公开(公告)号：US08586505B2

公开(公告)日：2013-11-19

申请号：US13378866

申请日：2010-07-15

申请人： Masaaki Sakai ,  Tomoaki Matsumura ,  Satohiro Midorikawa ,  Takashi Nomoto ,  Ryutaro Katsuki ,  Tomoko Muraki

发明人： Masaaki Sakai ,  Tomoaki Matsumura ,  Satohiro Midorikawa ,  Takashi Nomoto ,  Ryutaro Katsuki ,  Tomoko Muraki

IPC分类号： C07D239/42 ,  C07D239/94 ,  C07D417/12 ,  C07D487/04 ,  C07D495/04 ,  A01N43/90 ,  A01N47/02 ,  A01N47/24 ,  A01N55/00

CPC分类号： C07D239/42 ,  A01N43/54 ,  A01N43/90 ,  C07D239/70 ,  C07D239/94 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07F7/081 ,  C07F7/0812 ,  C07F7/1804

摘要： Novel 4-(3-butynyl)aminopyrimidine derivatives represented by general formula [I] are useful as pest control agents. In general formula [I], R1 is a mono- or bi-cyclic ring which may contain 0 to 3 heteroatoms, for example, phenyl or oxazolyl; R2 is a hydrogen atom, —R, —OR, —C(O)OR, —C(O)NHR, —CONR2 (wherein R is straight-chain or branched C1-8 alkyl, or the like), hydroxyalkyl, or the like; R3 is a hydrogen atom, a halogen atom, acyloxy represented by (straight-chain or branched C1-8 aliphatic hydrocarbon group) —CO—O—, or the like; and R4 is a hydrogen atom, a halogen atom, C1-6 alkyl, or the like, or alternatively, R4 and R3 together with the carbon atoms on the pyrimidine ring may form a thiophene ring, a pyrrole ring, an imidazole ring, a benzene ring, a pyrimidine ring, a furan ring, a pyrazine ring, or a pyrrolidine ring.

摘要翻译： 由通式[I]表示的新型4-（3-丁炔基）氨基嘧啶衍生物可用作害虫控制剂。 在通式[I]中，R 1是可以含有0至3个杂原子的单环或双环，例如苯基或恶唑基; R2是氢原子，-R，-OR，-C（O）OR，-C（O）NHR，-CONR2（其中R是直链或支链C 1-8烷基等），羟基烷基或 类似; R3是氢原子，卤素原子，由（直链或支链C 1-8脂族烃基）-CO-O-代表的酰氧基等; R4是氢原子，卤素原子，C1-6烷基等，或者R4和R3与嘧啶环上的碳原子一起形成噻吩环，吡咯环，咪唑环， 苯环，嘧啶环，呋喃环，吡嗪环或吡咯烷环。

公开(公告)号：US20120136150A1

公开(公告)日：2012-05-31

申请号：US13378866

申请日：2010-07-15

申请人： Masaaki Sakai ,  Tomoaki Matsumura ,  Satohiro Midorikawa ,  Takashi Nomoto ,  Ryutaro Katsuki ,  Tomoko Muraki

发明人： Masaaki Sakai ,  Tomoaki Matsumura ,  Satohiro Midorikawa ,  Takashi Nomoto ,  Ryutaro Katsuki ,  Tomoko Muraki

IPC分类号： C07D495/04 ,  C07F7/18 ,  C07D239/94 ,  C07D405/12 ,  C07D401/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  C07D239/42 ,  C07D239/48 ,  C07D471/04 ,  C07D401/10 ,  C07D239/70 ,  C07D473/34 ,  C07F7/10

CPC分类号： C07D239/42 ,  A01N43/54 ,  A01N43/90 ,  C07D239/70 ,  C07D239/94 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07F7/081 ,  C07F7/0812 ,  C07F7/1804

摘要： Novel 4-(3-butynyl)aminopyrimidine derivatives represented by general formula [I] are useful as pest control agents. In general formula [I], R1 is a mono- or bi-cyclic ring which may contain 0 to 3 heteroatoms, for example, phenyl or oxazolyl; R2 is a hydrogen atom, —R, —OR, —C(O)OR, —C(O)NHR, —CONR2 (wherein R is straight-chain or branched C1-8 alkyl, or the like), hydroxyalkyl, or the like; R3 is a hydrogen atom, a halogen atom, acyloxy represented by (straight-chain or branched C1-8 aliphatic hydrocarbon group) —CO—O—, or the like; and R4 is a hydrogen atom, a halogen atom, C1-6 alkyl, or the like, or alternatively, R4 and R3 together with the carbon atoms on the pyrimidine ring may form a thiophene ring, a pyrrole ring, an imidazole ring, a benzene ring, a pyrimidine ring, a furan ring, a pyrazine ring, or a pyrrolidine ring.

