WO2009041453A1 - 二環性γ－アミノ酸誘導体 - Google Patents

二環性γ－アミノ酸誘導体 Download PDF

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Publication number
WO2009041453A1
WO2009041453A1 PCT/JP2008/067223 JP2008067223W WO2009041453A1 WO 2009041453 A1 WO2009041453 A1 WO 2009041453A1 JP 2008067223 W JP2008067223 W JP 2008067223W WO 2009041453 A1 WO2009041453 A1 WO 2009041453A1
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WO
WIPO (PCT)
Prior art keywords
bicyclic
amino acid
acid derivative
hydrogen atom
formula
Prior art date
Application number
PCT/JP2008/067223
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English (en)
French (fr)
Inventor
Kousei Shimada
Asuka Kawamura
Naohisa Arakawa
Yuki Domon
Original Assignee
Daiichi Sankyo Company, Limited
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to AU2008304933A priority Critical patent/AU2008304933B2/en
Priority to JP2009534336A priority patent/JP4479974B2/ja
Application filed by Daiichi Sankyo Company, Limited filed Critical Daiichi Sankyo Company, Limited
Priority to EP08833399.2A priority patent/EP2192109B1/en
Priority to SI200831100T priority patent/SI2192109T1/sl
Priority to NZ584699A priority patent/NZ584699A/en
Priority to KR1020137020763A priority patent/KR101409079B1/ko
Priority to CA2701110A priority patent/CA2701110C/en
Priority to KR1020107006640A priority patent/KR101335784B1/ko
Priority to BRPI0818193A priority patent/BRPI0818193B8/pt
Priority to DK08833399.2T priority patent/DK2192109T3/da
Priority to CN200880118892.8A priority patent/CN101878193B/zh
Priority to MX2010003394A priority patent/MX2010003394A/es
Priority to PL08833399T priority patent/PL2192109T3/pl
Priority to BR122013020635-3A priority patent/BR122013020635A2/pt
Priority to ES08833399T priority patent/ES2433890T3/es
Publication of WO2009041453A1 publication Critical patent/WO2009041453A1/ja
Priority to US12/714,267 priority patent/US7947738B2/en
Priority to ZA2010/02013A priority patent/ZA201002013B/en
Priority to IL204621A priority patent/IL204621A/en
Priority to HK10106099.5A priority patent/HK1139381A1/xx
Priority to PH12013501663A priority patent/PH12013501663A1/en
Priority to HRP20130935AT priority patent/HRP20130935T1/hr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/587—Unsaturated compounds containing a keto groups being part of a ring
    • C07C49/613—Unsaturated compounds containing a keto groups being part of a ring polycyclic
    • C07C49/617—Unsaturated compounds containing a keto groups being part of a ring polycyclic a keto group being part of a condensed ring system
    • C07C49/623—Unsaturated compounds containing a keto groups being part of a ring polycyclic a keto group being part of a condensed ring system having two rings
    • C07C49/627—Unsaturated compounds containing a keto groups being part of a ring polycyclic a keto group being part of a condensed ring system having two rings the condensed ring system containing seven carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/32—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing rings other than six-membered aromatic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/221—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/57—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C323/58—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups with amino groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/04—Systems containing only non-condensed rings with a four-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/14—All rings being cycloaliphatic
    • C07C2602/20—All rings being cycloaliphatic the ring system containing seven carbon atoms
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/93—Spiro compounds
    • C07C2603/94—Spiro compounds containing "free" spiro atoms

Abstract

α2δリガンドとして優れた活性を有する二環性γ－アミノ酸誘導体を提供すること。 一般式（Ｉ）： 【化１】   　  ［式中、R1、R2、R2’、R4、R5、R6、R7、R8およびR8’は、水素原子等であり、R3は、水素原子、ハロゲン原子、C1－C6アルキル基等である］で表される化合物。
PCT/JP2008/067223 2007-09-28 2008-09-25 二環性γ－アミノ酸誘導体 WO2009041453A1 (ja)

Priority Applications (21)

