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1. 发明授权

US5604182A Milbemycin ether derivatives, their preparation and their therapeutic and agrochemical uses 失效
标题翻译：米尔贝霉素醚衍生物，其制备及其治疗和农药用途
公开(公告)号：US5604182A
公开(公告)日：1997-02-18
申请号：US273240
申请日：1994-07-11
申请人： Yasuhiro Morisawa , Akio Saito , Toshimitsu Toyama , Susumu Kaneko
发明人： Yasuhiro Morisawa , Akio Saito , Toshimitsu Toyama , Susumu Kaneko
IPC分类号： A01N43/90 , A01N47/28 , A61K31/35 , A61K31/365 , A61P33/00 , A61P33/10 , C07D493/22 , C07H19/01 , A01N43/04 , A61K31/335 , C07D315/00
CPC分类号： C07D493/22 , A01N43/90 , C07H19/01
摘要： Compounds of formula (I): ##STR1## and salts and esters thereof have valuable anthelmintic, acaricidal and insecticidal activities. Methods of preparing the compounds are also provided.
摘要翻译：式（I）化合物：其中（I）及其盐和酯具有有价值的驱虫，杀螨和杀虫活性。还提供了制备化合物的方法。

2. 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.

3. 发明授权

US06653342B2 13-substituted milbemycin derivatives, their preparation and their use against insects and other pests 失效
标题翻译： 13-取代的米尔倍霉素衍生物，它们的制备及其对昆虫和其它害虫的用途
公开(公告)号：US06653342B2
公开(公告)日：2003-11-25
申请号：US10277993
申请日：2002-10-22
申请人： Akio Saito , Yoko Sugiyama , Toshimitsu Toyama , Toshihiko Nanba
发明人： Akio Saito , Yoko Sugiyama , Toshimitsu Toyama , Toshihiko Nanba
IPC分类号： A61K31335
CPC分类号： C07H19/01 , A01N43/90
摘要： Compounds of formula (I) and salts thereof: Wherein R1 represents methyl, ethyl, isopropyl or s-butyl; and R2 represents hydrogen or alkyl. R3 represents hydrogen, optionally substituted alkanoyl, optionally substituted alkenoyl, optionally substituted alkynoyl, alkylsulfonyl, or alkoxycarbonyl, or R2 and R3 together with the nitrogen atom to which they are attached form a saturated, optionally substituted 4- to 6-membered heterocyclic ring group. The moiety -a- together with the carbon atom to which it is attached forms a 3- to 6-membered cycloalkyl group. These compounds have anthelmintic, acaricidal and insecticidal activity.
摘要翻译：式（I）化合物及其盐：其中R 1表示甲基，乙基，异丙基或仲丁基; R 2表示氢或烷基。 R 3表示氢，任选取代的烷酰基，任选取代的烯酰基，任选取代的炔酰基，烷基磺酰基或烷氧基羰基，或R 2和R 3与它们所连接的氮原子一起形成饱和的，任选取代的 4-至6-元杂环基团。部分 - 与其连接的碳原子一起形成3至6元环烷基。这些化合物具有驱虫，杀螨和杀虫活性。

4. 发明授权

US5428034A Milbemycin derivatives, their preparation and their use 失效
标题翻译：米尔霉素衍生物，其制备及其用途
公开(公告)号：US5428034A
公开(公告)日：1995-06-27
申请号：US71765
申请日：1993-06-09
申请人： Yasuhiro Morisawa , Akio Saito , Toshimitsu Toyama , Susumu Kaneko
发明人： Yasuhiro Morisawa , Akio Saito , Toshimitsu Toyama , Susumu Kaneko
IPC分类号： A01N43/90 , C07D493/22 , C07H19/01 , A61K31/535 , A61K31/335 , C07D315/00
CPC分类号： C07D493/22 , A01N43/90 , C07H19/01
摘要： Compounds of formula (I): ##STR1## thereof have valuable anthelmintic, acaricidal and insecticidal activities.
摘要翻译：式（I）的化合物：其具有有价值的驱虫，杀螨和杀虫活性。

