BENZODIAZONINE DERIVATIVES BINDING TO CHOLECYSTOKININ OR GASTRIN RECEPTORS
    2.
    发明申请
    BENZODIAZONINE DERIVATIVES BINDING TO CHOLECYSTOKININ OR GASTRIN RECEPTORS 审中-公开
    苯并吖嗪衍生物与胆碱酯酶或胃蛋白酶受体结合

    公开(公告)号:WO1997032860A1

    公开(公告)日:1997-09-12

    申请号:PCT/GB1997000632

    申请日:1997-03-07

    IPC分类号: C07D245/06

    摘要: Compounds of formula (I), wherein one of U and V is -CHR -, and the other of U and V is selected from -N(COR )-, -CH(COR )-,-N(SO2R )- and -CH(SO2R )-, in which R is H, -COOR , -CONR R or -COR and R is H, C1 to C6 hydrocarbyl (in which up to three of the carbon atoms may be replaced by a nitrogen, oxygen or sulphur atom), or a group of the formula -Q-R wherein Q is a bond, -NR - (in which R is H or C1 to C3 alkyl) or -O-, and R is aryl, substituted aryl, arylalkyl or (substituted aryl)alkyl; R is independently C1 to C3 alkyl; R is H or C1 to C15 hydrocarbyl wherein one or more hydrogen atoms may be replaced by halogen atoms, and one carbon atom may be replaced by a nitrogen, oxygen or sulphur atom; R is independently halo, alkyl, alkoxy, -NO2, -NH2 or -NHCOR ; X is H and Y is H or C1 to C10 hydrocarbyl wherein one or more hydrogen atoms may be replaced by halogen atoms, and one carbon atom may be replaced by a nitrogen, oxygen or sulphur atom; or X and Y together are =O or =CH2; Z is H, C1 to C15 hydrocarbyl (in which one or more hydrogen atoms may be replaced by a halogen atom, and up to three of the carbon atoms may be replaced by a nitrogen, oxygen or sulphur atom), or -(CHR )m-R (wherein R is H or C1 to C3 alkyl and R is phenyl, substituted phenyl or a group of the formula -COOR or -CONR R , in which R and R are independently H or C1 to C6 alkyl, or R and R together form a propylene, butylene, pentylene or hexylene group); m is from 1 to 3; and n and p are independently from 0 to 3, and pharmaceutically acceptable salts thereof are ligands at gastrin and/or cholecystokinin receptors.

    摘要翻译: 式(I)化合物,其中U和V中的一个为-CHR 2 - ,U和V中的另一个选自-N(COR 4) - , - CH(COR 4) - ,-N(SO 2 R 4) - 和-CH(SO 2 R 4) - ,其中R 2是H,-COOR 5,-CONR 6 R 7或-COR 7 并且R 4是H,C 1至C 6烃基(其中最多三个碳原子可以被氮,氧或硫原子替代)或式-QR 16的基团,其中Q是 R 17 - (其中R 17是H或C 1至C 3烷基)或-O-,R 16是芳基,取代的芳基,芳基烷基或(取代的芳基)烷基; R独立地为C 1至C 3烷基; R 1是H或C 1至C 15烃基,其中一个或多个氢原子可以被卤素原子取代,并且一个碳原子可被氮,氧或硫原子代替; R 3独立地为卤素,烷基,烷氧基,-NO 2,-NH 2或-NHCOR 5; X是H,Y是H或C 1至C 10烃基,其中一个或多个氢原子可以被卤素原子代替,一个碳原子可以被氮,氧或硫原子代替; 或X和Y一起为= O或= CH 2; Z是H,C 1至C 15烃基(其中一个或多个氢原子可以被卤素原子替代,并且多达三个碳原子可以被氮,氧或硫原子替代),或 - (CHR )其中R 18是H或C 1至C 3烷基,R 8是苯基,取代的苯基或式-COOR 9或-CONR 9 R 10的基团 >其中R 9和R 10独立地为H或C 1至C 6烷基,或R 9和R 10一起形成丙烯,亚丁基,亚戊基或亚己基)。 m为1〜3; 且n和p独立地为0至3,其药学上可接受的盐是胃泌素和/或胆囊收缩素受体的配体。

    1H-4(5)-SUBSTITUTED IMIDAZOLE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS HISTAMINE H3 RECEPTOR LIGANDS
    4.
    发明申请
    1H-4(5)-SUBSTITUTED IMIDAZOLE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS HISTAMINE H3 RECEPTOR LIGANDS 审中-公开
    1H-4(5) - 取代的咪唑衍生物,它们的制备及其作为组胺H3受体配体的用途

