INDAZOLE DERIVATIVE, METHOD FOR PREPARATION AND PHARMACEUTICAL USE THEREOF Russian patent published in 2024 - IPC C07D401/06 C07D401/14 C07D405/14 C07D413/14 A61K31/4439 A61K31/4545 A61K31/5377 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I) or its tautomer, mesomer, racemate, enantiomer, diastereomer, or a mixture thereof, or a pharmaceutically acceptable salt thereof. In formula (I): G is N; Z is selected from a group consisting of a chemical bond, -O-(CH₂)_t- and -NR⁷-(CH₂)_t-; ring A is selected from the group consisting of C₃-C₆ cycloalkyl and 3–6-membered heterocyclyl containing one N heteroatom; R^a is selected from a group consisting of -CH₂CH=CHC(O)NR⁸R⁹, -C(O)CH=CR¹⁰R¹¹ and -C(O)C≡CR¹²; R^b is selected from a group consisting of a hydrogen atom and C₁-C₆ alkyl; each R¹ is identical or different and each is independently selected from the group consisting of a hydrogen atom, halogen, C₁-C₆ alkyl and C₁-C₆ haloalkyl; R² is C₁-C₆ haloalkyl; each R³ is identical or different and each is independently selected from a group consisting of a hydrogen atom, halogen, C₁-C₆ alkyl, C₁-C₆ haloalkyl, cyano, NR¹³C(O)R¹⁴, C(O)NR¹³R¹⁴, SO₂R¹⁵; each R⁴ is a hydrogen atom; R⁷ is a hydrogen atom; R⁸ and R⁹ are identical or different and each is independently selected from a group consisting of a hydrogen atom, C₁-C₆ alkyl, C₁-C₆ haloalkyl, C₃-C₆ cycloalkyl and 3–6-membered heterocyclyl containing one heteroatom O; or R⁸ and R⁹ together with the nitrogen atom to which they are attached form 3–8-membered heterocyclyl, where 3–8-membered heterocyclyl optionally contains, in addition to one nitrogen atom, one heteroatom selected from the group consisting of N and O, and 3–8 membered heterocyclyl is optionally substituted with one or more substitutes selected from the group consisting of C₁-C₆ alkyl, halogen, hydroxy, C₁-C₆ hydroxyalkyl; R¹⁰ and R¹¹ are identical or different and each is independently selected from the group consisting of a hydrogen atom, C₁-C₆ alkyl and C₁-C₆ haloalkyl; R¹² is selected from a group consisting of a hydrogen atom, C₁-C₆ alkyl and C₁-C₆ haloalkyl; R¹³ and R¹⁴ are identical or different and each is independently selected from the group consisting of a hydrogen atom, C₁-C₆ alkyl and C₁-C₆ haloalkyl; R¹⁵ is selected from a group consisting of a hydrogen atom, C₁-C₆ alkyl and C₁-C₆ haloalkyl; m is 0 or 1; n is 0, 1, 2 or 3; q is 0, 1, 2, 3, 4 or 5; s is 0, 1, 2 or 3; and t is 0, 1, 2, 3, 4, 5 or 6. Also disclosed is a compound of formula (IA), a method of producing compound (I) from a compound of formula (IA), a pharmaceutical composition and use of the compound of formula (I).

EFFECT: disclosed compound of formula (I) is an oestrogen receptor antagonist and can be used to produce an oestrogen receptor modulator for preventing and/or treating a disease or condition mediated or dependent on the oestrogen receptor, wherein the disease is particularly preferably breast cancer.

19 cl, 6 tbl, 49 ex