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1. 发明授权

US4880827A Pyrrolidine derivatives having inhibitory action for proline specific endopepidase 失效
标题翻译：对脯氨酸特异性内肽酶具有抑制作用的吡咯烷衍生物
公开(公告)号：US4880827A
公开(公告)日：1989-11-14
申请号：US25664
申请日：1987-03-13
申请人： Katsumi Tamoto , Renzo Ohuchi , Keiichi Ono
发明人： Katsumi Tamoto , Renzo Ohuchi , Keiichi Ono
IPC分类号： C07D207/08
CPC分类号： C07D207/08
摘要： Pyrrolidine derivatives having inhibitory action for proline-specific endopeptidase which are useful for anti-amnestic agent. The disclosed pyrrolidine derivatives as well as their acid addition salts can be administered orally or parenterally in the form of conventional pharmaceutical preparations. For instance, they can be administered orally in the form of conventional solid pharmaceutical preparations such as tablets, capsules, syrups and suspensions. Alternatively, they can be administered parenterally by injection in the form of conventional liquid pharmaceutical preparations such as solutions, emulsions, suspensions, etc. Also, they may be directly applied to rectum in the form of suppository. Further, the preparations may contain physiologically acceptable carriers, excipients, activators, binding agents, stabilizers, etc. In the case of injections, physiologically acceptable buffers, solubilizing agents or isotonic agents may be incorporated therein. Methods of production are also disclosed.
摘要翻译：具有抑制脯氨酸特异性内肽酶的作用的吡咯烷衍生物可用于抗惊厥剂。公开的吡咯烷衍生物及其酸加成盐可以以常规药物制剂的形式口服或肠胃外给药。例如，它们可以以常规固体药物制剂如片剂，胶囊，糖浆和悬浮液的形式口服给药。或者，它们可以以常规液体药物制剂如溶液，乳剂，悬浮液等的形式通过注射肠胃外给药。此外，它们可以以栓剂的形式直接施用于直肠。此外，制剂可以含有生理上可接受的载体，赋形剂，活化剂，结合剂，稳定剂等。在注射的情况下，可以加入生理上可接受的缓冲剂，增溶剂或等渗剂。还公开了生产方法。

2. 发明授权

US5051444A Pyrrolidine derivatives as anti-amnesia agents 失效
标题翻译：吡咯烷衍生物作为抗遗忘剂
公开(公告)号：US5051444A
公开(公告)日：1991-09-24
申请号：US408562
申请日：1989-09-18
申请人： Katsumi Tamoto , Renzo Ohuchi , Keiichi Ono
发明人： Katsumi Tamoto , Renzo Ohuchi , Keiichi Ono
IPC分类号： C07D207/08
CPC分类号： C07D207/08
摘要： The present invention relates to pyrrolidine derivatives of the formula ##STR1## wherein R.sup.1 and R.sup.2 are defined as herein. The compounds are useful as anti-amnestic agent.

3. 发明授权

US4495103A Preparation of optically active 4-demethoxydaunomycinone 失效
标题翻译：光学活性4-脱甲氧基多霉素酮的制备
公开(公告)号：US4495103A
公开(公告)日：1985-01-22
申请号：US471338
申请日：1983-03-02
申请人： Shiro Terashima , Katsumi Tamoto , Masamichi Sugimori
发明人： Shiro Terashima , Katsumi Tamoto , Masamichi Sugimori
IPC分类号： C07C43/178 , C07C50/36 , C07C167/02
CPC分类号： C07C43/1786
摘要： A process for preparing optically active 4-demethoxy-7-deoxydaunomycinone which comprises reacting a racemic mixture of the .alpha.-hydroxyketone of the formula: ##STR1## with an optical isomer of the .alpha.-glycol of the formula: ##STR2## wherein R is a group of the formula: ##STR3## and X is a halogen atom or a lower alkyl group to give a diastereomeric mixture of the acetal of the formula: ##STR4## .
摘要翻译：一种制备光学活性4-脱甲氧基-7-脱氧果香霉素酮的方法，其包括将下式的α-羟基酮的外消旋混合物与下式的α-二醇的旋光异构体反应：（II）其中R是下式的基团：其中X是卤素原子或低级烷基，得到下式的缩醛的非对映体混合物：（III）。

