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    Thienodiazepine derivatives
    1.
    发明授权
    Thienodiazepine derivatives 失效
    噻吩并二氮杂衍生物

    公开(公告)号：US4017620A

    公开(公告)日：1977-04-12

    申请号：US575727

    申请日：1975-05-08

    申请人： Yutaka Kuwada ,  Kanji Meguro ,  Hiroyuki Tawada ,  Takashi Sohda ,  Hideaki Natsugari ,  Yoshiaki Sato

    发明人： Yutaka Kuwada ,  Kanji Meguro ,  Hiroyuki Tawada ,  Takashi Sohda ,  Hideaki Natsugari ,  Yoshiaki Sato

    IPC分类号： A61K31/55 ,  A61P25/00 ,  A61P25/20 ,  C07D495/14

    CPC分类号： C07D495/14

    摘要： There is disclosed new thienodiazepine derivatives of the general formula: ##STR1## wherein R.sup.1 represents a carboxyl group which may be esterified or amidated; each of R.sup.2 and R.sup.3 represents hydrogen atom or a lower alkyl group, or R.sup.2 and R.sup.3 may bond to each other to form an alkylene group; R.sup.4 represents a phenyl group which may have substituent; and R represents hydrogen atom, an acyl group or an alkyl group, or its pharmaceutically acceptable acid addition salts. The above compounds are useful as medicine in human and animal therapy, which act on the central nervous system, for example, as muscle relaxants, anticonvulsants, sedatives, minor tranquilizers, etc.

    摘要翻译： 公开了以下通式的新的噻吩并二氮杂衍生物：其中R 1表示可被酯化或酰胺化的羧基; R 2和R 3各自表示氢原子或低级烷基，或者R 2和R 3可以彼此键合形成亚烷基; R4表示可以具有取代基的苯基; R表示氢原子，酰基或烷基，或其药学上可接受的酸加成盐。 上述化合物可用作人和动物治疗中的药物，其作用于中枢神经系统，例如肌肉松弛剂，抗惊厥药，镇静剂，微量镇静剂等。

    Benzodiazepine carboxamides and pharmaceutical compositions with central nervous system activity
    3.
    发明授权
    Benzodiazepine carboxamides and pharmaceutical compositions with central nervous system activity 失效
    苯二氮卓类甲酰胺和具有中枢神经系统活性的药物组合物

    公开(公告)号：US4049812A

    公开(公告)日：1977-09-20

    申请号：US572943

    申请日：1975-04-30

    申请人： Yutaka Kuwada ,  Hideaki Natsugari ,  Kanji Meguro

    发明人： Yutaka Kuwada ,  Hideaki Natsugari ,  Kanji Meguro

    IPC分类号： A61K31/55 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  C07D213/50 ,  C07D249/08 ,  C07D487/14 ,  C07D498/14 ,  C07D513/14 ,  A61K31/44 ,  C07D223/16

    CPC分类号： C07D487/14 ,  C07D213/50

    摘要： There is disclosed a novel heterocyclic compound of the general formula: ##STR1## wherein each of R.sup.1 and R.sup.2 represents hydrogen atom, or an alkyl group which may be substituted by alkyl-substituted amino, hydroxy or alkoxy group, or R.sup.1 and R.sup.2 may form a heterocyclic ring together with the nitrogen atom adjacent thereto; R.sup.3 represents hydrogen atom or a lower alkyl group; P.sub.y represents a pyridyl group; B represents a lower alkylene group which may have lower alkyl group as a substituent; Y represents oxygen atom, sulfur atom or --NH-- group; and ring A is either unsubstituted or substituted by halogen atom, nitro, lower alkyl, lower alkoxy or polyhalo-lower alkyl group. This class of compounds is found to be useful as medicine in human and animal therapy, which act on the central nervous system, for example, muscle relaxants, anticonvulsants, sedatives, minor tranquilizers. There is also disclosed intermediates for the production of said compound.