Application Number Priority Date Filing Date Title
CN200880118892.8A CN101878193B (zh) 2007-09-28 2008-09-25 双环γ-氨基酸衍生物
DK08833399.2T DK2192109T3 (da) 2007-09-28 2008-09-25 BICYKLISKE y-AMINOSYREDERIVATER
EP08833399.2A EP2192109B1 (en) 2007-09-28 2008-09-25 Bicyclic -amino acid derivative
SI200831100T SI2192109T1 (sl) 2007-09-28 2008-09-25 Biciklični aminokislinski derivati
NZ584699A NZ584699A (en) 2007-09-28 2008-09-25 Bicyclic gamma-amino acid derivative
KR1020137020763A KR101409079B1 (ko) 2007-09-28 2008-09-25 2 고리성 γ-아미노산 유도체
JP2009534336A JP4479974B2 (ja) 2007-09-28 2008-09-25 二環性γ−アミノ酸誘導体
KR1020107006640A KR101335784B1 (ko) 2007-09-28 2008-09-25 2 고리성 γ-아미노산 유도체
MX2010003394A MX2010003394A (es) 2007-09-28 2008-09-25 Derivado de gamma-aminoacido biciclico.
AU2008304933A AU2008304933B2 (en) 2007-09-28 2008-09-25 Bicyclic y-amino acid derivative
CA2701110A CA2701110C (en) 2007-09-28 2008-09-25 Bicyclic .gamma.-amino acid derivative
BRPI0818193A BRPI0818193B8 (pt) 2007-09-28 2008-09-25 composto, composição farmacêutica, e, uso de um composto
PL08833399T PL2192109T3 (pl) 2007-09-28 2008-09-25 Bicykliczna pochodna γ-aminokwasu
BR122013020635-3A BR122013020635A2 (pt) 2007-09-28 2008-09-25 Composto
ES08833399T ES2433890T3 (es) 2007-09-28 2008-09-25 Derivado de aminoácido bicíclico
US12/714,267 US7947738B2 (en) 2007-09-28 2010-02-26 Bicyclic γ-amino acid derivative
ZA2010/02013A ZA201002013B (en) 2007-09-28 2010-03-19 BICYCLIC y-AMINO ACID DERIVATIVES
IL204621A IL204621A (en) 2007-09-28 2010-03-21 Amino Acid Derivatives - γ - In bicycles preparations containing them and their uses
HK10106099.5A HK1139381A1 (en) 2007-09-28 2010-06-21 Bicyclic -amino acid derivative
PH12013501663A PH12013501663A1 (en) 2007-09-28 2013-08-08 BYCYCLIC y-AMINO ACID DERIVATIVE
HRP20130935AT HRP20130935T1 (hr) 2007-09-28 2013-10-07 Bicikliäśki derivat aminokiseline

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007255430 2007-09-28
JP2007-255430 2007-09-28

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US12/714,267 Continuation US7947738B2 (en) 2007-09-28 2010-02-26 Bicyclic γ-amino acid derivative

Publications (1)

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WO2009041453A1 true WO2009041453A1 (ja) 2009-04-02

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PCT/JP2008/067223 WO2009041453A1 (ja) 2007-09-28 2008-09-25 二環性γ－アミノ酸誘導体

Country Status (26)

Country Link
US (1) US7947738B2 (ja)
EP (2) EP2657219B1 (ja)
JP (1) JP4479974B2 (ja)
KR (2) KR101335784B1 (ja)
CN (2) CN101878193B (ja)
AU (1) AU2008304933B2 (ja)
BR (2) BRPI0818193B8 (ja)
CA (1) CA2701110C (ja)
CO (1) CO6270314A2 (ja)
CY (1) CY1114836T1 (ja)
DK (1) DK2192109T3 (ja)
ES (2) ES2433890T3 (ja)
HK (2) HK1139381A1 (ja)
HR (1) HRP20130935T1 (ja)
IL (1) IL204621A (ja)
MX (1) MX2010003394A (ja)
MY (2) MY172034A (ja)
NZ (1) NZ584699A (ja)
PH (1) PH12013501663A1 (ja)
PL (1) PL2192109T3 (ja)
PT (1) PT2192109E (ja)
RU (1) RU2446148C2 (ja)
SI (1) SI2192109T1 (ja)
TW (2) TWI436762B (ja)
WO (1) WO2009041453A1 (ja)
ZA (1) ZA201002013B (ja)

Cited By (14)

* Cited by examiner, † Cited by third party
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WO2010079668A1 (ja) * 2009-01-08 2010-07-15 第一三共株式会社 オレフィン化合物
WO2010110361A1 (ja) * 2009-03-26 2010-09-30 第一三共株式会社 二環性γ－アミノ酸誘導体の製造方法
WO2012169474A1 (ja) * 2011-06-08 2012-12-13 第一三共株式会社 イミニウム塩を経由する二環性化合物の製造方法
WO2012169475A1 (ja) * 2011-06-08 2012-12-13 第一三共株式会社 クライゼン転位反応による二環性化合物の製造方法
WO2013154066A1 (ja) * 2012-04-10 2013-10-17 第一三共株式会社 酵素を用いる二環性化合物の光学分割方法
JP2017502020A (ja) * 2013-12-18 2017-01-19 ノヴァッセイ エスエー 疼痛および他の障害の治療のためのガンマ−アミノ酪酸（ｇａｂａ）類似体
WO2017183539A1 (ja) * 2016-04-18 2017-10-26 第一三共株式会社 メルドラム酸を用いる二環性化合物の製造方法
WO2018003980A1 (ja) * 2016-07-01 2018-01-04 第一三共株式会社 アミノカルボン酸の酸付加塩の結晶とその製造方法
JP2019038759A (ja) * 2017-08-23 2019-03-14 キヤノン株式会社 有機化合物及び光電変換素子
KR20190046892A (ko) * 2016-09-14 2019-05-07 스촨 하이스코 파마수티컬 씨오., 엘티디 융합 트리사이클릭 γ-아미노산 유도체, 그 제조방법, 및 그것의 의료 용도
JP2019521162A (ja) * 2016-07-21 2019-07-25 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッドChia Tai Tianqing Pharmaceutical Group Co., Ltd. Ｃｒｔｈ２阻害剤としてのインドール誘導体
WO2020011257A1 (zh) * 2018-07-12 2020-01-16 四川海思科制药有限公司 一种稠合三环γ-氨基酸衍生物的组合物及其制备
WO2020027019A1 (ja) * 2018-07-30 2020-02-06 第一三共株式会社 安定化剤を含有する医薬品の固形製剤
WO2021079887A1 (ja) 2019-10-25 2021-04-29 国立大学法人京都大学 タウオパチーの予防又は治療剤

