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1. 发明授权

US4535088A Propynylaminothiazole derivatives 失效
标题翻译：丙炔基氨基噻唑衍生物
公开(公告)号：US4535088A
公开(公告)日：1985-08-13
申请号：US557365
申请日：1983-12-02
申请人： Yasuo Makisumi , Akira Murabayashi , Katsuya Tawara , Yoshihachi Watanabe , Toshio Takahashi
发明人： Yasuo Makisumi , Akira Murabayashi , Katsuya Tawara , Yoshihachi Watanabe , Toshio Takahashi
IPC分类号： A01N43/78 , A61K31/425 , A61K31/426 , A61K31/428 , A61P31/04 , A61P31/10 , C07D277/20 , C07D277/42 , C07D277/56 , C07D277/82
CPC分类号： C07D277/82 , C07D277/42 , C07D277/56
摘要： New 2-(2-propynylamino)thiazole and 2-(3-iodo-2-propynylamino)thiazole derivatives having anti-microbial activity which are used as an active ingredient in anti-microbial compositions for medical and agricultural use.
摘要翻译：具有抗微生物活性的新的2-（2-丙炔基氨基）噻唑和2-（3-碘-2-丙炔基氨基）噻唑衍生物用作用于医疗和农业用途的抗微生物组合物中的活性成分。

2. 发明授权

US4576956A Iodo propargylaminoisoxazoles as fungicides 失效
标题翻译：碘代炔丙基氨基异恶唑作为杀真菌剂
公开(公告)号：US4576956A
公开(公告)日：1986-03-18
申请号：US530883
申请日：1983-09-09
申请人： Yasuo Makisumi , Akira Murabayashi , Katsuya Tawara , Yoshihachi Watanabe , Toshio Takahashi , Takao Konishi
发明人： Yasuo Makisumi , Akira Murabayashi , Katsuya Tawara , Yoshihachi Watanabe , Toshio Takahashi , Takao Konishi
IPC分类号： A01N43/80 , A61K31/42 , A61P31/04 , A61P31/10 , A61P33/02 , C07D261/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D521/00 , A61K31/41 , C07D261/12 , C07D261/20
CPC分类号： C07D231/12 , A01N43/80 , C07D233/56 , C07D249/08 , C07D261/14 , C07D413/04
摘要： New (2-propynylamino)isoxazole and (3-iodo-2-propynylamino)isoxazole derivatives having anti-microbial activity which are used as active ingredients in anti-microbial compositions for medical use, for agricultural use and also for veterinary use.
摘要翻译：新的（2-丙炔基氨基）异恶唑和具有抗微生物活性的（3-碘-2-丙炔基氨基）异恶唑衍生物，其用作医疗用途，农业用途和兽医用抗微生物组合物中的活性成分。

3. 发明授权

US4256899A Process for the production of 3-amino-5-t-butylisoxazole 失效
标题翻译：制备3-氨基-5-叔丁基异恶唑的方法
公开(公告)号：US4256899A
公开(公告)日：1981-03-17
申请号：US82405
申请日：1979-10-05
申请人： Yasuo Makisumi , Akira Murabayashi , Akira Takase , Ichiro Ishizuka , Shinzaburo Sumimoto
发明人： Yasuo Makisumi , Akira Murabayashi , Akira Takase , Ichiro Ishizuka , Shinzaburo Sumimoto
IPC分类号： C07D261/12 , C07D261/14
CPC分类号： C07D261/12 , C07D261/14
摘要： 3-Amino-5-t-butylisoxazole is prepared by reacting pivaloylacetonitrile with hydroxylamine in aqueous medium under basic conditions and treating the reaction products with an acid. The process is economical and industrial.
摘要翻译： 3-氨基-5-叔丁基异恶唑通过在碱性条件下在水介质中使新戊酰基乙腈与羟胺反应并用酸处理反应产物来制备。这个过程是经济实惠的。

