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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。
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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。
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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:< IMAGE> :
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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.
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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:
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公开(公告)号:US3953446A
公开(公告)日:1976-04-27
申请号:US494885
申请日:1974-08-05
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: C07D239/82 , C07D209/10 , C07D209/42 , C07D401/06 , C07D405/06 , C07D409/06 , C07D405/04
CPC分类号: C07C247/00 , C07D209/42
摘要: Quinazoline derivatives which have anti-inflammatory, antiviral, uricosuric activities are prepared by reacting an indole-2-carbonylazide derivative with an oxidizing agent under mild conditions.
摘要翻译: 具有抗炎,抗病毒,尿酸营养活性的喹唑啉衍生物通过在温和条件下使吲哚-2-羰基叠氮化物衍生物与氧化剂反应来制备。
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公开(公告)号:US3953441A
公开(公告)日:1976-04-27
申请号:US150841
申请日:1971-06-07
IPC分类号: C07D211/70 , C07D221/26
CPC分类号: C07D221/26 , C07D211/70
摘要: A novel process for preparing 2-benzoylalkylbenzomorphan derivatives and salts thereof, represented by the formula ##SPC1##Wherein n, R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification. The process comprises reacting a pyridinium derivative of the formula, ##SPC2##Wherein X is a halogen atom and Y' is an ethylenedioxy group; with a Grignard reagent of the formula, ##SPC3##Wherein R' is a hydrogen atom or a C.sub.1 -C.sub.3 alkoxy group and Z is a halogen atom, to yield a 1,2-dihydropyridine derivative of the formula; ##SPC4##And then reducing the said 1,2-dihydropyridine derivative to give a 1,2,5,6-tetrahydropyridine derivative of the formula, ##SPC5##Wherein Y is an oxygen atom or an ethylenedioxy group, and further cyclizing the obtained 1,2,5,6-tetrahydropyridine derivative.
摘要翻译: 由式WHEREIN N,R,R1,R2,R3和R4表示的用于制备2-苯甲酰基烷基苯并喃衍生物及其盐的新方法如本说明书中所定义。 该方法包括使下式的吡啶鎓衍生物WHEREIN X是卤素原子,Y'是亚乙二氧基; 与下式的格利雅试剂,其中R'是氢原子或C1-C3烷氧基,Z是卤素原子,得到下式的1,2-二氢吡啶衍生物; 然后减少所得的1,2-二氢吡啶衍生物,得到本发明的1,2,5,6-四氢吡啶衍生物,其中Y是氧原子或亚乙二氧基,进一步环化得到的1,2,5,6-四氢吡啶衍生物, 6-四氢吡啶衍生物。
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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:
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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:
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公开(公告)号:US20110084425A1
公开(公告)日:2011-04-14
申请号:US12971720
申请日:2010-12-17
申请人: Hisao Yamamoto
发明人: Hisao Yamamoto
CPC分类号: D04H1/74 , B60R13/0225 , D01D5/34 , D01F8/14 , D04H1/435 , D04H1/4382 , D04H1/541 , D04H1/55 , Y10T442/641
摘要: The present invention provides an automotive inner ceiling material difficult to deform at a high temperature. Sheath-core type conjugate polyester fibers are prepared. The sheath is a heat fusible component. The core is a non heat fusible component. The sheath is made of copolyester which comprises acid units made of terephthalic acid and diol unites made of ethylene glycol and 1,4-butanediol. The conjugate fibers and the main fibers of polyester are mixed and provided in a card machine to be opened and accumulated to obtain a fibrous web. The fibrous web is heated to melt the sheaths, which are thereafter solidified to bind the fibers to obtain a non woven fabric. The nonwoven fabric is heat-treated at a temperature equal to or higher than the melting point of the sheath. Immediately thereafter, the nonwoven fabric is heat-molded between a pair of a mold plates. During the heat-molding process, the inner temperature is maintained at 100˜130° C. for 60 seconds to obtain the ceiling material.
摘要翻译: 本发明提供一种难以在高温下变形的汽车内顶板材料。 制备护芯型共轭聚酯纤维。 护套是热熔组件。 核心是非热熔组件。 鞘由共聚酯制成,其包含由对苯二甲酸和由乙二醇和1,4-丁二醇制成的二醇单元制成的酸单元。 将复合纤维和聚酯的主纤维混合并提供在卡片机中以打开和聚集以获得纤维网。 纤维网被加热以熔化护套,然后将其固化以结合纤维以获得无纺织物。 无纺布在等于或高于护套熔点的温度下进行热处理。 此后,立即将非织造布在一对模板之间进行热压成形。 在热成型过程中,将内部温度保持在100〜130℃,持续60秒,得到天花板材料。
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