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1. 发明授权

US4099002A Quinazolinone derivatives and a process for production thereof 失效
标题翻译：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.

2. 发明授权

US4002755A Triazoloquinazolines 失效
标题翻译：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。

3. 发明授权

US3970654A Antiviral 2(1H)-quinazolinone derivatives 失效
标题翻译：抗病毒2（1H） - 喹唑啉酮衍生物
公开(公告)号：US3970654A
公开(公告)日：1976-07-20
申请号：US493240
申请日：1974-07-30
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： C07D239/82 , A61K31/38 , A61K31/44 , A61K31/495 , A61K31/505 , A61K31/517 , A61P31/12 , C07D20060101 , C07D213/53 , C07D215/56 , C07D239/72 , C07D239/80 , C07D333/22 , C07D333/24 , C07D401/04 , C07D409/04
CPC分类号： C07D239/82
摘要： Quinazolinone derivatives of the formula, ##SPC1##Wherein R is a polyalicyclic hydrocarbon group; R.sup.1 and R.sup.2 are independently a hydrogen atom, a nitro group, a trifluoromethyl group or a methylsulfonyl group; R.sup.3 is a phenyl group, a substituted phenyl group, a pyridyl group or a thienyl group; and n is 0 or an integer of 1 to 3, have potent antiviral activity with low toxicities. These compounds can be prepared using a variety of processes analogous to known methods, for example, by oxidizing a 3,4-dihydro-2(1H)-quinazolinone having a polyalicyclic hydrocarbon group bonded through an alkylene group at the 1 position.
摘要翻译：下式的喹唑啉酮衍生物，WHEREIN R是多元环烃基; R1和R2独立地为氢原子，硝基，三氟甲基或甲基磺酰基; R3是苯基，取代苯基，吡啶基或噻吩基; n为0或1〜3的整数，具有低毒性的抗病毒活性。这些化合物可以使用与已知方法类似的各种方法制备，例如通过氧化具有通过1位上的亚烷基键合的多脂环烃基的3,4-二氢-2（1H） - 喹唑啉酮。

4. 发明授权

US3950526A Quinazoline derivatives in pharmaceutical compositions for treating pain and inflammation 失效
标题翻译：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。

5. 发明授权

US4228167A Diuretic and vasodilating tricyclic quinazolines 失效
标题翻译：利尿和血管舒张三环喹唑啉
公开(公告)号：US4228167A
公开(公告)日：1980-10-14
申请号：US939869
申请日：1978-09-05
申请人： Michihiro Yamamoto , Masao Koshiba , Shunji Aono
发明人： Michihiro Yamamoto , Masao Koshiba , Shunji Aono
IPC分类号： A61K31/505 , A61P7/10 , C07D487/04 , C07D487/14
CPC分类号： C07D487/04 , Y10S514/869
摘要： Novel imidazo[2,1-b]quinazolines and pyrimido-[2,1-b]quinozolines represented by the formula, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and A are as defined in the specification were prepared. They have prominent pharmacological properties such as diuretic and vasodilating activity.
摘要翻译：由式表示的新型咪唑并[2,1-b]喹唑啉和嘧啶并[2,1-b]喹唑啉，其中R1，R2，R3，R4，R5和A如说明书中所定义。它们具有突出的药理学性质，如利尿和血管扩张活性。

6. 发明授权

US4183932A Fused quinazolinones and preparation thereof 失效
标题翻译：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。

7. 发明授权

US4146717A Nitroquinazolinone compounds having antiviral properties 失效
标题翻译：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.

8. 发明授权

US4096144A Process for preparing quinazolinone derivatives and their 2-(N-mono-substituted amino)-phenyl ketone intermediate derivatives 失效
标题翻译：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。

9. 发明授权

US4048168A Process for preparing 1-polyhaloalkyl-3,4-dihydro-2-(1H)-quinazolinones 失效
标题翻译： 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。

10. 发明授权

US4387223A Process for preparing 2(1H)-quinazolinone derivatives 失效
标题翻译：制备2（1H） - 喹唑啉酮衍生物的方法
公开(公告)号：US4387223A
公开(公告)日：1983-06-07
申请号：US748145
申请日：1976-12-06
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： C07D239/78 , C07D239/82 , C07D401/04 , C07D405/04 , C07D409/04 , C07D491/04 , C07D491/056 , C07D413/04 , C07D413/06
CPC分类号： C07D491/04 , C07D239/78 , C07D239/82
摘要： 2(1H)-Quinazolinone and quinazolinethione derivatives having excellent pharmacological activities are produced in high yield with high purity by heating the corresponding 3,4-dihydro-2(1H)-quinazolinone or quinazolinethione derivatives together with sulfur in an inert solvent.
摘要翻译：通过在惰性溶剂中与硫一起加热相应的3,4-二氢-2（1H） - 喹唑啉酮或喹唑啉硫酮衍生物，通过加热相应的3,4-二氢-2（1H） - 喹唑啉酮或喹唑啉硫酮衍生物，以高纯度产生具有优异药理活性的2（1H） - 喹唑啉酮和喹唑啉酮衍生物。

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