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    Benzothiazepine derivatives and their methods of preparation
    1.
    发明授权
    Benzothiazepine derivatives and their methods of preparation 失效
    苯并硫氮杂衍生物及其制备方法

    公开(公告)号：US4539150A

    公开(公告)日：1985-09-03

    申请号：US625656

    申请日：1984-06-28

    申请人： Tsutomu Katakami ,  Nobuyuki Fukazawa ,  Hajime Iizuka ,  Takashi Nishina ,  Isao Shirakawa

    发明人： Tsutomu Katakami ,  Nobuyuki Fukazawa ,  Hajime Iizuka ,  Takashi Nishina ,  Isao Shirakawa

    IPC分类号： C07D281/10 ,  C07D281/02

    CPC分类号： C07D281/10

    摘要： This invention relates to benzothiazepine derivatives of the general formula ##STR1## where K is hydrogen or a --CH.sub.2 COOR.sub.2 group where R.sub.2 is hydrogen or a lower alkyl group, Z is hydrogen or phenyl except when both K and Z are hydrogen, and Y is hydrogen, a --CHR.sub.3 --COOR.sub.1 group, an alkanoyl group or a --COO(CH.sub.2).sub.n R.sub.4 group where R.sub.1 is hydrogen or a lower alkyl group, R.sub.3 is hydrogen, an alkyl group, an alkylphenyl group or an aryl-lower alkyl group, R.sub.4 is an aryl group and n is a whole number of 1 to 10, and to their methods of preparation.The benzothiazepine derivatives of this invention, including their salts, have a powerful inhibitory effect on the angiotensin converting enzyme and exert a marked depressor effect in such models of hypertension as spontaneously occurring hypertensive rats and the like, so that they are useful as drugs for the treatment of hypertension and other cardiovascular diseases. In addition, these compounds are also useful as intermediates for the synthesis of coronary dilators, psychotropic drugs and the like.

    摘要翻译： 本发明涉及通式为（I）的苯并硫氮杂衍生物，其中K是氢或-CH 2 COOR 2基团，其中R 2是氢或低级烷基，Z是氢或苯基，除了当K和Z都是氢时， Y是氢，-CHR 3 -COOR 1基团，烷酰基或-COO（CH 2）n R 4基团，其中R 1是氢或低级烷基，R 3是氢，烷基，烷基苯基或芳基 - 低级烷基 基团，R 4为芳基，n为1〜10的整数，及其制备方法。 包括其盐在内的本发明的苯并硫氮杂衍生物对血管紧张素转化酶具有强大的抑制作用，并且在自发发生的高血压大鼠等高血压模型中发挥明显的抑制作用，因此它们可用作药物 治疗高血压等心血管疾病。 此外，这些化合物也可用作合成冠状动脉扩张剂，精神药物等的中间体。

    Pyridazinone derivatives
    4.
    发明授权
    Pyridazinone derivatives 失效
    哒嗪酮衍生物

    公开(公告)号：US4639451A

    公开(公告)日：1987-01-27

    申请号：US504039

    申请日：1983-06-03

    申请人： Tsutomu Katakami ,  Nobuyuki Fukazawa ,  Hajime Iizuka ,  Takashi Nishina ,  Joji Kamiya ,  Yasuhito Tanaka ,  Takuo Nakano

    发明人： Tsutomu Katakami ,  Nobuyuki Fukazawa ,  Hajime Iizuka ,  Takashi Nishina ,  Joji Kamiya ,  Yasuhito Tanaka ,  Takuo Nakano

    IPC分类号： C07D237/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  A61K31/50

    CPC分类号： C07D401/12 ,  C07D237/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

    摘要： This invention relates to pyridazinone derivatives of the general formula: ##STR1## [wherein R.sup.1 stands for a hydrogen atom or a lower alkyl group; R.sup.2 for a hydrogen atom or a lower alkyl group; and A for (i) a ring selected from a benzene ring, a furan ring, a thiophene ring and a pyridine ring (on which ring 1-3 substituents or atoms selected from amino groups, nitro groups, lower alkanoylamino groups, hydroxyl groups, lower alkanoyloxy groups, sulfamoyl groups and halogen atoms may be present), or (ii) a grouping of the formula: ##STR2## (wherein R.sup.3 stands for a hydrogen atom, a lower alkyl group, a phenyl(lower)alkyl, a hydroxyphenyl(lower)alkyl group, a lower alkylmercapto(lower)alkyl group, a benzylmercapto(lower)alkyl group, a guanidino(lower)alkyl group, a nitroguanidino(lower)alkyl group, an indolyl(lower)alkyl group, a carbamoyl(lower)alkyl group or a carboxy(lower)alkyl group, R.sup.4 for a hydrogen atom or a lower alkyl group, R.sup.5 for a hydrogen atom, a lower alkyl group, a lower alkanoyl group, a benzoyl or a benzyloxycarbonyl group, and R.sup.3 and R.sup.4 may be combined to form a grouping of the formula: ##STR3## which forms a ring), or (iii) a grouping of the formula: ##STR4## (wherein R.sup.6, R.sup.7 and R.sup.8 each stand for a hydrogen atom or a lower alkyl group, B is an oxygen atom or a sulfur atom, R.sup.9 stands for a hydrogen atom or a lower alkanoyl group, and n is 0 or 1)].

