| 摘要 |
<p>Benzazepine stereoisomeric compounds (I) are new. Benzazepine stereoisomeric compounds of formula (I) are new. R1>, R5>H or 1-5C alkyl; R2>substituent with +I or +M-effect; R3>, R4>H, 1-5C alkyl or halo; R6>OH, OR11> or O-(CO)R11>; R11>OH or 1-10C alkyl; R7>1-5C (fluoro)alkyl or 3-7C cycloalkyl; R8>halo or 1-10C alkyl (optionally substituted by OR12>, SR12>, N(R12>R13>) or 1-3 halo); R12>, R13>H, 1-5C alkyl or (CO)-1-5C-alkyl; R9>, R10>H, halo or 1-5C alkyl (substituted by OR11>, SR11>, N (R12>R13>) or CN); or CR9>+R10>3-6 cycloalkyl (optionally subsituted by OH, halo, or 1-5C cyanoalkyl); X : NH or N; and dotted line : single or double bond. An independent claim is also included for the preparation of (I). [Image] ACTIVITY : Antiinflammatory; Respiratory-Gen.; Antiarthritic; Dermatological; Cytostatic; Anabolic; Hypertensive; Ophthalmological; Hepatotropic; Vulnerary. MECHANISM OF ACTION : Glucocorticoid mimetic receptor inhibitor. The ability of (I) to inhibit glucocorticoid receptor was tested using biological assay. The result showed that IC50 value of 4,5-difluoro-7a,8,9,10-tetrahydro-2,10,10,12-tetramethyl-8-(trifluoromethyl)-7H-benzo[ef]quinazoline[5,4-bc][1]benzazepin-8,11-diol (Ib) was 91 Nm.</p> |
