公开(公告)号：US3957783A

公开(公告)日：1976-05-18

申请号：US357889

申请日：1973-05-07

申请人： Toshiyuki Hirohashi ,  Hiromi Sato ,  Shigeho Inaba ,  Hisao Yamamoto

发明人： Toshiyuki Hirohashi ,  Hiromi Sato ,  Shigeho Inaba ,  Hisao Yamamoto

IPC分类号： C07D333/36 ,  C07D333/66 ,  C07D495/04

CPC分类号： C07D495/04 ,  C07D333/36 ,  C07D333/66

摘要： Novel thienopyrimidine derivatives which have excellent pharmacological uricosuric activity are prepared by reacting a thiophene derivative with cyanic acid or a salt thereof, urea or a reactive ester of carbamic acid. If desired, alkylated, halogenated or nitrated thienopyrimidine derivatives are produced by reacting thienopyrimidine derivatives with an alkylating, halogenating or nitrating agent, respectively.

公开(公告)号：US4001412A

公开(公告)日：1977-01-04

申请号：US575042

申请日：1975-05-06

申请人： Toshiyuki Hirohashi ,  Hiromi Sato ,  Shigeho Inaba ,  Hisao Yamamoto

发明人： Toshiyuki Hirohashi ,  Hiromi Sato ,  Shigeho Inaba ,  Hisao Yamamoto

IPC分类号： C07D495/04 ,  A61K31/495

CPC分类号： C07D495/04

摘要： 1-Substituted-1,2-dihydrothieno[2,3-d]-pyrimidin-2-ones of the formula, ##STR1## wherein R is lower alkyl or cyclopropylmethyl, R.sub.1 is halogen, lower alkyl or nitro, R.sub.2 is hydrogen or lower alkyl and R.sub.3 is hydrogen or halogen, are obtained by treating a trihaloacetamidothiophene derivative with ammonia. These compounds have excellent pharmacological activities such as uricosuric activity.

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。

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。

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。

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

公开(公告)号：US4217349A

公开(公告)日：1980-08-12

申请号：US919221

申请日：1978-06-26

申请人： Junki Katsube ,  Tsuyoshi Kobayashi ,  Katsumi Tamoto ,  Yoshiaki Takebayashi ,  Kikuo Sasajima ,  Shigeho Inaba ,  Hisao Yamamoto

发明人： Junki Katsube ,  Tsuyoshi Kobayashi ,  Katsumi Tamoto ,  Yoshiaki Takebayashi ,  Kikuo Sasajima ,  Shigeho Inaba ,  Hisao Yamamoto

IPC分类号： C07D261/20 ,  A61K31/535 ,  C07D413/06

CPC分类号： C07D261/20

摘要： Novel benzisoxazole compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, ar(C.sub.1 -C.sub.3)alkoxy or halogen or, when taken together, they form C.sub.1 -C.sub.2 alkylenedioxy, Alk is C.sub.1 -C.sub.4 alkylene and A is a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each C.sub.1 -C.sub.4 alkyl or, when taken together with the adjacent nitrogen atom, they represent a 5-6 membered nitrogen-containing heterocyclic ring which may contain any additional hetero atom and R.sub.5 is C.sub.1 -C.sub.4 alkyl or aryl), and non-toxic salts thereof, which possess various pharmaceutical activities.

摘要翻译： 新的苯并恶唑化合物，其结构式如下：其中R 1和R 2各自为氢，C 1 -C 4烷基，C 1 -C 4烷氧基，芳（C 1 -C 3）烷氧基或卤素，或者一起形成C 1 -C 2亚烷基二氧基， Alk是C 1 -C 4亚烷基，A是下式的基团：其中R 3和R 4各自是C 1 -C 4烷基，或者当与相邻的氮原子一起时，它们代表5-6元含氮的 可含有任何另外的杂原子的杂环，R 5为C 1 -C 4烷基或芳基）及其无毒盐，其具有各种药物活性。

公开(公告)号：US4080328A

公开(公告)日：1978-03-21

申请号：US484274

申请日：1974-06-28

申请人： Isamu Maruyama ,  Masaru Nakao ,  Kikuo Sasajima ,  Shigeho Inaba ,  Izumi Yanagihara ,  Hisao Yamamoto

发明人： Isamu Maruyama ,  Masaru Nakao ,  Kikuo Sasajima ,  Shigeho Inaba ,  Izumi Yanagihara ,  Hisao Yamamoto

IPC分类号： C07D401/04

摘要： Novel N-substituted heterocyclic derivatives represented by the formula, ##STR1## wherein R is hydrogen or lower alkanoyl; R.sub.1 is hydrogen, lower alkyl, lower alkoxy, halogen, nitro, trifluoromethyl, amino or N-lower alkanoylamino; R.sub.2 is hydrogen, halogen, amino or N-lower alkanoylamino; W is oxygen, sulfur, sulfinyl or sulfonyl; and Y is ##STR2## (wherein R.sub.3 is hydrogen, lower alkyl or lower alkanoyl; and R.sub.4 is hydrogen, halogen or lower alkyl), and pharmaceutically acceptable salts thereof, which have excellent anti-inflammatory, analgesic, sedative, anti-convulsive or anti-hypertensive activities.

