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 PDFInfo
- Publication number
- 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
- Authority
- CN
- China
- Prior art keywords
- compound
- independently
- treatment
- bhba
- mmol
- Prior art date
- Legal status (The legal status 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 status listed.)
- Active
Links
Images
Classifications
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Gynecology & Obstetrics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB201422472 | 2014-12-17 | ||
| GB1422472.9 | 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107207488A CN107207488A (zh) | 2017-09-26 |
| CN107207488B true CN107207488B (zh) | 2020-11-17 |
Family
ID=55027725
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201580073462.9A Active CN107207488B (zh) | 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 |
Country Status (11)
| Country | Link |
|---|---|
| US (4) | US9994559B2 (enExample) |
| EP (1) | EP3233842B1 (enExample) |
| JP (1) | JP6596090B2 (enExample) |
| KR (1) | KR102526625B1 (enExample) |
| CN (1) | CN107207488B (enExample) |
| AU (1) | AU2015367531B2 (enExample) |
| BR (1) | BR112017012588B8 (enExample) |
| CA (1) | CA2970574C (enExample) |
| ES (1) | ES3029609T3 (enExample) |
| IL (1) | IL252882B (enExample) |
| WO (1) | WO2016097004A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3233842B1 (en) * | 2014-12-17 | 2025-03-26 | King's College London | Bicycloheteroaryl-heteroaryl-benzoic acid compounds as retinoic acid receptor beta (rarb) agonists |
| 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 |
| CN115427401B (zh) | 2020-05-29 | 2025-04-11 | 巴斯夫欧洲公司 | 取代4-(n′-羟基甲脒基)苯甲酸的制备 |
| 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)
| 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 |
| 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 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX9709475A (es) | 1995-06-07 | 1998-02-28 | Nippon Shinyaku Co Ltd | Derivados de pirrol y composicion medicinal. |
| 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 |
| GB9907461D0 (en) | 1999-03-31 | 1999-05-26 | King S College London | Neurite regeneration |
| JP2000154150A (ja) * | 1997-10-22 | 2000-06-06 | Eisai Co Ltd | 腎炎予防・治療剤としてのレチノイン酸アゴニスト |
| US20020048580A1 (en) * | 2000-06-07 | 2002-04-25 | Institut National De La Sante Et De La Recherche Medicale | Method of inducing lung branching |
| CA2449544A1 (en) | 2001-06-08 | 2002-12-19 | Cytovia, Inc. | Substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs |
| 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 |
| WO2003062230A1 (en) * | 2002-01-21 | 2003-07-31 | Eisai Co., Ltd. | Conbinatorial library of heterocycle compounds |
| PL375256A1 (en) | 2002-08-09 | 2005-11-28 | Astra Zeneca Ab | 1,2,4-oxadiazoles as modulators of metabotropic glutamate receptor-5 |
| PL2910551T3 (pl) | 2003-04-11 | 2017-09-29 | Ptc Therapeutics, Inc. | Związki kwasu 1,2,4-oksadiazolobenzoesowego i ich zastosowanie do supresji mutacji nonsensownych i leczenia choroby |
| WO2005077373A2 (en) | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Treatment of gastro-esophageal reflux disease (gerd) |
| MX2007004479A (es) * | 2004-10-13 | 2007-06-18 | Ptc Therapeutics Inc | Compuestoss para supresion sin sentido y metodos para su uso. |
| US20090176837A1 (en) | 2005-07-12 | 2009-07-09 | Sony Corporation | Compounds with activity at retinoic acid receptors |
