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US 2008/0176947 A1Published application
Heterocyclic-Substituted Alkanamides Useful as Renin Inhibitors
OwnerPeter Herold, Robert Mah +6inventors
InventorsPeter Herold, Robert Mah, Vincenzo Tschinke, Stefan Stutz, Dirk Behnke, Aleksandar Stojanovic, Stjepan Jelakovic, Christiane Marti
Life of this patent
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Abstract
Compounds of the general formula (I) in which the meanings of the substituents R1 and R2 are as stated in claim 1, have renin-inhibiting properties and can be used as medicines.
Claims14
1-13. (canceled)
A compound of the formula
- in which
- R1 is a) saturated heterocyclyl which is bonded via a C atom and where the heterocyclyl radical contains oxygen as heteroatom and which is optionally substituted one or more times by C1-8alkanoyl, C2-6alkenyl, C2-6alkynyl, C1-6alkoxy, C1-6alkoxy-C1-6alkoxy, C1-6alkoxy-C1-6alkyl, C1-6alkoxycarbonylamino, C1-6alkyl, C0-6alkylcarbonylamino, C1-6alkylcarbonyloxy, C1-6alkylenedioxy, optionally N-mono or N,N-di-C1-6-alkylated amino, aryl, optionally N-mono or N,N-di-C1-6-alkylated carbamoyl, optionally esterified carboxy, cyano, C3-8cycloalkoxy, C3-8cycloalkyl-C0-6alkyl, halogen, halo-C1-6alkoxy, halo-C1-6alkyl, heteroaryl, unsaturated, partially saturated or saturated heterocyclyl, hydroxy, nitro or oxo;
- or
- b) dioxanyl-, dioxepanyl-, dioxolanyl-, oxepanyl-, tetrahydropyranyl-, tetrahydrofuranyl-, or bicyclic saturated heterocyclyl-C1-4alkyl and where the heterocyclyl radical contains oxygen as heteroatom, each of which is optionally substituted one or more times by C1-8alkanoyl, C2-6alkenyl, C2-6alkynyl, C1-6alkoxy, C1-6alkoxy-C1-6alkoxy, C1-6alkoxy-C1-6alkyl, C1-6alkoxycarbonylamino, C1-6alkyl, C0-6alkylcarbonylamino, C1-6alkylcarbonyloxy, C1-6alkylenedioxy, optionally N-mono or N,N-di-C1-6-alkylated amino, aryl, optionally N-mono or N,N-di-C1-6-alkylated carbamoyl, optionally esterified carboxy, cyano, C3-8cycloalkoxy, C3-8cycloalkyl-C0-6alkyl, halogen, halo-C1-6alkoxy, halo-C1-6alkyl, heteroaryl, unsaturated, partially saturated or saturated heterocyclyl, hydroxy, nitro or oxo;
- or
- c) C2-8alkynyl which is optionally substituted one or more times by C1-8alkanoyl, C2-6alkenyl, C2-6alkynyl, C1-6alkoxy, C1-6alkoxy-C1-6alkoxy, C1-6alkoxy-C1-6alkyl, C1-6alkoxycarbonylamino, C1-6alkyl, C0-6alkylcarbonylamino, C1-6alkylcarbonyloxy, C1-6alkylenedioxy, optionally N-mono or N,N-di-C1-6-alkylated amino, aryl, optionally N-mono or N,N-di-C1-6-alkylated carbamoyl, optionally esterified carboxy, cyano, C3-8cycloalkoxy, C3-8cycloalkyl-C0-6alkyl, halogen, halo-C1-6-alkoxy, halo-C1-6alkyl, heteroaryl, unsaturated, partially saturated or saturated heterocyclyl, hydroxy, nitro or oxo;
- or
- R2 is, independently of one another, 1-4 radicals selected from:
