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1. 发明授权

US06982344B2 Process for preparation of optically active sulfonamides and intermediates for their synthesis 有权
标题翻译：制备光学活性磺酰胺及其合成中间体的方法
公开(公告)号：US06982344B2
公开(公告)日：2006-01-03
申请号：US10399165
申请日：2001-10-17
申请人： Tomomi Ikemoto , Atsuko Nishiguchi , Kiminori Tomimatsu
发明人： Tomomi Ikemoto , Atsuko Nishiguchi , Kiminori Tomimatsu
IPC分类号： C07C311/51 , C07C311/14 , C07C311/28 , C07C303/40 , C07B57/00
CPC分类号： C07C311/51 , C07B2200/07 , C07C303/40 , C07C303/44 , C07C311/14 , C07C2601/16
摘要： A method including resolution of a diastereomeric mixture represented by the formula wherein R1 and R2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, only one of R1 and R2 contains one asymmetric carbon, and Ra is an optically active and optionally substituted hydrocarbon group or an optically active and optionally substituted heterocyclic group, or a salt thereof, to produce the diastereomer having a steric configuration of the asymmetric carbon for R1 or R2 of an R configuration or an S configuration, or a salt thereof.
摘要翻译：一种包括由下式表示的非对映异构体混合物的拆分方法，其中R 1和R 2相同或不同，并且各自为任选取代的烃基或任选取代的杂环基团中，R 1和R 2中只有一个含有一个不对称碳，R a是光学活性和任选取代的烃基或光学活性和任选取代的杂环基或其盐，以产生R构型的R 1或R 2的不对称碳的立体构型的非对映异构体或 S构型或其盐。

2. 发明授权

US06566535B1 Processes for the preparation of 2,3-dihydrothiepine derivatives 失效
标题翻译： 2,3-二氢硫嘌呤衍生物的制备方法
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。

3. 发明授权

US07038042B2 Process for producing cyclic compound 失效
标题翻译：环状化合物的制备方法
公开(公告)号：US07038042B2
公开(公告)日：2006-05-02
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： C07D487/00 , C07C313/00
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 - 2 - -CH 2 - ，其中X 1表示硫或任选取代的氮，X 2表示任选取代的亚乙基）]} 或其盐的特征在于，在含有碳酸二酯的溶剂中使式（II）表示的化合物或其盐（其中符号具有与上述相同的含义）进行闭环反应。

4. 发明授权

US06743924B2 Method for producing 1-substituted-1,2,3-triazole derivative 失效
标题翻译： 1-取代-1,2,3-三唑衍生物的制备方法
公开(公告)号：US06743924B2
公开(公告)日：2004-06-01
申请号：US10019264
申请日：2002-04-19
申请人： Tomomi Ikemoto , Tatsuya Ito , Kiminori Tomimatsu , Yasuhiro Sawai , Hirohiko Nishiyama , Yasushi Isogami
发明人： Tomomi Ikemoto , Tatsuya Ito , Kiminori Tomimatsu , Yasuhiro Sawai , Hirohiko Nishiyama , Yasushi Isogami
IPC分类号： C07D24904
CPC分类号： C07D249/04
摘要： A method for producing a compound of the formula: (1) in a secondary or tertiary alcohol in the presence of a base, or (2) in the absence of a base is provided. According to this method, a 1-substituted-1,2,3-triazole compound having a tyrosine kinase inhibitory action can be produced efficiently in a high yield at an industrial large scale by a convenient method
摘要翻译：制备下式化合物的方法：（1）在仲醇或叔醇中，在碱的存在下，或（2）在不存在碱的情况下。根据该方法，可以通过方便的方法以工业大规模高效率地产生具有酪氨酸激酶抑制作用的1-取代-1,2,3-三唑化合物

5. 发明申请

US20050096475A1 Process for producing cyclic compound 失效
标题翻译：环状化合物的制备方法
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。

6. 发明授权

US06864367B2 Process for producing cyclic compound 失效
标题翻译：环状化合物的制备方法
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。

7. 发明申请

US20050107606A1 Process for producing optically active sulfoxide derivative 审中-公开
标题翻译：光学活性亚砜衍生物的制备方法
公开(公告)号：US20050107606A1
公开(公告)日：2005-05-19
申请号：US10506955
申请日：2003-03-11
申请人： Hiroyuki Tawada , Tomomi Ikemoto , Atsuko Nishiguchi , Tatsuya Ito , Mari Adachi
发明人： Hiroyuki Tawada , Tomomi Ikemoto , Atsuko Nishiguchi , Tatsuya Ito , Mari Adachi
IPC分类号： C07D233/64 , A61K31/4164 , A61K31/55 , A61P43/00 , C07D225/06 , C07D233/54 , C07D403/12 , C07D43/02
CPC分类号： C07D233/64 , C07D225/06 , C07D403/12 , Y02P20/582
摘要： A process for preparing an optically active sulfoxide derivative (I) having CCR5 antagonism without causing side reactions such as racemization and Pummerer rearrangement, which comprises reacting a compound (II) with a compound (III) as shown by the following scheme: wherein R1 represents hydrogen, an aliphatic hydrocarbon group or an aromatic group; R2 represents halogeno, alkyl, hydroxyl, amino, an aromatic group, etc.; R3 represents a 5- or 6-membered ring; R4 represents hydrogen, alkyl, alkoxy or halogeno; R5 represents hydrogen, a hydrocarbon group, a heterocyclic group, acyl, etc.; ring A represents an optionally substituted benzene ring; X represents a bond or divalent group comprising a linear part constituted of 1 to 4 atoms; m represents an integer of 1 to 5; n represents an integer of 0 to 3; p represents an integer of 0 to 2; and *1 represents an asymmetric center.
摘要翻译：一种制备具有CCR5拮抗作用的光学活性亚砜衍生物（I）的方法，不会引起副反应，例如外消旋化和Pummerer重排，其包括使化合物（II）与化合物（III）反应，如下列方案所示：其中R SUP> 1表示氢，脂族烃基或芳基; R 2表示卤代，烷基，羟基，氨基，芳基等; R 3表示5或6元环; R 4表示氢，烷基，烷氧基或卤代; R 5表示氢，烃基，杂环基，酰基等; 环A表示任选取代的苯环; X表示包含由1至4个原子构成的直链部分的键或二价基团; m表示1〜5的整数， n表示0〜3的整数， p表示0〜2的整数，和* 1 表示不对称中心。

8. 发明申请

US20050165064A1 Novel thiol derivative, process for producing the same and use thereof 审中-公开
标题翻译：新型硫醇衍生物，其制备方法及其用途
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。

9. 发明申请

US20050014813A1 Process for production of pyrazole compounds 审中-公开
标题翻译：吡唑化合物的制备方法
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。

10. 发明申请

US20080009539A1 Azo Compounds and Process for Production Thereof 失效
标题翻译：偶氮化合物及其制备方法
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。

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