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14 条记录 (耗时 0.022 秒)

    4-(2-Pyridylamino)phenylacetic acid derivatives
    1.
    发明授权
    4-(2-Pyridylamino)phenylacetic acid derivatives 失效
    4-（2-吡啶基氨基）苯乙酸衍生物

    公开(公告)号：US4256753A

    公开(公告)日：1981-03-17

    申请号：US95572

    申请日：1979-11-19

    申请人： Hitoshi Uno ,  Yasutaka Nagai ,  Katsuhiko Hino ,  Hideo Nakamura

    发明人： Hitoshi Uno ,  Yasutaka Nagai ,  Katsuhiko Hino ,  Hideo Nakamura

    IPC分类号： A61K31/44 ,  A61K31/4402 ,  A61K31/4418 ,  A61P25/04 ,  A61P29/00 ,  C07D213/74

    CPC分类号： C07D213/74

    摘要： Novel 4-(2'-pyridylamino)phenylacetic acid derivatives of the formula: ##STR1## wherein R.sub.1 is hydrogen, a halogen, a lower alkyl having 1 to 3 carbon atoms, or nitro, R.sub.2 is hydrogen, a halogen, or a lower alkyl having 1 to 3 carbon atoms, R.sub.3 is hydrogen, a halogen, or a lower alkyl having 1 to 3 carbon atoms, R.sub.4 is hydrogen or a lower alkyl having 1 to 3 carbon atoms, R.sub.5 is hydrogen or --CH.sub.2 CH.sub.2 OR.sub.6 wherein R.sub.6 is a lower alkyl having 2 or 3 carbon atoms and being substituted with 1 or 2 hydroxy groups, provided that R.sub.1 or R.sub.2 is not 4-halogen, or pharmaceutically acceptable salts thereof, and a process for the preparation thereof, pharmaceutical composition of said compounds, and a method of using said compounds as anti-inflammatory and analgesic agents. They have excellent anti-inflammatory and analgesic activities with an extremely weak ulcerogenicity in the gastrointestinal tract. Some of the compounds have superior inhibitory activity against chronic inflammation mediated by cellular immunity.

    摘要翻译： 下式的新型4-（2'-吡啶基氨基）苯乙酸衍生物：其中R 1是氢，卤素，具有1至3个碳原子的低级烷基或硝基，R 2是氢，卤素或低级 具有1至3个碳原子的烷基，R 3是氢，卤素或具有1至3个碳原子的低级烷基，R 4是氢或具有1至3个碳原子的低级烷基，R 5是氢或-CH 2 CH 2 OR 6，其中R 6是 具有2或3个碳原子并且被1或2个羟基取代的低级烷基，条件是R1或R2不是4-卤素，或其药学上可接受的盐，及其制备方法，所述化合物的药物组合物和 使用所述化合物作为抗炎和止痛剂的方法。 它们具有优异的抗炎和止痛活性，在胃肠道中具有非常弱的溃疡形成能力。 一些化合物对由细胞免疫介导的慢性炎症具有优异的抑制活性。

    2-(1-piperazinyl)-4-substituted phenylquinoline derivatives, processes for the preparation thereof, and pharmaceutical composition containing the same
    2.
    发明授权
    2-(1-piperazinyl)-4-substituted phenylquinoline derivatives, processes for the preparation thereof, and pharmaceutical composition containing the same 失效
    2-（1-哌嗪基）-4-取代苯基喹啉衍生物，其制备方法和含有它们的药物组合物

    公开(公告)号：US4758566A

    公开(公告)日：1988-07-19

    申请号：US893311

    申请日：1986-07-28

    申请人： Hitoshi Uno ,  Katsuhiko Hino ,  Toshiaki Kadokawa ,  Katsuyoshi Kawashima

    发明人： Hitoshi Uno ,  Katsuhiko Hino ,  Toshiaki Kadokawa ,  Katsuyoshi Kawashima

    IPC分类号： A61K31/47 ,  A61P1/04 ,  C07D215/38 ,  A61K31/495 ,  C07D401/02

    CPC分类号： C07D215/38

    摘要： Compounds of the formula: ##STR1## wherein R.sub.1 represents fluorine atom at the para position, chlorine atom at the para position, methyl group at the para position or trifluoromethyl group at the para or meta position; and R.sub.2 represents hydrogen atom, methyl group, ethyl group, 2-hydroxyethyl group or 3-hydroxypropyl group, provided that R.sub.2 represents ethyl group, 2-hydroxyethyl group or 3-hydroxypropyl group when R.sub.1 represents fluorine atom at the para position, methyl group at the para position or trifluoromethyl group at the para position, and a pharmaceutically acceptable salt therof, process for the preparation thereof, and pharmaceutical composition containing the same. The compounds and pharmaceutically acceptable salts thereof show excellent cytoprotective effect and useful for prophylaxis and treatment of peptic ulcer and inflammatory gastrointestinal diseases.

