FR-193262 free acid | 314289-63-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: FR-193262 free acid
• 英文别名: 2-[[(5R)-5-[(2R)-2-(4,5-diphenyl-1,3-oxazol-2-yl)pyrrolidin-1-yl]-5,6,7,8-tetrahydronaphthalen-1-yl]oxy]acetic acid
• CAS: 314289-63-9
• 化学式: C₃₁H₃₀N₂O₄
• 分子量: 494.6
• InChiKey: RIEYXRPBTRTFGV-CLJLJLNGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  37
• 可旋转键数：
  7
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  75.8
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• Pyrimido compounds having antiproliferative activity
  申请人：——

  公开号：US20040110773A1

  公开（公告）日：2004-06-10

  Disclosed are novel pyrimido compounds that are inhibitors of Src family of tyrosine kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, hepatic and pancreatic tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.

  本发明涉及一种新的嘧啶化合物，其为Src家族酪氨酸激酶的抑制剂。这些化合物及其药学上可接受的盐是抗增殖剂，可用于治疗或控制实体瘤，特别是乳腺癌、结肠癌、肝癌和胰腺癌。本发明还涉及含有这些化合物的药物组合物和治疗癌症的方法。
• REMEDIES FOR SKIN ULCER
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP1188447A1

  公开（公告）日：2002-03-20

  The invention provides an agent for the prevention and/or treatment of skin ulcer or bedsore which comprises a nonprostanoid prostaglandin I2 agonist as an active ingredient.

  本发明提供了一种用于预防和/或治疗皮肤溃疡或褥疮的制剂，其活性成分包括一种非前列腺素 I2 激动剂。
• 4,5-dipheny-oxazole derivatives and their use as platelet aggregation inhibitors
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP1213285A2

  公开（公告）日：2002-06-12

  Heterocyclic compounds of the formula:    wherein R1 is carboxy or esterified carboxy, R2 is phenyl or (C1-C6)alkylphenyl, R3 is phenyl or (C1-C6)alkylphenyl, R4 is hydrogen, (C1-C6)alkyl, hydroxy or phenyl, A1 is (C1-C6)alkylene,    in which -A4- is bond and    is cyclo (C5-C8)alkene, cyclo (C7-C8)alkane, bicycloheptane, bicycloheptene, tetrahydrofuran, tetrahydrothiophene, azetidine, pyrrolidine or piperidine, each of which may have suitable substituents,    selected from the group consisting of imino, oxo, hydroxy, (C1-C6)alkanoyl and mono (or di- or tri-)phenyl (C1-C6)alkyl, or    in which -A4- is -CH2- or -CO- and    is cyclo (C5-C8)alkene, cyclo (C7-C8)alkane, bicycloheptane, bicycloheptene and azetidine, each of which may have suitable substituents,    selected from the group consisting of imino, oxo, hydroxy, (C1-C6)alkanoyl and mono (or di- or tri-)phenyl (C1-C6)alkyl, or -A3- is -X-A6- in which ―X- is ―O-, -S- or ―N(-R5)- (in which R5 is hydrogen, (C1-C6)alkyl or acyl) and A6 is (C1-C6)alkylene which may have suitable substituent(s) selected from the group consisting of (C1-C6)alkyl and hydroxy(C1-C6)alkyl, or    in which ―A4- is -CH2- or ―CO- and    is tetrahydrofuran, tetrahydrothiophene, pyrrolidine or piperidine, each of which may have suitable substituents,    selected from the group consisting of imino, oxo, hydroxy, (C1-C6)alkanoyl and mono (or di- or tri-)phenyl (C1-C6)alkyl, or -A3- is -X-A6- in which ―X- is ―O-, -S- or ―N(-R5)- (in which R5 is hydrogen, (C1-C6)alkyl or acyl) and A6 is (C1-C6)alkylene which may have suitable substituent(s) selected from the group consisting of (C1-C6)alkyl and hydroxy(C1-C6)alkyl, and n is 0 or 1, and a pharmaceutically acceptable salt thereof, which are useful as a medicament.

  式中的杂环化合物： 其中 R1 是羧基或酯化羧基、 R2 是苯基或(C1-C6)烷基苯基 R3 是苯基或(C1-C6)烷基苯基 R4 是氢、(C1-C6)烷基、羟基或苯基、 A1 是（C1-C6）亚烷基、 其中 -A4- 是键和 是环(C5-C8)烯烃、环(C7-C8)烷烃、双环庚烷、双环庚烯、四氢呋喃、四氢噻吩、氮杂环丁烷、吡咯烷或哌啶，其中每种环(C5-C8)烯烃可带有合适的取代基、 选自由亚氨基、氧代、羟基、（C1-C6）烷酰基和单（或二或三）苯基（C1-C6）烷基组成的组，或 其中 -A4- 是 -CH2- 或 -CO- 且 是环(C5-C8)烯、环(C7-C8)烷、双环庚烷、双环庚烯和氮杂环丁烷，其中每个环(C5-C8)烯、环(C7-C8)烷、双环庚烷和氮杂环丁烷可具有适当的取代基、 选自由亚氨基、氧代、羟基、(C1-C6)烷酰基和单(或二或三)苯基 (C1-C6)烷基组成的组、 或-A3-是-X-A6-，其中-X-是-O-、-S-或-N(-R5)-（其中 R5 是氢、(C1-C6)烷基或酰基），A6 是(C1-C6)亚烷基，可具有选自(C1-C6)烷基和羟基(C1-C6)烷基组成的组的适当取代基，或 其中 -A4- 是 - - 或 -CO- 且 是四氢呋喃、四氢噻吩、吡咯烷或哌啶，其中每个都可以有合适的取代基、 选自亚氨基、氧代、羟基、(C1-C6)烷酰基和单(或二或三)苯基(C1-C6)烷基组成的组、 或-A3-是-X-A6-，其中-X-是-O-、-S-或-N(-R5)-（其中 R5 是氢、(C1-C6)烷基或酰基），A6 是(C1-C6)亚烷基，可具有选自(C1-C6)烷基和羟基(C1-C6)烷基组成的组的适当取代基、 和 n 为 0 或 1、 及其药学上可接受的盐、 可用作药物。
• TISSUE FIBROSIS INHIBITORS
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP1380307A1

  公开（公告）日：2004-01-14

  The invention provides a pharmaceutical composition containing, as the active ingredient thereof, a prostaglandin-I2 agonist, therefore providing a remedy or preventive for various disorders resulting from tissue fibrogenesis.

  本发明提供了一种药物组合物，其活性成分为前列腺素-I2 激动剂，因此可用于治疗或预防组织纤维化引起的各种疾病。
• Remedies for skin ulcer
  申请人：Fujisawa Pharmaceutical Co., Ltd.

  公开号：US20040127529A1

  公开（公告）日：2004-07-01

  The invention provides an agent for the prevention and/or treatment of skin ulcer or bedsore which comprises a nonprostanoid prostaglandin I 2 agonist as an active ingredient.

  本发明提供了一种用于预防和/或治疗皮肤溃疡或褥疮的制剂，它包括一种非前列腺素 I 2 激动剂作为活性成分。