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34 条记录 (耗时 0.016 秒)

    Substituted bi-alicyclic imides
    2.
    发明授权
    Substituted bi-alicyclic imides 失效
    取代的双脂环酰亚胺

    公开(公告)号：US4562255A

    公开(公告)日：1985-12-31

    申请号：US595138

    申请日：1984-03-30

    申请人： Meier E. Freed ,  Magid A. Abou-Gharbia

    发明人： Meier E. Freed ,  Magid A. Abou-Gharbia

    IPC分类号： C07D403/12 ,  C07D498/16 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14

    CPC分类号： C07D403/12

    摘要： There are disclosed compounds having the formula ##STR1## wherein X is a group selected from ##STR2## Y represents a single or double bond; R.sup.1 is hydrogen or lower alkyl;n is an integer 2-4;n' is an integer 1-2; andR is 2-pyrimidinyl, 2-pyridinyl, 2-pyrazinyl, halo-substituted 2-pyrazinyl, 5-tetrazolyl, phenyl or phenyl substituted by halo, lower alkyl or lower alkoxy;and the pharmacologically acceptable salts thereof, which exhibit anti-hypertensive activity.

    摘要翻译： 公开了具有式“IMAGE”的化合物，其中X是选自下式的基团：Y表示单键或双键; R1是氢或低级烷基; n是整数2-4; n'是整数1-2; 并且R是2-嘧啶基，2-吡啶基，2-吡嗪基，卤素取代的2-吡嗪基，5-四唑基，苯基或被卤素，低级烷基或低级烷氧基取代的苯基; 和其药理学上可接受的盐，其具有抗高血压活性。

    2,3,4,9-tetrahydro-2-heteroarylalkyl-1H-pyrido(3,4-B)indoles having antihypertensive properties
    3.
    发明授权
    2,3,4,9-tetrahydro-2-heteroarylalkyl-1H-pyrido(3,4-B)indoles having antihypertensive properties 失效
    具有抗高血压性质的2,3,4,9-四氢-2-杂芳基烷基-1H-吡啶并（3,4-B）吲哚

    公开(公告)号：US4719211A

    公开(公告)日：1988-01-12

    申请号：US837612

    申请日：1986-03-07

    申请人： Magid A. Abou-Gharbia ,  Meier E. Freed

    发明人： Magid A. Abou-Gharbia ,  Meier E. Freed

    IPC分类号： C07D471/04 ,  A61K31/495 ,  C07D471/06

    CPC分类号： C07D471/04

    摘要： This invention concerns tetrahydropyridoindoles of the formula: ##STR1## wherein Q represents ##STR2## in which R.sub.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, or --COO(C.sub.1-2) alkyl, and n is an integer from 1 to 7; R.sub.1 is hydrogen, halogen, hydroxy, or C.sub.1-3 alkyl; and R.sub.2 is hydrogen, C.sub.1-4 alkyl or --(CH.sub.2).sub.m --A where A is --N(CH.sub.3).sub.2,--N(C.sub.2 H.sub.5).sub.2, ##STR3## in which Ar is 2-pyrimidinyl, 2-pyrazinyl, phenyl, or phenyl substituted by a methyl, ethyl, methoxy, ethoxy, or trifluoromethyl group; and m is an integer from 1-4, or physiologically acceptable salts thereof, providing however that when n is 1, Q may not be quinolinyl. These compounds exhibit antihypertensive properties. Four of the disclosed compounds also exhibit antipsychotic properties.Also disclosed are compounds of Formula XX in which Q of Formula I is replaced by Q.sub.1, wherein Q.sub.1 is 2- or 3-pyridinyl, and R.sub.2 of Formula I is restricted to hydrogen. The compounds of Formula XX exhibit antipsychotic properties.

    摘要翻译： 本发明涉及下式的四氢吡啶并吲哚：其中Q代表其中R3是氢，C1-4烷基，C1-4烷氧基或-COO（C1-2）烷基，其中n是 1至7; R 1是氢，卤素，羟基或C 1-3烷基; 其中A为-N（CH 3）2，-N（C 2 H 5）2，其中Ar为2-嘧啶基，2-吡嗪基，苯基或 被甲基，乙基，甲氧基，乙氧基或三氟甲基取代的苯基; 并且m是1-4的整数或其生理上可接受的盐，但是当n为1时，Q可能不是喹啉基。 这些化合物显示抗高血压性质。 所公开的化合物中的四种也显示出抗精神病性质。 还公开了式XX的化合物，其中式I的Q被Q1代替，其中Q1是2-或3-吡啶基，式I的R2限于氢。 式XX的化合物显示出抗精神病性质。

    Antiarrhythmic cyclooct[b]indoles
    4.
    发明授权
    Antiarrhythmic cyclooct[b]indoles 失效
    抗心律失常环磷[b]吲哚

