CN109641887B - 可用作用于治疗癌症的突变idh1抑制剂的噻唑衍生物 - Google Patents

可用作用于治疗癌症的突变idh1抑制剂的噻唑衍生物 Download PDF

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CN109641887B
CN109641887B CN201780051410.0A CN201780051410A CN109641887B CN 109641887 B CN109641887 B CN 109641887B CN 201780051410 A CN201780051410 A CN 201780051410A CN 109641887 B CN109641887 B CN 109641887B
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compound
cancer
formula
salt
alkyl
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CN109641887A (zh
Inventor
马修·布莱恩·博克瑟
王晓东
凯勒·瑞恩·布里马科姆
曼迪·伊雷妮·艾米丽·戴维斯
方育红
马修·霍尔
阿吉特·贾达夫
苏伦德拉·卡拉瓦迪
刘莉
纳塔利娅·马丁内斯
安德鲁·路易斯·麦基弗
拉詹·普拉加尼
杰森·马修·罗德
安东·西梅奥诺夫
赵炜
沈敏
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University of North Carolina at Chapel Hill
United States Department of Health and Human Services
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University of North Carolina at Chapel Hill
United States Department of Health and Human Services
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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
    • C07D417/14—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 three or more hetero 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • 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
    • C07B2200/07—Optical isomers

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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)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201780051410.0A 2016-06-22 2017-06-21 可用作用于治疗癌症的突变idh1抑制剂的噻唑衍生物 Active CN109641887B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662353298P 2016-06-22 2016-06-22
US62/353,298 2016-06-22
PCT/US2017/038549 WO2017223202A1 (en) 2016-06-22 2017-06-21 Thiazole derivatives useful as mutant idh1 inhibitors for treating cancer

Publications (2)

Publication Number Publication Date
CN109641887A CN109641887A (zh) 2019-04-16
CN109641887B true CN109641887B (zh) 2022-09-20

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Country Status (7)

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US (1) US10836759B2 (enExample)
EP (1) EP3475276B1 (enExample)
JP (1) JP6987798B2 (enExample)
CN (1) CN109641887B (enExample)
AU (1) AU2017281088B2 (enExample)
ES (1) ES2880347T3 (enExample)
WO (1) WO2017223202A1 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2961807A1 (en) 2014-09-19 2016-03-24 Forma Therapeutics, Inc. Phenyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
WO2016044781A1 (en) 2014-09-19 2016-03-24 Forma Therapeutics, Inc. Quinolinone pyrimidines compositions as mutant-isocitrate dehydrogenase inhibitors
HUE062424T2 (hu) 2014-09-19 2023-11-28 Forma Therapeutics Inc Piridin-2(1H)-on kinolinon származékok mint mutáns izocitrát dehidrogenáz inhibitorok
WO2016044787A1 (en) 2014-09-19 2016-03-24 Forma Therapeutics, Inc. Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
US10407419B2 (en) 2015-04-21 2019-09-10 Forma Therapeutics, Inc. Quinolinone five-membered heterocyclic compounds as mutant-isocitrate dehydrogenase inhibitors
US9624175B2 (en) 2015-04-21 2017-04-18 Forma Therapeutics, Inc. Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
US11311527B2 (en) 2018-05-16 2022-04-26 Forma Therapeutics, Inc. Inhibiting mutant isocitrate dehydrogenase 1 (mIDH-1)
US11013734B2 (en) 2018-05-16 2021-05-25 Forma Therapeutics, Inc. Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation
SMT202300073T1 (it) 2018-05-16 2023-05-12 Forma Therapeutics Inc Inibizione di idh-1 mutante
WO2019222551A1 (en) 2018-05-16 2019-11-21 Forma Therapeutics, Inc. Solid forms of ((s)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile
US11013733B2 (en) 2018-05-16 2021-05-25 Forma Therapeutics, Inc. Inhibiting mutant isocitrate dehydrogenase 1 (mlDH-1)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102985557A (zh) * 2009-03-13 2013-03-20 安吉奥斯医药品有限公司 用于细胞增殖相关病症的方法和组合物
CN105209460A (zh) * 2013-03-14 2015-12-30 诺华股份有限公司 作为突变idh抑制剂的3-嘧啶-4-基-噁唑烷-2-酮化合物
WO2016106331A1 (en) * 2014-12-22 2016-06-30 The United States Of America Mutant idh1 inhibitors useful for treating cancer

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2010229968A1 (en) 2009-03-24 2011-10-13 Gilead Calistoga Llc Atropisomers of2-purinyl-3-tolyl-quinazolinone derivatives and methods of use

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102985557A (zh) * 2009-03-13 2013-03-20 安吉奥斯医药品有限公司 用于细胞增殖相关病症的方法和组合物
CN105209460A (zh) * 2013-03-14 2015-12-30 诺华股份有限公司 作为突变idh抑制剂的3-嘧啶-4-基-噁唑烷-2-酮化合物
WO2016106331A1 (en) * 2014-12-22 2016-06-30 The United States Of America Mutant idh1 inhibitors useful for treating cancer
CN107428690A (zh) * 2014-12-22 2017-12-01 美国政府健康及人类服务部 可用于治疗癌症的突变idh1抑制剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Crystallographic Investigation and Selective Inhibition of Mutant Isocitrate Dehydrogenase;Zheng, BS et al.;《ACS MEDICINAL CHEMISTRY LETTERS》;20130503;第4卷(第6期);第542-546页 *

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CA3028999A1 (en) 2017-12-28
WO2017223202A1 (en) 2017-12-28
EP3475276B1 (en) 2021-03-31
JP2019518770A (ja) 2019-07-04
AU2017281088B2 (en) 2021-05-27
US20190241551A1 (en) 2019-08-08
CN109641887A (zh) 2019-04-16
EP3475276A1 (en) 2019-05-01
ES2880347T3 (es) 2021-11-24
US10836759B2 (en) 2020-11-17
JP6987798B2 (ja) 2022-01-05
AU2017281088A1 (en) 2019-01-17

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