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    2-(1-piperazinyl)-4-phenylcycloalkanopyridine derivatives, processes for the production thereof, and pharmaceutical composition containing the same
    2.
    发明公开
    2-(1-piperazinyl)-4-phenylcycloalkanopyridine derivatives, processes for the production thereof, and pharmaceutical composition containing the same 失效
    2-（1-哌嗪基）-4- phenylcycloalkanpyridin衍生物，它们的制备方法和含有它们的药物组合物。

    公开(公告)号：EP0385237A2

    公开(公告)日：1990-09-05

    申请号：EP90103244.1

    申请日：1990-02-20

    申请人： DAINIPPON PHARMACEUTICAL CO., LTD.

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

    IPC分类号： C07D221/04 ,  C07D215/42 ,  A61K31/435 ,  C07D401/12 ,  C07D221/22

    CPC分类号： C07D215/38 ,  C07D221/04 ,  C07D221/22 ,  C07D401/04 ,  C07D401/12

    摘要： Novel 2-(1-piperazinyl)-4-phenyl-cycloalkano­pyridine derivatives of the formula (I):
    wherein n is 3, 4, 5, 6 or 7; R¹ is hydrogen atom, C₁-C₁₀ alkyl, C₂-C₆ alkenyl, C₂-C₆ alkynyl, C₃-C₈ cycloalkyl, C₃-C₆ cycloalkyl-(C₁-C₄) alkyl, hydroxy-(C₂-C₆) alkyl, C₁-C₃ alkoxy-(C₂-C₆) alkyl, acyloxy-(C₂-C₆) alkyl, unsubstituted or substituted aroyl-(C₁-C₆) alkyl, unsubstituted or substituted aryl, heteroaryl, or acyl; R² and R³ are the same or different and are each hydrogen atom, halogen atom, C₁-C₆ alkyl, C₁-C₆ alkoxy, trifluoromethyl, or hydroxy; R⁴, R⁵ and R⁶ are the same or different and are each hydrogen atom, C₁-C₆ alkyl, or phenyl, or two of R⁴, R⁵ and R⁶ combine to form a single bond or C₁-C₃ alkylene; R⁷ and R⁸ are the same or different and are each hydrogen atom or C₁-­C₃ alkyl; m is 2 or 3, or an acid addition salt thereof, which is useful as a psychotropic drug, and processes for the preparation thereof.

    摘要翻译： 新的2-（1-哌嗪基）（Ⅰ）式-4-苯基 - cycloalkanopyridine衍生物： worin n为3，4，5，6或7; [R <1>是氢原子，C1-C10烷基，C2-C6烯基，C2-C6炔基，C3-C8环烷基，C3-C6环烷基 - （C1-C4）烷基，羟基 - （C2-C6）烷基，C1 C3烷氧基 - （C2-C6）烷基，酰氧基 - （C2-C6）烷基，或取代的unsubstituiertem芳酰基（C1-C6）烷基，或unsubstituiertem取代的芳基，杂芳基，或酰基; [R <2>和R <3>是相同的或不同的，并且各自是氢原子，卤原子，C1-C6烷基，C1-C6烷氧基，三氟甲基，或羟基; [R <4> - [R <5>和R <6>是相同的或不同的，并且各自是氢原子，C1-C6烷基或苯基，或者两个R <4>的 - [R <5>和R <6> 结合以形成单键或C1-C3亚烷基; [R <7>和R <8>是相同的或不同的，并且各自是氢原子或C1-C3烷基; m是2或3，或它们的酸加成盐，所有这些是作为精神药物是有用的，并且流程其制备。

    4-(2'-Pyridylamino)-phenylacetic acid derivatives, process for their preparation, pharmaceuticals containing these compounds and their use
    5.
    发明公开
    4-(2'-Pyridylamino)-phenylacetic acid derivatives, process for their preparation, pharmaceuticals containing these compounds and their use 失效
    4-（2'-吡啶基氨基）苯基乙酸衍生物，它们的制备方法，含有这些化合物和它们的药物组合物。

    公开(公告)号：EP0011854A1

    公开(公告)日：1980-06-11

    申请号：EP79104726.9

    申请日：1979-11-27

    申请人： Dainippon Pharmaceutical Co., Ltd.