摘要翻译： 由下式表示的新型N-取代的杂环衍生物，其中R是氢或低级烷酰基; R 1是氢，低级烷基，低级烷氧基，卤素，硝基，三氟甲基，氨基或N-低级烷酰基氨基; R2是氢，卤素，氨基或N-低级烷酰氨基; W是氧，硫，亚磺酰基或磺酰基; （其中R3为氢，低级烷基或低级烷酰基，R4为氢，卤素或低级烷基）及其药学上可接受的盐，其具有优异的抗炎，止痛，镇静作用 ，抗惊厥或抗高血压活动。

公开(公告)号：US4017624A

公开(公告)日：1977-04-12

申请号：US603240

申请日：1975-08-08

申请人： Isamu Maruyama ,  Masaru Nakao ,  Kikuo Sasajima ,  Shigeho Inaba ,  Hisao Yamamoto

发明人： Isamu Maruyama ,  Masaru Nakao ,  Kikuo Sasajima ,  Shigeho Inaba ,  Hisao Yamamoto

IPC分类号： C07D211/52 ,  C07D295/12 ,  C07D401/04

CPC分类号： C07D211/52 ,  C07D295/12

摘要： An N-(.omega.-amino)alkylaniline derivative of the formula: ##STR1## and its pharmaceutically acceptable salts, which are useful as neuroleptic agents and can be prepared by reacting a compound of the formula: ##STR2## with a compound of the formula:H--A[wherein R is hydrogen, C.sub.1 -C.sub.7 alkyl, C.sub.1 -C.sub.7 alkanoyl or aroyl, R.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.7 alkyl or C.sub.1 -C.sub.7 alkoxy,A is ##STR3## (wherein R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.7 alkyl, C.sub.1 -C.sub.7 alkoxy or trifluoromethyl), ##STR4## (wherein R.sub.2 is as defined above and R.sub.3 is hydrogen, C.sub.1 -C.sub.7 alkyl or C.sub.1 -C.sub.7 alkanoyl), ##STR5## (wherein R.sub.2 is as defined above or ##STR6## (wherein R.sub.2 and R.sub.3 are each as defined above) and n is 2, 3 or 4].

摘要翻译： 下式的N-（ω-氨基）烷基苯胺衍生物及其药学上可接受的盐，其可用作抗精神病药，并且可以通过使下式化合物与下式化合物反应来制备：＆lt; IMAGE＆gt; ：

公开(公告)号：US4010280A

公开(公告)日：1977-03-01

申请号：US509952

申请日：1974-09-27

申请人： Isamu Maruyama ,  Masaru Nakao ,  Kikuo Sasajima ,  Shigeho Inaba ,  Hisao Yamamoto

发明人： Isamu Maruyama ,  Masaru Nakao ,  Kikuo Sasajima ,  Shigeho Inaba ,  Hisao Yamamoto

IPC分类号： C07C319/20 ,  A61K31/13 ,  A61K31/135 ,  C07C20060101 ,  C07C67/00 ,  C07C217/14 ,  C07C313/00 ,  C07C315/04 ,  C07C317/28 ,  C07C323/25 ,  A01N9/20 ,  C07C91/16 ,  C07C93/06

CPC分类号： C07D409/12

摘要： A phenoxyalkylamine derivative of the formula: ##STR1## and its pharmaceutically acceptable salts, which are useful as neuroleptic agents and a process for their preparation by reacting a compound of the formula: ##STR2## with a compound of the formula: ##STR3## wherein R.sub.1 and R.sub.2 are each hydrogen, halogen, C.sub.1 -C.sub.7 alkyl or C.sub.1 -C.sub.7 alkoxy, X is oxygen, sulfur, sulfinyl or NR (in which R is hydrogen or C.sub.1 -C.sub.7 alkyl), m and n are each an integer of 2, 3 or 4, and Y and Y' are each amino or halogen but they are different from each other.