    公开(公告)号：US4546193A

    公开(公告)日：1985-10-08

    申请号：US684211

    申请日：1984-12-20

    申请人： Magid A. Abou-Gharbia ,  Meier E. Freed ,  Thomas J. Colatsky

    发明人： Magid A. Abou-Gharbia ,  Meier E. Freed ,  Thomas J. Colatsky

    IPC分类号： C07D209/94 ,  C07D209/70

    CPC分类号： C07D209/94

    摘要： This invention provides a group of antiarrhythmic agents of the formula: ##STR1## in which R.sub.1 is --CO.sub.2 H, --CO.sub.2 (CH.sub.2).sub.n --NR.sub.4 R.sub.5, --CONR.sub.6 R.sub.7, --NHCO.sub.2 R.sub.8 or --NHCO.sub.2 (CH.sub.2).sub.o --NR.sub.9 R.sub.10 where R.sub.4 and R.sub.5 are H or alkyl of 1 to 6 carbon atoms and n is 1 to 6; R.sub.6 and R.sub.7 are H or alkyl of 1 to 6 carbon atoms; R.sub.8 is alkyl of 1 to 6 carbon atoms; and R.sub.9 and R.sub.10 are alkyl of 2 to 6 carbon atoms and o is 1 to 6;R.sub.2 and R.sub.3 are, independently, hydrogen or alkyl of 1 to 6 carbon atoms; andm is one of the integers 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof, and a method for their use.

    摘要翻译： 本发明提供一组下式的抗心律不齐药物：其中R 1是-CO 2 H，-CO 2（CH 2）n -NR 4 R 5，-CONR 6 R 7，-NHCO 2 R 8或-NHCO 2（CH 2）o -NR 9 R 10，其中R 4和R 5是 H或1〜6个碳原子的烷基，n为1〜6; R6和R7是H或1至6个碳原子的烷基; R8是1-6个碳原子的烷基; 并且R 9和R 10为2至6个碳原子的烷基，o为1至6; R2和R3独立地是氢或1至6个碳原子的烷基; 并且m是整数1,2,3或4之一; 或其药学上可接受的盐及其使用方法。

    Antiarrhythmic agents
    5.
    发明授权
    Antiarrhythmic agents 失效
    抗心律失常药

    公开(公告)号：US4638008A

    公开(公告)日：1987-01-20

    申请号：US740651

    申请日：1985-06-03

    申请人： Magid A. Abou-Gharbia ,  Meier E. Freed ,  Thomas J. Colatsky

    发明人： Magid A. Abou-Gharbia ,  Meier E. Freed ,  Thomas J. Colatsky

    IPC分类号： C07D209/94 ,  A61K31/40

    CPC分类号： C07D209/94 ,  Y10S514/821

    摘要： This invention provides a group of antiarrythmic agents of the formula: ##STR1## in which R.sub.1 is --CO.sub.2 H, --CO.sub.2 (CH.sub.2).sub.n --NR.sub.4 R.sub.5, --CONR.sub.6 R.sub.7, --NHCO.sub.2 R.sub.8 or --NHCO.sub.2 (CH.sub.2).sub.o --NR.sub.9 R.sub.10 where R.sub.4 and R.sub.5 are H or alkyl of 1 to 6 carbon atoms and n is 1 to 6; R.sub.6 and R.sub.7 are H or alkyl of 1 to 6 carbon atoms; R.sub.8 is alkyl of 1 to 6 carbon atoms; and R.sub.9 and R.sub.10 are alkyl of 2 to 6 carbon atoms and o is 1 to 6;R.sub.2 and R.sub.3 are, independently, hydrogen or alkyl of 1 to 6 carbon atoms; andm is one of the integers 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof, and a method for their use.

    摘要翻译： 本发明提供一组下式的抗焦虑剂：其中R 1是-CO 2 H，-CO 2（CH 2）n -NR 4 R 5，-CONR 6 R 7，-NHCO 2 R 8或-NHCO 2（CH 2）o -NR 9 R 10，其中R 4和R 5是 H或1〜6个碳原子的烷基，n为1〜6; R6和R7是H或1至6个碳原子的烷基; R8是1-6个碳原子的烷基; 并且R 9和R 10为2至6个碳原子的烷基，o为1至6; R2和R3独立地是氢或1至6个碳原子的烷基; 并且m是整数1,2,3或4之一; 或其药学上可接受的盐及其使用方法。

    Thiazepino-[4,3-b]-isoquinoline-1,5-dione derivatives and precursors
    7.
    发明授权
    Thiazepino-[4,3-b]-isoquinoline-1,5-dione derivatives and precursors 失效
    噻吩并[4,3-b] - 异喹啉-1,5-二酮衍生物和前体

    公开(公告)号：US4251444A

    公开(公告)日：1981-02-17

    申请号：US138011

    申请日：1980-04-07

    申请人： Meier E. Freed ,  James L. Diebold

    发明人： Meier E. Freed ,  James L. Diebold

    IPC分类号： C07D217/26 ,  C07D513/04 ,  A61K31/38

    CPC分类号： C07D513/04 ,  C07D217/26

    摘要： The thiazepino-[4,3-b]-isoquinoline-1,5-diones of the formula: ##STR1## where R.sup.1 is hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms or halo;R.sup.2 is hydrogen, alkyl of 1 to 6 carbon atoms or phenyl;andR.sup.3 is hydrogen or alkyl of 1 to 3 carbon atoms and the open ring 3-carboxy isoquinoline precursors inhibit angiotensin converting enzyme and are useful anti-hypertensive agents.

