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    1-(Substituted aminoalkyl)-1,4-dihydropyridines
    1.
    发明授权
    1-(Substituted aminoalkyl)-1,4-dihydropyridines 失效
    1-（取代的氨基烷基）-1,4-二氢吡啶

    公开(公告)号：US4500532A

    公开(公告)日：1985-02-19

    申请号：US471592

    申请日：1983-03-03

    申请人： Bernard Loev ,  Howard Jones ,  John T. Suh

    发明人： Bernard Loev ,  Howard Jones ,  John T. Suh

    IPC分类号： C07D211/90 ,  A61K31/505 ,  A61K31/455 ,  C07D211/82 ,  C07D401/04

    CPC分类号： C07D211/90

    摘要： Compounds of the formula ##STR1## wherein Z is alkylene containing 1 to 5 carbon atoms; R.sub.3 is aminoalkyl containing 2 to 4 carbon atoms; R.sub.4 is H, alkyl, cycloalkyl, aminoalkyl, hydroxyalkyl or alkoxyalkyl; and the remainder of the variables are as described in the specification are useful as anti-hypertensives.

    摘要翻译： 其中Z是含有1至5个碳原子的亚烷基的化合物＆lt; IMAGE＆gt; R3是含2至4个碳原子的氨基烷基; R4是H，烷基，环烷基，氨基烷基，羟基烷基或烷氧基烷基; 并且其余的变量如说明书中所述用作抗高血压药物。

    N-(substituted piperazino)-1,4-dihydropyridine-3,5-carboxylic acid
    2.
    发明授权
    N-(substituted piperazino)-1,4-dihydropyridine-3,5-carboxylic acid 失效
    N-（取代的哌嗪子基）-1,4-二氢吡啶-3,5-羧酸

    公开(公告)号：US4491582A

    公开(公告)日：1985-01-01

    申请号：US471594

    申请日：1983-03-03

    申请人： Bernard Loev ,  Howard Jones ,  John T. Suh

    发明人： Bernard Loev ,  Howard Jones ,  John T. Suh

    IPC分类号： C07D211/90 ,  C07D403/06 ,  A61K31/495

    CPC分类号： C07D211/90

    摘要： 1,4-Dihydropyridine carboxylic acid esters of the formula: ##STR1## wherein Ar is heteroaryl selected from the group consisting of thiophene, furan, pyridine, thiazole, pyrimidine, pyrrole, benzofuran, quinoline and benzothiophene, cycloalkyl having from 3 to 7 carbon atoms, naphthyl, indanyl, indenyl, tetrahydronaphthyl, or a radical of the formula ##STR2## wherein each of R.sub.5, R.sub.6 and R.sub.7 is independently H, alkyl, phenyl, tolyl, naphthyl, halo, lower alkoxy, nitro, amino, alkylmercapto, cyano, carboxy, carbalkoxy, sulfamyl, trifluoromethyl, hydroxy, methanesulfonyl, or alkylamino and R.sub.5 and R.sub.6 when taken together, form a methylenedioxy; Z is alkylene containing 1 to about 5 carbon atoms in the principal chain; each R.sub.1 is independently hydrogen, alkyl or alkoxyalkyl, with the proviso that only one R.sub.1 may be hydrogen; R.sub.2 is lower alkyl; and wherein N, R.sub.3 and R.sub.4 when taken together form piperazinyl; wherein the alkyl of the alkyl, carbalkoxy, alkylamino, alkoxy, alkylmercapto, alkylamino, and alkoxyalkyl contains 1-10 carbon atoms; are useful for their antihypertensive activity.

    摘要翻译： 其中Ar为选自噻吩，呋喃，吡啶，噻唑，嘧啶，吡咯，苯并呋喃，喹啉和苯并噻吩的杂芳基，具有3-7个碳原子的环烷基 烷基，苯基，甲苯基，萘基，卤素，低级烷氧基，硝基，氨基，烷基巯基，烷基， 氰基，羧基，烷氧基，氨基磺酰基，三氟甲基，羟基，甲磺酰基或烷基氨基，R 5和R 6一起形成亚甲二氧基; Z是主链中含有1至约5个碳原子的亚烷基; 每个R 1独立地是氢，烷基或烷氧基烷基，条件是只有一个R 1可以是氢; R2是低级烷基; 并且其中N，R 3和R 4一起形成哌嗪基; 其中烷基，烷氧基，烷基氨基，烷氧基，烷基巯基，烷基氨基和烷氧基烷基的烷基含有1-10个碳原子; 对其抗高血压活性有用。

