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    Phenylpiperazine derivatives
    3.
    发明授权
    Phenylpiperazine derivatives 失效
    苯基哌嗪衍生物

    公开(公告)号：US4841051A

    公开(公告)日：1989-06-20

    申请号：US936270

    申请日：1986-12-01

    申请人： Akira Shiozawa ,  Yuh-Ichiro Ichikawa ,  Takashi Takahira

    发明人： Akira Shiozawa ,  Yuh-Ichiro Ichikawa ,  Takashi Takahira

    IPC分类号： A61K31/505 ,  A61K31/517 ,  A61P9/12 ,  A61P25/02 ,  C07D239/88 ,  C07D471/04

    CPC分类号： C07D471/04 ,  C07D239/88

    摘要： The present invention relates to a phenylpiperazine derivative represented by the general formula: ##STR1## wherein R.sub.1 stands for a lower alkyl group; R.sub.2 stands for a group represented by the general formula: ##STR2## (wherein R.sub.3, R.sub.4 and R.sub.5 each stand for a hydrogen atom or a lower alkyl group and Y stands for CH or N); and n stands for an integer of 1 to 6,and pharmaceutically acceptable acid addition salts thereof, which exhibit an .alpha..sub.1 -blocking activity and therefore are expected to be useful as a hypotensive drug.

    摘要翻译： 本发明涉及以下通式表示的苯基哌嗪衍生物：其中R1代表低级烷基; R2代表由以下通式表示的基团：其中R 3，R 4和R 5各自代表氢原子或低级烷基，Y代表CH或N）。 n表示1〜6的整数，以及其药学上可接受的酸加成盐，其具有α1-阻断活性，因此预期可用作降压药物。

    1,6-Naphthyridine derivatives, and antidinic and cerebral circulation improver containing such derivatives
    4.
    发明授权
    1,6-Naphthyridine derivatives, and antidinic and cerebral circulation improver containing such derivatives 失效
    1,6-萘啶衍生物，以及含有这些衍生物的抗坏血酸和脑循环改进剂

    公开(公告)号：US4308273A

    公开(公告)日：1981-12-29

    申请号：US83556

    申请日：1979-10-10

    申请人： Hiroshi Yamanaka ,  Takao Sakamoto ,  Akira Shiozawa ,  Yuh-Ichiro Ichikawa ,  Michio Ishikawa ,  Hiroshi Miyazaki

    发明人： Hiroshi Yamanaka ,  Takao Sakamoto ,  Akira Shiozawa ,  Yuh-Ichiro Ichikawa ,  Michio Ishikawa ,  Hiroshi Miyazaki

    IPC分类号： A61K31/435 ,  A61P27/16 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： This invention relates to the novel 1,6-naphthyridine derivatives useful as antidinic and/or cerebral circulation improver, such novel derivatives being represented by the following general formula: ##STR1## (wherein R is a C.sub.2-10 alkyl which may have hydroxyl, lower alkylcarbonyl, lower alkyloxycarbonyl or phenoxy as a substituent; a C.sub.2-10 unsaturated aliphatic hydrocarbon group having unsaturated double bond(s); a phenyl-lower alkyl which may have halogen, lower alkyl, lower alkoxy or lower alkylthio as substituent(s) attached to the phenyl ring; a cinnamyl which may have halogen, nitro, lower alkyl or lower alkoxy as substituent(s) attached to the phenyl ring; propargyl; 1-naphthylmethyl; 2-thenyl; cyclohexenyl; a cycloalkyl-lower alkyl with a 3- to 6-membered ring; 1/2(C.sub.2-4 alkylene); 1/2(butenylene), or diphenylmethyl, and in case two alkoxyl groups are present attached to the phenyl ring, they may be bonded to form a ring) and salt thereof.

