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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

US4945105A 13-Halomilbemycin derivatives, their preparation and compositions containing them 失效
标题翻译： 13-哈美列霉素衍生物，其制备方法和含有它们的组合物
公开(公告)号：US4945105A
公开(公告)日：1990-07-31
申请号：US290835
申请日：1988-12-28
申请人： Kazuo Sato , Toshiaki Yanai , Noritoshi Kitano , Akira Nishida , Bruno Frei , Anthony O'Sullivan
发明人： Kazuo Sato , Toshiaki Yanai , Noritoshi Kitano , Akira Nishida , Bruno Frei , Anthony O'Sullivan
IPC分类号： C07D493/22 , A01N43/90 , A01P5/00 , A01P7/02 , A01P7/04 , A61K31/365 , A61P33/10 , C07D307/00 , C07D309/00 , C07H19/01
CPC分类号： C07H19/01 , A01N43/90
摘要： Derivatives of milbemycins D, A.sub.3 and A.sub.4 and of the corresponding sec-butyl compound have a halogen atom at the 13-position; at the 5-position, they have an oxygen (keto) atom, an oxime group or a substituted oxime group. They may be prepared from known compounds by any appropriate combination of halogenation, ketonization and oximation.
摘要翻译：米尔倍霉素D，A3和A4及相应的仲丁基化合物的衍生物在13位具有卤素原子; 在5位，它们具有氧（酮）原子，肟基或取代的肟基。它们可以通过卤化，酮化和肟化的任何适当组合由已知化合物制备。

4. 发明授权

US4912090A Antiparasitic milbemycin and avermectin derivatives 失效
标题翻译：抗寄生米尔倍霉素和阿维菌素衍生物
公开(公告)号：US4912090A
公开(公告)日：1990-03-27
申请号：US947615
申请日：1986-12-30
申请人： Toshiaki Yanai , Kazuo Sato , Akira Nishida , Keiji Tanaka
发明人： Toshiaki Yanai , Kazuo Sato , Akira Nishida , Keiji Tanaka
IPC分类号： C07H17/08 , A01N43/90 , A61K31/365 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P33/00 , A61P33/10 , C07D493/22 , C07H19/01
CPC分类号： C07H19/01 , A01N43/90
摘要： 8,9 and/or 14,15 epoxidized and 5-acylated milbemycins and avermectins are prepared from the parent milbemycins and avermectins by epoxidation and acylation (in either order). They have enhanced anthelmintic, acaricidal and insecticidal activities.
摘要翻译：通过环氧化和酰化（以任一顺序）从母体milbemycins和阿维菌素制备8,9和/或14,15环氧化和5-酰化的米尔倍霉素和除虫菌素。它们具有增强的驱虫，杀螨和杀虫活性。

5. 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。

6. 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。

7. 发明授权

US4959386A Pesticides 失效
标题翻译：农药
公开(公告)号：US4959386A
公开(公告)日：1990-09-25
申请号：US252031
申请日：1988-09-28
申请人： Bruno Frei , Hari B. Mereyala , Anthony C. O'Sullivan , Kazuo Sato , Toshiaki Yanai
发明人： Bruno Frei , Hari B. Mereyala , Anthony C. O'Sullivan , Kazuo Sato , Toshiaki Yanai
IPC分类号： A01N43/90 , A61K31/35 , A61K31/365 , A61K31/695 , A61P33/00 , A61P33/10 , C07D493/22 , C07F7/18 , C07H19/01
CPC分类号： C07H19/01
摘要： The present invention relates to novel compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, a silyl group or an acyl group,R.sub.2 is methyl, ethyl, is propyl or sec-butyl, and R is hydrogen, unsubstituted or substituted straight chain or branched C.sub.1 -Cl.sub.18 alkyl, an unsubstituted or substituted cycloaliphatic group containing 3 to 10 carbon atoms, unsubstituted or substituted C.sub.2 -C.sub.6 alkenyl, unsubstituted or substituted C.sub.2 -C.sub.6 -alkynyl, unsubstituted or substituted phenyl or unsubstituted or substituted benzyl. These compounds posseses advantageous pesticidal properties and are suitable in particular for controlling pests in agriculture and the storage sector.
摘要翻译：本发明涉及新的式（I）化合物，其中R 1是氢，甲硅烷基或酰基，R 2是甲基，乙基，是丙基或仲丁基，R是氢，未取代或取代的未取代或取代的C2-C6链烯基，未取代或取代的C2-C6-炔基，未取代或取代的苯基或未经取代或取代的苄基的直链或支链C 1 -C 18烷基，未取代或取代的含有3至10个碳原子的脂环族基团。这些化合物具有有利的杀虫特性，特别适用于防治农业和贮藏部门的害虫。

