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1. 发明授权

US4297360A 5-(Pyridinyl)pyridine-2,3-diamines, preparation thereof and their cardiotonic use 失效
标题翻译： 5-（吡啶基）吡啶-2,3-二胺，其制备及其强心使用
公开(公告)号：US4297360A
公开(公告)日：1981-10-27
申请号：US135100
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 , A61K31/4418 , A61P9/04 , C07D213/50 , C07D213/61 , C07D213/64 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/77 , C07D213/80 , C07D213/82 , C07D213/85 , C07D401/04 , A61K31/535 , C07D413/14
CPC分类号： C07D213/85 , C07D213/50 , C07D213/61 , C07D213/64 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/77 , C07D213/80 , C07D213/82
摘要： 2-R.sub.3 RN-3-R.sub.1 R'N-5-PY-6-Q-pyridines (I) or pharmaceutically-acceptable acid-addition salts thereof are useful as intermediates in the preparation of 1- or 3-substituted-1,3-dihydro-5-Q-6-PY-2H-imidazo[4,5-b]pyridin-2-ones or -2-thiones and also as intermediates for preparing 1- or 3-substituted-5-Q-6-PY-3H(or 1H)-imidazo[4,5-b]pyridines, where R.sub.1, R.sub.3, R, R', PY and Q are defined hereinbelow. Also shown are processes for preparing I and the following intermediates used therein: 2-halo-3-nitro-5-PY-6-Q-pyridines (III), 2-R.sub.3 RN-3-nitro-5-PY-6-Q-pyridines (V), 2-halo-5-PY-6-Q-pyridines (VII), 2-R.sub.3 RN-5-PY-6-Q-pyridines (VIII) and 2-R.sub.3 RN-3-halo-5-PY-6-Q-pyridines (IX) or salts thereof. Certain embodiments of II and VIII also are useful as cardiotonics and are shown as active components of cardiac compositions and methods for increasing cardiac contractility.
摘要翻译： 2-R3RN-3-R1R'N-5-PY-6-Q-吡啶（I）或其药学上可接受的酸加成盐可用作制备1-或3-取代-1,3- 二氢-5-Q-6-PY-2H-咪唑并[4,5-b]吡啶-2-酮或2-硫杂并且还可用作制备1-或3-取代的-5-Q-6-PY -3H（或1H） - 咪唑并[4,5-b]吡啶，其中R1，R3，R，R'，PY和Q定义如下。还示出了制备I及其中使用的以下中间体的方法：2-卤-3-硝基-5-PY-6-Q-吡啶（III），2-R3RN-3-硝基-5-PY-6-Q （V），2-卤代-5-PY-6-Q-吡啶（VII），2-R3RN-5-PY-6-Q-吡啶（VIII）和2-R3RN-3-卤代-5- PY-6-Q-吡啶（IX）或其盐。 II和VIII的某些实施方案也可用作强心剂，并且显示为心脏组合物的活性成分和用于增加心脏收缩力的方法。