4. 发明授权

US4217349A Benzisoxazole derivatives 失效
标题翻译：苯并异恶唑衍生物
公开(公告)号：US4217349A
公开(公告)日：1980-08-12
申请号：US919221
申请日：1978-06-26
申请人： Junki Katsube , Tsuyoshi Kobayashi , Katsumi Tamoto , Yoshiaki Takebayashi , Kikuo Sasajima , Shigeho Inaba , Hisao Yamamoto
发明人： Junki Katsube , Tsuyoshi Kobayashi , Katsumi Tamoto , Yoshiaki Takebayashi , Kikuo Sasajima , Shigeho Inaba , Hisao Yamamoto
IPC分类号： C07D261/20 , A61K31/535 , C07D413/06
CPC分类号： C07D261/20
摘要： Novel benzisoxazole compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, ar(C.sub.1 -C.sub.3)alkoxy or halogen or, when taken together, they form C.sub.1 -C.sub.2 alkylenedioxy, Alk is C.sub.1 -C.sub.4 alkylene and A is a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each C.sub.1 -C.sub.4 alkyl or, when taken together with the adjacent nitrogen atom, they represent a 5-6 membered nitrogen-containing heterocyclic ring which may contain any additional hetero atom and R.sub.5 is C.sub.1 -C.sub.4 alkyl or aryl), and non-toxic salts thereof, which possess various pharmaceutical activities.
摘要翻译：新的苯并恶唑化合物，其结构式如下：其中R 1和R 2各自为氢，C 1 -C 4烷基，C 1 -C 4烷氧基，芳（C 1 -C 3）烷氧基或卤素，或者一起形成C 1 -C 2亚烷基二氧基， Alk是C 1 -C 4亚烷基，A是下式的基团：其中R 3和R 4各自是C 1 -C 4烷基，或者当与相邻的氮原子一起时，它们代表5-6元含氮的可含有任何另外的杂原子的杂环，R 5为C 1 -C 4烷基或芳基）及其无毒盐，其具有各种药物活性。

5. 发明授权

US5231179A Heterocyclic compounds and their production 失效
标题翻译：杂环化合物及其生产
公开(公告)号：US5231179A
公开(公告)日：1993-07-27
申请号：US684488
申请日：1991-04-12
申请人： Shiro Terashima , Yoshio Ito , Takeo Kawabata , Kunikazu Sakai , Tamejiro Hiyama , Yoshikazu Kimura , Makoto Sunagawa , Katsumi Tamoto , Akira Sasaki
发明人： Shiro Terashima , Yoshio Ito , Takeo Kawabata , Kunikazu Sakai , Tamejiro Hiyama , Yoshikazu Kimura , Makoto Sunagawa , Katsumi Tamoto , Akira Sasaki
IPC分类号： C07D205/08 , C07D233/32 , C07D263/26 , C07D263/52 , C07D263/58 , C07D403/06 , C07D413/06
CPC分类号： C07D263/52 , C07D205/08 , C07D233/32 , C07D263/26 , C07D263/58 , C07D403/06 , C07D413/06
摘要： A compound of the formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each a hydrogen atom, a lower alkyl group, an ar(lower)alkyl group or an aryl group, or R.sub.1 and R.sub.2 may be combined together to form a lower alkylene group and/or R.sub.3 and R.sub.4 are combined together to form a lower alkylene group, or R.sub.1, R.sub.2, R.sub.3 and R.sub.4 may be combined together to form an o-phenylene group, X is a halogen atom and Y is an oxygen atom or a nitrogen atom substituted with lower alkyl or aryl, which is useful as an intermediate in the synthesis of 1.beta.-methylcarbapenem compounds valuable as antibiotics.
摘要翻译：下式的化合物：其中R 1，R 2，R 3和R 4各自为氢原子，低级烷基，芳（低级）烷基或芳基，或者R 1和R 2可以组合一起形成低级亚烷基和/或R 3和R 4结合在一起形成低级亚烷基，或者，R 1，R 2，R 3和R 4可以组合在一起形成邻亚苯基，X是卤素原子，Y 是氧原子或被低级烷基或芳基取代的氮原子，其可用作合成作为抗生素有价值的1β-甲基碳青霉烯化合物的中间体。

6. 发明授权

US4122176A 3-(Piperazinoalkyl)-benz-2,1-isoxazoles 失效
标题翻译： 3-（哌嗪基烷基） - 苯并-2,1 - 异恶唑
公开(公告)号：US4122176A
公开(公告)日：1978-10-24
申请号：US755139
申请日：1976-12-29
申请人： Junki Katsube , Tsuyoshi Kobayashi , Katsumi Tamoto , Yoshiaki Takebayashi , Kikuo Sasajima , Shigeho Inaba , Hisao Yamamoto
发明人： Junki Katsube , Tsuyoshi Kobayashi , Katsumi Tamoto , Yoshiaki Takebayashi , Kikuo Sasajima , Shigeho Inaba , Hisao Yamamoto
IPC分类号： C07D261/20 , A61K31/495 , C07D413/06 , C07D413/14
CPC分类号： C07D261/20 , Y10S514/826
摘要： Novel benzisoxazole compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, ar(C.sub.1 14 C.sub.3) alkoxy or halogen or, when taken together, they form C.sub.1 -C.sub.2 alkylenedioxy, Alk is C.sub.1 -C.sub.4 alkylene and A is a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each C.sub.1 -C.sub.4 alkyl or, when taken together with the adjacent nitrogen atom, they represent a 5-6 membered nitrogen-containing heterocyclic ring which may contain any additional hetero atom and R.sub.5 is C.sub.1 -C.sub.4 alkyl or aryl), and non-toxic salts thereof, which possess various pharmaceutical activities.
摘要翻译：下式的新型苯并异恶唑化合物：其中R 1和R 2各自为氢，C 1 -C 4烷基，C 1 -C 4烷氧基，芳（C 11 43 C 3）烷氧基或卤素，或者当它们一起形成C 1 -C 2亚烷基二氧基，Alk 是C 1 -C 4亚烷基，A是下式的基团：其中R 3和R 4各自是C 1 -C 4烷基，或者当与相邻的氮原子一起时，它们代表5-6元含氮杂环可以含有任何另外的杂原子的环，R 5是C 1 -C 4烷基或芳基）及其无毒盐，其具有各种药物活性。

