DOLENTE, COSIMO,SCHNIDER, PATRICK,RUNTZ-SCHMITT, VALERIE,FASCHING, BERNHARD
申请号：
PE0007222016
公开号：
PE08642016A1
申请日:
2014.12.16
申请国别(地区):
PE
年份:
2016
代理人:
摘要：
The present Invention relates to Derivatives of formula I oxazolonas Spiro - Where X1, X2, X3 and X4 are C - or n r1 r1 is Hydrogen, halogen, among others R2 and R3 are H or c1-c6 alkoxy or R2 and R3 are = o y1, y2, y3 and Y4 are C - or n R4 R4 is Hydrogen, halogen, among others and M is 1, 2 or 3 n is 0 OR 1.Preferred compounds are: (1R) - 2 - (3H 1\u00b4h, Spiro [2-benzofuran - 1,4\u00b4 - piperidin] - 1 - yl) - 4\u00b4h 2,3 dihydro - - - - 1,5\u00b4 spiro [indeno [1,3] oxazole - 4 - One (1S) - 2 - (3H 1\u00b4h, Spiro benzofuran - [2 - 1,4\u00b4 - piperidin] - 1 - yl) - 4\u00b4h 2,3 dihydro - - - - 1,5\u00b4 spiro [indeno [1,3] oxazole - 4 - One among others. It also relates to a Pharmaceutical composition.These compounds act as V1a Receptor Antagonists, being useful in the treatment of inappropriate secretion of vasopressin, anxiety, Depressive Disorders, Autism Spectrum Disorders, Schizophrenia, among others.La presente invencion se refiere a derivados de espiro-oxazolonas de formula I donde X1, X2, X3 y X4 son C-R1 o N R1 es hidrogeno, halogeno, entre otros R2 y R3 son H o alcoxi C1-C6 o R2 y R3 son =O Y1, Y2, Y3 y Y4 son C-R4 o N R4 es hidrogeno, halogeno, entre otros m es 1, 2 o 3 n es 0 o 1. Son compuestos preferidos: (1R)-2´-(1´H,3H-espiro[2-benzofuran-1,4´-piperidin]-1´-il)-2,3-dihidro-4´H-espiro[indeno-1,5´-[1,3]oxazol-4´-ona (1S)-2´-(1´H,3H-espiro[2-benzofuran-1,4´-piperidin]-1´-il)-2,3-dihidro-4´H-espiro[indeno-1,5´-[1,3]oxazol-4´-ona entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos actuan antagonistas del receptor V1a, siendo utiles en el tratamiento de secrecion inadecuada de vasopresina, ansiedad, trastornos depresivos, trastornos del espectro autista, esquizofrenia, entre otros.
