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35 条记录 (耗时 0.036 秒)

    N.sub.9 -cyclopentyl-substituted adenine derivatives useful as adenosine receptor agonists
    1.
    发明授权
    N.sub.9 -cyclopentyl-substituted adenine derivatives useful as adenosine receptor agonists 失效

    公开(公告)号：US5063233A

    公开(公告)日：1991-11-05

    申请号：US531499

    申请日：1990-05-31

    申请人： Jen Chen ,  Alan J. Hutchison

    发明人： Jen Chen ,  Alan J. Hutchison

    IPC分类号： C07D303/46 ,  C07D473/00 ,  C07D473/16

    CPC分类号： C07D473/00 ,  C07D303/46 ,  C07D473/16

    摘要： The compound of the formula I ##STR1## wherein R, R.sub.3 and R.sub.5 independently represent hydrogen or hydroxy provided that at least one of R, R.sub.3 and R.sub.5 represents hydroxy; R.sub.1 represents hydrogen, lower alkyl, C.sub.3 -C.sub.7 -alkenyl, hydroxy-lower alkyl, optionally substituted cycloalkyl or optionally substituted cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, adamantyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydropyranyl-lower alkyl, tetrahydrothiopyranyl-lower alkyl, adamantyl-lower alkyl, aryl-hydroxy-lower alkyl, aryl, aryl-lower alkyl, aryl-C.sub.3 -C.sub.6 -cycloalkyl, 9-fluorenyl, 9-fluorenyl-lower alkyl or cycloalkenyl-lower alkyl; or R.sub.1 represents a bicyclic benzo-fused 5 or 6-membered saturated carbocyclic radical or a benz-fused 5 or 6-membered saturated heterocyclic radical containing a heteroatom selected from oxygen and sulfur directly attached to the fused benzene ring, any said bicyclic radicals being optionally substituted on the benzo portion by lower alkyl, lower alkoxy or halogen, or R.sub.1 represents any said bicyclic radical substituted-lower alkyl; R.sub.2 represents hydrogen, halogen, --S--R.sub.1 ', --NR.sub.b --R.sub.1 ', or --NH--R.sub.1 ' in each of which R.sub.1 ' has meaning as defined for R.sub.1 provided that R.sub.1 ' in --SR.sub.1 ' does not represent hydrogen; R.sub.b represents lower alkyl; R.sub.4 represents hydroxymethyl provided that R.sub.2 does not represent either hydrogen or --NHR.sub.1 ' in which R.sub.1 ' represents either hydrogen or lower alkyl; or R.sub.4 represents lower alkoxymethyl or lower alkylthiomethyl; or R.sub.4 represents --CONHR.sub.6 in which R.sub.6 represents lower alkyl, aryl-lower alkyl, C.sub.3 -C.sub.6 -cycloalkyl or hydroxy-lower alkyl; pharmaceutically acceptable ester derivatives thereof in which free hydroxy groups are esterified in form of a pharmaceutically acceptable ester; and pharmaceutically acceptable salts thereof; methods for their preparation; and their use as adenosine receptor agonists are disclosed.

    N.sub.9 -cyclopentyl-substituted adenine derivatives having adenosine-2 receptor stimulating activity
    2.
    发明授权
    N.sub.9 -cyclopentyl-substituted adenine derivatives having adenosine-2 receptor stimulating activity 失效

