公开(公告)号：US08822694B2

公开(公告)日：2014-09-02

申请号：US13203441

申请日：2010-02-24

申请人： Tomomi Ikemoto ,  Misayo Sera ,  Naohiro Fukuda

发明人： Tomomi Ikemoto ,  Misayo Sera ,  Naohiro Fukuda

IPC分类号： C07D401/12

CPC分类号： C07D207/337 ,  C07D207/30 ,  C07D207/333 ,  C07D207/34 ,  C07D207/36 ,  C07D207/48 ,  C07D401/12

摘要： The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

摘要翻译： 本发明提供了可用作药物的磺酰基吡咯化合物的制备方法，用于该方法的中间体的制备方法和新的中间体。 本发明涉及一种制备磺酰基吡咯化合物（Ⅷ）的方法，其包括还原化合物（III）并水解还原产物得到化合物（Ⅳ），使化合物（Ⅳ）进行磺酰化反应得到化合物（Ⅵ）， 并使化合物（VI）进行胺化反应。

公开(公告)号：US20110306769A1

公开(公告)日：2011-12-15

申请号：US13203441

申请日：2010-02-24

申请人： Tomomi Ikemoto ,  Hideya Mizufune ,  Toshiaki Nagata ,  Misayo Sera ,  Naohiro Fukuda ,  Takeshi Yamasaki

发明人： Tomomi Ikemoto ,  Hideya Mizufune ,  Toshiaki Nagata ,  Misayo Sera ,  Naohiro Fukuda ,  Takeshi Yamasaki

IPC分类号： C07D401/12 ,  C07D207/36

CPC分类号： C07D207/337 ,  C07D207/30 ,  C07D207/333 ,  C07D207/34 ,  C07D207/36 ,  C07D207/48 ,  C07D401/12

摘要： The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

摘要翻译： 本发明提供了可用作药物的磺酰基吡咯化合物的制备方法，用于该方法的中间体的制备方法和新的中间体。 本发明涉及一种制备磺酰基吡咯化合物（Ⅷ）的方法，其包括还原化合物（III）并水解还原产物得到化合物（Ⅳ），使化合物（Ⅳ）进行磺酰化反应得到化合物（Ⅵ）， 并使化合物（VI）进行胺化反应。

公开(公告)号：US20090054655A1

公开(公告)日：2009-02-26

申请号：US12295779

申请日：2007-04-05

申请人： Tomomi Ikemoto ,  Naohiro Fukuda

发明人： Tomomi Ikemoto ,  Naohiro Fukuda

IPC分类号： C07C317/14 ,  C07C317/04 ,  C07D277/26 ,  C07D333/48 ,  C07D213/24 ,  C07D213/26 ,  C07D213/34

CPC分类号： C07C315/02 ,  C07D213/70 ,  C07D213/71 ,  C07D213/84 ,  C07D277/76 ,  C07D333/48

摘要： The present invention provides a method for producing an organic oxide, wherein a substrate is oxidized using hypohalous acid, hypohalous acid salt, chlorine, bromine or iodine in the presence of water and a catalytic amount of a compound represented by the following formula (I): R1—X1—NY—R2, wherein: X1 represents —CO— or —SO2—; Y represents a hydrogen atom, a potassium atom, a sodium atom, a chlorine atom, a bromine atom or an iodine atom; R1 represents a substituted or unsubstituted hydrocarbon group, —NYR3 group or —OR3 group (in the formulae, R3 represents a substituted or unsubstituted hydrocarbon group, and Y represents the same meaning as defined above); and R2 represents a hydrogen atom or —CO—R4 group (in the formula, R4 represents a substituted or unsubstituted hydrocarbon group, —NYR5 group or —OR5 group (in the formulae, R5 represents a substituted or unsubstituted hydrocarbon group, and Y represents the same meaning as defined above)); or R1 and R4 may bind to each other to form a further substituted or unsubstituted nitrogen-containing heterocyclic ring.

