JP7497046B2 - Ｅｇｆｒ二量体撹乱剤およびその使用 - Google Patents

Ｅｇｆｒ二量体撹乱剤およびその使用 Download PDF

Info

Publication number
JP7497046B2
JP7497046B2 JP2020544510A JP2020544510A JP7497046B2 JP 7497046 B2 JP7497046 B2 JP 7497046B2 JP 2020544510 A JP2020544510 A JP 2020544510A JP 2020544510 A JP2020544510 A JP 2020544510A JP 7497046 B2 JP7497046 B2 JP 7497046B2
Authority
JP
Japan
Prior art keywords
compound
reaction mixture
egfr
triazaspiro
cancer
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
JP2020544510A
Other languages
English (en)
Japanese (ja)
Other versions
JPWO2019165358A5 (https=
JP2021514001A5 (https=
JP2021514001A (ja
Inventor
ケー．ニャティ ムケシュ
エス．ローレンス セオドア
ホワイトヘッド クリストファー
クリストファー レッチ ジェイソン
テイラー ウォッチ ブレナン
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.)
University of Michigan System
Original Assignee
University of Michigan System
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 University of Michigan System filed Critical University of Michigan System
Publication of JP2021514001A publication Critical patent/JP2021514001A/ja
Publication of JPWO2019165358A5 publication Critical patent/JPWO2019165358A5/ja
Publication of JP2021514001A5 publication Critical patent/JP2021514001A5/ja
Priority to JP2024009496A priority Critical patent/JP2024056735A/ja
Application granted granted Critical
Publication of JP7497046B2 publication Critical patent/JP7497046B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/70—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/84—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2020544510A 2018-02-23 2019-02-25 Ｅｇｆｒ二量体撹乱剤およびその使用 Active JP7497046B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2024009496A JP2024056735A (ja) 2018-02-23 2024-01-25 Ｅｇｆｒ二量体撹乱剤およびその使用

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862634452P 2018-02-23 2018-02-23
US62/634,452 2018-02-23
PCT/US2019/019391 WO2019165358A1 (en) 2018-02-23 2019-02-25 Egfr dimer disruptors and use of the same

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2024009496A Division JP2024056735A (ja) 2018-02-23 2024-01-25 Ｅｇｆｒ二量体撹乱剤およびその使用

Publications (4)

Publication Number Publication Date
JP2021514001A JP2021514001A (ja) 2021-06-03
JPWO2019165358A5 JPWO2019165358A5 (https=) 2022-03-03
JP2021514001A5 JP2021514001A5 (https=) 2022-03-03
JP7497046B2 true JP7497046B2 (ja) 2024-06-10

Family

ID=67688515

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2020544510A Active JP7497046B2 (ja) 2018-02-23 2019-02-25 Ｅｇｆｒ二量体撹乱剤およびその使用
JP2024009496A Pending JP2024056735A (ja) 2018-02-23 2024-01-25 Ｅｇｆｒ二量体撹乱剤およびその使用

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2024009496A Pending JP2024056735A (ja) 2018-02-23 2024-01-25 Ｅｇｆｒ二量体撹乱剤およびその使用

Country Status (11)

Country Link
US (2) US11358965B2 (https=)
EP (1) EP3755323A4 (https=)
JP (2) JP7497046B2 (https=)
KR (1) KR102748047B1 (https=)
CN (1) CN111886009A (https=)
AU (1) AU2019223168B2 (https=)
BR (1) BR112020017184A2 (https=)
CA (1) CA3091834A1 (https=)
EA (1) EA202092000A1 (https=)
MX (1) MX2020008767A (https=)
WO (1) WO2019165358A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024056735A (ja) * 2018-02-23 2024-04-23 ザ・リージェンツ・オブ・ザ・ユニバーシティ・オブ・ミシガン Ｅｇｆｒ二量体撹乱剤およびその使用

