Patent AR-057765-A1 (AR)
Title: 2-(6-oxo-6,7-dihidro -5h- benzo(2,3)-azepino(4,5-b)indol-5 il)-acetamidas n-substituidas y composiciones farmaceuticas
Inventor: SCHINZER DIETER
Filed: 2006-08-22
Abstract: Estos compuestos son utiles como agentes farmacéuticamente activos, especialmente para la profilaxis y/o el tratamiento de tripanosomiasis Sudamericana, tripanosomiasis Africana, enfermedad del sueno, Kala-Azar, leischmaniasis visceral, enfermedad Bagdad boil o Aleppo boil, leishmaniasis cutánea (CL), espundia, enfermedad de Chagas, leischmaniasis mucocutánea (MCL), tricomoniasis, tricomonosis urogenital, giardiasis, disentería lamblia, amebiasis, meningoencefalitis amébica primaria (PAM), queratitis o meningitis, coccidiosis, sarcosporidosis, toxoplasmosis, Malaria tropical Malaria tertiana, Malaria quartana, neumocistis carinil, neumonía, neumocistosis, disentería por Balantidium y llaga oriental. Además, la presente se dirige hacia composiciones farmacéuticas que contienen al menos una de las 2-(6-oxo-6,7- dihidro-5H-benzo[2,3]azepino[4,5-b]indol-5-il)-acetamidas N-sustituidas y/o sales farmacéuticamente aceptables de las mismas. Reivindicacion 1: Compuestos, caracterizados porque tienen la formula general (1), donde: R1-R8, R81, R82 representan, independientemente entre sí, -R11, -R12, -R13, -R14, -R15, -R16, -R17, -R18, -CH2-R19, -CH2-R20, -CH2-R21, -CH2-R22, -CHR23R24, -CHR25R26,-CHR27R28, - CHR29R30, -CR31R32R33, - CR34R35R36, -CH2-CH2-R37, -CH2-CH2-R38, -CH2-CH-R39R40, -CH2-CH-R41R42, -CR43R44-CR45R46R47, - CR48R49-CR50R51R52, -(CH2)s-R65, -(CH2)t-R66, -CR53R54-CR55R56-CR57R58R59, -CR60R61-CR62R63-CR64R65R66, -(CH2)q- CR60R61-(CH2)rR64, o -H; R', R'' y R10 representan, independientemente entre sí, -H, -CPh3, -CH3, -C2H5, -C3H7, -ciclo-C3H7, -CH(CH3)2, - C4H9, -CH2-CH(CH3)2, -CH(CH3)-C2H5, -C(CH3)3, -C5H11, -C6H13, -C7H15, -C8H17, -C9H19, -C10H21, -Ph, -CH2-Ph, -CH=CH2, -CH2-CH=CH2, -C(CH3)=CH2, -CH=CH- CH3, -C2H4-CH=CH2, -CH=C(CH3)2, -CsCH, -CsC-CH3, -CH2-CsCH; R11-R66 representan, independientemente entre