    摘要翻译： 本发明涉及用作抗坏血酸和/或脑循环改进剂的新颖的1,6-二氮杂萘衍生物，这种新型衍生物由以下通式表示：其中R是可以 具有羟基，低级烷基羰基，低级烷氧基羰基或苯氧基作为取代基;具有不饱和双键的C 2-10不饱和脂族烃基;可具有卤素，低级烷基，低级烷氧基或低级烷硫基的苯基 - 低级烷基作为取代基 连接到苯环的苯甲酰基;可以具有卤素，硝基，低级烷基或低级烷氧基作为与苯环连接的取代基的肉桂基;炔丙基; 1-萘基甲基; 2-噻吩基;环己烯基;环烷基 - 低级 具有3-至6-元环的烷基; 1/2（C 2-4亚烷基）; 1/2（亚丁基）或二苯基甲基，并且在与苯环连接的情况下存在两个烷氧基的情况下，它们可以键合到 形成环）及其盐。

    Forskolin compounds
    5.
    发明授权
    Forskolin compounds 失效
    福斯康林化合物

    公开(公告)号：US4954642A

    公开(公告)日：1990-09-04

    申请号：US361763

    申请日：1989-05-30

    申请人： Tochiro Tatee ,  Takashi Takahira ,  Kouwa Yamashita ,  Masao Sakurai ,  Akira Shiozawa ,  Kazuhisa Narita

    发明人： Tochiro Tatee ,  Takashi Takahira ,  Kouwa Yamashita ,  Masao Sakurai ,  Akira Shiozawa ,  Kazuhisa Narita

    IPC分类号： A61K31/35 ,  C07D311/92 ,  C07D405/12

    CPC分类号： C07D311/92

    摘要： This invention relates to forskolin derivatives, their physiologically acceptable salts, and a process for producing these compounds. The forskolin derivative is represented by the general formula ##STR1## wherein; I. when R.sup.1 is hydrogen and R.sup.4 is vinyl, ethyl, or cyclopropyl,(1) either of R.sup.2 and R.sup.3 denotes a residue represented by the formula ##STR2## wherein each of R.sup.5 and R.sup.6 denotes hydrogen or lower alkyl or R.sup.5 and R.sup.6 combine with each other to form a lower alkylene chain which may or may not contain an oxygen or nitrogen atom and m is an integer of 1 to 5, and the other one of R.sup.2 and R.sup.3 denotes hydrogen or a residue represented by the formula CO(CH.sub.2).sub.n X, X being hydrogen or ##STR3## wherein, each of R.sup.7 and R.sup.8 denotes hydrogen or lower alkyl or R.sup.7 and R.sup.8 combine with each other to form a lower alkylene chain which may or may not contain an oxygen or nitrogen atom, and n being an integer of 1 to 5, or(2) R.sup.2 denotes hydrogen or --COCH.sub.2 CH.sub.2 CO.sub.2 H and R.sup.3 denotes hydrogen, --COCH.sub.3, --COCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H, or --COCH(OH)CH.sub.2 OH with the proviso that R.sup.3 is one of the last two residues when R.sup.2 is hydrogen, andII. whenR.sup.1 is a residue represented by a formula of CO(CH.sub.2).sub.p CO.sub.2 H and ##STR4## wherein, each of R.sup.9 and R.sup.10 denotes hydrogen or lower alkyl, p is an integer of 0 to 5, and q is an integer of 1 to 5,R.sup.2 denotes hydrogen , R.sup.3 denotes acetyl, and R.sup.4 denotes vinyl.

    摘要翻译： 本发明涉及毛喉素衍生物及其生理学上可接受的盐，以及这些化合物的制备方法。 毛喉素衍生物由通式表示，其中： 当R1是氢并且R4是乙烯基，乙基或环丙基时，（1）R2和R3中的任一个表示由下式表示的残基：其中R 5和R 6各自表示氢或低级烷基或R 5和R 6结合 彼此形成可以含有或不含有氧或氮原子并且m为1〜5的整数的低级亚烷基链，R2和R3中的另一个表示氢或由式CO（CH2）表示的残基 ）n X，X为氢或者其中，R 7和R 8各自表示氢或低级烷基，或者R 7和R 8彼此结合形成可含有或不含有氧或氮原子的低级亚烷基链，n 为1〜5的整数，或（2）R2表示氢或-COCH2 CH2CO2H，R3表示氢，-COCH3，-COCH2CH2CH2CO2H或-COCH（OH）CH2OH，条件是R3为最后两个残基之一， R2是氢，II。 当R 1是由CO（CH 2）p CO 2 H和的式表示的残基时，R 9和R 10各自表示氢或低级烷基，p是0至5的整数，q是1至5的整数 ，R2表示氢，R3表示乙酰基，R4表示乙烯基。

