JP6987798B2 - 癌の治療に変異体idh1阻害剤として有用なチアゾール誘導体 - Google Patents

癌の治療に変異体idh1阻害剤として有用なチアゾール誘導体 Download PDF

Info

Publication number
JP6987798B2
JP6987798B2 JP2018567108A JP2018567108A JP6987798B2 JP 6987798 B2 JP6987798 B2 JP 6987798B2 JP 2018567108 A JP2018567108 A JP 2018567108A JP 2018567108 A JP2018567108 A JP 2018567108A JP 6987798 B2 JP6987798 B2 JP 6987798B2
Authority
JP
Japan
Prior art keywords
compound
atropisomer
alkyl
group
formula
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
Application number
JP2018567108A
Other languages
English (en)
Japanese (ja)
Other versions
JP2019518770A (ja
JP2019518770A5 (OSRAM
Inventor
マシュー ブライアン ボクサー
シャオドン ワン
カイル ライアン ブリマコンブ
デイビス ミンディ アイリーン エミリー
ユーホン ファン
マシュー ホール
アジット ジャドハブ
スレンドラ カラヴァディ
リー リウ
ナタリア マルティネス
アンドリュー ルイス マクアイヴァー
ラジャン プラガニ
ジェイソン マシュー ローデ
アントン シメオノフ
ウェイ ヂャオ
ミン シェン
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
US Department of Health and Human Services
Original Assignee
US Department of Health and Human Services
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by US Department of Health and Human Services filed Critical US Department of Health and Human Services
Publication of JP2019518770A publication Critical patent/JP2019518770A/ja
Publication of JP2019518770A5 publication Critical patent/JP2019518770A5/ja
Application granted granted Critical
Publication of JP6987798B2 publication Critical patent/JP6987798B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4995Pyrazines or piperazines forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2018567108A 2016-06-22 2017-06-21 癌の治療に変異体idh1阻害剤として有用なチアゾール誘導体 Active JP6987798B2 (ja)

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 (3)

Publication Number Publication Date
JP2019518770A JP2019518770A (ja) 2019-07-04
JP2019518770A5 JP2019518770A5 (OSRAM) 2020-07-30
JP6987798B2 true JP6987798B2 (ja) 2022-01-05

Family

ID=59276859

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2018567108A Active JP6987798B2 (ja) 2016-06-22 2017-06-21 癌の治療に変異体idh1阻害剤として有用なチアゾール誘導体

Country Status (8)

Country Link
US (1) US10836759B2 (OSRAM)
EP (1) EP3475276B1 (OSRAM)
JP (1) JP6987798B2 (OSRAM)
CN (1) CN109641887B (OSRAM)
AU (1) AU2017281088B2 (OSRAM)
CA (1) CA3028999A1 (OSRAM)
ES (1) ES2880347T3 (OSRAM)
WO (1) WO2017223202A1 (OSRAM)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016044782A1 (en) 2014-09-19 2016-03-24 Forma Therapeutics, Inc. Phenyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
JP6751081B2 (ja) 2014-09-19 2020-09-02 フォーマ セラピューティクス,インコーポレイテッド 変異イソクエン酸デヒドロゲナーゼ阻害剤としてのピリジニルキノリノン誘導体
CA2961793C (en) 2014-09-19 2021-03-16 Forma Therapeutics, Inc. Quinolinone pyrimidines compositions as mutant-isocitrate dehydrogenase inhibitors
SI3447050T1 (sl) 2014-09-19 2020-08-31 Forma Therapeutics, Inc. Derivati piridin-2(1H)-on kinolinona kot inhibitorji mutirane izocitratne dehidrogenaze
US9624216B2 (en) 2015-04-21 2017-04-18 Forma Therapeutics, Inc. Quinolinone five-membered heterocyclic compounds as mutant-isocitrate dehydrogenase inhibitors
US10294206B2 (en) 2015-04-21 2019-05-21 Forma Tm2, Inc. Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
US11013734B2 (en) 2018-05-16 2021-05-25 Forma Therapeutics, Inc. Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation
US11576906B2 (en) 2018-05-16 2023-02-14 Forma Therapeutics, Inc. Inhibiting mutant IDH-1
US11311527B2 (en) 2018-05-16 2022-04-26 Forma Therapeutics, Inc. Inhibiting mutant isocitrate dehydrogenase 1 (mIDH-1)
US10532047B2 (en) 2018-05-16 2020-01-14 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)

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108524505A (zh) * 2009-03-13 2018-09-14 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
CA2756347A1 (en) 2009-03-24 2010-09-30 Gilead Calistoga Llc Atropisomers of 2-purinyl-3-tolyl-quinazolinone derivatives and methods of use
JP2016514124A (ja) * 2013-03-14 2016-05-19 ノバルティス アーゲー 変異idhの阻害薬としての3−ピリミジン−4−イル−オキサゾリジン−2−オン
CN107428690B (zh) * 2014-12-22 2021-04-13 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

Also Published As

Publication number Publication date
JP2019518770A (ja) 2019-07-04
EP3475276A1 (en) 2019-05-01
US20190241551A1 (en) 2019-08-08
CN109641887A (zh) 2019-04-16
EP3475276B1 (en) 2021-03-31
ES2880347T3 (es) 2021-11-24
US10836759B2 (en) 2020-11-17
CN109641887B (zh) 2022-09-20
AU2017281088A1 (en) 2019-01-17
WO2017223202A1 (en) 2017-12-28
CA3028999A1 (en) 2017-12-28
AU2017281088B2 (en) 2021-05-27

Similar Documents

Publication Publication Date Title
JP6987798B2 (ja) 癌の治療に変異体idh1阻害剤として有用なチアゾール誘導体
JP6901394B2 (ja) 癌の処置に有用な変異型idh1阻害剤
US9187474B2 (en) Raf inhibitor compounds
US20170056382A1 (en) Compounds and methods for kinase modulation, and indications therefor
JP2008545652A (ja) c−kitおよびc−fms活性を調節する化合物およびその用途
US8580815B2 (en) Derivatives of azaindoles as inhibitors of protein kinases ABL and SRC
KR20220066074A (ko) A2a / a2b 억제제로서의 트리아졸로피리미딘
JP2021519828A (ja) ジアリール大員環化合物、医薬組成物及びその用途
TW201731841A (zh) 6‐芳基或6‐異芳基‐4‐嗎啉‐4‐芳基‐吡啶‐2‐酮化合物
CN110357905A (zh) 作为蛋白激酶抑制剂的大环类衍生物及其制备方法和用途
JP2007500130A (ja) ベンゾジアゼピン受容体リガンドである、イミダゾ−ピリミジン及びトリアゾロ−ピリミジン
WO2013081094A1 (ja) イミダゾ[1,2-a]ピリジン誘導体及びその医薬用途
US20240002365A1 (en) Pyridazine and 1,2,4-triazine derivatives as fgfr kinase inhibitors
US20240190864A1 (en) Bruton's Tyrosine Kinase (BTK) INHIBITOR AND APPLICATION THEREOF

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190716

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190802

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200619

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20200619

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20210520

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A132

Effective date: 20210525

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20210824

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20211102

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20211201

R150 Certificate of patent or registration of utility model

Ref document number: 6987798

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250