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1. 发明授权

US4963582A Macrolide compounds, their preparation and their use 失效
标题翻译：大环内酯类化合物，其制备及其用途
公开(公告)号：US4963582A
公开(公告)日：1990-10-16
申请号：US30217
申请日：1987-03-24
申请人： Kazuo Sato , Toshiaki Yanai , Takao Kinoto , Keiji Tanaka , Akira Nishida , Toshimitsu Toyama , Bruno Frei , Anthony O'Sullivan
发明人： Kazuo Sato , Toshiaki Yanai , Takao Kinoto , Keiji Tanaka , Akira Nishida , Toshimitsu Toyama , Bruno Frei , Anthony O'Sullivan
IPC分类号： A01N43/90 , A01N47/06 , A01P5/00 , A01P7/02 , A01P7/04 , A61K31/365 , C07D493/22 , C07H19/01
CPC分类号： C07D493/22 , A01N43/90 , A01N47/06 , C07H19/01
摘要： Compounds having a 16-membered macrolide ring, and related to the milbemycins and avermectins, with substituents at positions 5, 13, 25 and optionally also 23, have acaricidal, insecticidal and anthelmintic properties. They are useful for treating various pests in plants and animals.

2. 发明授权

US5405867A Macrolide compounds, their preparation and their use 失效
标题翻译：大环内酯类化合物，其制备及其用途
公开(公告)号：US5405867A
公开(公告)日：1995-04-11
申请号：US133776
申请日：1993-10-08
申请人： Kazuo Sato , Toshiaki Yanai , Takao Kinoto , Keiji Tanaka , Akira Nishida , Toshimitsu Toyama , Bruno Frei , Anthony O'Sullivan
发明人： Kazuo Sato , Toshiaki Yanai , Takao Kinoto , Keiji Tanaka , Akira Nishida , Toshimitsu Toyama , Bruno Frei , Anthony O'Sullivan
IPC分类号： A01N43/90 , A01N47/06 , A01P5/00 , A01P7/02 , A01P7/04 , A61K31/365 , C07D493/22 , C07H19/01 , C07D313/00
CPC分类号： C07D493/22 , A01N43/90 , A01N47/06 , C07H19/01
摘要： Compounds having a 16-membered macrolide ring, and related to the milbemycins and avermectins, with substituents at positions 5.13, 25 and optionally also 23, have acaricidal, insecticidal and anthelmintic properties. They are useful for treating various pests in plants and animals.
摘要翻译：具有16位大环内酯环，与米尔倍霉素和阿凡曼菌素相关的化合物，其具有位置5.13,25和任选地23的取代基具有杀螨，杀虫和驱虫性质。它们可用于处理植物和动物中的各种害虫。

3. 发明授权

US4603201A Process for producing antifungal oyridazinone derivatives 失效
标题翻译：抗真菌哒嗪酮衍生物的制备方法
公开(公告)号：US4603201A
公开(公告)日：1986-07-29
申请号：US724800
申请日：1985-04-19
申请人： Hideo Takeshiba , Takao Kinoto , Teruomi Jojima
发明人： Hideo Takeshiba , Takao Kinoto , Teruomi Jojima
IPC分类号： A01N43/58 , C07C45/46 , C07C45/63 , C07C51/347 , C07C51/363 , C07C59/88 , C07D237/04 , C07D237/14 , C07D401/12 , C07D237/06 , A61K31/50
CPC分类号： C07D401/12 , A01N43/58 , C07C323/00 , C07C45/46 , C07C45/63 , C07C51/347 , C07C51/363 , C07C59/88 , C07D237/04 , C07D237/14
摘要： Compounds of formula (I): ##STR1## [wherein R.sup.1 and R.sup.3 represent hydrogen or halogen atoms, R.sup.2 represents a hydrogen or halogen atom or a lower alkyl or alkoxy group (provided R.sup.1, R.sup.2 and R.sup.3 are not simultaneously hydrogen), represents a single or double carbon-carbon bond and, where it is a single bond, R.sup.4 represents a group of formula --SR.sup.5 (wherein R.sup.5 represents an optionally substituted alkyl, phenyl, aralkyl or pyridyl group or a lower alkenyl group) and, where it is a double bond, R.sup.4 represents hydrogen] can be prepared by reacting a compound of formula (II): ##STR2## with a compound of formula R.sup.6 H [where R.sup.6 represents a group --SR.sup.5, a group --SR.sup.7 (where R.sup.7 represents a group of formula ##STR3## and Y represents oxygen or sulphur, R.sup.8 and R.sup.9 represent lower alkoxy groups and R.sup.10 represents a lower alkoxy, lower alkyl or phenyl group), a methoxy group or a halogen atom] to give a compound of formula (IV): ##STR4## or, where R.sup.6 represents a methoxy group, a methyl ester thereof; reacting this compound with hydrazine to give a compound of formula (V): ##STR5## and, if necessary, treating the compound of formula (V) with an acid or a base to produce the compound of formula (VI). All of the compounds of formula (I) are valuable antifungal agents and compounds of formula (V) where R.sup.6 represents a group of formula --SR.sup.5 are novel compounds.
摘要翻译：式（I）化合物：其中R 1和R 3表示氢或卤素原子，R 2表示氢或卤素原子或低级烷基或烷氧基（条件是R 1，R 2和R 3不同时为氢）表示单或双碳 - 碳键，并且其中单键，R 4表示式-SR 5的基团（其中R 5表示任选取代的烷基，苯基，芳烷基或吡啶基或低级烯基）其中它是双键，R 4代表氢]可以通过使式（II）化合物：其中R6代表基团-SR5，基团-SR7（Ⅱ）的化合物其中R 7表示式的基团，Y表示氧或硫，R 8和R 9表示低级烷氧基，R 10表示低级烷氧基，低级烷基或苯基），甲氧基或卤原子]，得到化合物（IV）的化合物：其中R 6表示甲氧基，其甲酯 ; 使该化合物与肼反应，得到式（Ⅴ）化合物：ι（Ⅴ）或（Ⅵ）：Ⅵ（VI），如果需要，用酸或制备式（VI）化合物。式（I）的所有化合物均为有价值的抗真菌剂，式（V）化合物，其中R 6表示式-SR 5的基团是新化合物。