7. 发明授权

US4501700A Preparation of optically active 4-demethoxydaunomycinone 失效
标题翻译：光学活性4-脱甲氧基多霉素酮的制备
公开(公告)号：US4501700A
公开(公告)日：1985-02-26
申请号：US471354
申请日：1983-03-02
申请人： Shiro Terashima , Katsumi Tamoto , Kenji Koga
发明人： Shiro Terashima , Katsumi Tamoto , Kenji Koga
IPC分类号： C07C45/67 , C07C43/178 , C07C45/00 , C07C46/00 , C07C49/577 , C07C50/38 , C07C67/00 , C07C50/36
CPC分类号： C07C43/1786
摘要： A process for preparing racemic 4-demethoxy-7-deoxydaunomycinone which comprises methylating an optically active .alpha.-hydroxyketone to give the corresponding methylated product of either one of the formulas: ##STR1## and reacting the latter with an acid to give a racemate of the .alpha.-hydroxyketone of the formula: ##STR2## .
摘要翻译：一种制备外消旋4-脱甲氧基-7-脱氧果香霉素酮的方法，其包括使光学活性的α-羟基酮甲基化，得到下式之一的相应的甲基化产物：（VI）和（VIB），并使后者与酸反应，得到下式的α-羟基酮的外消旋物：（I）。

8. 发明授权

US4343801A 1,2,4-Triazine derivatives, and their production and use 失效
标题翻译： 1,2,4-三嗪衍生物及其生产和使用
公开(公告)号：US4343801A
公开(公告)日：1982-08-10
申请号：US212442
申请日：1980-12-03
申请人： Hideo Agui , Katsumi Tamoto , Shunji Aono , Takao Okuda
发明人： Hideo Agui , Katsumi Tamoto , Shunji Aono , Takao Okuda
IPC分类号： C07D401/04 , C07D409/14 , A01N43/10 , A01N43/64 , C07D401/14
CPC分类号： C07D401/04 , C07D409/14
摘要： A compound of the formula: ##STR1## wherein Ar is a phenyl group substituted with halogen, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 alkylthio, C.sub.1 -C.sub.8 alkylsulfonyl, nitro, trihalomethyl, cyano, C.sub.1 -C.sub.8 alkylamino, di(C.sub.1 -C.sub.8)-alkylamino, amino, hydroxyl, phenyl and/or phenoxy, a naphthyl group or a thienyl group optionally substituted with halogen, which is useful as an antifungal agent.
摘要翻译：下式的化合物，其中Ar是被卤素取代的苯基，C1-C8烷基，C1-C8烷氧基，C1-C8烷硫基，C1-C8烷基磺酰基，硝基，三卤代甲基，氰基，C1-C8烷基氨基，二（C1-C8） - 烷基氨基，氨基，羟基，苯基和/或苯氧基，萘基或任选被卤素取代的噻吩基，其可用作抗真菌剂。

9. 发明授权

US4069230A Preparation of indole derivatives 失效
标题翻译：吲哚衍生物的制备
公开(公告)号：US4069230A
公开(公告)日：1978-01-17
申请号：US691777
申请日：1976-06-01
申请人： Shigeaki Morooka , Katsumi Tamoto , Akira Matuura
发明人： Shigeaki Morooka , Katsumi Tamoto , Akira Matuura
IPC分类号： C07D209/40 , C07D209/04 , C07D491/056
CPC分类号： C07D209/04
摘要： An improved process for preparing indole derivatives of the formula, ##STR1## wherein R.sub.1 and R.sub.2 each are hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, nitro, cyano or trifluoromethyl, or when taken together, form methylenedioxy; R.sub.3 is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, nitro, cyano or dimethylamino; and R.sub.4 is hydrogen or halogen, which comprises cyclizing a compound of the formula, ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined above, with an acidic condensing agent.The indole derivatives of the formula (I) mentioned above are useful as a key intermediate for the preparation of benzodiazepines, which are useful as tranquilizers, muscle relaxants and the like.
摘要翻译：制备下式的吲哚衍生物的改进方法：其中R 1和R 2各自为氢，卤素，C 1 -C 3烷基，C 1 -C 3烷氧基，硝基，氰基或三氟甲基，或当一起形成亚甲二氧基 ; R3是氢，卤素，C1-C3烷基，C1-C3烷氧基，硝基，氰基或二甲基氨基; 并且R 4是氢或卤素，其包括使式III化合物，其中R 1，R 2，R 3和R 4如上所定义的化合物与酸性缩合剂环化。

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