8. 发明授权

US5212322A 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：US5212322A
公开(公告)日：1993-05-18
申请号：US644100
申请日：1991-01-22
申请人： Takao Okazaki , Shuji Takahashi , Seigo Iwado , Keiji Tanaka , Toshiaki Yanai , Hisaki Kajino
发明人： Takao Okazaki , Shuji Takahashi , Seigo Iwado , Keiji Tanaka , Toshiaki Yanai , Hisaki Kajino
IPC分类号： A01N49/00 , C07H19/01 , C12P17/18
CPC分类号： C07H19/01 , A01N49/00 , C12P17/181 , Y02P20/55 , Y10S424/08
摘要： Compounds with acaricidal, insecticidal and anthelmintic activities have the formula: ##STR1## wherein: --X--Y-- is selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHOH--, --CH.dbd.CH--, and --CH.sub.2 --C(.dbd.O)--;R.sup.1 is selected from the group consisting of a methyl group, an ethyl group, an isopropyl group, a sec-butyl group and groups of formula --C(CH.sub.3).dbd.CHR.sup.5 in which R.sup.5 is selected from the group consisting of a methyl group, an ethyl group and an isopropyl group;R.sup.2 represents a group of formula --(CH.sub.2).sub.n --C(R.sup.6).dbd.C(R.sup.7)(R.sup.8) in which n is 0, 1 or 2, R.sup.6 and R.sup.7 each is selected from the group consisting of a hydrogen atom and a methyl group and R.sup.8 is selected from the group consisting of a hydrogen atom, a C.sub.1-4 alkyl group, a phenyl group and a phenyl group substituted with at least one substituent selected from the group consisting of halogen, methyl and nitro substituents;R.sup.3 is selected from the group consisting of a hydrogen atom, a methyl group, a hydroxy-protecting group, an ester-forming carboxylic acid residue, and an ester-forming carbonic acid residue; andR.sup.4 is selected from the group consisting of a hydrogen atom and an .alpha.-L-oleandrosyl-.alpha.-L-oleandrosyloxy group, with the proviso that R.sup.4 represents a hydrogen atom when the group R.sup.1 is selected from the group consisting of a methyl group, an ethyl group, and groups of formula --C(CH.sub.3).dbd.CHR.sup.5 in which R.sup.5 is selected from the group consisting of a methyl group, an ethyl group and an isopropyl group.
摘要翻译：具有杀螨，杀虫和驱虫活性的化合物具有下式：其中：-XY-选自-CH 2 -CH 2 - ， - CH 2 -CHOH - ， - CH = CH-和 - CH2-C（= O） - ; R 1选自甲基，乙基，异丙基，仲丁基和式-C（CH 3）= CHR 5的基团，其中R 5选自甲基，乙基和异丙基; R 2表示式 - （CH 2）n C（R 6）= C（R 7）（R 8）的基团，其中n为0,1或2，R 6和R 7各自为氢原子和甲基并且R 8选自氢原子，C 1-4烷基，苯基和被至少一个选自卤素，甲基和硝基取代基的取代基取代的苯基; R3选自氢原子，甲基，羟基保护基，成酯羧酸残基和形成酯的碳酸残基; 并且R 4选自氢原子和α-L-甘氨酰基-α-L-胆碱基氧基，条件是当R 1选自甲基时，R 4表示氢原子，乙基和式-C（CH 3）= CHR 5基团，其中R 5选自甲基，乙基和异丙基。