4. 发明授权

US4200757A Process for the production of 3-aminoisoxazoles 失效
标题翻译：生产3-氨基异恶唑的方法
公开(公告)号：US4200757A
公开(公告)日：1980-04-29
申请号：US912252
申请日：1978-06-05
申请人： Yasuo Makisumi , Akira Murabayashi , Takashi Sasatani
发明人： Yasuo Makisumi , Akira Murabayashi , Takashi Sasatani
IPC分类号： C07D261/14 , C07D261/08
CPC分类号： C07D261/14
摘要： 3-Aminoisoxazoles of the formula: ##STR1## (wherein R is C.sub.1 -C.sub.6 alkyl, phenyl or halo-phenyl) are prepared by reacting a .beta.-ketonitrile of the formula:R--CO--CH.sub.2 CN(wherein R is as defined above) with a compound of the formula:HY(wherein Y is C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio) in the presence of an acid in a solvent to give an iminium salt of the formula: ##STR2## (wherein X is the residue of said acid; R and Y are each as defined above) and further reacting the iminium salt with hydroxylamine in an inert solvent.
摘要翻译：下式的3-氨基异恶唑：其中R为C1-C6烷基，苯基或卤素 - 苯基）是通过使下式所示的β-甲酯与下式反应来制备的：式中R-CO-CH 2 CN（其中R如上定义）与下式的化合物HY（其中Y是C 1 -C 6烷氧基或C 1 -C 6烷硫基）在酸的存在下在溶剂中反应，得到下式的亚铵盐：其中X是所述酸; R和Y各自如上所定义），并进一步使亚胺盐与羟胺在惰性溶剂中反应。

5. 发明授权

US5091539A Azolyl cycloalkanol derivatives and agricultural fungicides 失效
标题翻译：氨基醇环己酮衍生物和农业防腐剂
公开(公告)号：US5091539A
公开(公告)日：1992-02-25
申请号：US531347
申请日：1990-05-31
申请人： Yasuo Makisumi , Akira Murabayashi , Takayuki Hatta , Takeo Ishiguro
发明人： Yasuo Makisumi , Akira Murabayashi , Takayuki Hatta , Takeo Ishiguro
IPC分类号： A01N43/50 , A01N43/653 , C07D233/60 , C07D249/08 , C07D333/28 , C07D521/00
CPC分类号： C07D231/12 , A01N43/50 , A01N43/653 , C07D233/56 , C07D249/08 , C07D333/28
摘要： Novel 1-substituted -2-imidazolyl (or 1,2,3-triazolyl)cyclohexanols or cycloheptanols having anti-fungal activity against wide range of agricultural fungi with vapor effect.
摘要翻译：对具有蒸汽作用的广泛农业真菌具有抗真菌活性的新型1-取代-2-咪唑基（或1,2,3-三唑基）环己醇或环庚醇。

6. 发明授权

US4183856A Process for the production of urea derivatives 失效
标题翻译：尿素衍生物生产工艺
公开(公告)号：US4183856A
公开(公告)日：1980-01-15
申请号：US895105
申请日：1978-04-10
申请人： Yasuo Makisumi , Takashi Sasatani , Akira Murabayashi
发明人： Yasuo Makisumi , Takashi Sasatani , Akira Murabayashi
IPC分类号： C07D275/02 , C07D213/75 , C07D261/14 , C07D263/48 , C07D275/03 , C07D277/20 , C07D277/38 , C07D277/46 , C07D277/48 , C07D277/82
CPC分类号： C07D213/75 , C07D261/14 , C07D275/03 , C07D277/48 , C07D277/82
摘要： Urea derivatives of the formula ##STR1## (wherein Ar represents a residue of 5- or 6-membered heteroaromatic ring; R represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; R.sup.1 represents a C.sub.1 -C.sub.6 alkyl group; and R.sup.2 represents a C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.1 -C.sub.6 alkoxy group) are produced by reacting an amine of the formulaAr--NH--R(wherein Ar and R have the significance given above) with a carbamoyl halogenide of the formula ##STR2## (wherein X represents a halogen atom, and R.sup.1 and R.sup.2 have the significance given above) in the presence of a Lewis acid in an inert solvent.
摘要翻译：下式的脲衍生物（其中Ar表示5或6元杂芳环的残基; R表示氢原子或C1-C6烷基; R1表示C1-C6烷基; R2表示 C 1 -C 6烷基，C 2 -C 6烯基或C 1 -C 6烷氧基）通过使式Ar-NH-R（其中Ar和R具有上述含义）具有下式的氨基甲酰卤化物：图像（其中X表示卤原子，R1和R2具有上述含义）在路易斯酸存在下在惰性溶剂中反应。

