12-halogenated forskolin derivatives
    51.
    发明授权
    12-halogenated forskolin derivatives 失效
    12卤代福斯克林衍生物

    公开(公告)号:US5023344A

    公开(公告)日:1991-06-11

    申请号:US522754

    申请日:1990-05-14

    CPC分类号: C07D407/12 C07D311/92

    摘要: Novel 12-halogenated forskolin derivatives, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.

    摘要翻译: 公开了新型12-卤化的福斯克林衍生物,其中间体及其制备方法,以及利用化合物或其组合物降低眼内压的方法。

    Method of preparing isoxazolo(5,4,3-kl)acridines
    53.
    发明授权
    Method of preparing isoxazolo(5,4,3-kl)acridines 失效
    异恶唑(5,4,3-kl)吖啶的制备方法

    公开(公告)号:US4942237A

    公开(公告)日:1990-07-17

    申请号:US494188

    申请日:1990-02-12

    IPC分类号: C07D498/06

    CPC分类号: C07D498/06

    摘要: There are disclosed compounds having the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, halogen or trifluoromethyl, andR when present is hydrogen, loweralkyl, allyl, arylloweralkyl, ##STR2## wherein R.sub.1 is loweralkyl, --CH.sub.2 C.tbd.CH, ##STR3## n being 2, 3 or 4 and R.sub.2 and R.sub.3 being independently loweralkyl, or the group ##STR4## taken as a whole constituting ##STR5## which compounds are useful as analgesic agents and also for the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease.

    摘要翻译: 公开了具有式“IMAGE”的化合物,其中X为氢,低级烷基,低级烷氧基,卤素或三氟甲基,R为氢,低级烷基,烯丙基,芳基低级烷基,其中R 1为低级烷基,-CH 2 C 3 CH 3, IMAGE> n为2,3或4,R2和R3独立地为低级烷基,或者组成整体构成 + TR ,该化合物可用作止痛剂,也可用于 治疗以胆碱能功能降低为特征的各种记忆障碍功能如阿尔茨海默病。

    4-(Benzisothiazol-3-yl)phenoxyacetic acid 1',1'-dioxides as diuretics
    54.
    发明授权
    4-(Benzisothiazol-3-yl)phenoxyacetic acid 1',1'-dioxides as diuretics 失效
    4-(苯并异噻唑-3-基)苯氧基乙酸1',1'-二氧化物作为利尿剂

    公开(公告)号:US4868188A

    公开(公告)日:1989-09-19

    申请号:US439098

    申请日:1982-11-03

    摘要: Novel 4-(benzisothiazol-3-yl)phenoxyacetic acid 1',1'-dioxides of the formula ##STR1## where X is hydrogen, halogen or loweralkyl; R.sub.1 is hydrogen or loweralkyl; R.sub.2 and R.sub.3 are each independently Cl, Br or CH.sub.3, and related compounds, methods for preparing same and methods of treatment by administering compositions containing such a compound are described. These compounds are useful as diuretics.

    摘要翻译: 新的4-(苯并异噻唑-3-基)苯氧基乙酸1',1'-二氧化物,其中X是氢,卤素或低级烷基; R1是氢或低级烷基; R 2和R 3各自独立地为Cl,Br或CH 3,并且描述了相关化合物,其制备方法和通过施用含有这种化合物的组合物的治疗方法。 这些化合物可用作利尿剂。

    9-Amino-3,4-dihydroacridines and related compounds useful for enhancing
memory
    55.
    发明授权
    9-Amino-3,4-dihydroacridines and related compounds useful for enhancing memory 失效
    9-氨基-3,4-二氢吖啶和有助于增强记忆的相关化合物

    公开(公告)号:US4839364A

    公开(公告)日:1989-06-13

    申请号:US7885

    申请日:1987-01-28

    摘要: There are disclosed compounds having the formula ##STR1## wherein n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, NHCOR.sub.2 where R.sub.2 is loweralkyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl; Y is C.dbd.O or CR.sub.5 OH where R.sub.5 is hydrogen or loweralkyl; Z is CH.sub.2 or C.dbd.CR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are independently hydrogen or loweralkyl; or Y and Z taken together is CR.sub.5 .dbd.Ch where CR.sub.5 and CH correspond to Y and Z respectively; an optical antipode thereof, or a pharmaceutically acceptable acid addition salt thereof, which are useful for enhancing memory, methods for synthesizing them, and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.

