| 摘要 |
The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes, 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 active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.; |
| 主权项 |
1. A compound of formula I, wherein R1 is halogen; R2 is selected from the group consisting of
i) heteroaryl, unsubstituted or substituted by 1 to 3 substituents individually selected from the group consisting of OH, halogen, cyano, C1-6-alkyl, C1-6-alkoxy, halogen-C1-6 alkyl, halogen-C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl and hydroxy-C1-6-alkyl;ii) aryl, unsubstituted or substituted by 1 to 3 substituents individually selected from the group consisting of OH, halogen, cyano, C1-6-alkyl, C1-6-alkoxy, halogen-C1-6-alkyl, halogen-C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl and hydroxy-C1-6-alkyl;iii) C3-7-cycloalkyl, unsubstituted or substituted by 1 to 3 substituents individually selected from the group consisting of OH, halogen, cyano, C1-6-alkyl, C1-6-alkoxy, halogen-C1-6-alkyl, halogen-C1-6-alkoxy, C1-6-alkoxy-C1-6-alkyl and hydroxy-C1-6-alkyl; andiv) C1-6-alkyl, unsubstituted or substituted by 1 to 3 substituents individually selected from the group consisting of OH, halogen, cyano, C3-7-cycloalkyl, C1-6-alkoxy and halogen-C1-6-alkoxy; or pharmaceutically acceptable salts thereof. |
