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Oxo Derivatives of 1 - 1, 2 - dihydro - isoqinolina, processes for their Preparation and Pharmaceutical compositions containing them

机译:1-1,2-二氢异秦基酮的含氧衍生物,其制备方法和含有它们的药物组合物

摘要

1. A compound of formula (I): where: R1 is selected from H, (C1-C6) alkyl, (C2-C6) alkenyl, (C3-C6) alkynyl, (CH2) aX-Ar and (CR101R102) aX-Ar, wherein said (C1-C6) alkyl is optionally substituted with 1, 2 or 3 groups independently selected from - (C1-C6) alkoxy, -halo, -OH, -heterocycloalkyl, (C3-C7) cycloalkyl and - NR8R9; R2 and R3 are independently selected from H, halo, (C1-C6) alkyl, (C1-C6) alkoxy and (CH2) dY; wherein said (C1-C6) alkyl is optionally substituted with 1, 2 or 3 groups independently selected from - (C1-C6) alkoxy, -halo and -OH; and where said (C1-C6) alkoxy is optionally substituted with 1,2 or 3 groups independently selected from -halo and -OH; and provided that when R2 is (CH2) d-Y, R3 is selected from H, halo, (C1-C6) alkyl and (C1-C6) alkoxy; and provided that when R3 is (CH2) d-Y, R2 is selected from H, halo, (C1-C6) alkyl and (C1-C6) alkoxy; R4 and R5 are independently selected from H, (C1-C6) alkyl, (C1-C6) alkoxy, halo, CF3 and CN; R16 is selected from H, (C1-C6) alkyl and heterocycloalkyl, wherein said (C1-C6) alkyl is optionally substituted with - (C1-C6) alkoxy, -OH, -halo, - (C3-C7) cycloalkyl and - NR25R26; R17 is selected from H and (C1-C6) alkyl;or R16 and R17 together with the nitrogen atom to which they are attached form a 3 to 7 member ring, optionally containing another heteroatom selected from NR27, S and O; and optionally containing, when possible, 1 or 2 double bonds; wherein said ring is optionally substituted on carbon with 1 or 2 substituents independently selected from - (C1-C6) alkyl, (C1-C6) alkoxy, (C2-C6) alkenyl, -OH, -CN, halo and -NR25R26, wherein said - (C1-C6) alkyl is optionally substituted with -OH. R25 and R26 are independently selected from H and (C1-C6) alkyl wherein said (C1-C6) alkyl is optionally substituted with - (C1-C6) alkoxy, -OH, -halo,-(C3-C7) cyclopentanediol and - nr22r23; or R25 and R26, together with the nitrogen atoms attached to them, form a ring of 3 to 7 members, optionally containing another heteromorphic atom selected from among Nr24, s and O;
机译:1.式(I)的化合物:其中:R 1选自H,(C 1 -C 6)烷基,(C 2 -C 6)烯基,(C 3 -C 6)炔基,(CH 2)aX-Ar和(CR101R102)aX -Ar,其中所述(C1-C6)烷基任选被1、2或3个独立地选自-(C1-C6)烷氧基,-卤代,-OH,-杂环烷基,(C3-C7)环烷基和-NR8R9的基团取代; R2和R3独立地选自H,卤素,(C1-C6)烷基,(C1-C6)烷氧基和(CH2)dY;其中所述(C1-C6)烷基任选被1、2或3个独立地选自-(C1-C6)烷氧基,-卤代和-OH的基团取代;所述(C1-C6)烷氧基任选地被1、2或3个独立地选自-卤代和-OH的基团取代;且当R 2为(CH 2)d-Y时,R 3选自H,卤素,(C 1 -C 6)烷基和(C 1 -C 6)烷氧基;且当R3为(CH2)d-Y时,R2选自H,卤素,(C1-C6)烷基和(C1-C6)烷氧基; R4和R5独立地选自H,(C1-C6)烷基,(C1-C6)烷氧基,卤素,CF3和CN; R16选自H,(C1-C6)烷基和杂环烷基,其中所述(C1-C6)烷基任选地被-(C1-C6)烷氧基,-OH,-卤代,-(C3-C7)环烷基和-取代。 NR25R26; R17选自H和(C1-C6)烷基;或R16和R17与它们所连接的氮原子一起形成3至7元环,任选地含有选自NR27,S和O的另一个杂原子;并在可能的情况下视情况包含1或2个双键;其中所述环在碳上任选被1或2个独立地选自-(C1-C6)烷基,(C1-C6)烷氧基,(C2-C6)烯基,-OH,-CN,卤素和-NR25R26的取代基取代,其中所述-(C 1 -C 6)烷基任选地被-OH取代。 R25和R26独立地选自H和(C1-C6)烷基,其中所述(C1-C6)烷基任选地被-(C1-C6)烷氧基,-OH,-卤代,-(C3-C7)环戊二醇和-取代。 nr22r23; R25和R26与与其相连的氮原子一起形成3至7元的环,该环任选地含有选自Nr24,s和O中的另一个杂晶原子。

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