2. 发明授权

US4199586A Di-(lower-alkyl) N-[1,2-dihydro-2-oxo-5-(pyridinyl)-3-pyridinyl]amino-methylanemalonates 失效
标题翻译：二 - （低级烷基）N- [1,2-二氢-2-氧代-5-（吡啶基）-3-吡啶基]氨基 - 甲基丙二酸酯
公开(公告)号：US4199586A
公开(公告)日：1980-04-22
申请号：US937120
申请日：1978-08-28
申请人： George Y. Lesher , Chester J. Opalka, Jr.
发明人： George Y. Lesher , Chester J. Opalka, Jr.
IPC分类号： A61K31/44 , C07D213/38 , C07D213/48 , C07D213/53 , C07D213/64 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/80 , C07D213/82 , C07D213/85
CPC分类号： C07D213/53 , C07D213/38 , C07D213/48 , C07D213/64 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/80 , C07D213/82 , C07D213/85
摘要： Compounds useful as cardiotonic agents are 1-R-3-Q-5-PY-2(1H)-pyridinones (I) where R is hydrogen, lower-alkyl or lower-hydroxyalkyl, Q is amino (preferred), lower-alkylamino, di-(lower-alkyl)amino or NHAc, Ac is lower-alkanoyl or lower-carbalkoxy, and PY is 4- or 3- or 2-pyridinyl or 4- or 3- or 2-pyridinyl having one or two lower-alkyl substituents. The corresponding compounds where Q is nitro, carbamyl, cyano, halo or hydrogen are useful as intermediates and those where Q is hydrogen or cyano also are useful as cardiotonic agents. Said compounds are prepared: by reacting .alpha.-PY-.beta.-(R.sub.1 R.sub.2 N)acrolein (II) with malonamide to produce 1,2-dihydro-2-oxo-5-PY-nicotinamide (Ia) and reacting Ia with a reagent capable of converting carbamyl to amino to produce 3-amino-5-PY-2(1H)-pyridinone (Ib); by reacting II or .alpha.-PY-malonaldehye (II') with .alpha.-cyanoacetamide to produce 1,2-dihydro-2-oxo-5-PY-nicotinonitrile (III) and partially hydrolyzing III to produce Ia; and, by heating 1,2-dihydro-2-oxo-5-PY-nicotininc acid (IV) with a mixture of concentrated sulfuric acid and concentrated nitric acid to produce 3-nitro-5-PY-2(1H)-pyridinone (Ic) and then either reducing Ic to produce Ib or first reacting Ic with an alkylating agent to produce 1-R'-3-nitro-5-PY-2(1H)-pyridinone (Id) and reducing Ic to produce 1-R'-3-amino-5-PY-2(1H)-pyridinone (Ib) where R' is lower-alkyl or lower-hydroxyalkyl. Other derivatives of I where Q is amino are shown.
摘要翻译：可用作强心剂的化合物是1-R-3-Q-5-PY-2（1H） - 吡啶酮（I），其中R是氢，低级烷基或低级羟基烷基，Q是氨基（优选），低级烷基氨基，二 - （低级烷基）氨基或NHAc，Ac是低级烷酰基或低级 - 烷酰氧基，PY是4-或3-或2-吡啶基或具有一个或两个低级烷酰氧基的4-或3-或2-吡啶基，烷基取代基。其中Q为硝基，氨基甲酰基，氰基，卤素或氢的相应化合物可用作中间体，Q为氢或氰基的化合物也可用作强心剂。制备所述化合物：通过使α-P-β - （R 1 R 2 N）丙烯醛（II）与丙二酰胺反应以产生1,2-二氢-2-氧代-5-PY-烟酰胺（Ia），并使Ia与能够将氨基甲酰转化为氨基，得到3-氨基-5-PY-2（1H） - 吡啶酮（Ib）; 通过使II或α-P-马来酸酐（II'）与α-氰基乙酰胺反应，生成1,2-二氢-2-氧代-5-PY-烟腈（III）并部分水解III产生Ia; 并通过用浓硫酸和浓硝酸的混合物加热1,2-二氢-2-氧代-5-PY-烟酸（IV）以产生3-硝基-5- PY-2（1H） - 吡啶酮（Ic），然后还原Ic以产生Ib或首先使Ic与烷基化剂反应以产生1-R'-3-硝基-5-PY-2（1H） - 吡啶酮（Id）并还原Ic以产生1- R'-3-氨基-5-PY-2（1H） - 吡啶酮（Ib）其中R'是低级烷基或低级 - 羟基烷基。其中Q为氨基的I的其它衍生物被显示。

3. 发明授权

US4465686A 5-(Hydroxy- and/or amino-phenyl)-6-(lower-alkyl)-2-(1H)-pyridinones, their cardiotonic use and preparation 失效
标题翻译： 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。