    摘要翻译： PCT No.PCT / JP82 / 00415 Sec。 371日期：1983年6月3日 102（e）日期1983年6月3日PCT提交1982年10月20日PCT公布。 第WO83 / 01447号公报 日本1983年4月28日。本发明涉及以下通式的哒嗪酮衍生物：其中R1代表氢原子或低级烷基; R2为氢原子或低级烷基; A为（i）选自苯环，呋喃环，噻吩环和吡啶环的环（其中1-3个取代基或选自氨基，硝基，低级烷酰基氨基，羟基， 低级烷酰氧基，氨磺酰基和卤素原子可以存在），或（ii）下式的基团：其中R3代表氢原子，低级烷基，苯基（低级）烷基，羟基苯基 （低级）烷基，低级烷基巯基（低级）烷基，苄基巯基（低级）烷基，胍基（低级）烷基，硝基胍基（低级）烷基，吲哚基（低级）烷基，氨基甲酰基 低级）烷基或羧基（低级）烷基，R4表示氢原子或低级烷基，R5表示氢原子，低级烷基，低级链烷酰基，苯甲酰基或苄氧基羰基，R3和 R4可以组合以形成下式的分组：形成环的），或（iii）下式的分组：（ 其中R6，R7和R8各自代表氢原子或低级烷基，B是氧原子或硫原子，R9代表氢原子或低级烷酰基，n是0或1）]。

    6-(Substituted phenyl)-4,5-dihydro-3(2H)-pyridazinone compounds
    5.
    发明授权
    6-(Substituted phenyl)-4,5-dihydro-3(2H)-pyridazinone compounds 失效
    （取代的苯基）-4,5-二氢-3（2H） - 哒嗪酮化合物

    公开(公告)号：US4521415A

    公开(公告)日：1985-06-04

    申请号：US454021

    申请日：1982-12-28

    申请人： Tsutomu Katakami ,  Nobuyuki Fukazawa ,  Hajime Iizuka ,  Takashi Nishina ,  Joji Kamiya ,  Yasuhito Tanaka ,  Takuo Nakano

    发明人： Tsutomu Katakami ,  Nobuyuki Fukazawa ,  Hajime Iizuka ,  Takashi Nishina ,  Joji Kamiya ,  Yasuhito Tanaka ,  Takuo Nakano

    IPC分类号： A61K31/50 ,  A61P7/02 ,  A61P9/12 ,  C07D237/04 ,  C07D401/12 ,  C07D403/12

    CPC分类号： C07D401/12 ,  C07D237/04 ,  C07D403/12

    摘要： 6-(Substituted phenyl)-4,5-dihydro-3(2H)-pyridazinone compounds possessing strong platelet aggregation inhibiting activity and blood pressure depressing activity, having the general formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2 is hydrogen, lower alkyl, lower alkylthio or the grouping R.sup.5 --NH-- where R.sup.5 is lower alkyl; R.sup.3 is phenyl, pyridyl, benzyl, lower alkyl or a substituted phenyl group carrying at any desired position on the benzene ring thereof the grouping: ##STR2## where R.sup.1 has the same meaning as given above; R.sup.4 is hydrogen or halogen; n is 0 or 1; and when both R.sup.2 and R.sup.3 are lower alkyl groups, R.sup.2 and R.sup.3 may be combined together with the bridging member ##STR3## where m is 2 or 3, as well as physiologically acceptable acid-addition salts thereof, and processes for preparing them.

    摘要翻译： 具有强烈的血小板聚集抑制活性和降低血压的6-（取代的苯基）-4,5-二氢-3（2H） - 哒嗪酮化合物，具有以下通式：其中R 1为氢或低级烷基 ; R2是氢，低级烷基，低级烷硫基或分组R5-NH-，其中R5是低级烷基; R3是苯基，吡啶基，苄基，低级烷基或在其苯环上的任何所需位置携带的取代苯基，其分子式如下：其中R 1具有与上述相同的含义; R4是氢或卤素; n为0或1; 当R 2和R 3均为低级烷基时，R 2和R 3可以与m为2或3的桥连基团以及其生理上可接受的酸加成盐组合在一起，以及制备方法 他们。

    Benzothiazepine derivatives and their method of preparation
    6.
    发明授权
    Benzothiazepine derivatives and their method of preparation 失效
    苯并硫氮杂衍生物及其制备方法

