Aminobenzoic acid derivatives

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 235/24 (2006.01) A61K 31/196 (2006.01) A61K 31/216 (2006.01) A61K 31/44 (2006.01) A61P 43/00 (2006.01) C07C 235/38 (2006.01) C07C 317/50 (2006.01) C07C 323/63 (2006.01) C07D 213/80 (2006.01)

Patent

CA 2376553

Aminobenzoic acid derivatives represented by general formula (1) or pharmaceutically acceptable salts thereof which are usable as VEGF receptor antagonists, in particular, remedies for diseases in which VEGF participates wherein R1 represents hydrogen, C1-6 alkyl, etc.; R2 represents hydrogen, C1-6 alkyl, etc.; R3 represents C8-25 alkyl, etc.; R4 represents hydrogen, OR9 or CO2R10 (wherein R9 and R10 represent each hydrogen or C1-6 alkyl); A represents S(O)qR15 [wherein q is 0, 1 or 2; and R15 represents C1-6 alkyl, phenyl (C1-3 alkyl) or (CH2)mOR16 (wherein m is 2 or 3; and R16 represents hydrogen or methoxymethyl)], etc.; X represents O, a single bond, CH=CH or NR27 (wherein R27 represents hydrogen or t-butoxycarbonyl); Y represents O, CONH, NHCO or NR28 (wherein R28 represents hydrogen or t-butoxycarbonyl); and n is an integer of from 0 to 15.

L'invention concerne des dérivés d'acide aminobenzoïque ou leurs sels acceptables sur le plan pharmaceutique, qui sont utilisables en tant qu'antagonistes de récepteurs de VEGF, et en particulier des remèdes à des maladies auxquelles participent le VEGF. Lesdits dérivés ou sels sont représentés par la formule générale (1), dans laquelle R?1¿ est hydrogène, alkyle C¿1-6?, etc. ; R?2¿ est hydrogène, alkyle C¿1-6?, etc. ; R?3¿ est alkyle C¿8-25?, etc. ; R?4¿ est hydrogène, OR?9¿ ou CO¿2?R?10¿ (où R?9¿ et R?10¿ sont chacun hydrogène ou alkyle C¿1-6?) ; A est S(O)¿q?R?15¿ [où q est 0, 1 ou 2; et R?15¿ est alkyle C¿1-6?, phényl(alkyle C¿1-3?) ou (CH¿2?)¿m?OR?16¿ (où m est 2 ou 3 ; et R?16 ¿est hydrogène ou méthoxyméthyle)], etc. ; X est O, une seule liaison, CH=CH ou NR?27¿ (où R?27¿ est hydrogène ou t-butoxycarbonyle) ; Y est O, CONH, NHCO ou NR?28¿ (où R?28¿ est hydrogène ou t- butoxycarbonyle) ; et n est un nombre entier compris entre 0 et 15.

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