| 摘要 |
<p>Aza-heterocycle compounds (I) and their salts, derivatives and/or stereoisomers, are new. Aza-heterocycle compounds of formula (I) and their salts, derivatives and/or stereoisomers, are new. R 1> : H, A, Ar, Ar-A or A-Ar; A : cyclic 1-14C alkyl (where one or two CH 2-group is replaced by O- or S- atom and/or NH, NA, CONH, NHCO or -CH=CH-, 1-7 H-atom is replaced by hal, and/or one or two CH 3 group is replaced by NH 2, NAH, NA 2, NHCOOA, NHCONHA, NHCONHAr or CN); Ar : one or two aromatic homo- or heterocyclic group with 1-4 N-, O- and/or S atoms and 5-10 scaffolding atoms, optionally substituted by carbonyloxide, hal, A, OH, OA, NH 2, NHA, NA 2, NO 2, CN, OCN, SCN, COOH, COOA, CONH 2, CONHA, CONA 2, NHCOA, NHCONH 2, NHSO 2A, CHO, COA, SO 2NH 2 and/or S(O) gA; Ar-A : aryl-alkyl; A-Ar : alkyl-aryl; hal : F, Cl, Br or I; X, Z : CH or N; Y 1> : CH 2 or saturated bond; R-2a, R-2b, R-2c, R-2d : H, hal, OH, CN, NH 2, 1-6C alkyl, where CH 2 is replaced by O or S and/or NH, NA, CONH, NHCO or -CH=CH and/or 1-4 H atoms is replaced by hal, and CH 3 is replaced by NH 2, NAH, NA 2, CN or Ar; R 3> : H, A or Ar-A; dotted line with solid line : single or a double bond; and g : 0-2. Where: one group of X is N then the other two groups of X is CH; and up to two group (preferably 0 or 1) of Z is NH. Independent claims are included for: (1) the preparation of (I); (2) a medicament comprising (I) and at least a further medically active agent; and (3) a kit comprising (I) and the medicament. [Image] ACTIVITY : Cytostatic; Antiangiogenic; Antiarteriosclerotic; Antidiabetic; Ophthalmological; Antiinflammatory. MECHANISM OF ACTION : Tyrosine kinase inhibitor; Insulin like growth factor-1 receptor inhibitor. The ability of (I) to inhibit insulin like growth factor-1 receptor was tested using biological assays. The results showed that N-pyridin-3-yl-[2-(3,4,5-trimethoxy-phenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]-amine (Ia) exhibited an IC 50 value of 0.76 mu M.</p> |
