公开(公告)号：US4260774A

公开(公告)日：1981-04-07

申请号：US51741

申请日：1979-06-25

申请人： Toshio Atsumi ,  Yoshiaki Takebayashi ,  Yuzo Tarumi ,  Hisao Yamamoto

发明人： Toshio Atsumi ,  Yoshiaki Takebayashi ,  Yuzo Tarumi ,  Hisao Yamamoto

IPC分类号： C07D233/90

CPC分类号： C07D233/90

摘要： There are provided compounds of the formula: ##STR1## wherein R is an adamantyl group, or a phenyl group unsubstituted or substituted with a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halogen atom, a nitro group, a cyano group, a methylenedioxy group or an acetamido group, useful as anti-transplanted-tumor agents and immunosuppressants.

摘要翻译： 提供下式的化合物：其中R是金刚烷基，或未取代或被低级烷基，低级烷氧基，低级烷硫基，卤原子，硝基， 氰基，亚甲二氧基或乙酰氨基，可用作抗移植肿瘤剂和免疫抑制剂。

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。

公开(公告)号：US4148796A

公开(公告)日：1979-04-10

申请号：US388561

申请日：1973-08-15

申请人： Hisao Yamamoto ,  Masaru Nakao ,  Kikuo Sasajima ,  Isamu Maruyama ,  Shigenari Katayama

发明人： Hisao Yamamoto ,  Masaru Nakao ,  Kikuo Sasajima ,  Isamu Maruyama ,  Shigenari Katayama

IPC分类号： C07D211/48 ,  C07D401/06 ,  C07D401/04 ,  C07D211/50

CPC分类号： C07D401/06 ,  C07D211/48

摘要： Novel .gamma.-piperidinobutyrophenone derivatives of the formula, ##STR1## wherein R.sup.1 is halogen, amino, alkanoylamino, alkylamino or N-(alkanoyl)alkylamino;R.sup.2 is hydrogen or halogen, provided that when R.sup.1 is halogen, R.sup.2 must be halogen; andZ is a piperidino group having the formula (A), ##STR2## (wherein each of R.sub.a and R.sub.b is hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; R.sup.3 is hydrogen or hydroxyl; and n is 1 or 2), or a piperidino group having the formula (B), ##STR3## (wherein R.sub.c is hydrogen or lower alkyl; and each of R.sub.d and R.sub.e is hydrogen, halogen, lower alkyl or lower alkoxy), provided that when R.sup.1 is amino and R.sup.2 is hydrogen, Z cannot be represented by the formula (A), and their pharmaceutically acceptable acid addition salts, which are useful as psychotropic, neuroleptic or analgesic agents.

摘要翻译： 其中R1是卤素，氨基，烷酰基氨基，烷基氨基或N-（烷酰基）烷基氨基的新颖的γ-哌啶基丁酰苯衍生物， R2是氢或卤素，条件是当R1是卤素时，R2必须是卤素; Z为具有式（A），（A）的哌啶子基，其中R a和R b各自为氢，卤素，低级烷基，低级烷氧基或三氟甲基; R 3为氢或羟基; n为1或 2）或具有式（B）的哌啶子基，其中R c是氢或低级烷基;并且R d和R e各自是氢，卤素，低级烷基或低级烷氧基），条件是当 R1是氨基，R2是氢，Z不能由式（A）表示，它们的药学上可接受的酸加成盐可用作精神药物，精神抑制剂或止痛剂。

公开(公告)号：US4125731A

公开(公告)日：1978-11-14

申请号：US748539

申请日：1976-12-08

申请人： Akihiko Sugie ,  Hiromi Shimomura ,  Junki Katsube ,  Hisao Yamamoto

发明人： Akihiko Sugie ,  Hiromi Shimomura ,  Junki Katsube ,  Hisao Yamamoto

IPC分类号： C07C17/32 ,  C07C33/38 ,  C07C405/00 ,  C07D307/93 ,  C07D309/12 ,  C07C69/76

CPC分类号： C07D309/12 ,  C07C17/32 ,  C07C33/38 ,  C07C405/00 ,  C07D307/93 ,  C07C2102/08 ,  Y10S514/927

摘要： Novel indan compounds of the formula ##STR1## wherein A and X are each ethylene or vinylene; B is C.sub.2-4 alkylene; R and R.sub.2 are each hydrogen or C.sub.1-4 alkyl; R.sub.1 is C.sub.1-8 alkyl;

摘要翻译： 式IMA的新型茚满化合物，其中A和X各自为亚乙烯基或亚乙烯基; B是C 2-4亚烷基; R和R 2各自为氢或C 1-4烷基; R1是C1-8烷基; 及其无毒盐，其可用作抗溃疡剂，胃分泌物抑制剂和假体。

公开(公告)号：US4110376A

公开(公告)日：1978-08-29

申请号：US605012

申请日：1975-08-15

申请人： Atsuyuki Kojima ,  Junki Katsube ,  Yoshito Kameno ,  Shigeho Inaba ,  Hisao Yamamoto

