Ferring B.v.

Vantia Limited

Kalvista Pharmaceuticals Limited

Christopher Martyn Yea

Peter Hudson

Doreen Mary Ashworth

Richard Jeremy Franklin

Gary Robert William Pitt

Graeme Semple

Gary R W Pitt

David Paul Jenkins

Andreas Maetzel

Edward Paul Feener

Sally Louise Marsh

Michael David Smith

This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, Vand Vare both H, OMe or F, or one of Vand Vis Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N, NH, NHBn or NH-acyl and the other is H, or Vand Vtogether are &#x2550;O, &#x2014;O(CH)O&#x2014; or &#x2014;S(CH)S&#x2014;; Wis either O or S; Xand Xare both H, or together are &#x2550;O or &#x2550;S; Y is ORor NRR; R, R, Rand Rare independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; Ris selected from H and lower alkyl; Rand Rare independently selected from H and lower alkyl, or together are &#x2014;(CH)&#x2014;; 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.

Condensed azepines as vasopressin agonists

Compounds according to general formulae (1 and 2), wherein Gis an azepine derivative and Gis a group according to general formulae (9&#x2013;11) are new. Compounds according to the invention are vasopressin Vreceptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents 

Fused azepine derivatives and their use as antidiuretic agents

This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, Vand Vare both H, OMe or F, or one of Vand Vis Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N, NH, NHBn or NH-acyl and the other is H, or Vand Vtogether are &#x2550;O, &#x2014;O(CH)O&#x2014; or &#x2014;S(CH)S&#x2014;; Wis either O or S; Xand Xare both H, or together are &#x2550;O or &#x2550;S; Y is ORor NRR; R, R, Rand Rare independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; Ris selected from H and lower alkyl; Rand Rare independently selected from H and lower alkyl, or together are &#x2014;(CH)&#x2014;; 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. 

Compounds according to general formula (1), and pharmaceutically acceptable salts thereof, wherein V is a covalent bond or NH, X is selected from CH , O and N-alkyl, Z is either S or &mdash;CH&boxH;CH&mdash;, R and R are independently selected from H, F, Cl, Br and alkyl, R is selected from OH, O-alkyl and NR R , R and R are each independently H or alkyl, or together are &mdash;(CH ) &mdash;, p is 0, 1, 2, 3 or 4, and q is 4 or 5, are new. They are agonists at the asopressin V receptor and are useful as antidiuretics and pro-coagulants.

Bicyclic vasopressin agonists

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Romsey, United Kingdom

Christopher Martyn Yea