Adenosine A1 agonists for the treatment of glaucoma and ocular hypertension
AssigneeBayer Intellectual Property GmbH
InventorsJürgen Klar, Georges Von Degenfeld, Hans-Georg Lerchen, Barbara Albrecht-Küpper, Andreas Knorr, Peter Sandner, Daniel Meibom
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Abstract
The present invention relates to the use of selective adenosine A1 agonists, in particular the dicyanopyridines of formula (I), for the treatment and/or prophylaxis of glaucoma and ocular hypertension as well as the their use for the production of a medicament for the treatment and/or prophylaxis of glaucoma and ocular hypertension.
Claims11
A method of treatment of glaucoma, normotensive glaucoma, ocular hypertension and/or combinations thereof comprising administering a therapeutically effective amount of a compound of formula (I) to a human or animal in need thereof, 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.
Dependencies are inferred from the claim text.