Aqueous liquid eyedrop composition

Details Aqueous liquid eyedrop composition Aqueous liquid eyedrop composition

A - Human Necessities

61

K

167/209

A61K 31/40 (2006.01) A61K 9/00 (2006.01) A61K 47/32 (2006.01) A61K 47/38 (2006.01) C07H 19/01 (2006.01)

Patent

CA 2020431

The composition contains a tricyclo compound of the formula: (see formula I) wherein each vicinal pair of substituents [R1 and R2], [R3 and R4], [R5 and R6] independently a) represent two vicinal hydrogen atoms, or b) form a second bond between the vicinal carbon atoms to which they are attached; in addition to its significance above, R2 may represent an alkyl group; R7 represents H, OH, protected hydroxy or O-alkyl, or in conjunction with R1 it may represent =O; R8 and R9 independently represent H or OH; R10 represents H, alkyl, alkyl substituted by one or more hydroxyl groups, alkenyl, alkenyl substituted by one or more hydroxyl groups, or alkyl substituted by =O; X represents O, (H,OH), (H,H) or -CH2O-; Y represents O, (H,OH), (H,H), N-NR11R12 or N-OR13; R11 and R12 independently represent H, alkyl, aryl or tosyl; R13, R14, R15, R16, R17, R18, R19, R22 and R23 independently represent H or alkyl; R20 and R21 independently represent O, or they may independently represent (R20a,H) and (R21a,H) respectively; R20a and R21a independently represent OH, O-alkyl or OCH2OCH2CH2OCH3 or R21a is protected hydroxy; in addition, R20a and R21a may together represent an oxygen atom in an epoxide ring; N is 1, 2 or 3; in addition to their significances above, y, R10 and R23, together with the carbon atoms to which they are attached, may represent a 5- or 6- membered N-, S- or O- containing heterocyclic ring, which may be saturated or unsaturated, and which may be substituted by one or more groups selected from alkyl, hydroxy, alkyl substituted by one or more hydroxyl groups, O-alkyl, benzyl and -CH2Se(C6H5); or a pharmaceutically acceptable salt thereof and a water-soluble solubilizer. This composition is particularly useful for the treatment and prevention of various diseases of the eye such as autoimmune diseases; such as vernal conjuncti- vitis, uveitis associated with Behcet's disease, keratitis, herpetic keratitis, conical cornea, dystrophia epithelialis cornea, leukoma, ocular pemphigus, Mooren's ulcer, Sclevitis, Graves' ophthalmopathy, and rejection in corneal transplan- tation.

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