γ-oxonorvaline hydrochloride | 197237-27-7

• 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: γ-oxonorvaline hydrochloride
• 英文别名: 2-amino-4-oxo-valeric acid ; hydrochloride；2-Amino-4-oxo-valeriansaeure; Hydrochlorid；aminolevulinic hydrochloride；2-Amino-4-oxopentanoic acid hydrochloride；2-amino-4-oxopentanoic acid;hydrochloride
• CAS: 197237-27-7
• 化学式: C₅H₉NO₃*ClH
• mdl: MFCD22578633
• 分子量: 167.592
• InChiKey: BYAFJYYQCWOTAX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.15
• 重原子数：
  10
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  80.4
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  γ-oxonorvaline hydrochloride 在 碳酸氢钠 作用下， 生成 (E)-4-氧代-2-烯酸
  参考文献：
  名称：

  569.氨基酸和肽。第四部分。α-乙酰丙氨酸（2-氨基-4-氧杂戊酸），N-甘氨酰-α-乙酰丙氨酸和相关化合物的碱性水解

  摘要：

  DOI：

  10.1039/jr9630003100
• 作为产物：
  描述：

  2-[1-(4-methoxyphenyl)ethylamino]-4-oxopentanoic acid 在 盐酸 作用下， 以 水 为溶剂， 反应 48.0h， 生成 γ-oxonorvaline hydrochloride
  参考文献：
  名称：

  立体合成合成γ-羟降冰片碱及相关α-氨基酸

  摘要：

  The total syntheses of three enantiomerically pure non-proteinogenic amino acids, l-norvaline, γ-oxonorvaline, and syn-γ-hydroxynorvaline, are reported. The chromatography-free route pivoted on the construction of highly enantiomerically enriched substituted α-amino-γ-oxopentanoic acid, from which all three members were accessed divergently via chemoselective and stereoselective reductions. The rapid

  DOI：

  10.1055/s-0039-1690705

文献信息

• [EN] 5-AMINO-2,4,7-TRIOXO-3,4,7,8-TETRAHYDRO-2H-PYRIDO'2,3-D! PYRIMIDINE DERIVATIVES AND RELATED COMPOUNDS FOR THE TREATMENT OF CANCER<br/>[FR] DÉRIVÉS DE 5-AMINO-2,4,7-TRIOXO-3,4,7,8-TÉTRAHYDRO-2H-PYRIDO'2,3-D! PYRIMIDINE ET COMPOSÉS APPARENTÉS POUR LE TRAITEMENT DU CANCER
  申请人：JAPAN TOBACCO INC

  公开号：WO2005121142A1

  公开（公告）日：2005-12-22

  The present invention relates to a pyrimidine compound represented by the following formula [I] wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and a pharmaceutical agent for the prophylaxis or treatment of a disease caused by undesirable cell proliferation, particularly an antitumor agent, which contains such compound. The compound of the present invention has superior undesirable cell proliferation suppressing action, particularly, an antitumor action, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, antirheumatoid agent and the like. In addition, by the combined use with other antitumor agent such as alkylating agent, metabolism antagonist and the like, it can be a more effective antitumor agent.

  本发明涉及一种由以下式[I]表示的嘧啶化合物，其中每个符号如规范中所定义，其药学上可接受的盐，以及用于预防或治疗由不良细胞增殖引起的疾病的药物剂，特别是一种抗肿瘤剂，其中包含这种化合物。本发明的化合物具有优越的不良细胞增殖抑制作用，特别是抗肿瘤作用，并且可用作预防或治疗癌症的抗肿瘤剂，抗风湿剂等。此外，通过与其他抗肿瘤剂如烷化剂、代谢拮抗剂等的联合使用，可以使其成为更有效的抗肿瘤剂。
• [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。