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1. 发明授权

US3923794A Novel propenylamine derivatives and process for the production thereof 失效
标题翻译：新型丙烯基胺衍生物及其制备方法
公开(公告)号：US3923794A
公开(公告)日：1975-12-02
申请号：US48740174
申请日：1974-07-10
申请人： SUMITOMO CHEMICAL CO
发明人： MARUYAMA ISAMU , NAKAO MASARU , SASAJIMA KIKUO , YANAGIHARA IZUMI , INABA SHIGEHO , YAMAMOTO HISAO
IPC分类号： C07D471/10
摘要： Novel propenylamine derivatives represented by the general formula

WHEREIN R1, R2, X and A are as defined hereinafter, and pharmaceutically acceptable salts thereof, useful as antipsychotic tranquillizing, analgesic, anti-convulsive, antihypertensive and anti-inflammatory agents are disclosed. The propenylamine derivatives of this invention can be prepared by reacting the corresponding propenyl halide with an amine derivative.
摘要翻译：公开了由通式为R 1，R 2，X和A表示的新型丙烯基胺衍生物及其药学上可接受的盐作为抗精神病药，镇静剂，镇痛药，抗惊厥药，抗高血压药和抗炎剂，。本发明的丙烯胺衍生物可以通过使相应的丙烯酰卤与胺衍生物反应来制备。

2. 发明授权

US3917598A N-(ortho-alkoxy-phenyl)-N{40 -anilino-propyl-piperazines 失效
标题翻译： N-（邻烷氧基 - 苯基）-N {40-苯胺基 - 丙基 - 哌嗪
公开(公告)号：US3917598A
公开(公告)日：1975-11-04
申请号：US43982774
申请日：1974-02-05
申请人： SUMITOMO CHEMICAL CO
发明人： MARUYAMA ISAMU , NAKAO MASARU , SASAJIMA KIKUO , INABA SHIGEHO , YAMAMOTO HISAO
IPC分类号： C07D295/12 , C07D211/52 , C07D295/13 , C07D401/04
CPC分类号： C07D295/13 , C07D211/52
摘要： An N-( omega -amino)alkylaniline derivative of the formula:

AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS, WHICH ARE USEFUL AS NEUROLEPTIC AGENTS ARE PREPARED BY REACTING A COMPOUND OF THE FORMULA:

WITH A COMPOUND OF THE FORMULA:
摘要翻译：下式的N-（ω-氨基）烷基苯胺衍生物：

3. 发明授权

US3925387A 1-{8 {65 -O-Amino-p-halophenyl-oxy, thio or sulfinyl)-propyl{9 -4-(alkoxy or halo phenyl)piperazines 失效
标题翻译： 1- {8- {6-（N-氨基 - 对卤代苯氧基，硫代或亚磺酰基） - 丙基{9-4（烷氧基或卤代苯基）哌嗪
公开(公告)号：US3925387A
公开(公告)日：1975-12-09
申请号：US31210672
申请日：1972-12-04
申请人： SUMITOMO CHEMICAL CO
发明人： MARUYAMA ISAMU , NAKAO MASARU , SASAJIMA KIKUO , ONO KEIICHI , TAKAYAMA MASAHARU , KATAYAMA SHIGENARI , TANAKA YOSHIHIRO , YANAGIHARA IZUMI , INABA SHIGEHO , YAMAMOTO HISAO
IPC分类号： C07D295/08 , A61K31/415 , A61K31/435 , A61K31/495 , A61P9/12 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/20 , C07D211/52 , C07D295/092 , C07D401/04 , C07D471/10 , C07D295/12
CPC分类号： C07D295/088 , C07D211/52
摘要： WHEREIN Y is as defined above.

