Bicyclononene derivatives
AssigneeActelion Pharmaceuticals Ltd.
InventorsOlivier Bezencon, Christoph Boss, Daniel Bur, Olivier Corminboeuf, Walter Fiśchli, Corinna Grisostomi, Lubos Remen, Sylvia Richard-Bildstein, Thierry Sifferlen, Thomas Weller
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Abstract
The invention relates to novel bicyclononene derivatives of Formula (I); and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.
Claims21
A compound selected from the group consisting of bicyclononene compounds of the formula (I)
- X represents —NH— or —N(L);
- W represents a five-membered heteroaryl containing a nitrogen and a sulfur, wherein said heteroaryl radical is optionally mono-substituted by C1-7-alkyl;
- V represents —CH2CH2—O—, —CH2CH2CH2—O—, —O—CH2CH2—O—, —O—CH2CH2CH2—O—, —CH2—O—CH2CH2—O—, —O—CH2CH2—O—CH2—, or —O—CH2CH2CH2—O—CH2—;
- U represents unsubstituted aryl;
- mono-, di-, tri- or tetra-substituted aryl, wherein the substituents are independently selected from C1-7-alkyl, C1-7-alkoxy, —CF3, —OCF3, halogen and hydroxy-C1-7-alkyl;
- or five-membered heteroaryl containing two heteroatoms independently selected from nitrogen, oxygen and sulfur, wherein said heteroaryl radical is optionally mono-, di- or tri-substituted, wherein the substitutents are independently selected from C1-7-alkyl, C1-7-alkoxy, —CF3, —OCF3 and halogen;
- T represents —CONR1— or —CH2CONR1—;
- Q represents methylene;
- M represents unsubstituted aryl;
- mono- di- or tri-substituted aryl, wherein the substituents are independently selected from C1-7-alkyl, C1-7-alkoxy, —OCF3, —CF3, hydroxy-C1-7-alkyl, and halogen;
- or mono- or di-substituted pyridinyl, wherein the substituents are independently selected from halogen, C1-7-alkyl, —OCF3, —CF3 and C1-7-alkoxy;
- with the proviso, that the halogen substituents are not in 2- or 6-position of the pyridinyl ring;
- L represents —R3, —COR3, —COOR3, —CONR2R3, —SO2R3, or —SO2NR2R3;
- R1 and R1′ independently represent C1-7-alkyl or cycloalkyl;
- R2 and R2′ independently represent hydrogen, C1-7-alkyl, C2-7-alkenyl, cycloalkyl, or cycloalkyl-C1-7-alkyl;
- R3 represents C1-7-alkyl, cycloalkyl, or cycloalkyl-C1-7-alkyl, wherein these groups may be unsubstituted or mono-, di- or tri-substituted, wherein the substituents are independently selected from hydroxy, —NH2, —OCOR2, —COOR2, —SO3H, —SO2CH3, C1-7-alkoxy, cyano, —CONR2R2′, —NH(NH)NH2, —NR1R1′, tetrazolyl, and C1-7-alkyl, with the proviso that a carbon atom is attached at the most to one heteroatom in case this carbon atom is sp3-hybridized;
- including its optically pure enantiomers, diastereomers, free base and salt forms.
Dependencies are inferred from the claim text.