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1. 发明授权

US4079053A Benzodiazepine derivatives 失效
标题翻译：苯并二氮杂衍生物
公开(公告)号：US4079053A
公开(公告)日：1978-03-14
申请号：US710665
申请日：1976-08-02
申请人： Hisao Yamamoto , Shigeho Inaba , Toshiyuki Hirohashi , Michihiro Yamamoto , Kikuo Ishizumi , Mitsuhiro Akatsu , Isamu Maruyama , Kazuo Mori , Yoshiharu Kume , Takahiro Izumi
发明人： Hisao Yamamoto , Shigeho Inaba , Toshiyuki Hirohashi , Michihiro Yamamoto , Kikuo Ishizumi , Mitsuhiro Akatsu , Isamu Maruyama , Kazuo Mori , Yoshiharu Kume , Takahiro Izumi
IPC分类号： A61K31/55 , C07D243/24 , C07D401/04
CPC分类号： C07D243/24 , A61K31/55 , C07D243/26 , C07D243/28 , C07D243/30 , C07D243/36 , C07D401/04
摘要： Novel 1-substituted benzodiazepine derivatives and salt thereof having the formula, ##STR1## wherein R.sub.1 is a hydrogen atom, a halogen atom, a nitro group, a cyano group, a lower alkoxy group or a trifluoromethyl group; R.sub.2 is a pyridyl group or a group of the formula ##STR2## wherein R.sub.5 and R.sub.6 represent individually a hydrogen atom, a halogen atom, a lower alkyl group or a trifluoromethyl group); R.sub.3 is a hydrogen atom or a lower alkyl group; R.sub.4 is a lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl group; m is 1 or 2; and n is an integer of 1 to 4, and a process for preparation thereof and pharmaceutical use of the same.The benzodiazepine derivatives are effective as tranquillizers, muscle-relaxants and hypnotics.
摘要翻译：新颖的1-取代苯并二氮杂衍生物及其盐，具有下式：其中R 1是氢原子，卤原子，硝基，氰基，低级烷氧基或三氟甲基; R2是吡啶基或式的基团，其中R5和R6分别表示氢原子，卤素原子，低级烷基或三氟甲基）。 R3是氢原子或低级烷基; R4是低级烷基，环烷基，环烷基烷基，芳基或芳烷基; m为1或2; n为1〜4的整数，其制备方法和药物用途。

2. 发明授权

US4010154A Benzodiazepinones 失效
标题翻译：苯并二氮杂
公开(公告)号：US4010154A
公开(公告)日：1977-03-01
申请号：US497936
申请日：1974-08-16
申请人： Hisao Yamamoto , Shigeho Inaba , Toshiyuki Hirohashi , Michihiro Yamamoto , Kikuo Ishizumi , Mitsuhiro Akatsu , Isamu Maruyama , Kazuo Mori , Yoshiharu Kume , Takahiro Izumi
发明人： Hisao Yamamoto , Shigeho Inaba , Toshiyuki Hirohashi , Michihiro Yamamoto , Kikuo Ishizumi , Mitsuhiro Akatsu , Isamu Maruyama , Kazuo Mori , Yoshiharu Kume , Takahiro Izumi
IPC分类号： A61K31/55 , C07D243/24 , C07D401/04 , C07D243/20
CPC分类号： C07D243/24 , A61K31/55 , C07D243/26 , C07D243/28 , C07D243/30 , C07D243/36 , C07D401/04
摘要： Novel 1-substituted benzodiazepine derivatives and salt thereof having the formula, ##STR1## wherein R.sub.1 is a hydrogen atom, a halogen atom, a nitro group, a cyano group, a lower alkoxy group or a trifluoromethyl group; R.sub.2 is a pyridyl group or a group of the formula ##STR2## wherein R.sub.5 and R.sub.6 represent individually a hydrogen atom, a halogen atom, a lower alkyl group or a trifluoromethyl group); R.sub.3 is a hydrogen atom or a lower alkyl group; R.sub.4 is a lower alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl group; m is 1 or 2; and n is an integer of 1 to 4, and a process for preparation thereof and pharmaceutical use of the same.
摘要翻译：新颖的1-取代苯并二氮杂衍生物及其盐，具有下式：其中R 1是氢原子，卤原子，硝基，氰基，低级烷氧基或三氟甲基; R2是吡啶基或式的基团，其中R5和R6分别表示氢原子，卤素原子，低级烷基或三氟甲基）。 R3是氢原子或低级烷基; R4是低级烷基，环烷基，环烷基烷基，芳基或芳烷基; m为1或2; n为1〜4的整数，其制备方法和药物用途。

