4-Cyclohexyl-5-(3-fluoro-4-methylsulfonylphenyl)-2-methyl-1,3-oxazole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-Cyclohexyl-5-(3-fluoro-4-methylsulfonylphenyl)-2-methyl-1,3-oxazole
• 化学式: C₁₇H₂₀FNO₃S
• 分子量: 337.4
• InChiKey: OJTXKPGPZRSMLT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  68.6
• 氢给体数：
  0
• 氢受体数：
  5

文献信息

• Therapeutic combinations for cardiovascular and inflammatory indications
  申请人：Pharmacia Corporation

  公开号：US20030199482A1

  公开（公告）日：2003-10-23

  The present invention provides therapeutic combinations and methods for treating or preventing a hypercholesterolemia-related or an inflammation-related condition in a subject in need of such treatment or prevention. One therapeutic combination comprises an ASBT inhibitor combined with COX-2 inhibitor. A further therapeutic combination comprises an ASBT inhibitor, a COX-2 inhibitor and an HMG Co-A reductase inhibitor. Another therapeutic combination comprises a chromene COX-2 inhibitor and an HMG Co-A reductase inhibitor.

  本发明提供了治疗组合物和方法，用于治疗或预防需要此类治疗或预防的受试者身上的高胆固醇血症相关或炎症相关疾病。一种治疗组合物包括ASBT抑制剂与COX-2抑制剂的组合。另一种治疗组合物包括ASBT抑制剂、COX-2抑制剂和HMG Co-A还原酶抑制剂。另一种治疗组合物包括一种香豆素类COX-2抑制剂和一种HMG Co-A还原酶抑制剂。
• Heterocyclic aromatic oxazole compounds and use thereof
  申请人：——

  公开号：US20020198244A1

  公开（公告）日：2002-12-26

  A heterocyclic aromatic oxazole compound of the formula (I) 1 wherein Z is an oxygen atom; one of R and R 1 is a group of the formula 2 wherein R 3 is lower alkyl, amino or lower alkylamino, and R 4 , R 5 , R 6 and R 7 are the same or different and each is hydrogen atom, halogen atom, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy or amino, provided that at least one of R 4 , R 5 , R 6 and R 7 is not hydrogen atom, and the other is an optionally substituted cycloalkyl, an optionally substituted heterocyclic group or an optionally substituted aryl; and R 2 is a lower alkyl or a halogenated lower alkyl, and a pharmaceutically acceptable salt thereof. The heterocyclic aromatic oxazole compound and pharmaceutically acceptable salts thereof have antipyretic action, analgesic action, anti-inflammatory action, and particularly, selective inhibitory action on cyclooxygenase-2 (COX-2), and are expected to be useful as anti-inflammatory agents with less side-effects such as digestive tract disorders.

  式(I)中，Z为氧原子；R和R1中的一个为式2的基团，其中R3为低碳基、氨基或低碳基氨基，R4、R5、R6和R7相同或不同，且每个为氢原子、卤素原子、低碳基、低碳氧基、三氟甲基、羟基或氨基，但至少有一个为非氢原子，另一个为可选取代的环烷基、可选取代的杂环基或可选取代的芳基；R2为低碳基或卤代低碳基，以及其药学上可接受的盐。该杂环芳香族噁唑化合物及其药学上可接受的盐具有退热作用、镇痛作用、抗炎作用，特别是对环氧合酶-2 (COX-2)的选择性抑制作用，并有望作为抗炎剂使用，具有较少的消化道副作用。
• HETEROAROMATIC OXAZOLE COMPOUNDS AND USE THEREOF
  申请人：Japan Tobacco Inc.

  公开号：EP0745596A1

  公开（公告）日：1996-12-04

  A heterocyclic aromatic oxazole compound of the formula (I) wherein Z is an oxygen atom; one of R and R1 is a group of the formula wherein R3 is lower alkyl, amino or lower alkylamino, and R4, R5, R6 and R7 are the same or different and each is hydrogen atom, halogen atom, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy or amino, provided that at least one of R4, R5, R6 and R7 is not hydrogen atom, and the other is an optionally substituted cycloalkyl, an optionally substituted heterocyclic group or an optionally substituted aryl; and R2 is a lower alkyl or a halogenated lower alkyl, and a pharmaceutically acceptable salt thereof. The heterocyclic aromatic oxazole compound and pharmaceutically acceptable salts thereof have antipyretic action, analgesic action, anti-inflammatory action, and particularly, selective inhibitory action on cyclooxygenase-2 (COX-2), and are expected to be useful as anti-inflammatory agents with less side-effects such as digestive tract disorders.

  式（I）的杂环芳香族噁唑化合物 其中 Z 是氧原子；R 和 R1 中的一个是式中的基团 其中 R3 是低级烷基、氨基或低级烷基氨基，R4、R5、R6 和 R7 相同或不同，且各自是氢原子、卤素原子、低级烷基、低级烷氧基、三氟甲基、羟基或氨基，条件是 R4、R5、R6 和 R7 中至少有一个不是氢原子，另一个是任选取代的环烷基、任选取代的杂环基团或任选取代的芳基；以及 R2 是低级烷基或卤代低级烷基，及其药学上可接受的盐。杂环芳香族噁唑化合物及其药学上可接受的盐具有解热作用、镇痛作用、抗炎作用，特别是对环氧化酶-2（COX-2）具有选择性抑制作用，可望作为副作用较少（如消化道功能紊乱）的抗炎药物。
• THERAPEUTIC COMBINATIONS FOR CARDIOVASCULAR AND INFLAMMATORY INDICATIONS
  申请人：Pharmacia Corporation

  公开号：EP1435956A2

  公开（公告）日：2004-07-14
• Homogeneous paste and gel formulations
  申请人：Nached Hassan

  公开号：US20080027011A1

  公开（公告）日：2008-01-31

  This invention provides for a pharmaceutical or veterinary paste or gel formulation which may comprise an effective amount of a therapeutic agent; optionally an absorbent or a viscosity modifier; optionally a hydrophilic carrier, a colorant, stabilizer, surfactant, or preservative and optionally an antioxidant, solvent, flavoring, buffering system or thickener and methods of preparing these formulations. This invention also provides for, inter alia, oral homogeneous veterinary pastes or gels for the treating, controlling and preventing of endo- and ectoparasite infections in warm-blooded animals, such as birds, horses and household pets.