利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

111 条记录 (耗时 0.019 秒)

    Process for preparing 1-polyhaloalkyl-3,4-dihydro-2-(1H)-quinazolinones
    1.
    发明授权
    Process for preparing 1-polyhaloalkyl-3,4-dihydro-2-(1H)-quinazolinones 失效
    1-多卤代烷基-3,4-二氢-2-（1H） - 喹唑啉酮的制备方法

    公开(公告)号：US4048168A

    公开(公告)日：1977-09-13

    申请号：US754640

    申请日：1976-12-27

    申请人： Michihiro Yamamoto ,  Shigenari Katayama ,  Masao Koshiba ,  Hisao Yamamoto

    发明人： Michihiro Yamamoto ,  Shigenari Katayama ,  Masao Koshiba ,  Hisao Yamamoto

    IPC分类号： A61K31/505 ,  A61K31/517 ,  A61P25/04 ,  A61P29/00 ,  C07D239/78 ,  C07D239/82 ,  C07D409/04 ,  C07D491/056

    CPC分类号： C07D239/78 ,  C07D239/82

    摘要： 3,4-Dihydro-2(1H)-quinazolinone derivatives of the formula, ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, lower alkyl, lower alkylthio or lower alkoxy, or, when taken together, R.sub.1 and R.sub.2 may form methylenedioxy; R.sub.3 is polyhalo-lower alkyl; R.sub.4 is phenyl, halophenyl, lower alkoxyphenyl, lower alkylphenyl or thienyl; and X is oxygen or sulfur, which are known to be very useful intermediates for the preparation of anti-inflammatory and analgesic agents, are obtained in a high yield by reacting a compound of the formula, ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and X are as defined above, with a compound of the formula,R.sub.4 --CHOwherein R.sub.4 is as defined above, with heating in the presence of a zinc halide as a catalyst.

    摘要翻译： 3,4-二氢-2（1H） - 喹唑啉酮衍生物，其中R 1和R 2各自为氢，低级烷基，低级烷硫基或低级烷氧基，或者当R 1和R 2一起形成亚甲二氧基时; R3是多卤代低级烷基; R4是苯基，卤代苯基，低级烷氧基苯基，低级烷基苯基或噻吩基; 通过使下式化合物，其中R 1，R 2，R 3和R 3与式（I）化合物反应，可以高收率获得已知是用于制备抗炎和止痛剂的非常有用的中间体的X是氧或硫。 X如上所定义，与卤化锌作为催化剂的存在下，加热下式的化合物，其中R 4如上定义。

    Fused quinazolinones and a process for production thereof
    5.
    发明授权
    Fused quinazolinones and a process for production thereof 失效
    熔融喹唑啉酮及其制备方法

    公开(公告)号：US3980645A

    公开(公告)日：1976-09-14

    申请号：US521768

    申请日：1974-11-07

    申请人： Shigeho Inaba ,  Michihiro Yamamoto ,  Kikuo Ishizumi ,  Kazuo Mori ,  Masao Koshiba ,  Hisao Yamamoto

    发明人： Shigeho Inaba ,  Michihiro Yamamoto ,  Kikuo Ishizumi ,  Kazuo Mori ,  Masao Koshiba ,  Hisao Yamamoto

