公开(公告)号：US5719145A

公开(公告)日：1998-02-17

申请号：US699346

申请日：1996-08-19

申请人： Hiroyuki Yamashita ,  Kunio Okumura ,  Toshiyuki Shimazaki ,  Akihito Kanematsu ,  Yoji Aoki ,  Yuki Nakajima ,  Kouhei Yazawa ,  Kenji Kibayashi

发明人： Hiroyuki Yamashita ,  Kunio Okumura ,  Toshiyuki Shimazaki ,  Akihito Kanematsu ,  Yoji Aoki ,  Yuki Nakajima ,  Kouhei Yazawa ,  Kenji Kibayashi

IPC分类号： C07C257/18 ,  C07D213/40 ,  C07D217/04 ,  C07D295/195 ,  C07D307/52 ,  C07D311/58 ,  C07D333/36 ,  C07D405/12 ,  C07D407/12 ,  A61K31/54 ,  A61K31/535 ,  C07D311/04 ,  C07D311/76

CPC分类号： C07D213/40 ,  C07C257/18 ,  C07D217/04 ,  C07D295/195 ,  C07D307/52 ,  C07D311/58 ,  C07D333/36 ,  C07D405/12 ,  C07D407/12

摘要： The invention relates to a substituted amidine derivative which has an excellent platelet aggregation inhibiting action on the basis of fibrinogen antagonism and is particularly excellent in effectiveness on oral administration, and the platelet aggregation inhibitor containing the substituted amidine derivative of the invention as an effective ingredient is effective for prevention and treatment of thrombosis, and restenosis or reocclusion after percutaneous transluminal coronary angioplasty or percutaneous transluminal coronary recanalization.

摘要翻译： 本发明涉及一种基于纤维蛋白原拮抗作用而具有优异的血小板聚集抑制作用的取代脒衍生物，口服给药特异性优异，含有本发明取代脒衍生物作为有效成分的血小板聚集抑制剂为 经皮腔内冠状动脉血管成形术或经皮冠状动脉冠状动脉再通后有效预防和治疗血栓形成，再狭窄或再狭窄。

公开(公告)号：US20110015406A1

公开(公告)日：2011-01-20

申请号：US12922959

申请日：2009-03-11

申请人： Hideki Umetani ,  Takeshi Kakimoto ,  Yoji Aoki

发明人： Hideki Umetani ,  Takeshi Kakimoto ,  Yoji Aoki

IPC分类号： C07D231/12 ,  C07C229/30

CPC分类号： C07C227/16 ,  C07D231/14 ,  C07C229/30

摘要： A halogenating agent is added to a mixture including a base, a fluoroalkylcarboxylic acid derivative and an acrylate derivative to produce a fluoroaclyacetic acid derivative represented by the following Formula (3): wherein Rf represents a fluorine containing alkyl group, R1 and R2 represent a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, an arylalkyl group or an acyl group, or together represent an atomic group that forms a 5- or 6-membered ring containing a nitrogen atom to which R1 and R2 are bonded; R3 represents a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, or an arylalkyl group; and R4 represents an alkyl group, a cycloalkyl group, an aryl group, or an aryl alkyl group.

摘要翻译： 将卤化剂加入到包含碱，氟代烷基羧酸衍生物和丙烯酸酯衍生物的混合物中以制备由下式（3）表示的氟代乙酸衍生物：其中Rf表示含氟烷基，R 1和R 2表示氢 原子，烷基，环烷基，芳基，芳基烷基或酰基，或者一起表示与R 1和R 2结合的含有氮原子的5元或6元环的原子团; R3表示氢原子，烷基，环烷基，芳基或芳基烷基; R4表示烷基，环烷基，芳基或芳基烷基。

公开(公告)号：US20090326247A1

公开(公告)日：2009-12-31

申请号：US12514090

申请日：2007-10-24

申请人： Takeshi Kakimoto ,  Yoji Aoki ,  Daisuke Ura ,  Miki Enomoto ,  Hisato Kamekawa ,  Toshio Kitashima

发明人： Takeshi Kakimoto ,  Yoji Aoki ,  Daisuke Ura ,  Miki Enomoto ,  Hisato Kamekawa ,  Toshio Kitashima

