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1. 发明申请

US20130345444A1 PRODUCTION METHOD OF OPTICALLY ACTIVE DIHYDROBENZOFURAN DERIVATIVE 有权
标题翻译：光学活性二氢吲哚衍生物的生产方法
公开(公告)号：US20130345444A1
公开(公告)日：2013-12-26
申请号：US13985395
申请日：2012-02-16
申请人： Mitsuhisa Yamano , Mitsutaka Goto , Takeshi Kajiwara , Hiroyuki Maeda , Takahiro Konishi , Misayo Sera , Yuichiro Kondo , Seiji Yamasaki
发明人： Mitsuhisa Yamano , Mitsutaka Goto , Takeshi Kajiwara , Hiroyuki Maeda , Takahiro Konishi , Misayo Sera , Yuichiro Kondo , Seiji Yamasaki
IPC分类号： B01J31/22 , C07C317/18 , C07D307/86
CPC分类号： B01J31/2295 , C07B2200/07 , C07C211/27 , C07C215/32 , C07C315/04 , C07C317/18 , C07D307/80 , C07D307/86 , C07F9/5004 , C07F9/5018 , C07F9/5022 , C07F9/5027 , C07F9/5031 , C07F9/572 , C07F9/5728 , C07F9/65683 , C07F15/006 , C07F17/02
摘要： Provided is a production method of an optically active dihydrobenzofuran derivative. A production method of an optically active form of a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof and the like.
摘要翻译：提供光学活性二氢苯并呋喃衍生物的制备方法。由下式表示的化合物的光学活性形式的制备方法：其中每个符号如说明书中所定义，或其盐等。

2. 发明申请

US20080287438A1 Agent for preventing or treating neuropathy 审中-公开
公开(公告)号：US20080287438A1
公开(公告)日：2008-11-20
申请号：US12219073
申请日：2008-07-15
申请人： Yu Momose , Nozomu Sakai , Tsuyoshi Maekawa , Masatoshi Hazama , Toru Kawamura , Misayo Sera
发明人： Yu Momose , Nozomu Sakai , Tsuyoshi Maekawa , Masatoshi Hazama , Toru Kawamura , Misayo Sera
IPC分类号： A61K31/5377 , A61K31/4196 , A61K31/4164 , A61K31/4152 , C07D403/02 , A61K31/4439 , A61P25/00 , C07D401/02 , C07D249/12 , C07D233/00 , C07D413/02
CPC分类号： C07D231/12 , A61K31/402 , A61K31/415 , A61K31/4155 , A61K31/416 , A61K31/4174 , A61K31/4178 , A61K31/4184 , A61K31/427 , A61K31/4439 , A61K31/66 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07F9/4056 , C07F9/5537 , C07F9/65031 , C07F9/6506 , C07F9/6518 , C07F9/653 , C07F9/65395 , C07F9/65586 , C07F9/657181
摘要： The present invention provides an agent for preventing or treating neuropathy having superior action and low toxicity. This agent comprises a compound represented by the formula: wherein ring A is a 5-membered aromatic heterocycle containing 2 or more nitrogen atoms, which may further have substituent(s); B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a divalent acyclic hydrocarbon group; Z is —O—, —S—, —NR2—, —CONR2— or —NR2CO— (R2 is a hydrogen atom or an optionally substituted alkyl group); Y is a bond or a divalent acyclic hydrocarbon group; R1 is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, provided that when the 5-membered aromatic heterocycle represented by ring A is imidazole, then Z should not be —O—, or a salt thereof.

3. 发明申请

US20060004069A1 Agent for preventing or treating neuropathy 失效
标题翻译：神经病防治药
公开(公告)号：US20060004069A1
公开(公告)日：2006-01-05
申请号：US10532667
申请日：2003-10-30
申请人： Yu Momose , Nozomu Sakai , Tsuyoshi Maekawa , Masatoshi Hazama , Toru Kawamura , Misayo Sera
发明人： Yu Momose , Nozomu Sakai , Tsuyoshi Maekawa , Masatoshi Hazama , Toru Kawamura , Misayo Sera
IPC分类号： A61K31/4196 , A61K31/4164 , A61K31/4152 , C07D43/02
CPC分类号： C07D231/12 , A61K31/402 , A61K31/415 , A61K31/4155 , A61K31/416 , A61K31/4174 , A61K31/4178 , A61K31/4184 , A61K31/427 , A61K31/4439 , A61K31/66 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07F9/4056 , C07F9/5537 , C07F9/65031 , C07F9/6506 , C07F9/6518 , C07F9/653 , C07F9/65395 , C07F9/65586 , C07F9/657181
摘要： The present invention provides an agent for preventing or treating neuropathy having superior action and low toxicity. This agent comprises a compound represented by the formula: wherein ring A is a 5-membered aromatic heterocycle containing 2 or more nitrogen atoms, which may further have substituent(s); B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a divalent acyclic hydrocarbon group; Z is —O—, —S—, —NR2—, —CONR2— or —NR2CO— (R2 is a hydrogen atom or an optionally substituted alkyl group); Y is a bond or a divalent acyclic hydrocarbon group; R1 is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, provided that when the 5-membered aromatic heterocycle represented by ring A is imidazole, then Z should not be —O—, or a salt thereof.
摘要翻译：本发明提供了用于预防或治疗具有优异作用和低毒性的神经病的药剂。该试剂包括由下式表示的化合物：其中环A是含有2个或更多个氮原子的5元芳族杂环，其可进一步具有取代基; B是任选取代的烃基或任选取代的杂环基; X是二价无环烃基; Z是-O - ， - S - ， - NR 2 - ， - CONR 2 - 或-NR 2 CO-（R SUB > 2 是氢原子或任选取代的烷基）; Y是键或二价无环烃基; R 1是任选取代的环状基团，任选取代的氨基或任选取代的酰基，条件是当由环A表示的5元芳族杂环是咪唑时，则Z不应该是 - O-或其盐。

