| 摘要 |
FIELD: chemistry. ^ SUBSTANCE: invention relates to novel 4-amino-5-cyanopyrimidine derivatives of formula (1) or their pharmaceutically acceptable salts which have agonistic effect on the adenosine A2a receptor. In formula (1): R1 is a hydrogen atom, lower alkylcarbonyl, lower alkenylcarbonyl, phenylcarbonyl or lower alkoxycarbonyl; R2 is a lower alkylene; R3 is any of (1) hydrogen atom, (2) lower alkyl or any of the following groups (3)-(9): group (3) group (4) group (5) group (6). group (7) group (8) group (9) in which: R4 is lower alkylene, R5 is a hydrogen atom or lower alkyl, Z1 , Z2 and Z3 are selected from groups (a1)-(a38), (b1)-(b8) and (c1)-(c22) respectively, which are defined below: Z1: (a1) lower alkyl, (a2) phenyl-lower alkyl, (a3) aminophenyl-lower alkyl, (a4) phenyl-lower alkenyl, (a5) heteroaryl-lower alkyl, (a6) heteroaryl-lower alkenyl, (a7) heteroarylphenyl-lower alkyl, (a8) hydroxy-lower alkyl, (a10) amino-lower alkyl, (a11) aminocarbonyl-lower alkyl, (a12) lower alkylcarbonyl, (a13) lower alkoxy-lower alkylcarbonyl, (a14) amino-lower alkylcarbonyl, (a15) phenylcarbonyl, (a16) phenyl-lower alkylcarbonyl, (a17) phenyl-lower alkenylcarbonyl, (a18) phenoxy-lower alkylcarbonyl, (a19) heteroarylcarbonyl, (a20) heteroaryl-lower alkylcarbonyl, (a21) heteroaryl-lower alkenylcarbonyl, (a22) heteroaryloxy-lower alkylcarbonyl, (a23) heteroarylsulphanyl-lower alkylcarbonyl, (a24) heteroarylphenylcarbonyl, (a25) phenylsulphanyl-lower alkylcarbonyl, (a26) phenylcarbonyl-lower alkylcarbonyl, (a28) lower alkoxycarbonyl, (a29) lower alkylsulphonyl, (a30) phenylsulphonyl, (a31) heteroarylsulphonyl, (a32) hydrogen atom, (a33) lower alkyl containing a saturated heterocycle, (a34) carbonyl-lower alkyl containing a saturated heterocycle, (a35) phenyl-lower alkyl containing a saturated heterocycle, (a36) carbonyl containing a saturated heterocycle, (a37) lower alkylcarbonyl containing a saturated heterocycle, or (a38) phenylcarbonyl containing a saturated heterocycle. ^ EFFECT: obtained compounds have intraocular pressure reducing properties and can be used in treating ocular hypertension and glaucoma. ^ 9 cl, 112 dwg, 32 tbl, 416 ex |