IPC分类号： C07D333/42

CPC分类号： C07B61/00 ,  C07D333/36 ,  Y02P20/55

摘要： The present invention provides a method of producing a 2-alkyl-3-aminothiophene derivative represented by formula (2) by reducing at least one of the 2-alkenyl-3-aminothiophene derivatives represented by formulae (1a) to (1d), or a mixture thereof, or a salt thereof, without using a protecting group for an amino group: wherein in formulae (1a) to (1d), R1 to R4 each independently represents a hydrogen atom, an alkyl group of 1 to 12 carbon atoms or the like; and R5 and R6 each independently represents a hydrogen atom, a halogen atom, an alkyl group of 1 to 12 carbon atoms or the like. According to the invention, a 2-alkyl-3-aminothiophene derivative usable as an intermediate of agricultural chemicals can be produced by a cost-efficient industrial process, without the use of a high-cost protective group for an amino group.

摘要翻译： 本发明提供通过还原由式（1a）〜（1d）表示的2-烯基-3-氨基噻吩衍生物中的至少一种或式（1a）〜（1d）所示的2-烷基-3-氨基噻吩衍生物，或 其混合物或其盐，不使用氨基的保护基团：其中在式（1a）至（1d）中，R 1至R 4各自独立地表示氢原子，1至12个碳原子的烷基或 类似; R 5和R 6各自独立地表示氢原子，卤素原子，碳原子数1〜12的烷基等。 根据本发明，可以通过成本效益高的工业过程制造可用作农药中间体的2-烷基-3-氨基噻吩衍生物，而不使用高成本的氨基保护基。

公开(公告)号：US08367846B2

公开(公告)日：2013-02-05

申请号：US12762083

申请日：2010-04-16

申请人： Yasuaki Fukazawa ,  Yoji Aoki ,  Haruko Mita ,  Hironori Komatsu

发明人： Yasuaki Fukazawa ,  Yoji Aoki ,  Haruko Mita ,  Hironori Komatsu

IPC分类号： C07D231/00

CPC分类号： C07C205/15 ,  C07C205/03 ,  C07C205/08 ,  C07C205/40 ,  C07D231/12 ,  C07D333/36 ,  C07D333/42

摘要： The present invention provides a method of producing 2-alkyl-3-aminothiophene derivative represented by Formula (4), the method comprising oxidizing a compound represented by the following Formula (1) to produce a compound represented by the following Formula (3) and reducing the compound represented by the following Formula (3): wherein in Formula (1), Formula (3), and Formula (4), R represents an alkyl group, a cycloalkyl group, or a bicycloalkyl group; and X represents a hydroxyl group, a halogen atom acyloxy group, an alkylsulfonyl group, or an arylsulfonyl group.

摘要翻译： 本发明提供一种制备由式（4）表示的2-烷基-3-氨基噻吩衍生物的方法，该方法包括将由下式（1）表示的化合物氧化以制备由下式（3）表示的化合物和 还原由下式（3）表示的化合物：其中在式（1），式（3）和式（4）中，R表示烷基，环烷基或双环烷基; X表示羟基，卤原子酰氧基，烷基磺酰基或芳基磺酰基。

公开(公告)号：US20110201687A1

公开(公告)日：2011-08-18

申请号：US13016604

申请日：2011-01-28

申请人： Yumi Kobayashi ,  Hidenori Daido ,  Hiroyuki Katsuta ,  Michikazu Nomura ,  Hidetaka Tsukada ,  Atsushi Hirabayashi ,  Yusuke Takahashi ,  Yoji Aoki ,  Atsuko Kawahara ,  Yasuaki Fukazawa ,  Mai Hirose

发明人： Yumi Kobayashi ,  Hidenori Daido ,  Hiroyuki Katsuta ,  Michikazu Nomura ,  Hidetaka Tsukada ,  Atsushi Hirabayashi ,  Yusuke Takahashi ,  Yoji Aoki ,  Atsuko Kawahara ,  Yasuaki Fukazawa ,  Mai Hirose

