SKOTT Jen L. (US),СКОТТ Йен Л. (US),KUKSA Vladimir A. (US),КУКСА Владимир А. (US),ORME Mark V. (US),ОРМЕ Марк В. (US),KhONG Feng (US),ХОНГ Фенг (US),LITT Tomas L., Ml. (US),ЛИТТ Томас Л., Мл. (US),KUB,SKOTT JEN L.,СКОТТ Йен Л.,KUKSA VLADIMIR A.,КУКСА Владимир А.,ORME MARK V.,ОРМЕ Марк В.,KHONG FENG,ХОНГ Фенг,LITT TOMAS L., ML.,ЛИТТ Томас Л., Мл.,KUBOTA RE,КУБОТА Рё
申请号:
RU2010122261/04
公开号:
RU0002536040C2
申请日:
2008.10.22
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
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 exИзобретение относится к новым аминопроизводным структурной формулы (А), обладающим свойствами ингибитора изомеразной активности ретиноидного цикла. В формуле (А) Z представляет собой -С(R9)(R10)-С(R1)(R2)- или -X-C(R31)(R32); Х представляет собой -O-, -S-, -S(=O)-