AR114354A2 - PYRIMIDINE DERIVATIVES - Google Patents

Abstract

Reivindicación 1: Un compuesto de fórmula (1), en donde cada uno de R⁰, R¹, R² y R³ es independientemente hidrógeno, alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈, cicloalquilo C₃₋₈, cicloalquilo C₃₋₈-alquilo C₁₋₈, aril C₅₋₁₀-alquilo C₁₋₈, hidroxialquilo C₁₋₈, alcoxi C₁₋₈-alquilo C₁₋₈, aminoalquilo C₁₋₈, haloalquilo C₁₋₈, arilo C₅₋₁₀ no sustituido o sustituido, heterociclilo de 5 ó 6 miembros no sustituido o sustituido que comprende 1, 2 ó 3 heteroátomos seleccionados de N, O y S, hidroxi, alcoxi C₁₋₈, hidroxialcoxi C₁₋₈, alcoxi C₁₋₈-alcoxi C₁₋₈, haloalcoxi C₁₋₈, aril C₅₋₁₀-alcoxi C₁₋₈ no sustituido o sustituido, heterocicliloxi no sustituido o sustituido, o heterociclilalcoxi C₁₋₈ no sustituido o sustituido, amino no sustituido o sustituido, alquiltio C₁₋₈, alquilsulfinilo C₁₋₈, alquilsulfonilo C₁₋₈, arilsulfonilo C₅₋₁₀, halógeno, carboxi, alcoxicarbonilo C₁₋₈, carbamoílo no sustituido o sustituido, sulfamoílo no sustituido o sustituido, ciano o nitro; o R⁰ y R¹, R¹ y R², y/o R² y R³ forman, junto con los átomos de carbono a los cuales están unidos, un anillo carbocíclico o heterocíclico de 5 ó 6 miembros que comprende 0, 1, 2 ó 3 heteroátomos seleccionados de N, O y S; R⁴ es hidrógeno o alquilo C₁₋₈; cada uno de R⁵ y R⁶ independientemente es hidrógeno, alquilo C₁₋₈, alcoxi C₁₋₈-alquilo C₁₋₈, haloalquilo C₁₋₈, alcoxi C₁₋₈, halógeno, carboxi, alcoxicarbonilo C₁₋₈, carbamoílo no sustituido o sustituido, ciano, o nitro; y cada uno de R⁷, R⁸, R⁹ y R¹⁰ independientemente es alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈, cicloalquilo C₃₋₈, cicloalquilo C₃₋₈-alquilo C₁₋₈, arilo C₅₋₁₀-alquilo C₁₋₈, hidroxialquilo C₁₋₈, alcoxi C₁₋₈-alquilo C₁₋₈, aminoalquilo C₁₋₈, haloalquilo C₁₋₈, arilo C₅₋₁₀ no sustituido o sustituido, heterociclilo de 5 ó 6 miembros no sustituido o sustituido que comprende 1, 2 ó 3 heteroátomos seleccionados de N, O y S, hidroxi, alcoxi C₁₋₈, hidroxialcoxi C₁₋₈, alcoxi C₁₋₈-alcoxi C₁₋₈, haloalcoxi C₁₋₈, arilo C₅₋₁₀-alcoxi C₁₋₈ no sustituido o sustituido, heterocicliloxi no sustituido o sustituido, o heterociclilalcoxi C₁₋₈ no sustituido o sustituido, amino no sustituido o sustituido, alquiltio C₁₋₈, alquilsulfinilo C₁₋₈, alquilsulfonilo C₁₋₈, arilsulfonilo C₅₋₁₀, halógeno, carboxi, alcoxicarbonilo C₁₋₈, carbamoílo no sustituido o sustituido, sulfamoílo no sustituido o sustituido, ciano o nitro; en donde R⁷, R⁸ y R⁹ independientemente entre sí también pueden ser hidrógeno; o R⁷ y R⁸, R⁸ y R⁹, y/o R⁹ y R¹⁰ forman junto con los átomos de carbono a los cuales están unidos, un anillo carbocíclico o heterocíclico de 5 ó 6 miembros que comprende 