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109 条记录 (耗时 0.064 秒)

    5-(Hydroxy- and/or amino-phenyl)-6-(lower-alkyl)-2-(1H)-pyridinones, their cardiotonic use and preparation
    1.
    发明授权
    5-(Hydroxy- and/or amino-phenyl)-6-(lower-alkyl)-2-(1H)-pyridinones, their cardiotonic use and preparation 失效
    5-（羟基 - 和/或氨基 - 苯基）-6-（低级烷基）-2-（1H） - 吡啶酮，它们的强心使用和制备

    公开(公告)号：US4465686A

    公开(公告)日：1984-08-14

    申请号：US372174

    申请日：1982-04-26

    申请人： George Y. Lesher ,  Chester J. Opalka, Jr. ,  Donald F. Page ,  Ruthann M. McGarry

    发明人： George Y. Lesher ,  Chester J. Opalka, Jr. ,  Donald F. Page ,  Ruthann M. McGarry

    IPC分类号： C07D213/64 ,  C07D213/73 ,  C07D213/82 ,  C07D213/85 ,  A61K31/44 ,  C07D211/72

    CPC分类号： C07D213/64 ,  C07D213/73 ,  C07D213/82 ,  C07D213/85

    摘要： Disclosed and claimed is the cardiotonic use of 1-R.sub.1 -5-(3-R'-4-R"-phenyl)-6-R-2(1H)-pyridinones (II), where R.sub.1 is hydrogen, lower-alkyl or lower-hydroxyalkyl, R is lower-alkyl or hydrogen, and, R' and R" are each hydrogen, amino or hydroxy, at least one of R' or R" being other than hydrogen, or where R' is nitro when R" is hydroxy, or pharmaceutically acceptable acid-addition salts thereof where at least one of R' and R" is amino. Also disclosed and claimed are 1-R.sub.1 -5-(3-R'-4-R"-phenyl)-6-R-2(1H)-pyridinones (I), where R.sub.1, R' and R" are defined as above and R is lower-alkyl and acid-addition salts thereof where at least one of R' and R" is amino. Also shown and claimed is the process which comprises reacting 1-R.sub.1 -1,2-dihydro-2-oxo-5-(3-R'-4-R"-phenyl)-6-R-nicotinonitrile, where R.sub.1 and R are defined as above for II, R' is hydrogen, hydroxy, methoxy or amino and R" is hydroxy, methoxy or hydrogen, preferably at least one of R' and R" being methoxy, or where R' is nitro and R" is hydrogen or methoxy, preferably methoxy, with 85% phosphoric acid to produce 1-R.sub.1 -5-(3-R'-4-R"-phenyl)-6-R-2(1H)-pyridinone.

    摘要翻译： 公开并要求保护的是强力使用1-R1-5-（3-R'-4-R“ - 苯基）-6-R-2（1H） - 吡啶酮（II），其中R 1是氢， 烷基或低级羟烷基，R为低级烷基或氢，R'和R“各自为氢，氨基或羟基，R'或R”中的至少一个为氢，或其中R'为 当R“为羟基时为硝基，或其药学上可接受的酸加成盐，其中R'和R”中的至少一个为氨基。 还公开和要求保护的是1-R1-5-（3-R'-4-R“ - 苯基）-6-R-2（1H） - 吡啶酮（I），其中R 1，R'和R” R是R'和R“中的至少一个是氨基的低级烷基和酸加成盐。 还显示和要求保护的方法包括使1-R1-1,2-二氢-2-氧代-5-（3-R'-4-R“ - 苯基）-6-R-烟腈反应，其中R 1和 R如上定义为II，R'是氢，羟基，甲氧基或氨基，R“是羟基，甲氧基或氢，优选R'和R”中的至少一个是甲氧基，或其中R'是硝基， R“是氢或甲氧基，优选甲氧基，与85％磷酸反应以产生1-R1-5-（3-R'-4-R” - 苯基）-6-R-2（1H） - 吡啶酮。

    1H-Indole-2,3-dione derivatives
    3.
    发明授权
    1H-Indole-2,3-dione derivatives 失效
    1H-吲哚-2,3-二酮衍生物

