HUMAN PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND APPLICATION METHODS THEREOF Russian patent published in 2011 - IPC C07D263/32 C07D277/28 C07D277/30 C07D277/42 C07D413/04 C07D413/12 C07D417/04 C07D417/12 C07D417/14 A61K31/422 A61K31/425 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of general formula where R denotes a thiazolyl group of formula R² and R³ are selected from: hydrogen, C₁-C₃linear alkyl; R⁴ is selected from: C₁-C₃linear or C₃cyclic alkyl, phenyl and thiophenyl; Z denotes a group of formula: -(L)_n-R¹; R¹ is selected from: i) C₁-C₃linear or branched alkyl, optionally substituted with C₁-C₄alkoxycarbonyl, halogen; ii) substituted phenyl or substituted with one or two substitutes selected from halogen, methoxy- or hydroxy group, C₁-C₄alkoxycarbonyl; iii) dioxopiperazinyl and 2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl, substituted with C₁-C₃alkyl; or iv) heteroaryl rings containing 5-10 atoms selected from thiazole, triazole, 1H-imidazole, thiadiazole, oxazole, isoxazole, oxadiazole, benzodioxole, benzo(1,4)dioxepanyl, pyridine, pyrimidine, 1H-indole, 2,3-dihydrobenzo[b][1,4]dioxynil, which can be substituted with oine or two substitutes selected from: a) hydroxy; b) C₁-C₃alkyl (which can be substituted with one more two substitutes selected from: ) phenyl; ii) C₁-C₄alkoxycarbonyl; iii) naphthalenyl; iv) 2-methylthiazolyl) ; c) NHC(O)C₁-C₃alkyl; d) C₁-C₄alkoxycarbonyl; e) 1 -(tert-butoxycarbonyl)-2-phenylethyl; f) methoxybenzyl; g) phenyl which can be substuted with C₁-C₄alkoxy, halogen, methoxycarbonyl or >NHC(O)CH₃; h) (methoxy-2-oxoethyl)carbamoyl; L denotes a group selected from: i) C(O)NH[C(R^5aR^5b)]_w-; ii) -C(O)[C(R^6aR^6b)]_x-; iii) -C(O)[C(R^7aR^7b)]_yC(O)-; iv) -SO₂[C(R^8aR^8b)]_z-; R^5a, R^5b, R^6a, R^6b, R^7a, R^7b, R^8a and R^8b, each independently denotes: i) hydrogen; ii) C₁-C₃ linear alkyl which can be substituted with 1 or 2 halogen atoms; iii) phenyl which can be substituted with 1-2 substitutes selected from halogen and lower alkoxy; iv) heteroaryl rings selected from imidazolyl, imidazolyl substituted with methyl, benzo(1,4)oxazinyl, oxadiazolyl substituted with methyl; index n equals 0 or 1; indices w, x, y and z are each independently equal to a number from 1 to 3. The invention also relates to pharmaceutically acceptable salts of compounds of formula (I) and use of compounds of formula (I) to prepare a medicinal agent for treating protein tyrosine phosphatase beta-mediated conditions.

EFFECT: obtaining compounds of formula (I) as human protein tyrosine phosphatase beta (HPTP-β) inhibitors.

15 cl, 17 dwg, 13 tbl, 16 ex