(S)-alfa-氨基-4-哌啶乙酸 | 459166-03-1

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: (S)-alfa-氨基-4-哌啶乙酸
• 英文名称: (S)-2-amino-2-(piperidin-4-yl)acetic acid
• 英文别名: (S)-alfa-Amino-4-piperidine acetic acid；(2S)-2-amino-2-piperidin-4-ylacetic acid
• CAS: 459166-03-1
• 化学式: C₇H₁₄N₂O₂
• 分子量: 158.2
• InChiKey: SRMWKNUAAAAUED-LURJTMIESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3
• 重原子数：
  11
• 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：
  75.4
• 氢给体数：
  3
• 氢受体数：
  4

安全信息

• 海关编码：
  2933399090

反应信息

• 作为反应物：
  描述：

  (S)-alfa-氨基-4-哌啶乙酸 在 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 为溶剂， 生成 L-4-piperidineglycinol
  参考文献：
  名称：

  (S)-N-(5-Chlorothiophene-2-sulfonyl)-β,β-diethylalaninol a Notch-1-sparing γ-secretase inhibitor

  摘要：

  Accumulation of beta-amyloid (A beta), produced by the proteolytic cleavage of amyloid precursor protein (APP) by beta- and gamma-secretase, is widely believed to be associated with Alzheimer's disease (AD). Research around the high-throughput screening hit (S)-4-chlorophenylsulfonyl isoleucinol led to the identification of the Notch-1-sparing (9.5-fold) gamma-secretase inhibitor (S)-N-(5-chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol 7.b.2 (A beta (40/42) EC50 = 28 nM), which is efficacious in reduction of A beta production in vivo. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.11.116

文献信息

• DIMERIC IAP INHIBITORS
  申请人：STRAUB Christopher Sean

  公开号：US20110206690A1

  公开（公告）日：2011-08-25

  The present invention provides compounds of formula M-L-M′ (where M and M′ are each independently a monomeric moiety of Formula (I) and L is a linker). The dimeric compounds have been found to be effective in promoting apoptosis in rapidly dividing cells.

  本发明提供了公式M-L-M′的化合物（其中M和M′分别是公式（I）中的单体基团，L是连接物）。已发现二聚化合物在促进快速分裂细胞凋亡方面具有有效性。
• Conjugate comprising a neurotensin receptor ligand and use thereof
  申请人：3B Pharmaceuticals GmbH

  公开号：EP2954934A1

  公开（公告）日：2015-12-16

  The present invention is related to a conjugate comprising a structure of general formula (1)         [TM1] - [AD1] - [LM] - [AD2] - [TM2]     (1), wherein TM1 is a first targeting moiety, wherein the first targeting moiety is capable of binding to a first target, AD1 is a first adapter moiety or is absent, LM is a linker moiety or is absent, AD2 is a second adapter moiety or is absent, and TM2 is a second targeting moiety, wherein the second targeting moiety is capable of binding to a second target; wherein the first targeting moiety and/or the second targeting moiety is a compound of formula (2): wherein R1 is selected from the group consisting of hydrogen, methyl and cyclopropylmethyl; AA-COOH is an amino acid selected from the group consisting of 2-amino-2-adamantane carboxylic acid, cyclohexylglycine and 9-amino-bicyclo[3.3.1]nonane-9-carboxylic acid; R2 is selected from the group consisting of (C1-C6)alkyl, (C3-C8)cycloalkyl, (C3C8)cycloalkylmethyl, halogen, nitro and trifluoromethyl; ALK is (C2-C5)alkylidene; R3, R4 and R5 are each and independently selected from the group consisting of hydrogen and (C1-C4)alkyl under the proviso that one of R3, R4 and R5 is of the following formula (3) wherein ALK' is (C2-C5)alkylidene; R6 is selected from the group consisting of hydrogen and (C1-C4)alkyl; and R7 is a bond; or a pharmacologically acceptable salt, solvate or hydrate thereof.

  本发明涉及一种包含通式（1）结构的共轭物 [TM1] - [AD1] - [LM] - [AD2] - [TM2] (1)、 其中 TM1 是第一靶向分子，其中第一靶向分子能够与第一靶点结合、 AD1 是第一适配基团或不存在、 LM 是连接分子或不存在、 AD2 是第二适配基团或不存在，以及 TM2 是第二靶向分子，其中第二靶向分子能与第二靶点结合； 其中第一靶向分子和/或第二靶向分子为式（2）化合物： 其中 R1 选自由氢、甲基和环丙基甲基组成的组； AA-COOH 是一种氨基酸，选自由 2-氨基-2-金刚烷羧酸、环己基甘氨酸和 9-氨基-双环[3.3.1]壬烷-9-羧酸组成的组； R2 选自(C1-C6)烷基、(C3-C8)环烷基、(C3C8)环烷基甲基、卤素、硝基和三氟甲基组成的组； ALK 是（C2-C5）亚烷基； R3、R4 和 R5 各自独立地选自氢和(C1-C4)烷基组成的组，但 R3、R4 和 R5 中的一个必须符合下式 (3) 其中 ALK' 是 (C2-C5) 亚烷基； R6 选自氢和（C1-C4）烷基组成的组；以及 R7 是键； 或其药理学上可接受的盐、溶液或水合物。
• NPR-B agonists
  申请人：Shire Orphan Therapies GmbH

  公开号：US10196423B2

  公开（公告）日：2019-02-05

  Disclosed are novel compounds having NPR-B agonistic activity. Preferred compounds are linear peptides containing 8-13 conventional or non-conventional L- or D-amino acid residues connected to one another via peptide bonds.

  所公开的是具有 NPR-B 激动活性的新型化合物。优选化合物是线性肽，含有 8-13 个通过肽键相互连接的常规或非常规 L 或 D 氨基酸残基。
• NOVEL NPR-B AGONISTS
  申请人：Shire Orphan Therapies GmbH

  公开号：EP2480247B1

  公开（公告）日：2020-02-12
• Novel NPR-B Agonists
  申请人：SHIRE ORPHAN THERAPIES GMBH

  公开号：US20160194357A1

  公开（公告）日：2016-07-07

  Disclosed are novel compounds having NPR-B agonistic activity. Preferred compounds are linear peptides containing 8-13 conventional or non-conventional L- or D-amino acid residues connected to one another via peptide bonds.