Spiro-oxazolones
AssigneeHoffmann-La Roche Inc.
InventorsValerie Runtz-Schmitt, Patrick Schnider, Cosimo Dolente, Bernhard Fasching
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Abstract
The present invention provides spiro-oxazolones, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The present compounds are useful as therapeutics acting peripherally and centrally in the conditions of inappropriate secretion of vasopressin, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, aggressive behavior and phase shift sleep disorders, in particular jetlag.
Claims5
A tablet formulation comprising:
- Lactose;
- Corn Starch;
- Magnesium stearate;
- Talc;
- and
- a compound of formula I,
- wherein
- X1 is C—R1 or N;
- X2 is C—R1 or N;
- X3 is C—R1 or N;
- X4 is C—R1 or N;
- whereby only one of X1, X2, X3 and X4 is N;
- R1 each separately is selected from the group consisting of hydrogen, halogen, hydroxy, C1-6-alkyl and C1-6-alkoxy;
- R2 is selected from the group consisting of H and C1-6-alkyl;
- R3 is selected from the group consisting of H and C1-6-alkyl;
- or R2 and R3 together are ═O;
- Y1 is C—R4 or N;
- Y2 is C—R4 or N;
- Y3 is C—R4 or N;
- Y4 is C—R4 or N;
- whereby only one of Y1, Y2, Y3 and Y4 is N;
- R4 each separately is selected from the group consisting of hydrogen, halogen, halogen-C1-6-alkyl, hydroxy, C1-6-alkyl, C1-6-alkoxy and Si(C1-6-alkyl)3;
- m is 1, 2 or 3;
- and
- n is 0 or 1;
- or pharmaceutically acceptable salts thereof.
A compound of formula I,
- wherein
- X1 is C—F;
- X2 is C—OCH3;
- X3 is C—R1 or N;
- X4 is C—Br;
- R2 is Me;
- R3 is Me;
- Y1 is N;
- Y2 is C—OH;
- Y3 is C—Si(CH3)3;
- Y4 is N;
- m is 1, 2 or 3;
- and
- n is 0 or 1;
- or pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.