ALKYNYL-PHENYL DERIVATIVE COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS Russian patent published in 2012 - IPC C07C211/27 C07C211/28 C07C215/08 C07C215/30 C07C215/42 C07C215/46 A61P27/02 

FIELD: chemistry.

SUBSTANCE: invention relates to novel alkynyl-phenyl derivatives which are inhibitors of isomerase activity in the visual cycle in case of ophthalmic diseases or disorders. In formula (A): , m equals 0 or 1; Z is -C(R²³)(R²⁴)-C(R¹)(R²)- or -C(R²³)(R²⁴)-C(R²⁵)(R²⁶)-C(R¹)(R²)-; Y is a bond, -C(R²⁷)(R²⁸)- or -C(R²⁷)(R²⁸)-C(R²⁹)(R³⁰)-; R¹ and R² are each independently selected from hydrogen, C₁-C₅alkyl or-OR⁶; R²³ and R²⁴ are each independently selected from hydrogen, C₁-C₅alkyl or -OR⁶; or R²³ and R²⁴ together form oxo; or possibly, R²³ and R¹ located nearby together form a direct bond while enabling formation of a double bond; R²⁵ and R²⁶ are each independently selected from hydrogen, C₁-C₅alkyl or -OR⁶; R³ and R⁴ are each independently selected from hydrogen or C₁-C₅alkyl; each R⁶ is identical or different from each other and independently denotes hydrogen or C₁-C₅alkyl; and each R¹⁴ is identical or different from each other and independently denotes C₁-C₅alkyl, halogen or -OR⁶; R²⁷, R²⁸ and R²⁹ are each identical or different and independently denote hydrogen, C₁-C₅alkyl or -OR⁶; and R³⁰ independently denotes hydrogen or C₁-C₅alkyl; values of radicals R⁵, R⁹, R¹², R¹³ are given in the claim.

EFFECT: improved method.

14 cl, 14 dwg, 21 tbl, 200 ex