CN102917703A - 新型ep4激动剂 - Google Patents
新型ep4激动剂 Download PDFInfo
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- CN102917703A CN102917703A CN2011800130103A CN201180013010A CN102917703A CN 102917703 A CN102917703 A CN 102917703A CN 2011800130103 A CN2011800130103 A CN 2011800130103A CN 201180013010 A CN201180013010 A CN 201180013010A CN 102917703 A CN102917703 A CN 102917703A
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Abstract
Description
R1 | R2 | R3 | |
化合物 A | H | H | H |
化合物 B | H | H | Me |
化合物 C | H | H | Cl |
化合物 D | H | H | CF3 |
化合物 E | Me | H | H |
化合物 F | Me | H | Me |
化合物 G | Me | H | Cl |
化合物 H | Me | H | CF3 |
化合物 I | H | Me | H |
化合物 J | H | Me | Me |
化合物 K | H | Me | Cl |
化合物 L | H | Me | CF3 |
化合物 M | Me | Me | H |
化合物 N | Me | Me | Me |
化合物 O | Me | Me | Cl |
化合物 P | Me | Me | CF3 |
化合物 | 残留率 (%) |
化合物 F | 91.6±6.8 |
化合物 J | 90.1±6.9 |
化合物 F的羧酸体 | 27.8±2.2 |
化合物 J的羧酸体 | 44.1±2.1 |
试验化合物 | 剂量 | t1/2 (分钟) |
作为与异构体的混合物进行给药的化合物 F | 50 μg/kg (与异构体的混合物) | 115±31 |
作为与异构体的混合物进行给药的化合物 J | 50 μg/kg (与异构体的混合物) | 77±19 |
化合物 F | 300 μg/kg | 158±15 |
作为与异构体的混合物进行给药的化合物 F的羧酸体 | 50 μg/kg (与异构体的混合物) | 9.6±1.7 |
作为与异构体的混合物进行给药的化合物 J的羧酸体 | 50 μg/kg (与异构体的混合物) | 8.9±0.3 |
试验化合物 | IC50 (nmol/L) |
BPS | 36 |
化合物 F | 917 |
化合物 J | 2725 |
化合物 F的羧酸体 | 120 |
化合物 J的羧酸体 | 190 |
Claims (29)
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2010051127 | 2010-03-08 | ||
JP2010-051127 | 2010-03-08 | ||
JP2010-246208 | 2010-11-02 | ||
JP2010246208 | 2010-11-02 | ||
PCT/JP2011/055411 WO2011111714A1 (ja) | 2010-03-08 | 2011-03-08 | 新規なep4アゴニスト |
Publications (2)
Publication Number | Publication Date |
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CN102917703A true CN102917703A (zh) | 2013-02-06 |
CN102917703B CN102917703B (zh) | 2015-08-19 |
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CN201180013010.3A Active CN102917703B (zh) | 2010-03-08 | 2011-03-08 | 新型ep4激动剂 |
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EP (1) | EP2545917B1 (zh) |
JP (1) | JP5734952B2 (zh) |
KR (1) | KR101760970B1 (zh) |
CN (1) | CN102917703B (zh) |
AU (1) | AU2011225259B2 (zh) |
BR (1) | BR112012022632B1 (zh) |
CA (1) | CA2792403C (zh) |
DK (1) | DK2545917T3 (zh) |
ES (1) | ES2593229T3 (zh) |
HU (1) | HUE030206T2 (zh) |
MX (1) | MX2012010483A (zh) |
PL (1) | PL2545917T3 (zh) |
PT (1) | PT2545917T (zh) |
RU (1) | RU2564414C2 (zh) |
TW (1) | TWI555744B (zh) |
WO (1) | WO2011111714A1 (zh) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107286160A (zh) * | 2017-06-05 | 2017-10-24 | 毛佳婧 | 一种抗肝炎药物的哌啶并吡啶并吡唑‑锌配合物的制备方法 |
CN111278464A (zh) * | 2017-08-31 | 2020-06-12 | 柏林夏瑞蒂医科大学 | 用于防止妥协性患者中肌肉骨骼损伤愈合不良的免疫调节 |
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IN2015DN02814A (zh) * | 2012-10-26 | 2015-09-11 | Asahi Glass Co Ltd | |
JP7233087B2 (ja) * | 2019-03-18 | 2023-03-06 | 公立大学法人横浜市立大学 | 抗動脈硬化剤 |
HU231350B1 (hu) | 2019-12-18 | 2023-01-28 | CHINOIN Gyógyszer és Vegyészeti Termékek Gyára Zrt | Eljárás királis prosztaglandin-enol intermedier előállítására, és az eljárásban hasznos köztitermék vegyületek |
TW202400150A (zh) * | 2022-05-16 | 2024-01-01 | 日商Agc股份有限公司 | IL-6及/或IL-1β抑制劑 |
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107286160A (zh) * | 2017-06-05 | 2017-10-24 | 毛佳婧 | 一种抗肝炎药物的哌啶并吡啶并吡唑‑锌配合物的制备方法 |
CN111278464A (zh) * | 2017-08-31 | 2020-06-12 | 柏林夏瑞蒂医科大学 | 用于防止妥协性患者中肌肉骨骼损伤愈合不良的免疫调节 |
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JPWO2011111714A1 (ja) | 2013-06-27 |
WO2011111714A1 (ja) | 2011-09-15 |
AU2011225259A1 (en) | 2012-10-11 |
TWI555744B (zh) | 2016-11-01 |
PT2545917T (pt) | 2016-10-25 |
BR112012022632A2 (pt) | 2017-10-03 |
KR101760970B1 (ko) | 2017-07-24 |
CA2792403C (en) | 2018-06-12 |
CA2792403A1 (en) | 2011-09-15 |
DK2545917T3 (en) | 2016-11-14 |
ES2593229T3 (es) | 2016-12-07 |
MX2012010483A (es) | 2012-10-09 |
TW201139421A (en) | 2011-11-16 |
RU2564414C2 (ru) | 2015-09-27 |
AU2011225259B2 (en) | 2015-07-23 |
CN102917703B (zh) | 2015-08-19 |
EP2545917A1 (en) | 2013-01-16 |
PL2545917T3 (pl) | 2017-01-31 |
BR112012022632B1 (pt) | 2020-03-31 |
EP2545917A4 (en) | 2014-09-10 |
JP5734952B2 (ja) | 2015-06-17 |
KR20130018753A (ko) | 2013-02-25 |
HUE030206T2 (en) | 2017-04-28 |
RU2012142653A (ru) | 2014-04-20 |
EP2545917B1 (en) | 2016-08-03 |
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