4. 发明申请

US20050171184A1 Process for preparing optically active 2,3-dihydrobenzofuran compounds 失效
标题翻译：光学活性2,3-二氢苯并呋喃化合物的制备方法
公开(公告)号：US20050171184A1
公开(公告)日：2005-08-04
申请号：US11054371
申请日：2005-02-09
申请人： Isao Aoki , Mari Adachi , Hiroyuki Tawada , Makoto Yamashita , Misayo Sera
发明人： Isao Aoki , Mari Adachi , Hiroyuki Tawada , Makoto Yamashita , Misayo Sera
IPC分类号： C07D307/79 , C07D405/04 , C07F9/6574 , A61K31/4035 , C07D45/02
CPC分类号： C07D307/79 , C07B2200/07 , C07D405/04 , C07F9/65742
摘要： A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: [wherein R1 and R2 are each hydrogen or an optionally substituted hydrocarbon group; R3 is an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.
摘要翻译：一种制备光学活性2,3-二氢苯并呋喃化合物的方法，其包括用光学活性酸化合物对其进行光学拆分的2,3-二氢苯并呋喃化合物或其盐进行光学拆分：其中R 1， SUP>和R 2各自为氢或任选取代的烃基; R 3是任选取代的芳族基团; 并且C是除了氨基之外还可以具有取代基的苯环]。该方法可以在工业上有利地生产用于合成可用作神经变性疾病等的预防和/或治疗药物的光学活性2,3-二氢苯并呋喃化合物的中间体。

5. 发明授权

US08822694B2 Process for producing pyrrole compound 有权
标题翻译：制备吡咯化合物的方法
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。

6. 发明申请

US20110306769A1 PROCESS FOR PRODUCING PYRROLE COMPOUND 有权
标题翻译：生产吡咯化合物的方法
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。

7. 发明申请

US20090326229A1 ALPHA-CARBOLINE DERIVATIVES AND METHODS FOR PREPARATION THEREOF 审中-公开
标题翻译： ALPHA-CARBOLINE衍生物及其制备方法
公开(公告)号：US20090326229A1
公开(公告)日：2009-12-31
申请号：US12376068
申请日：2007-08-02
申请人： Masahiro Mizuno , Hideya Mizufune , Misayo Sera , Masahiro Mineno , Tsuyoshi Ueda
发明人： Masahiro Mizuno , Hideya Mizufune , Misayo Sera , Masahiro Mineno , Tsuyoshi Ueda
IPC分类号： C07D471/02 , C07D213/72
CPC分类号： C07D471/04 , C07D213/74 , C07D213/75 , C07D405/12
摘要： To provide methods for preparing alpha-carboline derivatives in few steps, as well as conveniently and industrially advantageously. A method for preparation of a compound represented by Formula (II) or a salt thereof, comprising subjecting a compound represented by Formula (I) or a salt thereof to a ring closure reaction in the presence of a palladium catalyst, a ligand, and a base; a method for preparation of a compound represented by Formula (IX) or a salt thereof, comprising subjecting a compound represented by Formula (VII) or a salt thereof to a ring closure reaction in the presence of a palladium catalyst, a ligand, and a base, and subsequently to an aromatization reaction; and methods for preparation of compounds represented by Formulae (XV), (XVII), and (XIX) or a salt thereof, comprising subjecting respective compounds represented by Formulae (II) and (IX) or a salt thereof to a reaction for introducing a leaving group when necessary, and subsequently to a coupling reaction: wherein the symbols respectively represent the same meaning as defined in the present specification.
摘要翻译：提供在几个步骤中以及方便和工业上有利地制备α-咔啉衍生物的方法。一种制备由式（II）表示的化合物或其盐的方法，包括在钯催化剂，配体和配体存在下，将式（I）表示的化合物或其盐进行闭环反应基础; 一种制备由式（Ⅸ）表示的化合物或其盐的方法，包括在钯催化剂，配体和配体存在下使式（Ⅶ）表示的化合物或其盐进行闭环反应碱，然后进行芳构化反应; 以及由式（XV），（XVII）和（XIX）表示的化合物或其盐制备化合物或其盐的方法，包括使由式（Ⅱ）和（Ⅸ）表示的各种化合物或其盐进行引入在必要时离去基团，随后进行偶联反应：其中符号分别表示与本说明书中定义的相同的含义。

