야로크, 스테판,레빈켈, 하르트무트,샤케, 하이케,슈미스, 노르베르트,스쿠발라, 베르네르,슈나이데르, 마티아스,휘브네르, 얀,페트로프, 올린,딘테르, 크리스티안
申请号：
KR1020077010785
公开号：
KR1011684620000B1
申请日:
2005.11.11
申请国别(地区):
KR
年份:
2012
代理人:
摘要：
5-Substituted quinoline and isoquinoline derivatives (A) and their racemates, individual stereoisomers, enantiomers, salts and prodrugs are new. 5-Substituted quinoline and isoquinoline derivatives (A) of formula (IIa) or (IIb) and their racemates, individual stereoisomers, enantiomers, salts and prodrugs are new. R 1>；, R 2>；H, 1-3C alkyl, halo, CN, 1-3C alkoxy or OH. An independent claim is also included for the preparation of (A). [Image] ACTIVITY : Antiinflammatory； Respiratory-Gen.； Antirheumatic； Immunosuppressive； Antiallergic； Vasotropic, Dermatological； Antipsoriatic； Antipruritic； Nephrotropic； Hepatotropic； Gastrointestinal-Gen.； Ophthalmological； Auditory； Neuroprotective； Antibacterial； Cytostatic； Endocrine-Gen.； Antithyroid； Analgesic； Antidiabetic； CNS-Gen.； Cardiovascular-Gen.； Antiemetic； Hemostatic. MECHANISM OF ACTION : Glucocorticoid receptor binder； Steroid hormone receptor binder； Androgen receptor binder； Mineralocorticoid receptor binder； Progesterone receptor binder； Cytokine secretion inhibitor. The ability of (A) to inhibit lipopolysaccharide induced cytokine interleukin-8 secretion was tested in human monocyte cell line THP-1. The results showed that the median inhibitory concentration of 5-[4-(5-fluoro-2,3-dihydrobenzofuran-7-yl)-2-hydroxy-4-methylI-2-trifluoromethylpentylamino]-2-methylquinoline (II') was 5.9 nM.화학식 IIa 또는 IIb의 화합물<；화학식 IIa>；<；화학식 IIb>；및 그들의 약제로서의 용도.
