CN1233188A - 含Rho激酶抑制剂的药物制剂 - Google Patents
含Rho激酶抑制剂的药物制剂 Download PDFInfo
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- CN1233188A CN1233188A CN97198738A CN97198738A CN1233188A CN 1233188 A CN1233188 A CN 1233188A CN 97198738 A CN97198738 A CN 97198738A CN 97198738 A CN97198738 A CN 97198738A CN 1233188 A CN1233188 A CN 1233188A
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Abstract
Description
被测化合物 | 抑制率(%) |
化合物 109.2HCl (1μM)(10μM) | 81100 |
化合物 165.2HCl.3/2H2O (10μM) | 100 |
化合物 80.2HCl.H2O (10μM) | 100 |
化合物 204.2HCl (10μM) | 93 |
被测化合物 | IC50(μM) |
化合物 80.2HCl.H2O | 1.5 |
化合物 109.2HCl | 0.11 |
化合物 143.2HCl.H2O | 1.6 |
化合物 204.2HCl | 3.8 |
化合物 308.2HCl | 5.0 |
被测化合物 | IC50(μM) | |
p160ROCK | ROCK-Ⅱ | |
化合物 80.2HCl.H2O | 0.63 | 0.56 |
化合物 109.2HCl | 0.095 | 0.048 |
化合物 143.2HCl.H2O | 0.88 | 0.47 |
化合物 204.2HCl | 2.3 | 1.1 |
被测化合物 | 血管舒张作用(μM) | 气管舒张作用(μM) |
化合物 80.2HCl.H2O | 0.70 | 0.56 |
化合物 109.2HCl | 0.1 | 0.043 |
化合物 165.2HCl.3/2H2O | 0.051 | 0.066 |
化合物 179.2HBr.1/2H2O | 0.03 | 0.029 |
被测化合物 | 皮肤血流增加±标准误差(%) |
化合物 80.2HCl.H2O (1μg) | 135.0±13.4 |
化合物 157.HCl.H2O (1μg) | 211.6±13.6 |
化合物 165.2HCl.3/2H2O(0.03μg)(0.1μg) | 135.8±0.0144.7±0.0 |
化合物 166.2HCl.H2O (0.3μg)(1μg) | 143.2±25.4165.9±42.5 |
被测化合物 | 浓度 (μM) | 粘着诱导抑制率(%) |
化合物 80.2HCl.H2O | 100 | 70 |
化合物 109.2HCl | 100 | 67 |
化合物 143.2HCl.H2O | 100 | 77 |
化合物 165.2HCl.3/2H2O | 10 | 40 |
化合物 204.2HCl | 100 | 82 |
抗-β1抗体 | 20μg/ml | 118 |
IgG1 | 20μg/ml | -25 |
被测化合物 | 骨吸收抑制率%(μM) | 小鼠同源性MLR抑制活性IC50(μM) |
化合物 80.2HCl.H2O | 40.9(100) | 9.6 |
化合物 109.2HCl | 42.6(100) | 1.6 |
化合物 112.2HCl | 75.7(100) | 4.4 |
化合物 110.2HCl.H2O | 74.0(100) | 1.1 |
化合物 142.2HCl.H2O | 44.2(100) | |
化合物 143.2HCl.H2O | 39.4(100) | |
化合物 308.2HCl | 13.9 |
被测化合物 | 细胞生长抑制率IC50(μM) |
化合物 115.2HBr.1/4H2O | 9 |
化合物 109.2HCl | 58 |
化合物 142.2HCl.H2O | 59 |
化合物 145.2HCl.H2O | 62 |
被测化合物 | 管腔数 (10μM) |
化合物 109.2HCl | 153% |
化合物 80.2HCl.H2O | 174% |
化合物 110.2HCl.H2O | 203% |
化合物 165.2HCl.3/2H2O | 222% |
化合物 204.2HCl | 133% |
被测化合物 | IC50(μM) |
化合物 153.2HCl | 27 |
化合物 157.2HCl.H2O | 55 |
化合物 165.2HCl.3/2H2O | 38 |
化合物 163.2HBr | 63 |
Claims (66)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP212409/96 | 1996-08-12 | ||
JP21240996 | 1996-08-12 |
Publications (2)
Publication Number | Publication Date |
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CN1233188A true CN1233188A (zh) | 1999-10-27 |
CN100389828C CN100389828C (zh) | 2008-05-28 |
Family
ID=16622116
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNB971987386A Expired - Lifetime CN100389828C (zh) | 1996-08-12 | 1997-08-08 | 含Rho激酶抑制剂的药物制剂 |
Country Status (26)
Country | Link |
---|---|
US (3) | US6218410B1 (zh) |
EP (1) | EP0956865B2 (zh) |
JP (1) | JP3669711B2 (zh) |
KR (2) | KR100576148B1 (zh) |
CN (1) | CN100389828C (zh) |
AT (1) | ATE359822T1 (zh) |
AU (1) | AU738620B2 (zh) |
BG (4) | BG63991B1 (zh) |
BR (1) | BR9711154A (zh) |
CA (1) | CA2263425C (zh) |
CZ (1) | CZ301044B6 (zh) |
DE (1) | DE69737631T3 (zh) |
DK (1) | DK0956865T4 (zh) |
EE (1) | EE9900050A (zh) |
ES (1) | ES2286834T5 (zh) |
HK (1) | HK1022436A1 (zh) |
HU (1) | HU229864B1 (zh) |
IL (1) | IL128456A0 (zh) |
IS (1) | IS4973A (zh) |
NO (1) | NO990622L (zh) |
NZ (2) | NZ513800A (zh) |
PL (1) | PL331561A1 (zh) |
PT (1) | PT956865E (zh) |
RU (3) | RU2206321C2 (zh) |
SI (1) | SI0956865T2 (zh) |
WO (1) | WO1998006433A1 (zh) |
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CN102188697B (zh) * | 2010-03-03 | 2014-11-05 | 中国医学科学院药物研究所 | 重组人Rho激酶在制备药物中的应用 |
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