Certain phosphonic acid quinoline-2-carboxylic acids, esters or amides
useful for treatment of disorders responsive to N-methyl D-aspartate
receptor blockade
    21.
    发明授权
    Certain phosphonic acid quinoline-2-carboxylic acids, esters or amides useful for treatment of disorders responsive to N-methyl D-aspartate receptor blockade 失效
    某些膦酸喹啉-2-羧酸,酯或酰胺可用于治疗对N-甲基D-天冬氨酸受体阻断作用的病症

    公开(公告)号:US5217963A

    公开(公告)日:1993-06-08

    申请号:US738073

    申请日:1991-07-30

    摘要: The present invention is concerned with the phosphonic acids of formula I ##STR1## wherein one or both of the acidic hydroxy groups of the phosphonic acid moiety may be functionalized in form of pharmaceutically acceptable mono- or di- esters; wherein Y represents optionally substituted 2-carboxytetrahydroquinolinyl or 2-carboxyperhydroquinolinyl, and in each of which the carboxy group may be functionalized in form of a pharmaceutically acceptable ester or amide; A represents a direct bond, lower alkenylene, lower alkylidene or lower alkylene; and pharmaceutically acceptable salts thereof; which are useful for the treatment of nervous system disorders in mammals and as antagonists of the N-methyl-D-aspartate sensitive excitatory amino acid receptor.

    摘要翻译: 本发明涉及式I(I)的膦酸,其中膦酸部分的一个或两个酸性羟基可以以药学上可接受的单酯或二酯的形式官能化; 其中Y表示任选取代的2-羧基四氢喹啉基或2-羧基全氢化喹啉基,并且其中的每一个可以以药学上可接受的酯或酰胺的形式官能化; A表示直接键合,低级亚烯基,低级亚烷基或低级亚烷基; 及其药学上可接受的盐; 其可用于治疗哺乳动物中的神经系统疾病和作为N-甲基-D-天冬氨酸敏感性兴奋性氨基酸受体的拮抗剂。

    Certain benzopyran and benzothiopyran derivatives

    公开(公告)号:US5155130A

    公开(公告)日:1992-10-13

    申请号:US595153

    申请日:1990-10-10

    IPC分类号: C07D311/58 C07D335/06

    CPC分类号: C07D335/06 C07D311/58

    摘要: The invention relates to the compounds of the formula ##STR1## wherein each R independently represents hydrogen, lower alkyl, halogen, trifluoromethyl, lower alkoxy, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryloxy, carbocyclic or heterocyclic aryl-lower alkyloxy, carbocyclic or heterocyclic aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyloxy, or C.sub.3 -C.sub.7 -cycloalkyloxy; R.sub.1 represents hydrogen, lower alkyl or carbocyclic aryl; R.sub.2 represents hydrogen or lower alkyl; Y represents oxygen (O), sulfur (S), sulfinyl or sulfonyl; n represents 1, 2 or 3; A represents a direct bond or lower alkylene; Z represents ##STR2## wherein R.sub.3 represents hydrogen or acyl; R.sub.4 represents lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, or C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl; or Z represents ##STR3## wherein X represents oxygen or sulfur, R.sub.3 represents hydrogen, acyl, lower alkoxycarbonyl, aminocarbonyl, mono- or di-lower alkylaminocarbonyl, lower alkenylaminocarbonyl, lower alkynylaminocarbonyl, carbocyclic or heterocyclic aryl-lower alkylaminocarbonyl, carbocyclic or heterocyclic arylamino-carbonyl; C.sub.3 -C.sub.7 -cycloalkylaminocarbonyl, or C.sub.3 -C.sub.7 -cycloalkyl-lower alkylaminocarbonyl; R.sub.5 represents lower alkyl, lower alkoxycarbonyl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, amino, mono- or di-lower alkylamino, lower alkenylamino, lower alkynylamino, carbocyclic or heterocyclic aryl-lower alkylamino, carbocyclic or heterocyclic arylamino, C.sub.3 -C.sub.7 -cycloalkylamino, C.sub.3 -C.sub.7 -cycloalkyl-lower alkylamino, lower alkoxycarbonyl-lower alkylamino, or lower alkoxy; R.sub.6 and R.sub.7 independently represent hydrogen or lower alkyl; and pharmaceutically acceptable salts thereof; which are useful as 5-lipoxygenase inhibitors.

