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1. 发明授权

US3974145A Novel N'-acylated phenyl-hydrazine and hydrozone derivatives 失效
标题翻译：新型N {40-酰基苯基 - 肼和水解产物
公开(公告)号：US3974145A
公开(公告)日：1976-08-10
申请号：US439035
申请日：1974-02-04
申请人： Michio Kimura , Shigeho Inaba , Hisao Yamamoto
发明人： Michio Kimura , Shigeho Inaba , Hisao Yamamoto
IPC分类号： C07D209/60 , C07D209/70 , C07D307/54 , C07D317/66 , C07D317/68 , C07D319/18
CPC分类号： C07D307/54 , C07D209/60 , C07D209/70 , C07D317/66 , C07D317/68 , C07D319/18
摘要： Novel indolylacetic acid derivatives, which have excellent anti-inflammatory, antipyretic and analgesic activities, represented by the formula, ##SPC1##Wherein X.sub.1 and X.sub.2 each is a member selected from the group consisting of oxygen and methylene; A is a member selected from the group consisting of unsubstituted saturated hydrocarbon chain having up to 5 carbon atoms, unsubstituted unsaturated hydrocarbon chain having up to 5 carbon atoms and substituted saturated or substituted ethylenically unsaturated hydrocarbon chain having up to 5 carbon atoms, in which the substituents are selected from the group consisting of halogen or phenyl, the hydrocarbon chain being straight or blanched one; m is 0 or 1; n is 1 or 2; R.sub.1 and R.sub.2 each is a member selected from the group consisting of hydrogen and alkyl having up to 4 carbon atoms; R.sub.3 is a member selected from the group consisting of alkyl having up to 4 carbon atoms, unsubstituted or a lower alkyl-, lower alkoxy-, lower alkylthio-, nitro-, cyano-, methylenedioxy-, ethylenedioxy- or halogen-substituted aryl, each of said alkyl, alkoxy and alkylthio substituents containing up to 4 carbon atoms, or unsubstituted, or halogen-, alkyl- or phenyl-substituted or benzene ring-condensed, saturated or unsaturated mono- or poly-aclicyclic group, or alkyl group substituted by said alicyclic group, or unsubstituted or methyl-, ethyl- or halogen-substituted 5- or 6-membered heterocyclic ring group containing oxygen, sulfur or nitrogen atom; R.sub.4 is a member selected from the group consisting of alkyl having up to 4 carbon atoms or hydrogen, or a group of M (wherein M is a cation).The indolylacetic acid of the formula (I) is prepared by reacting a compound of the formula, ##SPC2##Wherein X.sub.1, X.sub.2 and n are the same as defined above and B is a member selected from the group consisting of ##EQU1## and Z (wherein Z is a nitrogen protecting system comprising at least one readily removable group), with an acid halide represented by the formula,R.sub.3 --(A).sub.m --CO--hal (V)wherein R.sub.3, A and m are the same as defined above and hal is halogen, to obtain N.sup.1 -acylated compound of the formula, ##SPC3##Wherein X.sub.1, X.sub.2, R.sub.3, A, B, m and n are the same as defined above, then reacting the resultant N.sup.1 -acylated compound (II) with an aliphatic acid derivative represented by the formula, ##EQU2## wherein R.sub.1, R.sub.2 and R.sub.4 are the same as defined above.
摘要翻译：新型吲哚乙酸衍生物，其具有优异的抗炎，解热和止痛活性，由式WHEREIN X1和X2各自为选自氧和亚甲基的成员; A是选自具有至多5个碳原子的未取代的饱和烃链，具有至多5个碳原子的未取代的不饱和烃链和具有至多5个碳原子的取代的饱和或取代的烯属不饱和烃链的成员，其中取代基选自卤素或苯基，烃链是直链或漂白的; m为0或1; n为1或2; R1和R2各自是选自氢和具有至多4个碳原子的烷基的成员; R3是选自具有至多4个碳原子的烷基，未取代的或低级烷基，低级烷氧基 - ，低级烷硫基 - ，硝基 - ，氰基 - ，亚甲二氧基 - ，亚乙二氧基或卤素取代的芳基的成员，所述烷基，烷氧基和烷硫基取代基含有至多4个碳原子，或未取代的或卤素，烷基或苯基取代的或苯环稠合的饱和或不饱和的单 - 或多 - 酰基基团或烷基取代的或含有氧，硫或氮原子的未取代或甲基，乙基或卤素取代的5元或6元杂环基; R4是选自具有至多4个碳原子的烷基或氢的成员，或一组M（其中M是阳离子）。

