4-Hydroxy-4-methyl-2-(methylamino)pentanoic 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: 4-Hydroxy-4-methyl-2-(methylamino)pentanoic acid
• 化学式: C₇H₁₅NO₃
• 分子量: 161.2
• InChiKey: JRKMRRWEUORVRJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.6
• 重原子数：
  11
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  69.6
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• DERIVES DE CYCLOSPORINE, LEUR PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT
  申请人：Aventis Pharma S.A.

  公开号：EP0979244B1

  公开（公告）日：2005-03-02
• Novel [N-Me-4-hydroxyleucine]-9-Cyclosporin Analogues for Treatment and Prevention of Hepatitis C Infection
  申请人：ENANTA PHARMACEUTICALS, INC.

  公开号：US20140154208A1

  公开（公告）日：2014-06-05

  The present invention relates to novel cyclosporine analogues having antiviral activity against HCV and useful in the treatment of HCV infections. More particularly, the invention relates to novel cyclosporine analogue compounds, compositions containing such compounds and methods for using the same, as well as processes for making such compounds.
• US8906853B2
  申请人：——

  公开号：US8906853B2

  公开（公告）日：2014-12-09
• [EN] NOVEL CYCLOSPORIN DERIVATIVES, PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME<br/>[FR] NOUVEAUX DERIVES DE CYCLOSPORINE, LEUR PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES QUI LES CONTIENNENT
  申请人：RHONE-POULENC RORER S.A.

  公开号：WO1998049193A1

  公开（公告）日：1998-11-05

  (EN) The invention concerns cyclosporin derivatives of general formula (I) in which R is H or a radical (Ia) for which Alk-R° is methyl or Alk is (C2-C6) alkylene linear or branched or (C3-C6) cycloalkylene and R° is either H, OH, COOH or alkyloxycarbonyl, or a -NR1R2 radical for which R1 and R2 identical or different represent H, alkyl, alkenyl, (C3-C6)cycloalkyl, phenyl optionally substituted, or represent benzyl or saturated or unsaturated heterocyclyl compound (5 or 6 chains and 1 to 3 heteroatoms), or for which R1 and R2 form with the nitrogen atom a heterocyclic compound with 5 or 6 chains containing another heteroatom: N, O or S and optionally substituted, or a radical (Ib) for which R1 and R2 are defined as above, R3 is H or alkyl and n = 2 to 4; R' is a radical (Ic) or (Id) for which R4 is alkylthio, aminoalkythio, alkylaminoalkylthio, dialkylaminoalkylthio, pyrimidinylthio, thiazolylthio, N-alkylimidazolylthio, hydroxyalkylphenylthio, hydroxyalkylphenyloxy, nitrophenylamino, 2-oxopyrimidin-1-yl, and R'4 represents alkyl; and R' represents H or OH, provided that R and R' are not H simultaneously, and their pharmaceutically acceptable salts when they exist. These novel products are particularly useful for treating and/or preventing retrovirus infections.(FR) Dérivés de la cyclosporine de formule générale (I) dans laquelle R est H ou un radical (Ia) pour lequel Alk-R° est méthyle ou bien, Alk est alcoylène (2 à 6C) droit ou ramifié ou cycloalcoylène (3 à 6C) et R° est soit H, OH, COOH ou alcoyloxycarbonyle, soit un radical -NR1R2 pour lequel R1 et R2 identiques ou différents représentent H, alcoyle, alcényle, cycloalcoyle (3 à 6C), phényle éventuellement substitué, ou représentent benzyle ou hétérocyclyle saturé ou insaturé (5 ou 6 chaînons et 1 à 3 hétéroatomes), ou pour lequel R1 et R2 forment avec l'atome d'azote un hétérocycle à 5 ou 6 chaînons pouvant contenir un autre hétéroatome: N, O ou S et éventuellement substitué, soit un radical (Ib) pour lequel R1 et R2 sont définis comme ci-dessus, R3 est H ou alcoyle et n = 2 à 4; R' est un radical (Ic) ou (Id) pour lequel R4 est alcoylthio, aminoalcoylthio, alcoylaminoalcoylthio, dialcoylaminoalcoylthio, pyrimidinylthio, thiazolylthio, N-alcoylimidazolylthio, hydroxyalcoylphénylthio, hydroxyalcolylphényloxy, nitrophénylamino, 2-oxopyrimidin-1-yle, et R'4 représente alcoyle; et R' représente H ou OH, sous réserve que R et R' ne soient pas simultanément H, et leurs sels pharmaceutiquement acceptables lorsqu'ils existent. Ces nouveaux produits sont particulièrement utiles pour le traitement et/ou la prophylaxie des infections à rétrovirus.
• [EN] NOVEL [N-ME-4-HYDROXYLEUCINE]-9-CYCLOSPORIN ANALOGUES<br/>[FR] NOUVEAUX ANALOGUES DE [N-ME-4-HYDROXYLEUCINE]-9-CYCLOSPORINE
  申请人：ENANTA PHARM INC

  公开号：WO2014085623A1

  公开（公告）日：2014-06-05

  The present invention relates to novel cyclosporine analogues having antiviral activity against HCV and useful in the treatment of HCV infections. More particularly, the invention relates to novel cyclosporine analogue compounds, compositions containing such compounds and methods for using the same, as well as processes for making such compounds.