0, 1, 2 ó 3 heteroátomos seleccionados de N, O y S; A es C o N; y sus sales.Claim 1: A compound of formula (1), wherein each of R⁰, R¹, R² and R³ is independently hydrogen, C₁₋₈ alkyl, C₂₋₈ alkenyl, C₂₋₈ alkynyl, C₃₋₈ cycloalkyl, C₃₋ cycloalkyl ₈-C₁₋₈ alkyl, C₅₋₁₀ aryl-C₁₋₈ alkyl, C₁₋₈ hydroxyalkyl, C₁₋₈ alkoxy-C₁₋₈ alkyl, C₁₋₈ aminoalkyl, C₁₋₈ haloalkyl, unsubstituted or substituted C₅₋₁₀ aryl , unsubstituted or substituted 5- or 6-membered heterocyclyl comprising 1, 2, or 3 heteroatoms selected from N, O and S, hydroxy, C₁₋₈ alkoxy, C₁₋₈ hydroxyalkoxy, C alco alkoxy-C₁₋₈ alkoxy, haloalkoxy C₁₋₈, unsubstituted or substituted C₅₋₁₀ aryl-C₁₋₈ alkoxy, unsubstituted or substituted heterocyclyloxy, or unsubstituted or substituted C₁₋₈ heterocyclylalkoxy, unsubstituted or substituted amino, C₁₋₈ alkylthio, C₁₋₈ alkylsulfinyl, C₁₋₈ alkylsulfonyl, C₅₋₁₀ arylsulfonyl, halogen, carboxy, C₁₋₈ alkoxycarbonyl, unsubstituted or substituted carbamoyl, unsubstituted or substituted sulfamoyl, cyano or nitro; or R⁰ and R¹, R¹ and R², and / or R² and R³ form, together with the carbon atoms to which they are attached, a 5- or 6-membered carbocyclic or heterocyclic ring comprising 0, 1, 2, or 3 selected heteroatoms of N, O and S; R⁴ is hydrogen or C₁₋₈ alkyl; each of R⁵ and R⁶ independently is hydrogen, C alqu alkyl, C₁₋₈ alkoxy-C₁₋₈ alkyl, C₁₋₈ haloalkyl, C₁₋₈ alkoxy, halogen, carboxy, C₁₋₈ alkoxycarbonyl, unsubstituted or substituted carbamoyl, cyano, or nitro; and each of R⁷, R⁸, R⁹ and R cada independently is C₁₋₈ alkyl, C₂₋₈ alkenyl, C₂₋₈ alkynyl, C₃₋₈ cycloalkyl, C₃₋₈ cycloalkyl-C alqu alkyl, C₅₋₁₀ aryl-C alqu alkyl ₋₈, C₁₋₈ hydroxyalkyl, C₁₋₈ alkoxy-C₁₋₈ alkyl, C₁₋₈ aminoalkyl, C₁₋₈ haloalkyl, unsubstituted or substituted C₅₋₁₀ aryl, unsubstituted or substituted 5- or 6-membered heterocyclyl comprising 1 , 2 or 3 heteroatoms selected from N, O and S, hydroxy, C₁₋₈ alkoxy, C₁₋₈ hydroxyalkoxy, C₁₋₈ alkoxy-C₁₋₈ alkoxy, C₁₋₈ haloalkoxy, C₅₋₁₀ aryl-C₁₋₈ alkoxy no substituted or substituted, unsubstituted or substituted heterocyclyloxy, or unsubstituted or substituted C₁₋₈ heterocyclylalkoxy, unsubstituted or substituted amino, C₁₋₈ alkylthio, C₁₋₈ alkylsulfinyl, C₁₋₈ alkylsulfonyl, C₅₋₁₀ arylsulfonyl, halogen, carboxy, C₁₋₈ alkoxycarbonyl, unsubstituted or substituted carbamoyl, unsubstituted or substituted sulfamoyl, cyano or nitro; where R⁷, R⁸ and R⁹ independently of each other can also be hydrogen; or R⁷ and R⁸, R⁸ and R⁹, and / or R⁹ and R¹⁰ form, together with the carbon atoms to which they are attached, a 5- or 6-membered carbocyclic or heterocyclic ring comprising 0, 1, 2, or 3 heteroatoms selected from N, O and S; A is C or N; and its salts.