19

  The invention relates to activators of small conductance calcium potassium channels of formula (I) and their use in the treatment of disorders responsive to enhanced calcium activated potassium channel activity.

  该发明涉及公式（I）的小电导钙钾通道激动剂及其在对增强钙激活钾通道活性敏感的疾病治疗中的应用。
• 2,4-DISUBSTITUTED PHENYLENE-1,5-DIAMINE DERIVATIVES AND APPLICATIONS THEREOF, AND PHARMACEUTICAL COMPOSITIONS AND PHARMACEUTICALLY ACCEPTABLE COMPOSITIONS PREPARED THEREFROM
  申请人：SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO. LTD.

  公开号：US20170008889A1

  公开（公告）日：2017-01-12

  The present invention provides a class of 2,4-substituted phenylene-1,5-diamine derivatives, having an inhibiting effect on EGFR tyrosine kinases, and pharmaceutically acceptable salt, stereoisomer, solvate or prodrug of said derivatives. See the description for the definition of each group in the formula. In addition, the present invention also discloses pharmaceutical compositions, pharmaceutically acceptable compositions and applications thereof.

  本发明提供了一类2,4-取代苯基-1,5-二胺衍生物，对EGFR酪氨酸激酶具有抑制作用，并提供了该衍生物的药用可接受盐、立体异构体、溶剂合物或前药。有关每个组在公式中的定义，请参阅说明。此外，本发明还揭示了药物组合物、药用可接受组合物及其应用。
• [EN] CYCLIC AMINE COMPOUNDS AS CCR5 ANTAGONISTS<br/>[FR] COMPOSES D'AMINE CYCLIQUE UTILISES COMME ANTAGONISTES DE CCR5
  申请人：TAKEDA CHEMICAL INDUSTRIES LTD

  公开号：WO2001025200A1

  公开（公告）日：2001-04-12

  A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R?1 and R2¿ may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N?+-R5 •Y-(R5¿ is a hydrocarbon group; Y- is a counter anion); R3 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; n is 0 or 1; R4 is a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, an alkoxy group which may be substituted, an aryloxy group which may be substituted, or an amino group which may be substituted, E is a divalent aliphatic hydrocarbon group which may be substituted by group(s) other than oxo; G1 is a bond, CO or SO¿2; G?2 is CO, SO¿2?, NHCO, CONH or OCO; J is methine or a nitrogen atom; and each of Q and R is a bond or a divalent C1-3 aliphatic hydrocarbon which may be substituted; provided that J is methine when G2 is OCO, that one of Q and R is not a bond when the other is a bond and that each of Q and R is not substituted by oxo group(s) when G?1¿ is a bond) or a salt thereof has a potent CCR5 antagonistic activity and can be advantageously used for the treatment or prevention of infectious disease of various HIV in human (e.g. AIDS).

  化合物式为（I）（其中R1是氢原子，可被取代的碳氢基团，可被取代的非芳香杂环基团，R2是可被取代的碳氢基团，可被取代的非芳香杂环基团，或R1和R2可以与A一起结合形成可被取代的杂环基团；A是N或N+ -R5 • Y-（R5是碳氢基团；Y-是反离子）；R3是可被取代的环烃基团或可被取代的杂环基团；n为0或1；R4是氢原子，可被取代的碳氢基团，可被取代的杂环基团，可被取代的烷氧基，可被取代的芳氧基，或可被取代的氨基，E是可被除氧基以外的基取代的二价脂肪烃基团；G1是键，CO或SO2；G2是CO，SO2，NHCO，CONH或OCO；J是甲基或氮原子；Q和R中的每一个都是一个键或一个可被取代的二价C1-3脂肪基团；前提是当G2是OCO时，J是甲基，当另一个是键时，其中一个不是键，当G1是键时，Q和R中的每一个都没有被氧基团取代）或其盐具有强效的CCR5拮抗活性，并可用于人类各种HIV感染疾病（例如艾滋病）的治疗或预防。
• PYRAZOLONE DERIVATIVES AS PDE4 INHIBITORS
  申请人：Schmidt Beate

  公开号：US20100120757A1

  公开（公告）日：2010-05-13

  The compounds of a certain formula 1, in which R1, R7, R8, R9 and n have the meanings as given in the description, are novel effective inhibitors of the type 4 phosphodiesterase.

  某种化学式为1的化合物，其中R1、R7、R8、R9和n的含义如描述所给，是一种新型有效的4型磷酸二酯酶抑制剂。