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111. 发明授权

US08183416B2 Heterocyclic amide derivatives useful as microbiocides 有权
标题翻译：用作杀微生物剂的杂环酰胺衍生物
公开(公告)号：US08183416B2
公开(公告)日：2012-05-22
申请号：US12765929
申请日：2010-04-23
申请人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi
发明人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi
IPC分类号： C07C205/06
CPC分类号： C07C205/06 , A01N43/32 , A01N43/36 , A01N43/40 , A01N43/56 , A01N43/647 , A01N43/76 , A01N43/78 , C07C205/11 , C07C205/12 , C07C205/37 , C07C205/45 , C07C211/61 , C07C2603/66 , C07D207/34 , C07D207/46 , C07D213/89 , C07D231/14 , C07D249/04 , C07D263/34 , C07D277/56 , C07D327/06
摘要： The invention relates to a fungicidally active compound of formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by the groups R6, R7 and R8; R1 is hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4alkoxy, C1-4haloalkoxy, CH2C≡CR9, CH2CR10═CHR11, CH═C═CH2 or COR12; R2 and R3 are each, independently, hydrogen, halo, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl or C1-4 haloalkoxy; R4 and R5 are each independently selected from halo, cyano and nitro; or one of R4 and R5 is hydrogen and the other is selected from halo, cyano and nitro; R6, R7 and R8 are each, independently, hydrogen, halo, cyano, nitro, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy(C1-4)alkyl, C1-4haloalkoxy(C1-4)alkyl or C1-4haloalkoxy, provided that at least one of R6, R7 and R8 is not hydrogen; R9, R10 and R11 are each, independently, hydrogen, halo, C1-4 alkyl, C1-4 haloalkyl or C1-4 alkoxy(C1-4)alkyl; and R12 is hydrogen, C1-6 alkyl, C1-6haloalkyl, C1-4 alkoxy(C1-4)alkyl, C1-4 alkylthio(C1-4)-alkyl, C1-4 alkoxy or aryl; to the preparation of these compounds, to novel intermediates used in the preparation of these compounds, to agrochemical compositions which comprise at least one of the novel compounds as active ingredient, to the preparation of the compositions mentioned and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
摘要翻译：本发明涉及式（I）的杀真菌活性化合物：其中Het是含有一至三个杂原子的5-或6-元杂环，各自独立地选自氧，氮和硫，该环被R6基团取代，R7和R8; R 1是氢，C 1-4烷基，C 1-4卤代烷基，C 1-4烷氧基，C 1-4卤代烷氧基，CH 2C≡CR9，CH 2 CR 10 = CHR 11，CH = C = CH 2或COR 12; R 2和R 3各自独立地为氢，卤素，C 1-4烷基，C 1-4烷氧基，C 1-4卤代烷基或C 1-4卤代烷氧基; R4和R5各自独立地选自卤素，氰基和硝基; 或者R 4和R 5中的一个是氢，另一个选自卤素，氰基和硝基; R 6，R 7和R 8各自独立地为氢，卤素，氰基，硝基，C 1-4烷基，C 1-4卤代烷基，C 1-4烷氧基（C 1-4）烷基，C 1-4卤代烷氧基（C 1-4）烷基或C 1 -4卤代烷氧基，条件是R 6，R 7和R 8中的至少一个不是氢; R 9，R 10和R 11各自独立地为氢，卤素，C 1-4烷基，C 1-4卤代烷基或C 1-4烷氧基（C 1-4）烷基; 并且R 12是氢，C 1-6烷基，C 1-6卤代烷基，C 1-4烷氧基（C 1-4）烷基，C 1-4烷硫基（C 1-4） - 烷基，C 1-4烷氧基或芳基; 涉及这些化合物的制备，用于制备这些化合物的新型中间体，包括至少一种新化合物作为活性成分的农用化学组合物，所述组合物的制备以及使用活性成分或用于通过植物病原微生物，优选真菌控制或预防植物感染的农业或园艺成分。

