3-氨基-4-[[(Z)-4-[4-(哌啶-1-基甲基)吡啶-2-基]氧基丁-2-烯基]氨基]环丁-3-烯-1,2-二酮盐酸盐 | 126463-66-9

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 3-氨基-4-[[(Z)-4-[4-(哌啶-1-基甲基)吡啶-2-基]氧基丁-2-烯基]氨基]环丁-3-烯-1,2-二酮盐酸盐
• 中文别名: 8-甲氧基-3-(2H-四唑-5-基)-2H-色烯-2-酮
• 英文名称: oxaldehyde
• 英文别名: IT 066；3-amino-4-[[(Z)-4-[4-(piperidin-1-ylmethyl)pyridin-2-yl]oxybut-2-enyl]amino]cyclobut-3-ene-1,2-dione;hydron;chloride
• CAS: 126463-66-9
• 化学式: C₁₉H₂₄N₄O₃*ClH
• 分子量: 392.885
• InChiKey: ODBOENMSSFCACZ-PVOKDAACSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.71
• 重原子数：
  27
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  97.6
• 氢给体数：
  3
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  4-氟苯肼 、 3-氨基-4-[[(Z)-4-[4-(哌啶-1-基甲基)吡啶-2-基]氧基丁-2-烯基]氨基]环丁-3-烯-1,2-二酮盐酸盐 以84 %的产率得到(E)-2-(2-(4-fluorophenyl)hydrazono)acetaldehyde
  参考文献：
  名称：

  PYRIDAZINONE-BASED COMPOUNDS AS AXL, C-MET, AND MER INHIBITORS AND METHODS OF USE THEREOF

  摘要：

  Provided is an inhibitor of AXL, Mer, and/or c-Met of Formula (I) or a pharmaceutically acceptable salt thereof: in which R 1 , R 2 , R 3 , G, and Q are described herein. Further provided is a method of treating or preventing an AXL-, Mer-, and/or c-Met-mediated disease using an effective amount of the compound of Formula (I) or a pharmaceutically acceptable salt thereof. When AXL, MER, and/or c-Met is inhibited, the compound or pharmaceutically acceptable salt thereof can re-sensitize cancer cells, such as non-small cell lung cancer cells, that have grown resistant to an anti-cancer agent.

  公开号：

  US20230257364A1
• 作为产物：
  描述：

  3-Cyclobutene-1,2-dione, 3-methoxy-4-[[4-[[4-(1-piperidinylmethyl)-2-pyridinyl]oxy]-2-butenyl]amino]-, (Z)- 以65.2的产率得到3-氨基-4-[[(Z)-4-[4-(哌啶-1-基甲基)吡啶-2-基]氧基丁-2-烯基]氨基]环丁-3-烯-1,2-二酮盐酸盐
  参考文献：
  名称：

  Pyridyloxy derivatives

  摘要：

  通式表示的吡啶氧基衍生物：##STR1##其中取代基Z是以下其中之一：##STR2##已被制备。这些衍生物对组胺H2受体具有拮抗作用，因此对治疗消化性溃疡有效。

  公开号：

  US04710498A1

文献信息

• [EN] POLYMERIC HYPERBRANCHED CARRIER-LINKED PRODRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À DES EXCIPIENTS POLYMÉRIQUES HYPERBRANCHÉS
  申请人：ASCENDIS PHARMA AS

  公开号：WO2013024048A1

  公开（公告）日：2013-02-21

  The present invention relates to water-soluble carrier-linked prodrugs of formula (I),wherein POL is a polymeric moiety,each Hyp is independently a hyperbranched moiety,each moiety SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, m is 0 or 1, each n is independently an integer from 2 to 200 and each x is independently 0 or 1. It further relates to pharmaceutical compositions comprising said water- soluble carrier-linked prodrugs and methods of treatment.