4. 发明授权

US4463008A 2-Alkoxy-5-(pyridinyl)pyridines and cardiotonic use thereof 失效
标题翻译： 2-烷氧基-5-（吡啶基）吡啶及其强心使用
公开(公告)号：US4463008A
公开(公告)日：1984-07-31
申请号：US440505
申请日：1982-11-10
申请人： George Y. Lesher , Chester J. Opalka, Jr. , Baldev Singh
发明人： George Y. Lesher , Chester J. Opalka, Jr. , Baldev Singh
IPC分类号： A61K31/44 , A61K31/4418 , A61P9/04 , C07D213/64 , C07D213/80 , C07D213/85 , C07D401/04
CPC分类号： C07D213/80 , C07D213/64 , C07D213/85
摘要： 2-(R.sub.1 O)-3-Q-5-PY-6-R-pyridine (I) or pharmaceutically acceptable acid-addition salts thereof are useful cardiotonics, where R.sub.1 is methyl or ethyl, R is hydrogen or lower-alkyl, PY is 4(or 3)-pyridinyl or 4(or 3)-pyridinyl having one or two lower-alkyl substituents, and Q is hydrogen, chloro or COOR' where R' is lower-alkyl, or Q is cyano only when R is hydrogen. The preparation of I and their cardiotonic use are shown.
摘要翻译： 2-（R 1 O）-3-Q-5-PY-6-R-吡啶（I）或其药学上可接受的酸加成盐是有用的强心剂，其中R1是甲基或乙基，R是氢或低级烷基，PY 是具有一个或两个低级烷基取代基的4（或3） - 吡啶基或4（或3） - 吡啶基，Q是氢，氯或COOR'，其中R'是低级烷基，或Q仅在R为氢。显示了我的准备及其强心使用。

5. 发明授权

US4420617A 5(Pyridinyl)pyridin-2-amines 失效
标题翻译： 5（吡啶基）吡啶-2-胺
公开(公告)号：US4420617A
公开(公告)日：1983-12-13
申请号：US395737
申请日：1982-07-06
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： 5-PY-6-Q-pyridin-2-amines (I) or pharmaceutically acceptable acid-addition salts thereof are useful cardiotonics, where Q is hydrogen or lower-alkyl, and PY is 4-pyridinyl or 4-pyridinyl having one or two lower-alkyl substituents. Their preparation from the corresponding 5-PY-6-Q-2(1H-pyridinones via the corresponding 2-halo-5-PY-6-Q-pyridines is shown.
摘要翻译： 5-PY-6-C-吡啶-2-胺（I）或其药学上可接受的酸加成盐是有用的强心剂，其中Q是氢或低级烷基，PY是4-吡啶基或4-吡啶基，其具有一个或两个低级烷基取代基。显示了其相应的5-PY-6-Q-2（1H-吡啶酮通过相应的2-卤代-5-PY-6-Q-吡啶的制备）。