WHEREIN R1, R2, R3, Z and m are as defined above and X is halogen atom, with a compound of the formula,

(WHEREIN R4 is hydrogen or halogen atom or lower alkyl or lower alkoxy group; R5 is hydrogen atom or lower alkyl or lower alkanoyl group; R6 is hydrogen or halogen atom or lower alkyl or lower alkoxy group; R7 is hydroxy, lower alkoxy or lower alkanoyloxy group; R8 is hydrogen or halogen atom or lower alkyl, lower alkoxy or trifluoromethyl group; R9 is hydrogen atom or lower alkyl or lower alkanoyl group; R10 is hydrogen or halogen atom or lower alkyl or lower alkoxy group; and n is 0, 1 or 2); and m is an integer from 2 to 5, and pharmaceutically acceptable salts thereof, which have excellent anti-psychotonic, analgesic, anti-inflammatory and anti-hypertensive activities, are produced by reacting a compound of the formula,

WHEREIN R1 and R2 are each hydrogen atom or lower alkyl, lower alkanoyl or aroyl group; R3 is hydrogen or halogen atom or lower alkyl or lower alkoxy group; Z is oxygen or sulfur atom or sulfinyl or sulfonyl group; Y is

Novel alkylamine derivatives represented by the formula,
摘要翻译：由式WHEREIN R1和R2表示的新型烷基胺衍生物各自为氢原子或低级烷基，低级烷酰基或芳酰基; R3是氢或卤素原子或低级烷基或低级烷氧基; Z是氧或硫原子或亚磺酰基或磺酰基; Y为（其中R4为氢或卤素原子或低级烷基或低级烷氧基; R5为氢原子或低级烷基或低级烷酰基; R6为氢或卤素原子或低级烷基或低级烷氧基; R7为羟基，低级烷氧基或低级烷酰氧基; R8为氢或卤素原子或低级烷基，低级烷氧基或三氟甲基; R9为氢原子或低级烷基或低级烷酰基; R10为氢或卤素原子或低级烷基或低级烷氧基; n为 0，1或2）; m为2〜5的整数，及其药学上可接受的盐，其具有优异的抗心理，镇痛，抗炎和抗高血压活性，是通过使下式的化合物，即WHEREIN R1，R2，R3 ，Z和m如上所定义，X是卤素原子，与下式的化合物，其中Y如上定义。

4. 发明授权

US3907812A Butyrophenone derivatives 失效
标题翻译：丁酰苯衍生物
公开(公告)号：US3907812A
公开(公告)日：1975-09-23
申请号：US32913073
申请日：1973-02-02
申请人： SUMITOMO CHEMICAL CO
发明人： YAMAMOTO HISAO , OKAMOTO TADASHI , SASAJIMA KIKUO , NAKAO MASARU , MARUYAMA ISAMU , KATAYAMA SHIGENARI
IPC分类号： C07D211/52
CPC分类号： C07D211/52 , Y10S514/96
摘要： A novel process for preparing central nervous system active butyrophenone derivatives in which gamma piperidinobutyrophenone derivatives of the formula,

wherein R1 is hydrogen, halogen, amino, acylamino, alkylamino or N-acylalkylamino; R2 is hydrogen or halogen; R3 is hydrogen or unsubstituted or alkyl-, alkoxy-, halogen- or trifluoromethylsubstituted phenyl; and R4 is hydrogen or hydroxyl, can be prepared by reacting an indole derivative of the formula,

wherein R2, R3 and R4 are as defined above, and R5 and R6 are each independently hydrogen or alkyl, with an oxidizing agent to yield an o-acylamino- gamma -piperidinobutyrophenone derivative of the formula,

wherein R2, R3, R4, R5 and R6 are as defined above, and further, if necessary, hydrolyzing the product to yield an o-amino- gamma -piperidinobutyrophenone derivative of the formula,