摘要翻译： 本发明提供一种有机氧化物的制造方法，其中在水和催化量的下式（I）表示的化合物的存在下，使用次卤酸，次卤酸，氯，溴或碘氧化底物， ：R1-X1-NY-R2，其中：X1表示-CO-或-SO2-; Y表示氢原子，钾原子，钠原子，氯原子，溴原子或碘原子; R 1表示取代或未取代的烃基，-NYR 3基或-OR 3基（式中，R 3表示取代或未取代的烃基，Y表示与上述相同的含义）。 R2表示氢原子或-CO-R4基团（式中，R4表示取代或未取代的烃基，-NYR5基或-OR5基）（式中，R5表示取代或未取代的烃基，Y表示 与上述定义相同））; 或者R 1和R 4可以彼此结合形成另外的取代或未取代的含氮杂环。

公开(公告)号：US20050165064A1

公开(公告)日：2005-07-28

申请号：US10512285

申请日：2003-04-24

申请人： Masahiro Kajino ,  Masayuki Takizawa ,  Kohei Notoya ,  Hiroshi Nara ,  Tomomi Ikemoto ,  Atsuko Nishiguchi

发明人： Masahiro Kajino ,  Masayuki Takizawa ,  Kohei Notoya ,  Hiroshi Nara ,  Tomomi Ikemoto ,  Atsuko Nishiguchi

IPC分类号： A61K31/4439 ,  A61P1/02 ,  A61P1/04 ,  A61P1/16 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P19/02 ,  A61P19/10 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D401/06 ,  C07D401/14 ,  C07D43/02

CPC分类号： C07D401/14 ,  A61K31/4439 ,  C07D401/06

摘要： The present invention provides a novel thiol derivative [I] which has an excellent matrix metalloprotease inhibiting activity and is useful as a pharmaceutical composition, particularly a therapeutic agent or prophylactic agent for osteoarthritis and rheumatoid arthritis and a salt thereof, the thiol derivative being a compound represented by the formula [I]: wherein ring A represents an optionally substituted aromatic heterocyclic ring; ring B represents an optionally substituted homocyclic or heterocyclic ring; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group, an optionally substituted heterocyclic group or SR2 (wherein R2 represents a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group); X represents an optionally substituted divalent C1-3 aliphatic hydrocarbon group; Y represents an optionally substituted hydrocarbon group, a halogen atom, a carboxy group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, SR3 (wherein R3 represents a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group or an optionally substituted heterocyclic group), an oxo group, a thioxo group, an optionally substituted imino group, a nitro group or a cyano group; and q represents an integer of 0 to 5.

摘要翻译： 本发明提供一种具有优异的基质金属蛋白酶抑制活性的新型硫醇衍生物[I]，可用作药物组合物，特别是用于骨关节炎和类风湿性关节炎的治疗剂或预防剂及其盐，硫醇衍生物为化合物 由式[I]表示：其中环A表示任选取代的芳族杂环; 环B表示任选取代的杂环或杂环; R 1表示氢原子，任选取代的烃基，酰基，任选取代的杂环基或SR 2（其中R 2， 表示氢原子，任选取代的烃基，酰基或任选取代的杂环基）; X表示任选取代的二价C 1-3脂族烃基; Y表示任选取代的烃基，卤素原子，羧基，酰基，任选取代的羟基，任选取代的氨基，SR 3（其中R 3， SUP>表示氢原子，任选取代的烃基，酰基或任选取代的杂环基），氧代基，硫代基，任选取代的亚氨基，硝基或氰基; q表示0〜5的整数。

公开(公告)号：US20050096475A1

公开(公告)日：2005-05-05

申请号：US11010215

申请日：2004-12-10

申请人： Tomomi Ikemoto ,  Tatsuya Ito ,  Kiminori Tomimatsu

发明人： Tomomi Ikemoto ,  Tatsuya Ito ,  Kiminori Tomimatsu

IPC分类号： C07D225/06 ,  C07D313/08 ,  C07D313/20 ,  C07D207/267 ,  C07D333/32 ,  C07D333/38

CPC分类号： C07D225/06 ,  C07D313/08 ,  C07D313/20

摘要： A process suitable for safely mass-producing, through a short step, cyclic compounds useful in medicines, agricultural chemicals, foods, cosmetics, and chemical products or as intermediates therefor. The process, which is for producing a compound represented by the formula: {wherein Z represents an electron-attracting group; W represents optionally substituted ethylene or optionally substituted vinylene; R3 represents hydrogen or an optionally substituted hydrocarbon group; and X represents a divalent group [provided that when W represents optionally substituted vinylene, then —X—CH2-Z is not —X1—X2—CH, -Z (wherein X1 represents sulfur or optionally substituted nitrogen and X2 represents optionally substituted ethylene)]} or a salt thereof, is characterized by subjecting a compound represented by the formula (II) or a salt thereof: (wherein the symbols have the same meanings as the above) to a ring closure reaction in a solvent containing a carbonic diester.

