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公开(公告)号:US5618812A
公开(公告)日:1997-04-08
申请号:US374748
申请日:1995-01-26
申请人: Jose L. Castro Pineiro , William R. Carling , Mark S. Chambers , Stephen R. Fletcher , Sarah C. Hobbs , Victor G. Matassa , Kevin W. Moore , Graham A. Showell , Michael G. Russell
发明人: Jose L. Castro Pineiro , William R. Carling , Mark S. Chambers , Stephen R. Fletcher , Sarah C. Hobbs , Victor G. Matassa , Kevin W. Moore , Graham A. Showell , Michael G. Russell
IPC分类号: A61K31/55 , A61K31/551 , A61K31/5513 , A61P1/00 , A61P1/04 , A61P1/12 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/26 , A61P25/30 , A61P27/06 , A61P35/00 , A61P39/00 , A61P43/00 , C07D221/24 , C07D243/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D413/04 , C07D453/06 , C07D471/08 , C07D487/08 , C07D491/10 , C07D491/107 , C07D491/113
CPC分类号: C07D401/04 , C07D221/24 , C07D243/14 , C07D401/12 , C07D403/04 , C07D453/06 , C07D487/08 , C07D491/10
摘要: Compounds of Formula (I), and salts and prodrugs thereof, wherein R.sup.1 represents H, optionally substituted C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 is NHR.sup.12 or (CH.sub.2).sub.s R.sup.13 where 5 is 0, 1 or 2; R.sup.3 represents C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; R.sup.4 and R.sup.5 are H, C.sub.1-12 alkyl optionally substituted by NR.sup.9 R.sup.9' or an azacyclic or azabicyclic group, optionally substituted C.sub.4-9 cycloalkyl, C.sub.4-9 cycloalkyl C.sub.1-4 alkyl, aryl, arylC.sub.1-6 alkyl or azacyclic or azabicyclic groups, or R.sup.4 and R.sup.5 together form the residue of an optionally substituted azacyclic or azabicyclic ring system; x is 0, 1, 2 or 3; R.sup.12 is optionally substituted phenyl or pyridyl; R.sup.13 represents a group (A) wherein R.sup.14 is H or C.sub.1-6 alkyl; R.sup.15 is H, C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; and the dotted line is an optional covalent bond; are CCK and/or gastrin antagonists useful in therapy. ##STR1##
摘要翻译: PCT No.PCT / GB93 / 01599 Sec。 371日期1995年1月26日 102(e)日期1995年1月26日PCT提交1993年7月28日PCT公布。 出版物WO94 / 03437 日期:1994年2月17日式(I)化合物及其盐和前药,其中R 1表示H,任选取代的C 1-6烷基或C 3-7环烷基; R2是NHR12或(CH2)sR13,其中5是0,1或2; R 3表示C 1-6烷基,卤代或NR 6 R 7; R 4和R 5是H,任选地被NR 9 R 9'或氮杂环或氮杂双环基团任选取代的C 1-12烷基,任选取代的C 4-9环烷基,C 4-9环烷基C 1-4烷基,芳基,芳基C 1-6烷基或氮杂环或氮杂双环基,或R 4和R 5一起 形成任选取代的氮杂环或氮杂双环系的残基; x为0,1,2或3; R 12是任选取代的苯基或吡啶基; R 13表示其中R 14为H或C 1-6烷基的基团(A) R 15是H,C 1-6烷基,卤素或NR 6 R 7; 并且虚线是任选的共价键; 是用于治疗的CCK和/或胃泌素拮抗剂。 (图)(一)