发明人： Atsuyuki Kojima ,  Junki Katsube ,  Yoshito Kameno ,  Shigeho Inaba ,  Hisao Yamamoto

IPC分类号： A61K31/135 ,  A61K31/13 ,  C07C20060101 ,  C07C67/00 ,  C07C209/00 ,  C07C209/50 ,  C07C211/26 ,  C07C87/32

CPC分类号： C07D401/12

摘要： Novel cyclopropylmethylamine compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen or halogen and R.sup.3 is hydrogen or methyl, 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 R.sup.1, R.sup.2 and R.sup.3 are each as defined above or their non-toxic salts, or by condensation of the corresponding compounds of the formula: ##STR3## wherein R.sup.1 and R.sup.2 are each defined above, and X is a conventional interchangeable group such as halogen or sulfonyloxy with methylamine or dimethylamine.

摘要翻译： 下式的新型环丙基甲胺化合物：其中R 1和R 2各自为氢或卤素，R 3为氢或甲基，及其无毒盐，其具有各种有用的药理活性，可通过还原相应化合物 其中R 1，R 2和R 3各自如上所定义，或其无毒盐，或通过下式的相应化合物的缩合：其中R 1和R 2各自如上所定义，X为 常规的可互换基团如卤素或磺酰氧基与甲胺或二甲胺。

公开(公告)号：US4085210A

公开(公告)日：1978-04-18

申请号：US646908

申请日：1976-01-06

申请人： Junki Katsube ,  Atsuyuki Kojima ,  Makoto Sunagawa ,  Yoshinori Takashima ,  Yoshito Kameno ,  Hisao Yamamoto

发明人： Junki Katsube ,  Atsuyuki Kojima ,  Makoto Sunagawa ,  Yoshinori Takashima ,  Yoshito Kameno ,  Hisao Yamamoto

IPC分类号： C07D265/30 ,  C07D267/10 ,  C07D409/06 ,  A61K31/535 ,  C07D405/06

CPC分类号： C07D265/30 ,  C07D267/10

摘要： Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, aryl-(C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, polyhalo(C.sub.2 -C.sub.4)alkyl or hydroxy(C.sub.2 -C.sub.4)alkyl, A represents straight or branched C.sub.2 -C.sub.4 alkylene, B represents a divalent radical selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 --O--, --CH.sub.2 --S--, --S-- and --O--, >D --E-- represents a trivalent radical selected from the group consisting of >CH--CH.sub.2 -- and >C.dbd.CH-- and C.sub.1 and C.sub.2 each represent 1,2-phenylene optionally substituted with one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy, and their non-toxic salts, which are useful as antidepressants and can be produced by various methods.

摘要翻译： 式中：R1代表氢或C1-C4烷基，R2代表氢，C1-C4烷基，C3-C5烯基，C3-C5炔基，芳基 - （C1-C4）烷基，（C3 -C 6）环烷基（C 1 -C 4）烷基，多卤代（C 2 -C 4）烷基或羟基（C 2 -C 4）烷基，A表示直链或支链C 2 -C 4亚烷基，B表示选自-CH 2 -CH 2 - ， - CH = CH-， -CH 2 -O-，-CH 2 -S-，-S-和-O-，> D-E-代表选自下组的三价基团：CH -CH 2 - 和> C = CH-且C 1和C 2各自表示任选被一个或多个选自卤素，C 1 -C 4烷基和C 1 -C 4烷氧基的取代基取代的1,2-亚苯基，它们的无毒 盐，其可用作抗抑郁药并且可以通过各种方法制备。

公开(公告)号：US4083981A

公开(公告)日：1978-04-11

申请号：US773936

申请日：1977-03-03

申请人： Hisao Yamamoto ,  Toshiya Inukai ,  Yoshihiko Koga

发明人： Hisao Yamamoto ,  Toshiya Inukai ,  Yoshihiko Koga

IPC分类号： C07D209/28 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61K31/435 ,  A61K31/445 ,  A61K31/485 ,  A61P25/04 ,  C07D211/64 ,  C07D221/28

CPC分类号： A61K31/485 ,  A61K31/435 ,  A61K31/445

摘要： An analgetic composition which comprises, as an active ingredient, a therapeutically effective amount of a synergistic mixture of an indole-3-acetic acid derivative of the formula, ##STR1## wherein R is a halobenzoyl, piperonylcyl or cinnamoyl group and R.sub.1 is a 5-methoxy or 5,6-methylenedioxy group; and a narcotic or anti-narcotic analgesic selected from the group consisting of a compound of the formula, ##STR2## wherein R.sub.2 and R.sub.3 are each a C.sub.1 - C.sub.3 alkyl group and R.sub.4 is a 4-(4-fluorophenyl)-4-oxobutyl, cyclopropylmethyl or 3-methyl-2-butenyl group; a compound of the formula, ##STR3## wherein R.sub.5 is a hydrogen atom or a C.sub.1 - C.sub.3 alkyl group; a compound of the formula, ##STR4## and a compound of the formula, ##STR5## wherein R.sub.6 is a C.sub.1 - C.sub.3 alkyl group; and a pharmaceutically acceptable carrier or diluent and its preparation and a method of obtaining analgesia which comprises administering the same to a patient.

摘要翻译： 一种止痛组合物，其包含作为活性成分的治疗有效量的下式的吲哚-3-乙酸衍生物，其中R是卤代苯甲酰基，胡烷基或肉桂酰基的吲哚-3-乙酸衍生物，R 1为5 - 甲氧基或5,6-亚甲二氧基; 以及选自由下式化合物组成的组的麻醉或抗麻醉止痛剂，其中R2和R3各自为C1-C3烷基，R4为4-（4-氟苯基）-4-氧代丁基 ，环丙基甲基或3-甲基-2-丁烯基; 下式的化合物，其中R 5是氢原子或C 1 -C 3烷基; 下式的化合物和下式的化合物，其中R 6是C 1 -C 3烷基; 和药学上可接受的载体或稀释剂及其制备方法和获得镇痛的方法，其包括将其施用于患者。

公开(公告)号：US4075346A

公开(公告)日：1978-02-21

申请号：US705840

申请日：1976-07-16

申请人： Kikuo Sasajima ,  Keiichi Ono ,  Yasuo Motoike ,  Shigeho Inaba ,  Hisao Yamamoto

发明人： Kikuo Sasajima ,  Keiichi Ono ,  Yasuo Motoike ,  Shigeho Inaba ,  Hisao Yamamoto

IPC分类号： C07D211/08 ,  C07D211/14 ,  C07D211/18 ,  C07D211/36 ,  C07D211/48 ,  C07D211/52 ,  C07D295/04 ,  C07D295/108 ,  C07D295/12 ,  C07D307/33 ,  C07D317/16 ,  C07D401/04 ,  C07D471/10 ,  C07D211/28 ,  A61K31/445

CPC分类号： C07D295/108 ,  C07C205/45 ,  C07D211/14 ,  C07D211/18 ,  C07D211/52 ,  C07D307/33 ,  C07D317/16

摘要： Novel compounds of the formula: ##STR1## wherein R is a hydrogen or fluorine atom, W is an oxygen atom or an ethylenedioxy or ethylenedithio group and Z is a certain secondary amino group, which are useful as central nervous system depressants, can be prepared by the reaction of a compound of the formula: ##STR2## wherein X is a halogen atom and R and W are each as defined above with a secondary amine of the formula: H--Z wherein Z is as defined above, in case of W being ethylenedioxy or ethylenedithio, optionally followed by hydrolysis and can be reduced to give a compound of the formula: ##STR3## wherein R and Z are each as defined above, which are useful as antipsychotic and/or analgesic agents.

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

公开(公告)号：US4044003A

公开(公告)日：1977-08-23

申请号：US598621

申请日：1975-07-24

申请人： Kikuo Ishizumi ,  Kazuo Mori ,  Tadashi Okamoto ,  Takeshi Akase ,  Takahiro Izumi ,  Mitsuhiro Akatsu ,  Yoshiharu Kume ,  Shigeho Inaba ,  Hisao Yamamoto

发明人： Kikuo Ishizumi ,  Kazuo Mori ,  Tadashi Okamoto ,  Takeshi Akase ,  Takahiro Izumi ,  Mitsuhiro Akatsu ,  Yoshiharu Kume ,  Shigeho Inaba ,  Hisao Yamamoto

IPC分类号： C07D243/16

CPC分类号： C07D243/16

摘要： 1,4-Benzodiazepine derivatives of the formula, ##STR1## wherein R.sub.1 is hydrogen, a lower alkyl, a haloalkyl, a cycloalkylalkyl, an alkoxyalkyl, an acyloxyalkyl, an alkylthioalkyl, an alkylaminoalkyl, a dialkylaminoalkyl, a hydroxyalkyl, carbamoyl, or an N-alkylcarbamoyl; R.sub.2 is hydrogen or a lower alkyl; X is hydrogen, a halogen, nitro, or trifluoromethyl; A is a group of the formula, ##STR2## (wherein Y and Z each represent hydrogen, a halogen, a lower alkyl, or nitro) and a salt thereof, are prepared by reacting a 1,4-benzodiazepin-2-one compound of the formula, ##STR3## wherein R.sub.1, R.sub.2, X, Y and Z are the same as defined above, with diborane in an inert solvent.

摘要翻译： 其中R1是氢，低级烷基，卤代烷基，环烷基烷基，烷氧基烷基，酰氧基烷基，烷基硫代烷基，烷基氨基烷基，二烷基氨基烷基，羟基烷基，氨基甲酰基或 N-烷基氨基甲酰基; R2是氢或低级烷基; X是氢，卤素，硝基或三氟甲基; A是通过使1,4-苯并二氮杂-2-酮化合物（其中Y和Z各自表示氢，卤素，低级烷基或硝基）及其盐的式 其中R1，R2，X，Y和Z与上述定义相同，与乙硼烷在惰性溶剂中反应。