3. 发明授权

US3989829A 1,4-Benzodiazepines 失效
标题翻译： 1,4-苯并二氮杂
公开(公告)号：US3989829A
公开(公告)日：1976-11-02
申请号：US594771
申请日：1975-07-10
申请人： Hisao Yamamoto , Shigeho Inaba , Toshiyuki Hirohashi , Michihiro Yamamoto , Kikuo Ishizumi , Mitsuhiro Akatsu , Isamu Maruyama , Yoshiharu Kume , Kazuo Mori , Takahiro Izumi
发明人： Hisao Yamamoto , Shigeho Inaba , Toshiyuki Hirohashi , Michihiro Yamamoto , Kikuo Ishizumi , Mitsuhiro Akatsu , Isamu Maruyama , Yoshiharu Kume , Kazuo Mori , Takahiro Izumi
IPC分类号： A61K31/395 , A61K31/55 , C07D243/14 , C07D243/24 , C07D243/30 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/06 , C07D409/04 , C07D413/06
CPC分类号： C07D243/24 , A61K31/395 , A61K31/55 , C07D243/14 , C07D243/30 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/06 , C07D409/04 , C07D413/06
摘要： Benzodiazepine derivatives of the formula, ##SPC1##Wherein R.sub.1 is a C.sub.2-4 alkenyl group, R.sub.2 is a halogen atom and R.sub.3 is a hydrogen or halogen atom, which are useful as minor tranquilizer and anticonvulsant. These compounds are prepared by reacting a compound of the formula, ##SPC2##Wherein R.sub.1, R.sub.2, and R.sub.3 are as defined above, with a compound of the formula, ##EQU1## wherein X is an oxygen or sulfur atom.
摘要翻译：下式的苯并二氮杂衍生物，其中R 1为C 2-4链烯基，R 2为卤素原子，R 3为氢或卤素原子，其可用作较小的镇静剂和抗惊厥药。这些化合物通过使下式的化合物，即WHEREIN R 1，R 2和R 3如上所定义的化合物与下式化合物O CH 2 -CONGOR | X NH-C ANGLE O反应而制备，其中X是氧或硫原子。

4. 发明授权

US4002611A Preparation of benzodiazepines 失效
标题翻译：苯二氮卓类的制备
公开(公告)号：US4002611A
公开(公告)日：1977-01-11
申请号：US797663
申请日：1969-02-07
申请人： Hisao Yamamoto , Shigeho Inaba , Tadashi Okamoto , Toshiyuki Hirohashi , Kikuo Ishizumi , Michihiro Yamamoto , Isamu Maruyama , Kazuo Mori , Tsuyoshi Kobayashi
发明人： Hisao Yamamoto , Shigeho Inaba , Tadashi Okamoto , Toshiyuki Hirohashi , Kikuo Ishizumi , Michihiro Yamamoto , Isamu Maruyama , Kazuo Mori , Tsuyoshi Kobayashi
IPC分类号： C07D209/04 , C07D209/08 , C07D243/16
CPC分类号： C07D209/04 , C07D209/08
摘要： A 1-alkyl-1,2,4,5-tetrahydro-3H-1,4-benzodiazepine derivative is produced by contacting a 1-aminoethyl-indole derivative with a suitable oxidizing agent and then reducing the resulting 1-acyl-2,3-dihydro-1H-1,4-benzodiazepine derivative. The starting 1-aminoethyl-indole derivative is prepared by subjecting a 3-phenyl-indole derivative to cyanomethylation (or carbamoylemethylation) and then reducing the resulting 1-cyanomethyl- (or 1-carbamoylmethyl)-indole derivative. The 1-acyl-1,2,4,5-tetrahydro-3H-1,4-benzodiazepine derivative is useful as a tranquillizer, muscle-relaxant, etc.
摘要翻译： 1-烷基-1,2,4,5-四氢-3H-1,4-苯并二氮杂衍生物是通过使1-氨基乙基 - 吲哚衍生物与合适的氧化剂接触，然后将所得1-酰基-2 3-二氢-1H-1,4-苯并二氮杂衍生物。起始的1-氨基乙基 - 吲哚衍生物通过使3-苯基 - 吲哚衍生物进行氰甲基化（或氨甲酰甲基化）然后还原所得的1-氰基甲基 - （或1-氨基甲酰基甲基） - 吲哚衍生物来制备。 1-酰基-1,2,4,5-四氢-3H-1,4-苯并二氮杂衍生物可用作镇静剂，肌肉松弛剂等

5. 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。

6. 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.

7. 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。

8. 发明授权

US4202895A 1-Polyhaloalkyl-2(1H)-quinazolinone derivatives 失效
标题翻译： 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。

9. 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。

10. 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。

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