Adenosine a1 agonists for the treatment of glaucoma and ocular hypertension

An ophthalmic composition, comprising a compound of the formula (I) and at least one active ingredients selected from the group consisting of alpha adrenergic agonist, beta blocker and carbonic anhydrase inhibitor, wherein the compound of formula (I) is:

• in which
• A is oxygen or sulfur,
• R1 is hydrogen or a group of the formula
• in which
• # is the attachment to the oxygen-atom,
• L1 is linear (C2-C4)-alkanediyl,
• L2 is linear (C1-C3)-alkanediyl,
• R5 and R8 are identical or different and independently selected from the group consisting of hydrogen or a side group of a natural α-amino acid or its homologues or isomers,
• R6 and R9 are independently selected from hydrogen or methyl,
• R7 is hydrogen or (C1-C4)-alkyl,
• or
• R7 and R5 form together with the atoms which they are attached to a pyrrolidine- or piperidine-ring,
• R10 and R11 are identical or different and are independently selected from hydrogen or (C1-C4)-alkyl,
• wherein (C1-C4)-alkyl may be substituted with one group selected from hydroxy, (C1-C4)-alkoxy, amino, mono-(C1-C4)-alkylamino or di-(C1-C4)-alkylamino,
• or
• R10 and R8 form together with the atoms which they are attached to a pyrrolidine- or piperidine-ring,
• and
• R12 is hydrogen or hydroxycarbonyl,
• R2 is hydrogen or a group of the formula —CH2OR1,
• wherein R1 is defined as above,
• R3 is hydrogen, methyl or ethyl,
• R4 is hydrogen, methyl or ethyl,
• or
• R3 and R4 form together with the nitrogen-atom, which they are bound to, a azetidine-, pyrrolidine- or piperidine-ring,
• wherein the azetidine-, pyrrolidine- or piperidine-ring may be substituted with one or 2 substituents independently selected from the group fluoro, trifluoromethyl, methyl, ethyl, methoxy and ethoxy,
• or a salt thereof.