BICYCLIC PYRAZOLON INHIBITORS OF CYTOKINES Russian patent published in 2009 - IPC C07D487/04 A61K31/4162 A61P29/00 A61P35/00 

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 "ФНО-α" and "ИЛ-1β" 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) -NR^4aR^4b; R³ is substituted or unsubstituted with phenyl, in which substitutes are chosen from halogen, C₁-C₄ alkyl; one of R^4a and R^4b is a independently a hydrogen atom; and the other of R^4a and R^4b is b) -[C(R^5aR^5b)]_mR⁶; R^5a and R^5b 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 C_1-6alkyl, 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