2. 发明授权

US3951984A 3-Benzazocine compounds 失效
标题翻译： 3-苯并吖嗪化合物
公开(公告)号：US3951984A
公开(公告)日：1976-04-20
申请号：US425717
申请日：1973-12-18
申请人： Michio Kimura , Takeshi Nakajima , Toshio Atsumi , Kenji Kobayashi , Yoshiaki Takebayashi , Shigeho Inaba , Hisao Yamamoto
发明人： Michio Kimura , Takeshi Nakajima , Toshio Atsumi , Kenji Kobayashi , Yoshiaki Takebayashi , Shigeho Inaba , Hisao Yamamoto
IPC分类号： C07D471/08 , C07D221/26
CPC分类号： C07D471/08
摘要： A 3-benzazocine compound of the formula: ##SPC1##Wherein R.sub.1, R.sub.3, R.sub.4, R.sub.5 and R.sub.8 are each hydrogen or lower alkyl, R.sub.2 is hydrogen, lower alkyl or phenyl and R.sub.6 and R.sub.7 are each lower alkyl, and its pharmaceutically acceptable acid addition salts, which are useful as analgesics and can be produced by reacting a tetrahydropyridine compound of the formula: ##SPC2##Wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are each as defined above or its salt with a Lewis acid.
摘要翻译：下式的3-苯并吖嗪化合物：

3. 发明授权

US4060550A Novel n'-acylated phenyl-hydrazine and -hydrazone derivatives 失效
标题翻译：新型n {40-酰基苯基 - 肼和腙衍生物
公开(公告)号：US4060550A
公开(公告)日：1977-11-29
申请号：US651831
申请日：1976-01-23
申请人： Michio Kimura , Shigeho Inaba , Hisao Yamamoto
发明人： Michio Kimura , Shigeho Inaba , Hisao Yamamoto
IPC分类号： C07D209/60 , C07D209/70 , C07D307/54 , C07D317/66 , C07D317/68 , C07D319/18 , C07C103/133
CPC分类号： C07D317/66 , C07D209/60 , C07D209/70 , C07D307/54 , C07D317/68 , C07D319/18
摘要： Indolylacetic acid derivatives, which have excellent anti-inflammatory, antipyretic and analgesic activities, represented by the formula, ##STR1## wherein X.sub.1 and X.sub.2 are each methylene; A is an unsubstituted ethylenically unsaturated hydrocarbon chain having up to 5 carbon atoms; m is 0 or 1; n is 1 or 2; R.sub.3 is alkyl having up to 4 carbon atoms; cycloalkyl having 3 to 7 carbon atoms, unsubstituted or C.sub.1 -C.sub.4 alkyl-, nitro-, trifluoromethyl-, methylenedioxy-, ethylenedioxy- or halogen-substituted phenyl, or halogen-, C.sub.1 -C.sub.4 alkyl- or phenyl-substituted or benzene ring-condensed C.sub.3 -C.sub.7 cycloalkyl, or unsubstituted or halogen-, C.sub.1 -C.sub.4 alkyl- or phenyl-substituted or benzene ring-condensed C.sub.5 -C.sub.6 cycloalkenyl; and B is ##STR2## .
摘要翻译：吲哚乙酸衍生物，其具有优异的抗炎，解热和止痛活性，由下式表示，其中X1和X2各自为亚甲基; A是具有至多5个碳原子的未取代的烯属不饱和烃链; m为0或1; n为1或2; R3是具有至多4个碳原子的烷基; 具有3-7个碳原子的环烷基，未取代的或C 1 -C 4烷基 - ，硝基 - ，三氟甲基 - ，亚甲二氧基 - ，亚乙二氧基或卤素取代的苯基，或卤素 - ，C 1 -C 4烷基 - 或苯基取代的或苯环 - 或未取代的或卤素的，C 1 -C 4烷基或苯基取代的或苯环稠合的C 5 -C 6环烯基; 而B是