    IPC分类号： C07D487/04 ,  C07D498/04 ,  C07D265/00 ,  C07D273/00 ,  C07D295/00

    CPC分类号： C07D487/04

    摘要： Fused quinazolinone derivatives of the formula, ##SPC1##Wherein R.sub.1 and R.sub.2 are individually hydrogen, C.sub.1.sub.-4 alkyl, C.sub.1.sub.-4 alkoxy, nitro, C.sub.1.sub.-4 alkylsulfonyl or halogen; R.sub.3 is pyridyl, thienyl or a group of the formula ##SPC2##Wherein R.sub. 4 is hydrogen or halogen; R is hydrogen, C.sub.1.sub.-4 alkyl, C.sub.2.sub.-5 alkenyl, aralkyl, (C.sub.3.sub.-6 cycloalkyl)C.sub.1.sub.-4 alkyl, (C.sub.1.sub.-4 alkoxy)C.sub.1.sub.-4 alkyl, (C.sub.1.sub.-4 alkylthio)C.sub.1.sub.-4 alkyl, hydroxy-C.sub.1.sub.-4 alkyl or C.sub.2.sub.-5 alkanoyloxy-C.sub.1.sub.-4 alkyl; Y is oxygen, or a group of the formula N - R.sub.5, wherein R.sub.5 is hydrogen or C.sub.1.sub.-4 alkyl; and Z is C.sub.2.sub.-5 alkylene or alkenylene, are prepared by reacting a trihaloacetamidophenyl ketone derivative of the formula, ##SPC3##Wherein R.sub.1, R.sub.2, R.sub. 3 and R are as defined above; and X.sub.1, X.sub.2 and X.sub.3 are halogen, with an amine of the formula, HY - Z - NH.sub.2, wherein Y and Z are as defined above, or a salt thereof, in the presence of a solvent or a mixture thereof. They have remarkable pharmacological properties such as anti-inflammatory, analgesic and/or uricosuric activities.

    摘要翻译： 下式的稠合喹唑啉酮衍生物WHEREIN R1和R2分别为氢，C1-4烷基，C1-4烷氧基，硝基，C1-4烷基磺酰基或卤素; R 3是吡啶基，噻吩基或式WHEREIN R 4是氢或卤素的基团; R为氢，C 1-4烷基，C 2-5烯基，芳烷基，（C 3-6环烷基）C 1-4烷基，（C 1-4烷氧基）C 1-4烷基，（C 1-4烷硫基）C 1-4烷基，羟基 C 1-4烷基或C 2-5烷酰氧基-C 1-4烷基; Y为氧，或式为N-R5的基团，其中R5为氢或C1-4烷基; Z是C2-5亚烷基或亚烯基，是通过下式的三卤代乙酰胺基苯基酮衍生物WHEREIN R1，R2，R3和R如上所定义而制备的; 并且X 1，X 2和X 3是卤素，在溶剂或其混合物的存在下，与下式的胺HY-Z-NH 2（其中Y和Z如上定义）或其盐。 它们具有显着的药理学性质，如抗炎，镇痛和/或尿酸活性。

    Fused quinazolinones and preparation thereof
    7.
    发明授权
    Fused quinazolinones and preparation thereof 失效
    熔融喹唑啉酮及其制备方法

    公开(公告)号：US4183932A

    公开(公告)日：1980-01-15

    申请号：US873785

    申请日：1978-01-31

    申请人： Michihiro Yamamoto ,  Masao Koshiba ,  Hisao Yamamoto

    发明人： Michihiro Yamamoto ,  Masao Koshiba ,  Hisao Yamamoto

    IPC分类号： A61K31/505 ,  A61P29/00 ,  C07D239/84 ,  C07D487/04 ,  C07D491/147 ,  A61K31/41 ,  C07D487/14

    CPC分类号： C07D487/04 ,  C07D239/84 ,  Y10S514/87

    摘要： Tricyclic quinazolines of the formula, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A are as defined in the specification, such as 4,5-dihydro-5-arylimidazo[1,2-a]quinazolines, 4,5-dihydro-5-aryl-s-triazolo[4,3-a]quinazolines and 4,5-dihydro-5-aryltetrazolo[1,5-a]quinazolines having anti-inflammatory and analgesic activity are, for example, prepared by reducing the corresponding 4,5-unsaturated compounds, and then, if necessary, by alkylating the thus produced compounds.

