5-SUBSTITUTED QUINOLINE AND ISOQUINOLINE DERIVATIVES, A METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS ANTIPHLOGISTICS

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.