    摘要翻译： 公开了以下通式的新型杂环化合物：其中R 1和R 2各自表示氢原子，或可被烷基取代的氨基，羟基或烷氧基取代的烷基，或R 1和R 2可形成 杂环与与其相邻的氮原子一起; R3表示氢原子或低级烷基; Py代表吡啶基; B表示可以具有低级烷基作为取代基的低级亚烷基; Y表示氧原子，硫原子或-NH-基团; 并且环A是未取代的或被卤素原子，硝基，低级烷基，低级烷氧基或多卤代低级烷基取代。 发现这类化合物可用作人和动物治疗中的药物，其作用于中枢神经系统，例如肌肉松弛剂，抗惊厥药，镇静剂，微量镇静剂。 还公开了用于生产所述化合物的中间体。

    Benzodiazepine derivatives
    4.
    发明授权
    Benzodiazepine derivatives 失效
    苯并二氮杂衍生物

    公开(公告)号：US4175079A

    公开(公告)日：1979-11-20

    申请号：US295575

    申请日：1972-10-06

    申请人： Yutaka Kuwada ,  Hideaki Natsugari ,  Kanji Meguro

    发明人： Yutaka Kuwada ,  Hideaki Natsugari ,  Kanji Meguro

    IPC分类号： A61K31/55 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  C07D487/04 ,  C07D499/62

    CPC分类号： C07D487/04 ,  Y10S514/906 ,  Y10S514/96

    摘要： The present invention relates to pyrimidobenzodiazepine derivatives of the formula (I) and 2-(N-acetoacetal)aminobenzodiazepine derivatives of the formula (II), which compounds have the following formulas: ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkyl group, R.sup.2 represents a hydrogen atom, a lower alkyl group or an aryl group, and rings A and/or B are unsubstituted or substituted by one or more of a halogen, nitro, trifluoromethyl, lower alkyl or lower alkoxy group; including the cases wherein the nitrogen atom at the 6-position of the compound (I) or the 4-position of the compound (II) may be in the form of N-oxide and wherein compound (I) may be in the form of a pharmaceutically acceptable acid addition salt thereof. The present invention also relates to a method of producing these compounds. The compounds (I) and (II) are useful as muscle relaxants, anticonvulsants, sedatives, tranquilizers, etc.

    摘要翻译： 本发明涉及式（I）的嘧啶并二氮杂衍生物和式（II）的2-（N-乙酰乙缩醛）氨基苯并二氮杂衍生物，该化合物具有下式：其中R 1表示氢 原子或低级烷基，R2表示氢原子，低级烷基或芳基，并且环A和/或B是未取代的或被一个或多个卤素，硝基，三氟甲基，低级烷基或低级烷氧基取代 组; 包括其中化合物（I）的6位的氮原子或化合物（II）的4-位可以是N-氧化物的形式，其中化合物（I）可以是 其药学上可接受的酸加成盐。 本发明还涉及生产这些化合物的方法。 化合物（I）和（II）可用作肌肉松弛剂，抗惊厥药，镇静剂，镇定剂等。

    4-Pyridine carbonyl phenyl 1,2,4 triazoles
    6.
    发明授权
    4-Pyridine carbonyl phenyl 1,2,4 triazoles 失效
    4-吡啶羰基苯基1,2,4-三唑

    公开(公告)号：US4044129A

    公开(公告)日：1977-08-23

    申请号：US592889

    申请日：1975-07-03

    申请人： Yutaka Kuwada ,  Kanji Meguro ,  Hideaki Natsugari ,  Yoshiaki Sato ,  Hiroyuki Tawada

    发明人： Yutaka Kuwada ,  Kanji Meguro ,  Hideaki Natsugari ,  Yoshiaki Sato ,  Hiroyuki Tawada

    IPC分类号： C07D401/04 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/535 ,  A61P21/02 ,  A61P25/00 ,  A61P25/08 ,  A61P25/20 ,  C07D213/50 ,  C07D249/08 ,  C07D401/10 ,  C07D413/14

    CPC分类号： C07D249/08 ,  C07D213/50

    摘要： A novel triazole derivative of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, represent alkyl group or aralkyl group and one of R.sup.1 and R.sup.2 may be hydrogen atom, or R.sup.1 and R.sup.2 form a heterocyclic ring together with the nitrogen atom adjacent thereto; R.sup.3 represents hydrogen atom or a hydrocarbon residue; R.sup.4 represents hydrogen atom or a lower alkyl group; Py represents a pyridyl group; and the ring A is either unsubstituted or substituted by halogen atom, nitro, alkyl, alkoxy or trifluoromethyl group, and pharmaceutically acceptable acid addition salts thereof are found to be useful as medicine in human and animal therapy, as these compounds act on the central nervous as for example, muscle relaxants, anticonvulsants, sedatives, minor tranquilizers, etc.