    公开(公告)号：US4954504A

    公开(公告)日：1990-09-04

    申请号：US193969

    申请日：1988-05-13

    申请人： Jen Chen ,  Alan J. Hutchison

    发明人： Jen Chen ,  Alan J. Hutchison

    IPC分类号： C07D303/46 ,  C07D473/00 ,  C07D473/16

    CPC分类号： C07D473/00 ,  C07D303/46 ,  C07D473/16

    摘要： The compound of the formula I ##STR1## wherein R, R.sub.3 and R.sub.5 independently represent hydrogen or hydroxy provided that at least one of R, R.sub.3 and R.sub.5 represents hydroxy; R.sub.1 represents hydrogen, lower alkyl, C.sub.3 -C.sub.7 -alkenyl, hydroxy-lower alkyl, optionally substituted cycloalkyl or optionally substituted cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, adamantyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydropyranyl-lower alkyl, tetrahydrothiopyranyl-lower alkyl, adamantyl-lower alkyl, aryl-hydroxy-lower alkyl, aryl, aryl-lower alkyl, aryl-C.sub.3 -C.sub.6 -cycloalkyl, 9-fluorenyl, 9-fluorenyl-lower alkyl or cycloalkenyl-lower alkyl; or R.sub.1 represents a bicyclic benzo-fused 5 or 6-membered saturated cyabocyclic radical or a benzo-fused 5 or 6-membered saturated heterocyclic radical containing a heteroatom selected from oxygen and sulfur directly attached to the fused benzene ring, any said bicyclic radicals being optionally substituted on the benzo portion by lower alkyl, lower alkoxy or halogen, or R.sub.1 represents any said bicyclic radical substituted-lower alkyl; R.sub.2 represents hydrogen, halogen, --S--R.sub.1 ', --NR.sub.b --R.sub.1 ', or --NH--R.sub.1 ' in each of which R.sub.1 ' has meaning as defined for R.sub.1 provided that R.sub.1 ' in --SR.sub.1 ' does not represent hydrogen; R.sub.b represents lower alkyl; R.sub.4 represents hydroxymethyl provided that R.sub.2 does not represent either hydrogen or --NHR.sub.1 ' in which R.sub.1 ' represents either hydrogen or lower alkyl; or R.sub.4 represents lower alkoxymethyl or lower alkylthiomethyl; or R.sub.4 represents --CONHR.sub.6 in which R.sub.6 represents lower alkyl; aryl-lower alkyl, C.sub.3 -C.sub.6 -cycloalkyl or hydroxy-lower alkyl; pharmaceutically acceptable ester derivatives thereof in which free hydroxy groups are esterified in form of a pharmaceutically acceptable ester; and pharmaceutically acceptable salts thereof; methods for their preparation; and their use as adenosine receptor agonists are disclosed.

    Certain hetero phosphonic acid derivatives of 2-piperidine or 2-tetrahydropyridinecarboxylates and esters thereof which are useful for the treatment of disorders responsive to blockade of the NMDA receptor in mammals
    6.
    发明授权
    Certain hetero phosphonic acid derivatives of 2-piperidine or 2-tetrahydropyridinecarboxylates and esters thereof which are useful for the treatment of disorders responsive to blockade of the NMDA receptor in mammals 失效
    可用于治疗对哺乳动物中NMDA受体的阻断作出反应的病症的2-哌啶或2-四氢吡啶羧酸酯及其酯的某些异膦酸衍生物

    公开(公告)号：US4746653A

    公开(公告)日：1988-05-24

    申请号：US834672

    申请日：1986-02-28

    申请人： Alan J. Hutchison ,  Kenneth R. Shaw ,  Josef A. Schneider

    发明人： Alan J. Hutchison ,  Kenneth R. Shaw ,  Josef A. Schneider

    IPC分类号： C07F9/59 ,  C07F9/60 ,  C07F9/58 ,  C07F9/65 ,  A61K31/675

    CPC分类号： C07F9/592 ,  C07F9/598 ,  C07F9/60

    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, 2-carboxyperhydroindolyl, and in each of which the carboxy group may be functionalized in form of a pharmaceutically acceptable ester or amide; A represents B--X--D wherein B represents a direct bond, or straight chain or branched lower alkylene; X represents O, S, SO, SO.sub.2, CO--NR.sub.b, R.sub.b N--CO or N--Ra; Ra represents hydrogen, lower alkyl, aryl, aryl-lower alkyl or acyl; R.sub.b represents hydrogen, lower alkyl or aryl-lower alkyl; D represents straight chain or branched lower alkylene; and pharmaceutically acceptable salts thereof; which are useful in mammals 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，2-羧基全氢吲哚基，其中羧基可以以药学上可接受的酯或酰胺的形式官能化; A表示B-X-D，其中B表示直接键，或直链或支链低级亚烷基; X表示O，S，SO，SO2，CO-NRb，RbN-CO或N-Ra; R a表示氢，低级烷基，芳基，芳基 - 低级烷基或酰基; Rb表示氢，低级烷基或芳基 - 低级烷基; D表示直链或支链低级亚烷基; 及其药学上可接受的盐; 其在哺乳动物中作为N-甲基-D-天冬氨酸敏感性兴奋性氨基酸受体的拮抗剂是有用的。

    3-amino-dihydro-(1)-benzopyrans
    9.
    发明授权
    3-amino-dihydro-(1)-benzopyrans 失效
    3-氨基 - 二氢 - （1） - 苯并吡喃

    公开(公告)号：US4992465A

    公开(公告)日：1991-02-12

    申请号：US481770

    申请日：1990-02-16

    申请人： Alan J. Hutchison

    发明人： Alan J. Hutchison

    IPC分类号： C07D311/58 ,  C07D311/64 ,  C07D335/06

    CPC分类号： C07D335/06 ,  C07D311/58 ,  C07D311/64

    摘要： R represents hydrogen or lower alkyl; R.sub.1 represents hydrogen, lower alkyl or aryl-lower alkyl; R.sub.2 represents hydrogen, lower alkyl or aryl-lower alkyl; or R.sub.1 and R.sub.2 together represent alkylene of 4 to 6 carbon atoms; R.sub.3 represents hydrogen, hydroxy, lower alkoxy, aryl-lower alkoxy, acyloxy or aryloxy in compounds wherein Z represents S; or R.sub.3 represents hydroxy, lower alkoxy, aryl-lower alkoxy, acyloxy or aryloxy, and is attached only at the 5- or 8- position in compounds wherein Z represents O; R.sub.4 and R.sub.5 represent independently hydrogen, lower alkyl or halogen; and pharmaceutically acceptable salts thereof; and mono or di- S-oxides of compounds of formula I wherein Z represents S and pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof; and use thereof as central nervous system active agents for the treatment of central nervous system disorders.

