CN111886009A - Egfr二聚体干扰物及其用途 - Google Patents

Egfr二聚体干扰物及其用途 Download PDF

Info

Publication number
CN111886009A
CN111886009A CN201980020234.3A CN201980020234A CN111886009A CN 111886009 A CN111886009 A CN 111886009A CN 201980020234 A CN201980020234 A CN 201980020234A CN 111886009 A CN111886009 A CN 111886009A
Authority
CN
China
Prior art keywords
compound
salt
equiv
egfr
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.)
Pending
Application number
CN201980020234.3A
Other languages
English (en)
Chinese (zh)
Inventor
穆克什·K·尼亚蒂
西奥多·S·劳伦斯
克里斯托弗·怀特黑德
詹森·克里斯托弗·雷希
布雷南·泰勒·瓦差
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 Ann Arbor
Original Assignee
University of Michigan Ann Arbor
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 Ann Arbor filed Critical University of Michigan Ann Arbor
Publication of CN111886009A publication Critical patent/CN111886009A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • 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
    • 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

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)
CN201980020234.3A 2018-02-23 2019-02-25 Egfr二聚体干扰物及其用途 Pending CN111886009A (zh)

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

Publications (1)

Publication Number Publication Date
CN111886009A true CN111886009A (zh) 2020-11-03

Family

ID=67688515

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980020234.3A Pending CN111886009A (zh) 2018-02-23 2019-02-25 Egfr二聚体干扰物及其用途

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
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

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3091834A1 (en) * 2018-02-23 2019-08-29 The Regents Of The University Of Michigan Egfr dimer disruptors and use of the same
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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090163545A1 (en) * 2007-12-21 2009-06-25 University Of Rochester Method For Altering The Lifespan Of Eukaryotic Organisms
WO2014176475A2 (en) * 2013-04-26 2014-10-30 The Regents Of The University Of Michigan Egfr inhibitors and uses thereof
CN105934248A (zh) * 2014-01-24 2016-09-07 融合生命科学公司 取代的吡咯并吡啶和吡咯并吡嗪用于治疗癌症或炎性疾病
CN107406442A (zh) * 2014-12-23 2017-11-28 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

Family Cites Families (4)

* 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
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
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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090163545A1 (en) * 2007-12-21 2009-06-25 University Of Rochester Method For Altering The Lifespan Of Eukaryotic Organisms
WO2014176475A2 (en) * 2013-04-26 2014-10-30 The Regents Of The University Of Michigan Egfr inhibitors and uses thereof
CN105934248A (zh) * 2014-01-24 2016-09-07 融合生命科学公司 取代的吡咯并吡啶和吡咯并吡嗪用于治疗癌症或炎性疾病
CN107406442A (zh) * 2014-12-23 2017-11-28 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

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
REGISTRY: "1189728-36-6,899931-40-9", 《STN》 *

Cited By (1)

* 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

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
US20220340572A1 (en) 2022-10-27
EP3755323A1 (en) 2020-12-30
AU2019223168B2 (en) 2024-09-12
JP7497046B2 (ja) 2024-06-10
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
CN111886009A (zh) Egfr二聚体干扰物及其用途
JP7602272B2 (ja) Ｋｒａｓ関連がんを治療する方法
CN115397413A (zh) Egfr、kras、braf和其他靶标的抑制剂及其用途
JP6161705B2 (ja) 新規キノリン置換化合物
JP2023515689A (ja) Ｅｇｆｒ、ｋｒａｓ、ｂｒａｆ、及び他の標的の阻害剤、並びにその使用
RS65884B1 (sr) Makrociklična jedinjenja i primene istih
EA034216B1 (ru) Производные 1-(5-трет-бутил-2-арилпиразол-3-ил)-3-[2-фтор-4-[(3-оксо-4h-пиридо[2,3-b]пиразин-8-ил)окси]фенил]мочевины в качестве ингибиторов raf для лечения рака
KR101760586B1 (ko) 넌센스 돌연변이 억제자로서의 피리미도 [4,5-b]퀴놀린-4,5 (3h,10h)-디온
KR101905295B1 (ko) 나프티리딘디온 유도체
CN103189357B (zh) 作为kcnq2/3调节剂的取代的2-氧代-和2-硫代-二氢喹啉-3-甲酰胺
IL293388A (en) History of benzylamide as a transforming growth factor inhibitor in the i/alk5 receptor cell
HK40034660A (en) Egfr dimer disruptors and use of the same
EA042609B1 (ru) Ингибиторы димеризации egfr и их использование
EA045526B1 (ru) Производные бензиламида в качестве ингибиторов рецептора i/alk5 трансформирующего фактора роста-бета

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40034660

Country of ref document: HK