- C1-8alkanoyl, C1-8alkanoyl-C2-4alkoxy bearing the alkanoyl group in a position higher than α, C1-8alkanoylamino-C1-4alkoxy, N—C1-4alkanoylamino-C1-4alkyl, C1-8alkanoyloxy-C1-4alkyl, N′—C2-8alkanoyIpiperazino-C1-4alkoxy, N′—C2-8alkanoyIpiperazino-C4alkyl, C1-8alkanesulphonyl-C1-4alkoxy, C1-8alkanesulphonyl-C1-4alkyl, C1-8alkanesulphonylamino-C1-4alkoxy, C1-4alkanesulphonylamino-C1-4alkyl, C1-8alkanesulphonyl-C1-4(hydroxy)alkoxy, C2-8alkenyloxy, C2-8alkenyloxy-C1-4alkoxy, C2-8alkenyloxy-C1-4alkyl, C1-8alkoxy, C1-6alkoxy-C1-6alkanoyl, C1-4alkoxy-C2-4alkenyl, C1-4alkoxy-C2-4alkenyloxy, C1-4alkoxy-C1-4alkoxy, C1-4alkoxy-C1-4alkoxy-C1-4alkyl, C1-4alkoxy-C1-4alkyl, C1-4alkoxycarbonyl-C1-4alkoxy, C1-4alkoxycarbonyl-C1-4alkyl, C1-8alkoxycarbonylamino-C1-4alkoxy, C1-8alkoxycarbonylamino-C1-4alkyl, C1-8alkyl, C1-4alkylamino, N,N-di-C1-4alkylamino, C1-4alkylamino-C1-4alkoxy, N,N-di-C1-4alkylamino-C1-4alkoxy, C1-4alkylamino-C1-4alkyl, N,N-di-C1-4alkylamino-C1-4alkyl, N-mono- or N,N-di-C1-4alkylcarbamoyl-C1-4alkoxy, N-mono- or N,N-di-C1-4alkylcarbamoyl-C1-4alkyl, N′—C1-4alkylpiperazino-C1-4alkoxy,N′—C1-4alkylpiperazino-C1-4alkyl, C1-4alkylthio-C1-4alkoxy, C1-4alkylthio-C1-4(hydroxy)alkoxy, C1-4alkylthio-C1-4alkyl, amino-C2-4alkoxy, amino-C1-4alkyl, carbamoyl-C1-4alkoxy, carbamoyl-C1-8alkyl, carboxy-C1-4alkoxy, carboxy-C1-4alkyl, cyano-C1-4alkoxy, cyano-C1-4alkyl, C3-8-cycloalkoxy, C3-8cycloalkoxy-C1-4alkoxy, C3-8cycloalkoxy-C1-4alkyl, C3-8cycloalkyl, S,S-dioxothiomorpholino-C1-4alkoxy, S,S-dioxothiomorpholino-C1-4alkyl, halogen, halo-C1-4alkoxy, halo-C1-4alkyl, halo-C2-8(hydroxy)alkoxy, hydroxy, hydroxy-C2-8alkoxy, hydroxy-C2-8alkyl, imidazolylthio-C1-4alkoxy, imidazolylthio-C1-4alkyl, optionally N-oxidized morpholino-C1-4alkoxy, morpholino-C1-4alkyl, S-oxothiomorpholino-C1-4alkoxy, S-oxothiomorpholino-C1-4alkyl, piperazino-C1-4alkoxy, piperazino-C1-4alkyl, piperidino-C1-4alkoxy, piperidino-C1-4alkyl, optionally partially hydrogenated pyridyl- or N-oxidopyridyl-C1-4alkoxy, optionally partially hydrogenated pyridyl- or N-oxidopyridyl-C1-4alkyl, optionally N-oxidized pyridylthio-C1-4alkoxy, optionally N-oxidized pyridylthio-C1-4alkyl, pyrimidinylthio-C1-4alkoxy, pyrimidinylthio-C1-4alkyl, pyrrolidino-C1-4alkoxy, pyrrolidino-C1-4alkyl, thiazolinylthio-C1-4alkoxy, thiazolinylthio-C1-4alkyl, thiazolyl-C1-4alkoxy, thiazolylthio-C1-4alkoxy, thiazolylthio-C1-4alkyl, thiomorpholino-C1-4alkoxy, thiomorpholino-C1-4alkyl, trifluoro-C1-8alkanesulphonyl-C1-4alkoxy, trifluoro-C1-8alkanesulphonylamino-C1-4alkyl, phenyl or naphthyl which is unsubstituted or mono-, di- or trisubstituted by C1-4alkoxy, C1-4alkyl, C1-4alkylamino, di-C1-4alkylamino, halogen, hydroxy and/or trifluoromethyl, and phenyl- or naphthyl-C1-4alkoxy which is unsubstituted or mono-, di- or trisubstituted by C1-4alkoxy, C1-4alkyl, C1-4alkylamino, di-C1-4alkylamino, halogen, hydroxy and/or trifluoromethyl, and its salt or compound in which one or more atoms are replaced by their stable, non-radioactive isotopes, especially pharmaceutically acceptable salt.
6 more elements
Dependencies are inferred from the claim text.