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1. 发明授权

US3953446A Process for preparing quinazolines 失效
标题翻译：制备喹唑啉的方法
公开(公告)号：US3953446A
公开(公告)日：1976-04-27
申请号：US494885
申请日：1974-08-05
申请人： Kikuo Ishizumi , Kazuo Mori , Michihiro Yamamoto , Masao Koshiba , Shigeho Inaba , Hisao Yamamoto
发明人： Kikuo Ishizumi , Kazuo Mori , Michihiro Yamamoto , Masao Koshiba , Shigeho Inaba , Hisao Yamamoto
IPC分类号： C07D239/82 , C07D209/10 , C07D209/42 , C07D401/06 , C07D405/06 , C07D409/06 , C07D405/04
CPC分类号： C07C247/00 , C07D209/42
摘要： Quinazoline derivatives which have anti-inflammatory, antiviral, uricosuric activities are prepared by reacting an indole-2-carbonylazide derivative with an oxidizing agent under mild conditions.
摘要翻译：具有抗炎，抗病毒，尿酸营养活性的喹唑啉衍生物通过在温和条件下使吲哚-2-羰基叠氮化物衍生物与氧化剂反应来制备。

2. 发明授权

US4067868A Production of quinazolinone compounds 失效
标题翻译：喹唑啉酮化合物的生产
公开(公告)号：US4067868A
公开(公告)日：1978-01-10
申请号：US670952
申请日：1976-03-26
申请人： Kikuo Ishizumi , Kazuo Mori , Michihiro Yamamoto , Masao Koshiba , Shigeho Inaba , Hisao Yamamoto
发明人： Kikuo Ishizumi , Kazuo Mori , Michihiro Yamamoto , Masao Koshiba , Shigeho Inaba , Hisao Yamamoto
IPC分类号： C07D207/40 , C07D233/96 , C07D239/82
CPC分类号： C07D207/40 , C07D233/96 , C07D239/82
摘要： 2(1H)-Quinazolinone derivatives, which are useful as anti-inflammatory agents, are prepared by heating or hydrolyzing an acylurea derivative. The acylurea derivative can be prepared by either reacting an indole derivative with an oxidizing agent or reacting an imidazolidine derivative with water, an alkanol or ammonia.
摘要翻译：通过加热或水解酰基脲衍生物制备可用作抗炎剂的2（1H） - 喹唑啉酮衍生物。酰基脲衍生物可以通过使吲哚衍生物与氧化剂反应或使咪唑烷衍生物与水，链烷醇或氨反应来制备。

3. 发明授权

US3980645A Fused quinazolinones and a process for production thereof 失效
标题翻译：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。

4. 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.

5. 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。

6. 发明授权

US4179560A Imidazo- and pyrimido[2,1-b]quinazolines and preparation thereof 失效
标题翻译：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。

7. 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。

8. 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。

9. 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.

10. 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。

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