(R)-2-{(4-chloro-benzyl)-[4-(4-fluoro-butoxy)-benzenesulfonyl]-amino}-N-hydroxy-3-phenyl-propionamide

• 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: (R)-2-{(4-chloro-benzyl)-[4-(4-fluoro-butoxy)-benzenesulfonyl]-amino}-N-hydroxy-3-phenyl-propionamide
• 英文别名: (2R)-2-[(4-chlorophenyl)methyl-[4-(4-fluorobutoxy)phenyl]sulfonylamino]-N-hydroxy-3-phenylpropanamide
• 化学式: C₂₆H₂₈ClFN₂O₅S
• 分子量: 535.036
• InChiKey: VKUXOMLWAAJWSW-RUZDIDTESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.1
• 重原子数：
  36
• 可旋转键数：
  13
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  104
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• Arylsulfonamido-substituted hydroxamic acid derivatives
  申请人：NOVARTIS AG

  公开号：EP2085379A1

  公开（公告）日：2009-08-05

  α-Amino hydroxamic acid derivative of the formula I, in which R is C2-C7-alkyl, which is mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C3-C5-cycloalkyl or unsubstituted or substituted C3-C6-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; or C3-C7-alkenyl or C3-C7-alkynyl, which in each case is unsubstituted or mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C3-C5-cydoalkyl or unsubstituted or substituted C3-C6-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; and the other symbols are as defined in claim 1, are described. These compounds are MMP and in particular MMP2 inhibitors and can be used for treatment of MMP dependent diseases, in particular inflammation conditions, rheumatoid arthritis, osteoarthritis, tumors (tumor growth, metastasis, progression or invasion) and pulmonary disorders (e.g. emphysema, COPD).

  式 I 的 α-氨基羟肟酸衍生物、 其中 R 是 C2-C7- 烷基，其被卤素、硝基、低级酰氧基、三氟甲氧基、氰基、C3-C5-环烷基或包含一个或两个选自 O、S 和 N 组成的杂原子的未取代或取代的 C3-C6- 异芳基单取代、二取代或三取代；或 C3-C7- 烷基或 C3-C7- 烷炔基，其在每种情况下均未被取代，或被卤素、硝基、低级酰氧基、三氟甲氧基、氰基、C3-C5-环烷基或未被取代或取代的 C3-C6- 杂芳基单取代、二取代或三取代，包含选自 O、S 和 N 所组成的组中的一个或两个杂原子； 其他符号如权利要求 1 所定义、 所述。 这些化合物是 MMP 特别是 MMP2 抑制剂，可用于治疗 MMP 依赖性疾病，特别是炎症、类风湿性关节炎、骨关节炎、肿瘤（肿瘤生长、转移、恶化或侵袭）和肺部疾病（如肺气肿、慢性阻塞性肺病）。
• ARYLSULFONAMIDO-SUBSTITUTED HYDROXAMIC ACID DERIVATIVES
  申请人：Novartis AG

  公开号：EP1202961B1

  公开（公告）日：2010-01-20
• US7138432B1
  申请人：——

  公开号：US7138432B1

  公开（公告）日：2006-11-21
• [EN] ARYLSULFONAMIDO-SUBSTITUTED HYDROXAMIC ACID DERIVATIVES<br/>[FR] DERIVES D'ACIDE HYDROXAMIQUE ARYLSULFONAMIDO-SUBSTITUES
  申请人：NOVARTIS AG

  公开号：WO2001010827A1

  公开（公告）日：2001-02-15

  α-Amino hydroxamic acid derivative of formula (I), in which R is C2-C7-alkyl, which is mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C3-C5-cycloalkyl or unsubstituted or substituted C3-C6-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; or C3-C7-alkenyl or C3-C7-alkynyl, which in each case is unsubstituted or mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C3-C5-cycloalkyl or unsubstituted or substituted C3-C6-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; and the other symbols are as defined in claim 1, are described. These compounds are MMP and in particular MMP2 inhibitors and can be used for treatment of MMP dependent diseases, in particular inflammation conditions, rheumatoid arthritis, osteoarthritis, tumors (tumor growth, metastasis, progression or invasion) and pulmonary disorders (e.g. emphysema, COPD).