摘要翻译： 由通式[I]表示的新型4-（3-丁炔基）氨基嘧啶衍生物可用作害虫控制剂。 在通式[I]中，R 1是可以含有0至3个杂原子的单环或双环，例如苯基或恶唑基; R2是氢原子，-R，-OR，-C（O）OR，-C（O）NHR，-CONR2（其中R是直链或支链C 1-8烷基等），羟基烷基或 类似; R3是氢原子，卤素原子，由（直链或支链C 1-8脂族烃基）-CO-O-代表的酰氧基等; R4是氢原子，卤素原子，C1-6烷基等，或者R4和R3与嘧啶环上的碳原子一起形成噻吩环，吡咯环，咪唑环， 苯环，嘧啶环，呋喃环，吡嗪环或吡咯烷环。

公开(公告)号：US09089139B2

公开(公告)日：2015-07-28

申请号：US13979306

申请日：2011-12-27

申请人： Masaaki Sakai ,  Tomoaki Matsumura ,  Satohiro Midorikawa ,  Takashi Nomoto ,  Tomoko Muraki ,  Ryutaro Katsuki

发明人： Masaaki Sakai ,  Tomoaki Matsumura ,  Satohiro Midorikawa ,  Takashi Nomoto ,  Tomoko Muraki ,  Ryutaro Katsuki

IPC分类号： A61K31/517 ,  A01N55/00 ,  A01N37/34 ,  A01N37/50 ,  A01N37/52 ,  A01N43/42 ,  A01N43/50 ,  A01N43/54 ,  A01N43/56 ,  A01N43/653 ,  A01N43/78 ,  A01N43/84 ,  A01N43/90 ,  A01N47/24 ,  A01N47/34 ,  A01N47/44 ,  A01N43/82 ,  A01N53/00 ,  A01N57/26 ,  A01N59/16

CPC分类号： A01N55/00 ,  A01N37/34 ,  A01N37/50 ,  A01N37/52 ,  A01N43/42 ,  A01N43/50 ,  A01N43/54 ,  A01N43/56 ,  A01N43/653 ,  A01N43/78 ,  A01N43/82 ,  A01N43/84 ,  A01N43/90 ,  A01N47/24 ,  A01N47/34 ,  A01N47/44 ,  A01N53/00 ,  A01N57/26 ,  A01N59/16 ,  A01N37/36 ,  A01N37/38 ,  A01N37/46 ,  A01N43/40 ,  A01N47/12 ,  A01N47/14 ,  A01N51/00 ,  A01N57/28 ,  A01N2300/00

摘要： Agri-horticultural pest control compositions having outstanding control effect on pests, in particular, agri-horticultural pests, which comprise as active ingredients one or more 4-(3-butynyl)aminopyrimidine derivatives represented by the general formula [I], namely, where R1 is typically selected from among: a) phenyl c) —SiR5R6R7 (R5, R6, and R7 which may be the same or different represent a linear or branched alkyl having 1-6 carbon atoms, a linear or branched haloalkyl having 1-3 carbon atoms which is substituted by one halogen atom, a linear or branched cyanoalkyl having 1-3 carbon atoms which is substituted by one cyano group, and phenyl); d) hydropgen atom; R2 typically represents a hydrogen atom; R3 typically represents a hydrogen atom; R4 represents a hydrogen atom and one or more agri-horticultural pest control compounds selected from among agri-horticultural antimicrobial compounds, say, multi-site contact active compounds, nucleic acids synthesis inhibitory active compounds, mitosis and cell division inhibitory active compounds, and/or agri-horticultural insecticidal, miticidal or nematicidal compounds, say, acetylcholinesterase inhibitors, GABA-gated chloride antagonists, and sodium channel modulators. Since the 4-(3-butynyl)aminopyrimidine derivatives and the existing antimicrobial active compounds and/or insecticidal active compounds are used in admixture, the 4-(3-butynyl)aminopyrimidine derivatives which are useful as pest control agents, particularly as agri-horticultural pest control agents, need be used in smaller amounts and yet their antimicrobial or insecticidal activity can be improved.

摘要翻译： 具有对害虫，特别是农业园艺害虫具有突出防治效果的农业园艺害虫防治组合物，其包含作为活性成分的一种或多种由通式[I]表示的4-（3-丁炔基）氨基嘧啶衍生物，即其中 R1通常选自：a）苯基c）-SiR 5 R 6 R 7（可以相同或不同的R 5，R 6和R 7表示具有1-6个碳原子的直链或支链烷基，具有1-3个直链或支链烷基的直链或支链烷基） 被一个卤素原子取代的碳原子，被一个氰基取代的具有1-3个碳原子的直链或支链氰基烷基和苯基）; d）氢原子; R2通常表示氢原子; R3通常表示氢原子; R4表示氢原子和一种或多种选自农业园艺抗微生物化合物，例如多位点接触活性化合物，核酸合成抑制活性化合物，有丝分裂和细胞分裂抑制活性化合物的农业园艺害虫控制化合物和/ 或农业园艺杀虫，杀螨或杀线虫化合物，例如乙酰胆碱酯酶抑制剂，GABA门控氯化物拮抗剂和钠通道调节剂。 由于4-（3-丁炔基）氨基嘧啶衍生物和现有的抗微生物活性化合物和/或杀虫活性化合物混合使用，可用作害虫防治剂的4-（3-丁炔基）氨基嘧啶衍生物，特别是农业 - 园艺害虫防治剂需要较少量使用，但可以提高其抗微生物或杀虫活性。