6. 发明授权

US4225715A Preparation of 3-amino(or carbamyl)-5-(pyridinyl)-2(1H)-pyridinones 失效
标题翻译：制备3-氨基（或氨基甲酰基）-5-（吡啶基）-2（1H） - 吡啶酮
公开(公告)号：US4225715A
公开(公告)日：1980-09-30
申请号：US50507
申请日：1979-06-20
申请人： George Y. Lesher , Chester J. Opalka, Jr.
发明人： George Y. Lesher , Chester J. Opalka, Jr.
IPC分类号： A61K31/44 , C07D213/38 , C07D213/48 , C07D213/53 , C07D213/64 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/80 , C07D213/82 , C07D213/85 , C07D213/56
CPC分类号： C07D213/53 , C07D213/38 , C07D213/48 , C07D213/64 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/80 , C07D213/82 , C07D213/85
摘要： Compounds useful as cardiotonic agents are 1-R-3-Q-5-PY-2(1H)-pyridinones (I) where R is hydrogen, lower-alkyl or lower-hydroxyalkyl, Q is amino (preferred), lower-alkylamino, di-(lower-alkyl)amino or NHAc, Ac is lower-alkanoyl or lower-carbalkoxy, and PY is 4- or 3- or 2-pyridinyl or 4- or 3- or 2-pyridinyl having one or two lower-alkyl substituents. The corresponding compounds where Q is nitro, carbamyl, cyano, halo or hydrogen are useful as intermediates and those where Q is hydrogen or cyano also are useful as cardiotonic agents. Said compounds are prepared: by reacting .alpha.-PY-.beta.-(R.sub.1 R.sub.2 N)acrolein (II) with malonamide to produce 1,2-dihydro-2-oxo-5-PY-nicotinamide (Ia) and reacting Ia with a reagent capable of converting carbamyl to amino to produce 3-amino-5-PY-2(1H)-pyridinone (Ib); by reacting II or .alpha.-PY-malonaldehyde (II') with .alpha.-cyanoacetamide to produce 1,2-dihydro-2-oxo-5-PY-nicotinonitrile (III) and partially hydrolyzing III to produce Ia; and, by heating 1,2-dihydro-2-oxo-5-PY-nicotincic acid (IV) with a mixture of concentrated sulfuric acid and concentrated nitric acid to produce 3-nitro-5-PY-2(1H)-pyridinone (Ic) and then either reducing Ic to produce Ib or first reacting Ic with an alkylating agent to produce 1-R'-3-nitro-5-PY-2(1H)-pyridinone (Id) and reducing Id to produce 1-R'-3-amino-5-PY-2(1H)-pyridinone (Ib) where R' is lower-alkyl or lower-hydroxyalkyl. Other derivatives of I where Q is amino are shown.
摘要翻译：可用作强心剂的化合物是1-R-3-Q-5-PY-2（1H） - 吡啶酮（I），其中R是氢，低级烷基或低级羟基烷基，Q是氨基（优选），低级烷基氨基，二 - （低级烷基）氨基或NHAc，Ac是低级烷酰基或低级 - 烷酰氧基，PY是4-或3-或2-吡啶基或具有一个或两个低级烷酰氧基的4-或3-或2-吡啶基，烷基取代基。其中Q为硝基，氨基甲酰基，氰基，卤素或氢的相应化合物可用作中间体，Q为氢或氰基的化合物也可用作强心剂。制备所述化合物：通过使α-P-β - （R 1 R 2 N）丙烯醛（II）与丙二酰胺反应以产生1,2-二氢-2-氧代-5-PY-烟酰胺（Ia），并使Ia与能够将氨基甲酰转化为氨基，得到3-氨基-5-PY-2（1H） - 吡啶酮（Ib）; 通过使II或α-P-丙二醛（II'）与α-氰基乙酰胺反应以产生1,2-二氢-2-氧代-5-PY-烟腈（III）并部分水解III产生Ia; 并通过用浓硫酸和浓硝酸的混合物加热1,2-二氢-2-氧代-5-PY-烟酸（IV），得到3-硝基-5-苯基-2（1H） - 吡啶酮（Ic），然后还原Ic以产生Ib或者首先使Ic与烷基化剂反应以产生1-R'-3-硝基-5-苯基-2（1H） - 吡啶酮（Id）并还原Id以产生1- R'-3-氨基-5-PY-2（1H） - 吡啶酮（Ib）其中R'是低级烷基或低级 - 羟基烷基。其中Q为氨基的I的其它衍生物被显示。

7. 发明授权

US4223149A Process for producing 3-cyano-5-(pyridinyl)-2(1H)-pyridinones 失效
标题翻译：制备3-氰基-5-（吡啶基）-2（1H） - 吡啶酮的方法
公开(公告)号：US4223149A
公开(公告)日：1980-09-16
申请号：US60758
申请日：1979-07-26
申请人： Chester J. Opalka, Jr. , George Y. Lesher
发明人： Chester J. Opalka, Jr. , George Y. Lesher
IPC分类号： C07D213/85 , C07D401/04
CPC分类号： C07D213/85
摘要： A process for preparing 1,2-dihydro-2-oxo-5-(pyridinyl) nicotinonitriles by reacting .alpha.-(pyridinyl)-.beta.-[di-(lower-alkyl)amino]acrolein with malononitrile in a lower-alkanol. The products are useful as cardiotonic agents and, also, as intermediates for preparing corresponding 3-amino-5-(pyridinyl-2(1H)-pyridinones, in turn, useful as cardiotonic agents.
摘要翻译：一种通过α-（吡啶基）-β-[二（低级 - 烷基）氨基]丙烯醛与丙二腈在低级链烷醇中反应制备1,2-二氢-2-氧代-5-（吡啶基）烟腈的方法。该产品可用作强心剂，也可用作制备相应的3-氨基-5-（吡啶基-2（1H） - 吡啶酮的中间体，其又可用作强心剂。

8. 发明授权

US4391811A 2-Amino-6-(pyridinyl)-3H-imidazo[4,5-b]pyridines and their cardiotonic use 失效
标题翻译： 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。

9. 发明授权

US4362734A 2-(Substituted-amino)-5-(pyridinyl-nicotinonitriles, and their cardiotonic use 失效
标题翻译： 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。

10. 发明授权

US4331672A 5-(Pyridinyl)pyridine-2-hydrazines, their preparation and their cardiotonic use 失效
标题翻译： 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。

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