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    Quinazolinone derivatives and a process for production thereof
    2.
    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.

    Quinazoline derivatives in pharmaceutical compositions for treating pain and inflammation
    3.
    发明授权
    Quinazoline derivatives in pharmaceutical compositions for treating pain and inflammation 失效
    用于治疗疼痛和炎症的药物组合物中的喹唑啉衍生物

    公开(公告)号：US3950526A

    公开(公告)日：1976-04-13

    申请号：US518070

    申请日：1974-10-25

    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： C07D239/80 ,  C07D239/82 ,  C07D333/22 ,  C07D401/04 ,  C07D409/04 ,  A61K31/505

    CPC分类号： C07D401/04 ,  C07D239/80 ,  C07D239/82 ,  C07D333/22 ,  C07D409/04

    摘要： Quinazoline derivatives represented by the formula ##SPC1##Wherein R.sub.1 and R.sub.2 are individually a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, a lower alkylthio group or a lower alkylsulfonyl group; R.sub.3 is a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, a napthyl group, a furyl group or a thienyl group; R.sub.4 is a lower cycloalkyl group or a trihalomethyl group; and n is an integer of 1 to 3, are novel compounds and have excellent pharmacological properties, particularly as anti-inflammatory and analgesic effects with low toxicity. They can be prepared by treating with ammonia a trihaloacetamidophenylketone derivative of the formula, ##SPC2##Wherein R.sub.1, R.sub.2 and R.sub.3 are as defined above; R is a hydrogen atom or a group of the formula --C.sub.n H.sub.2n --R.sub.4 ; and X is a halogen atom.

    摘要翻译： 由式WHEREIN R1和R2表示的喹唑啉衍生物分别为氢原子，卤素原子，低级烷基，低级烷氧基，硝基，低级烷硫基或低级烷基磺酰基; R3是氢原子，低级烷基，低级环烷基，萘基，呋喃基或噻吩基; R4是低级环烷基或三卤代甲基; n为1〜3的整数，为新化合物，具有优异的药理特性，特别是具有低毒性的抗炎镇痛作用。 它们可以通过用氨处理下式的三卤代乙酰胺基苯基酮衍生物，即WHEREIN R1，R2和R3如上所定义; R是氢原子或式-C n H 2n -R 4的基团; X为卤素原子。

    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。

    1-Polyhaloalkyl-2(1H)-quinazolinone derivatives
    8.
    发明授权
    1-Polyhaloalkyl-2(1H)-quinazolinone derivatives 失效
    1-多卤烷基-2（1H） - 喹唑啉酮衍生物

    公开(公告)号：US4202895A

    公开(公告)日：1980-05-13

    申请号：US479464

    申请日：1974-06-14

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

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

    IPC分类号： C07D239/82 ,  A61K31/505

    CPC分类号： C07D239/82 ,  Y10S514/825

    摘要： 1-Polyhaloalkyl-2(1H)-quinazoline derivatives of the formula, ##STR1## wherein R is polyhaloalkyl having C.sub.2 -C.sub.4 alkyl; and R.sub.1, R.sub.2 and R.sub.3 are individually hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, trifluoromethyl or halogen, have excellent anti-inflammatory and analgesic activities with very low toxicity. These quinazolinone derivatives can be prepared, for example, by reacting a trihalogenoacetamidobenzophenone derivative with ammonia.

    摘要翻译： 具有下式的1-多卤烷基-2（1H） - 喹唑啉衍生物，其中R是具有C 2 -C 4烷基的多卤代烷基; R1，R2和R3分别为氢，C1-C4烷基，C1-C4烷氧基，硝基，三氟甲基或卤素，具有优异的抗炎和止痛活性，毒性非常低。 这些喹唑啉酮衍生物可以通过例如三卤代乙酰胺二苯甲酮衍生物与氨反应来制备。