Amino acid ester prodrugs and the use thereof
AssigneeBayer Schering Pharma Aktiengesellschaft
InventorsDaniel Meibom, Hans-Georg Lerchen, Alexandros Vakalopoulos, Barbara Albrech-Küpper, Peter Nell, Jörg Keldenich, Katja Zimmermann, Ursula Krenz
Life of this patent
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Abstract
The present application relates to amino acid ester prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-oxazol-4-yl]methyl}sulfanyl)-4-(4-{[2,3-dihydroxypropyl]oxy}phenyl)pyridine-3,5-dicarbonitriles, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of cardiovascular disorders.
Claims10
A compound of the formula (I)
- in which
- RA is hydrogen or methyl
- and
- RPD is a group of the formula
- in which
- # means the point of linkage to the respective O atom,
- L1 is a bond or —CH2—,
- L2 is straight-chain (C3-C6)-alkanediyl, which may be substituted up to two times, identically or differently by (C1-C4)-alkyl, hydroxyl and/or (C1-C4)-alkoxy,
- R1 and R2 are identical or different and independently of one another are hydrogen or (C1-C4)-alkyl which may be substituted by hydroxyl, (C1-C4)-alkoxy, amino, mono-(C1-C4)-alkylamino or di-(C1-C4)-alkylamino
- or
- R1 and R2 are linked to one another and, together with the nitrogen atom to which they are attached, form a 5- or 6-membered saturated heterocycle which may comprise a further ring heteroatom from the series consisting of N and O, and may be substituted one or two times, identically or differently, by (C1-C4)-alkyl, amino, hydroxyl and/or (C1-C4)-alkoxy,
- R3 is hydrogen or the side group of a natural α-amino acid or its homologs or isomers,
- or
- R3 is linked to R1 and both, together with the atoms to which they are attached, form a 5- or 6-membered saturated heterocycle which may be substituted once or twice by identical or different (C1-C4)-alkyl, amino, hydroxyl and/or (C1-C4)-alkoxy substituents,
- R4 is hydrogen or methyl
- or
- R3 and R4 are linked to one another and, together with the carbon atom to which they are attached, form a 3- to 6-membered saturated carbocycle,
- and
- R5 and R6 are identical or different and independently of one another are hydrogen or (C1-C4)-alkyl which may be substituted by hydroxyl, (C1-C4)-alkoxy, amino, mono-(C1-C4)-alkylamino or di-(C1-C4)-alkylamino,
- and the salts thereof.
7-9. (canceled)
11-13. (canceled)
Dependencies are inferred from the claim text.