4-(4-aminophenyl)-1,2,5-oxadiazol-3-amine | 440110-71-4

• 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: 4-(4-aminophenyl)-1,2,5-oxadiazol-3-amine
• CAS: 440110-71-4
• 化学式: C₈H₈N₄O
• mdl: MFCD02647381
• 分子量: 176.178
• InChiKey: PXNZHWOGIVAURZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  91
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  N-叔丁氧羰基-3-哌啶酮 、 4-(4-aminophenyl)-1,2,5-oxadiazol-3-amine 生成 tert-Butyl 3-(4-(4-Amino-1,2,5-oxadiazol-3-yl)phenylamino)piperidine-1-carboxylate
  参考文献：
  名称：

  Cytoskeletal active rho kinase inhibitor compounds, composition and use

  摘要：

  本发明涉及合成的细胞骨架活性化合物，其为rho相关蛋白激酶的抑制剂。本发明还涉及包含这种化合物和药学上可接受的载体的制药组合物。此外，本发明还涉及一种预防或治疗与细胞骨架重组相关的疾病或症状的方法。在本发明的一种实施方式中，该方法治疗增加的眼内压，例如原发性开角型青光眼。该方法包括向受试者施用公式I或公式II的细胞骨架活性化合物的治疗有效量，其中该量有效地影响肌动蛋白相互作用，例如通过导致细胞松弛和细胞-基质粘附的改变。

  公开号：

  US08071779B2
• 作为产物：
  描述：

  3-amino-4-(4'-nitrophenyl)-1,2,5-oxadiazole 在 tin(ll) chloride 作用下， 以 水 、 乙酸乙酯 为溶剂， 以94%的产率得到4-(4-aminophenyl)-1,2,5-oxadiazol-3-amine
  参考文献：
  名称：

  CYTOSKELETAL ACTIVE RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE

  摘要：

  本发明涉及一种合成的细胞骨架活性化合物，其为rho相关蛋白激酶的抑制剂。本发明还涉及包含此类化合物和药用载体的制药组合物。此外，本发明还涉及一种预防或治疗与细胞骨架重组相关的疾病或病症的方法。在本发明的一个实施例中，该方法治疗增加的眼内压，如原发性开角型青光眼。该方法包括向受体施用公式I或公式II的细胞骨架活性化合物的治疗有效量，其中该量能够影响肌动蛋白相互作用，例如通过导致细胞松弛和细胞基质附着的改变。

  公开号：

  US20080214614A1

文献信息

• BRIDGED BICYCLIC RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE
  申请人：Lampe John W.

  公开号：US20110144150A1

  公开（公告）日：2011-06-16

  The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. The method comprises administering to a subject a therapeutically effective amount of a Rho kinase inhibitory compound of Formula I, wherein said amount is effective to influence the actomyosin interactions, for example, by leading to cellular relaxation and alterations in cell-substratum adhesions. In one embodiment, the method treats increased intraocular pressure, such as primary open-angle glaucoma. In another embodiment, the method treats diseases or conditions of the lung associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema.

  本发明涉及一种合成的桥接双环化合物，该化合物是rho相关蛋白激酶的抑制剂。本发明还涉及包括这些化合物和药用可接受载体的药物组合物。此外，本发明还涉及一种预防或治疗与细胞骨架重组相关的疾病或症状的方法。该方法包括向受试者施用一定量的具有治疗作用的公式I的Rho激酶抑制剂化合物，其中该量有效地影响肌动蛋白互作，例如，通过导致细胞松弛和细胞-基质粘附的改变。在一种实施方式中，该方法治疗增加的眼内压，如原发性开角青光眼。在另一种实施方式中，该方法治疗与肺部细胞过度增殖、重塑、炎症、血管收缩、支气管收缩、气道高反应性和水肿相关的疾病或症状。
• Bridged bicyclic RHO kinase inhibitor compounds, composition and use
  申请人：Lampe John W.