IPC分类号： A61K31/167 ,  C07C237/42 ,  A01N37/22 ,  A61P33/14 ,  A01P7/02

CPC分类号： A01N37/22 ,  A01N37/46 ,  A01N43/40 ,  A01N43/78 ,  A61K31/167 ,  C07C233/88 ,  C07C237/42 ,  C07C255/57 ,  C07C255/60 ,  C07D213/82

摘要： An amide derivative represented by the following Formula (1) is provided as an amide derivative showing a significantly excellent effect for a pest control action.In the following Formula (1), A represents a carbon atom, a nitrogen atom, or the like, and K represents a non-metal atomic group necessary for forming a cyclic linking group derived from benzene or a heterocyclie. X represents a halogen atom or the like; n represents an integer of from 0 to 4. R1 and R2 represent hydrogen atoms, alkyl groups, or the like. T represents —C(=G1)-Q1 or —C(=G1)-G2Q2, and G1 to G3 each represent oxygen atoms or the like. Q1 and Q2 each represent a hydrogen atom, an alkyl group, an aryl group, or the like. Y1 and Y5 each represent a halogen atom or the like, Y2 and Y4 each represent a hydrogen atom or the like, and Y3 represents a C2-C5 haloalkyl group.

摘要翻译： 提供由下式（1）表示的酰胺衍生物作为酰胺衍生物，其对害虫防治作用显示出显着优异的效果。 在下式（1）中，A表示碳原子，氮原子等，K表示形成来自苯或杂环的环状连接基所需的非金属原子团。 X表示卤素原子等; n表示0〜4的整数.R 1，R 2表示氢原子，烷基等。 T表示-C（= G1）-Q1或-C（= G1）-G2Q2，并且G1至G3各自表示氧原子等。 Q1和Q2各自表示氢原子，烷基，芳基等。 Y 1和Y 5各自表示卤素原子等，Y 2和Y 4各自表示氢原子等，Y 3表示C 2〜C 5卤代烷基。

公开(公告)号：US07884216B2

公开(公告)日：2011-02-08

申请号：US12527739

申请日：2008-02-13

申请人： Hideki Umetani ,  Takeshi Kakimoto ,  Yoji Aoki

发明人： Hideki Umetani ,  Takeshi Kakimoto ,  Yoji Aoki

IPC分类号： C07D231/10 ,  A61K31/415 ,  A01N43/56

CPC分类号： C07D231/14 ,  C07D231/16

摘要： The present invention provides a fluorine-containing pyrazolecarbonitrile derivative and a method for producing the same, and a fluorine-containing pyrazolecarboxylic acid derivative obtained by using the fluorine-containing pyrazolecarbonitrile derivative and a method for producing the same.A fluorine-containing acyacrylonitrile derivative prepared from a fluoroacyl derivative and an aminoacrylonitrile derivative, is reacted with a hydrazine derivative to produce a fluorine-containing pyrazolecarbonitrile derivative represented by Formula (1). In Formula (1), Rf represents an alkyl group having 1 to 6 carbon atoms and substituted with at least one fluorine atom; R1 represents an alkyl group having 1 to 6 carbon atoms and R2 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like.The fluorine-containing pyrazolecarbonitrile derivative represented by Formula (1) is reacted with water to produce a fluorine-containing pyrazolecarboxylic acid derivative.

摘要翻译： 本发明提供一种含氟吡唑腈衍生物及其制造方法，使用含氟吡唑腈衍生物得到的含氟吡唑羧酸衍生物及其制造方法。 将由氟代酰基衍生物和氨基丙烯腈衍生物制备的含氟丙烯腈衍生物与肼衍生物反应以制备由式（1）表示的含氟吡唑腈衍生物。 在式（1）中，R f表示碳原子数为1〜6的烷基，被至少一个氟原子取代; R1表示碳原子数1〜6的烷基，R2表示氢原子，碳原子数1〜6的烷基等。 由式（1）表示的含氟吡唑腈衍生物与水反应生成含氟吡唑羧酸衍生物。