112. 发明申请

US20120065239A1 PROCESS FOR THE PRODUCTION OF AMIDES 有权
标题翻译：生产助剂的方法
公开(公告)号：US20120065239A1
公开(公告)日：2012-03-15
申请号：US13198739
申请日：2011-08-05
申请人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Kevin Jones , Paul Edward Bonnett
发明人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Kevin Jones , Paul Edward Bonnett
IPC分类号： A01N43/56 , A01P3/00 , C07D231/14
CPC分类号： C07C211/61 , A01N43/56 , C07C205/06 , C07C209/325 , C07C209/70 , C07C2603/66 , C07D231/14
摘要： The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are each independently of the other hydrogen or C1-C5alkyl and R3 is CF3 or CF2H, by a) reaction of a compound of formula II wherein R1 and R2 are as defined for formula I, with at least one reducing agent to form a compound of formula wherein R1 and R2 are as defined for formula I, and b) reaction of that compound with at least one reducing agent to form a compound of formula IV wherein R1 and R2 are as defined for formula I, and (c) reaction of that compound with a compound of formula V wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C1-C6alkoxy and R3 is as defined for formula I, to form the compound of formula I; and to novel intermediates for use in that process.
摘要翻译：本发明涉及一种制备式Ⅰ化合物的方法，其中R1和R2分别独立地为氢或C1-C5烷基，R3为CF3或CF2H，通过a）式II化合物的反应其中R 1和 R 2如式I所定义，与至少一种还原剂形成下式化合物，其中R 1和R 2如式I所定义，和b）该化合物与至少一种还原剂的反应形成式 IV其中R1和R2如式I所定义，和（c）该化合物与式V化合物的反应，其中Q是氯，氟，溴，碘，羟基或C 1 -C 6烷氧基，R 3如式I所定义，形成式I化合物; 以及用于该过程的新型中间体。

113. 发明申请

US20110207771A1 N-(L-ALKYL-2-PHENYLETHYL)-CARBOXAMIDE DERIVATIVES AND USE THEREOF AS FUNGICIDES 审中-公开
标题翻译： N-（L-烷基-2-苯基）乙酰胺衍生物及其作为杀真菌剂的用途
公开(公告)号：US20110207771A1
公开(公告)日：2011-08-25
申请号：US12303763
申请日：2007-06-06
申请人： Daniel Stierli , John J. Taylor , Harald Walter , Paul Anthony Worthington , Ramya Rajan
发明人： Daniel Stierli , John J. Taylor , Harald Walter , Paul Anthony Worthington , Ramya Rajan
IPC分类号： A01N43/56 , C07D231/14 , C07D401/12 , C07D277/56 , A01N43/78 , C07D417/12 , C07D207/34 , A01N43/36 , A01N43/40 , C07D249/04 , A01N43/647 , A01N43/42 , A01P3/00
CPC分类号： C07D231/14 , A01N43/36 , A01N43/42 , A01N43/56 , A01N43/647 , A01N43/78 , C07D207/34 , C07D249/04 , C07D277/32
摘要： Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
摘要翻译：其中取代基如权利要求1中所定义的式（I）化合物适合用作杀微生物剂。

114. 发明授权

US07850886B2 Method for the manufacturing of a diffraction grating structure on the surface of pharmaceutical tablet 有权
$Method for the manufacturing of a diffraction grating structure on the surface of pharmaceutical tablet$
标题翻译：在药片的表面上制造衍射光栅结构的方法
公开(公告)号：US07850886B2
公开(公告)日：2010-12-14
申请号：US11811901
申请日：2007-06-12
申请人： Harald Walter
发明人： Harald Walter
IPC分类号： B29C43/02
CPC分类号： B30B15/065 , A61J3/007 , A61J3/06 , A61J2205/20 , A61J2205/40
摘要： A diffractive microstructure (11) is implemented as a security feature in the surface of tablet (4). For this purpose the punches (1a, 1b) comprise a microstructure (11), which during the compression process produce the diffractive microstructure on the surface of the tablet (4), by plastic and/or visco-elastic deformation of the powder particles. The method according to the invention is compatible to the existing tablet manufacturing methods with their high production speeds and compression forces. It is also compatible to the usual tabletting adjuvants.
摘要翻译：衍射微结构（11）被实现为片剂（4）的表面中的安全特征。为此目的，冲头（1a，1b）包括微结构（11），其在压缩过程中通过粉末颗粒的塑性和/或粘弹性变形在片剂（4）的表面上产生衍射微结构。根据本发明的方法与其高生产速度和压缩力的现有片剂制造方法兼容。它也与普通的压片佐剂相容。

115. 发明授权

US07820830B2 Process for the production of carboxanilides 有权
标题翻译：生产甲酰苯胺的方法
公开(公告)号：US07820830B2
公开(公告)日：2010-10-26
申请号：US12093619
申请日：2006-11-13
申请人： Harald Walter , Camilla Corsi , Josef Ehrenfreund , Hans Tobler
发明人： Harald Walter , Camilla Corsi , Josef Ehrenfreund , Hans Tobler
IPC分类号： C07D231/14
CPC分类号： C07D231/14
摘要： The present invention relates to a novel process for the preparation of a compound of general formula (I): wherein R1 is H or C1-4 alkyl and R2 is difluoromethyl or trifluoromethyl, which comprises reacting a compound of general formula (II): wherein R1 has the meaning given above and X is chloro or bromo, with a compound of general formula (III): wherein R2 has the meaning given above, in the presence of a base, a palladium catalyst and a ferrocenyl biphoshine ligand of the Josiphos type, the reaction being carried out in an ether solvent at a reflux temperature of at least 100° C.
摘要翻译：本发明涉及一种制备通式（I）化合物的新方法：其中R1是H或C1-4烷基，R2是二氟甲基或三氟甲基，其包括使通式（II）的化合物：其中 R1具有上面给出的含义，X是氯或溴，与通式（III）的化合物：其中R 2具有上面给出的含义，在碱存在下，钯催化剂和Josiphos型的二茂铁基二膦配体，反应在乙醚溶剂中在至少100℃的回流温度下进行。

116. 发明申请

US20100204482A1 HETEROCYCLIC AMIDE DERIVATIVES USEFUL AS MICROBIOCIDES 有权
标题翻译：杂环酰胺衍生物作为微生物有用
公开(公告)号：US20100204482A1
公开(公告)日：2010-08-12
申请号：US12765929
申请日：2010-04-23
申请人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi
发明人： Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi
IPC分类号： C07C205/06 , C07D277/56
CPC分类号： C07C205/06 , A01N43/32 , A01N43/36 , A01N43/40 , A01N43/56 , A01N43/647 , A01N43/76 , A01N43/78 , C07C205/11 , C07C205/12 , C07C205/37 , C07C205/45 , C07C211/61 , C07C2603/66 , C07D207/34 , C07D207/46 , C07D213/89 , C07D231/14 , C07D249/04 , C07D263/34 , C07D277/56 , C07D327/06
摘要： The invention relates to a fungicidally active compound of formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by the groups R6, R7 and R8; R1 is hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4alkoxy, C1-4haloalkoxy, CH2C≡CR9, CH2CR10═CHR11, CH═C═CH2 or COR12; R2 and R3 are each, independently, hydrogen, halo, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl or C1-4 haloalkoxy; R4 and R5 are each independently selected from halo, cyano and nitro; or one of R4 and R5 is hydrogen and the other is selected from halo, cyano and nitro; R6, R7 and R8 are each, independently, hydrogen, halo, cyano, nitro, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy(C1-4)alkyl, C1-4haloalkoxy(C1-4)alkyl or C1-4haloalkoxy, provided that at least one of R6, R7 and R8 is not hydrogen; R9, R10 and R11 are each, independently, hydrogen, halo, C1-4 alkyl, C1-4 haloalkyl or C1-4 alkoxy(C1-4)alkyl; and R12 is hydrogen, C1-6 alkyl, C1-6haloalkyl, C1-4 alkoxy(C1-4)alkyl, C1-4 alkylthio(C1-4)-alkyl, C1-4 alkoxy or aryl; to the preparation of these compounds, to novel intermediates used in the preparation of these compounds, to agrochemical compositions which comprise at least one of the novel compounds as active ingredient, to the preparation of the compositions mentioned and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
摘要翻译：本发明涉及式（I）的杀真菌活性化合物：其中Het是含有一至三个杂原子的5-或6-元杂环，各自独立地选自氧，氮和硫，该环被R6基团取代，R7和R8; R 1是氢，C 1-4烷基，C 1-4卤代烷基，C 1-4烷氧基，C 1-4卤代烷氧基，CH 2C≡CR9，CH 2 CR 10 = CHR 11，CH = C = CH 2或COR 12; R 2和R 3各自独立地是氢，卤素，C 1-4烷基，C 1-4烷氧基，C 1-4卤代烷基或C 1-4卤代烷氧基; R4和R5各自独立地选自卤素，氰基和硝基; 或者R4和R5之一是氢，另一个选自卤素，氰基和硝基; R 6，R 7和R 8各自独立地为氢，卤素，氰基，硝基，C 1-4烷基，C 1-4卤代烷基，C 1-4烷氧基（C 1-4）烷基，C 1-4卤代烷氧基（C 1-4）烷基或C 1 -4卤代烷氧基，条件是R 6，R 7和R 8中的至少一个不是氢; R 9，R 10和R 11各自独立地为氢，卤素，C 1-4烷基，C 1-4卤代烷基或C 1-4烷氧基（C 1-4）烷基; 并且R 12是氢，C 1-6烷基，C 1-6卤代烷基，C 1-4烷氧基（C 1-4）烷基，C 1-4烷硫基（C 1-4） - 烷基，C 1-4烷氧基或芳基; 涉及这些化合物的制备，用于制备这些化合物的新型中间体，包括至少一种新化合物作为活性成分的农用化学组合物，所述组合物的制备以及使用活性成分或用于通过植物病原微生物，优选真菌控制或预防植物感染的农业或园艺成分。