7. 发明授权

US4256640A Tetrahydrothiopyrano[2,3-b]indole derivatives 失效
标题翻译：四氢噻喃并[2,3-b]吲哚衍生物
公开(公告)号：US4256640A
公开(公告)日：1981-03-17
申请号：US39382
申请日：1979-05-15
申请人： Yasuo Makisumi , Susumu Takada , Takashi Sasatani , Natsuki Ishizuka
发明人： Yasuo Makisumi , Susumu Takada , Takashi Sasatani , Natsuki Ishizuka
IPC分类号： A61K31/40 , A61K31/445 , A61P25/04 , A61P29/00 , C07D209/30 , C07D495/04
CPC分类号： C07D495/04 , C07D209/30
摘要： Tetrahydrothiopyrano[2,3-b]indole derivative represented by the formula I: ##STR1## wherein R.sup.1 is hydrogen, alkyl, hydroxyalkyl, alkenyl, aralkyl, aryl, --COR.sup.5 (wherein R.sup.5 is alkyl, alkenyl, aryl or alkoxy) or ##STR2## (wherein Y is alkylene, oxoalkylene, hydroxyalkylene and R.sup.6 and R.sup.7 are each hydrogen or alkyl): R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen, alkyl, hydroxyalkyl, alkenyl, aralkyl, aryl or dialkylaminoalkyl or ##STR3## is pyrrolidino, piperidino, piperazino, 4-alkylpiperazino, 4-arylpiperazino or morpholino; R.sup.4 is hydrogen or alkyl; A is methylene, alkylmethylene, ethylene, alkylethylene; X is hydrogen or one or two groups selected from the group consisting of halogen, alkyl, alkoxy, hydroxy and halogenoalkyl; and n is an integer of 0 to 2 and its pharmaceutically acceptacle salts; synthesized from 2-propargylthioindole or 2-(4-hydroxy-2-butynylthio)-indole; useful as analgesic and anti-inflammatory agent.
摘要翻译：由式I表示的四氢噻喃[2,3-b]吲哚衍生物：其中R 1是氢，烷基，羟烷基，烯基，芳烷基，芳基，-COR 5（其中R 5是烷基，烯基，芳基或烷氧基）或（其中Y是亚烷基，氧代亚烷基，羟基亚烷基，R 6和R 7各自是氢或烷基）：R 2是氢或烷基; R 3是氢，烷基，羟基烷基，烯基，芳烷基，芳基或二烷基氨基烷基，或者是吡咯烷子基，哌啶子基，哌嗪子基，4-烷基哌嗪基，4-芳基哌嗪基或吗啉代; R4是氢或烷基; A是亚甲基，烷基亚甲基，亚乙基，烷基亚乙基; X是氢或选自卤素，烷基，烷氧基，羟基和卤代烷基的一个或两个基团; n为0〜2的整数及其药学上可接受的盐; 由2-炔丙基硫吲哚或2-（4-羟基-2-丁炔硫基） - 吲哚合成; 用作镇痛和抗炎剂。

8. 发明授权

US4910318A Tetrahydrothiopyrano(3,2-b)-indole derivatives 失效
标题翻译：四氢噻喃（3,2-b） - 吲哚衍生物
公开(公告)号：US4910318A
公开(公告)日：1990-03-20
申请号：US633686
申请日：1984-07-25
申请人： Yasuo Makisumi , Takashi Sasatani
发明人： Yasuo Makisumi , Takashi Sasatani
IPC分类号： A61K31/40 , A61K31/445 , A61K31/495 , A61P25/04 , A61P29/00 , C07D209/30 , C07D495/04
CPC分类号： C07D495/04 , C07D209/30
摘要： Tetrahydrothiopyrano[3,2-b]indole derivatives represented by the formula I: ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, phenyl-C.sub.1-4 alkyl, C.sub.2-5 alkanoyl, or ##STR2## wherein Y is C.sub.1-4 alkylene or C.sub.1-4 oxoalkylene and R.sup.5 and R.sup.6 each is hydrogen or C.sub.1-4 alkyl;R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.3-6 cycloalkyl;R.sup.3 is hydrogen, C.sub.1-4 alkyl or ##STR3## wherein Y, R.sup.5 and R.sup.6 each is as defined above; or ##STR4## is pyrrolidino, piperdinyl, piperazinyl, 4-C.sub.1-4 alkylpiperazinyl or morpholino;R.sup.4 is hydrogen or C.sub.1-4 alkyl; andn is 0 or an integer of 1 or 2and the pharmaceutically acceptable salts being useful as analgesic and anti-inflammatory agents as well as psychoanaleptic and nootropic drug.
摘要翻译：由式I表示的四氢噻喃并[3,2-b]吲哚衍生物：其中R 1是氢，C 1-4烷基，C 2-4烯基，C 2-4炔基，苯基-C 1-4烷基，C 2-5 烷酰基或者其中Y是C 1-4亚烷基或C 1-4亚氧基亚烷基，R 5和R 6各自是氢或C 1-4烷基; R2是氢，C1-4烷基或C3-6环烷基; R 3是氢，C 1-4烷基或者其中Y，R 5和R 6各自如上所定义; 或是吡咯烷子基，哌啶基，哌嗪基，4-C 1-4烷基哌嗪基或吗啉代; R4是氢或C1-4烷基; 并且n为0或1或2的整数，并且其药学上可接受的盐可用作镇痛和抗炎剂以及精神无菌和益智药。

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