4-Benzyl-3-(2-methylpropanoyl)-1,3-oxazolidin-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 英文名称: 4-Benzyl-3-(2-methylpropanoyl)-1,3-oxazolidin-2-one
• 化学式: C₁₄H₁₇NO₃
• 分子量: 247.29
• InChiKey: MUIYUSOHHCEUTC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  46.6
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• Peptides
  申请人：Bauer Wilfried

  公开号：US20050009147A1

  公开（公告）日：2005-01-13

  PTH compounds having PTH-like activity and comprising at least one modification, said modification being either 1. at least one radical selected from a L- or D-α-amino acid, C 2-6 alcoxycarbonyl and optionally substituted C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, aralkyl, aralkenyl or C 3-6 cycloalkyl-C 1-4 alkyl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C 2-6 alcoxycarbonyl and optionally substituted C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, aralkyl, aralkenyl or C 3-6 cycloalkyl-C 1-4 alkyl and attached to one or more side chain amino groups of the PTH compound, or 2. at least one α-amino acid unit in the positions 1 to 38 of a naturally occurring PTH sequence being replaced by a natural or unnatural amino acid unit optionally in protected form, whereby the α-amino acid units present in positions 1 and 2 at the amino terminus of the PTH sequence may be replaced by a pseudo-peptide, or a combination of such modifications, in free form or in salt form, have pharmacological activity, e.g. for preventing or treating all bone conditions which are associated with increased calcium depletion or resorption or in which calcium fixation in the bone is desirable.

  具有 PTH 样活性并包含至少一种修饰的 PTH 化合物，所述修饰为： 1. 至少一个选自 L- 或 D-α- 氨基酸、C 2-6 至少一个选自 L-或 D-α-氨基酸、C 2-6 1-8 烷基、C 2-8 烯基、C 2-8 炔基、烷基、烯基或 C 3-6 环烷基-C 1-4 烷基，并与 PTH 化合物的末端氨基相连，和/或至少一个选自 C 2-6 烷氧基羰基和任选取代的 C 1-8 烷基、C 2-8 烯基、C 2-8 炔基、烷基、烯基或 C 3-6 环烷基-C 1-4 天然存在的 PTH 序列 1 至 38 位上的至少一个 α-氨基酸单元被天然或非天然氨基酸单元（可选择以保护形式）取代，由此，PTH 序列氨基末端 1 和 2 位上的α-氨基酸单元可被假肽取代，或此类修饰的组合，以游离形式或盐形式存在，具有药理活性，例如，用于预防或治疗与钙耗竭或吸收增加有关的所有骨病，或用于预防或治疗与钙耗竭或吸收增加有关的所有骨病，或用于预防或治疗与钙耗竭或吸收增加有关的所有骨病，或用于预防或治疗与钙耗竭或吸收增加有关的所有骨病，或用于预防或治疗与钙耗竭或吸收增加有关的所有骨病，或用于预防或治疗与钙耗竭或吸收增加有关的所有骨病。例如，可用于预防或治疗所有与钙消耗或吸收增加有关的骨病，或希望钙固定在骨中的骨病。
• PEPTIDES
  申请人：Bauer Wilfried

  公开号：US20080318838A1

  公开（公告）日：2008-12-25

  PTH compounds having PTH-like activity and comprising at least one modification, said modification being either 1. at least one radical selected from a L- or D-α-amino acid, C 2-6 alcoxycarbonyl and optionally substituted C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, aralkyl, aralkenyl or C 3-6 cycloalkyl-C 1-4 alkyl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C 2-6 alcoxycarbonyl and optionally substituted C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, aralkyl, aralkenyl or C 3-6 cycloalkyl-C 1-4 alkyl and attached to one or more side chain amino groups of the PTH compound, or 2. at least one α-amino acid unit in the positions 1 to 38 of a naturally occurring PTH sequence being replaced by a natural or unnatural amino acid unit optionally in protected form, whereby the α-amino acid units present in positions 1 and 2 at the amino terminus of the PTH sequence may be replaced by a pseudo-peptide, or a combination of such modifications, in free form or in salt form, have pharmacological activity, e.g. for preventing or treating all bone conditions which are associated with increased calcium depletion or resorption or in which calcium fixation in the bone is desirable.
• [EN] ANALOGS OF PTH<br/>[FR] ANALOGUES DE PARATHORMONE
  申请人：——

  公开号：WO1994002510A2

  公开（公告）日：1994-02-03

  [EN] PTH compounds having PTH-like activity and comprising at least one modification, said modification being either 1) at least one radical selected from an L- or D-(alpha)-amino acid, C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to one or more side chain amino groups of the PTH compound; or 2) at least one (alpha)-amino acid unit in the positions 1 to 38 of a naturally occurring PTH sequence being replaced by a natural or unnatural amino acid unit optionally in protected form, whereby the (alpha)-amino acid units present in positions 1 and 2 at the amino terminus of the PTH sequence may be replaced by a pseudo-peptide, or a combination of such modifications, in free form or in salt form, have pharmacological activity, e.g. for preventing or treating all bone conditions which are associated with increased calcium depletion or resorption or in which calcium fixation in the bone is desirable.
  [FR] L'invention concerne des composés de parathormone et ayant l'activité de cette hormone, avec au moins une modification. Cette modification peut consister soit 1) en au moins un radical choisi parmi les acides alpha-aminés L ou D, un groupe alcoxycarbonyle C2-6 et les groupes (le cas échéant substitués) alkyle C1-8, alcényle C2-8, alcynyle C2-8, aralkyle, aralcényle ou cycloalkyl C3-6- alkyle C1-4 et fixé au groupe amino terminal de la parathormone, et/ou au moins un radical choisi parmi les groupes alcoxycarbonyle C2-6 et les groupes (le cas échéant substitués) alkyle C1-8, alcényle C2-8, alcynyle C2-8, aralkyle, aralcényle ou cycloalkyl C3-6-alkyle C1-4 et fixé à un ou plusieurs groupes amino à chaînes latérales du composé de parathormone, soit 2) en au moins une unité d'acide alpha-aminé dans les positions 1 à 38 de la séquence naturelle de la parathormone remplacée par une unité d'acide alpha-aminé naturel ou non, le cas échéant sous une forme protégée, les unités d'acide alpha-aminé en position 1 et 2 à la terminaison amino de la séquence de la parathormone pouvant être remplacées par un pseudo-peptide, soit en une combinaison de telles modifications. Ce polypeptide sous forme libre ou d'un sel a une activité pharmacologique utile dans la prévention ou le traitement d'états pathologiques osseux provoqués par une décalcification osseuse ou une résorption osseuse, ou encore dans le traitement d'états nécessitant une amélioration de la fixation du calcium dans les os.