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61. 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.

62. 发明授权

US3991048A Process for the preparation of 1,4-benzodiazepine derivatives 失效
标题翻译： 1,4-苯并二氮杂衍生物的制备方法
公开(公告)号：US3991048A
公开(公告)日：1976-11-09
申请号：US552888
申请日：1975-02-25
申请人： Kikuo Ishizumi , Kazuo Mori , Shigeho Inaba , Hisao Yamamoto
发明人： Kikuo Ishizumi , Kazuo Mori , Shigeho Inaba , Hisao Yamamoto
IPC分类号： A47G27/04 , A61K31/55 , C07D20060101 , C07D243/16 , C07D243/18 , C07D243/24 , C07D243/28
CPC分类号： C07C265/00
摘要： A 1,4-benzodiazepine derivative, or a pharmaceutically acceptable acid salt thereof, of the formula, ##SPC1##Wherein R.sub.1 is hydrogen, halogen, nitro or trifluoromethyl; R.sub.2 and R.sub.3 are independently hydrogen, halogen, lower alkyl or trifluoromethyl; R.sub.4 is lower alkyl, alkenyl, trihaloalkyl, alkoxyalkyl, alkenyloxyalkyl, alkoxyalkoxyalkyl, alkanoyloxyalkyl, cycloalkylalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl or a group of the formula ##EQU1## in which R.sub.6 and R.sub.7 are independently lower alkyl, and n is an integer of 1 to 4; and R.sub.5 is hydrogen or lower alkyl, is obtained by reacting a benzophenone derivative of the formula, ##SPC2##Wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined above, with a 2-isocyanatoacetyl chloride derivative of the formula ##EQU2## wherein R.sub.5 is as defined above.
摘要翻译：下式的1,4-苯并二氮杂衍生物或其药学上可接受的酸盐，其中R 1是氢，卤素，硝基或三氟甲基; R2和R3独立地是氢，卤素，低级烷基或三氟甲基; R4是低级烷基，链烯基，三卤代烷基，烷氧基烷基，烯氧基烷基，烷氧基烷氧基烷基，烷酰氧基烷基，环烷基烷基，烷基硫代烷基，烷基亚磺酰基烷基，烷基磺酰基烷基或式R6-nH2n-N型阴离子R7，其中R6和R7独立地为低级烷基，n为 1〜4的整数; 通过使下式的二苯甲酮衍生物，即WHEREIN R 1，R 2，R 3和R 4如上定义的二苯甲酮衍生物与下式的2-异氰酸根合乙酰氯衍生物反应，得到式 = O，其中R5如上所定义。

63. 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。

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