    摘要翻译: 公开了具有式“IMAGE”的化合物,其中n为1,2或3; X是氢,低级烷基,低级烷氧基,卤素,羟基,硝基,三氟甲基,NHCOR 2,其中R2是低级烷基,或NR3R4,其中R3和R4独立地是氢或低级烷基; R是氢或低级烷基; R 1是氢,低级烷基,二低级烷基氨基低级烷基,芳基低级烷基,二芳基低级烷基,呋喃基烷基,噻吩基低级烷基,氧桥连的芳基低级烷基,氧桥连的二芳基低级烷基,氧桥连的呋喃基低级烷基或氧桥连的噻吩基低级烷基。 Y是C = O或CR5OH,其中R5是氢或低级烷基; Z是CH 2或C = CR 6 R 7,其中R 6和R 7独立地是氢或低级烷基; 或Y和Z一起为CR5 = Ch,其中CR5和CH分别对应于Y和Z; 可用于增强记忆力的光学对映体或其药学上可接受的酸加成盐,以及合成它们的方法和包含有效记忆增加量的这种化合物的药物组合物。

    Method of preparing 9-amino-1,2,3,4,-tetrahydroacridin-1-ones and
related compounds
    56.
    发明授权
    Method of preparing 9-amino-1,2,3,4,-tetrahydroacridin-1-ones and related compounds 失效
    制备9-氨基-1,2,3,4-四氢吖啶-1-酮和相关化合物的方法

    公开(公告)号:US4835275A

    公开(公告)日:1989-05-30

    申请号:US125109

    申请日:1987-11-25

    摘要: There are disclosed compounds having the formula ##STR1## wherein n is 1, 2 or 3; X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, NHCOR.sub.2 where R.sub.2 is loweralkyl, or NR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, furylloweralkyl, thienylloweralkyl, oxygen-bridged arylloweralkyl, oxygen-bridged diarylloweralkyl, oxygen-bridged furylloweralkyl or oxygen-bridged thienylloweralkyl; Y is C.dbd.O or CR.sub.5 OH where R.sub.5 is hydrogen or loweralkyl; Z is CH.sub.2 or C.dbd.CR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are independently hydrogen or loweralkyl; or Y and Z taken together is CR.sub.5 .dbd.CH where CR.sub.5 and CH correspond to Y and Z respectively; an optical antipode thereof, or a pharmaceutically acceptable acid addition salt thereof, which are useful for enhancing memory, methods for synthesizing them, and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.

    摘要翻译: 公开了具有式“IMAGE”的化合物,其中n为1,2或3; X是氢,低级烷基,低级烷氧基,卤素,羟基,硝基,三氟甲基,NHCOR 2,其中R2是低级烷基,或NR3R4,其中R3和R4独立地是氢或低级烷基; R是氢或低级烷基; R 1是氢,低级烷基,二低级烷基氨基低级烷基,芳基低级烷基,二芳基低级烷基,呋喃基烷基,噻吩基低级烷基,氧桥连的芳基低级烷基,氧桥连的二芳基低级烷基,氧桥连的呋喃基低级烷基或氧桥连的噻吩基低级烷基。 Y是C = O或CR5OH,其中R5是氢或低级烷基; Z是CH 2或C = CR 6 R 7,其中R 6和R 7独立地是氢或低级烷基; 或Y和Z一起为CR5 = CH,其中CR5和CH分别对应于Y和Z; 可用于增强记忆力的光学对映体或其药学上可接受的酸加成盐,以及合成它们的方法和包含有效记忆增加量的这种化合物的药物组合物。

    6H-isoxazolo(5,4-d)pyrazolo(3,4-b)pyridines, and their use as
antihypertensive and analgesic agents
    57.
    发明授权
    6H-isoxazolo(5,4-d)pyrazolo(3,4-b)pyridines, and their use as antihypertensive and analgesic agents 失效
    6H-异恶唑(5,4-d)吡唑并(3,4-b)吡啶,并且它们用作抗高血压和止痛剂

    公开(公告)号:US4622326A

    公开(公告)日:1986-11-11

    申请号:US812590

    申请日:1985-12-23

    CPC分类号: C07D471/04

    摘要: There are disclosed compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, aryl or heteroaryl; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkyl, loweralkoxyloweralkyl, cycloalkyl, arylloweralkyl or heteroarylmethyl; and R.sub.4 is hydrogen or loweralkyl; or a pharmaceutically acceptable acid addition salt thereof, which are useful for alleviating pain and lowering blood pressure, methods for synthesizing them, and pharmaceutical compositions comprising an effective amount of such a compound.

    摘要翻译: 公开了具有式“IMAGE”的化合物,其中R 1是氢,低级烷基,芳基低级烷基,芳基或杂芳基; R2是氢或低级烷基; R3为低级烷基,低级烷氧基低级烷基,环烷基,芳基低级烷基或杂芳基甲基; 和R4是氢或低级烷基; 或其药学上可接受的酸加成盐,其可用于缓解疼痛和降低血压,合成它们的方法和包含有效量的这种化合物的药物组合物。