    Derivatives of .alpha.-methyl-.beta.-aminopropiophenone and use thereof
    6.
    发明授权
    Derivatives of .alpha.-methyl-.beta.-aminopropiophenone and use thereof 失效
    α-甲基-β-氨基苯丙酮的衍生物及其用途

    公开(公告)号：US4237141A

    公开(公告)日：1980-12-02

    申请号：US910024

    申请日：1978-05-26

    申请人： Akira Shiozawa ,  Shuji Kurashige ,  Hiroaki Hamano ,  Yasuhiko Furuta ,  Masako Ikeda ,  Hiroshi Miyazaki ,  Chiyoko Aoyagi ,  Yasuo Ishii

    发明人： Akira Shiozawa ,  Shuji Kurashige ,  Hiroaki Hamano ,  Yasuhiko Furuta ,  Masako Ikeda ,  Hiroshi Miyazaki ,  Chiyoko Aoyagi ,  Yasuo Ishii

    IPC分类号： C07D295/108 ,  C07D295/10 ,  A61K31/445

    CPC分类号： C07D295/108

    摘要： Novel .alpha.-methyl-.beta.-aminopropiophenone derivatives having bronchodilator activity represented by the following general formula: ##STR1## where R represents alkyl having 1-6 carbon atom benzyl or phenyl; R.sub.1 and R.sub.2 individually represent alkyl having 1-6 carbon atom or they form, joining to each other together with the adjacent nitrogen atom with or without intervening an atom other than carbon atom, a saturated heterocyclic ring which may be substituted with lower alkyl; n is an integer of 0, 1 or 2 on the proviso that R represents methyl or ethyl if n is 0, as well as their non-toxic salts are presented. Method of producing the new derivatives and the bronchodilatation method using them are disclosed as well.

    摘要翻译： 具有由以下通式表示的支气管扩张剂活性的新型α-甲基-β-氨基苯丙酮衍生物：其中R表示具有1-6个碳原子的烷基苄基或苯基; R1和R2分别代表具有1-6个碳原子的烷基或它们形成，可以与相邻的氮原子相互连接或不连接除碳原子以外的原子，可以被低级烷基取代的饱和杂环; n为0或1或2的整数，条件是R表示甲基或乙基，如果n为0，以及它们的无毒盐。 还公开了制备新衍生物的方法和使用它们的支气管扩张方法。

    Process for the preparation of 6,7-diacyl-7-deacteylforskolin derivatives
    7.
    发明授权
    Process for the preparation of 6,7-diacyl-7-deacteylforskolin derivatives 失效
    制备6,7-二酰基-7-去甲基福斯克林衍生物的方法

    公开(公告)号：US5484954A

    公开(公告)日：1996-01-16

    申请号：US179826

    申请日：1994-01-19

    申请人： Tochiro Tatee ,  Akira Shiozawa ,  Hirotaka Yamamoto ,  Yuh-ichiro Ichikawa ,  Aya Narita

    发明人： Tochiro Tatee ,  Akira Shiozawa ,  Hirotaka Yamamoto ,  Yuh-ichiro Ichikawa ,  Aya Narita

    IPC分类号： C07D311/92

    CPC分类号： C07D311/92

    摘要： This invention relates to a process for the preparation of a 6,7-diacyl-7-deacetylforskolin derivative represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 each stands for an acyl group and R.sup.3 stands for an aliphatic group having 2 to 3 carbon atoms, which comprises eliminating the acyl group at position 1 in a 1,6,7-triacyl-7-deacetylforskolin derivative represented by the general formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, by solvolysis. The compound of the formula (I) is expected as medicine.

