CARBOXYLIC ACIDS COMPOUNDS Russian patent published in 2017 - IPC C07D239/48 C07D239/47 C07D403/10 C07D403/12 A61K31/505 A61K31/506 A61P11/00 A61P35/00 A61P31/00 

FIELD: pharmacology.

SUBSTANCE: compounds may find use in the treatment of a disease mediated by TLR7. This disease can be a cancer selected from bladder cancer, head and neck cancers, prostate cancer, breast cancer, lung cancer, uterine cancer, pancreatic cancer, liver cancer, kidney cancer, ovarian cancer, colon cancer, stomach cancer, skin cancer, brain tumour, myeloma and lymphoproliferative tumours, such a disease or condition can also be represented by asthma, COPD (chronic obstructive pulmonary disease), allergic rhinitis, allergic conjunctivitis, allergic dermatitis, hepatitis B, hepatitis C, HIV, HPV (human papillomavirus), bacterial infection, or dermatosis. In the formula

,

n is equal to 0, 1 or 2; m is 1 or 2; p is 1, 2 or 3, provided that when X is oxygen, p is 2 or 3, and when X is a single bond, p is 1; X is oxygen or a single bond; R¹ is chosen from C_1-4 alkyl group, C_1-3alkyl-(CH₂)group, in which C_1-3 alkyl functional group is substituted by 1, 2 or 3 fluorine atoms, and C_1-4 an alkylcarbonyl group; R² is hydrogen; or R¹ and R² together with the nitrogen and carbon atoms to which they are attached form a saturated or unsaturated 5-membered heterocyclic ring optionally containing an additional heteroatom selected from N; R³ is selected from hydrogen, hydroxymethyl and 2-hydroxyethyl. The invention also relates to a method for preparation of a compound of formula (I) and to an intermediate of formula

wherein n, p, X, R¹, R² have the above values, Y is a hydroxy or substituted group selected from mesitylenesulfonyloxy, or tri(isopropyl)phenylsulfonyloxy; and PG¹ is a carboxylic acid protecting group selected from C_1-4 alkyl; or a salt thereof.

EFFECT: compound application efficiency increase.

37 cl, 13 dwg, 7 tbl, 30 ex