    公开(公告)号：US4539151A

    公开(公告)日：1985-09-03

    申请号：US625815

    申请日：1984-06-28

    申请人： Tsutomu Katakami ,  Nobuyuki Fukazawa ,  Hajime Iizuka

    发明人： Tsutomu Katakami ,  Nobuyuki Fukazawa ,  Hajime Iizuka

    IPC分类号： C07D281/10 ,  C07D281/02

    CPC分类号： C07D281/10 ,  Y02P20/55

    摘要： This invention relates to benzothiazepine derivatives of the general formula ##STR1## where Y is hydrogen, a CHR.sub.3 --COOR.sub.1 group, an alkanoyl group or a --COO(CH.sub.2).sub.n R.sub.4 group where R.sub.1 is hydrogen or a lower alkyl group, R.sub.3 is hydrogen, an alkyl group, an alkylphenyl group or an aryl-lower alkyl group, R.sub.4 is an aryl group and n is a whole number of 1 to 10, and to their method of preparation.The benzothiazepine derivatives of this invention, including their salts, have an inhibitory effect on the angiotensin converting enzyme and are useful as raw materials or intermediates for the synthesis of antihypertensive agents and as intermediates for the manufacture of other drugs, agricultural chemicals and industrial chemicals.

    摘要翻译： 本发明涉及通式为（I）的苯并硫氮杂衍生物，其中Y为氢，CHR 3 -COOR 1基，烷酰基或-COO（CH 2）n R 4基，其中R 1为氢或低级烷基，R 3 是氢，烷基，烷基苯基或芳基 - 低级烷基，R4是芳基，n是整数1〜10，以及它们的制备方法。 本发明的苯并硫氮杂衍生物，包括其盐，对血管紧张素转化酶具有抑制作用，可用作合成抗高血压药物的原料或中间体，也可用作制造其它药物，农药和工业化学品的中间体。

    Pyrimidinedione derivatives and antiarrythmic agents containing the same
    7.
    发明授权
    Pyrimidinedione derivatives and antiarrythmic agents containing the same 失效
    嘧啶二酮衍生物和含有它们的抗焦虑剂

    公开(公告)号：US5308848A

    公开(公告)日：1994-05-03

    申请号：US927738

    申请日：1992-08-12

    申请人： Michihiko Miyamoto ,  Tsutomu Katakami ,  Nobuya Kawauchi ,  Tadahito Nobori ,  Joji Kamiya ,  Masaaki Ishii

    发明人： Michihiko Miyamoto ,  Tsutomu Katakami ,  Nobuya Kawauchi ,  Tadahito Nobori ,  Joji Kamiya ,  Masaaki Ishii

    IPC分类号： C07D239/54 ,  C07D239/545 ,  C07D401/12 ,  A61K31/505 ,  C07D239/10

    CPC分类号： C07D239/545 ,  C07D401/12

    摘要： A pyrimidinedione derivative compound has a basic backbone in which a phenyl group part and a pyrimidinedione part are linked by a linking structure comprising an alkyl chain containing two nitrogen atoms. This linking structure is represented by ##STR1## [wherein A is --(CH.sub.2).sub.n --, --CO-- or --O--(CH.sub.2).sub.m --; each of R.sup.1 and R.sup.2 is independently a hydrogen atom or a lower alkyl group which may be substituted by a hydroxyl group, or R.sup.1 and R.sup.2 may be so linked with each other as to make an alkylene chain and thus form a heterocyclic structure; R.sup.5 is a halogen atom, a hydroxyl group, a lower alkyloxycarbonyl group, a lower alkyloxy group which may be substituted by a lower alkyloxy group, or a lower alkyl group which may be substituted by a hydroxyl group, or R.sup.5 may be so linked with R.sup.1 as to make an alkylene chain and thus form a heterocyclic structure; n is 0, 1, 2 or 3 (when R.sup.5 is the hydroxyl group, n.noteq.0); m is 0, 1, 2 or 3; and k is 0, 1, 2 or 3 (however, a compound in which A is --O--(CH.sub.2).sub.m -- and R.sup.5 is the hydroxyl group is excluded from the pyrimidinedione derivative)]. The pyrimidinedione derivative and its acid addition salt are useful for a medical treatment of cardiac arrhythmias.

    摘要翻译： 嘧啶二酮衍生物化合物具有其中苯基部分和嘧啶二酮部分通过包含含有两个氮原子的烷基链的连接结构连接的碱性主链。 该连接结构由表示，其中A是 - （CH 2）n - ， - CO-或-O-（CH 2）m - ; R 1和R 2各自独立地为氢原子或可以被羟基取代的低级烷基，或者R 1和R 2可以相互连接形成亚烷基链，从而形成杂环结构; R5是卤素原子，羟基，低级烷氧基羰基，可被低级烷氧基取代的低级烷氧基或可被羟基取代的低级烷基，或R5可以与 R1形成亚烷基链，从而形成杂环结构; n是0,1,2或3（当R5是羟基时，n是等于0）; m为0,1,2或3; 并且k为0,1,2或3（然而，其中A为-O-（CH 2）m - 且R 5为羟基的化合物不包括在嘧啶二酮衍生物中]]。 嘧啶二酮衍生物及其酸加成盐可用于治疗心律失常。