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US 2015/0087644 A1Published application
Pyrrolidino heterocycles
AssigneeHoffmann-La Roche Inc.
InventorsAlexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Christian Lerner
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Abstract
The invention relates to compounds of formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
Claims12
A compound of formula (I)
- wherein
- A1, A2 and A3 are independently N or C, with the proviso that A1, A2 and A3 are not simultaneously N,
- B is C1-C4-alkylene, C2-C4-alkenylene, —O—C1-C4 alkyl or —NH—C1-C4alkyl
- R1 and R2, are independently selected from hydrogen, C1-C7-alkyl, C1-C7-hydroxyalkyl, C3-C8-cycloalkyl, R1 and R2 together with the nitrogen atom to which they are attached, form a heterocycloalkyl which can be substituted by 1 to 3 substituents independently selected from the group consisting of halogen, C1-C7-alkyl, C1-C7-hydroxyalkyl, C1-C7 alkoxy, C1-C7-haloalkyl, hydroxyl and oxo;
- R3 is selected from heteroaryl optionally substituted by 1 to 3 substituents selected from halogen, C1-C7-alkyl, cycloalkyl, C1-C7 alkoxy, C1-C7-haloalkyl, aryl, heteroaryl, —NR5R6, —O—R7, —C(O)—NR′R″, wherein heteroaryl contains at least one nitrogen atom which is adjacent to the connecting ring carbon atom,
- R4 is selected from hydrogen, C1-C7-alkyl, C3-C8-cycloalkyl,
- R5 and R6 are independently selected from hydrogen, C1-C7-alkyl, R5 and R6 together with the nitrogen atom to which they are attached, form a heterocycloalkyl which can be substituted by 1 to 3 substituents independently selected from the group consisting of halogen, C1-C7-alkyl, C1-C7-hydroxyalkyl, C1-C7 alkoxy, C1-C7-haloalkyl and oxo;
- R7 is selected from C1-C7-alkyl, C1-C7-haloalkyl and heterocycloalkyl,
- R′ and R″ are independently selected from hydrogen and C1-C7-alkyl.
6 more elements
Dependencies are inferred from the claim text.