公开(公告)号：US20100168173A1

公开(公告)日：2010-07-01

申请号：US12704637

申请日：2010-02-12

申请人： Keigo Tanaka ,  Satoshi Inoue ,  Norio Murai ,  Masayuki Matsukura ,  Kazutaka Nakamoto ,  Shuji Shirotori ,  Shinya Abe

发明人： Keigo Tanaka ,  Satoshi Inoue ,  Norio Murai ,  Masayuki Matsukura ,  Kazutaka Nakamoto ,  Shuji Shirotori ,  Shinya Abe

IPC分类号： A61K31/444 ,  C07D413/04 ,  A61K31/4439 ,  C07D401/14 ,  A61P31/10

CPC分类号： A01N43/56 ,  A01N43/80 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

摘要： An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: wherein R1 represents a hydrogen atom, a halogen atom, an amino group, a C1-6 alkyl group, a C1-6 alkoxy group or a C1-6 alkoxy C1-6 alkyl group; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group or a di C1-6 alkylamino group; one of X and Y is a nitrogen atom while the other is a nitrogen atom or an oxygen atom; ring A represents a 5- or 6-member heteroaryl ring or a benzene ring which may have a halogen atom, or 1 or 2 C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, a sulfur atom, —CH2O—, —OCH2—, —NH—, —CH2NH—, —NHCH2—, —CH2S—, or —SCH2—; R3 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C6-10 aryl group, a 5- or 6-member heteroaryl group, or 5- or 6-member non-aromatic heterocyclic group which may have 1 or 2 substituents; and R4 represents a hydrogen atom or a halogen atom.

公开(公告)号：US08273885B2

公开(公告)日：2012-09-25

申请号：US12440557

申请日：2007-09-11

申请人： Keigo Tanaka ,  Norio Murai ,  Shuji Shirotori ,  Satoshi Nagao ,  Yuzo Watanabe

发明人： Keigo Tanaka ,  Norio Murai ,  Shuji Shirotori ,  Satoshi Nagao ,  Yuzo Watanabe

IPC分类号： C07F5/02

CPC分类号： C07D215/20 ,  C07D307/87 ,  C07D307/92 ,  C07D311/76 ,  C07D491/048 ,  C07F5/02

摘要： Provided is a fluoroboron compound which is highly safe and stable and is capable of forming a cyclic ether-fused ring by the intramolecular alkoxymethylation reaction, or a salt thereof. The compound can be synthesized by the intramolecular alkoxymethylation reaction of a fluoroboron compound represented by the formula (I) or a salt thereof in the presence of a metal catalyst. (wherein the moiety represented by the formula represents an aromatic ring; L represents a substituent such as a halogen atom; R represents a substituted or unsubstituted alkylene group having 1 or 2 carbon atoms; and M represents an alkali metal cation or the like, with the proviso that L and —R—OCH2BF3M are respectively located on contiguous carbon atoms on the aromatic ring, or in the case of a fused aromatic ring, on two carbon atoms adjacent to one carbon at the fused position).

摘要翻译： 本发明提供一种高度安全稳定且能够通过分子内烷氧基甲基化反应形成环状醚稠合环的氟硼烷化合物或其盐。 该化合物可以通过在式（I）表示的氟硼烷化合物或其盐在金属催化剂的存在下的分子内烷氧基甲基化反应来合成。 （式中，由式表示的部分表示芳香环，L表示卤素原子等取代基，R表示取代或未取代的碳原子数1或2的亚烷基，M表示碱金属阳离子等， 条件是L和-R-OCH2BF3M分别位于芳环上的连续碳原子上，或在稠合芳环的情况下位于与稠合位置的一个碳相邻的两个碳原子上）。

公开(公告)号：US08153662B2

公开(公告)日：2012-04-10

申请号：US12704643

申请日：2010-02-12

申请人： Keigo Tanaka ,  Satoshi Inoue ,  Norio Murai ,  Masayuki Matsukura ,  Kazutaka Nakamoto ,  Shuji Shirotori ,  Shinya Abe

发明人： Keigo Tanaka ,  Satoshi Inoue ,  Norio Murai ,  Masayuki Matsukura ,  Kazutaka Nakamoto ,  Shuji Shirotori ,  Shinya Abe

IPC分类号： A61K31/42 ,  A61K31/443 ,  C07D413/14

CPC分类号： A01N43/56 ,  A01N43/80 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

摘要： An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: wherein R1 represents a hydrogen atom, a halogen atom, an amino group, a C1-6 alkyl group, a C1-6 alkoxy group or a C1-6 alkoxy C1-6 alkyl group; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group or a di C1-6 alkylamino group; one of X and Y is a nitrogen atom while the other is a nitrogen atom or an oxygen atom; ring A represents a 5- or 6-member heteroaryl ring or a benzene ring which may have a halogen atom, or 1 or 2 C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, a sulfur atom, —CH2O—, —OCH2—, —NH—, —CH2NH—, —NHCH2—, —CH2S—, or —SCH2—; R3 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C6-10 aryl group, a 5- or 6-member heteroaryl group, or 5- or 6-member non-aromatic heterocyclic group which may have 1 or 2 substituents; and R4 represents a hydrogen atom or a halogen atom.

