4,4-difluoro-1,2,3,4-tetrahydro-5h-1-benzazepine derivative...

C - Chemistry – Metallurgy – 07 – D

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C07D 223/16 (2006.01) A61K 31/55 (2006.01) A61P 7/12 (2006.01) A61P 13/00 (2006.01) A61P 43/00 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/06 (2006.01) C07D 403/10 (2006.01) C07D 403/12 (2006.01) C07D 403/14 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2464069

4,4-Difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivatives represented by the general formula (I), which have excellent arginine vasopressin V2 activity and are useful in the treatment of central diabetes insipidus and/or night pollakisuria: (I) wherein R1 is -OH, -O-lower alkyl, or optionally substituted amino; R2 is lower alkyl which may be substituted with one or more halogen atoms, or halogeno; one of R3 and R4 is -H, lower alkyl, or halogeno, and the other is optionally substituted nonaromatic cyclic amino or optionally substituted aromatic cyclic amino; and R5 is -H, lower alkyl, or halogeno.

L'invention concerne des dérivés de 4,4-difluoro-1,2,3,4-tétrahydro-5H-1-benzazépine de la formule générale (I), qui présentent une excellente activité de la vasopressine arginine V¿2?, et sont utiles pour le traitement du diabète insipide central et/ou de la pollakiurie nocturne. Dans ladite formule, R?1¿est -OH, alkyle -O-inférieur, ou amino éventuellement substitué; R?2¿ est un alkyle inférieur pouvant être substitué par un plusieurs atomes d'halogène, ou halogéno; R?3¿ ou R?4¿ est -H, alkyle inférieur, ou halogéno, l'autre étant un amino cyclique non aromatique éventuellement substitué ou un amino cyclique aromatique éventuellement substitué; et R?5¿ est -H, alkyle inférieur, ou halogéno.

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