AMINE DERIVATIVES AND THEIR USE FOR TREATMENT OF OPHTHALMOLOGICAL DISEASES AND ILLNESSES Russian patent published in 2014 - IPC A61K31/135 C07C215/28 C07C215/38 C07C211/27 C07C211/28 C07C217/74 C07C237/20 C07D335/02 C07D213/38 C07D333/06 C07D309/04 A61K31/137 A61K31/138 A61K31/165 A61P27/02 

Abstract RU 2536040 C2

FIELD: biotechnologies.

SUBSTANCE: invention relates to new amine derivatives of the following structural formula:

(A),

which have properties of an inhibitor of isomerase activity of a retinoid cycle. In formula (A) Z represents -C(R9)(R10)-C(R1)(R2)- or -X-C(R31)(R32); X represents -O-, -S-, -S(=O)-, -S(=O)2- or -N(R30)-; G is chosen from -C(R41)2-C(R41)2-R40, -C(R42)2-S-R40, -C(R42)2-SO-R40, -C(R42)2-SO2-R40 or -C(R42)2-O-R40; R40 is chosen from -C(R16)(R17)(R18), C6-10aryl; each R6, R19, R34, R42 has been independently chosen from hydrogen or C1-C5alkyl; each R1 and R2 has been chosen independently from each other from hydrogen, halogen, C1-C5alkyl or -OR6; or R1 and R2 together form oxo; each R3, R4, R30, R31, R32, R41 represents hydrogen; each R9 and R10 has been chosen independently from each other from hydrogen, halogen, C1-C5alkyl or -OR19; or R9 and R10 form oxo; or possibly R9 and R1 together form a direct link to provide a double link; or possibly R9 and R1 together form a direct link and R10 and R2 together form a direct link to provide a triple link; n is equal to 0 or 1; values of radicals R11, R12, R16-R18, R23, R33 are given in the formula of the invention. The invention also relates to a pharmaceutical composition containing the above compounds, to application of compounds for production of a medicinal agent for treatment of a retinal ophthalmological disease, reduction of a lipofuscin pigment accumulated in an eye, for inhibition of dark adaptation of rod photoreceptor cell of retina, inhibition of regeneration of rhodopsin in the rod photoreceptor cell of retina or inhibition of degeneration of a retinal cell in retina.

EFFECT: improved properties of derivatives.

18 cl, 2 dwg, 17 tbl, 195 ex

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RU 2 536 040 C2

Authors

Skott Jen L.

Kuksa Vladimir A.

Orme Mark V.

Khong Feng

Litt Tomas L., Ml.

Kubota Re

Dates

2014-12-20Published

2008-10-22Filed