    摘要翻译： 本发明涉及一种制备由以下通式表示的6,7-二酰基-7-脱乙酰福斯克林衍生物的方法：其中R1和R2各自代表酰基，R3代表脂族基团 具有2至3个碳原子，其包括在通式（III）表示的1,6,7-三酰基-7-脱乙酰福斯克林衍生物中除去第1位的酰基，其中R 1，R 2和R 3为 通过溶剂分解来定义。 预期式（I）化合物为药物。

    Certain chroman derivatives useful for treating symptoms caused by contraction of smooth muscles, circulatory diseases or epilepsy
    8.
    发明授权
    Certain chroman derivatives useful for treating symptoms caused by contraction of smooth muscles, circulatory diseases or epilepsy 失效
    某些苯并二氢吡喃衍生物可用于治疗由平滑肌，循环系统疾病或癫痫的收缩引起的症状

    公开(公告)号：US5296492A

    公开(公告)日：1994-03-22

    申请号：US893403

    申请日：1992-06-03

    申请人： Akira Shiozawa ,  Atsuro Inubushi ,  Kazuhisa Narita ,  Yukihiro Sagawa ,  Makoto Hosono ,  Masashi Iida

    发明人： Akira Shiozawa ,  Atsuro Inubushi ,  Kazuhisa Narita ,  Yukihiro Sagawa ,  Makoto Hosono ,  Masashi Iida

    IPC分类号： A61K31/35 ,  A61K31/353 ,  A61K31/44 ,  A61K31/4433 ,  A61P9/00 ,  A61P21/00 ,  C07D213/50 ,  C07D213/64 ,  C07D311/20 ,  C07D311/68 ,  C07D405/04 ,  C07F7/18 ,  C07D407/04 ,  C07F7/02 ,  A61K31/695

    CPC分类号： C07D405/04 ,  C07F7/1856

    摘要： A chroman derivative represented by the following general formula [1]: ##STR1## wherein R.sub.1 represents cyano group, nitro group, halogenomethyl group or --SO.sub.2 --X group (X represents lower alkyl group having 1-6 carbon atoms or aryl group); R.sub.2 represents hydrogen atom or OA group (A represents hydrogen atom, nitro group, lower acyl group having 1-6 carbon atoms, arylcarbonyl group, lower alkylsulfonyl group having 1-6 carbon atoms, arylsulfonyl group, arylalkyl group, tetrahydropyranyl group, lower alkoxycarbonyl group having 1-6 carbon atoms, arylalkoxycarbonyl group or silyl derivative group); R.sub.3 singly represents a hydrogen atom; or R.sub.3 forms a bond jointly with R.sub.2 ; and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 each represent hydrogen atom, vinyl group, formyl group, --Y--(OA).sub.n group (Y represents straight or branched chain alkylene group having 1-6 carbon atoms or lower alkenyl group having 1-6 carbon atoms, A is as defined above, and n represents an integer of 1-3.The compound of this invention is expected to be effectively usable as an agent for treatment of various symptoms due to the contraction of smooth muscles, for treatment of the diseases of the circulatory system and for treatment of epilepsy.

    摘要翻译： 由下列通式（1）表示的苯并二氢吡喃衍生物：（*化学结构*）（1）其中R1表示氰基，硝基，卤代甲基或-SO2-X基（X表示具有1-6个碳原子的低级烷基 原子或芳基）; R2表示氢原子或OA基（A表示氢原子，硝基，具有1-6个碳原子的低级酰基，芳基羰基，具有1-6个碳原子的低级烷基磺酰基，芳基磺酰基，芳基烷基，四氢吡喃基，低级烷氧基羰基 具有1-6个碳原子的基团，芳基烷氧基羰基或甲硅烷基衍生物基团）; R3单独表示氢原子; 或R3与R2一起形成键; 和R 4，R 5，R 6和R 7各自表示氢原子，乙烯基，甲酰基，-Y-（OA）n基（Y表示具有1-6个碳原子的直链或支链亚烷基或具有1-6个碳原子的低级链烯基 碳原子，A如上所定义，n表示1-3的整数。预期本发明化合物可有效地用作治疗由于平滑肌收缩引起的各种症状的药剂，用于治疗 循环系统疾病和治疗癫痫。