CN104822672B - 治疗性化合物和组合物以及其作为pkm2调节剂的用途 - Google Patents
治疗性化合物和组合物以及其作为pkm2调节剂的用途 Download PDFInfo
- Publication number
- CN104822672B CN104822672B CN201380063407.2A CN201380063407A CN104822672B CN 104822672 B CN104822672 B CN 104822672B CN 201380063407 A CN201380063407 A CN 201380063407A CN 104822672 B CN104822672 B CN 104822672B
- Authority
- CN
- China
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- compounds
- pkm2
- 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.)
- Expired - Fee Related
Links
- 0 CCC(C)C(C)=CC=*C(C1(C=NC1)O)=C Chemical compound CCC(C)C(C)=CC=*C(C1(C=NC1)O)=C 0.000 description 1
- PYFBFOQZFPIVDR-UHFFFAOYSA-N C[S](CNc(cc1)ccc1C(O)=O)(c1c2N=CC=CCc2ccc1)(=O)=O Chemical compound C[S](CNc(cc1)ccc1C(O)=O)(c1c2N=CC=CCc2ccc1)(=O)=O PYFBFOQZFPIVDR-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epidemiology (AREA)
- Enzymes And Modification Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261724266P | 2012-11-08 | 2012-11-08 | |
| US61/724,266 | 2012-11-08 | ||
| PCT/US2013/069193 WO2014074848A1 (en) | 2012-11-08 | 2013-11-08 | Therapeutic compounds and compositions and their use as pkm2 modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104822672A CN104822672A (zh) | 2015-08-05 |
| CN104822672B true CN104822672B (zh) | 2018-08-28 |
Family
ID=49667584
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380063407.2A Expired - Fee Related CN104822672B (zh) | 2012-11-08 | 2013-11-08 | 治疗性化合物和组合物以及其作为pkm2调节剂的用途 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US9458132B2 (https=) |
| EP (1) | EP2917207A1 (https=) |
| JP (1) | JP6362610B2 (https=) |
| KR (1) | KR20150080619A (https=) |
| CN (1) | CN104822672B (https=) |
| AU (1) | AU2013342203B2 (https=) |
| CA (1) | CA2890664A1 (https=) |
| EA (1) | EA032007B1 (https=) |
| HK (1) | HK1213888A1 (https=) |
| MX (1) | MX2015005841A (https=) |
| NZ (1) | NZ707778A (https=) |
| WO (1) | WO2014074848A1 (https=) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2909181T3 (da) | 2012-10-16 | 2017-11-20 | Tolero Pharmaceuticals Inc | PKM2-modulatorer og fremgangsmåder til anvendelse deraf |
| JP6669499B2 (ja) | 2013-02-15 | 2020-03-18 | カラ ファーマシューティカルズ インコーポレイテッド | 治療用化合物 |
| JP2016510000A (ja) | 2013-02-20 | 2016-04-04 | カラ ファーマシューティカルズ インコーポレイテッド | 治療用化合物およびその使用 |
| US9688688B2 (en) | 2013-02-20 | 2017-06-27 | Kala Pharmaceuticals, Inc. | Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof |
| NZ719185A (en) | 2013-11-01 | 2017-11-24 | Kala Pharmaceuticals Inc | Crystalline forms of therapeutic compounds and uses thereof |
| US9890173B2 (en) | 2013-11-01 | 2018-02-13 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| CN104817490B (zh) * | 2015-05-13 | 2017-10-13 | 北京大学 | 氨基二硫代甲酸酯类化合物及其制备方法与应用 |
| WO2017095751A1 (en) | 2015-12-02 | 2017-06-08 | Partikula Llc | Compositions and methods for modulating cancer cell metabolism |
| CA3252823A1 (en) | 2016-06-13 | 2025-02-25 | Gilead Sciences, Inc. | Substituted tert-butyl-3-(2-chloro-phenyl)-3-hydroxyazetidine-1-carboxylate compounds |
| EP3509423A4 (en) | 2016-09-08 | 2020-05-13 | Kala Pharmaceuticals, Inc. | CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF |
| AU2017324713B2 (en) | 2016-09-08 | 2020-08-13 | KALA BIO, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| KR20190051010A (ko) | 2016-09-08 | 2019-05-14 | 칼라 파마슈티컬스, 인크. | 치료 화합물의 결정형 및 그의 용도 |
| ES2747768T3 (es) | 2017-03-20 | 2020-03-11 | Forma Therapeutics Inc | Composiciones de pirrolopirrol como activadores de quinasa de piruvato (PKR) |
| DK3668513T3 (da) | 2017-08-15 | 2022-01-10 | Agios Pharmaceuticals Inc | Pyruvatkinase-aktiveringsmidler til anvendelse til behandling af blodsygdomme |
| US20200237766A1 (en) | 2017-10-13 | 2020-07-30 | Tolero Pharmaceuticals, Inc. | Pkm2 activators in combination with reactive oxygen species for treatment of cancer |
| ES2989438T3 (es) * | 2018-09-19 | 2024-11-26 | Novo Nordisk Healthcare Ag | Activación de la piruvato cinasa R |
| US12053458B2 (en) | 2018-09-19 | 2024-08-06 | Novo Nordisk Health Care Ag | Treating sickle cell disease with a pyruvate kinase R activating compound |
| CA3233305A1 (en) | 2019-02-19 | 2020-08-27 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
| CA3133460A1 (en) | 2019-03-22 | 2020-10-01 | Sumitomo Dainippon Pharma Oncology, Inc. | Compositions comprising pkm2 modulators and methods of treatment using the same |
| US20220378756A1 (en) | 2019-09-19 | 2022-12-01 | Forma Therapeutics, Inc. | Activating pyruvate kinase r |
| US11566030B2 (en) | 2021-02-08 | 2023-01-31 | Global Blood Therapeutics, Inc. | Substituted 2,6-dihydropyrrolo[3,4-c]pyrazoles as pyruvate kinase activators |
| US12128035B2 (en) | 2021-03-19 | 2024-10-29 | Novo Nordisk Health Care Ag | Activating pyruvate kinase R |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012083246A1 (en) * | 2010-12-17 | 2012-06-21 | Agios Pharmaceuticals, Inc. | Novel n- (4- (azetidine - 1 - carbonyl) phenyl) - (hetero - ) arylsulfonamide derivatives as pyruvate kinase m2 (pmk2) modulators |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3545461B2 (ja) | 1993-09-10 | 2004-07-21 | エーザイ株式会社 | 二環式ヘテロ環含有スルホンアミド誘導体 |
| US6214879B1 (en) | 1998-03-24 | 2001-04-10 | Virginia Commonwealth University | Allosteric inhibitors of pyruvate kinase |
| MXPA02002319A (es) | 1999-09-04 | 2002-07-30 | Astrazeneca Ab | Derivados 2-hidroxi-2-metil-3,3,3-trifluoropropanamida con n-fenilo susbtituido que elevan la actividad de la deshidrogenasa de piruvato. |
| EP1797076A1 (en) | 2004-09-24 | 2007-06-20 | AstraZeneca AB | Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof |
| AU2009303335B2 (en) * | 2008-10-09 | 2016-05-19 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Activators of human pyruvate kinase |
| AU2010223919B2 (en) | 2009-03-13 | 2016-03-31 | Les Laboratoires Servier | Methods and compositions for cell-proliferation-related disorders |
| WO2010118063A2 (en) | 2009-04-06 | 2010-10-14 | Agios Pharmaceuticals, Inc. | Therapeutic compositions and related methods of use |
| US8455476B2 (en) | 2009-04-22 | 2013-06-04 | Janssen Pharmaceutica, Nv | Azetidinyl diamides as monoacylglycerol lipase inhibitors |