8. 发明授权

US07420070B2 Process for preparing optically active 2,3-dihydrobenzofuran compounds 失效
标题翻译：光学活性2,3-二氢苯并呋喃化合物的制备方法
公开(公告)号：US07420070B2
公开(公告)日：2008-09-02
申请号：US11054371
申请日：2005-02-09
申请人： Isao Aoki , Mari Adachi , Hiroyuki Tawada , Makoto Yamashita , Misayo Sera
发明人： Isao Aoki , Mari Adachi , Hiroyuki Tawada , Makoto Yamashita , Misayo Sera
IPC分类号： C07D405/00 , C07D307/00
CPC分类号： C07D307/79 , C07B2200/07 , C07D405/04 , C07F9/65742
摘要： A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: [wherein R1 and R2 are each hydrogen or an optionally substituted hydrocarbon group; R3 is an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.
摘要翻译：一种制备光学活性2,3-二氢苯并呋喃化合物的方法，其包括用光学活性酸化合物对其进行光学拆分的2,3-二氢苯并呋喃化合物或其盐进行光学拆分：其中R 1， SUP>和R 2各自为氢或任选取代的烃基; R 3是任选取代的芳族基团; 并且C是除了氨基之外还可以具有取代基的苯环]。该方法可以在工业上有利地生产用于合成可用作神经变性疾病等的预防和/或治疗药物的光学活性2,3-二氢苯并呋喃化合物的中间体。

9. 发明申请

US20070238721A1 Highly Selective Novel Amidation Method 审中-公开
标题翻译：高选择性的新型酰胺化方法
公开(公告)号：US20070238721A1
公开(公告)日：2007-10-11
申请号：US11628906
申请日：2005-06-10
申请人： Atsushi Inagaki , Misayo Sera
发明人： Atsushi Inagaki , Misayo Sera
IPC分类号： A61K31/553 , C07D498/00
CPC分类号： C07D267/14 , C07D413/06
摘要： The present invention provides an industrial production method with a short process having a high yield of an aliphatic cyclic carboxamide having carboxyl group, which comprises reacting functional group-selectively using an inexpensive condensing agent without protecting the carboxyl group by esterification, that is, reacting carboxylic acid anhydride obtained by reacting carboxylic acid and tertiary carboxylic acid halide with aliphatic cyclic secondary amine having carboxyl group.
摘要翻译：本发明提供了具有高产率的具有羧基的脂肪族环状羧酰胺的短工艺的工业生产方法，其包括使用廉价的缩合剂选择性地使官能团反应而不通过酯化保护羧基，即使羧基通过羧酸和叔羧酸卤化物与具有羧基的脂族环状仲胺反应获得的酸酐。

10. 发明授权

US06878831B2 Process for preparing optically active 2,3-dihydrobenzofuran compounds 失效
标题翻译：光学活性2,3-二氢苯并呋喃化合物的制备方法
公开(公告)号：US06878831B2
公开(公告)日：2005-04-12
申请号：US10451723
申请日：2001-12-27
申请人： Isao Aoki , Mari Adachi , Hiroyuki Tawada , Makoto Yamashita , Misayo Sera
发明人： Isao Aoki , Mari Adachi , Hiroyuki Tawada , Makoto Yamashita , Misayo Sera
IPC分类号： C07D307/79 , C07D405/04 , C07F9/6574 , C07D307/78
CPC分类号： C07D307/79 , C07B2200/07 , C07D405/04 , C07F9/65742
摘要： A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: [wherein R1 and R2 are each hydrogen or an optionally substituted hydrocarbon group; R3 is an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.
摘要翻译：一种制备光学活性2,3-二氢苯并呋喃化合物的方法，其包括用光学活性酸化合物使其由通式或其盐表示的2,3-二氢苯并呋喃化合物进行光学拆分：[其中R 1和R 2' 2>各自为氢或任选取代的烃基; R 3是任选取代的芳基; 并且C是除了氨基之外还可以具有取代基的苯环]。该方法可以在工业上有利地生产用于合成可用作神经变性疾病等的预防和/或治疗药物的光学活性2,3-二氢苯并呋喃化合物的中间体。

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