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    5-(Hydroxy- and/or amino-phenyl)-6-(lower-alkyl)-2-(1H)-pyridinones, their cardiotonic use and preparation
    2.
    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。

    2-Amino-6-(pyridinyl)-3H-imidazo[4,5-b]pyridines and their cardiotonic use
    4.
    发明授权
    2-Amino-6-(pyridinyl)-3H-imidazo[4,5-b]pyridines and their cardiotonic use 失效
    2-氨基-6-（吡啶基）-3H-咪唑并[4,5-b]吡啶及其强心剂用途

    公开(公告)号：US4391811A

    公开(公告)日：1983-07-05

    申请号：US307777

    申请日：1981-10-02

    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： C07D471/04 ,  C07D487/04 ,  A61K31/44

    CPC分类号： C07D471/04

    摘要： 2-(NB)-3-R-6-PY-5-Q-3H-imidazo[4,5-b]pyridines (I) and salts, useful as cardiotonics, where NB is amino or dimethylamino, R is lower-alkyl, Q is hydrogen or lower-alkyl, and PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two lower-alkyl substituents, are prepared by reacting a 2-RNH-3-amino-5-PY-6-Q-pyridine with a di-(lower-alkyl) 2-methylthiopseudourea-1,3-dicarboxylate to produce 2-carbo(lower-alkoxy)amino-3-R-6-PY-5-Q-3H-imidazo[4,5-b] pyridine and hydrolyzing the latter to produce I where NB is amino and by reacting a 2-RNH-3-amino-5-PY-6-Q-pyridine with dichloromethylene-N,N-dimethylammonium chloride to produce I where NB is dimethylamino. Cardiotonic use of I is disclosed and claimed.

    摘要翻译： 2-（NB）-3-R-6-PY-5-Q-3H-咪唑并[4,5-b]吡啶（I）和盐，其可以用作强心剂，其中NB是氨基或二甲基氨基， 烷基，Q是氢或低级烷基，PY是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，是通过使2-RNH-3-氨基-5- （低级烷基）2-甲硫基假脲-1,3-二羧酸酯的2-（低级烷氧基）氨基-3-R-6-PY-5-Q-3H - 咪唑并[4,5-b]吡啶，并水解后者，得到其中NB为氨基的I，并通过使2-RNH-3-氨基-5-PY-6-C-吡啶与二氯亚甲基-N，N-二甲基铵 其中NB是二甲基氨基。 披露并声称对I的强心使用。

    2-(Substituted-amino)-5-(pyridinyl-nicotinonitriles, and their cardiotonic use
    5.
    发明授权
    2-(Substituted-amino)-5-(pyridinyl-nicotinonitriles, and their cardiotonic use 失效
    2-（取代的 - 氨基）-5-（吡啶基 - 烟腈，及其强心使用

    公开(公告)号：US4362734A

    公开(公告)日：1982-12-07

    申请号：US296300

    申请日：1981-08-26

    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： C07D213/85 ,  A61K31/455 ,  A61K31/44

    CPC分类号： C07D213/85

    摘要： Shown are cardiotonically active 2-RR'N-5-PY-6-Q-nicotinonitriles where R is methyl or ethyl, R' is hydrogen or methyl, PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two substituents, and Q is hydrogen or methyl, the latter only when R' is hydrogen, or pharmaceutically acceptable acid-addition salts thereof. Also shown are cardiotonic compositions and a method for increasing cardiac contractility using as active components 2-RR'N-5-PY-6-Q-nicotinonitriles or pharmaceutically acceptable acid-addition salts thereof, where R, R', PY and Q are defined as above. Also shown is the process for preparing said 2-RR'N-5-PY-6-Q-nicotinonitriles by reacting a 2-halo-5-PY-6-Q-nicotinonitrile with an amine of the formula RR'NH.