公开(公告)号：US06417368B1

公开(公告)日：2002-07-09

申请号：US09646042

申请日：2000-11-08

申请人： Shu Kobayashi ,  Yoji Aoki

发明人： Shu Kobayashi ,  Yoji Aoki

IPC分类号： C07C25124

CPC分类号： C08F8/30 ,  C07B2200/11 ,  C07C227/10 ,  C07C227/16 ,  C07C229/28 ,  C07C229/34 ,  C07C251/24 ,  C07C327/22 ,  C07C2601/14 ,  C07D213/55 ,  C07D213/74 ,  C40B40/00 ,  C40B50/14

摘要： The invention provides a resin-immobilized imine represented by the following formula: P—Q—N—═CH—R   I [in the formula, P represents the principal chain of a resin polymer; Q represents a substituted or unsubstituted hydrocarbon side chain or a substituted or unsubstituted hydrocarbon side chain with a heteroatom interposed therein; R represents a substituted or unsubstituted hydrocarbon group or heterocyclic group] and a resin-immobilized &bgr;-aminocarbonyl compound of the following formula: which can be released as &bgr;-aminocarbonyl compound from the solid phase; and the invention also provide a resin-immobilized amine of the following formula: —P—Q1—O—Q2—NH2   III [Q1 and Q2 independently represent a hydrocarbon chain such as arylene, alkylenearylene or arylenealkylene], which is essential for solid state synthesis; and the invention has enabled the solid state synthesis of &bgr;-aminocarbonyl compound by the application of iminoaldol reaction.

摘要翻译： 本发明提供由下式表示的固化有树脂的亚胺：[式中，P表示树脂聚合物的主链; Q表示取代或未取代的烃侧链或其中插入有杂原子的取代或未取代的烃侧链; R表示取代或未取代的烃基或杂环基]和下式的树脂固定的β-氨基羰基化合物：其可从固相作为β-氨基羰基化合物释放; 本发明还提供下式的树脂固定胺：[Q1和Q2独立地表示烃链如亚芳基，亚烷基亚芳基或亚芳基亚烷基]，这对于固态合成是必需的; 本发明通过应用亚氨基醛醇反应使得β-氨基羰基化合物的固态合成成为可能。

公开(公告)号：US08686044B2

公开(公告)日：2014-04-01

申请号：US13016604

申请日：2011-01-28

申请人： Yumi Kobayashi ,  Hidenori Daido ,  Hiroyuki Katsuta ,  Michikazu Nomura ,  Hidetaka Tsukada ,  Atsushi Hirabayashi ,  Yusuke Takahashi ,  Yoji Aoki ,  Atsuko Kawahara ,  Yasuaki Fukazawa ,  Mai Hirose

发明人： Yumi Kobayashi ,  Hidenori Daido ,  Hiroyuki Katsuta ,  Michikazu Nomura ,  Hidetaka Tsukada ,  Atsushi Hirabayashi ,  Yusuke Takahashi ,  Yoji Aoki ,  Atsuko Kawahara ,  Yasuaki Fukazawa ,  Mai Hirose

IPC分类号： A01N37/18 ,  A61K31/16 ,  A61K31/165

CPC分类号： A01N37/22 ,  A01N37/46 ,  A01N43/40 ,  A01N43/78 ,  A61K31/167 ,  C07C233/88 ,  C07C237/42 ,  C07C255/57 ,  C07C255/60 ,  C07D213/82

摘要： An amide derivative represented by the following Formula (1) is provided as an amide derivative showing a significantly excellent effect for a pest control action.In the following Formula (1), A represents a carbon atom, a nitrogen atom, or the like, and K represents a non-metal atomic group necessary for forming a cyclic linking group derived from benzene or a heterocyclie. X represents a halogen atom or the like; n represents an integer of from 0 to 4. R1 and R2 represent hydrogen atoms, alkyl groups, or the like. T represents —C(=G1)-Q1 or —C(=G1)-G2Q2, and G1 to G3 each represent oxygen atoms or the like. Q1 and Q2 each represent a hydrogen atom, an alkyl group, an aryl group, or the like. Y1 and Y5 each represent a halogen atom or the like, Y2 and Y4 each represent a hydrogen atom or the like, and Y3 represents a C2-C5 haloalkyl group.