    N-Substituted-1-aminoalkyl-1,4-dihydropyridines
    3.
    发明授权
    N-Substituted-1-aminoalkyl-1,4-dihydropyridines 失效
    N-取代的-1-氨基烷基-1,4-二氢吡啶

    公开(公告)号：US4472584A

    公开(公告)日：1984-09-18

    申请号：US471959

    申请日：1983-03-03

    申请人： Bernard Loev ,  Howard Jones ,  John T. Suh

    发明人： Bernard Loev ,  Howard Jones ,  John T. Suh

    IPC分类号： C07D211/90 ,  C07D211/82 ,  A61K31/455 ,  C07D401/04 ,  C07D405/04

    CPC分类号： C07D211/90

    摘要： Compounds of the formula: ##STR1## wherein Ar is heteroaryl, cycloalkyl having from 3 to 7 carbon atoms, naphthyl, indanyl, indenyl, tetrahydro naphthyl, or a radical of the formula ##STR2## wherein each of R.sub.5, R.sub.6 and R.sub.7 is independently H, alkyl, aryl, halo, lower alkoxy, nitro, amino, alkylmercapto, cyano, carboxy, carbalkoxy, sulfamyl, trifluoromethyl, hydroxy, acyloxy, methanesulfonyl, alkylamino or acylamino; and R.sub.5 and R.sub.6 when taken together, form a methylenedioxy; Z is alkylene containing 1 to about 5 carbon atoms in the principal chain; each R.sub.1 is independently hydrogen, alkyl or alkoxyalkyl, with the proviso that only one R.sub.1 may be hydrogen; R.sub.2 is lower alkyl; R.sub.3 is hydroxyalkyl containing 2 to 4 carbon atoms and R.sub.4 is H, alkyl, cycloalkyl or hydroxyalkyl containing 2 to 4 carbon atoms; wherein the alkyl, alkoxy, and acyl groups contain up to 10 carbon atoms, and their pharmaceutically-acceptable salts are disclosed. These compounds have anti-hypertensive activity.

    摘要翻译： 下式的化合物：其中Ar是杂芳基，具有3至7个碳原子的环烷基，萘基，茚满基，茚基，四氢萘基或下式的基团其中R 5，R 6和R 7各自独立地是 H，烷基，芳基，卤素，低级烷氧基，硝基，氨基，烷基巯基，氰基，羧基，烷氧基，氨基磺酰基，三氟甲基，羟基，酰氧基，甲磺酰基，烷基氨基或酰基氨基; 并且R 5和R 6一起形成亚甲二氧基; Z是主链中含有1至约5个碳原子的亚烷基; 每个R 1独立地是氢，烷基或烷氧基烷基，条件是只有一个R 1可以是氢; R2是低级烷基; R3是含有2至4个碳原子的羟基烷基，R4是H，含2至4个碳原子的烷基，环烷基或羟基烷基; 其中烷基，烷氧基和酰基含有至多10个碳原子，并且公开了它们的药学上可接受的盐。 这些化合物具有抗高血压活性。

    Antihypertensive 1,4-thiazepine-ones, 1,4-thiazonine-ones, and method of use thereof
    6.
    发明授权
    Antihypertensive 1,4-thiazepine-ones, 1,4-thiazonine-ones, and method of use thereof 失效
    抗高血压药物1,4-硫氮杂菌素，1,4-噻嗪酮类药物及其应用方法

    公开(公告)号：US4287203A

    公开(公告)日：1981-09-01

    申请号：US142945

    申请日：1980-04-23

    申请人： John T. Suh ,  Bruce E. Williams ,  Jerry W. Skiles ,  Bernard Loev

    发明人： John T. Suh ,  Bruce E. Williams ,  Jerry W. Skiles ,  Bernard Loev

    IPC分类号： A61K31/55 ,  A61K31/554 ,  A61P9/12 ,  A61P43/00 ,  C07D277/06 ,  C07D279/12 ,  C07D281/06 ,  C07D513/04 ,  C07D281/04 ,  C07D281/18