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

    IPC分类号： C07D213/74 ,  A61K31/44

    CPC分类号： C07D213/74

    摘要： The invention relates to novel 4-(2'-pyridylamino) -phenylacetic acid derivatives of the formula I

    Wherein R 1 is hydrogen, a halogen, a lower alkyl having 1 to 3 carbon atoms, or nitro, R 2 is hydrogen, a halogen, or a lower alkyl having 1 to 3 carbon atoms, R 3 is hydrogen, a halogen, or a lower alkyl having 1 to 3 carbon atoms, R 4 is hydrogen or a lower alkyl having 1 to 3 carbon atoms, R s is hydrogen or-CH 2 CH 2 OR 6 wherein R 6 is lower alkyl having 2 or 3 carbon atoms and being substituted with 1 or 2 hydroxy groups, provided that R 1 or R 2 is not 4-halogen,
    or pharmaceutically acceptable salts thereof, a process fortheir preparation (e.g.2-[4-(2'-pyridylamino)pehnyl] propionic acid (compound A) is prepared by reacting methyl 2-(4-amino -phenyl)propionate with 2-chloropyridine, followed by hydrolysis), pharmaceutcial composition containing these compounds, and their use 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.
    In the figure the prophylactic effect on adjuvant-induced arthritis in rats is shown (vehicle control (line 1), reference compound Ibuprofen (line 2), new compound A (line 3)].

    摘要翻译： 本发明涉及新的4-卤（2分钟-pyridylamino）下式的苯基乙酸衍生物：... ...... 其中R 1是氢，具有1至3个碳原子的低级烷基，或 硝基，R 2是氢，卤素，或具有1至3个碳原子的低级烷基，R3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个碳的低级烷基 原子，R 5是氢或-CH2CH2OR6 worin R 6为具有2或3个碳原子和具有1个或2个羟基取代的被做R1或R2不是4-卤，或它们的药学上可接受的盐的低级烷基，条件...，用于处理 其制备方法，pharmaceutcial组合物（例如2- [4-（2分钟-pyridylamino）pehnyl]（丙酸（化合物A）是通过使2- 4-氨基 - 苯基） - 丙酸酯与2-氯吡啶，然后水解制备） 含有合成的化合物以及它们作为抗炎剂和止痛剂的用途。 它们具有优异的抗炎镇痛作用与胃肠道ulcerogenicity极其微弱。 一些化合物具有抵抗由细胞免疫介导的慢性炎症优异的抑制活性。 ... 在被示出对大鼠佐剂诱导的关节炎的预防作用图（溶媒对照（第1行），参考化合物布洛芬（线2），新的化合物A（第3行）。

    Medicament for treating cerebral insufficiency diseases containing 2-(1-piperazinyl)-4-phenylcycloalkanopyrimidine derivatives, and process for the production thereof
    7.
    发明公开
    Medicament for treating cerebral insufficiency diseases containing 2-(1-piperazinyl)-4-phenylcycloalkanopyrimidine derivatives, and process for the production thereof 失效
    为2-（1-哌嗪基）的基础上治疗脑供血不足的疾病的补救措施-4- Phenylcycloalkanpyrimidinderivaten和它们的制备方法。

    公开(公告)号：EP0384228A1

    公开(公告)日：1990-08-29

    申请号：EP90102478.6

    申请日：1990-02-08

    申请人： DAINIPPON PHARMACEUTICAL CO., LTD.

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

    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:
    wherein n is 3, 4, 5 or 6; R¹ is hydrogen atom, C₁-C₆ alkyl, C₃-C₈ cycloalkyl, hydroxy-(C₂-C₆) alkyl, unsubstituted or substituted aryl, heteroaryl, unsubstituted or substituted aryl-(C₁-C₆) alkyl, unsubstituted or substituted aryl­carbonyl-(C₁-C₆) alkyl, or acyl; R² is hydrogen atom, halogen atom, C₁-C₆ alkyl, C₁-C₆ alkoxy, or trifluoromethyl; and R³ is hydrogen atom or C₁-C₆ 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： 药物对脑供血不足的疾病，其包括作为活性成分的治疗下式的化合物： worin n为3，4，5或6; [R <1>是氢原子，C1-C6烷基，C3-C8环烷基，羟基 - （C2-C6）烷基，或unsubstituiertem取代的芳基，杂芳基或取代的unsubstituiertem芳基 - （C1-C6）烷基，或unsubstituiertem芳基羰基substituiertem - （C1-C6）烷基，或酰基; [R <2>是氢原子，原子，C1-C6烷基卤，C1-C6烷氧基，或三氟甲基; 且R <3>为氢原子或C1-C6烷基，或以它们的酸加成盐，新的2-（1-哌嗪基），具有优良的脑功能改善作用-4-苯基cycloalkanopyrimidine衍生物，它们的制备方法。