Indole derivatives

Details Indole derivatives Indole derivatives

C - Chemistry, Metallurgy

07

D

C07D 217/24 (2006.01) C07D 217/06 (2006.01) C07D 405/06 (2006.01) C07D 409/06 (2006.01) C07D 471/04 (2006.01) C07D 491/056 (2006.01)

Patent

CA 2224047

An indole derivative represented by general formula (1), a pharmacologically acceptable salt thereof, and an immunosuppressant containing the same as an active ingredient, wherein R1 represents C1 to C5 alkyl, C4 to C7 cycloalkylalkyl, C5 to C7 cycloalkenylalkyl, C7 to C14 aralkyl, C4 or C5 transalkenyl, alkyl, C1 to C5 furanyl-2-ylalkyl, C1 to C5 thienyl-2-ylalkyl, vinyloxycarbonyl, trichloroethoxycarbonyl, benzyloxycarbonyl, C1 to C5 alkanoyl, C7 to C14 aralkylcarbonyl, 2-furoyl, thiophene-2-carbonyl, C4 to C7 cycloalkylcarbonyl, C3 to C8 alkenylcarbonyl or anisoyl; R2 represents hydrogen, C1 to C3 alkyl, benzyl or C1 to C5 alkanoyl; R3 represents hydrogen, fluorine, chlorine, bromine, nitro or C1 to C5 alkyl; R4 represents hydrogen, C1 to C5 alkyl, benzyl or phenyl; R5 represents hydrogen, hydroxy or C1 to C5 alkanoyloxy; and the general formula includes all of the (+), (-) and (~) forms.

Un dérivé indole représenté par la formule générale (1), un sel pharmacologiquement acceptable de ce dernier et un immunosuppresseur contenant ce dérivé comme ingrédient actif, où R1 représente un alkyle en C1-C5, un cycloalkylalkyle en C4-C7, un cycloalkénylalkyle en C5-C7, un aralkyle en C7-C14, un transalkényle en C4 ou C5, un alkyle, furanyl-2-ylalkyle en C1-C5, un thiényl-2-ylalkyle en C1-C5, un vinyloxycarbonyle, un trichloroéthoxycarbonyle, un benzyloxycarbonyle, un alcanoyle en C1-C5, un aralkyl en C7-C14-carbonyle, un 2-furoyle, un thiophène-2-carbonyle, un cycloalkyl en C4-C7-carbonyle, un alkényl en C3-C8-carbonyle ou un anisoyle; R2 représente un hydrogène, un alkyle en C1-C3, un benzyle ou un alcanoyle en C1-C5; R3 représente un hydrogène, un fluor, un chlore, un brome, un nitro ou un alkyle en C1-C5; R4 représente un hydrogène, un alkyle en C1-C5, un benzyle ou un phényle; R5 représente un hydrogène, un hydroxy ou un alcanoyloxy en C1-C5; et la formule générale comprend toutes les formes (+), (-) et (~).

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