CN107207488B - 作为视黄酸受体β(RARβ)激动剂的双环杂芳基-杂芳基-苯甲酸化合物 - Google Patents

作为视黄酸受体β(RARβ)激动剂的双环杂芳基-杂芳基-苯甲酸化合物 Download PDF

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CN107207488B
CN107207488B CN201580073462.9A CN201580073462A CN107207488B CN 107207488 B CN107207488 B CN 107207488B CN 201580073462 A CN201580073462 A CN 201580073462A CN 107207488 B CN107207488 B CN 107207488B
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CN107207488A (zh
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艾伦·大卫·博斯威克
马克·特雷弗·米尔斯
简·特丽萨·布朗
乔纳森·帕特里克·托马斯·科克瑞恩
玛丽亚·比亚特丽斯·德卡斯特罗瓦斯孔塞洛斯贡卡尔维斯
萨尔基斯·巴雷特·卡林吉恩
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Kings College London
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Life Sciences & Earth Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201580073462.9A 2014-12-17 2015-12-16 作为视黄酸受体β(RARβ)激动剂的双环杂芳基-杂芳基-苯甲酸化合物 Active CN107207488B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1422472.9 2014-12-17
GB201422472 2014-12-17
PCT/EP2015/080029 WO2016097004A1 (en) 2014-12-17 2015-12-16 BICYCLOHETEROARYL-HETEROARYL-BENZOIC ACID COMPOUNDS AS RETINOIC ACID RECEPTOR BETA (RARβ) AGONISTS

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CN107207488A CN107207488A (zh) 2017-09-26
CN107207488B true CN107207488B (zh) 2020-11-17

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US (4) US9994559B2 (https=)
EP (1) EP3233842B1 (https=)
JP (1) JP6596090B2 (https=)
KR (1) KR102526625B1 (https=)
CN (1) CN107207488B (https=)
AU (1) AU2015367531B2 (https=)
BR (1) BR112017012588B8 (https=)
CA (1) CA2970574C (https=)
ES (1) ES3029609T3 (https=)
IL (1) IL252882B (https=)
WO (1) WO2016097004A1 (https=)

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JP6596090B2 (ja) 2014-12-17 2019-10-23 キングス カレッジ ロンドン レチノイン酸受容体ベータ（ＲＡＲβ）アゴニストとしてのビシクロヘテロアリール−ヘテロアリール−安息香酸化合物
GB201610867D0 (en) 2016-06-22 2016-08-03 King S College London Crystalline forms of a therapeutic compound and processes for their preparation
CN111892591A (zh) * 2019-05-06 2020-11-06 南京科技职业学院 一种维奈托克关键中间体的合成方法
GB201907647D0 (en) * 2019-05-30 2019-07-17 King S College London Therapeutic methods
ES3033642T3 (en) 2020-05-29 2025-08-06 Basf Se Preparation of substituted 4-(n'-hydroxycarbamimidoyl)benzoic acids
CN112552252B (zh) * 2020-09-30 2024-01-02 浙江美诺华药物化学有限公司 一种氟雷拉纳中间体的制备方法
CN113264832A (zh) * 2021-05-13 2021-08-17 南京爱可德夫科技开发有限公司 一种合成高纯度2-氟-4-溴苯甲酸叔丁酯的方法
CN116640071B (zh) * 2023-05-04 2024-08-30 四川青木制药有限公司 一种制备2-甲基4-甲醛肟基苯甲酸及其酯类衍生物的方法

Citations (4)

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CN1214042A (zh) * 1996-03-18 1999-04-14 卫材株式会社 含有稠环的羧酸衍生物
US6355669B1 (en) * 1997-10-22 2002-03-12 Eisai Co., Ltd. Retinoic acid agonists as preventive and therapeutic agents for nephritis
CN1382140A (zh) * 1999-07-09 2002-11-27 奥索-麦克尼尔药品公司 具有神经营养活性的吡咯烷和哌啶、以及含有它们的相关组合物
CN102333764A (zh) * 2009-02-25 2012-01-25 爱思开生物制药株式会社 取代的吡咯衍生物、含这些衍生物的药用组合物以及用其治疗帕金森氏病的方法

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EP0842923B1 (en) 1995-06-07 2006-03-01 Nippon Shinyaku Company, Limited Pyrrole derivatives and medicinal composition
JP3964478B2 (ja) 1995-06-30 2007-08-22 エーザイ・アール・アンド・ディー・マネジメント株式会社 ヘテロ環含有カルボン酸誘導体及びそれを含有する医薬
JPH10158192A (ja) 1996-10-03 1998-06-16 Eisai Co Ltd 移植片対宿主疾患（ｇｖｈｄ）の治療および臓器移植時の移植片拒絶反応抑制のための医薬組成物
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JP2005504014A (ja) 2001-06-08 2005-02-10 サイトビア インコーポレイテッド カスパーゼの活性化因子およびアポトーシスの誘導因子としての置換された３−アリール−５−アリール−［１，２，４］−オキサジアゾール類および類似体、並びにその使用法
JP2003081832A (ja) 2001-06-26 2003-03-19 Takeda Chem Ind Ltd レチノイド関連受容体機能調節剤
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JP6596090B2 (ja) * 2014-12-17 2019-10-23 キングス カレッジ ロンドン レチノイン酸受容体ベータ（ＲＡＲβ）アゴニストとしてのビシクロヘテロアリール−ヘテロアリール−安息香酸化合物

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1214042A (zh) * 1996-03-18 1999-04-14 卫材株式会社 含有稠环的羧酸衍生物
US6110959A (en) * 1996-03-18 2000-08-29 Eisai Co., Ltd. Carboxylic acid derivatives having fused rings
US6355669B1 (en) * 1997-10-22 2002-03-12 Eisai Co., Ltd. Retinoic acid agonists as preventive and therapeutic agents for nephritis
CN1382140A (zh) * 1999-07-09 2002-11-27 奥索-麦克尼尔药品公司 具有神经营养活性的吡咯烷和哌啶、以及含有它们的相关组合物
CN102333764A (zh) * 2009-02-25 2012-01-25 爱思开生物制药株式会社 取代的吡咯衍生物、含这些衍生物的药用组合物以及用其治疗帕金森氏病的方法

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US10385044B2 (en) 2019-08-20
US20210130337A1 (en) 2021-05-06
CA2970574A1 (en) 2016-06-23
EP3233842C0 (en) 2025-03-26
CN107207488A (zh) 2017-09-26
EP3233842B1 (en) 2025-03-26
BR112017012588B1 (pt) 2023-11-07
KR20170097125A (ko) 2017-08-25
US10752616B2 (en) 2020-08-25
BR112017012588A2 (pt) 2018-11-13
US20170327489A1 (en) 2017-11-16
AU2015367531A1 (en) 2017-07-06
US11401265B2 (en) 2022-08-02
US20190010146A1 (en) 2019-01-10
IL252882B (en) 2020-04-30
KR102526625B1 (ko) 2023-04-27
JP6596090B2 (ja) 2019-10-23
AU2015367531B2 (en) 2020-04-30
CA2970574C (en) 2023-09-19
US9994559B2 (en) 2018-06-12
BR112017012588B8 (pt) 2024-02-15
US20200131165A1 (en) 2020-04-30
WO2016097004A1 (en) 2016-06-23
JP2017537967A (ja) 2017-12-21
ES3029609T3 (en) 2025-06-24
IL252882A0 (en) 2017-08-31
EP3233842A1 (en) 2017-10-25

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