117. 发明申请

US20100145100A1 PROCESS FOR THE PREPARATION OF AMINES 审中-公开
标题翻译：制备氨基酸的方法
公开(公告)号：US20100145100A1
公开(公告)日：2010-06-10
申请号：US12443082
申请日：2007-09-26
申请人： Harald Walter , Hans Tobler , Fanny Giordano , Martin Zeller
发明人： Harald Walter , Hans Tobler , Fanny Giordano , Martin Zeller
IPC分类号： C07C209/36
CPC分类号： C07C209/36 , C07C2603/66 , C07C211/61
摘要： The present invention relates to a process for the preparation of syn-enriched 5-amino-9-isopropyl-benzonorbomene in which the ratio of compounds of formula (Ia(syn)) to compounds of formula (Ib(anti)) is from 70:30 to 99:1, which process comprises reacting a compound of formula (Il) in a pressure vessel with hydrogen in the presence of a palladium catalyst and a solvent, at a pressure of at least 2 bar and a temperature of from 00 C to 45° C., to form syn-enriched 5-amino-9-isopropyl-benzonorbomene.
摘要翻译：本发明涉及制备合成富集的5-氨基-9-异丙基 - 苯并异戊烯的方法，其中式（Ia（顺式））化合物与式（Ib（反））化合物的比例为70 ：30至99:1，该方法包括在钯催化剂和溶剂存在下，将压力容器中的式（II）化合物与氢气在至少2巴的压力和0℃的温度下反应至45℃，以形成合成富集的5-氨基-9-异丙基 - 苯并异戊烯。

118. 发明授权

US07723371B2 Microbiocides 失效
标题翻译：杀微生物剂
公开(公告)号：US07723371B2
公开(公告)日：2010-05-25
申请号：US12092338
申请日：2006-11-13
申请人： Harald Walter , Camilla Corsi , Josef Ehrenfreund , Hans Tobler
发明人： Harald Walter , Camilla Corsi , Josef Ehrenfreund , Hans Tobler
IPC分类号： A01N43/56
CPC分类号： A01N43/36 , A01N43/40 , A01N43/56 , A01N43/78 , A01N43/84 , C07C211/45 , C07C211/52 , C07C2601/02 , C07C2601/04 , C07D207/34 , C07D213/82 , C07D231/14 , C07D249/04 , C07D277/56 , C07D327/06
摘要： The invention relates to a fungicidally active compound of the general Formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by the groups R3, R4 and R5; R1 and R2 are independently H, halo, C1-4 alkyl or C1-4 haloalkyl; and R3, R4 and R5 are each, independently, H, halo, C1-4 alkyl, C1-4 haloalkyl or C1-4 haloalkoxy, provided that at least one of R3, R4 and R5 is not H; to the preparation of these compounds, to novel intermediates used in their preparation, to agrochemical compositions which comprise at least one of the novel compounds as an active ingredient, to the preparation of the compositions and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestations of plants by phytopathogenic microorganisms, especially fungi.
摘要翻译：本发明涉及通式（I）的杀真菌活性化合物：其中Het是含有一至三个杂原子的5-或6-元杂环，各自独立地选自氧，氮和硫，所述环被基团R3，R4和R5; R 1和R 2独立地为H，卤素，C 1-4烷基或C 1-4卤代烷基; 并且R 3，R 4和R 5各自独立地为H，卤素，C 1-4烷基，C 1-4卤代烷基或C 1-4卤代烷氧基，条件是R 3，R 4和R 5中的至少一个不为H; 涉及这些化合物的制备，其制备中使用的新型中间体，包含至少一种新化合物作为活性成分的农用化学组合物，用于制备组合物以及在农业中使用活性成分或组合物或园艺用于通过植物病原微生物，特别是真菌控制或预防植物侵染。

