Methods and compositions for the treatment of diseases of the eye

A method for treatment of a disease of the eye of a patient resulting from angiogenesis in the eye comprising injecting a therapeutically effective amount of an αvβ3 and/or αvβ5 inhibitor, sufficient to inhibit angiogenesis and inhibit neovascularization in the treated eye, into the sclera layer of the eye of the patient through the location of the exterior surface of the sclera that overlies retinal tissue, wherein the αvβ3 and/or αvβ5 inhibitor is a compound of formula II

• wherein
• R1 is H, alkyl having 1-6 C atoms or benzyl,
• R2 is R10, CO—R10, COOR6, COOR10, SO2R6 or SO2R10,
• R3 is H, Hal, OA, NHR10, N(R10)2, —NH-acyl, —O-acyl, CN, NO2, OR10, SR10, R2 or CONHR10,
• R4 is H, ═O, ═S, C1-C6-alkyl or acyl,
• R5 is NH2, H2N—C(═NH) or H2N—(C═NH)—NH, where the primary amino groups are optionally provided with conventional amino protective groups or are optionally mono-, di- or trisubstituted by R10, CO—R10, COOR10 or SO2R10, or R6,
• R7, R8 are each independently of one another absent or H, or
• R7 and R8 together are a bond,
• X, Y are each independently of one another ═N—, —N—, O, S, —CH2— or ═C—,
• with the proviso that at least one of the two definitions X, Y is ═N—, —N—, O or S,
• W, Z are each independently of one another absent, O, S, NR1, C(═O), CONH, NHCO, C(═S)NH, NHC(═S), C(═S), SO2NH, NHSO2 or CA=CA′,
• R6 is a mono- or binuclear heterocycle which has 1 to 4 N, O and/or S atoms and is unsubstituted or mono-, di- or trisubstituted by Hal, A, —CO-A, OH, CN, COOH, COOA, CONH2, NO2, ═NH or ═O,
• R9 is H, Hal, OA, NHA, NAA′, NHacyl, Oacyl, CN, NO2, SA, SOA, SO2A, SO2Ar or SO3H,
• R10 is H, A, Ar or aralkyl having 7-14 C atoms,
• R11 is H or alkyl having 1-6 C atoms,
• A, A′ are each independently of one another H or unsubstituted or mono-, di- or tri- R9-substituted alkyl or cycloalkyl, each of which has 1-15 C atoms and in which one, two or three methylene groups are optionally replaced by N, O and/or S,
• Ar is an unsubstituted or mono-, di- or tri-A- and/or R9-substituted mono- or binuclear aromatic ring system having 0, 1, 2, 3 or 4 N, O and/or S atoms,
• Hal is F, Cl, Br or I and
• m, n are each independently of one another 0, 1, 2, 3 or 4,
• or a physiologically acceptable salt thereof.