CO4600676A1

CO4600676A1 - DERIVATIVES OF BENZOCICLOALQUILAZOLETIONA

Info

Publication number: CO4600676A1
Application number: CO95017120A
Authority: CO
Inventors: Gregory Ricardo Martinez; David Bruce Repke; Philip Jay Teitelbaum; Adrian Murray Walker Keith; Will Gooding Owen; Roger Lewis Whiting; Premnath Bansal Rekha; Alexander Victor Muehldorf; Yang Counde O
Original assignee: Syntex Inc
Priority date: 1994-04-26
Filing date: 1995-04-25
Publication date: 1998-05-08

Abstract

Un compuesto de Fórmula I o un precursor de éste:en la cual:n toma valores de 0, 1 o 2; t toma valores de 0, 1, 2 o 3;R1 se selecciona independientemente de un conjunto conformado por halo, hidroxi, o un alquiloxi (C1-4 ); yR2 se encuentra ligado en la posición -a-, ß, o ?-, el cual corresponde a un grupo sustituyente seleccionado de un conjunto conformado por las Fórmulas (a), (b), y (c);en las cuales:R4 es hidro, R3 es hidro o -(CH2 )q R9 {en donde q toma valores de 0, 1, 2, 3 o 4, y R9 es carboxi, alquiloxicarbonil (C1-4 ), carbamoil o un grupo seleccionado entre aril o heteroaril (grupo que bien puede opcionalmente ir sustituido con uno o dos sustituyentes independientemente seleccionados de un conjunto conformado por: hidroxi, alquiloxi (C1-4 ), ciano, 1 -tetrazol-5-il, carboxi, alquiloxicarbonil (C1-4 )]; R5 es hidro o -NHR10 {en donde R10 es hidro, alcanoil (C1-4 ), trifluoro alcanoil (C1-4 ), carbamoil, alquiloxicarbonil (C1-4 ), alquilcarbamoil (C1-4 ), di-alquilcarbamoil (C1-4 ), aminoalcanoil (C1-4 ), alquilamino (C1-4 )-alcanoil (C1-4 ), dialquilamino (C1-4 )-alcanoil (C1-4 ), un grupo seleccionado entre aril o heteroaroil (en donde dichos grupos aroil o heteroaril van opcional y adicionalmente sustituidos con uno a dos sustituyentes independientemente seleccionados entre hidroxi alquiloxi (C1-4 ), ciano, 1H-tetrazol-5-il, carboxi, alquiloxicarbonil (C1-4 ) o -C(NR11 )NHR12 (en donde R11 y R12 son independientemente hidro, acetil o -butoxicarbonil)}; o el caso en donde R4 y R5 son ambos hidro, y R3 es -NHR10 (en donde R10 corresponde a lo definido anteriormente); o el caso en que R5 es hidro, R3 es hidro o (CH2 )q R9 (en donde q y R9 corresponden a lo definido anteriormente) y R4 es alquil (C1-4 ),...A compound of Formula I or a precursor thereof: in which: n takes values of 0, 1 or 2; t takes values of 0, 1, 2 or 3, R1 is independently selected from a group consisting of halo, hydroxy, or a (C1-4) alkyloxy; yR2 is linked at the -a-, ß, or? - position, which corresponds to a substituent group selected from a set consisting of Formulas (a), (b), and (c); in which: R4 is hydro, R3 is hydro or - (CH2) q R9 {where q takes values of 0, 1, 2, 3 or 4, and R9 is carboxy, (C1-4) alkyloxycarbonyl, carbamoyl or a group selected from aryl or heteroaryl (group that may optionally be substituted by one or two substituents independently selected from a group consisting of: hydroxy, (C1-4) alkyloxy, cyano, 1-tetrazol-5-yl, carboxy, (C1-4) alkyloxycarbonyl] ; R5 is hydro or -NHR10 {where R10 is hydro, (C1-4) alkanoyl, trifluoro (C1-4) alkanoyl, carbamoyl, (C1-4) alkyloxycarbonyl, (C1-4) alkylcarbamoyl, di (C1-4) alkylcarbamoyl -4), (C1-4) aminoalkanoyl, (C1-4) alkylamino (C1-4) alkanoyl, (C1-4) dialkylamino-(C1-4) alkanoyl, a group selected from aryl or heteroaroyl (wherein said aroil or heteroaryl groups are optional and additional substituted by one to two substituents independently selected from hydroxy (C1-4) alkyloxy, cyano, 1H-tetrazol-5-yl, carboxy, (C1-4) alkyloxycarbonyl or -C (NR11) NHR12 (where R11 and R12 are independently hydro, acetyl or -butoxycarbonyl)}; or the case where R4 and R5 are both hydro, and R3 is -NHR10 (where R10 corresponds to that defined above); or the case where R5 is hydro, R3 is hydro or (CH2) q R9 (where q and R9 correspond to what is defined above) and R4 is (C1-4) alkyl, ...