Adenosine Derivatives with an acetylene Group in position 4 ', with Adenosine A1 receptor agonist activity

摘要

6. Pure amine compound replaced by formula (1),Where X represents or CH2; R1 represents: (I) cycloquilo (c3-9) - (Alq) N-O cycloquenio (c3-9) - (Alq) n -,the cycloalkyl or cycloalkenyl group being optionally substituted by one or more substituents selected from OH, halogen, C1-6 alkyl, -C1-6alkoxy, alkenyloxy, C2-6 C2-6 alkynyloxy and phenyl, where (alq) represents C1-alkyl -3 and n represents 0 or 1, and the group (alq) can optionally be substituted by the C3-6 cycloalkyl group; (ii) a phenyl group optionally substituted by one or more substituents selected from: halogen, CF3, cyano, -C1-6alkyl, -C2-6alkyl, -C2-6alkynyl-,Alcoxi C1-6---Oh c1-6-co2h and CO2 tar C1-6; III non periodic C4-7 group containing at least one heteroatom selected from O, n or s, optionally replaced by one or more alternatives selected from oh-c1-6-tar,-Alcoxic C1-6, - co2quil C1-4, - coal quil C1-4, - coa2arilo cycloquil (C3-6) - CO2 (Alq) n, wherein (Alq) represents c1-3 tar and N represents 0 or 1; (IV) a group of C1-12 straight chain tar or branches, optionally replaced by one or more selected phenyl, halogen, hydroxy and cyclopropyl-7. The carbon of C1-12 tar group can be replaced by s (= O) n (n is 0, 1 or 2) and N group;(v) A bicyclic aromatic compound (2) ring, in which a represents C4-6 ring or phenyl, B represents phenyl, is replaced by c1-3 tar, and the bicyclic aromatic compounds are connected to the pure-6-amine part by a ring atom; R2 represents a group of c1-3 tar, halogen, hydrogen or alcoxi c1-3; R3 and R4 independently represent a mixture of H or C1-6; or a pharmaceutically acceptable and / or dissolved salt. Also published: the pharmaceutical ingredients that contain these substances,This substance is used in the production of drugs for the treatment of patients, in which case it is advantageous to reduce the concentration of plasma free fatty acids or to reduce the heart rate and the treatment of patients.