    摘要翻译： 其中R 1，R 2，R 3，R 4和A如本说明书中所定义，如4,5-二氢-5-芳基咪唑并[1,2-a]喹唑啉，4,5-双 二氢-5-芳基-s-三唑并[4,3-a]喹唑啉和具有抗炎和止痛活性的4,5-二氢-5-芳基四唑[1,5-a]喹唑啉例如可以通过还原 相应的4,5-不饱和化合物，然后如果需要，通过烷基化所生成的化合物。

    Nitroquinazolinone compounds having antiviral properties
    8.
    发明授权
    Nitroquinazolinone compounds having antiviral properties 失效
    具有抗病性的硝基喹唑啉酮化合物

    公开(公告)号：US4146717A

    公开(公告)日：1979-03-27

    申请号：US454284

    申请日：1974-03-25

    申请人： Michihiro Yamamoto ,  Shigeaki Morooka ,  Masao Koshiba ,  Toshiaki Komatsu ,  Hiroshi Noguchi ,  Shigeho Inaba ,  Hisao Yamamoto

    发明人： Michihiro Yamamoto ,  Shigeaki Morooka ,  Masao Koshiba ,  Toshiaki Komatsu ,  Hiroshi Noguchi ,  Shigeho Inaba ,  Hisao Yamamoto

    IPC分类号： C07D239/82

    CPC分类号： C07D239/82

    摘要： Viral infections caused by viruses which belong to, e.g. Pox, Herpes, Adeno, Myxo, Paramyxo groups are controlled by administering an effective amount of quinazoline derivatives of the formula ##STR1## wherein R.sub.1 is cyclo, C.sub.3 -C.sub.8 alkyl, cyclo C.sub.3 -C.sub.8 alkyl C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy C.sub.1 -C.sub.4 alkyl, C.sub.2-C.sub.5 alkenyloxy C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkylthio C.sub.1 -C.sub.4 alkyl, polyhalo C.sub.1- C.sub.4 alkyl, a group of the formula ##STR2## (wherein m is an integer of 1 to 3; and R.sub.4 and R.sub.5 are individually C.sub.1 -C.sub.4 alkyl, and may form together with the adjacent nitrogen atom an unsubstituted or C.sub.1 -C.sub.4 alkyl substituted 3 to 6 membered saturated heterocyclic ring, which may contain another nitrogen or oxygen atom) or a group of the formula --C.sub.n H.sub.2n --R.sub.6 (wherein n is 0 or an integer of 1 to 3; and R.sub.6 is a phenyl group, a substituted phenyl group or an aromatic or non-aromatic 3 to 6 membered heterocyclic ring which contains one or two hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur atom, and may be optionally substituted by one or two C.sub.1 -C.sub.4 alkyl, and further, those substituents on adjacent carbon atoms may be joined to form a benzene or cyclohexane ring); R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, trifluoromethyl or nitro; and R.sub.3 is phenyl, substituted phenyl, cyclo C.sub.3 -C.sub.6 alkyl, pyridyl, furyl, nitrofuryl, thienyl, nitrothienyl, methylthienyl or pyrimidinyl.

    Process for preparing quinazolinone derivatives and their 2-(N-mono-substituted amino)-phenyl ketone intermediate derivatives
    9.
    发明授权
    Process for preparing quinazolinone derivatives and their 2-(N-mono-substituted amino)-phenyl ketone intermediate derivatives 失效
    制备喹唑啉酮衍生物及其2-（N-单取代氨基） - 苯基酮中间体衍生物的方法

    公开(公告)号：US4096144A

    公开(公告)日：1978-06-20

    申请号：US592241

    申请日：1975-07-01

    申请人： Michihiro Yamamoto ,  Masao Koshiba ,  Shigeho Inaba ,  Hisao Yamamoto

    发明人： Michihiro Yamamoto ,  Masao Koshiba ,  Shigeho Inaba ,  Hisao Yamamoto

    IPC分类号： C07D213/50 ,  C07D333/20 ,  C07D333/22 ,  C07D239/82 ,  C07C97/10

    CPC分类号： C07D333/22 ,  C07D213/50 ,  C07D333/20

    摘要： 1,4-Substituted-2(1H)-quinazolinone derivatives are prepared by contactng a 2-aminophenyl ketone derivative with an alkaline agent such as alkali metal, alkali metal hydride, alkali metal amide, etc., reacting the thus obtained metal salt of 2-aminophenyl ketone derivative with a reactive ester of alcohols, reacting the thus obtained 2-(N-mono-substituted amino)-phenyl ketone derivative with a lower alkyl haloformate or a benzyl haloformate, and reacting the thus obtained carbamate derivative with ammonia. The 1,4-substituted-2(1H)-quinazolinone derivatives have excellent pharmacological properties, particularly as anti-inflammatory and analgesic effects.