wherein R2, R3, R4 and R5 are as defined above, and further diazotizing, if desired, in case R5 is hydrogen, the obtained oamino- gamma -piperidinobutyrophenone derivative and subsequently decomposing the resultant diazonium compound to replace the diazonium group by hydrogen or halogen. Among the butyrophenone derivatives thus obtained, those in which R1 is halogen, amino, acylamino, alkylamino or N-acylalkylamino are novel compounds.
摘要翻译：一种用于制备中枢神经系统活性丁酰苯衍生物的新方法，其中式为CO-CH 2 -CH 2 -CH 2 -YGLE R 1的γ-哌啶基丁酰苯衍生物，其中R 1为氢，卤素，氨基，酰氨基，烷基氨基或N-酰基烷基氨基; R2是氢或卤素; R3是氢或未取代的或烷基，烷氧基，卤素或三氟甲基取代的苯基; 并且R 4是氢或羟基，可以通过使下式的吲哚衍生物CH2-CH2-CH2-ANGLE R6 | R5（其中R2，R3和R4如上定义）与R5和R6各自独立地是氢或烷基与氧化剂反应得到下式的邻酰基氨基-γ-哌啶基丁酰苯衍生物，其中R2，R3，R4，R5和R6的定义如上所定义，CO- 此外，如果需要，水解产物以产生下式的邻氨基-γ-哌啶基丁酰苯衍生物，其中R2，R3，R4和R5如上所定义，进一步重氮化，如果需要，在R5为氢的情况下，得到的邻氨基-γ-哌啶基丁酰苯衍生物，随后分解所得重氮化合物以用氢或卤素代替重氮基团。在由此获得的丁酰苯衍生物中，R 1为卤素，氨基，酰氨基，烷基氨基或N-酰基烷基氨基的那些是新化合物。

5. 发明授权

US3922266A Aryl ketones and production thereof 失效
标题翻译：芳基酮及其制备
公开(公告)号：US3922266A
公开(公告)日：1975-11-25
申请号：US31602672
申请日：1972-12-18
申请人： SUMITOMO CHEMICAL CO
发明人： KATSUBE JUNKI , NAKAO MASARU , SASAJIMA KIKUO , MARUYAMA ISAMU , TAKAYAMA MASAHARU , ONO KEIICHI , KATAYAMA SHIGENARI , TANAKA YOSHIHIRO , INABA SHIGEHO , YAMAMOTO HISAO
IPC分类号： C07D211/52 , C07D295/084 , C07D295/104 , C07D295/108 , C09B23/00 , C07D295/00
CPC分类号： C07D295/108 , C07D211/52 , C07D295/092 , C07D295/104
摘要： A process for preparing aryl ketones of the formula:

FROM A COMPOUND OF THE FORMULA:

THROUGH A COMPOUND OF THE FORMULA:

A COMPOUND OF THE FORMULA:

AND A COMPOUND OF THE FORMULA:

THE SAID ARYL KETONES BEING (I) being useful as central nervous system depressants and the intermediary compounds (II), (III), and (IV) showing some pharmacological activities.
摘要翻译：一种制备下式的芳基酮的方法：

6. 发明授权

US3903091A 1,2,3,4-Tetrahydroisoquinoline derivatives 失效
标题翻译： 1,2,3,4-四氢异喹啉衍生物
公开(公告)号：US3903091A
公开(公告)日：1975-09-02
申请号：US25354772
申请日：1972-05-15
申请人： SUMITOMO CHEMICAL CO
发明人： YAMAMOTO HISAO , NAKAO MASARU , SASAJIMA KIKUO , MARUYAMA ISAMU , KATAYAMA SHIGENARI
IPC分类号： C07D217/04 , C07D35/36
CPC分类号： C07D217/04
摘要： 1,2,3,4-Tetrahydroisoquinoline derivatives having excellent psychotropic activity and represented by the formula,

WHEREIN

R1 is hydrogen, halogen, C1-C3 alkyl, C1-C3 alkoxy or trifluoromethyl; R2 is hydrogen, halogen, amino, C1-C3 alkylamino, N-(C1-C3 alkyl)acylamino or acylamino; R3 is hydrogen, halogen, C1-C3 alkyl, C1-C3 alkoxy, hydroxy or trifluoromethyl, and processes for the production of the same.
摘要翻译： 1,2,3,4-四氢异喹啉衍生物具有优良的精神活性，由下式表示，其中R1是氢，卤素，C1-C3烷基，C1-C3烷氧基或三氟甲基; R2是氢，卤素，氨基，C1-C3烷基氨基，N-（C1-C3烷基）酰氨基或酰基氨基; R3是氢，卤素，C1-C3烷基，C1-C3烷氧基，羟基或三氟甲基，以及其制备方法。

