发明申请
WO2003029187A1 QUATERNARY AMMONIUM SALTS OF OMEGA-AMINOALKYLAMIDES OF R-2-ARYL-PROPIONIC ACIDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
审中-公开
基本信息:
- 专利标题： QUATERNARY AMMONIUM SALTS OF OMEGA-AMINOALKYLAMIDES OF R-2-ARYL-PROPIONIC ACIDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
- 专利标题（中）：R-2-ARYL-PROPIONIC酸和含有它们的药物组合物的OMEGA-氨基甲酰胺的季铵盐
- 申请号：PCT/EP2002/010746 申请日：2002-09-25
- 公开(公告)号：WO2003029187A1 公开(公告)日：2003-04-10
- 发明人： ALLEGRETTI, Marcello , BERTINI, Riccardo , BIZZARRI, Cinzia , CESTA, Maria, Candida
- 申请人： DOMPE S.P.A. , ALLEGRETTI, Marcello , BERTINI, Riccardo , BIZZARRI, Cinzia , CESTA, Maria, Candida
- 申请人地址： Via Campo di Pile, I-67100 L'Aquila IT
- 专利权人： DOMPE S.P.A.,ALLEGRETTI, Marcello,BERTINI, Riccardo,BIZZARRI, Cinzia,CESTA, Maria, Candida
- 当前专利权人： DOMPE S.P.A.,ALLEGRETTI, Marcello,BERTINI, Riccardo,BIZZARRI, Cinzia,CESTA, Maria, Candida
- 当前专利权人地址： Via Campo di Pile, I-67100 L'Aquila IT
- 代理机构： PIERACCIOLI, Daniele
- 优先权： ITMI2001A002025 20010928
- 主分类号： C07C233/40
- IPC分类号： C07C233/40
摘要：
(R)-Enantiomers of quaternary ammonium salts of general formula (I) are described: (I) where R, R 1 , R 2 , R 3 , X and Z are as defined in the description. The process for their preparation and pharmaceutical preparations thereof are also described. The quaternary salts of the invention are useful in the inhibition of chemotaxis of neutrophils and monocytes induced by the fraction C5a of the complement and are used in the treatment of psoriasis, pemphigus and pemphigoid, rheumatoid arthritis, intestinal chronic inflammatory pathologies including ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, cystic fibrosis, chronic obstructive pulmonary disease and glomerulonephritis. The compounds of the invention are advantageously used in the prevention and the treatment of injury caused by ischemia and reperfusion.
摘要（中）：
（I）的季铵盐的对映异构体描述为：（I）其中R，R 1，R 2，R 3，X和Z如说明书中所定义。 还描述了其制备方法及其制备药物。 本发明的季盐可用于抑制由补体的级分C5a诱导的嗜中性粒细胞和单核细胞的趋化性，并用于治疗牛皮癣，天疱疮和类天疱疮，类风湿性关节炎，肠道慢性炎性病理包括溃疡性结肠炎，急性 呼吸窘迫综合征，特发性纤维化，囊性纤维化，慢性阻塞性肺病和肾小球性肾炎。 本发明的化合物有利地用于预防和治疗由缺血和再灌注引起的损伤。
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07C | 无环或碳环化合物 |
| ------C07C233/00 | 羧酸酰胺 |
| --------C07C233/01 | .羧酰胺基的碳原子连接在氢原子或非环碳原子上 |
| ----------C07C233/02 | ..羧酰胺基的氮原子连接在氢原子或未取代烃基碳原子上 |
| ------------C07C233/35 | ...有由非环碳原子连接在羧酰胺基的氮原子上的取代烃基 |
| --------------C07C233/40 | ....羧酰胺基的碳原子连接在含有六元芳环的碳架的非环碳原子上 |