    摘要翻译： 1,4-取代-2（1H） - 喹唑啉酮衍生物是通过使2-氨基苯基酮衍生物与碱金属如碱金属，碱金属氢化物，碱金属氨化物等接触而制得的，使得到的 2-氨基苯基酮衍生物与醇的反应性酯反应，将由此得到的2-（N-单取代氨基） - 苯基酮衍生物与卤代甲酸低级烷基酯或卤代甲酸苄酯反应，并使得到的氨基甲酸酯衍生物与氨反应。 1,4-取代-2（1H） - 喹唑啉酮衍生物具有优异的药理学特性，特别是抗炎和止痛作用。

    Quinazolinone derivatives and a process for production thereof
    10.
    发明授权
    Quinazolinone derivatives and a process for production thereof 失效
    喹唑啉酮衍生物及其生产方法

    公开(公告)号：US4099002A

    公开(公告)日：1978-07-04

    申请号：US495829

    申请日：1974-08-08

    申请人： Shigeho Inaba ,  Michihiro Yamamoto ,  Kikuo Ishizumi ,  Kazuo Mori ,  Masao Koshiba ,  Hisao Yamamoto

    发明人： Shigeho Inaba ,  Michihiro Yamamoto ,  Kikuo Ishizumi ,  Kazuo Mori ,  Masao Koshiba ,  Hisao Yamamoto

    IPC分类号： C07D239/82 ,  C07D403/06 ,  C07D413/06

    CPC分类号： C07D403/06 ,  C07D239/82 ,  C07D413/06

    摘要： 3,4-Dihydro-2(1H)-quinazolinone derivatives of the formula, ##STR1## wherein R.sub.1 and R.sub.2 signify individually a hydrogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, a trifluoromethyl group, a lower alkylthio group, a lower alkylsulfonyl group or a halogen atom; R.sub.3 signifies a phenyl group, a halophenyl group, a lower alkylphenyl group, a lower alkoxyphenyl group, a trifluoromethylphenyl group, a lower cycloalkyl group, a lower cycloalkenyl group, a pyridyl group, a pyrrolyl group, a furyl group, a thienyl group or a naphthyl group; R.sub.4 signifies a lower alkyl group, a lower alkenyl group, an aralkyl group, a lower cycloalkylalkyl group, a lower cycloalkyl group, a lower alkoxyalkyl group, a lower alkylthioalkyl group, a lower hydroxyalkyl group, a lower alkanoyloxyalkyl group, a phenyl group, a halophenyl group, a trifluoromethylphenyl group, a lower alkylphenyl group a lower alkoxyphenyl group, a pyridyl group or a group of the formula ##STR2## wherein n signifies an integer of 1 to 4; and R.sub.5 and R.sub.6 signify individually a lower alkyl group, provided that they may form together with the adjacent nitorgen atom an optionally substituted 5- or 6-membered heterocyclic ring, which may further contain a hetero atom); and R signifies a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkoxyalkyl group, a lower alkylthioalkyl group, an aralkyl group, a lower cycloalkylalkyl group, a lower trihalomethylalkyl group or a group of the formula ##STR3## (wherein n, R.sub.5 and R.sub.6 signify the same as defined above), which have excellent pharmacological properties such as central nervous system depressant, anti-inflammatory, analgestic and anti-microbial activities, can be produced by reducing a compound of the formula, ##STR4## wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the same meanings as defined above; and X.sub.1, X.sub.2 and X.sub.3 signify individually a halogen atom, or by the substitution reaction of the ring nitrogen atom of a 1 or 3-unsubstituted 3,4-dihydro-2(1H)-quinazolinone derivative.