摘要翻译： 提供由下式（1）表示的酰胺衍生物作为酰胺衍生物，其对害虫防治作用显示出显着优异的效果。 在下式（1）中，A表示碳原子，氮原子等，K表示形成来自苯或杂环的环状连接基所需的非金属原子团。 X表示卤素原子等; n表示0〜4的整数.R 1，R 2表示氢原子，烷基等。 T表示-C（= G1）-Q1或-C（= G1）-G2Q2，并且G1至G3各自表示氧原子等。 Q1和Q2各自表示氢原子，烷基，芳基等。 Y 1和Y 5各自表示卤素原子等，Y 2和Y 4各自表示氢原子等，Y 3表示C 2〜C 5卤代烷基。

公开(公告)号：US20100016612A1

公开(公告)日：2010-01-21

申请号：US12527739

申请日：2008-02-13

申请人： Hideki Umetani ,  Takeshi Kakimoto ,  Yoji Aoki

发明人： Hideki Umetani ,  Takeshi Kakimoto ,  Yoji Aoki

IPC分类号： C07D231/14

CPC分类号： C07D231/14 ,  C07D231/16

摘要： The present invention provides a fluorine-containing pyrazolecarbonitrile derivative and a method for producing the same, and a fluorine-containing pyrazolecarboxylic acid derivative obtained by using the fluorine-containing pyrazolecarbonitrile derivative and a method for producing the same.A fluorine-containing acyacrylonitrile derivative prepared from a fluoroacyl derivative and an aminoacrylonitrile derivative, is reacted with a hydrazine derivative to produce a fluorine-containing pyrazolecarbonitrile derivative represented by Formula (1). In Formula (1), Rf represents an alkyl group having 1 to 6 carbon atoms and substituted with at least one fluorine atom; R1 represents an alkyl group having 1 to 6 carbon atoms and R2 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like.The fluorine-containing pyrazolecarbonitrile derivative represented by Formula (1) is reacted with water to produce a fluorine-containing pyrazolecarboxylic acid derivative.

摘要翻译： 本发明提供一种含氟吡唑腈衍生物及其制造方法，使用含氟吡唑腈衍生物得到的含氟吡唑羧酸衍生物及其制造方法。 将由氟代酰基衍生物和氨基丙烯腈衍生物制备的含氟丙烯腈衍生物与肼衍生物反应以制备由式（1）表示的含氟吡唑腈衍生物。 在式（1）中，R f表示碳原子数为1〜6的烷基，被至少一个氟原子取代; R1表示碳原子数1〜6的烷基，R2表示氢原子，碳原子数1〜6的烷基等。 由式（1）表示的含氟吡唑腈衍生物与水反应生成含氟吡唑羧酸衍生物。

公开(公告)号：US20100010216A1

公开(公告)日：2010-01-14

申请号：US12521436

申请日：2007-12-18

申请人： Hideki Umetani ,  Yoji Aoki ,  Takeshi Kakimoto

发明人： Hideki Umetani ,  Yoji Aoki ,  Takeshi Kakimoto

IPC分类号： C01C3/14 ,  C07D207/04 ,  C07D295/14

CPC分类号： C07C255/30 ,  C07C2601/14 ,  C07D295/145

摘要： The invention provides a 2-fluorinated acyl-3-aminoacrylonitrile derivative, and a method for producing the same. A desired 2-fluorinated acyl-3-aminoacrylonitrile derivative represented by the following Formula (3) is obtained by reacting a fluorinated acyl derivative with an aminoacrylonitrile derivative. In Formula (3), Rf represents an alkyl group having 1 to 6 carbon atoms which is substituted with at least one fluorine atom, R1 and R2 each independently represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like, and R3 represents an alkyl group having 1 to 6 carbon atoms or the like.

摘要翻译： 本发明提供2-氟化的酰基-3-氨基丙烯腈衍生物及其制备方法。 通过使氟代酰基衍生物与氨基丙烯腈衍生物反应，获得由下式（3）表示的所需2-氟化酰基-3-氨基丙烯腈衍生物。 在式（3）中，R f表示被至少一个氟原子取代的具有1〜6个碳原子的烷基，R 1和R 2各自独立地表示氢原子，碳原子数1〜6的烷基等， R3表示碳原子数1〜6的烷基等。