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 PDF

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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
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China
Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
compounds
pkm2
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Expired - Fee Related
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CN201380063407.2A
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English (en)
Chinese (zh)
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CN104822672A (zh
Inventor
J·泊泊威次-马勒
J·O·撒德斯
R·扎勒
G·柴彻塔
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Agios Pharmaceuticals Inc
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Agios Pharmaceuticals Inc
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epidemiology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
CN201380063407.2A 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 Expired - Fee Related CN104822672B (zh)

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

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Country Status (12)

Country Link
US (1) US9458132B2 (enExample)
EP (1) EP2917207A1 (enExample)
JP (1) JP6362610B2 (enExample)
KR (1) KR20150080619A (enExample)
CN (1) CN104822672B (enExample)
AU (1) AU2013342203B2 (enExample)
CA (1) CA2890664A1 (enExample)
EA (1) EA032007B1 (enExample)
HK (1) HK1213888A1 (enExample)
MX (1) MX2015005841A (enExample)
NZ (1) NZ707778A (enExample)
WO (1) WO2014074848A1 (enExample)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
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
CA2900652C (en) 2013-02-15 2021-05-04 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
CN107915751A (zh) 2013-02-20 2018-04-17 卡拉制药公司 治疗性化合物和其用途
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
WO2015066482A1 (en) 2013-11-01 2015-05-07 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
AU2017324716B2 (en) 2016-09-08 2020-08-13 KALA BIO, Inc. Crystalline forms of therapeutic compounds and uses thereof
MX2019002629A (es) 2016-09-08 2019-10-07 Kala Pharmaceuticals Inc Formas cristalinas de compuestos terapéuticos y usos de los mismos.
AU2017324713B2 (en) 2016-09-08 2020-08-13 KALA BIO, Inc. Crystalline forms of therapeutic compounds and uses thereof
EP3680241A1 (en) * 2017-03-20 2020-07-15 Forma Therapeutics, Inc. Pyrrolopyrrole compositions as pyruvate kinase (pkr) activators
CN111032045B (zh) 2017-08-15 2023-08-15 安吉奥斯医药品有限公司 用于治疗血液病症的丙酮酸激酶激活剂
US20200237766A1 (en) 2017-10-13 2020-07-30 Tolero Pharmaceuticals, Inc. Pkm2 activators in combination with reactive oxygen species for treatment of cancer
WO2020061255A1 (en) * 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Activating pyruvate kinase r
US10675274B2 (en) 2018-09-19 2020-06-09 Forma Therapeutics, Inc. Activating pyruvate kinase R
US11524005B2 (en) 2019-02-19 2022-12-13 Gilead Sciences, Inc. Solid forms of FXR agonists
EP3941463A1 (en) 2019-03-22 2022-01-26 Sumitomo Dainippon Pharma Oncology, Inc. Compositions comprising pkm2 modulators and methods of treatment using the same
HUE072832T2 (hu) 2019-09-19 2025-12-28 Novo Nordisk Healthcare Ag Piruvát kináz R-t (PKR) aktiváló készítmények
WO2022170200A1 (en) 2021-02-08 2022-08-11 Global Blood Therapeutics, Inc. 1-(2-sulfonyl-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4h)-yl]-ethanone derivatives as pyruvate kinase (pkr) and pkm2 activators for the treatment of sickle cell disease
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R

Citations (1)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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
WO2001017956A1 (en) 1999-09-04 2001-03-15 Astrazeneca Ab Substituted n-phenyl 2-hydroxy-2-methyl-3,3,3-trifluoropropanamide derivatives which elevate pyruvate dehydrogenase activity
WO2006033628A1 (en) 2004-09-24 2006-03-30 Astrazeneca Ab Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof
US8841305B2 (en) * 2008-10-09 2014-09-23 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Activators of the human pyruvate kinase M2 receptor
ES2740424T3 (es) 2009-03-13 2020-02-05 Agios Pharmaceuticals Inc Métodos y composiciones para trastornos relacionados con la proliferación celular
CA2758071C (en) * 2009-04-06 2018-01-09 Agios Pharmaceuticals, Inc. Pyruvate kinase m2 modulators, therapeutic compositions and related methods of use
AU2010239188B2 (en) 2009-04-22 2016-03-31 Janssen Pharmaceutica Nv Azetidinyl diamides as monoacylglycerol lipase inhibitors
SG10201403696UA (en) * 2009-06-29 2014-10-30 Agios Pharmaceuticals Inc Therapeutic compounds and compositions
EP2448581B1 (en) * 2009-06-29 2016-12-07 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
WO2011137089A1 (en) * 2010-04-29 2011-11-03 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services 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
JP6272754B2 (ja) * 2011-05-03 2018-01-31 アジオス ファーマシューティカルズ， インコーポレイテッド ピルビン酸キナーゼ活性化剤の使用方法
WO2012151448A1 (en) * 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use in therapy

Patent Citations (1)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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
MX2015005841A (es) 2016-01-08
US9458132B2 (en) 2016-10-04
NZ707778A (en) 2019-03-29
AU2013342203B2 (en) 2017-11-23
HK1213888A1 (zh) 2016-07-15
JP6362610B2 (ja) 2018-07-25
EA201590881A1 (ru) 2015-08-31
CA2890664A1 (en) 2014-05-15
JP2016501189A (ja) 2016-01-18
US20150307473A1 (en) 2015-10-29
WO2014074848A1 (en) 2014-05-15
AU2013342203A1 (en) 2015-05-21
EA032007B1 (ru) 2019-03-29
CN104822672A (zh) 2015-08-05
KR20150080619A (ko) 2015-07-09

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