摘要翻译： 本发明的目的是提供一种具有优异的抗真菌作用并且在其物理性质，安全性和代谢稳定性方面优异的抗真菌剂。 根据本发明，公开了由下式（I）表示的化合物或其盐：其中R1表示氢原子，卤素原子，氨基，C1-6烷基，C1- 6烷氧基或C 1-6烷氧基C 1-6烷基; R2表示氢原子，C1-6烷基，氨基或二C1-6烷基氨基; X和Y之一是氮原子，而另一个是氮原子或氧原子; 环A表示可以具有卤素原子或1或2个C 1-6烷基的5或6元杂芳基环或苯环; Z表示单键，亚甲基，亚乙基，氧原子，硫原子，-CH 2 O - ， - OCH 2 - ， - NH - ， - CH 2 NH - ， - NHCH 2 - ， - CH 2 S-或-SCH 2 - ; R 3表示氢原子，卤素原子，C 1-6烷基，C 3-8环烷基，C 6-10芳基，5-或6-元杂芳基，或5-或6-元非 - 可以具有1或2个取代基的芳族杂环基; R4表示氢原子或卤素原子。

公开(公告)号：US20120029023A1

公开(公告)日：2012-02-02

申请号：US13242702

申请日：2011-09-23

申请人： Keigo TANAKA ,  Satoshi Inoue ,  Norio Murai ,  Masayuki Matsukura ,  Kazutaka Nakamoto ,  Shuji Shirotori ,  Shinya Abe

发明人： Keigo TANAKA ,  Satoshi Inoue ,  Norio Murai ,  Masayuki Matsukura ,  Kazutaka Nakamoto ,  Shuji Shirotori ,  Shinya Abe

IPC分类号： A61K31/4439 ,  A61P31/10 ,  A61K31/444 ,  C07D401/14 ,  C07D401/04

CPC分类号： A01N43/56 ,  A01N43/80 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

摘要： An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: wherein R1, R2, X, Y, ring A, Z, R3 and R4 are as defined in the specification.

摘要翻译： 本发明的目的是提供一种具有优异的抗真菌作用并且在其物理性质，安全性和代谢稳定性方面优异的抗真菌剂。 根据本发明，公开了由下式（I）表示的化合物或其盐：其中R1，R2，X，Y，环A，Z，R3和R4如说明书中所定义。

公开(公告)号：US20100160379A1

公开(公告)日：2010-06-24

申请号：US12704643

申请日：2010-02-12

申请人： Keigo TANAKA ,  Satoshi Inoue ,  Norio Murai ,  Masayuki Matsukua ,  Kazutaka Nakamoto ,  Shuji Shirotori ,  Shinya Abe

发明人： Keigo TANAKA ,  Satoshi Inoue ,  Norio Murai ,  Masayuki Matsukua ,  Kazutaka Nakamoto ,  Shuji Shirotori ,  Shinya Abe

IPC分类号： A61K31/4439 ,  C07D413/04 ,  C07D413/14 ,  A61P31/00

CPC分类号： A01N43/56 ,  A01N43/80 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

摘要： An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: wherein R1 represents a hydrogen atom, a halogen atom, an amino group, a C1-6 alkyl group, a C1-6 alkoxy group or a C1-6 alkoxy C1-6 alkyl group; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group or a di C1-6 alkylamino group; one of X and Y is a nitrogen atom while the other is a nitrogen atom or an oxygen atom; ring A represents a 5- or 6-member heteroaryl ring or a benzene ring which may have a halogen atom, or 1 or 2 C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, a sulfur atom, —CH2O—, —OCH2—, —NH—, —CH2NH—, —NHCH2—, —CH2S—, or —SCH2—; R3 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C6-10 aryl group, a 5- or 6-member heteroaryl group, or 5- or 6-member non-aromatic heterocyclic group which may have 1 or 2 substituents; and R4 represents a hydrogen atom or a halogen atom.

