| 摘要 |
FIELD: chemistry. ^ SUBSTANCE: present invention relates to 6,7-dihydro-5H-pyrazolo[1,2a]pyrazol-1-ones with general formula (I), including all their enantiomeric and diastereomeric forms, as well as their pharmaceutically used salts, which inhibit undesirable or excessive excretion of cells of phlogistic cytokines, chosen from "ñ-" and "ÿ-1" and can be used for treating congestive heart failure, for example. In formula (I): R is: a) -O[CH2]kR3, where k=0; or b) -NR4aR4b; R3 is substituted or unsubstituted with phenyl, in which substitutes are chosen from halogen, C1-C4 alkyl; one of R4a and R4b is a independently a hydrogen atom; and the other of R4a and R4b is b) -[C(R5aR5b)]mR6; R5a and R5b each is independently a hydrogen atom, straight, or branched alkyl C1-C4, R6 is substituted or unsubstituted with alkyl C1-C4, in which substitutes are chosen from -OR7, cyano, phenyl, 6-member saturated heterocycle, containing a heteroatom in form of nitrogen, unsubstituted 5-6-member heteroaryl, containing 1-2 heteroatoms, chosen from nitrogen and oxygen; group R7 is a hydrogen atom, water soluble cation, alkyl C1-C4, index m assumes values from 0 to 5; R1 is: a) unsubstituted or substituted by 1-2 substitutes, chosen from halogen or C1-6alkyl, phenyl; L is a bridge group, chosen from: 1) -[C(R12)2]n-, where each R12 denotes hydrogen or together with two R12 groups form a carbonyl group, n= 1-2 ; 2) -[C(R12)2]nNR12[C(R12)2]n-, chosen from -[CH2]nNHC(O)- group, where n=1-2; and 3)-[C(R12)2]nO[C(R12)2]n-, where n=0; each R2 fragment is independently chosen from hydrogen; Z is O. ^ EFFECT: agents are highly effective. ^ 24 cl, 4 dwg, 10 tbl, 4 ex |
