phenyl(methoxy-L-alaninyl)phosphorochloridate

• 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: phenyl(methoxy-L-alaninyl)phosphorochloridate
• 英文别名: phenyl L-methoxyalaninyl phosphorochloridate；phenyl L-methoxyalaninyl phosphorchloridate；[chloro(phenoxy)phosphoryl] (2S)-2-(methoxyamino)propanoate
• 化学式: C₁₀H₁₃ClNO₅P
• 分子量: 293.644
• InChiKey: WKMSVJAOGVVHFO-RFXRWSEHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  18
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  73.9
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  phenyl(methoxy-L-alaninyl)phosphorochloridate 、 5-氟-2'-脱氧脲核苷 在 咪唑 作用下， 以 DMF (N,N-dimethyl-formamide) 为溶剂， 生成 5-Fluoro-2'-deoxy-5'-uridylphenyl L-alaninylphosphoramidate
  参考文献：
  名称：

  Enzyme catalyzed therapeutic agents

  摘要：

  该发明提供了一种通过将靶细胞与一种候选治疗剂接触来识别潜在治疗剂的方法，该候选治疗剂是细胞内源内切酶的选择性底物，该内切酶由于生物或化疗的选择而在细胞中表达增强。该发明还提供了一种通过将细胞与一种选择性底物为内源细胞内酶的前药接触来选择性杀死病理细胞的方法和示例。该前药随后转化为细胞毒素。此外，该发明还提供了一种通过向患有病理性、过度增殖细胞的受试者投与一种选择性底物为内源、过度表达的细胞内酶的前药，并由酶在过度增殖细胞中转化为细胞毒素来治疗病理的方法。

  公开号：

  US06339151B1

文献信息

• [EN] NOVEL FERROCENYL COMPOUNDS<br/>[FR] NOUVEAUX COMPOSÉS DE FERROCÉNYL
  申请人：UNIV BIRMINGHAM

  公开号：WO2015092432A1

  公开（公告）日：2015-06-25

  A ferrocenyl compound having the general formula (I) : (I) Het is a substituted or unsubstituted heterocyclic moiety. L1, L2 and L3 are each a linker independently selected from alkylene, alkyleneoxy, alkyleneoxyalkylene, alkylenecarbonyl, alkyleneoxycarbonyl, alkyleneamido, alkyleneoxyamido, alkenylene, alkenyleneoxy, alkenylenecarbonyl, alkenyleneamido, alkynylene, alkynyleneoxy, alkynylenecarbonyl and alkynyleneamido, all of which may be straight chain or branched, substituted or unsubstituted. R1 and R2 are each independently selected from H, substituted or unsubstituted alkyl carbonyl, substituted or unsubstituted aryl carbonyl, substituted or unsubstituted phosphate, substituted or unsubstituted phosphonate and substituted or unsubstituted phosphoramidate. M and n are each 0 or 1 and m + n ≠0.1

  一种具有通式(I)的二茂铁化合物：(I) Het是取代或未取代的杂环基团。L1、L2和L3分别是从烷基、烷氧基、烷氧基烷基、烷基羰基、烷氧羰基、烷基酰胺、烷氧基酰胺、烯基、烯基氧基、烯基羰基、烯基酰胺、炔基、炔基氧基、炔基羰基和炔基酰胺中独立选择的连接基，所有这些基团可以是直链或支链，取代或未取代。R1和R2分别独立选择自H、取代或未取代的烷基羰基、取代或未取代的芳基羰基、取代或未取代的磷酸酯、取代或未取代的膦酸酯和取代或未取代的磷酰胺基。M和n分别为0或1，且m + n ≠ 0.
• [EN] 4'-ALLENE-SUBSTITUTED NUCLEOSIDE DERIVATIVES<br/>[FR] DÉRIVÉS DE NUCLÉOSIDES 4'-ALLÈNE-SUBSTITUÉS
  申请人：ENANTA PHARM INC

  公开号：WO2010030858A1

  公开（公告）日：2010-03-18

  The present invention discloses compounds of formula (I), or its β-L enantiomer, or a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, solvate, prodrug, or combination thereof: Formula (I) which inhibit, preventing or treating abnormal cellular proliferation and/or a viral infection, particularly by HIV, HCV or HBV. Consequently, the compounds of the present invention interfere with the replication cycle of a virus and are also useful as antiviral agents, or interfere with host cellular biochemical process and are also useful as antiproliferative agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from viral infection and/or cell proliferation. The invention also relates to methods of treating a viral infection and/or cell proliferation in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral/anti-proliferative compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral infection in a subject in need of such therapy with said compounds.