摘要翻译： 本发明的目的是提供一种具有优异的抗真菌作用并且在其物理性质，安全性和代谢稳定性方面优异的抗真菌剂。 根据本发明，公开了由下式（I）表示的化合物或其盐：其中R1表示氢原子，卤素原子，氨基，C1-6烷基，C1- 6烷氧基或C 1-6烷氧基C 1-6烷基; R2表示氢原子，C1-6烷基，氨基或二C1-6烷基氨基; X和Y之一是氮原子，而另一个是氮原子或氧原子; 环A表示可以具有卤素原子或1或2个C 1-6烷基的5或6元杂芳基环或苯环; Z表示单键，亚甲基，亚乙基，氧原子，硫原子，-CH 2 O - ， - OCH 2 - ， - NH - ， - CH 2 NH - ， - NHCH 2 - ， - CH 2 S-或-SCH 2 - ; R 3表示氢原子，卤素原子，C 1-6烷基，C 3-8环烷基，C 6-10芳基，5-或6-元杂芳基，或5-或6-元非 - 可以具有1或2个取代基的芳族杂环基; R4表示氢原子或卤素原子。

公开(公告)号：US07696347B2

公开(公告)日：2010-04-13

申请号：US11886340

申请日：2006-03-13

申请人： Keigo Tanaka ,  Satoshi Inoue ,  Daisuke Ito ,  Norio Murai ,  Yosuke Kaburagi ,  Shuji Shirotori ,  Shuichi Suzuki ,  Yoshiaki Ohashi

发明人： Keigo Tanaka ,  Satoshi Inoue ,  Daisuke Ito ,  Norio Murai ,  Yosuke Kaburagi ,  Shuji Shirotori ,  Shuichi Suzuki ,  Yoshiaki Ohashi

IPC分类号： C07F273/04

CPC分类号： C07F5/02

摘要： The present invention provides compounds which are useful as safe substitutes for the organotin reagent used in coupling reaction for the oxymethylation of aromatic rings, such as alkoxymethylation or hydroxymethylation, with a palladium catalyst and which can dispense with chromatographic purification with silica gel in the production and are suitable for mass production; and compounds applicable even to the oxymethylation of aromatic ring substrates which do not permit coupling reaction by conventional technique or have low reactivity.

摘要翻译： 本发明提供的化合物可用作用于钯催化剂的芳族环的甲基化，例如烷氧基甲基化或羟甲基化的偶联反应中使用的有机锡试剂的安全替代物，并且可以在生产中省去用硅胶进行色谱纯化， 适合批量生产; 以及甚至适用于通过常规技术不能进行偶联反应或具有低反应性的芳环底物的氧甲基化的化合物。

公开(公告)号：US08158657B2

公开(公告)日：2012-04-17

申请号：US12704637

申请日：2010-02-12

申请人： Keigo Tanaka ,  Satoshi Inoue ,  Norio Murai ,  Masayuki Matsukura ,  Kazutaka Nakamoto ,  Shuji Shirotori ,  Shinya Abe

发明人： Keigo Tanaka ,  Satoshi Inoue ,  Norio Murai ,  Masayuki Matsukura ,  Kazutaka Nakamoto ,  Shuji Shirotori ,  Shinya Abe

IPC分类号： A61K31/443 ,  C07D413/04

CPC分类号： A01N43/56 ,  A01N43/80 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

摘要： An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: wherein R1 represents a hydrogen atom, a halogen atom, an amino group, a C1-6 alkyl group, a C1-6 alkoxy group or a C1-6 alkoxy C1-6 alkyl group; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group or a di C1-6 alkylamino group; one of X and Y is a nitrogen atom while the other is a nitrogen atom or an oxygen atom; ring A represents a 5- or 6-member heteroaryl ring or a benzene ring which may have a halogen atom, or 1 or 2 C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, a sulfur atom, —CH2O—, —OCH2—, —NH—, —CH2NH—, —NHCH2—, —CH2S—, or —SCH2—; R3 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C6-10 aryl group, a 5- or 6-member heteroaryl group, or 5- or 6-member non-aromatic heterocyclic group which may have 1 or 2 substituents; and R4 represents a hydrogen atom or a halogen atom.

