Biphenyl vasopressin agonists
    22.
    发明授权
    Biphenyl vasopressin agonists 失效
    联苯加压素激动剂

    公开(公告)号:US07465722B2

    公开(公告)日:2008-12-16

    申请号:US11502982

    申请日:2006-08-11

    IPC分类号: C07D487/02 A61K31/551

    摘要: A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or(2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or(2) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, (C1-C6) lower alkoxy, or halogen; or(3) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; represents a 5-membered aromatic (unsaturated) heterocyclic ring having one sulfur atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; R1 is a moiety of the formula and R2, R3, R7, R8 and R9 are, independently, selected from a group consisting of hydrogen, (C1-C3) lower alkyl, OCH3, halogen, CF3, —SCH3, OCF3, SCF3, or CN; or a pharmaceutically acceptable salt, or pro-drug form thereof.

    摘要翻译: 式(I)或(II)的化合物:其中:Y是选自NR或 - (CH 2)n的部分; 其中R是氢或(C1-C6)低级烷基,n是1; (C1-C6)低级烷基,卤素,氰基,CF3,羟基,(C1-C6)低级烷氧基,(C1-C6)低级烷氧基,(C1-C6)低级烷氧基,(C1-C6) C 1 -C 6低级烷氧基羰基,羧基-CONH 2,-CONH [(C 1 -C 6)低级烷基],-CON [(C 1 -C 6)低级烷基] 或(2)任选被(C 1 -C 6)低级烷基,卤素或(C 1 -C 6)低级烷氧基取代的具有一个氮原子的6元芳族(不饱和)杂环; 表示:(1)任选被一个或两个取代基取代的苯环,所述取代基独立地选自氢,(C 1 -C 6)低级烷基,卤素,氰基,CF 3,羟基,(C 1 -C 6)低级烷氧基或 (C 1 -C 6)低级烷氧基羰基,羧基,-CONH 2,-CONH [(C 1 -C 6)低级烷基],-CON [(C 1 -C 6)低级烷基] 或(2)任选被(C 1 -C 6)低级烷基,(C 1 -C 6)低级烷氧基或卤素取代的具有一个氮原子的5元芳族(不饱和)杂环; 或(3)具有一个氮原子,任选被(C 1 -C 6)低级烷基,卤素或(C 1 -C 6)低级烷氧基取代的6元芳族(不饱和)杂环; 表示任选被(C 1 -C 6)低级烷基,卤素或(C 1 -C 6)低级烷氧基取代的具有一个硫原子的5元芳族(不饱和)杂环; R1是下式的部分,R2,R3,R7,R8和R9独立地选自氢,(C1-C3)低级烷基,OCH3,卤素,CF3,-SCH3,OCF3,SCF3, 或CN; 或其药学上可接受的盐或其前体药物形式。

    Biphenyl vasopressin agonists
    23.
    发明授权

    公开(公告)号:US07223752B2

    公开(公告)日:2007-05-29

    申请号:US10980939

    申请日:2004-11-04

    摘要: A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1–C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1–C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1–C6) lower alkoxy, (C1–C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1–C6) lower alkyl], —CON[(C1–C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1–C6) lower alkyl, halogen or (C1–C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1–C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1–C6) lower alkoxy, or (C1–C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1–C6) lower alkyl], —CON[(C1–C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1–C6) lower alkyl, (C1–C6) lower alkoxy, or halogen; or (3) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1–C6) lower alkyl, halogen, or (C1–C6) lower alkoxy; represents a 5-membered aromatic (unsaturated) heterocyclic ring having one sulfur atom, optionally substituted by (C1–C6) lower alkyl, halogen, or (C1–C6) lower alkoxy; R1 is a moiety of the formula and R2, R3, R7, R8 and R9 are, independently, selected from a group consisting of hydrogen, (C1–C3) lower alkyl, OCH3, halogen, CF3, —SCH3, OCF3, SCF3, or CN; or a pharmaceutically acceptable salt, or pro-drug form thereof.

    N-oxides of 5-oxo-1-phenyl-2-benzazepines
    26.
    发明授权
    N-oxides of 5-oxo-1-phenyl-2-benzazepines 失效
    5-氧代-1-苯基-2-苯并吖庚因的N-氧化物

    公开(公告)号:US4469633A

    公开(公告)日:1984-09-04

    申请号:US324292

    申请日:1981-11-23

    摘要: Compounds of the formula ##STR1## wherein X and Y are selected from the group consisting of hydrogen, halogen and trifluoromethyl, are disclosed.The compounds are useful as intermediates in the production of 2-benzazepines, compounds of pharmacological activity.Also disclosed are other intermediates and processes for their production.

    摘要翻译: 公开了其中X和Y选自氢,卤素和三氟甲基的式“IMAGE”的化合物。 该化合物可用作生产2-苯并氮杂的药物活性化合物的中间体。 还公开了其生产的其它中间体和方法。

    Production of 2-benzazepines
    27.
    发明授权
    Production of 2-benzazepines 失效
    生产2-苯并氮杂

    公开(公告)号:US4394311A

    公开(公告)日:1983-07-19

    申请号:US324208

    申请日:1981-11-23

    摘要: Compounds of the formula ##STR1## wherein X and Y are selected from the group consisting of hydrogen, halogen and trifluoromethyl, are disclosed.The compounds are useful as intermediates in the production of 2-benzazepines, compounds of pharmacological activity.Also disclosed are other intermediates and processes for their production.

    摘要翻译: 公开了其中X和Y选自氢,卤素和三氟甲基的式“IMAGE”的化合物。 该化合物可用作生产2-苯并氮杂的药物活性化合物的中间体。 还公开了其生产的其它中间体和方法。