  公开号：US08476295B2

  公开（公告）日：2013-07-02

  The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. The method comprises administering to a subject a therapeutically effective amount of a Rho kinase inhibitory compound of Formula I, wherein said amount is effective to influence the actomyosin interactions, for example, by leading to cellular relaxation and alterations in cell-substratum adhesions. In one embodiment, the method treats increased intraocular pressure, such as primary open-angle glaucoma. In another embodiment, the method treats diseases or conditions of the lung associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema.

  本发明涉及合成的桥式双环化合物，它们是rho相关蛋白激酶的抑制剂。本发明还涉及包含这种化合物和药用载体的制药组合物。此外，本发明还涉及一种预防或治疗与细胞骨架重组相关的疾病或病况的方法。该方法包括向受试者施用式I的Rho激酶抑制剂的治疗有效量，其中所述量对影响肌动蛋白相互作用是有效的，例如，通过导致细胞松弛和细胞基质附着的改变。在一种实施例中，该方法治疗增加的眼压，如原发性开角型青光眼。在另一种实施例中，该方法治疗与细胞增殖、重塑、炎症、血管收缩、支气管收缩、气道高反应性和水肿过度相关的肺部疾病或病况。
• BRIDGED BICYCLIC RHO KINASE INHIBITOR COMPOUNDS, COMPOSITIONS AND USE
  申请人：Lampe John W.

  公开号：US20130281485A1

  公开（公告）日：2013-10-24

  The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. The method comprises administering to a subject a therapeutically effective amount of a Rho kinase inhibitory compound of Formula I, wherein said amount is effective to influence the actomyosin interactions, for example, by leading to cellular relaxation and alterations in cell-substratum adhesions. In one embodiment, the method treats increased intraocular pressure, such as primary open-angle glaucoma. In another embodiment, the method treats diseases or conditions of the lung associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema.

  本发明涉及一种合成的桥接双环化合物，它们是rho相关蛋白激酶的抑制剂。本发明还涉及包含这种化合物和药用载体的制药组合物。此外，本发明还涉及一种预防或治疗与细胞骨架重组相关的疾病或病症的方法。该方法包括向受试者施用一种公式I的Rho激酶抑制化合物的治疗有效量，其中该量对影响肌动蛋白相互作用有效，例如通过导致细胞松弛和细胞-基质附着的变化。在一种实施方式中，该方法治疗增加的眼压，例如原发性开角型青光眼。在另一种实施方式中，该方法治疗与过度细胞增殖、重塑、炎症、血管收缩、支气管收缩、气道高反应性和水肿相关的肺部疾病或病症。
• Bridged bicyclic RHO kinase inhibitor compounds, compositions and use
  申请人：Lampe John W.

  公开号：US08835457B2

  公开（公告）日：2014-09-16

  The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. The method comprises administering to a subject a therapeutically effective amount of a Rho kinase inhibitory compound of Formula I, wherein said amount is effective to influence the actomyosin interactions, for example, by leading to cellular relaxation and alterations in cell-substratum adhesions. In one embodiment, the method treats increased intraocular pressure, such as primary open-angle glaucoma. In another embodiment, the method treats diseases or conditions of the lung associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema.

  本发明涉及合成的桥接双环化合物，其为rho相关蛋白激酶的抑制剂。本发明还涉及包含这样的化合物和药学上可接受的载体的制药组合物。此外，本发明还涉及一种预防或治疗与细胞骨架重组相关的疾病或症状的方法。该方法包括向受试者施用公式I的Rho激酶抑制剂的治疗有效量，其中该量有效地影响肌动蛋白相互作用，例如通过导致细胞松弛和细胞基质黏附的改变。在一种实施方式中，该方法治疗增加的眼压，如原发性开角型青光眼。在另一种实施方式中，该方法治疗与细胞增殖过度、重塑、炎症、血管收缩、支气管收缩、气道高反应性和水肿相关的肺部疾病或症状。
• US8071779B2
  申请人：——

  公开号：US8071779B2

  公开（公告）日：2011-12-06