4. 发明授权

US5208349A Process for preparing milbemycin derivatives and certain novel compounds employed therein 失效
标题翻译：米尔霉素衍生物及其中所用的某些新化合物的制备方法
公开(公告)号：US5208349A
公开(公告)日：1993-05-04
申请号：US644880
申请日：1991-01-24
申请人： Kazuo Sato , Takao Kinoto , Shigeru Mio , Toshiaki Yanai
发明人： Kazuo Sato , Takao Kinoto , Shigeru Mio , Toshiaki Yanai
IPC分类号： C07H19/01
CPC分类号： C07H19/01
摘要： 13-Hydroxy-5-ketomilbemycin derivatives are prepared by oxidizing a 5-ketomilbemycin with selenium dioxide in the presence of a lower aliphatic carboxylic acid. A range of new 13-acyloxy-5-ketomilbemycins and a method of preparing them are also disclosed.
摘要翻译：通过在低级脂肪族羧酸的存在下用二氧化硒氧化5-酮米尔贝霉素来制备13-羟基-5-酮米尔贝霉素衍生物。还公开了一系列新的13-酰氧基-5-酮基尔贝莫霉素及其制备方法。

5. 发明授权

US4835290A Process for preparing 13-hydroxy-5-ketomibemycin derivatives having acaricidal, insecticidal and anthelmintic activity 失效
标题翻译：制备具有杀螨，杀虫和驱虫活性的13-羟基-5-酮基霉素衍生物的方法
公开(公告)号：US4835290A
公开(公告)日：1989-05-30
申请号：US115642
申请日：1987-10-26
申请人： Kazuo Sato , Takao Kinoto , Shigeru Mio , Toshiaki Yanai
发明人： Kazuo Sato , Takao Kinoto , Shigeru Mio , Toshiaki Yanai
IPC分类号： C07H19/01
CPC分类号： C07H19/01
摘要： 13-Hydroxy-5-ketomilbemycin derivatives are prepared by oxidizing a 5-ketomilbemycin with selenium dioxide in the presence of a lower aliphatic carboxylic acic. A range of new 13-acyloxy-5-ketomilbemycins and a method or preparing them are also disclosed.
摘要翻译：通过在低级脂肪族羧酸存在下，用二氧化硒氧化5-酮米尔贝霉素来制备13-羟基-5-酮米尔贝霉素衍生物。还公开了一系列新的13-酰氧基-5-酮基尔贝莫霉素及其制备方法或制备方法。

6. 发明授权

US4661486A Pyridazinone derivatives and their use as agricultural fungicides 失效
标题翻译：哒嗪酮衍生物及其作为农药的用途
公开(公告)号：US4661486A
公开(公告)日：1987-04-28
申请号：US649499
申请日：1984-09-11
申请人： Hideo Takeshiba , Takao Kinoto , Teruomi Jojima
发明人： Hideo Takeshiba , Takao Kinoto , Teruomi Jojima
IPC分类号： A01N43/58 , C07D237/04
CPC分类号： C07D237/04 , A01N43/58
摘要： Compounds of formula (I): ##STR1## (in which R.sup.1 and R.sup.3 are hydrogen or halogen: R.sup.2 is hydrogen, alkyl, alkoxy or halogen; R.sup.4 is hydrogen and R.sup.5 is hydroxy or alkoxy; or R.sup.4 is hydroxy and R.sup.5 is hydrogen; except that R.sup.1, R.sup.2 and R.sup.3 may not all simultaneously be hydrogen) are valuable agricultural fungicides.
摘要翻译：式（I）化合物：其中R 1和R 3是氢或卤素：R 2是氢，烷基，烷氧基或卤素; R 4是氢，R 5是羟基或烷氧基;或者R 4是羟基和R 5 是氢;除了R1，R2和R3可能不全部同时为氢）是有价值的农药杀菌剂。

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