9. 发明授权

US5276033A 13-(substituted thio)acetoxymilbemycin derivatives, their preparation and their agrochemical uses 失效
标题翻译： 13-（取代硫代）乙酰氧基米尔伯霉素衍生物，其制备方法及其农用化学品用途
公开(公告)号：US5276033A
公开(公告)日：1994-01-04
申请号：US992865
申请日：1992-12-17
申请人： Toshiaki Yanai , Soji Sugai , Hideo Takeshiba , Junzo Tobitsuka , Kazuo Sato , Shinji Yokoi , Shinya Niimi , Akio Saito
发明人： Toshiaki Yanai , Soji Sugai , Hideo Takeshiba , Junzo Tobitsuka , Kazuo Sato , Shinji Yokoi , Shinya Niimi , Akio Saito
IPC分类号： A01N43/90 , A01P7/04 , C07D493/22 , C07H19/01 , A61K31/53 , A61K31/505 , C07D239/38
CPC分类号： C07H19/01 , A01N43/90
摘要： Compounds having the formula (I) ##STR1## wherein: R.sup.1 is methyl, ethyl or isopropyl; R.sup.2 is alkyl, aralkyl, cycloalkyl, cycloalkylmethyl, aryl, heterocyclic, or heterocyclic-substituted thio; R.sup.3 is hydrogen, methyl or ethyl; or R.sup.2 together with R.sup.3 is --(CH.sub.2).sub.n --, wherein n is 3,4 or 5; and A is aromatic heterocyclic; and salts thereof, are valuable agricultural and horticultural anthelmintic, acaricidal and insecticidal agents.
摘要翻译：具有式（I）的化合物（I）其中：R1是甲基，乙基或异丙基; R2是烷基，芳烷基，环烷基，环烷基甲基，芳基，杂环或杂环取代的硫代; R3是氢，甲基或乙基; 或R 2与R 3一起为 - （CH 2）n - ，其中n为3,4或5; A是芳族杂环; 和其盐是有价值的农业和园艺驱虫剂，杀螨剂和杀虫剂。

10. 发明授权

US5008191A 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：US5008191A
公开(公告)日：1991-04-16
申请号：US131413
申请日：1987-12-10
申请人： Takao Okazaki , Shuji Takahashi , Seigo Iwado , Keiji Tanaka , Toshiaki Yanai , Hisaki Kajino
发明人： Takao Okazaki , Shuji Takahashi , Seigo Iwado , Keiji Tanaka , Toshiaki Yanai , Hisaki Kajino
IPC分类号： C07D493/22 , A01N43/90 , A01N49/00 , A01P7/02 , A01P7/04 , C07D307/00 , C07D309/00 , C07H19/01 , C12P17/18 , C12P19/54
CPC分类号： C07H19/01 , A01N49/00 , C12P17/181 , Y02P20/55 , Y10S435/898
摘要： Compounds with acaricidal, insecticidal and anthelmintic activities have the formula: ##STR1## wherein: --X--Y-- is selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHOH--, --CH.dbd.CH--, and --CH.sub.2 --C(.dbd.O)--;R.sup.1 is selected from the group consisting of a methyl group, an ethyl group, an isopropyl group, a sec-butyl group and groups of formula --C(CH.sub.3).dbd.CHR.sup.5 in which R.sup.5 is selected from the group consisting of a methyl group, an ethyl group and an isopropyl group;R.sup.2 represents a group of formula --(CH.sub.2).sub.n --C(R.sup.6).dbd.C(R.sup.7)(R.sup.8) in which n is 0, 1 or 2, R.sup.6 and R.sup.7 each is selected from the group consisting of a hydrogen atom and a methyl group and R.sup.8 is selected from the group consisting of a hydrogen atom, a C.sub.1-4 alkyl group, a phenyl group and a phenyl group substituted with at least one substituent selected from the group consisting of halogen, methyl and nitro substitutents;R.sup.3 is selected from the group consisting of a hydrogen atom, a methyl group, a hydroxy-protecting group, an ester-forming carboxylic acid residue, and an ester-forming carbonic acid residue; andR.sup.4 is selected from the group consisting of a hydrogen atom and an .alpha.-L-oleandrosyl-.alpha.-L-oleandrosyloxy group, with the proviso that R.sup.4 represents a hydrogen atom when the group R.sup.1 is selected from the group consisting of a methyl group, an ethyl group, and groups of formula --C(CH.sub.3).dbd.CHR.sup.5 in which R.sup.5 is selected from the group consisting of a methyl group, an ethyl group and an isopropyl group.

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