    Certain 2-carboxypiperidyl-alkylene phosphonic acids and esters thereof
useful for the treatment of disorders responsive to
N-methyl-D-aspartate receptor blockade
    24.
    发明授权
    Certain 2-carboxypiperidyl-alkylene phosphonic acids and esters thereof useful for the treatment of disorders responsive to N-methyl-D-aspartate receptor blockade 失效
    某些2-羧基哌啶基亚烷基膦酸及其酯可用于治疗对N-甲基-D-天冬氨酸受体阻断作用的病症

    公开(公告)号:US4906621A

    公开(公告)日:1990-03-06

    申请号:US124226

    申请日:1987-11-23

    摘要: The present invention is concerned with the phosphonic acids of formula I ##STR1## wherein one or both of the acidic hydroxy groups of the phosphonic acid moiety may be functionalized in form of pharmaceutically acceptable mono- or di- esters; wherein Y represents optionally substituted 2-carboxypyrrolidinyl, 2-carboxy-2,5-dihydropyrrolyl, 2-carboxy-1,2,3,6-tetrahydropyridinyl, 2-carboxy-1,2,5,6-tetrahydropyridinyl, 2-carboxypiperidinyl, 2-carboxytetrahydroquinolinyl or 2-carboxyperhydroquinolinyl, 2-carboxy-2,3-dihydroindolyl or 2-carboxyperhydroindolyl as described herein, and in each of which the carboxy group may be functionalized in form of a pharmaceutically acceptable ester or amide; A represents a direct bond, lower alkenylene, lower alkylidene or lower alkylene provided that A does not represent a direct bond when Y represents 2-carboxypyrrolidinyl; and pharmaceutically acceptable salts thereof; which are useful for the treatment of nervous system disorders in mammals and as antagonists of the N-methyl-D-aspartate sensitive excitatory amino acid receptor.

    摘要翻译: 本发明涉及式I(I)的膦酸,其中膦酸部分的一个或两个酸性羟基可以以药学上可接受的单酯或二酯的形式官能化; 其中Y表示任选取代的2-羧基吡咯烷基,2-羧基-2,5-二氢吡咯基,2-羧基-1,2,3,6-四氢吡啶基,2-羧基-1,2,5,6-四氢吡啶基,2-羧基哌啶基 ,2-羧基四氢喹啉基或2-羧基全氢化喹啉基,2-羧基-2,3-二氢吲哚基或2-羧基全氢吲哚,并且其中的每一个可以以药学上可接受的酯或酰胺的形式官能化; A表示直接键,低级亚烯基,低级亚烷基或低级亚烷基,条件是当Y表示2-羧基吡咯烷基时,A不表示直接键; 及其药学上可接受的盐; 其可用于治疗哺乳动物中的神经系统疾病和作为N-甲基-D-天冬氨酸敏感性兴奋性氨基酸受体的拮抗剂。

    Certain 2-carboxypiperidyl-(alkylene or alkenylene)-phosphonic acids and
esters thereof useful for the treatment of disorders responsive to
n-methyl-d-aspartate receptor blockade
    25.
    发明授权
    Certain 2-carboxypiperidyl-(alkylene or alkenylene)-phosphonic acids and esters thereof useful for the treatment of disorders responsive to n-methyl-d-aspartate receptor blockade 失效
    某些2-羧基哌啶基 - (亚烷基或亚烯基) - 膦酸及其酯可用于治疗对甲基-d-天冬氨酸受体阻断作用的病症

    公开(公告)号:US4898854A

    公开(公告)日:1990-02-06

    申请号:US217120

    申请日:1988-07-11

    摘要: The present invention is concerned with the phosphonic acids of formula I ##STR1## wherein one or both of the acidic hydroxy groups of the phosphonic acid moiety may be functionalized in form of pharmaceutically acceptable mono- or di- esters; wherein Y represents optionally substituted 2-carboxypyrrolidinyl, 2-carboxy-2,5-dihydropyrrolyl, 2-carboxy-1,2,3,6-tetrahydropyridinyl, 2-carboxy-1,2,5,6-tetrahydropyridinyl, 2-carboxypiperidinyl, 2-carboxytetrahydroquinolinyl or 2-carboxyperhydroquinolinyl, 2-carboxy-2,3-dihydroindolyl or 2-carboxyperhydroindolyl as described herein, and in each of which the carboxy group may be functionalized in form of a pharmaceutically acceptable ester or amide; A represents a direct bond, lower alkenylene, lower alkylidene or lower alkylene provided that A does not represent a direct bond when Y represents 2-carboxypyrrolidinyl; and pharmaceutically acceptable salts thereof; which are useful for the treatment of nervous system disorders in mammals and as antagonists of the N-methyl-D-aspartate sensitive excitatory amino acid receptor.

    摘要翻译: 本发明涉及式I(I)的膦酸,其中膦酸部分的一个或两个酸性羟基可以以药学上可接受的单酯或二酯的形式官能化; 其中Y表示任选取代的2-羧基吡咯烷基,2-羧基-2,5-二氢吡咯基,2-羧基-1,2,3,6-四氢吡啶基,2-羧基-1,2,5,6-四氢吡啶基,2-羧基哌啶基 ,2-羧基四氢喹啉基或2-羧基全氢化喹啉基,2-羧基-2,3-二氢吲哚基或2-羧基全氢吲哚,并且其中的每一个可以以药学上可接受的酯或酰胺的形式官能化; A表示直接键,低级亚烯基,低级亚烷基或低级亚烷基,条件是当Y表示2-羧基吡咯烷基时,A不表示直接键; 及其药学上可接受的盐; 其可用于治疗哺乳动物中的神经系统疾病和作为N-甲基-D-天冬氨酸敏感性兴奋性氨基酸受体的拮抗剂。