| ES2618630T3 (es) * | 2009-06-29 | 2017-06-21 | Agios Pharmaceuticals, Inc. | Composiciones terapéuticas y métodos de uso relacionados |
| RU2561132C2 (ru) * | 2009-06-29 | 2015-08-20 | Аджиос Фармасьютикалз, Инк. | Производные хинолинсульфонамидов и их применение для модулирования пкм2 активности |
| US20130109672A1 (en) * | 2010-04-29 | 2013-05-02 | The United States Of America,As Represented By The Secretary, Department Of Health And Human Service | Activators of human pyruvate kinase |
| DE102010048800A1 (de) | 2010-10-20 | 2012-05-10 | Merck Patent Gmbh | Chinoxalinderivate |
| TWI549947B (zh) * | 2010-12-29 | 2016-09-21 | 阿吉歐斯製藥公司 | 治療化合物及組成物 |
| WO2012151448A1 (en) * | 2011-05-03 | 2012-11-08 | Agios Pharmaceuticals, Inc. | Pyruvate kinase activators for use in therapy |
| SG194697A1 (en) * | 2011-05-03 | 2013-12-30 | Agios Pharmaceuticals Inc | Pyruvate kinase activators for use in therapy |
-
2013
- 2013-11-08 KR KR1020157014747A patent/KR20150080619A/ko not_active Withdrawn
- 2013-11-08 HK HK16101847.5A patent/HK1213888A1/zh unknown
- 2013-11-08 CA CA2890664A patent/CA2890664A1/en not_active Abandoned
- 2013-11-08 EP EP13795929.2A patent/EP2917207A1/en not_active Withdrawn
- 2013-11-08 US US14/441,746 patent/US9458132B2/en not_active Expired - Fee Related
- 2013-11-08 MX MX2015005841A patent/MX2015005841A/es unknown
- 2013-11-08 CN CN201380063407.2A patent/CN104822672B/zh not_active Expired - Fee Related
- 2013-11-08 AU AU2013342203A patent/AU2013342203B2/en not_active Ceased
- 2013-11-08 JP JP2015541933A patent/JP6362610B2/ja not_active Expired - Fee Related
- 2013-11-08 EA EA201590881A patent/EA032007B1/ru not_active IP Right Cessation
- 2013-11-08 WO PCT/US2013/069193 patent/WO2014074848A1/en not_active Ceased
- 2013-11-08 NZ NZ707778A patent/NZ707778A/en not_active IP Right Cessation
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012083246A1 (en) * | 2010-12-17 | 2012-06-21 | Agios Pharmaceuticals, Inc. | Novel n- (4- (azetidine - 1 - carbonyl) phenyl) - (hetero - ) arylsulfonamide derivatives as pyruvate kinase m2 (pmk2) modulators |
Non-Patent Citations (1)
| Title |
|---|
| 丙酮酸缺陷症研究现状;潘竹林等;《中华血液学杂志》;19990430;第20卷(第4期);223-224 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EP2917207A1 (en) | 2015-09-16 |
| CA2890664A1 (en) | 2014-05-15 |
| US20150307473A1 (en) | 2015-10-29 |
| KR20150080619A (ko) | 2015-07-09 |
| EA032007B1 (ru) | 2019-03-29 |
| MX2015005841A (es) | 2016-01-08 |
| JP6362610B2 (ja) | 2018-07-25 |
| WO2014074848A1 (en) | 2014-05-15 |
| CN104822672A (zh) | 2015-08-05 |
| EA201590881A1 (ru) | 2015-08-31 |
| HK1213888A1 (zh) | 2016-07-15 |
| JP2016501189A (ja) | 2016-01-18 |
| AU2013342203A1 (en) | 2015-05-21 |
| AU2013342203B2 (en) | 2017-11-23 |
| NZ707778A (en) | 2019-03-29 |
| US9458132B2 (en) | 2016-10-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| EXSB | Decision made by sipo to initiate substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20180828 Termination date: 20201108 |
|
| CF01 | Termination of patent right due to non-payment of annual fee |