基本信息:
- 专利标题： CYTOSKELETAL ACTIVE RHO KINASE INHIBITOR COMPOUNDS, COMPOSITION AND USE
- 专利标题（中）：CYTOSKELETAL活性RHO激酶抑制剂化合物，组合物和用途
- 申请号：PCT/US2007087973 申请日：2007-12-18
- 公开(公告)号：WO2008077057A3 公开(公告)日：2008-08-21
- 发明人： LAMPE JOHN W , WATSON PAUL S , SLADE DAVID J , PETERSON WARD M , CREAN CHRISTOPHER S , VITTITOW JASON L , DECAMP JONATHAN BRYAN , PELZ NICHOLAS F
- 申请人： INSPIRE PHARMACEUTICALS INC , LAMPE JOHN W , WATSON PAUL S , SLADE DAVID J , PETERSON WARD M , CREAN CHRISTOPHER S , VITTITOW JASON L , DECAMP JONATHAN BRYAN , PELZ NICHOLAS F
- 专利权人： INSPIRE PHARMACEUTICALS INC,LAMPE JOHN W,WATSON PAUL S,SLADE DAVID J,PETERSON WARD M,CREAN CHRISTOPHER S,VITTITOW JASON L,DECAMP JONATHAN BRYAN,PELZ NICHOLAS F
- 当前专利权人： INSPIRE PHARMACEUTICALS INC,LAMPE JOHN W,WATSON PAUL S,SLADE DAVID J,PETERSON WARD M,CREAN CHRISTOPHER S,VITTITOW JASON L,DECAMP JONATHAN BRYAN,PELZ NICHOLAS F
- 优先权： US87055506 2006-12-18; US95821407 2007-12-17
- 主分类号： A61K31/505
- IPC分类号： A61K31/505 ; A61K31/47
摘要：
The present invention is directed to synthetic cytoskeletal active 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. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.
摘要（中）：
本发明涉及作为ρ相关蛋白激酶抑制剂的合成细胞骨架活性化合物。 本发明还涉及包含这些化合物和药学上可接受的载体的药物组合物。 本发明还涉及预防或治疗与细胞骨架重组有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，例如原发性开角型青光眼。 该方法包括向受试者施用治疗有效量的式I或式II的细胞骨架活性化合物，其中所述量有效影响肌动球蛋白相互作用，例如通过导致细胞松弛和细胞 - 基质粘连的改变。
IPC结构图谱:
| A | 人类生活必需 |
| --A61 | 医学或兽医学；卫生学 |
| ----A61K | 医用、牙科用或梳妆用的配制品 |
| ------A61K31/00 | 含有机有效成分的医药配制品 |
| --------A61K31/33 | .杂环化合物 |
| ----------A61K31/335 | ..仅有氧作为环杂原子的，例如制霉色基素 |
| ------------A61K31/40 | ...有仅以1个氮作为环杂原子的五元环的，例如舒必利、琥珀酰亚胺、托尔米丁、甲氧吡丁苯 |
| --------------A61K31/505 | ....嘧啶；氢化嘧啶，例如甲氧苄啶 |