公开(公告)号：US20100099718A1

公开(公告)日：2010-04-22

申请号：US12442293

申请日：2007-09-20

申请人： Masayuki Matsukura ,  Satoshi Inoue ,  Keigo Tanaka ,  Norio Murai ,  Shuji Shirotori

发明人： Masayuki Matsukura ,  Satoshi Inoue ,  Keigo Tanaka ,  Norio Murai ,  Shuji Shirotori

IPC分类号： A61K31/4439 ,  C07D401/04 ,  A61P31/10

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D417/04

摘要： The present invention provides an antifungal agent that has excellent antifungal action, and is also excellent in terms of its properties, safety, and metabolic stability. The present invention discloses a compound represented by the following formula I or a salt thereof, and an antifungal agent comprising the compound or the salt: wherein R1 represents a hydrogen atom, a halogen atom, an amino group, a C1-6 alkyl group, a C1-6 alkoxy group, or a C1-6-alkoxy-C1-6-alkyl group; R2 represents a hydrogen atom or an amino group; X, Y, Z, and W independently represent a nitrogen atom, an oxygen atom, a sulfur atom, or —CH—, provided that at least two among X, Y, and W are nitrogen atoms; the ring A represents a 5- or 6-membered heteroaryl ring or a benzene ring; Q represents a methylene group, an oxygen atom, —CH2O—, —OCH2—, —NH—, —NHCH2—, or —CH2NH—; and R3 represents a C1-6 alkyl group, a C3-8 cycloalkyl group, a C6-10 aryl group, or a 5- or 6-membered heteroaryl group, each of which may have one or two substituents.

摘要翻译： 本发明提供具有优异抗真菌作用的抗真菌剂，并且在其性质，安全性和代谢稳定性方面也是优异的。 本发明公开了由下式I表示的化合物或其盐，以及包含该化合物或其盐的抗真菌剂：其中R1表示氢原子，卤素原子，氨基，C1-6烷基， C 1-6烷氧基或C 1-6 - 烷氧基-C 1-6 - 烷基; R2表示氢原子或氨基; X，Y，Z和W独立地表示氮原子，氧原子，硫原子或-CH-，条件是X，Y和W中的至少两个是氮原子; 环A表示5-或6-元杂芳基环或苯环; Q表示亚甲基，氧原子，-CH 2 O - ， - OCH 2 - ， - NH - ， - NHCH 2 - 或-CH 2 NH-; 并且R 3表示可以具有一个或两个取代基的C 1-6烷基，C 3-8环烷基，C 6-10芳基或5或6元杂芳基。

公开(公告)号：US20080242859A1

公开(公告)日：2008-10-02

申请号：US11886340

申请日：2006-03-13

申请人： Keigo Tanaka ,  Satoshi Inoue ,  Daisuke Ito ,  Norio Murai ,  Yosuke Kaburagi ,  Shuji Shirotori ,  Shuichi Suzuki ,  Yoshiaki Ohashi

发明人： Keigo Tanaka ,  Satoshi Inoue ,  Daisuke Ito ,  Norio Murai ,  Yosuke Kaburagi ,  Shuji Shirotori ,  Shuichi Suzuki ,  Yoshiaki Ohashi

IPC分类号： C07F5/02

CPC分类号： C07F5/02

摘要： The present invention provides compounds which are useful as safe substitutes for the organotin reagent used in coupling reaction for the oxymethylation of aromatic rings, such as alkoxymethylation or hydroxymethylation, with a palladium catalyst and which can dispense with chromatographic purification with silica gel in the production and are suitable for mass production; and compounds applicable even to the oxymethylation of aromatic ring substrates which do not permit coupling reaction by conventional technique or have low reactivity.

摘要翻译： 本发明提供的化合物可用作用于钯催化剂的芳族环的甲基化，例如烷氧基甲基化或羟甲基化的偶联反应中使用的有机锡试剂的安全替代物，并且可以在生产中省去用硅胶进行色谱纯化， 适合批量生产; 以及甚至适用于通过常规技术不能进行偶联反应或具有低反应性的芳环底物的氧甲基化的化合物。

公开(公告)号：US08841327B2

公开(公告)日：2014-09-23

申请号：US13242702

申请日：2011-09-23

申请人： Keigo Tanaka ,  Satoshi Inoue ,  Norio Murai ,  Masayuki Matsukura ,  Kazutaka Nakamoto ,  Shuji Shirotori ,  Shinya Abe

发明人： Keigo Tanaka ,  Satoshi Inoue ,  Norio Murai ,  Masayuki Matsukura ,  Kazutaka Nakamoto ,  Shuji Shirotori ,  Shinya Abe

IPC分类号： A61K31/4439 ,  C07D401/14 ,  C07D413/14 ,  A01N43/80 ,  C07D413/04 ,  A01N43/56 ,  C07D417/14 ,  C07D401/04

CPC分类号： A01N43/56 ,  A01N43/80 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

摘要： An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: wherein R1, R2, X, Y, ring A, Z, R3 and R4 are as defined in the specification.

摘要翻译： 本发明的目的是提供一种具有优异的抗真菌作用并且在其物理性质，安全性和代谢稳定性方面优异的抗真菌剂。 根据本发明，公开了由下式（I）表示的化合物或其盐：其中R1，R2，X，Y，环A，Z，R3和R4如说明书中所定义。