SKOTT Jen L. (US),СКОТТ Йен Л. (US),KUKSA Vladimir A. (US),КУКСА Владимир А. (US),ORME Mark V. (US),ОРМЕ Марк В. (US),LITTL Tomas (US),ЛИТТЛ Томас (US),GEhLL Anna (US),ГЭЛЛ Анна (US),KhONG Feng (US),Х,SKOTT JEN L.,СКОТТ Йен Л.,KUKSA VLADIMIR A.,КУКСА Владимир А.,ORME MARK V.,ОРМЕ Марк В.,LITTL TOMAS,ЛИТТЛ Томас,GEHLL ANNA,ГЭЛЛ Анна,KHONG FENG,ХОНГ Фенг
申请号：
RU2010117740/04
公开号：
RU0002541430C2
申请日:
2008.10.03
申请国别(地区):
RU
年份:
2015
代理人:
摘要：
FIELD: medicine, pharmaceutics.SUBSTANCE: claimed invention relates to novel compounds of general formula (A), their stereoisomers or pharmaceutically acceptable salts, possessing ability to inhibit activity of isomerase, taking part in visual cycle. Compounds can be applied for treatment of ophthalmological disease or disorder, such as age-related macular degeneration or Stargardt's macular dystrophy. In general formula (A) Z represents-C(R9)(R10)-C(R1)(R2)-； R1 and R2 each, independently on each other, are selected from hydrogen, halogen, C1-C5alkyl, or -OR6； or R1 and R2 together from oxo； R3 and R4 each, independently on each other, are selected from hydrogen； R6 is selected from a) C5-C15alkyl, optionally substituted with hydroxy, C1-C8alkoxy； or b) C5-C10carbocyclylalkyl, in which carbocycle is 4-, 5-, 6-, 7- or 8-member non-aromatic carbocycle, optionally substituted with hydroxy, halogen or R6CO2-； R9 and R10 each, independently on each other, is selected from hydrogen, halogen, C1-C5alkyl, optionally substituted with hydroxy, or -OR19； or R9 and R10 form oxo； or optionally, R9 and R1 together form direct bond to provide double bond； or optionally, R9 and R1 together form direct bond, and R10 and R2 together form direct bond to provide triple bond； R11 and R12 each, independently on each other, is selected from hydrogen, -C(=O)R23 or -C(NH)NH2, R23 is selected from C1-C8alkyl； R6, R19 and R34 are independently on each other are hydrogen or C1-C8alkyl； each R33 is independently selected from halogen, hydroxyl, C1-C5carboalkoxy, C1-C8alkyl, optionally substituted with hydroxy； and n equals 0 or 1.EFFECT: compounds inhibit degeneration of retinal cell, in particular neuronal cell, such as photoreceptor cell, in patient's retina.45 cl, 11 dwg, 11 tbl, 206 exНастоящее изобретение относится к новым соединениям общей Формулы (А), их стереоизомерам или фармацевтически приемлемым солям, обладающим способностью ингибировать активность изомеразы, участвующей в зрите
