2-Amino-2-(piperidin-4-yl)acetic acid

• 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
• 英文名称: 2-Amino-2-(piperidin-4-yl)acetic acid
• 英文别名: 2-amino-2-piperidin-4-ylacetic acid
• 化学式: C₇H₁₄N₂O₂
• mdl: MFCD18651602
• 分子量: 158.2
• InChiKey: SRMWKNUAAAAUED-UHFFFAOYSA-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：
  0.857
• 拓扑面积：
  75.4
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• [EN] THIOSEMICARBAZATES AND USES THEREOF<br/>[FR] THIOSEMICARBAZATES ET LEURS UTILISATIONS
  申请人：FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH

  公开号：WO2020227592A1

  公开（公告）日：2020-11-12

  Thioesters, thiocarbamates, thiocarbazates, semithiocarbazates, peptides, aza-amino acid conjugates, and azapeptides; and a chemoselective and site-specific functionalization protocol of protected thiocarbazates and semithiocarbazates are described. The protocol features the use of Mitsunobu reaction to alkylate specifically the nitrogen atom close to the acylthiol moiety with alcohols to produce protected mono-substituted thiocarbazates that can be stored for months, activated under mild conditions at low temperature using halonium reagents and integrated orthogonally to make substituted semicarbazides that can be used, e.g., as synthons in synthesis of aza-amino acid conjugates, azapeptides and other peptidomimetics. Methods for preparing and using ureases, carbazides, semicarbazides, beta-peptides, azapeptides, and other peptidomimetics and azapeptide conjugates, and uses of ureases, carbazides, semicarbazides, beta-peptides, azapeptides in drug discovery, diagnosis, inhibition, prevention and treatment of diseases are also described.

  巯酯，硫代氨基甲酸酯，硫代氨基甲酸酯，半硫代氨基甲酸酯，肽，氮代氨基酸共轭物和氮代肽；以及一种对受保护的硫代氨基甲酸酯和半硫代氨基甲酸酯进行化学选择性和位点特异性功能化的方法被描述。该方法采用三甲基脲反应特异性烷基化靠近酰硫醇基团的氮原子，使用醇生成可储存数月的受保护的单取代硫代氨基甲酸酯，在低温下使用卤化物试剂轻微条件下激活，并与其他基团正交集成以制备取代半氨基甲酸酰胺，例如，可用作氮代氨基酸共轭物，氮代肽和其他肽类模拟物的合成中间体。还描述了制备和使用尿酶，卡巴酰胺，半氨基甲酸酰胺，β-肽，氮代肽和其他肽类模拟物以及氮代肽共轭物的方法，以及尿酶，卡巴酰胺，半氨基甲酸酰胺，β-肽，氮代肽在药物发现，诊断，抑制，预防和治疗疾病中的用途。
• NOVEL MULTIMERIC MOLECULES, A PROCESS FOR PREPARING THE SAME AND THE USE THEREOF FOR MANUFACTURING MEDICINAL DRUGS
  申请人：Guichard Gilles

  公开号：US20100136034A1

  公开（公告）日：2010-06-03

  The invention relates to a compound of the formula (I): in which k and j are independently 0 or 1, Y is a macrocycle in which the cycle includes 9 to 36 carbon atoms and is functionalised by three amino functions and by a chain for attaching the spacer arm Z via an X bond, R c is a binding pattern with a receptor of the TNF superfamily, X is a chemical function for binding the Y group to the space arm, and Z is a bi-, tri- or tetra-functional spacer arm.

  该发明涉及以下式（I）的化合物： 其中k和j独立地为0或1，Y是一个大环，其中该环包括9至36个碳原子，并且通过三个氨基功能和通过链将间隔臂Z通过X键连接的功能化，Rc是与TNF超家族受体的结合模式，X是用于将Y基固定到空间臂的化学功能，Z是双功能、三功能或四功能间隔臂。
• NOVEL MULTIMERIC CD40 LIGANDS, METHOD FOR PREPARING SAME AND USE THEREOF FOR PREPARING DRUGS
  申请人：Guichard Gilles

  公开号：US20100183642A1

  公开（公告）日：2010-07-22

  The invention concerns a compound of formula (I), wherein Y represents a macrocycle whereof the cycle comprises 9 to 36 atoms, and is functionalized by three amine or COOH functions; R c represents a group of formula H—X a —X b —X c —X d —X e —(X f ) i —, wherein i represents 0 or 1, X n is in particular selected among lysine, arginine, ornithine residues, X b is in particular selected among glycine, asparagine, L-proline or D-proline residues, X c et X d are in particular selected among tyrosine, phenylalanine or 3-nitrotyrosine residues, X e et X f are in particular selected among the following amino acid residues: NH 2 —(CH 2 ) n —COOH, n ranging from 1 to 10 or NH 2 —(CH 2 —CH 2 —O) m —CH 2 CH 2 COOH, m ranging from 3 to 6, provided that one at least of the amino acid residues X a , X b , X c and X d is different from the corresponding amino acid in the sequence of the natural CD40 143 Lys-Gly-Tyr-Tyr 146 fragment