    公开(公告)号：US4322533A

    公开(公告)日：1982-03-30

    申请号：US225773

    申请日：1981-01-16

    申请人： George Y. Lesher ,  Donald F. Page ,  Monte D. Gruett

    发明人： George Y. Lesher ,  Donald F. Page ,  Monte D. Gruett

    IPC分类号： C07D213/40 ,  C07D401/04 ,  C07D401/06

    CPC分类号： C07D213/40 ,  Y10S514/93

    摘要： 1-R.sub.1 -4- or 5-[4-pyridinyl-(CH.sub.2).sub.n ]-1H-indole-2,3-dione 3-Q derivatives, useful as cardiotonics, bronchodilators, anti-asthmatics, anti-allergics and anti-cholinergics, are prepared by cyclization of N-{3- or 4-[4-pyridinyl-(CH.sub.2).sub.n ]phenyl}glyoxalamide oxime with acid; reaction of the product thus obtained with a carbonyl reactive reagent to prepare a compound where Q is other than O; and reaction of a compound where Q is either O or other than O with a lower-alkyl, hydroxy-lower-alkyl or di-lower-alkylamino-lower-alkyl ester of a strong mineral acid or with a carbo-lower-alkoxy-lower-alkyl halide to prepare compounds where R.sub.1 is other than hydrogen.

    摘要翻译： 1-R1-4-或5- [4-吡啶基 - （CH2）n] -1H-吲哚-2,3-二酮3-Q衍生物，可用作强心剂，支气管扩张剂，抗哮喘药，抗过敏剂和抗 - 通过N-（3-或4- [4-吡啶基 - （CH2）n]苯基}乙二醛酰胺肟与酸的环化制备胆碱能， 将由此获得的产物与羰基反应试剂反应以制备其中Q不为O的化合物; 和Q为O或O以外的化合物与强无机酸的低级烷基，羟基 - 低级 - 烷基或二 - 低级 - 烷基氨基 - 低级 - 烷基酯或与碳 - 低级 - 烷氧基 - 低级烷基卤化物，以制备其中R 1不是氢的化合物。

    1,2-Dihydro-2-oxo-5-(hydroxy-and/or amino-phenyl)-nicotinonitriles and cardiotonic use thereof
    5.
    发明授权
    1,2-Dihydro-2-oxo-5-(hydroxy-and/or amino-phenyl)-nicotinonitriles and cardiotonic use thereof 失效
    1,2-二氢-2-氧代-5-（羟基 - 和/或氨基 - 苯基） - 烟腈腈及其强心使用

    公开(公告)号：US4559352A

    公开(公告)日：1985-12-17

    申请号：US635947

    申请日：1984-07-30

    申请人： George Y. Lesher ,  Chester J. Opalka, Jr. ,  Donald F. Page

    发明人： George Y. Lesher ,  Chester J. Opalka, Jr. ,  Donald F. Page

    IPC分类号： C07D213/73 ,  C07D213/82 ,  C07D213/85 ,  A61K31/44 ,  C07D311/02

    CPC分类号： C07D213/73 ,  C07D213/82 ,  C07D213/85

    摘要： 1-R.sub.1 -3-amino-5-(3-R'-4-R"-phenyl)-6-R-2(1H)-pyridinones or salts thereof, which are useful as cardiotonics, where R.sub.1 is hydrogen, lower-alkyl, or lower-hydroxyalkyl, R is hydrogen or lower-alkyl, and, R' and R" are each hydrogen, hydroxy or amino at least one of R' or R" being other than hydrogen, are prepared by reacting the corresponding 3-carbamyl compound with a reagent capable of converting carbamyl to amino or by first reacting the corresponding 3-carbamyl compound where R' and R" are each hydrogen, nitro or lower-alkoxy at least one of R' and R" being other than hydrogen with a reagent capable of converting carbamyl to amino and then reacting the resulting 3-amino compound where R' and/or R" are/is lower-alkoxy and/or nitro with a reagent capable of converting lower-alkoxy to hydroxy and/or with a reagent capable of converting nitro to amino. Preparation of the corresponding 3-carbamyl and 3-cyano compounds is shown, the latter including cardiotonically active novel 1-R.sub.1 -1,2-dihydro-5-(3-R.sub.2 -4-R.sub.3 -phenyl)-6-R-nicotinonitriles where R.sub.1 and R are defined as above, and R.sub.2 and R.sub.3 have the above given definitions for R' and R" or where R.sub.2 is nitro and R.sub.3 is hydroxy. Also shown are cardiotonic compositions and cardiotonic method of use of above-said compounds.