7. 发明授权

US3901898A 8-aroylalkyl-1,3,8-triazaspiro (4,5)+0 decanes 失效
标题翻译： 8-AROYLALKYL-1,3,8-TRIAZASPIRO（4,5）+0 DECANES
公开(公告)号：US3901898A
公开(公告)日：1975-08-26
申请号：US41612073
申请日：1973-11-15
申请人： SUMITOMO CHEMICAL CO
发明人： YAMAMOTO HISAO , NAKAO MASARU , SASAJIMA KIKUO , MARUYAMA ISAMU , KATAYAMA SHIGENARI
IPC分类号： C07D211/26
摘要： Aminophenylketone derivatives having excellent psychotropic activities and represented by the formula,

WHEREIN R1 is hydrogen, C1-C4 alkyl or aryl; R is hydrogen or a group having the formula, -COR2 (wherein R2 is hydrogen, C1-C4 alkyl or aryl); R3 is hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy or trifluoromethyl; R4 is hydrogen, C1-C4 alkyl or C1-C4 alkanoyl; R5 is C1-C4 alkyl or aryl; X is carbonyl or methylene; and Z is a group having the formula,

(wherein R6 and R7 are each hydrogen, C1-C4 alkyl, aryl or aralkyl and R6 and R7 may form bivalent C2-C5 alkylene).

8. 发明授权

US3890323A Phenylketone derivatives 失效
标题翻译：苯乙酮衍生物
公开(公告)号：US3890323A
公开(公告)日：1975-06-17
申请号：US36946173
申请日：1973-06-13
申请人： SUMITOMO CHEMICAL CO
发明人： YAMAMOTO HISAO , INABA SHIGEHO , SASAJIMA KIKUO , NAKAO MASARU , MARUYAMA ISAMU , ONO KEIICHI , KATAYAMA SHIGENARI
IPC分类号： C07D295/12 , A61K31/445 , A61K31/451 , A61P9/12 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/20 , C07C49/76 , C07D211/14 , C07D211/52 , C07D217/04 , C07D241/04 , C07D295/108 , C07D295/13 , C07D471/10 , C07D51/70
CPC分类号： C07D295/108 , C07D211/52 , C07D295/13
摘要： Phenylketone derivatives of the formula:

WHICH CAN BE PREPARED BY REACTING A KETONE OF THE FORMULA:

WITH A COMPOUND OF THE FORMULA:

9. 发明专利

CH635841A5 SPIROAMINDERIVATE, VERFAHREN ZU IHRER HERSTELLUNG UND DIESE ENTHALTENDE ARZNEIMITTEL. 未知
公开(公告)号：CH635841A5
公开(公告)日：1983-04-29
申请号：CH566278
申请日：1978-05-24
申请人： SUMITOMO CHEMICAL CO
发明人： ONO KEIICHI , SASAJIMA KIKUO , KATSUBE JUNKI , YAMAMOTO HISAO
IPC分类号： A61K31/435 , A61P9/08 , A61P25/00 , C07D471/10 , C07D471/20 , A61K31/445

10. 发明专利

FI60390C 未知
公开(公告)号：FI60390C
公开(公告)日：1982-01-11
申请号：FI760415
申请日：1976-02-19
申请人： SUMITOMO CHEMICAL CO
发明人： SASAJIMA KIKUO , ONO KEIICHI , YAMAMOTO HISAO
IPC分类号： C07D211/32 , C07D211/44 , C07D211/52 , C07D295/108 , C07D401/04 , C07D471/10
摘要： Butyrophenone compounds having excellent psychotropic activity and represented by the formula: wherein Z is defined hereinbelow.

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