| 摘要 |
7-Azaindole derivatives (I) and their salts, tautomers or stereoisomers, including their mixtures in all ratios, are new. 7-Azaindole derivatives of formula (I) and their salts, tautomers or stereoisomers, including their mixtures in all ratios, are new. R : indazole-3-, -4- or -7-yl, imidazo[1,2-a]pyrimidin-3- or -5-yl, quinolin-4-, -5- or -8-yl, isoquinolin-1-, -4 - or -5-yl, 1H-pyrrolo [3,2-c]pyridine-3 -, -4- or -7-yl, 1H-pyrrolo[2,3-c] pyridine-3-, -4- or -7-yl, furo[2,3-c]pyridine-3-, -4- or -7- yl, furo[3,2-b]pyridine-3- or -7-yl, 2,6-naphthyridin-1-or-4-yl or amino-quinoline-4-, -5 - or -8-yl (all optionally mono- or di-substituted by R 5>-), 1,8-naphthyridin-4-yl (optionally substituted by R 5>at 7th position) or 1,8-naphthyridin-4-yl (optionally substituted by A, Hal, CN, -[C(R 6>) 2] n-Cyc, OR 6>, N(R 6>) 2, SO 2A Or SO 2Ar 1>); R 1> : H or A1a; R 2> : H, A1a or -[C(R 6>) 2] n-Ar 1>; R 3> : H, A, Hal, CN, -[C(R 6>) 2] n-Ar 1>, -[C(R 6>) 2] n-Het, -[C(R 6>) 2] n-Cyc, OR 6>or N(R 6>) 2; R 5> : A, Hal, CN, -[C(R 6>) 2] n-Ar 1>, -[C(R 6>) 2] n-Het, -[C(R 6>) 2] n-Cyc, OR 6>. N(R 6>) 2, SO 2A or SO 2Ar 1>; R 6> : H or A1a; A : 1-6C-alkyl (where one or two CH 2groups are optionally replaced by O, N, S and/or -CH=CH, and 1-7 H atoms are replaced by F); A1a : 1-4C-alkyl; Cyc : 3-7C-cycloalkyl; Ar 1> : phenyl (optionally substituted by 1-3 Hal, A, -[C(R 6>) 2] n-OR 6>, N(R 6>) 2, CN, COOR 6>, CON(R 6>) 2, NR 6>COA, NR 6>SO 2A, COR 6>, SO 2N(R 6>) 2and/or S(O) nA); Het : optionally saturated mono-or bicyclic aryl heterocycle with 1-4 N, O and/or S (optionally mono- or di-substituted by Hal, A, -[C(R 6>) 2] nOR 6>, N(R 6>) 2, NO 2, CN, COOR 6>, CON(R 6>) 2, NR 6>COA, NR 6>SO 2A, COR 6>, SO 2NR 6>and/or S(O) n), preferably furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyrimidinyl, triazolyl, tetrazolyl, thiadiazolyl, pyridazinyl or pyrazinyl (optionally substituted by 1 or 2 A); Hal : F, Cl, Br or I; and n : 0-2. Independent claims are included for: (1) the preparation of (I); and (2) the use of (I) for treating tumor, tumor growth, tumor metastasis and/or AIDS. [Image] ACTIVITY : Cytostatic; Anti-HIV; Antiinflammatory; Vasotropic; Neuroprotective; Nootropic; Antiarteriosclerotic; Antiarthritic; Osteopathic; Vulnerary. MECHANISM OF ACTION : 3-Phosphoinositide-dependent kinase 1 inhibitor; IkappaB kinase-epsilon inhibitor; Transforming growth factor-beta inhibitor; Serine/threonine-protein kinase 1 inhibitor. The ability of (I) to inhibit Transforming growth factor-beta was tested using in vitro. The results showed that 5-(1H-pyrrolo[2,3-b]pyridin-3-yl)-isoquinoline exhibited an IC 5 0value of 0.5 nm to 1 mu M. |
