Heterocyclic spiro-compounds as aldosterone synthase inhibitors
View Patent ↗The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R 1 , R 2 , W, X, Y, Z and n have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.
1. A compound of the formula (Ia′) or (Ib′)
in which
R is hydrogen, C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy-C 0 -C 4 -alkyl, halogen, tri-C 1 -C 4 -alkylsilyl, deuterium or trifluoromethyl;
R 1 together with R 2 is a ring selected from the group consisting of
which rings may be substituted by 1-4 members selected from the group consisting of oxo, cyano-C 0 -C 6 -alkyl, C 0 -C 8 -alkylcarbonyl, thiophene, furan, oxazole, thiophenylcarbonyl, furanylcarbonyl and oxazolylcarbonyl, it being possible for thiophene, furan, oxazole, thiophenylcarbonyl, furanylcarbonyl and oxazolylcarbonyl to be unsubstituted or substituted by 1-4 members selected from the group consisting of C 1 -C 8 -alkyl, halogen, cyano and C 0 -C 8 -alkylcarbonyl; and
“*” denotes an asymmetric carbon atom;
or a pharmaceutically acceptable salt thereof.
2. A compound according to claim 1 , wherein R is hydrogen or deuterium.
3. A compound according to claim 1 , wherein R 1 together with R 2 is a ring selected from the group consisting of
which rings may be substituted by thiophene, furan, oxazole, thiophenylcarbonyl, furanylcarbonyl or oxazolylcarbonyl, it being possible for thiophene, furan, oxazole, thiophenylcarbonyl, furanylcarbonyl and oxazolylcarbonyl to be unsubstituted or substituted by 1-4 members selected from the group consisting of C 1 -C 8 -alkyl, halogen and cyano.
4. A compound according to claim 1 , wherein R 1 together with R 2 is ring selected from the group consisting of
which rings may be substituted by thiophene, furan, oxazole, thiophenylcarbonyl, furanylcarbonyl or oxazolylcarbonyl, it being possible for thiophene, furan, oxazole, thiophenylcarbonyl, furanylcarbonyl and oxazolylcarbonyl to be unsubstituted or substituted by 1-4 members selected from the group consisting of C 1 -C 8 -alkyl, halogen and cyano.
5. A compound according to claim 1 , wherein
R is hydrogen or deuterium; and
R 1 together with R 2 is a ring selected from the group consisting of
which rings may be substituted by thiophene, furan, oxazole or oxazolylcarbonyl, it being possible for thiophene, furan, oxazole and oxazolylcarbonyl to be unsubstituted or substituted by 1-4 members selected from the group consisting of C 1 -C 8 -alkyl, halogen and cyano.
6. A pharmaceutical composition comprising a compound of the formula (Ia′) or (Ib′) according to claim 1 and conventional excipients.