5. 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。

6. 发明授权

US5346918A Milbemycin ether derivatives, their preparation and their therapeutic and agrochemical uses 失效
标题翻译：米尔贝霉素醚衍生物，其制备及其治疗和农药用途
公开(公告)号：US5346918A
公开(公告)日：1994-09-13
申请号：US661833
申请日：1991-02-27
申请人： Yasuhiro Morisawa , Akio Saito , Toshimitsu Toyama , Susumu Kaneko
发明人： Yasuhiro Morisawa , Akio Saito , Toshimitsu Toyama , Susumu Kaneko
IPC分类号： A01N43/90 , A01N47/28 , A61K31/35 , A61K31/365 , A61P33/00 , A61P33/10 , C07D493/22 , C07H19/01 , C07D325/00
CPC分类号： C07D493/22 , A01N43/90 , C07H19/01
摘要： Compounds of formula (I): ##STR1## in which: R.sup.1 is a variety of organic groups; R.sup.5 is methyl, ethyl, isopropyl or sec-butyl; and X is hydroxy, alkanoyloxy or hydroxyimino and salts and esters thereof have valuable anthelmintic, acaricidal and insecticidal activities. Methods of preparing the compounds are also provided.
摘要翻译：式（I）的化合物：其中：R1是各种有机基团; R5是甲基，乙基，异丙基或仲丁基; X是羟基，烷酰氧基或羟基亚氨基，其盐和酯具有有价值的驱虫，杀螨和杀虫活性。还提供了制备化合物的方法。

7. 发明授权

US5861429A 13-substituted milbemycin 5-oxime derivatives, their preparation and their use against insects and other pests 失效
标题翻译： 13-取代的米尔倍霉素5-肟衍生物，它们的制备及其对昆虫和其它害虫的用途
公开(公告)号：US5861429A
公开(公告)日：1999-01-19
申请号：US723835
申请日：1996-09-30
申请人： Kazuo Sato , Akio Saito , Toshimitsu Toyama
发明人： Kazuo Sato , Akio Saito , Toshimitsu Toyama
IPC分类号： C07D493/22 , A01N43/08 , A01N43/16 , A01N43/90 , A61K31/343 , A61K31/35 , A61P31/14 , A61P33/10 , C07D307/26 , C07D311/96 , C07D313/00 , C07H19/01 , A61K31/335 , A61K31/38 , A61K31/425 , A61K31/505
CPC分类号： C07H19/01
摘要： Compounds of formula (I): ##STR1## wherein: R.sup.1 is methyl, ethyl, isopropyl or sec-butyl; X is carbonyl or methylene; Z is .dbd.C.dbd.(R.sup.2).sub.2 or .dbd.C.dbd.(CH.sub.2).sub.m, in which R.sup.2 is alkyl, and m is integer of from 2 to 5); n is 0 or 1; R.sup.3 is nitro, amino, alkylamino, dialkylamino, alkoxy, alkoxyalkoxy, or a group (iii), (iv), (v), (vi), (vii), (viii) or (ix): ##STR2## , wherein: R.sup.4 represents: alkyl; substituted alkyl; cycloalkyl having from 3 to 6 carbon atoms; substituted cycloalkyl; alkenyl; alkynyl; carbocyclic aryl; or heterocyclic; R.sup.5 is hydrogen atom or alkyl; R.sup.6 represents: hydrogen; alkyl; or cycloalkyl; R.sup.7 represents: alkyl; cycloalkyl; carbocyclic aryl; or aralkyl; or R.sup.6 and R.sup.7, together with the nitrogen atom to which they are attached, are fuised to form heterocyclic ring; Y is oxygen or sulfur; r is 1, 2 or 3; Q is methylene or carbonyl; R.sup.8 is: alkyl or carbocyclic aryl; R.sup.9 is: alkyl; cycloalkyl; carbocyclic aryl; or aralkyl; R.sup.10 is heterocyclic; and R.sup.11 is aLkyl; have valuable acaricidal, insecticidal and anthelmintic activities.
摘要翻译：式（I）的化合物：其中：R1是甲基，乙基，异丙基或仲丁基; X是羰基或亚甲基; Z为= C =（R2）2或= C =（CH2）m，其中R2为烷基，m为2至5的整数）; n为0或1; （iii），（iv），（v），（vi），（vii），（viii）或（ix）：（iii）（ix）ix;;;;;;;;;;;;;;;;：：：：：：：：：：：：：：：;;;;;;;;;;; 取代的烷基; 具有3至6个碳原子的环烷基; 取代的环烷基; 烯基; 炔基; 碳环芳基; 或杂环; R5是氢原子或烷基; R6表示：氢; 烷基; 或环烷基; R 7表示：烷基; 环烷基碳环芳基; 或芳烷基; 或R6和R7与它们所连接的氮原子一起被引发形成杂环; Y是氧或硫; r为1,2或3; Q是亚甲基或羰基; R8是：烷基或碳环芳基; R9是：烷基; 环烷基碳环芳基; 或芳烷基; R10是杂环的; R11为烷基; 具有有效的杀螨，杀虫和驱虫活动。

