NITROXY GROUP-CONTAINING BENZYLAMINE DERIVATIVES AND THEIR USE FOR TREATING CARDIOVASCULAR DISEASES, AS WELL AS INCREASED INTRA-OCULAR PRESSURE,

摘要

The present invention relates to compounds of the general formula (I) and salts thereof.;(7);Wherein A1 is C_1-15Alkylene, C_5-7Of cycloalkylene or di-C_1-4Alkylene-C_5-7Cycloalkane; R1 is hydrogen, C_1-7Alkyl or C_3-8/RTI R2 is hydrogen, C_1-7Alkyl, C_3-8Or R 1 and R 2 are taken together with the nitrogen atom to form unsubstituted or substituted 5 RTI-, 6-or 7-membered heterocycle; A2 is C_1-15Alkylene, C_5-7Of cycloalkylene or di-C_1-4Alkylene-C_5-7Cycloalkane; Y is R3, NH₂, NH-R4 or S-R5, the-substituted picolide group is C_1-4Alkyl, C_1-4Alkoxy and hydroxy, the substituted piperidine group is substituted with one or two identical or different substituents selected from the group consisting of C_1-4Alkyl, C_1-4Alkoxy and hydroxy, the substituted piperazine group is substituted by one or more of the same or different substituents selected from the group consisting of C_1-4May be substituted at the 2-, 3-, 5-, or 6-position, and the 4-position may be substituted with C_1-4Alkyl, C_1-4Alkoxycarbonyl, C_1-4Phenyl substituted with R6, R7 and R8, phenyl-substituted with R6, R7 and R8 in the phenyl group_1-4-alkyl, benzoyl, picolinoyl, nicotinoyl, isonicotinoyl, optionally halogen or C RTI ID = 0.0 _1-4-alkyl substituted benzhydryl and the R4 group, the substituted morpholin group is substituted with one or two identical or different C_1-4Substituted homofiperazines are substituted with an alkyl group of C_1-4-alkyl, C_1-4-alkoxycarbonyl, C_1-4-alkylcarbonyl, phenyl substituted with R6, R7 and R8, phenyl-C-substituted with R6, R7 and R8 in the phenyl group_1-4-benzoyl substituted in the alkyl and phenyl group with R6, R7 and R8; R3 is furyl, naphthyl, tetrahydronaphthyl,-O-Al-ONO₂Substituted phenyl or phenyl substituted by R6, R7 and R8; R4 is C_1-7-alkyl /RTI or substituted-CH₂-CH (OH)-(CH₂O)_p-Ar; R5 is R6, R7 and R8 substituted phenyl, R6, R7 and R8 are substituted phenyl-C_1-4-alkyl, optionally halogen or C RTI ID = 0.0 _1-4Alkyl-substituted benzhydryl, dibenzo-C_5-7-cycloalkanyl, dibenzocycloheptenyl or benzo-pyrido-C_5-7-cycloalkanyl; R6 is hydrogen, C_1-4-alkyl, C_1-4-alkoxy, C_1-4-alkoxy, C_1-4-alkylcarbonyl, halogenamino, mono-or di-(C_1-4Alkyl) amino or nitro; R7 is hydrogen, C_1-4-alkyl, C_1-4-alkoxy, halogen or nitro; R 8 is hydrogen or trifluoromethyl; P is an integer of 0 or 1; Ar is a hydrocarbon ring system of fully or partially unsaturated monocyclic (containing 5 to 6 ring atoms) or bicyclic (containing 9 to 10 ring atoms) wherein 1, 2 or 3 carbon atoms contain nitrogen (N ), Oxygen (O) or sulfur (S) may be inserted, and C_1-4-alkyl, C_1-4-alkoxy, C_1-4-alkylthio, C_1-4Alkoxy-C_1-4-alkyl, C_1-4-alkoxy-C_1-4-alkoxy, C_3-4-alkenyl, C_3-4-alkenyloxy, C_3-8-cycloalkyl, C_5-10-cycloalkylalkoxyalkyl, C RTI ID = 0.0 _1-4-alkylcarbonyl, C_1-4-alkylcarbonylamino, carbamoyl, carbamoyl-C_1-4-alkyl, halogen, hydroxy, oxonitro, cyan C_1-4-alkylsulfonamido, amino, mono-or di-(C_1-4-alkyl) amino, ureido, mono-or di-(C_1-4-alkyl) ureido, mono-or di-(C_3-8-cycloalkyl) ureido, trifluoromethyl, fully or partially fluoro substituted C_1-4-alkoxy, C_1-4-alkoxycarbonyl, tetrahydrofurfuryloxy or morpholino, or a pharmaceutically acceptable salt thereof. These compounds are useful in the treatment of cardiovascular diseases and elevated intraocular pressure.