Cinnoline compounds

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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Details

C544S235000

Reexamination Certificate

active

06887874

ABSTRACT:
The invention relatest to compounds of the formula (I) wherein either any one of G1, G2, G3, G4and G5is nitrogen and the other four are —CH—, or G1, G2, G3, G4and G5are all —CH—; Z is —O—, —NH—, —S—, —CH2— or a direct bond; Z is linked to any one of G1, G2, G3and G4which is a free carbon atom; n is an integer from 0 to 5; any of the substitutents R1may be attached at any free carbon atom of the indole, azaindole or indazole group; m is an integer from 0 to 3; Rarepresents hydrogen; Rbrepresents hydrogen or another value as defined herein; R1represents hydrogen, oxo, hydroxy, halogeno, C1-4alkyl, C1-4alkoxy, C1-4alkoxy, C1-4-alkyl, aminoC1-4alkyl, C1-3alkylaminoC1-4alkyl, di(C1-3alkyl)aminoC1-4alkyl, —C1-5alkyl(ring B) wherein ring B is selected from azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, N-methylpiperazinly, N-ethylpiperazinyl, morpholino and thiomorpholino; R2represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3aklylsulphanyl, —NR3R4(wherein R3and R4, which may be the same or different, each represents hydrogen or C1-3alkyl), or R5X1— (wherein R5and X1are as defined herein) and salts thereof, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and the use of a compound of formula I in the manufacture of medicament for the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

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