摘要翻译： 一种适用于通过短步安全批量生产用于药物，农药，食品，化妆品和化学产品的环状化合物或其中间体的方法。 该方法用于制备由下式表示的化合物：其中Z表示吸电子基团; W表示任选取代的乙烯或任选取代的亚乙烯基; R 3表示氢或任选取代的烃基; 并且X表示二价基团[条件是当W表示任选取代的亚乙烯基时，则-X-CH 2 -Z不为-X 1 -X 2 - 其中X 1表示硫或任选取代的氮，X 2表示任选取代的乙烯）]}或其盐，其特征在于： 将含有式（II）的化合物或其盐（其中符号具有与上述相同的含义）与含有碳酸二酯的溶剂进行闭环反应。

公开(公告)号：US06864367B2

公开(公告)日：2005-03-08

申请号：US10204315

申请日：2001-02-20

申请人： Tomomi Ikemoto ,  Tatsuya Ito ,  Kiminori Tomimatsu

发明人： Tomomi Ikemoto ,  Tatsuya Ito ,  Kiminori Tomimatsu

IPC分类号： C07D225/06 ,  C07D313/08 ,  C07D313/20 ,  C07D487/00 ,  C07D223/16 ,  C07D313/00 ,  C07D491/00

CPC分类号： C07D225/06 ,  C07D313/08 ,  C07D313/20

摘要： A process suitable for safely mass-producing, through a short step, cyclic compounds useful in medicines, agricultural chemicals, foods, cosmetics, and chemical products or as intermediates therefor. The process, which is for producing a compound represented by the formula: {wherein Z represents an electron-attracting group; W represents optionally substituted ethylene or optionally substituted vinylene; R3 represents hydrogen or an optionally substituted hydrocarbon group; and X represents a divalent group [provided that when W represents optionally substituted vinylene, then —X—CH2—Z is not —X1—X2—CH2—Z (wherein X1 represents sulfur or optionally substituted nitrogen and X2 represents optionally substituted ethylene)]} or a salt thereof, is characterized by subjecting a compound represented by the formula (II) or a salt thereof: (wherein the symbols have the same meanings as the above) to a ring closure reaction in a solvent containing a carbonic diester.

摘要翻译： 一种适用于通过短步安全批量生产用于药物，农药，食品，化妆品和化学产品的环状化合物或其中间体的方法。 该方法用于制备由下式表示的化合物：其中Z表示吸电子基团; W表示任选取代的乙烯或任选取代的亚乙烯基; R 3表示氢或任选取代的烃基; 并且X表示二价基团[条件是当W表示任选取代的亚乙烯基时，则-X-CH 2 -Z不是-X 1 -X 2 -CH 2 -Z（其中X 1表示硫或任选取代的 氮和X 2表示任选取代的乙烯）]}或其盐，其特征在于将式（II）表示的化合物或其盐：（其中符号具有与上述相同的含义） 在含有碳酸二酯的溶剂中进行闭环反应。

公开(公告)号：US20050014813A1

公开(公告)日：2005-01-20

申请号：US10495173

申请日：2002-11-12

申请人： Hiroyuki Tawada ,  Makoto Yamashita ,  Tomomi Ikemoto ,  Atsuko Nishiguchi

发明人： Hiroyuki Tawada ,  Makoto Yamashita ,  Tomomi Ikemoto ,  Atsuko Nishiguchi

IPC分类号： C07D231/20 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D231/04 ,  A61K31/4152

CPC分类号： C07D401/12 ,  C07D231/20 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： As a method capable of conveniently producing a pyrazole compound in a high yield, which is useful as a synthetic intermediate for a pharmaceutical agent such as a therapeutic agent for diabetes and the like, a production method of a compound represented by the formula (I) wherein n is an integer of 1 to 4 and R1 is a. hydrocarbon group optionally having substituents, or a salt thereof, is provided, which includes reacting a compound represented by the formula, (II) wherein Q is a hydroxy group optionally having substituents or an amino group optionally having substituents, R is a hydrocarbon group optionally having substituents and other symbols are as defined above, or a salt thereof, with hydrazine or a salt thereof.

