Tricyclic compounds
    4.
    发明授权
    Tricyclic compounds 失效
    三环化合物

    公开(公告)号:US5248679A

    公开(公告)日:1993-09-28

    申请号:US919265

    申请日:1992-07-27

    CPC分类号: C07D471/06 C07D487/06

    摘要: The invention relates to novel cholecystokinin antagonists of the formula ##STR1## wherein R.sup.1 is aryl which may have suitable substituent(s), X is --O-- or ##STR2## in which R.sup.3 is hydrogen or lower alkyl, A is bond; or methylene, ethylene, trimethylene, tetramethylene, pentamethylene or hexamethylene, each of which may have lower alkyl group(s), andR.sup.2 is heterocyclic(C.sub.3 -C.sub.6) alkenoyl or heterocycliciccarbonyl, or a pharmaceutically acceptable salt thereof, useful as a cholecystokinin antagonist.

    摘要翻译: 本发明涉及新颖的式“IMAGE”胆囊囊素拮抗剂,其中R 1为可具有合适取代基的芳基,X为-O-或其中R 3为氢或低级烷基,A为键; 或亚甲基,亚乙基,三亚甲基,四亚甲基,五亚甲基或六亚甲基,各自可以具有低级烷基,R 2为可用作缩胆囊素拮抗剂的杂环(C 3 -C 6)烯酰基或杂环羰基或其药学上可接受的盐 。

    Tricyclic compounds
    6.
    发明授权
    Tricyclic compounds 失效
    三环化合物

    公开(公告)号:US5401737A

    公开(公告)日:1995-03-28

    申请号:US77607

    申请日:1993-07-23

    CPC分类号: C07D471/06 C07D487/06

    摘要: The invention relates to a compound of the formula ##STR1## wherein R.sup.1 is aryl which may have suitable substituent(s), X is --O-- or ##STR2## in which R.sup.3 is hydrogen or lower alkyl, A is a bond or lower alkylene which may have lower alkyl group(s), andR.sup.2 is arylcarbamoyl which may have halogen or lower alkoxy,or a pharmaceutically acceptable salt thereof, useful as a cholecystokinin antagonist.

    摘要翻译: 本发明涉及式IMA的化合物,其中R 1是可具有合适取代基的芳基,X是-O-或其中R 3是氢或低级烷基,A是键或低级亚烷基 其可以具有低级烷基,并且R 2是可用作缩胆囊素拮抗剂的可具有卤素或低级烷氧基的芳基氨基甲酰基或其药学上可接受的盐。

    Benzodiazepine derivatives
    7.
    发明授权
    Benzodiazepine derivatives 失效
    苯并二氮杂衍生物

    公开(公告)号:US5382664A

    公开(公告)日:1995-01-17

    申请号:US103236

    申请日:1993-08-09

    摘要: Intermediates of the formula: ##STR1## wherein R.sup.1 is tetrazolyl or imidazolyl, each of which may have an imino protective group,R.sup.2 is phenyl which may have a halogen atom,R.sup.3 is hydrogen or halogen, andA is lower alkylene, or a salt thereof.They are useful in the preparation of benzodiazepine derivatives and pharmaceutically acceptable salts thereof which are cholecystokinin (CCK) antagonists and therefore can be used as therapeutical agents for emesis, pancreatitis, satiety and appetite control, pain control, insulinoma, gastroparesis, acute obstructive cholecystitis, irritable bowel disease and carcinoma of pancreas.

    摘要翻译: 下式的中间体:其中R1是四唑基或咪唑基,其各自可以具有亚氨基保护基,R 2是可以具有卤素原子的苯基,R 3是氢或卤素,A是低级亚烷基或盐 其中。 它们可用于制备作为胆囊收缩素(CCK)拮抗剂的苯并二氮杂衍生物及其药学上可接受的盐,因此可用作呕吐,胰腺炎,饱腹感和食欲控制,疼痛控制,胰岛素瘤,胃轻瘫,急性阻塞性胆囊炎, 肠易激综合征和胰腺癌。