    摘要翻译： 显示的是强心活性的2-RR'N-5-PY-6-Q-烟腈，其中R是甲基或乙基，R'是氢或甲基，PY是4-或3-吡啶基或具有一个的4-或3-吡啶基 或两个取代基，Q为氢或甲基，后者仅在R'为氢时，或其药学上可接受的酸加成盐。 还示出了强心剂组合物和使用作为活性成分2-RR'N-5-PY-6-Q-烟腈腈或其药学上可接受的酸加成盐来增加心脏收缩力的方法，其中R，R'，PY和Q为 如上所述。 还示出了通过使2-卤代-5-PY-6-Q-烟腈与式RR'NH的胺反应来制备所述2-RR'N-5-PY-6-Q-烟腈的方法。

    5-(Pyridinyl)pyridine-2-hydrazines, their preparation and their cardiotonic use
    6.
    发明授权
    5-(Pyridinyl)pyridine-2-hydrazines, their preparation and their cardiotonic use 失效
    5-（吡啶基）吡啶-2-肼，它们的制备及其强心使用

    公开(公告)号：US4331672A

    公开(公告)日：1982-05-25

    申请号：US231312

    申请日：1981-02-04

    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 ,  A61K31/44

    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。

    Compositions and their preparation
    7.
    发明授权
    Compositions and their preparation 失效
    组合及其准备

    公开(公告)号：US4276293A

    公开(公告)日：1981-06-30

    申请号：US135211

    申请日：1980-03-28

    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： A61K31/44 ,  A61P9/04 ,  C07D213/50 ,  C07D213/61 ,  C07D213/77 ,  C07D471/04 ,  A61K31/415

    CPC分类号： C07D213/77 ,  C07D213/50 ,  C07D213/61 ,  C07D471/04

    摘要： 2-R.sub.2 -3-R.sub.3 -6-PY-5-Q-3H-imidazo[4,5-b]pyridines (I) or 1-R.sub.1 -2-R.sub.2 -6-PY-5-Q-1H-imidazo[4,5-b]pyridines (IA) or pharmaceutically-acceptable acid-addition salts thereof, where Q and R.sub.2 are each hydrogen or lower-alkyl, R.sub.1 and R.sub.3 are each hydrogen, lower-alkyl, lower-hydroxyalkyl, 2,3-dihydroxypropyl, lower-alkoxyalkyl or Y-NB where Y is lower-alkylene having at least two carbon atoms between its connecting linkages and NB is di-(lower-alkyl)amino or 4-morpholinyl, at least one of R.sub.1 or R.sub.3 being hydrogen, and PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two lower-alkyl substituents, which are useful as cardiotonics, are prepared by reacting 2-R.sub.3 NH-3-R.sub.1 NH-5-PY-6-Q-pyridine (II) with a tri-(lower-alkyl) ortho-(lower-alkanoate). Also shown are: the use of I or IA or salts in cardiotonic compositions and a method for increasing cardiac contractility; and, the preparation of the intermediates II, as well as intermediates used to prepare II.

    摘要翻译： 2-R2-3-R3-6-PY-5-Q-3H-咪唑并[4,5-b]吡啶（I）或1-R1-2-R2-6-PY-5-Q-1H-咪唑 [4,5-b]吡啶（IA）或其药学上可接受的酸加成盐，其中Q和R 2各自为氢或低级烷基，R 1和R 3各自为氢，低级烷基，低级羟烷基， 其中Y是其连接键和NB之间具有至少两个碳原子的低级亚烷基的低级烷氧基烷基或Y-NB是二 - （低级 - 烷基）氨基或4-吗啉基，R 1或R 3中的至少一个 是氢，并且PY是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，其可用作强心剂，是通过使2-R 3 NH-3-R 1 NH-5-PY- 具有三（低级烷基）邻 - （低级链烷酸酯）的6-Q-吡啶（II）。 还显示：在强心剂组合物中使用I或IA或盐，以及增加心脏收缩力的方法; 以及中间体II的制备，以及用于制备II的中间体。

    Preparation of 5-(hydroxy- and/or aminophenyl-6-lower-alkyl)-2(1H)-pyridinones
    8.
    发明授权
    Preparation of 5-(hydroxy- and/or aminophenyl-6-lower-alkyl)-2(1H)-pyridinones 失效
    制备5-（羟基 - 和/或氨基苯基-6-低级烷基）-2（1H） - 吡啶酮

    公开(公告)号：US4599423A

    公开(公告)日：1986-07-08

    申请号：US595751

    申请日：1984-04-02

    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 ,  C07D211/76

    CPC分类号： C07D213/64

    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, where R.sub.1 and R are defined as above for II, R' is hydrogen, hydroxy or amino and R" is hydroxy or hydrogen, at least one of R' and R" being hydroxy, or where R' is nitro and R" is hydroxy.