    摘要翻译： （I）其中Z表示O或S; R代表氢或低级烷基; R1代表氢，低级烷基或芳基 - 低级烷基; R2代表氢，低级烷基或芳基 - 低级烷基; 或R 1和R 2一起表示4至6个碳原子的亚烷基; R 3表示其中Z表示S的化合物中的氢，羟基，低级烷氧基，芳基 - 低级烷氧基，酰氧基或芳氧基; 或R 3表示羟基，低级烷氧基，芳基 - 低级烷氧基，酰氧基或芳氧基，并且仅在其中Z表示O的化合物中的5-或8-位上连接; R4和R5独立地表示氢，低级烷基或卤素; 及其药学上可接受的盐; 和其中Z表示S的式I化合物的单或二 - S-氧化物及其药学上可接受的盐，其药物组合物; 并将其用作治疗中枢神经系统疾病的中枢神经系统活性剂。

    2-substituted adenosine 5'-carboxamides as antihypertensive agents
    10.
    发明授权
    2-substituted adenosine 5'-carboxamides as antihypertensive agents 失效

    公开(公告)号：US4968697A

    公开(公告)日：1990-11-06

    申请号：US389663

    申请日：1989-08-04

    申请人： Alan J. Hutchison

    发明人： Alan J. Hutchison

    IPC分类号： C07H19/16

    CPC分类号： C07H19/16

    摘要： The compounds of the formula I ##STR1## wherein R represents hydrogen or lower alkyl; R.sub.1 represents C.sub.3 -C.sub.6 -cycloalkyl optionally substituted by lower alkyl, C.sub.3 -C.sub.6 -cycloalkyl-lower alkyl optionally substituted by lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, aryl, aryl-lower alkyl, aryl-C.sub.3 -C.sub.6 -cycloalkyl, 9-fluorenyl, diaryl-lower alkyl, 9-fluorenyl-lower alkyl, cycloalkenyl-lower alkyl, bicycloalkenyl-lower alkyl, tetrahydropyranyl-lower alkyl, tetrahydrothiopyranyl-lower alkyl or adamantyl-lower alkyl; or R.sub.1 represents a bicyclic benzo-fused 5- or 6-membered saturated carbocyclic radical or a benzo-fused 5- or 6-membered saturated heterocyclic radical containing a heteroatom selected from oxygen and sulfur which is directly attached to the fused benzene ring, any said bicyclic radical being unsubstituted or substituted on the benzo portion by lower alkyl, lower alkoxy, hydroxy, halogen or trifluoromethyl, or by a substituent -W-Z in which W represents a direct bond, lower alkylene, lower alkenylene, thio-lower alkylene or oxy-lower alkylene and Z represents cyano, carboxy or carboxy derivatized in the form of a pharmaceutically acceptable ester or amide, or R.sub.1 represents any said bicyclic radical substituted-lower alkyl; or R.sub.1 represents aryl-hydroxy-lower alkyl; R.sub.2 represents hydrogen, lower alkyl or aryl-lower alkyl; R.sub.3 represents hydrogen or hydroxy; R.sub.4 represents hydrogen, lower alkyl, aryl-lower alkyl, C.sub.3 -C.sub.6 -cycloalkyl or hydroxy-lower alkyl; aryl represents an optionally substituted carbocyclic aromatic radical, being preferably 1- or 2-naphthyl, phenyl, or naphthyl or phenyl substituted by one to three of lower alkyl, lower alkoxy, hydroxy, halogen or trifluoromethyl, or naphthyl or phenyl substituted by a substitutent -W-Z in which W represents a direct bond, lower alkylene, lower alkenylene, thio-lower alkylene or oxy-lower alkylene and Z represents cyano, carboxy or carboxy derivatized in the form of a pharmaceutically acceptable ester or amide; or aryl represents a heterocyclic aromatic radical, being preferably pyridyl or thienyl, each optionally substituted as described above for phenyl; pharmaceutically acceptable ester derivatives thereof in which free hydroxy groups are esterified in the form of a pharmaceutically acceptable ester; and pharmaceutically acceptable salts thereof; their preparation; and their use as adenosine-2 receptor agonists are disclosed.