  本发明涉及水溶性载体连接的前药，其化学式为（I），其中POL是聚合物基团，每个Hyp是独立的超支化基团，每个基团SP是独立的间隔基团，每个L是独立的可逆前药连接基团，m为0或1，每个n是独立的整数，范围从2到200，每个x是独立的0或1。此外，还涉及包含所述水溶性载体连接的前药的药物组合物和治疗方法。
• [EN] HIGH-LOADING WATER-SOLUBLE CARRIER-LINKED PRODRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À DES EXCIPIENTS HYDROSOLUBLES DE FORTE CHARGE
  申请人：ASCENDIS PHARMA AS

  公开号：WO2013024047A1

  公开（公告）日：2013-02-21

  The present invention relates to water-soluble carrier-linked prodrugs of formula (I), wherein B, A and Hyp form the carrier, B is a branching core, each A is independently a poly(ethylene glycol)-based polymeric chain, each Hyp is independently a branched moiety, each SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, each D is independendly a biologically active moiety, each x is independently 0 or 1, each m is independently an integer of from 2 to 64, n is an integer from 3 to 32; or the pharmaceutically acceptable salt thereof. It further relates to pharmaceutical compositions comprising said water-soluble carrier-linked prodrugs, their use asmedicament or diagnostic, and methods of treatment.

  本发明涉及水溶性载体连接的前药，其化学式为(I)，其中B、A和Hyp形成载体，B是一个分支核心，每个A独立地是一条聚乙二醇基聚合链，每个Hyp独立地是一个分支基团，每个SP独立地是一个间隔基团，每个L独立地是一个可逆前药连接基团，每个D独立地是一个生物活性基团，每个x独立地为0或1，每个m独立地是从2到64的整数，n是从3到32的整数；或其药学上可接受的盐。进一步涉及包括所述水溶性载体连接的前药的药物组合物，其用作药物或诊断，以及治疗方法。
• [EN] RELEASABLE CONJUGATES<br/>[FR] CONJUGUÉS LIBÉRABLES
  申请人：QUIAPEG PHARMACEUTICALS AB

  公开号：WO2018163131A1

  公开（公告）日：2018-09-13

  The present application provides compounds of Formula (B), or pharmaceutically acceptable salts thereof, wherein D is a residue of a biologically active drug, which underdo hydrolysis under physiological conditions to release the biologically active drug and which are useful in the treatment of disorders that could be beneficially treated with the drug.

  本申请提供了化合物的公式（B），或其药用盐，其中D是生物活性药物的残留物，在生理条件下经过水解释放出生物活性药物，并且对可能受益于该药物治疗的疾病具有用处。
• [EN] PROTEIN CARRIER-LINKED PRODRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À UN EXCIPIENT PROTÉIQUE
  申请人：ASCENDIS PHARMA AS

  公开号：WO2013024049A1

  公开（公告）日：2013-02-21

  The present invention relates to water-soluble protein carrier- linked prodrugs wherein the protein carrier comprises an amino acid sequence consisting of at least 100 amino acid residues forming random coil conformation and comprising alanine, serine and proline residues. It further relates to pharmaceutical compositions comprising said water-soluble protein carrier- linked prodrugs, their use as a medicament as well as methods of treatment and administration.

  本发明涉及水溶性蛋白载体连接的前药，其中蛋白载体包括至少100个氨基酸残基组成的氨基酸序列，形成随机卷曲构象，包括丙氨酸、丝氨酸和脯氨酸残基。还涉及包含上述水溶性蛋白载体连接的前药的药物组合物，它们作为药物的用途，以及治疗和管理的方法。
• [EN] HYDROGEL-LINKED PRODRUGS RELEASING MODIFIED DRUGS<br/>[FR] PROMÉDICAMENTS LIÉS À UN HYDROGEL LIBÉRANT DES MÉDICAMENTS MODIFIÉS
  申请人：ASCENDIS PHARMA AS

  公开号：WO2014173759A1

  公开（公告）日：2014-10-30

  The present invention relates to a process for the preparation of a hydrogel-linked prodrug releasing a tag moiety-bio logically active moiety conjugate, to a hydrogel-linked prodrug releasing a tag moiety-bio logically active moiety conjugate obtainable by such process, to pharmaceutical compositions comprising said prodrug and their use as a medicament.

  本发明涉及一种制备水凝胶连接的前药释放标签基团-生物活性基团结合物的方法，以及通过该方法获得的水凝胶连接的前药释放标签基团-生物活性基团结合物，还涉及包含该前药的药物组合物及其作为药物的用途。