    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，得到1-R1-5-（3-R'-4-R” - 苯基）-6-R-2（1H） - 吡啶酮， 其中R 1和R如上面对于II定义，R'是氢，羟基或氨基，R“是羟基或氢，R'和R”中的至少一个是羟基，或其中R'是硝基，R' '是羟基。

    3-Amino-5-(hydroxy- and/or aminophenyl)-6-(lower-alkyl)-2(1H)-pyridinones and cardiotonic use thereof
    9.
    发明授权
    3-Amino-5-(hydroxy- and/or aminophenyl)-6-(lower-alkyl)-2(1H)-pyridinones and cardiotonic use thereof 失效
    3-氨基-5-（羟基 - 和/或氨基苯基）-6-（低级烷基）-2（1H） - 吡啶酮及其强心使用

    公开(公告)号：US4515797A

    公开(公告)日：1985-05-07

    申请号：US355229

    申请日：1982-03-05

    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 ,  C07D211/72

    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。

    1,3-Dihydro-6-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones and -imidazo[4,5-b]pyridine-2-thiones and their cardiotonic use
    10.
    发明授权
    1,3-Dihydro-6-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones and -imidazo[4,5-b]pyridine-2-thiones and their cardiotonic use 失效
    1,3-二氢-6-（吡啶基）-2H-咪唑并[4,5-b]吡啶-2-酮和咪唑并[4,5-b]吡啶-2-硫杂及其强心使用

    公开(公告)号：US4294837A

    公开(公告)日：1981-10-13

    申请号：US135105

    申请日：1980-03-28

    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： C07D213/61 ,  C07D213/64 ,  C07D213/73 ,  C07D471/04 ,  A61K31/415

    CPC分类号： C07D213/64 ,  C07D213/61 ,  C07D213/73 ,  C07D471/04

    摘要： 1,3-Dihydro-1-R.sub.1 -3-R.sub.3 -6-PY-5-Q-2H-imidazo[4,5-b]pyridin-2-ones or -2-thiones or pharmaceutically-acceptable acid-addition salts thereof, which are useful as cardiotonic agents, where Q is hydrogen or lower-alkyl, R.sub.1 and R.sub.3 are each hydrogen, lower-alkyl, lower-hydroxyalkyl, 2,3-dihydroxypropyl, lower-alkoxyalkyl or Y-NB where Y is lower-alkylene and NB is di-(lower-alkyl)amino or 4-morpholinyl, at least one of R.sub.1 and R.sub.3 being hydrogen, and PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two substituents, are prepared by reacting a 2-R.sub.3 NH-3-R.sub.1 NH-5-PY-6-Q-pyridine with urea or carbonyldiimidazole to produce said -2-one or with an alkali metal xanthate, thiourea or thiocarbonyldiimidazole to produce said -2-thione. Also shown and claimed are cardiotonic compositions and a method for increasing cardiac contractility using said cardiotonic agents. Also shown are processes for preparing said intermediate 2-R.sub.3 NH-3-R.sub.1 NH-5-PY-6-Q-pyridines and other intermediates used in said processes.

    摘要翻译： 1,3-二氢-1-R1-3-R3-6-PY-5-Q-2H-咪唑并[4,5-b]吡啶-2-酮或-2-硫酮或其药学上可接受的酸加成盐 其可用作强心剂，其中Q为氢或低级烷基，R 1和R 3各自为氢，低级烷基，低级羟烷基，2,3-二羟基丙基，低级烷氧基烷基或Y-NB，其中Y为低级 - 亚烷基和NB是二 - （低级 - 烷基）氨基或4-吗啉基，R 1和R 3中的至少一个是氢，PY是具有一个或两个取代基的4-或3-吡啶基或4-或3-吡啶基， 通过使2-R3NH-3-R1NH-5-PY-6-Q-吡啶与脲或羰基二咪唑反应制备所述-2-酮或与碱金属黄原酸盐，硫脲或硫代羰基二咪唑反应制备所述-2-硫酮 。 还显示和要求保护的是强心剂组合物和使用所述强心剂增加心肌收缩力的方法。 还显示了制备所述中间体2-R3NH-3-R1NH-5-PY-6-Q-吡啶以及用于所述方法的其它中间体的方法。