(R)-2-methyl-6-nitro-2-{4-[4-(4-trifluoromethoxyphenoxymethyl)piperidine-1-yl]phenoxymethyl}-2,3-dihydroimidazolo[2,1-b]oxazole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (R)-2-methyl-6-nitro-2-{4-[4-(4-trifluoromethoxyphenoxymethyl)piperidine-1-yl]phenoxymethyl}-2,3-dihydroimidazolo[2,1-b]oxazole
• 英文别名: (R)-2-methyl-6-nitro-2-{4-[4-(4-trifluoromethoxyphenoxymethyl)piperidin-1-yl]phenoxymethyl}-2,3-dihydroimidazolo[2,1-b]oxazole；(R)-2-methyl-6-nitro-2-{4-[4-(4-trifluoromethoxyphenoxymethyl)piperidin-1-yl]phenoxymethyl}-2,3-dihydroimidazo[2,1-b]oxazole；(2R)-2-methyl-6-nitro-2-[[4-[4-[[4-(trifluoromethoxy)phenoxy]methyl]-1-piperidyl]phenoxy]methyl]-3H-imidazo[2,1-b]oxazole；(2R)-2-methyl-6-nitro-2-[[4-[4-[[4-(trifluoromethoxy)phenoxy]methyl]piperidin-1-yl]phenoxy]methyl]-3H-imidazo[2,1-b][1,3]oxazole
• 化学式: C₂₆H₂₇F₃N₄O₆
• 分子量: 548.519
• InChiKey: DHZIIWNTTUHXHK-RUZDIDTESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.8
• 重原子数：
  39
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  104
• 氢给体数：
  0
• 氢受体数：
  11

文献信息

• Antituberculous composition comprising oxazole compounds
  申请人：OTSUKA PHARMACEUTICAL CO., LTD.

  公开号：EP2269694A2

  公开（公告）日：2011-01-05

  The present invention provides antituberculous therapeutic drugs with a higher potency. The present invention provides also antituberculous therapeutic drugs containing oxazole compounds represented by (I) general formula (1): [wherein R1 represents a hydrogen atom or C1-6 alkyl group, n represents an integer of 0-6, and R2 represents general formula (A) or the like, wherein R represents a phenoxy group (at least one group selected from the group consisting of a halogen atom, an optionally halogen-substituted C1-6 alkyl group and an optionally halogen-substituted C1-6 alkoxy group may be substituted on the phenyl ring) or the like], optically active forms thereof or salts thereof, and drugs (II) such as secondary antituberculous drugs.

  本发明提供了效力更高的抗结核治疗药物。本发明还提供了含有由(I)通式(1)代表的噁唑化合物的抗结核治疗药物：[其中R1代表氢原子或C1-6烷基，n代表0-6的整数，R2代表通式(A)或类似物，其中R代表苯氧基（至少一个选自卤素原子、任选卤素取代的C1-6烷基和任选卤素取代的C1-6烷氧基组成的组中的基团可在苯基环上被取代）或类似物]，其光学活性形式或其盐，以及药物(II)如二级抗结核药物。
• ANTITUBERCULOUS COMPOSITION COMPRISING OXAZOLE COMPOUNDS
  申请人：Matsumoto Makoto

  公开号：US20090275528A1

  公开（公告）日：2009-11-05

  The present invention provides antituberculous therapeutic drugs with a higher potency. The present invention provides also antituberculous therapeutic drugs containing oxazole compounds represented by (I) general formula (1): [wherein R 1 represents a hydrogen atom or C1-6 alkyl group, n represents an integer of 0-6, and R 2 represents general formula (A) or the like, wherein R 3 represents a phenoxy group (at least one group selected from the group consisting of a halogen atom, an optionally halogen-substituted C1-6 alkyl group and an optionally halogen-substituted C1-6 alkoxy group may be substituted on the phenyl ring) or the like], optically active forms thereof or salts thereof, and drugs (II) such as primary antituberculous drugs.
• US8987304B2
  申请人：——

  公开号：US8987304B2

  公开（公告）日：2015-03-24
• [EN] ANTITUBERCULOUS COMPOSITION COMPRISING OXAZOLE COMPOUNDS<br/>[FR] COMPOSITION ANTI-TUBERCULOSE CONTENANT DES COMPOSES A BASE D'OXAZOLE
  申请人：OTSUKA PHARMA CO LTD

  公开号：WO2007043542A9

  公开（公告）日：2008-05-08

  [EN] The present invention provides antituberculous therapeutic drugs with a higher potency. The present invention provides also antituberculous therapeutic drugs containing oxazole compounds represented by (I) general formula (1): [wherein R¹ represents a hydrogen atom or C1-6 alkyl group, n represents an integer of 0-6, and R² represents general formula (A) or the like, wherein R³ represents a phenoxy group (at least one group selected from the group consisting of a halogen atom, an optionally halogen-substituted C1-6 alkyl group and an optionally halogen-substituted C1-6 alkoxy group may be substituted on the phenyl ring) or the like], optically active forms thereof or salts thereof, and drugs (II) such as primary antituberculous drugs.
  [FR] La présente invention a trait à des médicaments thérapeutiques contre la tuberculose avec une puissance supérieure. La présente invention a trait à des médicaments thérapeutiques contre la tuberculose contenant des composés à base d'oxazole de formule générale (I), dans laquelle: R¹ représente un atome d'hydrogène ou un groupe alkyle en C₁-C₆; n représente un nombre entier de 0 à 6; et R² représente la formule générale (A) ou analogue, dans laquelle R³ représente un groupe phénoxy (au moins un groupe choisi parmi le groupe constitué d'un atome d'halogène, d'un groupe alkyle en C₁-C₆ éventuellement substitué par halogène et un groupe alcoxy en C₁-C₆ éventuellement substitué par halogène pouvant éventuellement être substitué sur le noyau phényle) ou analogue, et des formes optiquement actives ou des sels de ceux-ci, ainsi que des médicaments (II) tels que des médicaments primaires contre la tuberculose.