  本发明揭示了化合物的结构式（I），或其β-L对映体，或药学上可接受的盐、酯、立体异构体、互变异构体、溶剂合物、前药或其组合物：结构式（I），其能够抑制、预防或治疗异常细胞增殖和/或病毒感染，特别是HIV、HCV或HBV。因此，本发明的化合物干扰病毒的复制周期，并且也可作为抗病毒剂使用，或干扰宿主细胞的生化过程，也可作为抗增殖剂使用。本发明还涉及包含上述化合物的药物组合物，用于治疗患有病毒感染和/或细胞增殖的受试者。该发明还涉及通过给患有病毒感染和/或细胞增殖的受试者使用包含本发明化合物的药物组合物来治疗病毒感染和/或细胞增殖的方法。本发明涉及上述新型抗病毒/抗增殖化合物，包括这些化合物的药物组合物和治疗或预防需要此类化疗的受试者的病毒感染的方法。
• NUCLEOSIDE PHOSPHORAMIDATE PRODRUGS
  申请人：SOFIA MICHAEL JOSEPH

  公开号：US20100016251A1

  公开（公告）日：2010-01-21

  Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.

  本文披露了用于治疗哺乳动物病毒感染的核苷类衍生物的磷酰胺酯前药，该前药是一种化合物，其立体异构体、盐（酸性或碱性加合盐）、水合物、溶剂合物或结晶形式，由以下结构表示：同时还披露了治疗方法、用途和制备过程，每种方法均利用由式I表示的化合物。
• [EN] CARBA-NUCLEOSIDE ANALOGS FOR ANTIVIRAL TREATMENT<br/>[FR] ANALOGUES DE CARBA-NUCLÉOSIDE POUR UN TRAITEMENT ANTIVIRAL
  申请人：GILEAD SCIENCES INC

  公开号：WO2009132123A1

  公开（公告）日：2009-10-29

  Provided are imidazol [1,5-f] [1,2.4]triazinyl, imidazol [1,2,4]triazinyl, and [1,2,4] triazolo [4,3-f] [1,2,4] triazinyl nucleosides of formula I nucleoside phosphates and prodrugs thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections. Wherein X1 or X2 is indepently C-R10 or N and wherein at least one of X1 or X2 is N.

  提供的是式I核苷酸磷酸酯和其前药，包括咪唑[1,5-f][1,2.4]三唑基、咪唑[1,2,4]三唑基和[1,2,4]三唑[4,3-f][1,2,4]三唑基。所提供的化合物、组合物和方法对于治疗黄病毒科病毒感染，特别是丙型肝炎感染，具有益处。其中X1或X2独立地为C-R10或N，且至少其中之一为N。
• [EN] SALTS OF DIPHOSPHATE PHOSPHORAMIDATE OF NUCLEOSIDES AS ANTICANCER COMPOUNDS<br/>[FR] SELS DE PHOSPHORAMIDATE DIPHOSPHATE DE NUCLÉOSIDES UTILISÉS EN TANT QUE COMPOSÉS ANTICANCÉREUX
  申请人：NUCANA PLC

  公开号：WO2019110991A1

  公开（公告）日：2019-06-13

  The present invention relates to compounds comprising a salt of a diphosphate phosphoramidate of a nucleoside drug, e.g. clofarabine. The compounds are useful in the treatment of cancer, e.g. leukemia.

  本发明涉及包括核苷药物的二磷酸磷酰胺盐化合物，例如克洛法滨。这些化合物在癌症治疗中，如白血病治疗中具有用途。