  该发明涉及一种化合物，其化学式为（I），其中Y代表一个大环，该环包含9至36个原子，并且通过三个胺基或COOH功能官能化；Rc代表一个化学式为H—Xa—Xb—Xc—Xd—Xe—（Xf）i—的基团，其中i代表0或1，Xn特别选自赖氨酸、精氨酸、鸟氨酸残基之一，Xb特别选自甘氨酸、天冬氨酸、L-脯氨酸或D-脯氨酸残基之一，Xc和Xd特别选自酪氨酸、苯丙氨酸或3-硝基酪氨酸残基之一，Xe和Xf特别选自以下氨基酸残基之一：NH2—（CH2）n—COOH，其中n取1至10之间的值，或NH2—（ — —O）m— COOH，其中m取3至6之间的值，前提是氨基酸残基Xa、Xb、Xc和Xd中至少有一个与天然CD40143Lys-Gly-Tyr-Tyr146片段中相应的氨基酸不同。
• [EN] RADIOLABELED BOMBESIN-DERIVED COMPOUNDS FOR IN VIVO IMAGING OF GASTRIN-RELEASING PEPTIDE RECEPTOR (GRPR) AND TREATMENT OF GRPR-RELATED DISORDERS<br/>[FR] COMPOSÉS RADIOMARQUÉS DÉRIVÉS DE LA BOMBÉSINE POUR L'IMAGERIE IN VIVO DU RÉCEPTEUR DU PEPTIDE LIBÉRANT DE LA GASTRINE (GRPR) ET TRAITEMENT DES TROUBLES LIÉS AU GRPR
  申请人：PROVINCIAL HEALTH SERVICES AUTHORITY

  公开号：WO2021068051A1

  公开（公告）日：2021-04-15

  There is provided bombesin-derived compounds of Formula Ia (RX-L-Xaa1-Gln-Trp-Ala-Val-Xaa2-His-Xaa3-ψ-Xaa4-NH2). RX comprises a radionuclide chelator or a trifluoroborate-containing prosthetic group. L is a linker. Xaa1 is D-Phe, Cpa (4-chlorophenylalanine), D-Cpa, Tpi (2,3,4,9-tetrahydro-1H-pyrido[3,4b]indol-3-carboxylic acid), D-Tpi, Nal (naphthylalanine), or D-Nal. Xaa2 is Gly, N-methyl-Gly or D-Ala. Xaa3 is Leu, Pro, D-Pro, or Phe. Xaa4 is Pro, Phe, Tac (thiazolidine-4-carboxylic acid), Nle (norleucine), 4-oxa-L-Pro (oxazolidine-4-carboxylic acid). The symbol ψ represents a reduced peptide bond between Xaa3 and Xaa4 in which ψ is CH2-N when Xaa4 is Pro, Tac or 4-oxa-L-Pro, or ψ is CH2N(R) when Xaa4 is Phe or Nle wherein R is H or C1-C5 linear or branched alkyl. There is also provided the use of such compounds as imaging agents or therapeutic agents.

  提供了Formula Ia（RX-L-Xaa1-Gln-Trp-Ala-Val-Xaa2-His-Xaa3-ψ-Xaa4-NH2）的波美斯因衍生物。RX包括放射性同位素螯合剂或三氟硼酸酯含基团。L是连接剂。Xaa1是D-Phe，Cpa（4-氯苯丙氨酸），D-Cpa，Tpi（2,3,4,9-四氢-1H-吡啶[3,4b]吲哚-3-羧酸），D-Tpi，Nal（萘丙氨酸）或D-Nal。Xaa2是Gly，N-甲基-Gly或D-Ala。Xaa3是Leu，Pro，D-Pro或Phe。Xaa4是Pro，Phe，Tac（噻唑啉-4-羧酸），Nle（正癸氨酸），4-氧代-L-Pro（噁唑啉-4-羧酸）。符号ψ代表Xaa3和Xaa4之间的还原肽键，其中当Xaa4为Pro，Tac或4-氧代-L-Pro时，ψ为CH2-N，或当Xaa4为Phe或Nle时，ψ为 N(R)，其中R为H或C1-C5线性或支链烷基。还提供了将这些化合物用作成像剂或治疗剂的用途。
• [EN] PIPECOLIC LINKER AND ITS USE FOR CHEMISTRY ON SOLID SUPPORT<br/>[FR] LIEUR PIPÉCOLIQUE ET SON UTILISATION POUR UNE CHIMIE SUR SUPPORT SOLIDE
  申请人：CENTRE NAT RECH SCIENT

  公开号：WO2010023295A1

  公开（公告）日：2010-03-04

  The present invention relates to a pipecolic linker and its use as a solid-phase linker in organic synthesis. Said pipecolic solid-phase linker may be used for coupling functional groups chosen between primary amines, secondary amines, aromatic amines, alcohols, phenols and thiols. In particular, said pipecolic solid-phase linker may be used for peptide or pseudopeptide synthesis, such as the reverse N to C peptide synthesis or the retro-inverso peptide synthesis, or for the synthesis of small organic molecules.

  本发明涉及一种吡啶哌酸链连接剂及其在有机合成中作为固相连接剂的用途。所述吡啶哌酸固相连接剂可用于将功能基团偶联在一起，这些功能基团可选择为一级胺、二级胺、芳香胺、醇、酚和硫醇。特别地，所述吡啶哌酸固相连接剂可用于肽或伪肽合成，例如反向N到C肽合成或反向逆转肽合成，或用于小有机分子的合成。