8. 发明授权

US5686484A Milbemycin derivatives, their preparation and their use 失效
标题翻译：米尔霉素衍生物，其制备及其用途
公开(公告)号：US5686484A
公开(公告)日：1997-11-11
申请号：US396662
申请日：1995-03-01
申请人： Yasuhiro Morisawa , Akio Saito , Satoru Naito , Toshimitsu Toyama , Susumu Kaneko , Louis-Pierre Molleyres , Jean-Claude Gehret
发明人： Yasuhiro Morisawa , Akio Saito , Satoru Naito , Toshimitsu Toyama , Susumu Kaneko , Louis-Pierre Molleyres , Jean-Claude Gehret
IPC分类号： A01N43/90 , C07D493/22 , C07H19/01 , A61K31/335 , C07D315/00
CPC分类号： C07D493/22 , A01N43/90 , C07H19/01
摘要： Compounds of formula (I): ##STR1## and of formula (I).sub.w : ##STR2## in which: A represents group having one of the following formulae: ##STR3## wherein R.sup.2, R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen atoms, halogen atoms, alkyl groups having from 1 to 4 carbon atoms, and alkoxy groups having from 1 to 4 carbon atoms; R.sup.1, R.sub.w.sup.1 and R.sub.w.sup.2 are, for example, hydrogen, halogen, cyano, nitro, optically substituted alkyl, alkoxy or alkoxyalkoxy; X or X.sub.w is hydroxy, alkanoyloxy, substituted alkanoyloxy or hydroxyimino; R.sup.3.sub.w and R.sup.4.sub.w are each hydrogen, alkyl or alkoxy; R.sup.5 and R.sup.5.sub.w are methyl, ethyl, isopropyl or sec-butyl; and salts thereof have valuable anthelmintic, acaricidal and insecticidal activities.
摘要翻译：式（I）化合物：其中：A表示具有下式之一的基团：CHR 2 CHR 3 CHR 4 CR 2 CR 3 CHR 4或（I）其中R 2，R 3和R 4独立地选自氢原子，卤素原子，具有1至4个碳原子的烷基和具有1至4个碳原子的烷氧基; R1，Rw1和Rw2是例如氢，卤素，氰基，硝基，光学取代的烷基，烷氧基或烷氧基烷氧基; X或Xw是羟基，烷酰氧基，取代的烷酰氧基或羟基亚氨基; R3w和R4w各自为氢，烷基或烷氧基; R5和R5w是甲基，乙基，异丙基或仲丁基; 其盐具有宝贵的驱虫，杀螨和杀虫活性。

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