发明名称 AMINE DERIVATIVES AND THEIR USE FOR TREATMENT OF OPHTHALMOLOGICAL DISEASES AND ILLNESSES
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(R)(R)-C(R)(R)- or -X-C(R)(R); X represents -O-, -S-, -S(=O)-, -S(=O)- or -N(R)-; G is chosen from -C(R)-C(R)-R, -C(R)-S-R, -C(R)-SO-R, -C(R)-SO-Ror -C(R)-O-R; Ris chosen from -C(R)(R)(R), Caryl; each R, R, R, Rhas been independently chosen from hydrogen or C-Calkyl; each Rand Rhas been chosen independently from each other from hydrogen, halogen, C-Calkyl or -OR; or Rand Rtogether form oxo; each R, R, R, R, R, Rrepresents hydrogen; each Rand Rhas been chosen independently from each other from hydrogen, halogen, C-Calkyl or -OR; or Rand Rform oxo; or possibly Rand Rtogether form a direct link to provide a double link; or possibly Rand Rtogether form a direct link and Rand Rtogether form a direct link to provide a triple link; n is equal to 0 or 1; values of radicals R, R, R-R, R, Rare 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
申请公布号 RU2536040(C2) 申请公布日期 2014.12.20
申请号 RU20100122261 申请日期 2008.10.22
申请人 AKUSELA INK. 发明人 SKOTT JEN L.;KUKSA VLADIMIR A.;ORME MARK V.;KHONG FENG;LITT TOMAS L., ML.;KUBOTA RE
分类号 A61K31/135;A61K31/137;A61K31/138;A61K31/165;A61P27/02;C07C211/27;C07C211/28;C07C215/28;C07C215/38;C07C217/74;C07C237/20;C07D213/38;C07D309/04;C07D333/06;C07D335/02 主分类号 A61K31/135
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