| 摘要 |
Use of 1, 2, 3 substituted indolizine derivatives (I) or their salts in the preparation of medicaments for the treatment of diseases related to the pathological choroid angiogenesis. - Use of 1, 2, 3 substituted indolizine derivatives of formula (I) or their salts in the preparation of medicament for the treatment of diseases related to the pathological choroid angiogenesis - R1 = OH, 1-5C alkoxy, carboxy, 2-6C alcoxycarbonyl, -NR5R6, -NH-SO2-Alk, -NH-SO2-Ph, -NH-CO-Ph, -N(Alk)-CO-Ph, -NH-CO-NH-Ph, -NH-CO-Alk, -NH-CO2-Alk, -O-(CH2)n-cAlk, -O-Alk-COOR7, -O-Alk-O-R8, -O-Alk-OH, -O-Alk-C(NH2):NOH, -O-Alk-NR5R6, -O-Alk-CN, -O-(CH2)n-Ph, -O-Alk-CO-NR5R6, -CO-NH-(CH2)m-COOR7 or -CO-NH-Alk; - Alk = 1-5C alkyl or 1-5C alkylene; - cAlk = 3-6C cycloalkyl; - R5, R6 = H, 1-5C alkyl or benzyl; - R7 = H or 1-5C alkyl; - R8 = 1-5C alkyl or -CO-Alk; - Ph = phenyl (optionally substituted by one or more of halo, 1-5C alkoxy, carboxy or 2-6C alkoxycarbonyl); - R2 = H, 1-5C alkyl, 1-5C haloalkyl comprising 3-5 halogen atoms, 3-6C cycloalkyl or phenyl optionally substituted by one or more halo, 1-5C alkoxy, carboxy or 2-6C alkoxycarbonyl; - A = -CO-, -SO- or -SO2-; - R9, R10 = H or 1-5C alkyl; - R11 = H or -Alk-COOR12; - R12 = H, 1-5C alkyl or benzyl; - HetN = heterocycle having 5 or 6 chains comprising at least one atom of N and optionally another heteroatom of N or O; either - R3, R4 = H, 1-5C alkoxy, NH2, carboxy, 2-6C alkoxycarbonyl, OH, NO2, hydroxyamino, -Alk-COOR7, -NR5R6, -NH-Alk-COOR7, -NH-COO-Alk, -N(R11)-SO2-Alk-NR9R10, -N(R11)-SO2-Alk, -N(R11)-Alk-NR5R6, -N(R11)-CO-Alk-NR9R10, -N(R11)-CO-Alk, -N(R11)-CO-CF3, -NH-Alk-HetN, -O-Alk-NR9R10, -O-Alk-CO-NR5R6 or -O-Alk-HetN; or - R3+R4 = an unsaturated heterocycle having 5-6 chains (when R3 is alkoxy, R4 is -O-Alk-NR9R10 or OH, and R1 does not represent an alkoxy); - m = 1-5; and - n = 0-5. - ACTIVITY - Antiangiogenic; Ophthalmological; Antiinflammatory; Vasotropic. - MECHANISM OF ACTION - Fibroblast growth factor inhibitor.
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