    CPC分类号： C07D513/04 ,  C07D277/06 ,  C07D279/12 ,  C07D281/06

    摘要： Antihypertensive compounds of the structure ##STR1## wherein: n is an integer from 0 to 2 inclusive,R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 are independently hydrogen, alkyl having from 1 to 6 carbon atoms, alkenyl having from 2 to 6 carbon atoms, alkynyl having from 2 to 6 carbon atoms, cycloalkyl having from 3 to 16 carbon atoms, phenyl, benzyl, tolyl, naphthyl, phenethyl, indanyl, tetrahydronaphthyl, decanydronaphthyl, pyridyl, quinolyl, pyrrolidyl, pyrrolyl, morpholinyl, thiomorpholinyl, furyl, furfuryl, tetrahydrofurfuryl, benzimidazole, thienyl, imidolyl, or tetrahydroindolyl, and where the R.sub.1 to R.sub.7 groups are alkyl, said groups carrying a substituent selected from hydroxy, alkoxy, amino, carboxy, or carbalkoxy, the alkyl group in alkoxy and carbalkoxy having from 1 to 6 carbon atoms, or R.sub.2 taken together with R.sub.3 and the carbons to which they are attached is tetrahydronaphthyl or phenyl, and when phenyl R.sub.1 and R.sub.4 are absent, or R.sub.6 and R.sub.7 taken together with the carbon to which R.sub.6 is attached and the nitrogen to which R.sub.7 is attached form a heterocycle selected from pyrrolidyl, thiazolidine, tetrahydro-isoquinoline, thiomorpholine, or 2,2,5,5-tetramethylthiazolidinie, andY is .dbd.O, .dbd.S, .dbd.NR.sub.1, .dbd.NOR.sub.1 or .dbd.N--NH.sub.2, R.sub.1 being the same as defined above.

    摘要翻译： 结构的抗高血压化合物其中：n为0〜2的整数，R1，R2，R3，R4，R5，R6和R7独立地为氢，具有1-6个碳原子的烷基， 2至6个碳原子，具有2至6个碳原子的炔基，具有3至16个碳原子的环烷基，苯基，苄基，甲苯基，萘基，苯乙基，茚满基，四氢萘基，癸烷基萘基，吡啶基，喹啉基，吡咯烷基，吡咯基，吗啉基， 硫代吗啉基，呋喃基，糠基，四氢糠基，苯并咪唑，噻吩基，亚氨基或四氢吲哚基，其中R 1至R 7基团是烷基，所述基团含有选自羟基，烷氧基，氨基，羧基或烷氧基的取代基，烷氧基 和具有1至6个碳原子的烷氧基，或者R 2与R 3和它们所连接的碳一起为四氢萘基或苯基，当不存在R 1和R 4时，或者R 6和R 7与R 6一起 是attac 和R7连接的氮形成选自吡咯烷基，噻唑烷，四氢 - 异喹啉，硫代吗啉或2,2,5,5-四甲基噻唑烷的杂环，Y = O，= S，= NR1，= NOR1或 = N-NH 2，R 1与上述定义相同。

    Antihypertensive lactams
    7.
    发明授权
    Antihypertensive lactams 失效
    抗高血压内酰胺

    公开(公告)号：US4766210A

    公开(公告)日：1988-08-23

    申请号：US288134

    申请日：1981-07-29

    申请人： John T. Suh ,  Bruce E. Williams ,  Jerry W. Skiles ,  Bernard Loev

    发明人： John T. Suh ,  Bruce E. Williams ,  Jerry W. Skiles ,  Bernard Loev

    IPC分类号： C07D277/06 ,  C07D279/12 ,  C07D281/06 ,  C07D513/04

    CPC分类号： C07D513/04 ,  C07D277/06 ,  C07D279/12 ,  C07D281/06

    摘要： Antihypertensive compounds of the structure ##STR1## wherein: n is an integer from 0 to 2 inclusive,R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 are independently hydrogen, alkyl having from 1 to 6 carbon atoms, alkenyl having from 2 to 6 carbon atoms, alkynyl having from 2 to 6 carbon atoms, cycloalkyl having from 3 to 16 carbon atoms, phenyl, benzyl, tolyl, naphthyl, phenethyl, indanyl, tetrahydronaphthyl, decahydronaphthyl, pyridyl, quinolyl, pyrrolidyl, pyrrolyl, morpholinyl, thiomorpholinyl, furyl, furfuryl, tetrahydrofurfuryl, benzimidazole, thienyl, imidolyl, or tetrahydroindolyl, and where the R.sub.1 to R.sub.7 groups are alkyl, said groups carrying a substituent selected from hydroxy, alkoxy, amino, carboxy, or carbalkoxy, the alkyl group in alkoxy and carbalkoxy having from 1 to 6 carbon atoms, or R.sub.2 taken together with R.sub.3 and the carbons to which they are attached is tetrahydronapthyl or phenyl, and when phenyl R.sub.1 and R.sub.4 are absent, or R.sub.6 and R.sub.7 taken together with the carbon to which R.sub.6 is attached and the nitrogen to which R.sub.7 is attached form a heterocycle selected from pyrrolidyl, thiazolidine, tetrahydro-isoquinoline, thiomorpholine, or 2,2,5,5-tetramethylthiazolidinie, andY is .dbd.O, .dbd.S, .dbd.NR.sub.1, .dbd.NOR.sub.1 or .dbd.N--NH.sub.2, R.sub.1 being the same as defined above.