| EP2304366A2 (en) | 2008-05-30 | 2011-04-06 | Foster Wheeler Energia Oy | Method of and system for generating power by oxyfuel combustion |
| GB0915196D0 (en) * | 2009-09-01 | 2009-10-07 | King S College London | Therapeutic compounds and their use |
| WO2011072281A1 (en) | 2009-12-11 | 2011-06-16 | Ptc Therapeutics, Inc. | Methods for treating methylmalonic acidemia |
| GB201403093D0 (en) | 2014-02-21 | 2014-04-09 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| EP3233842B1 (en) * | 2014-12-17 | 2025-03-26 | King's College London | Bicycloheteroaryl-heteroaryl-benzoic acid compounds as retinoic acid receptor beta (rarb) agonists |
-
2015
- 2015-12-16 EP EP15817206.4A patent/EP3233842B1/en active Active
- 2015-12-16 US US15/533,492 patent/US9994559B2/en active Active
- 2015-12-16 AU AU2015367531A patent/AU2015367531B2/en active Active
- 2015-12-16 WO PCT/EP2015/080029 patent/WO2016097004A1/en not_active Ceased
- 2015-12-16 BR BR112017012588A patent/BR112017012588B8/pt active IP Right Grant
- 2015-12-16 CA CA2970574A patent/CA2970574C/en active Active
- 2015-12-16 CN CN201580073462.9A patent/CN107207488B/zh active Active
- 2015-12-16 ES ES15817206T patent/ES3029609T3/es active Active
- 2015-12-16 JP JP2017532660A patent/JP6596090B2/ja active Active
- 2015-12-16 KR KR1020177019558A patent/KR102526625B1/ko active Active
-
2017
- 2017-06-13 IL IL252882A patent/IL252882B/en active IP Right Grant
-
2018
- 2018-06-05 US US15/997,796 patent/US10385044B2/en active Active
-
2019
- 2019-08-09 US US16/536,441 patent/US10752616B2/en active Active
-
2020
- 2020-08-19 US US16/997,855 patent/US11401265B2/en active Active
Patent Citations (5)
| 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 |
Also Published As
| Publication number | Publication date |
|---|---|
| US10385044B2 (en) | 2019-08-20 |
| US20200131165A1 (en) | 2020-04-30 |
| US20210130337A1 (en) | 2021-05-06 |
| CA2970574C (en) | 2023-09-19 |
| EP3233842B1 (en) | 2025-03-26 |
| EP3233842C0 (en) | 2025-03-26 |
| CN107207488A (zh) | 2017-09-26 |
| US11401265B2 (en) | 2022-08-02 |
| AU2015367531B2 (en) | 2020-04-30 |
| KR102526625B1 (ko) | 2023-04-27 |
| IL252882A0 (en) | 2017-08-31 |
| CA2970574A1 (en) | 2016-06-23 |
| US10752616B2 (en) | 2020-08-25 |
| ES3029609T3 (en) | 2025-06-24 |
| JP2017537967A (ja) | 2017-12-21 |
| BR112017012588A2 (pt) | 2018-11-13 |
| EP3233842A1 (en) | 2017-10-25 |
| US9994559B2 (en) | 2018-06-12 |
| BR112017012588B1 (pt) | 2023-11-07 |
| US20190010146A1 (en) | 2019-01-10 |
| WO2016097004A1 (en) | 2016-06-23 |
| IL252882B (en) | 2020-04-30 |
| BR112017012588B8 (pt) | 2024-02-15 |
| AU2015367531A1 (en) | 2017-07-06 |
| KR20170097125A (ko) | 2017-08-25 |
| US20170327489A1 (en) | 2017-11-16 |
| JP6596090B2 (ja) | 2019-10-23 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN107207488B (zh) | 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 | |
| KR102373700B1 (ko) | 항섬유성 피리디논 | |
| RU2712163C2 (ru) | Активатор kcnq2-5 каналов | |
| JP7511557B2 (ja) | ブロモドメインタンパク質阻害薬としてのイミノスルホン化合物、医薬組成物及びその医薬用途 | |
| JP6456392B2 (ja) | 3−アリール−5−置換イソキノリン−1−オン化合物及びその治療的使用 | |
| JP2005503414A (ja) | Dna−pk阻害薬 | |
| WO2019101086A1 (zh) | 卤代烯丙基胺类ssao/vap-1抑制剂及其应用 | |
| CN103649079A (zh) | 丙型肝炎抑制剂及其用途 | |
| CN111727186B (zh) | 双杂环取代的吡啶-2(1h)-酮衍生物、其制法与医药上的用途 | |
| TW202012379A (zh) | 化合物 | |
| KR20060066722A (ko) | 아미노피론 및 atm억제제로서의 이의 용도 | |
| AU2018303186A1 (en) | Amine or (thio)amide containing LXR modulators | |
| WO2010090304A1 (ja) | アシルグアニジン誘導体 | |
| WO2019144765A1 (zh) | 芳香杂环取代烯烃化合物、其制备方法、药物组合物和应用 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant |