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2. 发明申请

US20060154916A1 Condensed azepines as vasopressin agonists 有权
标题翻译：浓缩吖庚因作为血管加压素激动剂
公开(公告)号：US20060154916A1
公开(公告)日：2006-07-13
申请号：US11370861
申请日：2006-03-09
申请人： Doreen Ashworth , Gary Pitt , Peter Hudson , Christopher Yea , Richard Franklin
发明人： Doreen Ashworth , Gary Pitt , Peter Hudson , Christopher Yea , Richard Franklin
IPC分类号： A61K31/553 , A61K31/551
CPC分类号： C07D403/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： 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.
摘要翻译：本发明提供了根据通式（1）的新化合物，其中A是双环或三环吖庚因衍生物，V 1和V 2均为H，OMe或F，或 V 1和V 2之一是Br，Cl，F，OH，OMe，OBn，OPh，O-酰基，N 3， NH 2，NHBn或NH-酰基，另一个是H，或V 1和V 2一起是-O，-O（CH O - 或-S（CH 2）n -S-; -S-（CH 2）n - O 1或O 2是O或S; X 1和X 2均为H或一起为-O或-S; Y是OR 5或NR 6 R 7; R 1，R 2，R 3和R 4独立地选自H，低级烷基，低级烷氧基，F，Cl和Br; R 5选自H和低级烷基; R 6和R 7独立地选自H和低级烷基，或者一起是 - （CH 2）n ; n = 3,4,5,6; p是2或3.化合物是加压素V2受体的激动剂，可用作抗利尿剂和促凝剂。本发明还包括掺入这些加压素激动剂的药物组合物，该组合物特别可用于治疗中枢性尿崩症，夜间遗尿和夜尿症。

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