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filingDate 2009-07-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_22cbce8c477f3d5802189fcb11ba68d1
publicationDate 2010-01-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-2010009953-A1
titleOfInvention Cyclosporin derivatives for treating ocular and dermal diseases and conditions
abstract The present invention provides a method for the treatment of ocular or dermal diseases and/or conditions, e.g. an aqueous deficient dry eye state, uveitis or phacoanaphylactic endophthalmitis in an eye, or balanitis, psoriasis, or atopic dermatitis of the skin, said method comprising administering, topically to the eye or the skin, a therapeutically effective amount of a novel cyclosporin A derivative selected from the group consisting of compounds represented by the formula: n n n n n n n n n n wherein R 1 is S-Alk-R wherein Alk is an alkylene linkage, preferably a methylene or poly methylene linkage, e.g. a C 2 to C 6 polymethylene linkage, or a polyalkenylene linkage, e.g. a C 3 to C 6 alkenylenyl linkage, R is R is —N═C(NR 3 R 4 )(NR 5 R 6 ) orn NR 7 [(NR 3 R 4 )C═NR 5 ], i.e. guanidines or —N═C(R 8 )(NR 9 R 10 ), i.e. amidines wherein R 3 -R 7 10 is H, Alk, Ar or (CH 2 )nAr wherein Ar is an aryl group and n is an integer of from 1 to 13 or R 3 and R4 or R 4 and R 5 or R 5 and R 7 or R 3 and R 7 , or R 9 and R 10 , together may be —CH 2 —CH 2 — or —CH 2 —CH 2 —CH 2 — and R 2 is selected from the group consisting of hydroxyl, lower alkyl and hydroxyl-substituted lower alkyl and R 2 is selected from the group consisting of hydroxy and lower alkyl.
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