Resumen

Reduction of intraocular pressure involves the administration of indole derivatives. Reduction of intraocular pressure involves the administration of indole derivatives of formula (I) - (IV). n = 0 - 5, m = 0 or 1; R1 and R2 = A1, R6(CO)-, F, OR5 or R6R7N(CO)-; A1 = H, optionally substituted linear branched cyclo-alkyl, -alkenyl, -alkynyl, -aryl, -aralkyl, -aralkenyl, -aralkynyl; R1+R2 and R3+R4 = oxo or optionally substituted 4 - 7-membered carbocycle or heterocycle; R3 and R4 = A1 or R6(CO)-; R2+R4 = optionally substituted 4 - 7-membered carbocycle or heterocycle; A and B = T1; T1 = halo, NO2, CN or R5-X1; X1 = O, S, NR9, CF2, CH2, -CH2CH2, -CH2CH2CH2- or absent; R5 = A1, R6R7N(CO)-, R6(CO)-, R8O(CO)-, R8S(O)2-, R8S(O)-, R8OS(O)2-, R8OS(O)-, R6R7NS(O)2-, R6R7NP(O)(OR9)-, R8P(O)(OR9)-, (R8O)P(O)(OR9)- or CF3; R6 and R7 = A1 or heterocyclic ring; R6+R7 = NR6R7 representing optionally substituted ring of 3 - 7 member; R8 = optionally substituted linear, branched or cyclo-alkyl, -alkenyl, -alkynyl, -aryl, -aralkyl, -aralkenyl, -aralkynyl, heterocyclic ring or CF3; R9 = A1 or H; R6+R9 = 5 - 7 membered ring; E = A1, R8O(CO)-, R8S(O)2-, OR6, R6(CO)-, R6R7N(CO)- or H; D1 = T1; Z1 = OR5 or NR10R11; Z1+R1 = optionally substituted 4 - 7 membered heterocycle; R10 and R'10 = A1, heterocycle, R6R7N(CO)-, R6(CO)-, R8O(CO)-, R8S(O)2-, R8OS(O)2-, R6R7NS(O)2- or CF3; R11, Z2 and Z3 = NR6R7(CO)-, R6(CO)-, R8O(CO)-, R8S(O)2-, R8OS(O)2- or R6R7NS(O)2-; Z2-N-R10 and Z3-N-R10 = 4 - 7 membered ring; D1+R6 = ring; D2 = H, optionally substituted cyclo-alkyl, halo or optionally substituted phenyl or arylalkyl. Provided when E is either R6(CO) or R6R7N(CO)- then Z1 is NR10R11, (where R10 is H) or OR5, (where R5 is not H, alkyl, aryl or aralkyl); when B is in the 4-position of indole and is not equal to halo, NO2, CN or H, then B+R1, B+R3 or B+Z1 is optionally substituted 5 - 7 membered carbocyclic or heterocyclic ring; when B is not equal to halo, NO2, CN or H and is on the 7-position of indole then B+E is optionally substituted 5 - 7-membered heterocyclic ring; when D1 = R5-X1 then D1+E is optionally substituted 4 - 7 membered heterocyclic ring, D1+R1 and D1+R3 are optionally substituted 5 - 7 membered carbocyclic or heterocyclic ring, D1+Z1 is optionally substituted 5 - 7 membered heterocyclic ring; When n = 1, m = 0, R5 = CH3, X1 = O, B = D1 = E = R3 = R4 = H, then Z is other than -NHAc; when D1 and R6 are absent then the carbonyl participate in a ring bridging the two positions; when R5 = R6 = CH3 then D2 is not equal to H.