COMPOUND WITH STING AGONISTIC ACTIVITY Russian patent published in 2023 - IPC C07D498/04 C07D513/04 A61K31/437 A61P31/00 A61P35/02 A61P37/00 

FIELD: pharmaceutical industry.

SUBSTANCE: problem solved by the invention is to provide a medicinal product containing as an active ingredient a compound having STING agonist activity. The invention relates to a compound of formula (I-1), a pharmaceutically acceptable salt or solvate thereof, having STING agonist activity. In this formula, X and Y are -CH= or a nitrogen atom (provided that X and Y are not simultaneously -CH=), Z is an oxygen atom or a sulfur atom, T is a nitrogen atom, ring A is 5–6 membered monocyclic aromatic heterocyclic ring containing 1 or 2 nitrogen atoms, ring B is a benzene ring, L¹ is a bond, -O-, -CONH-, -CO-, -CO₂ -, -S- , -SO₂ - or -SO-, L² is a bond, a C1-3 alkylene group, R¹ is a hydrogen atom, a halogen atom, a hydroxyl group, N(R^1a)₂ (wherein each of the two R^1a independently represents is a hydrogen atom or a C1-4 alkyl group), a C1-4 alkyl group, a carboxyl group, a C1-4 alkoxycarbonyl group, a C1-4 haloalkyl group, a methyl-d₃ group, R^2c is a hydrogen atom, a hydroxyl group, a nitro group, C1-4 alkoxy or NR^2dR^2e (where R^2d is a hydrogen atom, C1-4 alkyl group or R^FR, R^2e is a hydrogen atom), m is an integer 0 or 1, R³ is a hydrogen atom, a halogen atom, a hydroxyl group, or a C1-4 alkoxy group, n is an integer from 1 to 16, R^4a is a hydrogen atom or R^FR, R⁵ is a C1-4 alkyl group, p is an integer from 0 to 1, R^6a is a hydrogen atom, R⁷ is a hydrogen atom, b is the attachment position of the B ring, R^FR is -(CR^Fb₂)_q OP(=O)(OR^Fa)₂ [wherein each R^Fa is independently a hydrogen atom, a C1-4 alkyl group, R^Fb is a hydrogen atom or a methyl group, q is the integer 1 or 2 (where the groups represented by R^Fb may be the same or different)], provided that two or more of R^2d and R^4a do not simultaneously represent R^FR].

EFFECT: invention also relates to a pharmaceutically acceptable alkali metal salt of a compound of formula (I-1), a hydrate thereof, a pharmaceutical composition having STING agonist activity, comprising a compound of general formula (I-1) and a pharmaceutically acceptable carrier, a developmental suppressant drug, recurrence and/or treatment of cancer associated with STING agonist activity.

30 cl, 3 dwg, 1 tbl, 17 ex