119. 发明申请

US20100022570A1 NOVEL MICROBIOCIDES 失效
标题翻译：新型微生物
公开(公告)号：US20100022570A1
公开(公告)日：2010-01-28
申请号：US12301080
申请日：2007-05-16
申请人： Daniel Stierli , John J. Taylor , Harald Walter , Paul Anthony Worthington
发明人： Daniel Stierli , John J. Taylor , Harald Walter , Paul Anthony Worthington
IPC分类号： A01N43/40 , C07C211/00 , A01N33/02 , C07D231/00 , C07D277/04 , A01N43/78 , C07D213/61 , C07D215/00 , A01N43/42
CPC分类号： C07D231/14 , A01N43/56 , C07C233/66 , C07D207/34 , C07D209/48 , C07D213/81 , C07D215/00 , C07D249/04 , C07D277/56 , C07D327/06 , C07D401/12 , C07D411/12 , C07D417/12
摘要： Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides. Formula (I), wherein X is oxygen or sulfur; A is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, or a phenyl ring; the heterocyclic ring or the phenyl being substituted by the groups R6, R7 and R8; R6, R7 and R8 are each, independently, hydrogen, halogen, cyano, nitro, C1-4 alky, C1-4 halogenalkyl, C1-4 halogenalkoxy, C1-4 alkoxy(C1-4)alkyl or C1-4halo-genalkoxy(C1-4)alkyl, provided that at least one of R6, R7 and R8 is not hydrogen; B is a phenyl, naphthyl or quinolinyl group, which is substituted by one or more substituents R9.
摘要翻译：其中取代基如权利要求1中所定义的式（I）化合物适合用作杀微生物剂。式（I），其中X是氧或硫; A是含有1至3个各自独立地选自氧，氮和硫的杂原子或苯环的5-或6-元杂环; 杂环或被R6，R7和R8基团取代的苯基; R 6，R 7和R 8各自独立地为氢，卤素，氰基，硝基，C 1-4烷基，C 1-4卤代烷基，C 1-4卤代烷氧基，C 1-4烷氧基（C 1-4）烷基或C 1-4卤代烷氧基 C 1-4）烷基，条件是R 6，R 7和R 8中的至少一个不是氢; B是被一个或多个取代基R 9取代的苯基，萘基或喹啉基。

120. 发明授权

US07652059B2 Pyrrolcarboxamides and pyrrolcarbothioamides 失效
标题翻译：吡咯烷酰胺和吡咯烷硫代酰胺
公开(公告)号：US07652059B2
公开(公告)日：2010-01-26
申请号：US11380735
申请日：2006-04-28
申请人： Harald Walter
发明人： Harald Walter
IPC分类号： A61K31/40 , C07D295/00
CPC分类号： C07D207/34 , A01N43/36 , C07C211/45 , C07C215/68 , C07C215/70 , C07C2601/02 , C07C2602/44
摘要： The invention relates to novel pesticidal pyrrolcarboxamides of formula I wherein X is oxygen or sulfur; R1 is CF3, CF2H or CFH2; R2 is C1-C3alkyl, C1-C3haloalkyl, C1-C3alkoxy-C1-C3alkyl or C1-C3haloalkoxy-C1-C3alkyl; R3 is hydrogen, methyl, CF3 or fluoro; Q is R4 is C6-C14bicycloalkyl unsubstituted or substituted by methyl, ethyl or CF3; C6-C14bicycloalkenyl unsubstituted or substituted by methyl, ethyl or CF3; C6-C14bicycloalkadienyl unsubstituted or substituted by methyl, ethyl or CF3; a group of the form wherein R7, R8 and R9 are independently of each other C1-C3alkyl or C1-C3haloalkyl; or a group wherein R10 and R11 are independently of each other hydrogen or halogen and n=1 or 2; and R5 and R6 are independently of each other hydrogen or halogen. The novel compounds have plant-protecting properties and are suitable for protecting plants against infestation by phytopathogenic microorganisms.
摘要翻译：本发明涉及式I的新型杀虫吡咯烷酰胺，其中X是氧或硫; R1是CF3，CF2H或CFH2; R 2是C 1 -C 3烷基，C 1 -C 3卤代烷基，C 1 -C 3烷氧基-C 1 -C 3烷基或C 1 -C 3卤代烷氧基-C 1 -C 3烷基; R3是氢，甲基，CF3或氟; Q是R 4是未被取代或被甲基，乙基或CF 3取代的C 6 -C 14双环烷基; 未被取代或被甲基，乙基或CF 3取代的C 6 -C 14双环烯基; 未取代或被甲基，乙基或CF 3取代的C 6 -C 14双环链烷二烯基; 其中R 7，R 8和R 9彼此独立地为C 1 -C 3烷基或C 1 -C 3卤代烷基; 或其中R 10和R 11彼此独立地为氢或卤素且n = 1或2的基团; 并且R 5和R 6彼此独立地为氢或卤素。新型化合物具有植物保护性质，适用于保护植物免受植物病原微生物的侵袭。

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