    公开(公告)号:WO9905114A3

    公开(公告)日:1999-04-22

    申请号:PCT/GB9802067

    申请日:1998-07-14

    CPC分类号: C07D233/64 C07D417/04

    摘要: Compounds of formula (I) wherein R is selected from C1 to C6 alkyl, C1 to C6 alkoxy, C1 to C6 alkylthio, carboxy, carboxy (C1 to C6)alkyl, formyl, C1 to C6 alkylcarbonyl, C1 to C6 alkylcarbonylalkoxy, nitro, trihalomethyl, hydroxy, amino, C1 to C6 alkylamino, di(C1 to C6 alkyl)amino, aryl, C1 to C6 alkylaryl, halo, sulfamoyl and cyano; R is C1 to C20 hydrocarbylene, in which one or more hydrogen atoms may be replaced by halogen atoms and up to 6 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms, provided that R does not contain a -O-O- group, and provided also that the atom in R which is linked to the -SO2- moiety is a carbon atom; R is hydrogen or C1 to C15 hydrocarbyl, in which one or more hydrogen atoms may be replaced by halogen atoms and up to 3 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms, provided that R does not contain a -O-O- group; X is a bond or -NR -, wherein R is hydrogen or non-aromatic C1 to C5 hydrocarbyl (in which one or more hydrogen atoms may be replaced by halogen atoms and up to 2 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms, provided that R does not contain a -O-O- group), aryl(C1 to C3)alkyl or R represents a bond to R ; and a is from 0 to 2, and their pharmaceutically acceptable salts are useful as histamine H3 receptor ligands.

    摘要翻译: 其中R 1选自C 1 -C 6烷基,C 1 -C 6烷氧基,C 1 -C 6烷硫基,羧基,羧基(C 1 -C 6)烷基,甲酰基,C 1 -C 6烷基羰基,C 1 -C 6烷基羰基烷氧基 硝基,三卤代甲基,羟基,氨基,C1-C6烷基氨基,二(C1-C6烷基)氨基,芳基,C1-C6烷基芳基,卤素,氨磺酰基和氰基; R 2为C 1至C 20亚烃基,其中一个或多个氢原子可以被卤素原子置换,且至多6个碳原子可以被氧,氮或硫原子置换,条件是R 2不含 并且还提供了与-SO 2 - 部分连接的R 2中的原子是碳原子; R 3是氢或C 1至C 15烃基,其中一个或多个氢原子可以被卤素原子代替并且至多3个碳原子可以被氧,氮或硫原子代替,条件是R 3不是 包含一个-OO-组; X是键或-NR 4 - ,其中R 4是氢或非芳族C 1 -C 5烃基(其中一个或多个氢原子可以被卤素原子取代并且至多2个碳原子可以被取代 (其中R 4不含-OO-基团),芳基(C 1 -C 3)烷基或R 4表示与R 2的键; a为0-2,并且它们的药学上可接受的盐可用作组胺H3受体配体。

    HISTAMINE H3 RECEPTOR LIGANDS
    8.
    发明申请
    HISTAMINE H3 RECEPTOR LIGANDS 审中-公开
    组胺H3受体配体

    公开(公告)号:WO1997029092A1

    公开(公告)日:1997-08-14

    申请号:PCT/GB1997000358

    申请日:1997-02-10

    IPC分类号: C07D233/54

    CPC分类号: C07D233/64 C07D401/12

    摘要: Compounds of formula (I) or (II) wherein R is C4 to C20 hydrocarbyl (in which one or more hydrogen atoms may be replaced by halogen, and up to three carbon atoms may be replaced by oxygen, nitrogen or sulphur atoms, provided that R does not contain an -O-O- group), R is H or C1 to C3 alkyl, m is from 1 to 15, n is from 2 to 6, each X group is independently (a), or one X group is -N(R )-, -O- or -S- and the remaining X groups are independently (a), wherein R is H, C1 to C6 alkyl, -CO2R , -CONR 2, -CR 2OR or -OR (in which R and R are H or C1 to C3 alkyl), and R is H or C1 to C6 alkyl, each Y group is independently -C(R )R -, or up to two Y groups are -N(R )-, -O- or -S- and the remaining Y groups are independently -C(R )R -, wherein R is as defined above, one R group in the structure is imidazoyl or imidazoylalkyl and the remaining R groups are H or C1 to C6 alkyl, and Z is > C(R )NR - or > N-, wherein R is any of the groups recited above for R , and pharmaceutically acceptable salts thereof are ligands at histamine H3 receptors.

    摘要翻译: 其中R 1为C 4 -C 20烃基(其中一个或多个氢原子可被卤素取代,最多三个碳原子)可以被氧,氮或硫原子代替的式(I)或(II)化合物 条件是R 1不含-OO-基),R 2为H或C 1至C 3烷基,m为1至15,n为2至6,每个X基团独立地为(a )或一个X基团是-N(R 4) - , - O-或-S-,其余的X基团独立地为(a),其中R 3为H,C 1至C 6烷基,-CO 2 R -CONR 5,-CR 5 OR 2或-OR 5(其中R 5和R 6为H或C 1至C 3烷基) 4>是H或C 1至C 6烷基,每个Y基团独立地是-C(R 3)R 4 - 或至多两个Y基团是-N(R 4) - , - O-或 -S-,其余的Y基团独立地是-C(R 3)R 4 - ,其中R 3如上定义,结构中的一个R 4基团是咪唑基或咪唑基烷基,剩余的 R 4基团是H或C 1至C 6烷基,Z是> C(R 7)NR 2 - 或> N-,其中R 7是任何基团 R 3所示的化合物及其药学上可接受的盐是组胺H3受体的配体。