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114286676A (zh) * 2019-08-22 2022-04-05 密歇根大学董事会 治疗kras相关癌症的方法
CA3172812A1 (en) * 2020-03-05 2021-09-10 The Regents Of The University Of Michigan Inhibitors of egfr, kras, braf, and other targets and use of the same
MX2022010977A (es) * 2020-03-05 2022-12-02 Univ Michigan Regents Inhibidores de egfr, kras, braf y otros objetivos y uso de los mismos.
IL301532A (en) 2020-09-23 2023-05-01 Scorpion Therapeutics Inc History Pyrrolo[2,3-C]pyridin-4-one is useful in cancer treatment
WO2022072632A1 (en) 2020-09-30 2022-04-07 Scorpion Therapeutics, Inc. Bicyclic compounds for use in the treatment cancer
WO2022072645A2 (en) 2020-09-30 2022-04-07 Scorpion Therapeutics, Inc. Methods for treating cancer
TW202229282A (zh) 2020-09-30 2022-08-01 美商史考皮恩治療有限公司 治療癌症之方法
BR112023006531A2 (pt) 2020-10-09 2023-10-03 Scorpion Therapeutics Inc Inibidores heterocílicos de egfr e/ou her2, para uso no tratamento de câncer
EP4225304B1 (en) * 2020-10-12 2025-12-17 The Regents of The University of Michigan Synthesis of egfr modulators
WO2022077154A1 (en) * 2020-10-12 2022-04-21 The Regents Of The University Of Michigan Synthesis of egfr modulators
WO2022094271A1 (en) 2020-10-30 2022-05-05 Scorpion Therapeutics, Inc. Methods for treating cancer
WO2022098992A1 (en) 2020-11-05 2022-05-12 Scorpion Therapeutics, Inc. Use of macrocyclic compounds in methods of treating cancer
WO2022197913A1 (en) 2021-03-18 2022-09-22 Scorpion Therapeutics, Inc. Bicyclic derivatives which can be used to treat cancer
EP4323356A1 (en) 2021-04-13 2024-02-21 Nuvalent, Inc. Amino-substituted heterocycles for treating cancers with egfr mutations
WO2023173083A1 (en) 2022-03-11 2023-09-14 Scorpion Therapeutics, Inc. Tetrahydroindole derivatives as egfr and/or her2 inhibtors useful for the treatment of cancer
CN121909190A (zh) 2023-06-08 2026-04-21 安塔列斯疗法股份有限公司 1,5-二氢-4H-吡咯并[3,2-c]吡啶-4-酮用于癌症治疗
CN121712773A (zh) 2023-06-08 2026-03-20 安塔列斯疗法股份有限公司 1,5-二氢-4h-吡咯并[3,2-c]吡啶-4-酮用于癌症治疗

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014176475A2 (en) 2013-04-26 2014-10-30 The Regents Of The University Of Michigan Egfr inhibitors and uses thereof

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3547977A (en) 1967-10-27 1970-12-15 Velsicol Chemical Corp Novel carbanilates
US5466468A (en) 1990-04-03 1995-11-14 Ciba-Geigy Corporation Parenterally administrable liposome formulation comprising synthetic lipids
CA2709784A1 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
WO2012087943A2 (en) 2010-12-20 2012-06-28 The Regents Of The University Of Michigan Inhibitors of the epidermal growth factor receptor-heat shock protein 90 binding interaction
US9499551B2 (en) * 2014-01-24 2016-11-22 Confluence Life Sciences, Inc. Substituted pyrrolo[2,3-b]pyridines for treating cancer or inflammatory diseases
CN113563332B (zh) * 2014-12-23 2024-12-17 达纳－法伯癌症研究所公司 作为egfr抑制剂的新的嘧啶和治疗病症的方法
CA3091834A1 (en) 2018-02-23 2019-08-29 The Regents Of The University Of Michigan Egfr dimer disruptors and use of the same

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014176475A2 (en) 2013-04-26 2014-10-30 The Regents Of The University Of Michigan Egfr inhibitors and uses thereof

Non-Patent Citations (13)