    Tricyclic compounds
    8.
    发明授权
    Tricyclic compounds 失效
    三环化合物

    公开(公告)号:US5155101A

    公开(公告)日:1992-10-13

    申请号:US612955

    申请日:1990-11-15

    CPC分类号: C07D471/06 C07D487/06

    摘要: The invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is aryl which may have suitable substituents(s), X is --O-- or ##STR2## in which R.sup.3 is hydrogen or lower alkyl, A is a bond or lower alkylene which may have lower alkyl group(s), andR.sup.2 is hydrogen; heterocyclic(lower)alkenoyl which may have carboxy or protected carboxy; heterocycliccarbonyl which may have N,N-di(lower)alkylamino(lower)alkyl, hydroxyimino(lower)alkyl, aryliminio(lower)alkyl, acyl or hydroxy(lower)alkylheterocyclic(lower)alkyl; aroyl which may have 1 to 3 substituent(s) selected from the group consisting of halogen, amino and mono(or di or tri)halo(lower)alkyl; arylcarbamoyl which may have halogen or lower alkoxy; arylamino(lower)alkanoyl; or ar(lower)alkanoyl which may have amino or protected amino,or a pharmaceutically acceptable salt thereof, useful as a cholecystokinin antagonist.

    摘要翻译: 本发明涉及下式的化合物:其中R 1为可具有合适取代基的芳基,X为-O-或其中R 3为氢或低级烷基,A为键或低级 可以具有低级烷基的亚烷基,并且R 2是氢; 可以具有羧基或被保护的羧基的杂环(低级)烯酰基; 可以具有N,N-二(低级)烷基氨基(低级)烷基,羟基亚氨基(低级)烷基,芳基亚氨基(低级)烷基,酰基或羟基(低级)烷基杂环(低级)烷基)的杂环羰基; 芳酰基,其可以具有1至3个选自卤素,氨基和单(或二或三)卤代(低级)烷基的取代基; 可以具有卤素或低级烷氧基的芳基氨基甲酰基; 芳基氨基(低级)烷酰基; 或可具有氨基或被保护的氨基的芳(低级)烷酰基或其药学上可接受的盐作为缩胆囊素拮抗剂。

    Triazine derivatives, and pharmaceutical compositions comprising the same
    10.
    发明授权
    Triazine derivatives, and pharmaceutical compositions comprising the same 失效
    三嗪衍生物和包含其的药物组合物

    公开(公告)号:US4618610A

    公开(公告)日:1986-10-21

    申请号:US603173

    申请日:1984-04-23

    CPC分类号: C07D253/06

    摘要: New triazine derivatives represented by the formula: ##STR1## wherein R.sup.1 is hydrogen or halogen;R.sup.2 is a hydroxy, protected hydroxy, amino, cyano, mercapto, lower alkylthio, arylthio, sulfamoyl, lower alkylsulfonylamino, lower alkylureido, arylureido, lower alkyl-thioureido, aryl-thioureido, lower alkenoylamino, lower alkoxycarbonylamino, lower alkoxy(thiocarbonyl)thio, or cyclic or acyclic alkanoylamino in which the cyclic and acyclic alkanoylamino group may have a substituent selected from lower alkoxy, aryl, hydroxyaryl and protected hydroxyaryl; andX is O or S;and pharmaceutically acceptable salt thereof, which are useful in the treatment of hypertension, thrombosis and ulcer in human beings and animals.

    摘要翻译: 由下式表示的新的三嗪衍生物:其中R 1是氢或卤素; R2是羟基,保护的羟基,氨基,氰基,巯基,低级烷硫基,芳硫基,氨磺酰基,低级烷基磺酰基氨基,低级烷基脲基,芳基脲基,低级烷基 - 硫脲基,芳基 - 硫脲基,低级烯酰基氨基,低级烷氧基羰基氨基,低级烷氧基(硫代羰基) 或环状或无环烷酰氨基,其中环状和非环状烷酰基氨基可以具有选自低级烷氧基,芳基,羟基芳基和被保护的羟基芳基的取代基; X为O或S; 和其药学上可接受的盐,其可用于治疗人和动物中的高血压,血栓形成和溃疡。