    摘要翻译： 结构的抗高血压化合物其中：n为0〜2的整数，R1，R2，R3，R4，R5，R6和R7独立地为氢，具有1-6个碳原子的烷基， 2至6个碳原子，具有2至6个碳原子的炔基，具有3至16个碳原子的环烷基，苯基，苄基，甲苯基，萘基，苯乙基，茚满基，四氢萘基，十氢萘基，吡啶基，喹啉基，吡咯烷基，吡咯基，吗啉基， 硫代吗啉基，呋喃基，糠基，四氢糠基，苯并咪唑，噻吩基，亚氨基或四氢吲哚基，其中R 1至R 7基团是烷基，所述基团含有选自羟基，烷氧基，氨基，羧基或烷氧基的取代基，烷氧基 和具有1至6个碳原子的烷氧基，或者R 2与R 3和它们所连接的碳一起是四氢萘基或苯基，当R 1和R 4不存在时，或者R 6和R 7与R 6一起 附上 并且R 7连接的氮形成选自吡咯烷基，噻唑烷，四氢 - 异喹啉，硫代吗啉或2,2,5,5-四甲基噻唑烷的杂环，Y = O，= S，= NR1，= NOR1或 = N-NH 2，R 1与上述定义相同。

    Antihypertensive lactams
    9.
    发明授权
    Antihypertensive lactams 失效
    抗高血压内酰胺

    公开(公告)号：US4347246A

    公开(公告)日：1982-08-31

    申请号：US263824

    申请日：1980-05-15

    申请人： John T. Suh ,  Bruce E. Williams ,  Jerry W. Skiles ,  Bernard Loev

    发明人： John T. Suh ,  Bruce E. Williams ,  Jerry W. Skiles ,  Bernard Loev

    IPC分类号： C07D277/06 ,  C07D279/12 ,  C07D281/06 ,  C07D513/04 ,  A61K31/55 ,  C07D281/04 ,  C07D281/18

    CPC分类号： C07D513/04 ,  C07D277/06 ,  C07D279/12 ,  C07D281/06

    摘要： A compound of the formula ##STR1## wherein: R.sub.1 is independently lower alkyl having from 1 to 6 carbon atoms, lower alkenyl having from 2 to 6 carbon atoms, lower alkynyl having from 2 to 6 carbon atoms, hydroxy, hydroxyalkyl, alkoxy, thio, thioalkyl, alkylmercapto, amino, aminoalkyl, alkylamino, nitro, cyano, alkanoyl, carboxy, carboxyalkyl, carbalkoxy, carbalkoxyalkyl, halogen, alkylsulfoxy, alkylsulfonyl, sulfonyl, sulfonamido, trifluoromethyl, or methylenedioxy, wherein the alkyl group in hydroxyalkyl, thioalkyl, aminoalkyl, carboxyalkyl, alkoxy, alkylmercapto, alkylsulfoxy, alkanoyl, carbalkoxy, and carbalkoxyalkyl has from 1 to 6 carbon atoms,n is an integer from 1 to 4 inclusive,R.sub.2 is selected from the group consisting of hydrogen and cycloalkyl, wherein the cycloalkyl group contains from 3 to 16 carbon atoms,R.sub.3 and R.sub.4 are hydrogen, andY is oxygen, sulphur, .dbd.NR.sub.1, .dbd.NOR.sub.1 or .dbd.N--NH.sub.2, R.sub.1 being the same as defined above.The compounds are useful as antihypertensives, and have angiotensin converting enzyme inhibitory activity.

    摘要翻译： 下式化合物其中：R 1独立地为具有1至6个碳原子的低级烷基，具有2至6个碳原子的低级烯基，具有2至6个碳原子的低级炔基，羟基，羟基烷基，烷氧基，硫代 ，烷基巯基，氨基，氨基烷基，烷基氨基，硝基，氰基，烷酰基，羧基，羧基烷基，烷氧基，烷氧基烷基，卤素，烷基磺酰氧基，烷基磺酰基，磺酰基，亚磺酰氨基，三氟甲基或亚甲二氧基，其中羟基烷基， ，羧基烷基，烷氧基，烷基巯基，烷基亚磺酰基，烷酰基，烷氧基和烷氧基烷基具有1至6个碳原子，n是1至4的整数，其中R 2选自氢和环烷基，其中环烷基包含 3至16个碳原子，R3和R4是氢，Y是氧，硫，= NR1，= NOR1或= N-NH2，R1与上述定义相同。 该化合物可用作抗高血压药，并具有血管紧张素转换酶抑制活性。