* Cited by examiner, † Cited by third party
Title
STN International，file REGISTRY [online]，[令和５年１月１３日検索]，CAS Registry No. 1223854-83-8(Entered STN: 16 May 2010)
STN International，file REGISTRY [online]，[令和５年１月１３日検索]，CAS Registry No. 1351770-20-1(Entered STN: 23 Dec 2011)
STN International，file REGISTRY [online]，[令和５年１月２０日検索]，CAS Registry No. 1184994-02-2(Entered STN: 16 Sep 2009)
STN International，file REGISTRY [online]，[令和５年１月２０日検索]，CAS Registry No. 1185121-75-8(Entered STN: 16 Sep 2009)
STN International，file REGISTRY [online]，[令和５年１月２０日検索]，CAS Registry No. 1189452-92-3(Entered STN: 22 Oct 2009)
STN International，file REGISTRY [online]，[令和５年１月２０日検索]，CAS Registry No. 1189913-29-8(Entered STN: 25 Oct 2009)
STN International，file REGISTRY [online]，[令和５年１月２０日検索]，CAS Registry No. 1189949-77-6(Entered STN: 25 Oct 2009)
STN International，file REGISTRY [online]，[令和５年１月２０日検索]，CAS Registry No. 1190012-29-3(Entered STN: 25 Oct 2009)
STN International，file REGISTRY [online]，[令和５年１月２０日検索]，CAS Registry No. 1216783-49-1(Entered STN: 05 Apr 2010)
STN International，file REGISTRY [online]，[令和５年１月２０日検索]，CAS Registry No. 1216844-66-4(Entered STN: 05 Apr 2010)
STN International，file REGISTRY [online]，[令和５年１月２０日検索]，CAS Registry No. 1223821-89-3(Entered STN: 16 May 2010)
STN International，file REGISTRY [online]，[令和５年１月２０日検索]，CAS Registry No. 899932-27-5(Entered STN: 09 Aug 2006)
STN International，file REGISTRY [online]，[令和５年１月２０日検索]，CAS Registry No. 899932-84-4(Entered STN: 09 Aug 2006)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024056735A (ja) * 2018-02-23 2024-04-23 ザ・リージェンツ・オブ・ザ・ユニバーシティ・オブ・ミシガン Ｅｇｆｒ二量体撹乱剤およびその使用

Also Published As

Publication number Publication date
KR20200124709A (ko) 2020-11-03
BR112020017184A2 (pt) 2020-12-22
EA202092000A1 (ru) 2020-12-09
US20200377503A1 (en) 2020-12-03
WO2019165358A1 (en) 2019-08-29
AU2019223168A1 (en) 2020-09-10
CN111886009A (zh) 2020-11-03
US20220340572A1 (en) 2022-10-27
EP3755323A1 (en) 2020-12-30
AU2019223168B2 (en) 2024-09-12
EP3755323A4 (en) 2021-11-24
JP2024056735A (ja) 2024-04-23
US11999731B2 (en) 2024-06-04
CA3091834A1 (en) 2019-08-29
MX2020008767A (es) 2021-01-08
US11358965B2 (en) 2022-06-14
KR102748047B1 (ko) 2024-12-27
JP2021514001A (ja) 2021-06-03

Similar Documents

Publication Publication Date Title
JP7497046B2 (ja) Ｅｇｆｒ二量体撹乱剤およびその使用
TWI825637B (zh) 啶－１，６（２ｈ，７ｈ）－二酮
JP7602272B2 (ja) Ｋｒａｓ関連がんを治療する方法
AU2016296878B2 (en) Chiral diaryl macrocycles and uses thereof
CN109369671B (zh) 作为Raf激酶和/或Raf激酶二聚体抑制剂的稠合三环脲类化合物
US10105359B2 (en) Tetrahydroisoquinoline derivatives
ES2610226T3 (es) Compuestos de 6-amino-piridazin-3-il-carboxamida sustituidos como moduladores de proteínas cinasas
JP2023515691A (ja) Ｅｇｆｒ、ｋｒａｓ、ｂｒａｆ、および他の標的の阻害剤およびそれらの使用
RS65884B1 (sr) Makrociklična jedinjenja i primene istih
JP2018522858A (ja) Ｈｐｋ１阻害剤およびそれを用いる方法
CN107922403A (zh) 作为胆碱能毒蕈碱m1受体的调节剂的2,3‑二氢‑4h‑1,3‑苯并噁嗪‑4‑酮衍生物
US20240174659A1 (en) Compounds and methods for yap/tead modulation and indications therefor
TW201902892A (zh) 化合物
EA042609B1 (ru) Ингибиторы димеризации egfr и их использование
HK40034660A (en) Egfr dimer disruptors and use of the same
JP2024047569A (ja) Ｍｅｋ阻害剤としての３，４－ジヒドロ－２，７－ナフチリジン－１，６（２ｈ，７ｈ）－ジオン
TW202214585A (zh) 經取代之異喹啉基甲基醯胺類、其類似物及使用其之方法
HK40057478B (zh) Hpk1抑制剂及其使用方法
HK1263053A1 (en) Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitors
HK1210166A1 (en) Fused tricyclic amide compounds as multiple kinase inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220222

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20220222

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20230130

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20230207

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20230508

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20230728

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20230926

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20240125

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20240307

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: 20240423

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20240522

R150 Certificate of patent or registration of utility model

Ref document number: 7497046

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150