5,6-CONDENSED BICYCLIC COMPOUNDS AND COMPOSITIONS FOR TREATING PARASITIC DISEASES Russian patent published in 2020 - IPC C07D471/04 C07D487/04 C07D519/00 A61K31/437 A61P33/02 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I) and use thereof in preparing a medicinal agent for treating disorders or diseases selected from leishmaniasis, forms of Chagas disease and human African trypanosomiasis. In formula (I) ring A is phenyl or pyridinyl; R¹ is selected from (a) C_1-6alkyl, which is unsubstituted or substituted with 1–3 substituents, independently selected from halogen and C_3-6cycloalkyl; (b) C_1-4alkoxy which is unsubstituted or substituted with C_1-4haloalkyl; (c) -NR^5aR^5b, where R^5a and R^5b independently represent hydrogen, C_1-4alkyl or C_1-4haloalkyl or R^5a and R^5b together with the nitrogen atom to which they are both bonded, form 4–7 membered heterocycloalkyl containing 1–3 heteroatoms independently selected from N, O and S; (d) monocyclic C_3-6cycloalkyl, C_3-6cycloalkenyl or spiropentyl; each of which is unsubstituted or substituted with 1–3 substitutes independently selected from halogen, cyano, C_1-4alkyl, C_1-4haloalkyl and C_1-4alkoxy; (e) phenyl or 5–6-member heteroaryl containing 1–2 heteroatoms independently selected from N, O and S; each of which is unsubstituted or substituted with 1–2 substitutes independently selected from halogen, cyano, C_1-4alkyl, C_1-4haloalkyl, di-C_1-4alkylamino-C_1-4alkyl, C_1-4alkoxyC_1-4alkyl, C_1-4hydroxyalkyl, C_1-4alkoxy and C_3-6cycloalkyl; R² and R⁷ independently represent hydrogen or C_1-4alkyl; R³ denotes hydrogen or halogen and n equals 0 or 1; R⁴ is selected from (a) hydrogen; (b) halogen; (c) C_1-6haloalkyl or C_1-6alkyl, which is unsubstituted or substituted with C_3-6cycloalkyl; (d) -NR^6aR^6b, where R^6a is hydrogen or C_1-4alkyl; R^6b is hydrogen, C_1-4alkoxycarbonyl, C_1-4haloalkyl, C_3-6cycloalkyl or C_1-4alkyl, which is unsubstituted or substituted with C_1-4alkoxy; or R^6a and R^6b together with the nitrogen atom, to which they are both bonded, form 4–7 membered heterocycloalkyl containing 1–2 heteroatoms independently selected from N, O and S; (e) C_3-6cycloalkyl; (f) 4–6-member heterocycloalkyl containing 1–2 heteroatoms independently selected from N, O and S; wherein it is unsubstituted or substituted with -C(O)OR⁸, -C(O)R⁸, where R⁸ is C_1-4alkyl, and arilC_1-4alkyl which is unsubstituted or substituted by 1–2 substituents is halogen; and (g) 5–6-member heteroaryl containing 1–2 heteroatoms independently selected from N, O and S; which is unsubstituted or substituted with 1–2 substitutes independently selected from halogen, C_1-4alkyl, C_1-4hydroxyalkyl and C_3-6cycloalkyl. Invention also relates to specific compounds of formula (I).

EFFECT: treating disorders or diseases selected from leishmaniasis, forms of Chagas disease and human African trypanosomiasis.

18 cl, 4 tbl, 31 ex