    摘要翻译： 1-R1-3-氨基-5-（3-R'-4-R“ - 苯基）-6-R-2（1H） - 吡啶酮或其盐，其可用作强心剂，其中R 1是氢， 低级烷基或低级羟基烷基，R是氢或低级烷基，R'和R“各自为氢，羟基或氨基，R'或R”中的至少一个不是氢，是由 使相应的3-氨基甲酰基化合物与能将氨基甲酰转化为氨基的试剂反应，或者首先使相应的3-氨基甲酰基化合物反应，其中R'和R“各自为氢，硝基或低级烷氧基，R'和R “氢”不能与氨基甲酰氨基转化为氨基的试剂反应，然后将所得3-氨基化合物（其中R'和/或R“为低级烷氧基和/或硝基）与能够转化为较低级的试剂反应 - 烷氧基与/或与能够将硝基转化成氨基的试剂。 显示相应的3-氨基甲酰基和3-氰基化合物的制备，后者包括强心活性的新的1-R1-1,2-二氢-5-（3-R2-4-R3-苯基）-6-R-烟腈腈 其中R 1和R如上定义，并且R 2和R 3对R'和R“具有上述定义，或其中R 2是硝基，R 3是羟基。 还显示了使用上述化合物的强心剂组合物和强心剂方法。

    Use of 4-[4(or 3)-aminophenyl]pyridines as cardiotonic agents
    6.
    发明授权
    Use of 4-[4(or 3)-aminophenyl]pyridines as cardiotonic agents 失效
    使用4- [或（3） - 氨基苯基]吡啶作为强心剂

    公开(公告)号：US4377585A

    公开(公告)日：1983-03-22

    申请号：US284771

    申请日：1981-07-20

    申请人： George Y. Lesher ,  Donald F. Page

    发明人： George Y. Lesher ,  Donald F. Page

    IPC分类号： C07D213/40 ,  A61K31/44

    CPC分类号： C07D213/40

    摘要： Disclosed and claimed are a cardiac composition and a method for increasing cardiac contractility using an effective amount of a cardiotonic 4-[4-(or 3)-AcNH-phenyl]-2-R.sub.2 -3-R.sub.3 -5-R.sub.5 -6-R.sub.6 -pyridine (I) or pharmaceutically-acceptable salt thereof, where R.sub.2 is hydrogen, methyl, ethyl or hydroxyl, R.sub.6 is hydrogen, methyl or ethyl, R.sub.3 and R.sub.5 are each hydrogen or methyl, and Ac is hydrogen, hydroxyacetyl, acetoxyacetyl, .alpha.-hydroxypropionyl, .alpha.-acetoxypropionyl, methyoxyacetyl, 2-butenoyl or carbamyl or when NHAc is attached to the 4-position of the phenyl ring Ac also is formyl, n-propanoyl, 2,2-dimethyl-n-propanoyl or 3-carboxypropanoyl or when NHAc is attached to the 3-position of the phenyl ring Ac also is acetyl. Novel compounds shown and claimed are 4-[4-(or 3)-Ac'NH-phenyl]-2-R.sub.2 -3-R.sub.3 -5-R.sub.5 -6-R.sub.6 -pyridines (II) or pharmaceutically-acceptable acid-addition salts thereof, where R.sub.2, R.sub.3, R.sub.5 and R.sub.6 are defined as above for I and Ac' is hydroxyacetyl, acetoxyacetyl, .alpha.-hydroxypropanoyl, .alpha.-acetoxypropionyl, methoxyacetyl, 2-butenoyl or carbamyl or where Ac'NH is attached to the 4-position of the phenyl ring Ac' is formyl, n-propanoyl, 2,2-dimethyl-n-propanoyl or 3-carboxypropanoyl. Also disclosed and claimed is the process for preparing said novel compounds (II).

