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CYCLOSPORIN DERIVATIVES FOR TREATMENT OF EYE AND SKIN DISEASES AND CONDITIONS
专利权人:
Инк. (US);Аллерган
发明人:
ГАРСТ Майкл Е. (US)
申请号:
RU2011104584/15
公开号:
RU2011104584A
申请日:
2009.07.09
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
1. A method of treating a water-deficient dry eye, uveitis, or phacoanaphylactic endophthalmitis in the eye, or balanitis, psoriasis, or atopic dermatitis of the skin, wherein said method comprises the steps of topically administering to the eye or skin a therapeutically effective amount of a cyclosporin A derivative selected from the group consisting of compounds represented by the formula:! ! where R1 is S-Alk-R, where Alk is an alkylene or alkylenyl bond, R is —N = C (NR3R4) (NR5R6) or —NR7 [(NR3R4) C = NR5], i.e. guanidines or -N = C (R8) (NR9R10), i.e. amidines where R3-R10 represents H, Alk, Ar or (CH2) nAr, where Ar represents an aryl group, and n represents an integer from 1 to 13, or R3 and R4, or R4 and R5, or R5 and R7, or R3 and R7, or R9 and R10, or R8 and R9 together can be - (CH2) x-, where x is an integer from 2 to 5, and R2 is selected from the group consisting of hydroxyl, lower alkyl and hydroxyl substituted lower alkyl. ! 2. The method according to claim 1, where R1 is methylene or a C2-C6 polymethylene bond. ! 3. The method according to claim 1, where R1 is a C3-C6 alkenylenyl bond. ! 4. The method according to claim 1 where R is —N = C (NR3R4) (NR5R6) or —NR7C (NR3) (C = NR5), where R3-R7 is H, Alk, Ar or (CH2) nAr, where Ar is an aryl group and n is an integer from 1 to 13, or R3 and R4, or R4 and R5, or R5 and R7, or R3 and R7 together can be —CH 2 —CH 2 - or —CH 2 —CH 2 -CH2-. ! 5. The method according to claim 1, wherein said cyclosporin derivative A is a 3-substituted diaminoiminoalkylthiocyclosporin A. derivative! 6. The method according to claim 1, where the specified derivative of cyclosporin A is selected from the group consisting of derivatives of ((R) - (diamino) iminoal1. Способ лечения вододефицитного состояния сухого глаза, увеита или факоанафилактического эндофтальмита в глазу, или баланита, псориаза или атопического дерматита кожи, где указанный способ включает стадии местного введения в глаз или на кожу терапевтически эффективн
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