    摘要翻译： PCT No.PCT / JP85 / 00654 Sec。 371日期1986年7月28日第 102（e）日期1986年7月28日PCT提交1985年11月27日PCT公布。 公开号WO86 / 03198 日期：1986年6月5日。下式的化合物：其中R1表示对位的氟原子，对位的氯原子，对位的甲基或对位或间位的三氟甲基; R2表示氢原子，甲基，乙基，2-羟乙基或3-羟丙基，条件是当R1表示对位的氟原子时，R2表示乙基，2-羟基乙基或3-羟丙基，甲基 在对位或在对位的三氟甲基，和其药学上可接受的盐，其制备方法和含有它们的药物组合物。 所述化合物及其药学上可接受的盐显示出优异的细胞保护作用并且可用于预防和治疗消化性溃疡和炎性胃肠道疾病。

    Anti-peptic ulcer agent
    3.
    发明授权
    Anti-peptic ulcer agent 失效
    抗消化性溃疡剂

    公开(公告)号：US4677107A

    公开(公告)日：1987-06-30

    申请号：US784215

    申请日：1985-10-04

    申请人： Toshiaki Kadokawa ,  Katsuyoshi Kawashima ,  Hitoshi Uno ,  Katsuhiko Hino

    发明人： Toshiaki Kadokawa ,  Katsuyoshi Kawashima ,  Hitoshi Uno ,  Katsuhiko Hino

    IPC分类号： A61K31/47 ,  C07D215/38 ,  A61K31/495

    CPC分类号： C07D215/38 ,  A61K31/47 ,  Y10S514/926 ,  Y10S514/927

    摘要： Use of a compound of the formula: ##STR1## wherein R is hydrogen atom or ethyl group, or a pharmaceutically acceptable salt thereof for prophylaxis and/or treatment of peptic ulcer, and a method for prophylaxis and/or treatment of peptic ulcer disease which comprises administering an effective amount of the above-mentioned compound to warm blooded aninal, especially human. Said active compounds have excellent pharmacological activities such as inhibition of ulceration and inhibition of gastric secretion, and hence, are useful as an anti-peptic ulcer agent.

    摘要翻译： 下式化合物：其中R是氢原子或乙基的化合物或其药学上可接受的盐用于消化性溃疡的预防和/或治疗，以及预防和/或治疗消化性溃疡疾病的方法，其中 包括将有效量的上述化合物给予温血的阴性，特别是人。 所述活性化合物具有优异的药理活性，例如抑制溃疡和抑制胃分泌，因此可用作抗消化性溃疡剂。

    Medicament for treating cerebral insufficiency diseases, novel 2-(1-piperazinyl)-4-phenylcycloalkanopyrimidine derivatives, and process for the production thereof
    8.
    发明授权
    Medicament for treating cerebral insufficiency diseases, novel 2-(1-piperazinyl)-4-phenylcycloalkanopyrimidine derivatives, and process for the production thereof 失效
    治疗脑功能不全疾病的药物，新型2-（1-哌嗪基）-4-苯基环烷基嘧啶衍生物及其制备方法

    公开(公告)号：US5185338A

    公开(公告)日：1993-02-09

    申请号：US711894

    申请日：1991-06-07

    申请人： Katsuhiko Hino ,  Naoki Kai ,  Masato Sakamoto ,  Tatsuya Kon ,  Makoto Oka ,  Kiyoshi Furukawa ,  Yoshiaki Ochi

    发明人： Katsuhiko Hino ,  Naoki Kai ,  Masato Sakamoto ,  Tatsuya Kon ,  Makoto Oka ,  Kiyoshi Furukawa ,  Yoshiaki Ochi

    IPC分类号： A61K31/505 ,  C07D239/70

    CPC分类号： C07D239/70 ,  A61K31/505

    摘要： Medicament for the treatment of cerebral insufficiency diseases comprising as an active ingredient a compound of the formula: ##STR1## wherein n is 3, 4, 5 or 6; R.sup.1 is hydrogen atom, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, hydroxy-C.sub.2 -C.sub.6) alkyl, unsubstituted or substituted aryl, heteroaryl, unsubstituted or substituted aryl-(C.sub.1 -C.sub.6) alkyl, unsubstituted or substituted aryl-carbonyl-(C.sub.1 -C.sub.6) alkyl, or acyl; R.sup.2 is hydrogen atom, halogen atom, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, or trifluoromethyl; and R.sup.3 is hydrogen atom or C.sub.1 -C.sub.6 alkyl, or an acid addition salt thereof, novel 2-(1-piperazinyl)-4-phenyl-cycloalkanopyrimidine derivatives having excellent cerebral function improving activity, processes for the preparation thereof.

    摘要翻译： 用于治疗脑功能不全疾病的药物，其包含下式的化合物作为活性成分：其中n为3,4,5或6;其中n为3,4,5或6; R 1是氢原子，C 1 -C 6烷基，C 3 -C 8环烷基，羟基-C 2 -C 6）烷基，未取代或取代的芳基，杂芳基，未取代或取代的芳基 - （C 1 -C 6）烷基，未取代或取代的芳基 - 羰基 - （ C 1 -C 6）烷基或酰基; R2是氢原子，卤素原子，C1-C6烷基，C1-C6烷氧基或三氟甲基; 和R3是氢原子或C1-C6烷基或其酸加成盐，具有优异的脑功能改善活性的新型2-（1-哌嗪基）-4-苯基 - 环烷基嘧啶衍生物，其制备方法。