INDAZOLE COMPOUNDS FOR USE IN TENDON AND/OR LIGAMENT INJURIES Russian patent published in 2021 - IPC C07D231/56 C07D401/12 C07D403/12 C07D405/04 A61K31/416 A61K31/454 A61P19/04 

Abstract RU 2749547 C2

FIELD: biochemistry.

SUBSTANCE: invention relates to a compound of Formula (I) in free form, wherein R1 is selected from C1-C3alkyl, halogen and C1-C3alkoxy; R2 is independently selected from C1-C3alkyl and halogen; n is equal to 1 or 2; R3 is selected from H and C1-C3alkyl, and R4 is selected from C4-C6cycloalkyl, optionally substituted once or twice R5; and a 6-membered heterocyclic aromatic ring containing at least one heteroatom selected from O, optionally substituted with hydroxyl; at the same time R4 is other than 4-hydroxycyclohexyl; or R3 and R4 together with the N atom to which they are attached form a 4-, 5- or 6-membered heterocyclic non-aromatic ring, the said ring being substituted once or more than once with R6; R5 is independently selected from hydroxyl, halogenC1-C3alkyl, halogen, C1-C2alkyl, phenyl, benzyl, C3-C6cycloalkyl, cyano; and R6 is independently selected from halogen, hydroxyC1-C3alkyl, C(O)NH2, hydroxyl, C1-C3alkyl, cyano, halogenC1-C3alkyl. The invention also relates to a pharmaceutical composition having inducing activity against the scleraxis gene, tenomodulin gene and/or Type I collagen (Col1a2), based on the compound of Formula (I).

EFFECT: new compounds and a pharmaceutical composition based on them have been obtained, which can find application in medicine for the treatment of tendon and/or ligament injury.

(I)

16 cl, 4 dwg, 4 tbl, 94 ex

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RU 2 749 547 C2

Authors

Bursulaya, Badry

Fisch, Andreas

Lajiness, James Paul

Machauer, Rainer

Malekar, Swapnil

Petrassi, Hank Michael James

Ramazani, Farshad

Remond, Anne-Catherine

Ullrich, Thomas

Usselmann, Peggy

Vangrevelinghe, Eric

Dates

2021-06-15Published

2017-09-21Filed