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8 条记录 (耗时 0.011 秒)

    Antihypertensive N-piperazinylalkanoylanilides
    2.
    发明授权
    Antihypertensive N-piperazinylalkanoylanilides 失效
    抗高血压的N-哌嗪基烷酰基酰苯胺

    公开(公告)号：US4940711A

    公开(公告)日：1990-07-10

    申请号：US373451

    申请日：1989-06-30

    申请人： Dante Nardi ,  Amedeo Leonardi ,  Alberto Catto ,  Gabriele Graziani

    发明人： Dante Nardi ,  Amedeo Leonardi ,  Alberto Catto ,  Gabriele Graziani

    IPC分类号： C07D295/14 ,  A61K31/495 ,  A61P9/12 ,  C07D295/15 ,  C07D317/66

    CPC分类号： C07D295/15 ,  C07D317/66

    摘要： N-piperazinylalkanoylanilides of the formula ##STR1## wherein n is 0, 1 or 2, each of R and R.sub.1 is H or alkyl, and each of R.sub.2, R.sub.3 and R.sub.4 is H, halogen, alkyl, hydroxyalkyl, alkoxy, aralkoxy, alkylthio, aralkylthio, alkylsulphonyl, alkylsulphenyl, NO.sub.2, NH.sub.2, alkylamino, acylamino, ureido, alkylureido, alkylsulphonylamino, CF.sub.3, acyl, CN, COOH, alkoxycarbonyl, NH.sub.2 CO, SO.sub.3 H, guanidinosulphonyl, carbamoyloxy, OH, acyloxy, alkylsulphonyloxy, alkylenedioxy or SO.sub.2 NR.sub.5 R.sub.6 wherein each of R.sub.5 and R.sub.6 is H, alkyl, aryl or acyl and their pharmaceutically acceptable acid addition salts, are antihypertensive agents.

    摘要翻译： 式（I）的N-哌嗪基烷酰基酰苯胺其中n为0,1或2，R和R 1各自为H或烷基，R 2，R 3和R 4各自为H，卤素，烷基，羟基烷基，烷氧基， 芳烷氧基，烷硫基，芳烷硫基，烷基磺酰基，烷基亚磺酰基，NO2，NH2，烷基氨基，酰基氨基，脲基，烷基脲基，酰基氨基，脲基，烷基脲基，烷基磺酰基氨基，CF3，酰基，CN，COOH，烷氧基羰基，NH2CO，SO3H，胍基磺酰基，氨基甲酰氧基，OH，酰氧基，烷基磺酰氧基，亚烷基二氧基或 SO 2 NR 5 R 6，其中R 5和R 6各自为H，烷基，芳基或酰基及其药学上可接受的酸加成盐，为抗高血压药。

    Therapeutically effective .omega.-(4-(2-pyridyl)-piperazino)-alkanoylanilides
    3.
    发明授权
    Therapeutically effective .omega.-(4-(2-pyridyl)-piperazino)-alkanoylanilides 失效
    治疗上有效的ω-（4-（2-吡啶基）哌嗪基） - 烷酰基苯胺

    公开(公告)号：US4510140A

    公开(公告)日：1985-04-09

    申请号：US412818

    申请日：1982-08-30

    申请人： Dante Nardi ,  Alberto Catto ,  Alberto Tajana ,  Pietro Cazzulani ,  Gabriele Graziani

    发明人： Dante Nardi ,  Alberto Catto ,  Alberto Tajana ,  Pietro Cazzulani ,  Gabriele Graziani