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DK2192109T3 (da) 2007-09-28 2013-12-16 Daiichi Sankyo Co Ltd BICYKLISKE y-AMINOSYREDERIVATER
IN2014MN01046A (ja) 2011-12-15 2015-05-01 Daiichi Sankyo Companyltd
WO2013089189A1 (ja) * 2011-12-16 2013-06-20 第一三共株式会社 ヒドロキシスルホン酸を経由する二環性化合物の光学分割方法
JP5947821B2 (ja) * 2012-02-08 2016-07-06 ステラファーマ株式会社 セレウリドおよびその誘導体の製造方法、セレウリド製造の為の中間体ならびにセレウリド誘導体
CA2870675C (en) * 2013-04-04 2017-03-28 Daiichi Sankyo Company, Limited Solid composition comprising salt of aminocarboxylic acid
TWI635071B (zh) * 2013-07-08 2018-09-11 第一三共股份有限公司 光學活性二環γ－胺基酸衍生物及其製造方法
CN107427483B (zh) 2015-03-19 2021-06-29 第一三共株式会社 含有着色剂的固体制剂
CN107405322B (zh) 2015-03-19 2020-08-18 第一三共株式会社 含有抗氧化剂的固体制剂
WO2017107907A1 (zh) * 2015-12-25 2017-06-29 四川海思科制药有限公司 稠合环γ-氨基酸衍生物及其制备方法和在医药上的应用
WO2017114225A1 (zh) * 2015-12-31 2017-07-06 四川海思科制药有限公司 稠合三环γ-氨基酸衍生物及其制备方法和在医药上的应用
CN106928080B (zh) * 2015-12-31 2020-12-25 四川海思科制药有限公司 稠合环γ-氨基酸衍生物及其制备方法和在医药上的应用
CN111918859B (zh) * 2018-07-12 2023-06-30 四川海思科制药有限公司 稠合三环γ-氨基酸衍生物的盐的晶型及制备和应用
WO2020029762A1 (zh) * 2018-08-09 2020-02-13 四川海思科制药有限公司 稠合三环γ-氨基酸衍生物的制备方法及中间体
CN114402198A (zh) * 2019-09-03 2022-04-26 四川海思科制药有限公司 2-((1s,2s,3r,6s,8s)-2-(氨甲基)三环[4.2.1.03,8]壬烷-2-基)乙酸苯磺酸盐或其组合物杂质检测方法
CN110511141B (zh) * 2019-09-09 2022-04-29 上海凌凯医药科技有限公司 一种丙戊酰脲的合成方法
CN110818582B (zh) * 2019-11-20 2023-06-09 合肥拓锐生物科技有限公司 一种gaba类似物及其盐，及其合成方法、应用、药物
CN111116345A (zh) * 2019-12-30 2020-05-08 上海华理生物医药股份有限公司 一种制备Mirogabalin的新方法
AU2022273980A1 (en) 2021-05-12 2023-10-12 Boehringer Ingelheim International Gmbh Pyridine derivatives with c-linked cyclic substituents as cgas inhibitors
CN114195661B (zh) * 2021-12-21 2023-12-22 苏州楚凯药业有限公司 一种苯磺酸米洛巴林的制备方法
CN116903468B (zh) * 2023-07-14 2024-01-26 山东新时代药业有限公司 一种米洛巴林中间体的制备方法

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JP2004527544A (ja) * 2001-04-19 2004-09-09 ワーナー−ランバート・カンパニー・エルエルシー 縮合した二環式又は三環式アミノ酸
JP2006501297A (ja) * 2002-10-04 2006-01-12 ファイザー・インク 環式ニトロメチル酢酸誘導体

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RU2010116708A (ru) 2011-11-10
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AU2008304933A1 (en) 2009-04-02
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