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    1-(Substituted aminoalkyl)-1,4-dihydropyridines
    41.
    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
    42.
    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。

    Compositions for treating acne
    45.
    发明授权
    Compositions for treating acne 失效
    用于治疗痤疮的组合物

    公开(公告)号：US4364940A

    公开(公告)日：1982-12-21

    申请号：US237234

    申请日：1981-02-23

    申请人： Edward S. Neiss ,  Bernard Loev

    发明人： Edward S. Neiss ,  Bernard Loev

    IPC分类号： A61K31/60 ,  A61K8/38 ,  A61K31/235 ,  A61K33/40 ,  A61P17/00 ,  A61Q19/00 ,  C07C409/34

    CPC分类号： A61Q19/00 ,  A61K8/38 ,  Y10S514/859

    摘要： A composition for the treatment of acne in the form of a solution, lotion or cream containing from about 1 to 10% by weight of a compound of the formula ##STR1## wherein R is an alkyl having up to 6 carbon atoms or aryl having up to 10 carbon atoms and R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl having up to 6 carbon atoms, phenyl, phenyl-lower alkyl, lower alkylphenyl, halogen, halophenyl, trifluoromethyl, trifluoromethylphenyl, lower alkoxy, methylenedioxy, and lower alkoxyphenyl.

    摘要翻译： 用于治疗痤疮形式的组合物，其含有约1-10重量％的下式化合物，其中R是具有至多6个碳原子的烷基或具有至多6个碳原子的芳基 至10个碳原子，R 1和R 2独立地为氢，具有至多6个碳原子的低级烷基，苯基，苯基 - 低级烷基，低级烷基苯基，卤素，卤代苯基，三氟甲基，三氟甲基苯基，低级烷氧基，亚甲二氧基和低级烷氧基苯基。

    8-Alkyl and alkenyl-10-hydroxy-5H[1]benzopyranopyridine derivatives having polyphagic activity
    49.
    发明授权
    8-Alkyl and alkenyl-10-hydroxy-5H[1]benzopyranopyridine derivatives having polyphagic activity 失效
    8-烷基和链烯基-10-羟基-5H- {具有多肽活性的{8 1 {9-苯并吡喃并吡啶衍生物

    公开(公告)号：US3962448A

    公开(公告)日：1976-06-08

    申请号：US570130

    申请日：1975-04-21

    申请人： Clifton A. Baile ,  Paul E. Bender ,  Bernard Loev

    发明人： Clifton A. Baile ,  Paul E. Bender ,  Bernard Loev

    IPC分类号： C07D491/04 ,  A61K31/44

    CPC分类号： C07D491/04

    摘要： 8-Alkyl and alkenyl-10-hydroxy-5H[1]benzopyranopyridines are prepared by dehydrogenation of the corresponding N-benzyl or N-hydrogen-8-alkyl or alkenyl-1,2,3,4-tetrahydro-5H[1]benzopyranopyridines in a high boiling solvent in the presence of a noble metal dehydrogenation catalyst. Alkyl derivatives of 5-11 carbon atoms are particularly useful. Also the O-acetyl derivatives are very useful. The compounds are central nervous system depressants and animal polyphagic agents.

    摘要翻译： 8-烷基和链烯基-10-羟基-5H [1]苯并吡喃并吡啶通过相应的N-苄基或N-氢-8-烷基或链烯基-1,2,3,4-四氢-5H- [1] 苯并吡喃并吡啶在高沸点溶剂中，在贵金属脱氢催化剂存在下进行。 5-11个碳原子的烷基衍生物是特别有用的。 O-乙酰基衍生物也是非常有用的。 这些化合物是中枢神经系统抑制剂和动物多药剂。

    5-Heterocyclic-1,2,3,6-tetrahydro-4(5H) pyrimidinone
    50.
    发明授权
    5-Heterocyclic-1,2,3,6-tetrahydro-4(5H) pyrimidinone 失效
    5-杂环-1,2,3,6-四氢-4（5H）嘧啶酮

    公开(公告)号：US3956325A

    公开(公告)日：1976-05-11

    申请号：US584327

    申请日：1975-06-06

    申请人： Bernard Loev

    发明人： Bernard Loev

    IPC分类号： C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D239/04

    CPC分类号： C07D417/04 ,  C07D401/04 ,  C07D403/04 ,  Y10S514/825

    摘要： The compounds of this invention are 5-heterocyclic-1,2,3,6-tetrahydro-4(5H)-pyrimidinethiones which have pharmacological activity, in particular gastric acid secretion inhibitory activity, and 5-heterocyclic-1,2,3,6-tetrahydro-4(5H)-pyrimidinones which are intermediates in the preparation therefor.

    摘要翻译： 本发明的化合物是具有药理活性，特别是胃酸分泌抑制活性的5-杂环-1,2,3,6-四氢-4（5H） - 嘧啶硫酮，和5-杂环-1,2,3,4-四氢-4 6-（四氢-4H） - 嘧啶酮，其制备中间体。