    摘要翻译： 公开并要求保护的是心脏组合物和使用有效量的强心剂4- [4-（或3）-AcNH-苯基] -2-R2-3-R3-5-R5-6- R6-吡啶（I）或其药学上可接受的盐，其中R 2是氢，甲基，乙基或羟基，R 6是氢，甲基或乙基，R 3和R 5各自是氢或甲基，Ac是氢，羟基乙酰基，乙酰氧基乙酰基， α-羟基丙酰基，α-乙酰氧基丙酰基，甲氧基乙酰基，2-丁烯酰基或氨基甲酰基，或当NHAc与苯环的4-位连接时，Ac也是甲酰基，正丙酰基，2,2-二甲基 - 正丙酰基或3- 羧基丙酰基或当NHAc与苯环的3-位连接时，Ac也是乙酰基。 所示和要求保护的新化合物是4- [4-（或3）-Ac'NH-苯基] -2-R2-3-R3-5-R5-6-R6-吡啶（II）或药学上可接受的酸加成 其盐，其中R2，R3，R5和R6如上对I所定义，Ac'是羟基乙酰基，乙酰氧基乙酰基，α-羟基丙酰基，α-乙酰氧基丙酰基，甲氧基乙酰基，2-丁烯酰基或氨基甲酰基，或其中Ac'NH连接到4 苯环Ac'的位置是甲酰基，正丙酰基，2,2-二甲基 - 正丙酰基或3-羧基丙酰基。 还公开并要求保护的是制备所述新化合物（II）的方法。

    N-[4-(4-Pyridinyl)phenyl]ureas and their cardiotonic use
    7.
    发明授权
    N-[4-(4-Pyridinyl)phenyl]ureas and their cardiotonic use 失效
    N- [4-（4-吡啶基）苯基]脲及其强心剂用途

    公开(公告)号：US4376775A

    公开(公告)日：1983-03-15

    申请号：US285379

    申请日：1981-07-20

    申请人： George Y. Lesher ,  Donald F. Page

    发明人： George Y. Lesher ,  Donald F. Page

    IPC分类号： C07D213/40 ,  C07D213/54 ,  A61K31/44

    CPC分类号： C07D213/40

    摘要： Disclosed and claimed are N-R-N-40 [4-(4-2-R.sub.2 -3-R.sub.3 -5-R.sub.5 -6-R.sub.6 -4-pyridinyl)phenyl]ureas (I) or pharmaceutically-acceptable acid-addition salts thereof, where R is hydrogen, methyl or ethyl, R.sub.2 is hydrogen, methyl, ethyl or hydroxyl, R.sub.6 hydrogen, methyl or ethyl, and R.sub.3 and R.sub.5 are each hydrogen or methyl, their cardiotonic use and their preparation.

    摘要翻译： 公开并要求保护的是NRN-40 [4-（4-2-R2-3-R3-5-R5-6-R6-4-吡啶基）苯基]脲（I）或其药学上可接受的酸加成盐，其中 R是氢，甲基或乙基，R2是氢，甲基，乙基或羟基，R6是氢，甲基或乙基，R3和R5分别是氢或甲基，它们的强心使用及其制备。

    2-Substituted amino-5-(pyridinyl)-nicotinamides and their cardiotonic use
    8.
    发明授权
    2-Substituted amino-5-(pyridinyl)-nicotinamides and their cardiotonic use 失效
    2-取代的氨基-5-（吡啶基） - 烟酰胺及其强心使用

    公开(公告)号：US4374141A

    公开(公告)日：1983-02-15

    申请号：US293248

    申请日：1981-08-17

    申请人： George Y. Lesher ,  Chester J. Opalka, Jr. ,  Donald F. Page

    发明人： George Y. Lesher ,  Chester J. Opalka, Jr. ,  Donald F. Page

    IPC分类号： C07D213/82 ,  C07D471/04 ,  C07D401/04 ,  A61K31/455

    CPC分类号： C07D213/82 ,  C07D471/04

    摘要： Shown is a process for preparing cardiotonically active 1,3-dihydro-3-R-6-PY-5-Q-2H-imidazo[4,5-b]pyridin-2-ones, where Q is hydrogen or lower-alkyl, R is lower-alkyl, lower-hydroxyalkyl, lower-alkoxyalkyl or Y-NB where Y is lower-alkylene and NB is di-(lower-alkyl)amino or 4-morpholinyl, and PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two substituents, by reacting a 2-RNH-5-PY-6-Q-nicotinamide with an alkali metal hypohalite. Also shown are cardiotonic compositions and a method for increasing cardiac contractility using 2-RR'N-5-PY-6-Q-nicotinamides or pharmaceutically acceptable acid-addition salts thereof, where R' is hydrogen or methyl. Also shown is the process for preparing said 2-RR'N-5-PY-6-Q-nicotinamides by reacting a 2-halo-5-PY-6-Q-nicotinamide with an amine of the formula RR'NH.

