| 摘要 |
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. |
| 主权项 |
1. A compound of formula I, wherein X1 C—R1 or N; X2 C—R1 or N; X3 C—R1 or N; X4 C—R1 or N; whereby only one of X1, X2, X3 and X4 is N or all of X1, X2, X3 and X4 are C—R1; Y is O or S(O)m; m is 0, 1 or 2; 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; R4 is selected from the group consisting of
i) aryl-C1-6-alkyl-, wherein the aryl moiety can be optionally substituted by halogen,ii) C1-6-alkoxy-CH2—,iii) C1-6-alkyl-,iv) C2-6-alkenyl-CH2—,v) C2-6-alkynyl-CH2—,vi) halogen-C1-6-alkyl-,vii) halogen-C2-6-alkenyl-CH2—, andviii) hydrogen; R5 is selected from the group consisting of
i) aryl-,ii) aryl-C1-6-alkyl-, wherein
the aryl moiety can be optionally substituted by C1-6-alkyl, halogen-C1-6-alkyl or halogen, andthe C1-6-alkyl moiety can optionally be substituted by C1-6-alkyl-COO—, halogen or hydroxy,iii) C3-10-cycloalkyl-C1-6-alkyl-,iv) halogen-C1-6-alkyl-,v) heteroaryl-C1-6-alkyl-, wherein the heteroaryl moiety can be optionally substituted by halogen,vi) heterocycloalkyl-C1-6-alkyl-,vii) C1-6-alkyl-,viii) C2-6-alkenyl-CH2— that is optionally substituted by halogen, (C1-6-alkyl)3SiO—, C1-6-alkyl-COO— or C1-6-alkyl-OOC—,ix) C1-6-alkoxy-CH2—, andx) C2-6-alkynyl-CH2—; or R4 and R5 together are selected from the group consisting of
i) C3-10-cycloalkyl that is optionally substituted by C1-6-alkyl, C1-6-alkoxy, C1-6-alkyl-OOC—, C1-6-alkyl-COO—, halogen, halogen-C1-6-alkyl, hydroxy-C16-alkyl or oxo;ii) heterocycloalkyl that is optionally substituted by benzyl, C1-6-alkyl, C1-6-alkyl-OOC—, halogen-C1-6-alkyl or oxo;iii) C3-10-cycloalkenyl that is optionally substituted by C1-6-alkyl, C1-6-alkyl-OOC—, halogen-C1-6-alkyl, (C1-6-alkyl)3SiO—C1-6-alkyl- or hydroxy-C1-6-alkyl, andiv) indanyl when Y is SO2;or pharmaceutically acceptable salts thereof. |