    IPC分类号： A61K31/495 ,  A61P11/14 ,  A61P37/08 ,  C07D213/74 ,  C07D241/04

    CPC分类号： C07D213/74

    摘要： The .omega.-[4-(2-pyridyl)-piperazino]-alkanoylanilide compounds having the structural formula (I): ##STR1## wherein n is 1, 2 or 3, each of R, R.sub.1, R.sub.2 R.sub.3, and R.sub.4 is independently hydrogen, halogen, alkyl, alkoxy, OH, NH.sub.2, CF.sub.3, CN, alkylthio, 1-hydroxyalkyl, alkanoyl, NH.sub.2 CO, NH.sub.2 SO.sub.2, alkoxycarbonyl, alkylsulfonyl, benzyloxy, alkanoylamino, NH.sub.2 CONH, 3-phenylureido, 3-alkylureido or alkoxyoxalylamino, R.sub.5 is hydrogen or alkyl, and R.sub.6 is hydrogen or alkoxy, and the pharmaceutically acceptable salts thereof, are effective antianaphylactics, antibronchospastics, antihistaminics, sedatives, analgesics, antiserotonics and blood-pressure-lowering agents.

    摘要翻译： 具有结构式（I）的ω-[4-（2-吡啶基） - 哌嗪基] - 烷酰基苯胺化合物：其中n为1,2或3，各自为R，R 1，R 2，R 3和 R4独立地是氢，卤素，烷基，烷氧基，OH，NH2，CF3，CN，烷硫基，1-羟基烷基，烷酰基，NH2CO，NH2SO2，烷氧基羰基，烷基磺酰基，苄氧基，烷酰基氨基，NH2CONH，3-苯基脲基，3-烷基脲基或烷氧基酰氨基 R5为氢或烷基，R6为氢或烷氧基，其药学上可接受的盐为有效的抗过敏药，抗骨质疏松药，抗组胺药，镇静剂，镇痛药，抗组胺药和降血压药。

    N-(3,3-diphenylpropyl) aminoethyl esters of 1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylic acid, compositions and use
    4.
    发明授权
    N-(3,3-diphenylpropyl) aminoethyl esters of 1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylic acid, compositions and use 失效
    1,4-二氢-2,6-二甲基 - 吡啶-3,5-二羧酸的N-（3,3-二苯基丙基）氨基乙基酯，组合物和用途

    公开(公告)号：US4705797A

    公开(公告)日：1987-11-10

    申请号：US701672

    申请日：1985-02-14

    申请人： Dante Nardi ,  Amedeo Leonardi ,  Gabriele Graziani ,  Giorgio Bianchi

    发明人： Dante Nardi ,  Amedeo Leonardi ,  Gabriele Graziani ,  Giorgio Bianchi

    IPC分类号： A61K31/41 ,  A61K31/435 ,  A61K31/44 ,  A61K31/455 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  C07C67/00 ,  C07C201/00 ,  C07C205/56 ,  C07D211/90 ,  C07D413/04 ,  C07D413/14

    CPC分类号： C07D413/04 ,  C07C205/56 ,  C07D211/90

    摘要： Novel antihypertensive and coronary dilating asymmetric diesters of 1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylic acid (or the stereoisomers or pharmaceutically acceptable acid addition salts thereof) have the general formula (I): ##STR1## wherein Ph is phenyl, Ar is 2-nitrophenyl, 3-nitrophenyl, 2,3-dichlorophenyl or benzofurazan-4-yl, A is a straight or branched chain alkylene radical having from 2 to 6 carbon atoms, R is a straight or branched chain alkyl radical having from 1 to 6 carbon atoms, optionally mono-substituted by an alkoxy substituent having from 1 to 6 carbon atoms, R.sub.1 is hydrogen, hydroxy or an alkyl radical having from 1 to 4 carbon atoms, and R.sub.2 is hydrogen or methyl. The subject diesters are facilely prepared from the aldehydes ArCHO and esters of acetoacetic and 3-aminocrotonic acids.