摘要翻译： 作为能够以高收率制备吡唑化合物的方法，作为糖尿病治疗剂等药剂的合成中间体是有用的，由式（I）表示的化合物的制造方法， 其中n为1〜4的整数，R 1为a。 提供任选具有取代基的烃基或其盐，其包括使式（II）表示的化合物，其中Q是任选具有取代基的羟基或任选具有取代基的氨基，R是任选的烃基 具有取代基和其它符号如上所定义，或其盐与肼或其盐反应。

公开(公告)号：US06566535B1

公开(公告)日：2003-05-20

申请号：US10019987

申请日：2001-11-07

申请人： Tatsuya Ito ,  Tomomi Ikemoto ,  Kiminori Tomimatsu

发明人： Tatsuya Ito ,  Tomomi Ikemoto ,  Kiminori Tomimatsu

IPC分类号： C07D33712

CPC分类号： C07D337/08 ,  C07D337/04

摘要： A process for preparing a compound represented by the following formula: wherein each symbol is as defined below, or a salt thereof, characterized by subjecting a compound represented by the following formula: wherein R1 is an electron-attracting group; R2, R3, R4, R5, R6 and R7 are each a hydrogen atom, a halogen atom, an optionally substituted amino group, an optionally substituted hydroxyl group, an optionally substituted thiol group, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group, provided that R6 and R7 may be united to form a ring; and R8 is a hydrogen atom or an optionally substituted hydrocarbon group, or a salt thereof, to a ring-closing reaction.

摘要翻译： 一种制备由下式表示的化合物的方法：其中每个符号如下所定义，或其盐，其特征在于使下式表示的化合物：其中R1是吸电子基团; R2，R3，R4，R5，R6和R7各自为氢原子，卤素原子，任选取代的氨基，任选取代的羟基，任选取代的硫醇基，任选取代的烃基或任选取代的杂环 组合，条件是R 6和R 7可以结合形成环; 并且R8是氢原子或任选取代的烃基或其盐进行闭环反应。

公开(公告)号：US5623069A

公开(公告)日：1997-04-22

申请号：US437984

申请日：1995-05-10

申请人： Akira Haze ,  Hiroyuki Hatano ,  Tomomi Ikemoto ,  Yoshifumi Kitamoto

发明人： Akira Haze ,  Hiroyuki Hatano ,  Tomomi Ikemoto ,  Yoshifumi Kitamoto

IPC分类号： C07D20060101 ,  C07H1/02 ,  C07H19/04 ,  C07H19/10 ,  C07H19/20 ,  C07H19/207 ,  C07H1/00 ,  C07H19/06 ,  C07H19/16

CPC分类号： C07H19/04

摘要： A method of producing 5'-nucleotide, which comprises maintaining a nucleoside suspension in an organic solvent at a temperature not lower than about 20.degree. C., and then subjecting the resultant suspension to a phosphorylatipon of the nucleoside(s).According to the present invention, 5'-nucleotide can be produced from a nucleoside at high purity and high yield in a shortened reaction time, and impurity removal in the nucleotide purification process is easily accomplished.

摘要翻译： 一种生产5'-核苷酸的方法，其包括在不低于约20℃的温度下将核苷悬浮液保持在有机溶剂中，然后使所得悬浮液经受核苷的磷酸化。 根据本发明，在缩短的反应时间内可以以高纯度和高产率从核苷生产5'-核苷酸，并且容易实现核苷酸纯化过程中的杂质去除。

公开(公告)号：US20080009539A1

公开(公告)日：2008-01-10

申请号：US11661183

申请日：2005-08-25

申请人： Tomomi Ikemoto ,  Takeshi Yamasaki

发明人： Tomomi Ikemoto ,  Takeshi Yamasaki

IPC分类号： A61K31/40 ,  A61K31/34 ,  A61P25/00 ,  C07D209/04 ,  C07D307/00

CPC分类号： C07D307/79 ,  C07D307/81 ,  C07D405/04

摘要： A process for the production of an aromatic azo compound having a 2,3-dihydrobenzofuran ring bearing a diazo group at the 5-position of the ring by conducting the diazo coupling of a 2,3-dihydrobenzofuran derivative represented by the general formula (II): [wherein R1 and R2 are each independently C1-6 alkyl; R3 is optionally substituted aryl; and R4, R5 and R6 are each independently hydrogen, C1-6 alkyl, halogeno, C1-6 alkoxy, or C1-6 alkylthio] with a benzenediazonium salt having an electron-withdrawing group at the p- and/or o-position in a mixed solvent composed of water and a polar organic solvent.

摘要翻译： 通过进行由通式（II）表示的2,3-二氢苯并呋喃衍生物的重氮偶联，制备具有环的5-位上具有重氮基的2,3-二氢苯并呋喃环的芳族偶氮化合物的方法 ）：[其中R 1和R 2各自独立地为C 1-6烷基; R 3是任选取代的芳基; 和R 4，R 5和R 6各自独立地为氢，C 1-6烷基，卤代， C 1-6烷氧基或C 1-6烷基硫基]与在混合的p-和/或o位上具有吸电子基团的苯二氮鎓盐 溶剂由水和极性有机溶剂组成。