| 摘要 |
<p>The present invention relates to a pharmaceutical composition comprising a compound of general formula (I),
wherein
- Z1 is S or O, preferably S;
- - Z2 - is -N R a -, wherein R a is H, OH, alkyl, alkoxy, aryle, alkenyl, alkynyl, amine, preferably R a is H; -N=; O; S; -C R b =, wherein R b is H, OH, alkyl, alkoxy, aryle, alkenyl, alkynyl, amine, NO 2 , Cl, Br, I, F, preferably H; -CH R c -, wherein R c is H, OH, alkyl, alkoxy, aryle, alkenyl, alkynyl, amine, NO 2 , Cl, Br, I, F, or -CH 2 -; preferably - Z2 - is -NH- or -N=;
- each of R1 and R2 is independently H, OH, alkyl, alkoxy, aryle, alkenyl, alkynyl, amine, NO 2 , Cl, Br, I, F; preferably R1 and R2 together and with N and Z2 form an heterocycle eventually substituted, more preferably a substituted azocine, 3H-indole, indazole, 2-imidazoline, 2-pyrazoline, benzthiazole, purine, pyrimidine, pyridine, pyridazine, pyrazine, pyrazole, thiazole, isothiazole, oxazole, isoxazole, quinoline, isoquinoline, quinoxaline, quinazoline, 1-8-naphthyridine, perimidine, [1,10]-phenantroline, phthalazine, pteridine, triazole, triazine, furazan, 6H-1,2,5-thiadiazine, 1,3,4-thiadiazole, tetrazole, or a substituted imidazole and even more preferably a benzimidazole;
- R5 is H, OH, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkenyl, C 1-4 alkynyl, amine, preferably R5 is NH 2 , NO 2 , Cl, F, Br, I; more preferably R5 is H or CH 3 ; even more preferably R5 is CH 3 ;
- each of R8 and R9 is independently, H, OH, alkyl, alkoxy, aryle, alkenyl, alkynyl, amine, NO 2 , Cl, Br, I, F; preferably R 8 and R 9 together form a cycle comprising 5 or 6 atoms, preferably an heterocycle comprising 5 or 6 atoms, more preferably a 1,3-dioxacyclopentene or a 1,4-dioxane; and
- each of R3, R4, R6, R7, R10 and R11 is independently, H, OH, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkenyl, C 1-4 alkynyl, amine, NO 2 , F, Cl, Br, I; preferably H, CH 3 , OCH 3 , OH, NH 2 , NO 2 , Cl, F, Br, I; more preferably is H or CH 3 ; even more preferably is H,
or esters or salts thereof; in association with at least one pharmaceutically acceptable vehicle; and to the use thereof for inhibiting the Neuropilin pathways in the treatment of cancer and of angiogenic diseases.</p> |