    摘要翻译： 示出了制备强心活性的1,3-二氢-3-R-6-PY-5-Q-2H-咪唑并[4,5-b]吡啶-2-酮的方法，其中Q是氢或低级烷基 R是低级烷基，低级羟烷基，低级烷氧基烷基或Y-NB，其中Y是低级亚烷基，NB是二 - （低级 - 烷基）氨基或4-吗啉基，PY是4-或3-吡啶基或 具有一个或两个取代基的4-或3-吡啶基，通过使2-RNH-5-PY-6-Q-烟酰胺与碱金属次卤酸盐反应。 还示出了强心剂组合物和使用2-RR'N-5-PY-6-Q-烟酰胺或其药学上可接受的酸加成盐增加心脏收缩力的方法，其中R'是氢或甲基。 还示出了通过使2-卤代-5-PY-6-C-烟酰胺与式RR'NH的胺反应来制备所述2-RR'N-5-PY-6-Q-烟酰胺的方法。

    Pyridinyl-pyridines
    9.
    发明授权
    Pyridinyl-pyridines 失效
    吡啶基 - 吡啶

    公开(公告)号：US4351941A

    公开(公告)日：1982-09-28

    申请号：US317548

    申请日：1981-11-02

    申请人： George Y. Lesher ,  Chester J. Opalka, Jr. ,  Donald F. Page

    发明人： George Y. Lesher ,  Chester J. Opalka, Jr. ,  Donald F. Page

    IPC分类号： C07D213/50 ,  C07D213/64 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/80 ,  C07D213/82 ,  C07D213/85 ,  C07D401/04

    CPC分类号： C07D213/64 ,  C07D213/50 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/80 ,  C07D213/82 ,  C07D213/85

    摘要： 2-[R.sub.1 NHN(R)]-3-Q'-5-PY-6-Q-pyridines or pharmaceutically-acceptable acid-addition salts thereof are useful as cardiotonic agents, where Q is hydrogen or lower-alkyl, PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two lower-alkyl substituents, Q' is hydrogen or halo, R is hydrogen, lower-alkyl or lower-hydroxyalkyl, and R.sub.1 is hydrogen or when R is other than hydrogen R.sub.1 is the same as R. These compounds are prepared by reacting a 2-halo-3-Q'-5-PY-6-Q-pyridine with R.sub.1 NHNHR where 2-halo is bromo or chloro. Also shown are: the use of said 2-[R.sub.1 NN(R)]-3-Q'-5-PY-6-Q-pyridines as cardiotonic agents; and, the intermediates, 2,3-dihalo-5-PY-6-Q-pyridines, and their preparation from 3-nitro-5-PY-6-Q-2(1H)-pyridinones.

    摘要翻译： 2- [R1NHN（R）] - 3-Q'-5-PY-6-Q-吡啶或其药学上可接受的酸加成盐可用作强心剂，其中Q为氢或低级烷基，PY为4 - 或3-吡啶基或具有一个或两个低级烷基取代基的4-或3-吡啶基，Q'是氢或卤素，R是氢，低级烷基或低级 - 羟基烷基，并且R 1是氢或当R不是 氢R1与R相同。这些化合物通过2-卤代-3-Q'-5-PY-6-Q-吡啶与R1NHNHR反应来制备，其中2-卤代是溴或氯。 还显示：使用所述2- [R1NN（R）] - 3-Q'-5-PY-6-Q-吡啶作为强心剂; 和中间体2,3-二卤代-5-PY-6-Q-吡啶，以及它们由3-硝基-5-PY-6-Q-2（1H） - 吡啶酮的制备。