Condensed azepines as vasopressin agonists

Details Condensed azepines as vasopressin agonists Condensed azepines as vasopressin agonists

C - Chemistry, Metallurgy

07

D

C07D 403/12 (2006.01) A61K 31/55 (2006.01) A61P 13/00 (2006.01) C07D 209/00 (2006.01) C07D 221/00 (2006.01) C07D 223/00 (2006.01) C07D 231/00 (2006.01) C07D 243/00 (2006.01) C07D 249/00 (2006.01) C07D 255/00 (2006.01) C07D 333/00 (2006.01) C07D 413/12 (2006.01) C07D 471/04 (2006.01) C07D 487/04 (2006.01) C07D 495/04 (2006.01) C07D 498/04 (2006.01)

Patent

CA 2396277

This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are =O, - O(CH2)pO- or -S(CH2)pS-; W1 is either O or S; X1 and X2 are both H, or together are =O or =S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are -(CH2)n-; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.

L'invention concerne des composés de la formule générale (1) Dans ladite formule (1), A est un dérivé d'azépine bicyclique ou tricyclique, V?1¿ et V?2¿ sont tous deux H, OMe ou F, ou un de V?1¿ et V?2¿ est Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N¿3?, NH¿2?, NHBn ou NH-acyl et l'autre est H, ou V?1¿ et V?2¿ sont ensemble =O, -O(CH¿2?)¿p?O- ou -S(CH¿2?)¿p?S-; W?1¿ est soit O soit S; X?1¿ et X?2¿ sont tous deux H, ou sont ensemble =O ou =S; Y est OR?5¿ ou NR?6¿R?7¿; R?1¿, R?2¿, R?3¿ et R¿4? sont sélectionnés indépendamment à partir de H, d'alkyle inférieur, d'alkyloxy inférieur, de F, Cl et Br; R?5¿ est sélectionné à partir de H et d'alkyle inférieur; R?6¿ et R?7¿ sont sélectionnés indépendamment à partir de H et d'alkyle inférieur, ou sont ensemble -(CH¿2?)¿n?-; n=3, 4, 5 ou 6; et p est 2 ou 3. Lesdits composés sont agonistes du récepteur V2 de vasopressine et s'avèrent utiles en tant qu'antidiurétiques et procoagulants. L'invention concerne en outre des compositions phamaceutiques incorporant ces agonistes de vasopressine, lesquelles compositions s'avèrent des plus utiles dans le traitement du diabète insipide central, de l'énurésie nocturne et de la polyurie nocturne.

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