Heterocyclic compounds and their use as aldosterone synthase inhibitors
View Patent ↗The application relates to novel heterocyclic compounds of the general formula (I) in which R, R 1 , R 2 , W, X, Y, Z and n have the meanings defined in the description, to a process for their preparation and to the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.
1. A compound of the formula
W is C, or if X is C, is also N;
X is C or N;
Y is C;
Z is a bond;
R a) is hydrogen; or
b) is C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, halogen or trifluoromethyl;
R 1 is C 3 -C 8 -cycloalkyl-C 0 -C 4 -alkyl or a saturated, 4-8-membered, monocyclic heterocyclyl-C 0 -C 4 -alkyl, each of which is unsubstituted or substituted by 1-4 C 1 -C 8 -alkoxy, C 1 -C 8 -alkoxycarbonyl, C 1 -C 8 -alkyl, C 0 -C 8 -alkylcarbonyl, C 1 -C 8 -alkylsulfonyl, aryl-C 0 -C 4 -alkoxycarbonyl, aryl, cyano, halogen, unsaturated heterocyclyl, oxo, trifluoromethoxy, trifluoromethyl or tri-C 1 -C 4 -alkylsilyl, wherein the heterocycle contains 1-3 heteroatoms selected from N, O, and S;
R 2 is hydrogen;
n is 0-2; or a pharmaceutically acceptable salt thereof.
2. The compound according to claim 1 , characterized in that it corresponds to the formulae
where the meanings of the substituents R, R 1 and R 2 are as indicated for compounds of the formula (I) according to claim 1 .
3. The compound according to claim 1 , where R is hydrogen or C 1 -C 8 -alkyl.
4. The compound according to claim 1 , where n is a number 0 or 1.
5. The compound according to claim 2 , where
R is hydrogen or C 1 -C 8 -alkyl;
R 1 is C 3 -C 8 -cycloalkyl-C 0 -C 4 -alkyl or heterocyclyl, in each case optionally substituted by halogen, cyano, trifluoromethyl, heterocyclyl or C 0 -C 8 -alkylcarbonyl; and
R 2 is hydrogen.
6. A pharmaceutical product comprising a compound of the formula (I) according to claim 1 , and conventional excipients.
7. The compound according to claim 2 , where R is hydrogen or C 1 -C 8 -alkyl.
8. A pharmaceutical product comprising a compound of the formula (Ia), or (Ib) according to claim 2 , and conventional excipients.
9. The compound according to claim 3 , where R is hydrogen or methyl.
10. The compound according to claim 7 , where R is hydrogen or methyl.
11. The compound according to claim 1 , wherein the compound is: