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1. 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。

2. 发明授权

US4012515A Aryl ketones and production thereof 失效
标题翻译：芳基酮及其制备
公开(公告)号：US4012515A
公开(公告)日：1977-03-15
申请号：US600119
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 , C07D295/108
CPC分类号： C07D295/108 , C07D211/52 , C07D295/092
摘要： Novel olefinic aryl ketone compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, halogen, C.sub.1.sub.-4 alkyl, or C.sub.1.sub.-4 alkoxy, R.sup.2 is hydrogen or halogen, and R.sup.3 and R.sup.4 are each hydrogen, halogen, C.sub.1.sub.-4 alkyl or trifluoromethyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reaction of an acetylenic alcohol of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are each as defined above, with formaldehyde and an amine of the formula: ##STR3## wherein R.sup.3 and R.sup.4 are each as defined above; 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，R 3和R 4各自是氢，卤素，C 1-4烷基或三氟甲基及其无毒盐，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其中的甲醛和胺反应制备下式的炔属醇：其中R1和R2各自如上定义式：其中R 3和R 4各自如上所定义; 所得炔属芳基醇的还原; 和所得烯属芳基醇的氧化。

3. 发明授权

US3979390A Butyrophenone derivatives and production thereof 失效
标题翻译：丁酰苯衍生物及其生产
公开(公告)号：US3979390A
公开(公告)日：1976-09-07
申请号：US341858
申请日：1973-03-16
申请人： Kikuo Sasajima , Keiichi Ono , Masaru Nakao , Isamu Maruyama , Masaharu Takayama , Shigenari Katayama , Junki Katsube , Shigeho Inaba , Hisao Yamamoto
发明人： Kikuo Sasajima , Keiichi Ono , Masaru Nakao , Isamu Maruyama , Masaharu Takayama , Shigenari Katayama , Junki Katsube , Shigeho Inaba , Hisao Yamamoto
IPC分类号： C07D295/10 , A61K31/445 , A61K31/451 , A61K31/452 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/20 , C07C45/46 , C07C49/80 , C07D211/52 , C07D215/14 , C07D217/04 , C07D295/108 , C07D317/16 , C07D471/10
CPC分类号： C07D295/108 , C07C45/46 , C07C49/80 , C07D211/52 , C07D217/04 , C07D317/16
摘要： A process for producing butyrophenone derivatives of the formula: ##EQU1## which comprises reacting a compound of the formula: ##SPC1##With an amine of the formulaH-W(wherein Ar represents a group of either one of the formulas: ##SPC2##Z is a secondary amino group and W is the residue of an amine excluding a hydrogen atom therefrom). The said butyrophenone derivatives and their salts exhibit a variety of beneficial pharmacological activities including a central and autonomic nervous system depressing activity.
摘要翻译：制备下式的丁酰苯酮衍生物的方法：O-PARALE-Ar-C-CH 2 CH 2 CH 2 -Z，其包括使下式化合物：

4. 发明授权

US4065565A Acylhydrazones and anti-psychotic compositions thereof 失效
标题翻译：酰腙及其抗精神病药组合物
公开(公告)号：US4065565A
公开(公告)日：1977-12-27
申请号：US603813
申请日：1975-08-12
申请人： Kikuo Sasajima , Keiichi Ono , Masaru Nakao , Isamu Maruyama , Shigenari Katayama , Shigeho Inaba , Hisao Yamamoto
发明人： Kikuo Sasajima , Keiichi Ono , Masaru Nakao , Isamu Maruyama , Shigenari Katayama , Shigeho Inaba , Hisao Yamamoto
IPC分类号： C07D295/12 , A61K31/15 , A61K31/445 , A61K31/451 , A61P9/12 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/18 , A61P25/20 , C07D211/00 , C07D211/52 , C07D235/00 , C07D241/00 , C07D241/04
CPC分类号： C07D211/52
摘要： Acylhydrazone compounds having excellent pyschotropic activity which are represented by the formula: ##STR1## wherein Z is selected from the groups having the formulas: ##STR2## wherein n is an integer of from 0 to 2 and R.sup.1 -R.sup.12 are as defined hereinbelow.
摘要翻译：其中Z选自具有下式的基团：其中n为0至2的整数，R 1 -R 12的整数为1，其中Z为选自下列基团的酰基腙化合物：如下文所定义。

5. 发明授权

US4009173A Butyrophenone derivatives 失效
标题翻译：丁酰苯衍生物
公开(公告)号：US4009173A
公开(公告)日：1977-02-22
申请号：US617730
申请日：1975-09-29
申请人： Kikuo Sasajima , Masaru Nakao , Isamu Maruyama , Keiichi Ono , Shigenari Katayama , Shigeho Inaba , Hisao Yamamoto
发明人： Kikuo Sasajima , Masaru Nakao , Isamu Maruyama , Keiichi Ono , Shigenari Katayama , Shigeho Inaba , Hisao Yamamoto
IPC分类号： C07D211/64 , C07D403/04
CPC分类号： C07D211/64
摘要： Novel butyrophenone derivatives of the formula: ##STR1## wherein R.sub.1 represents a hydroxyl group or ##STR2## (wherein R.sub.6 and R.sub.7 are each a hydrogen atom or a lower alkyl group or, when taken together with the adjacent nitrogen atom, may form a heterocyclic group), R.sub.2 represents an optionally substituted phenyl group or ##STR3## (wherein R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl group or, when taken together with the adjacent nitrogen atom, may form a heterocyclic group), R.sub.4 represents a hydrogen atom, a lower alkyl group or an optionally substituted phenyl group, R.sub.5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or a trifluoromethyl group, R.sub.10 represents a hydrogen atom or an acyl group represented by R.sub.3 CO- (wherein R.sub.3 is a hydrogen atom, a lower alkyl group or an optionally substituted phenyl group) and Z represents two hydrogen atoms or an oxygen atom, provided that when Z is an oxygen atom and R.sub.1 is ##STR4## R.sub.10 can not be a hydrogen atom, and their acid addition salts, which are useful as central and autonomic nervous system depressants.
摘要翻译：下式的新型丁基苯酚衍生物：其中R 1表示羟基或（其中R 6和R 7各自为氢原子或低级烷基，或者当与相邻的氮原子一起形成杂环时基团），R 2表示任选取代的苯基或者其中R 8和R 9各自为氢原子或低级烷基，或者当与相邻的氮原子一起形成杂环基时，R 4表示氢原子，低级烷基或任选取代的苯基，R 5表示氢原子，卤素原子，低级烷基，低级烷氧基或三氟甲基，R 10表示氢原子或R 3 CO 3表示的酰基 - （其中R 3是氢原子，低级烷基或任选取代的苯基），Z代表两个氢原子或氧原子，条件是当Z是氧原子且R 1不能是氢原子，和它们的酸加成盐，其可用作中枢神经系统抑制剂和自主神经系统抑制剂。

6. 发明授权

US4080328A N-substituted heterocyclic derivatives and preparation thereof 失效
标题翻译： N-取代的杂环衍生物及其制备
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。

7. 发明授权

US4017624A N-(.omega.-Amino)alkylaniline derivatives 失效
标题翻译： N - （{107 - 氨基）烷基苯胺衍生物
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; ：

8. 发明授权

US4010280A Phenoxyalkylamine derivatives and preparation thereof 失效
标题翻译：苯甲酰胺衍生物及其制备方法
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.

9. 发明授权

US3951986A Novel 2-propanol derivatives and preparation thereof 失效
标题翻译：新型2-丙醇衍生物及其制备方法
公开(公告)号：US3951986A
公开(公告)日：1976-04-20
申请号：US370693
申请日：1973-06-18
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 , C07D295/092 , C07D403/12
CPC分类号： C07D295/088 , C07D211/52 , C07D403/12 , Y10S514/821
摘要： 2-Propanol derivatives of the formula: ##SPC1##And their pharmaceutically acceptable acid addition salts, which are useful as medicaments and can be produced by reacting a compound of the formula: A-CH.sub.2 -Z with a compound of the formula: A'-H [wherein R is hydrogen or lower alkanoyl; R.sub.1 is hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; W is oxygen, sulfur, sulfinyl or sulfonyl; Y is a group of either one of the formulae: ##SPC2##(wherein R.sub.2 is hydrogen, halogen, lower alkyl or lower alkoxy and R.sub.3 is hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl); A and A' are each a group of either one of the formulae: ##SPC3##(wherein R.sub.1, W and Y are each as defined above), provided that A and A' are different each other; and Z is a group of either one of the formulae: ##EQU1## (wherein X is halogen, alkylsulfonyloxy or arylsulfonyloxy and R is as defined above)].
摘要翻译：下式的2-丙醇衍生物：

10. 发明授权

US3960873A 1-Phenylthiopropyl-4-hydroxy-4-phenyl piperidines 失效
标题翻译： 1-苯基硫丙基-4-羟基-4-苯基哌啶
公开(公告)号：US3960873A
公开(公告)日：1976-06-01
申请号：US481796
申请日：1974-06-21
申请人： Isamu Maruyama , Hisao Yamamoto , Masaru Nakao , Shigeru Sakai , Kikuo Sasajima , Sumio Kitagawa , Shigeho Inaba
发明人： Isamu Maruyama , Hisao Yamamoto , Masaru Nakao , Shigeru Sakai , Kikuo Sasajima , Sumio Kitagawa , Shigeho Inaba
IPC分类号： C07D295/092 , C07D211/52
CPC分类号： C07D295/088
摘要： Novel N-substituted heterocyclic derivatives represented by the formula, ##SPC1##Wherein R.sub.1 is hydrogen atom, lower alkyl, lower alkoxy, nitro, halogen or trifluoromethyl group; R.sub.2 is hydrogen atom or lower alkyl group; X is sulfur atom, sulfinyl or sulfonyl group; Y is ##EQU1## group (wherein R.sub.3 is phenyl or substituted phenyl group; R.sub.4 is hydrogen atom, hydroxy, lower alkyl, lower alkoxy, lower alkanoyl, lower alkanoyloxy, carbamoyl, N-(lower alkyl)-carbamoyl or N,N-di(lower akyl)-carbamoyl group; R.sub.5 is hydrogen atom, morpholino, pyrrolidinyl, piperidinyl, hexamethylenimino, lower alkyl, cyclo(lower alkyl), cyclo(lower alkyl)-(lower alkyl), hydroxy-(lower alkyl), (lower alkoxy)-(lower alkyl), phenyl or substituted phenyl group; k is 0 or 1 and m is 0, 1 or 2); and n is 3 or 4, and pharmaceutically acceptable salts thereof, which have excellent tranquillizing, anti-psychotonic, anti-emotional, anti-convulsive, anti-psychosis, sedative, analgesic or anti-hypertensive activities.
摘要翻译：由式WHEREIN R1表示的新型N-取代的杂环衍生物是氢原子，低级烷基，低级烷氧基，硝基，卤素或三氟甲基; R2是氢原子或低级烷基; X是硫原子，亚磺酰基或磺酰基; Y是|| - （CH2）kN-（CH2）m-R3， - （CH2）kC-（CH2）m-R5或| R4 | -CH = C-（CH2）m-R5基（其中R3是苯基或取代的苯基; R 4是氢原子，羟基，低级烷基，低级烷氧基，低级烷酰基，低级烷酰氧基，氨基甲酰基，N-（低级烷基） - 氨基甲酰基或N，N-二（低级烷基） - 氨基甲酰基; 氢原子，吗啉代，吡咯烷基，哌啶基，六亚甲基亚氨基，低级烷基，环（低级烷基），环（低级烷基） - （低级烷基），羟基 - （低级烷基），（低级烷氧基） - （低级烷基）取代苯基; k为0或1，m为0,1或2）; 和n为3或4，及其药学上可接受的盐，其具有优异的镇静，抗心律失常，抗感觉，抗惊厥，抗精神病，镇静，止痛或抗高血压活性。

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