公开(公告)号：US20130296271A1

公开(公告)日：2013-11-07

申请号：US13979306

申请日：2011-12-27

申请人： Masaaki Sakai ,  Tomoaki Matsumura ,  Satohiro Midorikawa ,  Takashi Nomoto ,  Tomoko Muraki ,  Ryutaro Katsuki

发明人： Masaaki Sakai ,  Tomoaki Matsumura ,  Satohiro Midorikawa ,  Takashi Nomoto ,  Tomoko Muraki ,  Ryutaro Katsuki

IPC分类号： A01N43/54 ,  A01N55/00 ,  A01N37/34 ,  A01N47/44 ,  A01N43/50 ,  A01N43/653 ,  A01N43/84 ,  A01N47/24 ,  A01N37/50 ,  A01N37/52 ,  A01N43/78 ,  A01N43/42 ,  A01N47/34 ,  A01N43/82 ,  A01N59/16 ,  A01N57/26 ,  A01N53/00 ,  A01N43/56 ,  A01N43/90

CPC分类号： A01N55/00 ,  A01N37/34 ,  A01N37/50 ,  A01N37/52 ,  A01N43/42 ,  A01N43/50 ,  A01N43/54 ,  A01N43/56 ,  A01N43/653 ,  A01N43/78 ,  A01N43/82 ,  A01N43/84 ,  A01N43/90 ,  A01N47/24 ,  A01N47/34 ,  A01N47/44 ,  A01N53/00 ,  A01N57/26 ,  A01N59/16 ,  A01N37/36 ,  A01N37/38 ,  A01N37/46 ,  A01N43/40 ,  A01N47/12 ,  A01N47/14 ,  A01N51/00 ,  A01N57/28 ,  A01N2300/00

摘要： Agri-horticultural pest control compositions having outstanding control effect on pests, in particular, agri-horticultural pests, which comprise as active ingredients one or more 4-(3-butynyl)aminopyrimidine derivatives represented by the general formula [I], namely, where R1 is typically selected from among: a) phenyl c) —SiR5R6R7 (R5, R6, and R7 which may be the same or different represent a linear or branched alkyl having 1-6 carbon atoms, a linear or branched haloalkyl having 1-3 carbon atoms which is substituted by one halogen atom, a linear or branched cyanoalkyl having 1-3 carbon atoms which is substituted by one cyano group, and phenyl); d) hydropgen atom; R2 typically represents a hydrogen atom; R3 typically represents a hydrogen atom; R4 represents a hydrogen atom and one or more agri-horticultural pest control compounds selected from among agri-horticultural antimicrobial compounds, say, multi-site contact active compouns, nucleic acids synthesis inhibitory active compounds, mitosis and cell divesion inhibitory active compounds, and/or agri-horticultural insecticidal, miticidal or nematicidal compounds, say, acetylcholinesterase inhibitors, GABA-gated chloride antagonists, and sodium channel modulators. Since the 4-(3-butynyl)aminopyrimidine derivatives and the existing antimicrobial active compounds and/or insecticidal active compounds are used in admixture, the 4-(3-butynyl)aminopyrimidine derivatives which are useful as pest control agents, particularly as agri-horticultural pest control agents, need be used in smaller amounts and yet their antimicrobial or insecticidal activity can be improved.

摘要翻译： 具有对害虫，特别是农业园艺害虫具有突出防治效果的农业园艺害虫防治组合物，其包含作为活性成分的一种或多种由通式[I]表示的4-（3-丁炔基）氨基嘧啶衍生物，即其中 R1通常选自：a）苯基c）-SiR 5 R 6 R 7（可以相同或不同的R 5，R 6和R 7表示具有1-6个碳原子的直链或支链烷基，具有1-3个直链或支链烷基的直链或支链烷基） 被一个卤素原子取代的碳原子，被一个氰基取代的具有1-3个碳原子的直链或支链氰基烷基和苯基）; d）氢原子; R2通常表示氢原子; R3通常表示氢原子; R4表示氢原子和一种或多种选自农业园艺抗微生物化合物，例如多位点接触活性化合物，核酸合成抑制活性化合物，有丝分裂和细胞转移抑制活性化合物的农业园艺害虫控制化合物和/ 或农业园艺杀虫，杀螨或杀线虫化合物，例如乙酰胆碱酯酶抑制剂，GABA门控氯化物拮抗剂和钠通道调节剂。 由于4-（3-丁炔基）氨基嘧啶衍生物和现有的抗微生物活性化合物和/或杀虫活性化合物混合使用，可用作害虫防治剂的4-（3-丁炔基）氨基嘧啶衍生物，特别是农业 - 园艺害虫防治剂需要较少量使用，但可以提高其抗微生物或杀虫活性。