4. 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。

5. 发明授权

US4103030A Novel cyclopropylmethylamine derivatives 失效
标题翻译：新型环丙基甲胺衍生物
公开(公告)号：US4103030A
公开(公告)日：1978-07-25
申请号：US635331
申请日：1975-11-26
申请人： Atsuyuki Kojima , Yoshito Kameno , Junki Katsube , Shigeho Inaba , Hisao Yamamoto
发明人： Atsuyuki Kojima , Yoshito Kameno , Junki Katsube , Shigeho Inaba , Hisao Yamamoto
IPC分类号： A61K31/13 , A61K31/135 , A01N9/20 , A01N9/24 , C07C91/16 , C07C91/28
摘要： Novel cyclopropylmethylamine compounds of the formula: ##STR1## wherein Ar.sup.1 represents a phenyl group having one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and trifluoromethyl, of which at least one is present at the o- or m-position, Ar.sup.2 represents an unsubstituted phenyl group or a phenyl group substituted with one or more substituents selected from the group consisting of halogen and C.sub.1 -C.sub.4 alkyl, R represents hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 hydroxyalkyl and R' represents C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 hydroxyalkyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reduction of the corresponding compounds of the formula: ##STR2## wherein Ar.sup.1, Ar.sup.2, R and R' are each as defined above or by condensation of the corresponding compounds of the formula: ##STR3## wherein Ar.sup.1 and Ar.sup.2 are each as defined above and X is a conventional leaving (removable) group with amines of the formula: ##STR4## wherein R and R' are each as defined above.
摘要翻译：新的下式的环丙基甲胺化合物：其中Ar 1表示具有一个或多个选自卤素，C 1 -C 4烷基，C 1 -C 4烷氧基和三氟甲基的取代基的苯基，其中至少一个存在于或位置，Ar 2表示未取代的苯基或被一个或多个选自卤素和C 1 -C 4烷基的取代基取代的苯基，R表示氢，C 1 -C 4烷基或C 2 -C 4羟烷基， R'表示C1-C4烷基或C2-C4羟基烷基及其无毒盐，它们具有各种有用的药理活性，可以通过还原相应的下式化合物来制备：其中Ar1，Ar2，R和 R'各自如上所定义，或通过下式的相应化合物的缩合：其中Ar 1和Ar 2各自如上所定义，X是具有下式的胺的常规离去（可除去）基团：其中 R和R'各自如上所定义。

6. 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。

7. 发明授权

US4012514A Aryl ketones and production thereof 失效
标题翻译：芳基酮及其制备
公开(公告)号：US4012514A
公开(公告)日：1977-03-15
申请号：US600118
申请日：1975-07-29
申请人： Junki Katsube , Masaru Nakao , Kikuo Sasajima , Isamu Maruyama , Masaharu Takayama , Keiichi Ono , Shigenari Katayama , Yoshihiro Tanaka , Shigeho Inaba , Hisao Yamamoto
发明人： Junki Katsube , Masaru Nakao , Kikuo Sasajima , Isamu Maruyama , Masaharu Takayama , Keiichi Ono , Shigenari Katayama , Yoshihiro Tanaka , Shigeho Inaba , Hisao Yamamoto
IPC分类号： C07D211/52 , C07D295/084 , C07D295/104 , C07D295/108 , C07D233/32
CPC分类号： C07D295/108 , C07D211/52 , C07D295/092 , C07D295/104
摘要： Novel olefinic aryl ketone compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, halogen, C.sub.1-4 alkyl, or C.sub.1-4 alkoxy, R.sup.2 is hydrogen or halogen, and X is a group of the formula: ##STR2## and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reaction of an acetylenic alcohol of the formula: ##STR3##wherein R.sup.1 and R.sup.2 are each as defined above with formaldehyde and an piperidine compound of the formula: , or its non-toxic salt; reduction of the resultant acetylenic aryl alcohol; and oxidation of the resultant olefinic aryl alcohol.
摘要翻译：新颖的下式的烯属芳基酮化合物：其中R 1是氢，卤素，C 1-4烷基或C 1-4烷氧基，R 2是氢或卤素，X是下式的基团： IMAGE>及其无毒盐，其具有各种有用的药理活性，并且可以通过下式的炔属醇与下式结合产生：其中R 1和R 2各自如上所定义，其中R 1和R 2各自为甲醛，式：或，或其无毒盐; 所得炔属芳基醇的还原; 和所得烯属芳基醇的氧化。

8. 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。

9. 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。

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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