    摘要翻译： 1,4-二氢-2,6-二甲基 - 吡啶-3,5-二羧酸（或其立体异构体或其药学上可接受的酸加成盐）的新型抗高血压和冠状动脉扩张不对称二酯具有通式（I）：（I）其中Ph是苯基，Ar是2-硝基苯基，3-硝基苯基，2,3-二氯苯基或苯并呋咱-4-基，A是具有2至6个碳原子的直链或支链亚烷基，R是 具有1至6个碳原子的直链或支链烷基，任选被具有1至6个碳原子的烷氧基取代基单取代，R 1是氢，羟基或具有1至4个碳原子的烷基，R 2 是氢或甲基。 受试二酯由醛ArCHO和乙酰乙酸和3-氨基巴豆酸的酯容易地制备。

    Therapeutically effective piperidyl N-(4-quinolyl)-anthraniloyloxyalkanoates
    6.
    发明授权
    Therapeutically effective piperidyl N-(4-quinolyl)-anthraniloyloxyalkanoates 失效
    治疗上有效的N-（4-喹啉基） - 芴基氧代烷酸烷基酯

    公开(公告)号：US4482561A

    公开(公告)日：1984-11-13

    申请号：US441093

    申请日：1982-11-12

    申请人： Dante Nardi ,  Gianni Motta ,  Rodolfo Testa ,  Gabriele Graziani

    发明人： Dante Nardi ,  Gianni Motta ,  Rodolfo Testa ,  Gabriele Graziani

    IPC分类号： A61K31/47 ,  A61P25/04 ,  A61P29/00 ,  C07D211/42 ,  C07D211/46 ,  C07D211/52 ,  C07D401/12 ,  C07D215/44

    CPC分类号： C07D401/12 ,  C07D211/42 ,  C07D211/46 ,  C07D211/52

    摘要： The N-substituted-4-(optionally substituted)-2-, 3- or 4-piperidyl N-(7- or 8-substituted-4-quinolyl)-anthraniloyloxyalkanoates having the structural formula (I): ##STR1## in which R is a straight or branched chain alkyl radical having from 1 to 4 carbon atoms; an alkenyl or alkynyl radical having from 2 to 6 carbon atoms; a benzyl, phenethyl, 4-nitrophenethyl or 4-aminophenethyl radical; or a phenacyl, benzoylethyl, .beta.-hydroxyphenethyl or .alpha.-hydroxyphenylpropyl radical, optionally substituted on the phenyl ring by one or more halogen atom, trifluoromethyl, nitro or amino substituents, or an alkyl substituent having from 1 to 4 carbon atoms or an alkoxy substituent having from 1 to 4 carbon atoms; R.sub.1 is a hydrogen atom or a phenyl radical; each of R.sub.2 and R.sub.3 is independently a hydrogen atom or an alkyl radical having from 1 to 4 carbon atoms; one of R.sub.4 and R.sub.5 is a chlorine atom or a trifluoromethyl radical and the other of R.sub.4 and R.sub.5 is a hydrogen atom; and the pharmaceutically acceptable salts of such esters; are effective analgesics, anti-inflammatories and antidepressants; are also strong inhibitors of platelet aggregation, and thus too are useful in the treatment of cerebral thrombosis, cerebral and cardiac infarction, and arteriosclerotic disorders.

    摘要翻译： 具有结构式（I）的N-取代-4-（任选取代的）2-，3-或4-哌啶基N-（7-或8-取代-4-喹啉基） - 芴基氧氟烷基酯： ）其中R是具有1至4个碳原子的直链或支链烷基; 具有2至6个碳原子的烯基或炔基; 苄基，苯乙基，4-硝基苯乙基或4-氨基苯乙基; 或苯基酰基苯甲酰基，β-羟基苯乙基或α-羟基苯基丙基，其在苯环上被一个或多个卤素原子，三氟甲基，硝基或氨基取代基取代，或具有1至4个碳原子的烷基取代基或烷氧基取代基 具有1至4个碳原子; R1是氢原子或苯基; R 2和R 3各自独立地为氢原子或具有1至4个碳原子的烷基; R4和R5之一是氯原子或三氟甲基，R4和R5中的另一个是氢原子; 和这些酯的药学上可接受的盐; 是有效的镇痛药，抗炎药和抗抑郁药; 也是血小板聚集的强抑制剂，因此也可用于治疗脑血栓形成，脑和心肌梗死以及动脉硬化性疾病。