    摘要翻译： 下式的噻吩并[4,3-b] - 异喹啉-1,5-二酮：其中R 1是氢，1至6个碳原子的烷基，1至6个碳原子的烷氧基或卤素; R2是氢，1至6个碳原子的烷基或苯基; R3是氢或1〜3个碳原子的烷基，开环3-羧基异喹啉前体抑制血管紧张素转化酶，是有用的抗高血压药。

    3-[Pyridinylalkyl and piperidinylalkyl]-2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5(6H) -ones
    8.
    发明授权
    3-[Pyridinylalkyl and piperidinylalkyl]-2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5(6H) -ones 失效
    3- [吡啶基烷基和哌啶基烷基] -2,3,4,4a-四氢-1H-吡嗪并[1,2-a]喹喔啉-5（6H） - 酮

    公开(公告)号：US4203987A

    公开(公告)日：1980-05-20

    申请号：US40609

    申请日：1979-05-21

    申请人： Meier E. Freed

    发明人： Meier E. Freed

    IPC分类号： C07D487/04 ,  A61K31/495

    CPC分类号： C07D487/04 ,  Y10S514/926 ,  Y10S514/927

    摘要： Disclosed herein are compounds of the formula: ##STR1## wherein n is an integer from 1 to 8;R is hydrogen or lower alkyl;Y is hydrogen, lower alkyl, lower alkoxy, chlorine, fluorine, or trifluoromethyl in the 7, 8, or 9 position;A is hydrogen, lower alkyl, phen(lower)alkyl, or diphenyl(lower)alkyl; andthe pyridinyl or piperidinyl moiety is joined to the alkylene bridging group at the 2 or 4 position; or non-toxic acid addition salts thereof. These compounds exhibit hypotensive effects in hypertensive animals and also exhibit anti-secretory properties.

    摘要翻译： 本文公开的是下式的化合物：其中n是1至8的整数; R是氢或低级烷基; 在7,8或9位，Y是氢，低级烷基，低级烷氧基，氯，氟或三氟甲基; A是氢，低级烷基，苯基（低级）烷基或二苯基（低级）烷基; 并且吡啶基或哌啶基部分在2或4位连接到亚烷基桥连基团; 或无毒的酸加成盐。 这些化合物在高血压动物中表现出降血压作用并且还表现出抗分泌性质。

    2,3,4,4A-Tetrahydro-1H-pyrazino[1,2]quinoxalin-5(6)-ones and derivatives thereof
    10.
    发明授权
    2,3,4,4A-Tetrahydro-1H-pyrazino[1,2]quinoxalin-5(6)-ones and derivatives thereof 失效
    2,3,4,4a-四氢-1H-吡嗪{8 1,2 {9喹喔啉-5（6）酮及其衍生物

    公开(公告)号：US4089958A

    公开(公告)日：1978-05-16

    申请号：US752577

    申请日：1976-12-20

    申请人： Meier E. Freed ,  John R. Potoski

    发明人： Meier E. Freed ,  John R. Potoski

    IPC分类号： C07C205/12 ,  C07D239/42 ,  C07D241/04 ,  C07D487/04 ,  C07F1/00 ,  C07F1/08 ,  A61K31/495

    CPC分类号： C07D239/42 ,  C07C205/12 ,  C07D241/04 ,  C07D487/04 ,  C07F1/005 ,  C07F1/08

    摘要： Compounds of the formula ##STR1## WHEREIN R is hydrogen (lower)alkyl, phen(lower)-alkyl, benzoyl(lower)alkyl, or p-halobenzoyl-(lower)alkyl; R.sup.1 is hydrogen or (lower)alkyl; R.sup.2 is hydrogen, (lower)alkyl, (lower)alkoxy, chlorine, fluorine, trifluoromethyl, or amino in the 7-, 8-, or 9-position; R.sup.3 is hydrogen, or (lower)alkyl; and R.sup.4 is hydrogen, (lower)-alkyl, (lower)alkoxy, chlorine, fluorine, or trifluoromethyl in the 7-, 8-, or 9-position; or the non-toxic acid addition salts thereof; exert a hyptotensive effect in hypertensive animals.

    摘要翻译： 式（Ia）化合物，其中R为氢（低级）烷基，苯基（低级）烷基，苯甲酰基（低级）烷基或对卤代苯甲酰基（低级）烷基; R1是氢或（低级）烷基; R2是氢，（低级）烷基，（低级）烷氧基，氯，氟，三氟甲基或氨基在7-，8-或9-位; R3是氢或（低级）烷基; 并且R 4为氢，（低级） - 烷基，（低级）烷氧基，氯，氟或三氟甲基的7-，8-或9-位; 或其无毒的酸加成盐; 在高血压动物中发挥降压作用。