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15 条记录 (耗时 0.024 秒)

    Process for preparing 1-polyhaloalkyl-3,4-dihydro-2-(1H)-quinazolinones
    2.
    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。

    Imidazo- and pyrimido[2,1-b]quinazolines and preparation thereof
    5.
    发明授权
    Imidazo- and pyrimido[2,1-b]quinazolines and preparation thereof 失效
    咪唑并嘧啶并[2,3-b]喹唑啉及其制备方法

    公开(公告)号：US4179560A

    公开(公告)日：1979-12-18

    申请号：US553676

    申请日：1975-02-27

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

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

    IPC分类号： A61K31/505 ,  A61P7/10 ,  A61P9/12 ,  A61P25/24 ,  A61P25/26 ,  C07D487/04 ,  C07D491/147 ,  A61K31/395

    CPC分类号： C07D487/04

    摘要： Imidazo- and pyrimido[2,1-b]quinazolines of the formula, ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, trifluoromethyl, nitro, C.sub.1-4 alkyl or C.sub.1-4 alkoxy, or R.sub.1 and R.sub.2 may together represent methylenedioxy; R.sub.3 is hydrogen, C.sub.1-4 alkyl, phenyl or substituted phenyl of the formula, ##STR2## (wherein R is halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy); R.sub.4 is hydrogen, C.sub.1-4 alkyl or aralkyl; and A is C.sub.2-3 alkylene wich may be optionally substituted by one or two C.sub.1-2 alkyl radicals, and pharmaceutically acceptable acid addition salts thereof, are prepared by reacting a compound of the formula, ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A are as defined above; and X is oxygen or sulfur, with a halogenating agent at a temperature of about 30.degree. C. to about 180.degree. C. In the above imidaxo- and pyrimido[2,1-b]quinazolines, those having C.sub.1-4 alkyl, or ##STR4## as R.sub.3 are novel compounds and show antidepressant and/or antihypertensive activities.

    摘要翻译： 其中R 1和R 2独立地为氢，卤素，三氟甲基，硝基，C 1-4烷基或C 1-4烷氧基，或者R 1和R 2可以一起代表下式的咪唑并 - 嘧啶并[2,3-b]喹唑啉， 亚甲二氧基; R 3是氢，C 1-4烷基，苯基或下式的取代的苯基，其中R是卤素，C 1-4烷基或C 1-4烷氧基; R4是氢，C1-4烷基或芳烷基; 并且A是可以任选被一个或两个C 1-2烷基取代的C 2-3亚烷基及其药学上可接受的酸加成盐，其通过使下式化合物，其中R1，R2，R3， R4和A如上所定义; 在上述酰胺基 - 和嘧啶并[2,1-b]喹唑啉中，具有C 1-4烷基的那些，或其中X是氧或硫，与卤化剂在约30℃至约180℃的温度下反应。 作为R3是新化合物并显示抗抑郁药和/或抗高血压活性的图像。

    Quinazolinone derivatives and a process for production thereof
    6.
    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.

    Triazoloquinazolines
    7.
    发明授权
    Triazoloquinazolines 失效
    三唑并喹唑啉

    公开(公告)号：US4002755A

    公开(公告)日：1977-01-11

    申请号：US552889

    申请日：1975-02-25

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

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

    IPC分类号： C07D239/84 ,  C07D249/08 ,  C07D487/04 ,  C07D491/147

    CPC分类号： C07D487/04 ,  C07D239/84

    摘要： Triazoloquinazolines of the formula, ##STR1## wherein R.sub.1 is C.sub.1.sub.-4 alkyl or aryl; R.sub.2 and R.sub.3 are independently hydrogen, halogen, trifluoromethyl, nitro, C.sub.1.sub.-4 alkyl or C.sub.1.sub.-4 alkoxy, or R.sub.2 and R.sub.3 together may form methylenedioxy; and R.sub.4 is hydrogen, C.sub.1.sub.-4 alkyl, aralkyl, C.sub.1.sub.-4 haloalkyl, or C.sub.3.sub.-6 cycloalkyl; and pharmaceutically acceptable acid addition salts thereof are prepared by (a) reacting a 2-hydrazinoquinazoline derivative with a carboxylic acid or reactive derivative thereof, (b) cyclizing a 2-acylhydrazinoquinazoline derivative with heating or (c) reacting a triazolylbenzophenone derivative with ammonia. Said triazoloquinazolines and pharmaceutically acceptable acid addition salts thereof show excellent anti-inflammatory and analgesic activities.

    摘要翻译： 式中的三唑并喹唑啉，其中R 1为C 1-4烷基或芳基; R2和R3独立地是氢，卤素，三氟甲基，硝基，C1-4烷基或C1-4烷氧基，或者R2和R3一起可以形成亚甲二氧基; 和R 4是氢，C 1-4烷基，芳烷基，C 1-4卤代烷基或C 3-6环烷基; （a）使2-肼基喹唑啉衍生物与羧酸或其反应性衍生物反应，（b）使2-酰基肼基喹唑啉衍生物加热环化，或（c）使三唑基二苯甲酮衍生物与氨反应，制备其药学上可接受的酸加成盐。 所述三唑并喹唑啉及其药学上可接受的酸加成盐显示出优异的抗炎和止痛活性。

    Quinazoline derivatives in pharmaceutical compositions for treating pain and inflammation
    9.
    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。