FIELD: medicine.
SUBSTANCE: invention relates to a compound of the formula (I) in free form having activity as inducers of scleraxis, a tenomodulin gene and/or type I collagen (Col1a2), a pharmaceutical composition based on them and their use in the preparation of a drug for the treatment of tendon and/or ligament injury that are susceptible to the induction of scleraxis, the tenomodulin gene and/or type I collagen (Col1a2). In the general formula (I), R1 is selected from C1-C3alkyl and halogen; R2 is selected from NHSO2(CH2)nR3 or SO2NR5R6; n is 0 or 1; R3 is selected from phenyl optionally substituted once or twice with R4; C3-C6cycloalkyl optionally substituted with hydroxyl; a condensed 12-element bicyclic aromatic ring system; R4 is independently selected from halogen, C1-C3alkoxy, cyano, C1-C3alkyl, hydroxyl, halogenC1-C3alkyl, NHC(O)CH3, halogenC1-C3alkoxy, SO2NH(CH3); and/or two R4 with adjacent carbon atoms form 5- or 6-element heterocyclic non-aromatic ring containing one or two heteroatoms selected from N and O, while the specified heterocyclic ring is condensed with phenyl ring and is optionally substituted with C(O)CH3; R5 is selected from H, C1-C3alkyl; R6 is selected from C3-C6cycloalkyl optionally substituted once or twice with R7; phenyl optionally substituted once or twice with halogen; C1-C6alkyl optionally substituted with hydroxyl; 4-6-element heterocyclic non-aromatic ring containing one heteroatom, which is S, optionally substituted twice with oxo; benzyl; R7 is independently selected from hydroxyl, halogenC1-C3alkyl, halogen, C1-C3alkyl, hydroxyC1-C3alkyl; or R5 and R6 together with N atom, to which they are attached, form 5- or 6-element heterocyclic non-aromatic ring optionally containing one additional heteroatom, which is N, while the specified ring is optionally substituted once, twice or thrice with R8; 6-8-element saturated bicyclic ring system; R8 is independently selected from halogen; hydroxyC1-C3alkyl; C(O)NH2; hydroxyl; halogenC1-C3alkyl optionally substituted with hydroxyl; phenoxy; SO2C1-C3alkyl.
EFFECT: preparation of a drug for the treatment of tendon and/or ligament injury.
(I)
16 cl, 3 tbl, 1 dwg, 97 ex
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