    摘要翻译： 通式（I）的新的三唑衍生物：（I）其中R 1和R 2可以相同或不同，表示烷基或芳烷基，R 1和R 2之一可以是氢原子或R 1 R2与邻近的氮原子一起形成杂环; R3表示氢原子或烃残基; R4代表氢原子或低级烷基; Py代表吡啶基; 发现环A是未取代的或被卤素原子取代的硝基，烷基，烷氧基或三氟甲基，其药学上可接受的酸加成盐可用作人和动物治疗中的药物，因为这些化合物作用于中枢神经 例如，肌肉松弛剂，抗惊厥药，镇静剂，小镇静剂等

    Pyrimido[1,2-a][1,5]
    7.
    发明授权
    Pyrimido[1,2-a][1,5] 失效
    嘧啶{8 1,2-a {9 {8,5 {9

    公开(公告)号：US3978058A

    公开(公告)日：1976-08-31

    申请号：US315313

    申请日：1972-12-15

    申请人： Yutaka Kuwada ,  Hideaki Natsugari ,  Kanji Meguro

    发明人： Yutaka Kuwada ,  Hideaki Natsugari ,  Kanji Meguro

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04

    摘要： Novel compounds of the formula, ##SPC1##Wherein ##EQU1## stands for the partial structure ##SPC2## WHEREIN R.sup.1 stands for hydrogen atom, an alkyl group or phenyl group, R.sup.2 and R.sup.3 stand for, the same or different, hydrogen atom or a lower alkyl group and rings A and B are unsubstituted or substituted by one or more, he same or different, of halogen atom, nitro, trifluoromethyl, a lower alkyl group or a lower alkoxy group, have sedative, anti-inflammatory, anti-convulsive, sleep-potentiating and diuretic activites.

    摘要翻译： 新型式的化合物，WHEREIN Z代表部分结构，其中R1代表氢原子，烷基或苯基，R2和R3代表相同或不同的氢原子或低级烷基，环A和B 未取代或被一个或多个相同或不同的卤原子硝基，三氟甲基，低级烷基或低级烷氧基取代，具有镇静，抗炎，抗惊厥，睡眠增强和利尿作用。

    Thienopyridine substituted cephalosporins
    8.
    发明授权
    Thienopyridine substituted cephalosporins 失效
    噻吗啉替代CEPHALOSPORINS

    公开(公告)号：US4145418A

    公开(公告)日：1979-03-20

    申请号：US755428

    申请日：1976-12-29

    申请人： Yutaka Kuwada ,  Kanji Meguro

    发明人： Yutaka Kuwada ,  Kanji Meguro

    IPC分类号： C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D501/20 ,  C07D501/36 ,  A61K31/545

    CPC分类号： C07D499/00

    摘要： Thienopyridine derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each is hydrogen, an alkyl, an aryl, an aralkyl or a halogen; R.sup.1 and R.sup.2 may, taken together, represent an alkylene group; X is hydrogen or an alkyl; Y is oxygen or sulfur; Z is phenyl which may optionally be substituted; R.sup.3 is hydrogen or an alkoxy; and R is a group of the formula: ##STR2## or of the formula: ##STR3## (wherein R.sup.4 is hydrogen, an acyloxy or a nucleophilic compound residue) or a pharmaceutically acceptable salt thereof are found to have activity against a broad spectrum of gram-positive and gram-negative bacteria, particularly against bacteria of the genus Pseudomonas .

    Benzodiazepine derivatives
    9.
    发明授权
    Benzodiazepine derivatives 失效
    苯并咪唑衍生物

    公开(公告)号：US4116956A

    公开(公告)日：1978-09-26

    申请号：US718194

    申请日：1976-08-26

    申请人： Kanji Meguro ,  Yutaka Kuwada

    发明人： Kanji Meguro ,  Yutaka Kuwada

    IPC分类号： C07D243/20

    CPC分类号： C07D243/20 ,  Y10S514/906

    摘要： Benzodiazepine derivatives of the general formula ##STR1## where R.sub.1 is hydrogen or a hydrocarbon residue of 1-8 carbon atoms, R.sub.2 is hydrogen or lower alkyl and rings A and B are unsubstituted or substituted by nitro, trifluoromethyl, halogen, lower alkyl or lower alkoxy, the nitrogen atom in the 5-position being unsubstituted or substituted by an oxygen atom, useful as muscle relaxants, anticonvulsants, sedatives and tranquilizing agents, and processes for production thereof. Also provided are novel intermediates of the general formula ##STR2## where R.sub.2 has the above meaning, rings A and B are unsubstituted or substituted as above and the nitrogen atom in the 4-position is unsubstituted or substituted by an oxygen atom.