PROLYL HYDROXYLASE INHIBITORS AND APPLICATION METHODS THEREOF Russian patent published in 2011 - IPC C07C235/60 C07C237/42 C07C255/57 C07D213/81 A61K31/44 A61P9/10 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula

, where R and R¹ independently denote a link selected from: i) hydrogen; ii) substituted or unsubstituted phenyl and iii) substituted or unsubstituted 5- or 6-member heteroaryl in which heteroatoms are selected from nitrogen, oxygen, sulphur or combinations thereof; said substitutes are selected from: i) C₁-C₄ linear, C₃-C₄ branched or C₃-C₄ cyclic alkyl; ii) C₁-C₄ linear, C₃-C₄ branched or C₃-C₄ cyclic alkoxy; iii) C₁-C₄ linear, C₃-C₄ branched or C₃-C₄ cyclic halogenalkyl; iv) halogen; v) -CN; vi) -NHC(O)R⁴ vii) -C(O)NR^5aR^5b; viii) 5- or 6-member heteroaryl in which heteroatoms are selected from nitrogen, oxygen, sulphur or combinations thereof; or ix) two substitutes may be taken together to form a condensed ring containing 5-7 atoms; R⁴ is C₁-C₄ linear, C₃-C₄ branched or C₃-C₄ cyclic alkyl; R^5a and R^5b each independently denotes: 1) hydrogen; ii) C₁-C₄ linear, C₃-C₄ branched or C₃-C₄ cyclic alkyl; or iii) R^5a and R^5b can be taken together to form a ring containing 3-7 atoms; R² is selected from: i) -OR⁶; or ii) -NR^7aR^7b; R⁶ is hydrogen or C₁-C₄ linear, C₃-C₄ branched or C₃-C₄ cyclic alkyl; R^7a and R^7b each independently denotes: i) hydrogen; ii) C₁-C₄ linear, C₃-C₄ branched or C₃-C₄ cyclic alkyl; or iii) R^7a and R^7b may be taken together to form a ring containing 3-7 atoms; R³ is hydrogen, methyl or ethyl; L is a binding link of formula -[C(R^8aR^8b)]_n -R^8a and R^8b each independently denotes hydrogen, methyl or ethyl; n ranges from 1 to 3; R⁹ is hydrogen or methyl; or pharmaceutically acceptable salt thereof; provided that R and R¹ both denote hydrogen. The invention also relates to compositions based on the described compounds for treating anaemia or assisting wound healing and use of said compounds to prepare a composition for treating anaemia or wounds.

EFFECT: novel compounds which are HIF-16 prolyl hydroxylase inhibitors are obtained.

14 cl, 18 ex, 15 tbl, 2 dwg