sí, -H, -OH, -OCH3, -OC2H5, -OC3H7, -O-ciclo-C3H5, -OCH(CH3)2, -OC(CH3)3, -OC4H9, -OPh, -OCH2-Ph, -OCPh3, -SH, -SCH3, -SC2H5, -SC3H7, -S-ciclo- C3H5, -SCH(CH3)2, -NO2, -F, -Cl, -Br, -I, -N3, -CN, -OCN, -NCO, -SCN, -NCS, -CHO, -COCH3, -COC2H5, -COC3H7, -CO-ciclo-C3H5, - COCH(CH3)2, -COC(CH3)3, -COOH, -COCN, -COOCH3, -COOC2H5, -COOC3H7, -COO-ciclo-C3H5, -COOCH(CH3)2, -COOC(CH3)3, -OOC-CH3, - OOC-C2H5, -OOC-C3H7, -OOC-ciclo-C3H5, -OOC-CH(CH3)2, -OOC(CH3)3, -CONH2, -CONHCH3, -CONHC2H5, -CONHC3H7, -CONH-ciclo-C3H5, - CONH[CH(CH3)2], -CONH[C(CH3)3], -CON(CH3)2, -CON(C2H5)2, -CON(C3H7)2, -CON(ciclo-C3H5)2, -CON[CH(CH3)2]2, -CON[C(CH3)3]2, - NH2, -NHCH3, -NHC2H5, -NHC3H7, -NH-ciclo-C3H5, -NHCH(CH3)2, -NHC(CH3)3, -N(CH3)2, -N(C2H5)2, -N(C3H7)2, -N(ciclo-C3H5)2, -N[CH(CH3)2]2, - N[C(CH3)3]2, -SOCH3, -SOC2H5, -SOC3H7, -SO-ciclo-C3H5, -SOCH(CH3)2, -SOC(CH3)3, -SO2CH3, -SO2C2H5, -SO2C3H7, - SO2-ciclo-C3H5, - SO2CH(CH3)2, -SO2C(CH3)3, -SO3CH3, -SO3C2H5, -SO3C3H7, -SO3-ciclo-C3H5, -SO3CH(CH3)2, -SO3C(CH3)3, -OCF3, -OC2F5, -O-COOCH3, - O-COOC2H5, -O-COOC3H7, -O-COO-ciclo-C3H5, -O-COOCH(CH3)2, -O-COOC(CH3)3, -NH-CO-NH2, -NH-CO-NHCH3, -NH-CO- NHC2H5, -NH-CO- NHC3H7, -NH-CO-NH-ciclo-C3H5, -NH-CO-NH[CH(CH3)2], NH-CO-NH[C(CH3)3], -NH-CO-N(CH3)2, -NH-CO-N(C2H5)2, -NH-CO-N(C3H7)2, -NH-CO- N(ciclo-C3H5)2, -NH-CON[CH(CH3)2]2, -NH-CO-N[C(CH3)3]2, -NH-CS-NH2, -NH-CS-NHCH3, -NH-CS-NHC2H5, -NH-CS- NHC3H7, -NH-CS-NH- ciclo-C3H5, -NH-CS-NH[CH(CH3)2], -NH-CS-NH[C(CH3)3], -NH-CS-N(CH3)2, -NH-CS-N(C2H5)2, -NH-CS-N(C3H7)2, -NH-CS-N(ciclo-C3H5)2, -NH- CS-N[CH(CH3)2]2, -NH-CS-N[C(CH3)3]2, -NH-C(=NH)-NH2, -O-CO-NH2, -O-CONHCH3, -O-CONHC2H5, -O-CONHC3H7, -O-CONH-ciclo-C3H5, -O- CONH[CH(CH3)2], -O-CONH[C(CH3)3], -O-CON(CH3)2, -O-CON(C2H5)2, -O-CON(C3H7)2, -O-CON(ciclo-C3H5)2, -O-CON[CH(CH3)2]2, -O- CON[C(CH3)3]2, -CH2F,-CF2H, -CF3, -CH2Cl, -CHCl2, -CCl3, -CH2Br, -CHBr2, -CBr3, -CPh3, -CH2-CH2F, -CH2- CHF2, -CH2-CF3, -CH2-CH2Cl, - CH2-CHCl2, -CH2-CCl3, -CH2-CH2Br, -CH2-CHBr2, -CH2-CBr3, -CH3, -C2H5, -C3H7, -ciclo-C3H5, -CH(CH3)2, -C(CH3)3, -C4H9, -CH2-CH(CH3)2, - CH(CH3)-C2H5, -C5H11, -C6H13, -C7H15, -C8H17, -C9H19, -C10H21, -Ph, -CH2-Ph, -CH=CH2, - CH2-CH=CH2, -CH(CH3)=CH2, -CH=CH-CH3, - C2H4-CH=CH2, -CH=C(CH3)2, -CsCH, -CsC-CH3, -CH2-CsCH; -CH2-CH2S-CH3, -CH2-OH, -CH(OH)-CH3, -CH2-NH2, -CH2-CO-NH2, -CH2-CH2- CO-NH2, -CH2-SH, -(CH2)3-NH-C(=NH)NH2, -(CH2)4-NH2, -CH2-COOH, -CH2-CH2-COOH; NR81R82 también puede representar un resto seleccionado del grupo de formulas (2); q, r, s, t son, independiente entre sí, enteros de 0-10; y las formas estereoisoméricas, prodrogas, solvatos, hidratos y/o sales farmacéuticamente aceptables de los mismos.