AU2020279253A1 - KRAS G12C inhibitors and uses thereof - Google Patents

KRAS G12C inhibitors and uses thereof Download PDF

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Publication number
AU2020279253A1
AU2020279253A1 AU2020279253A AU2020279253A AU2020279253A1 AU 2020279253 A1 AU2020279253 A1 AU 2020279253A1 AU 2020279253 A AU2020279253 A AU 2020279253A AU 2020279253 A AU2020279253 A AU 2020279253A AU 2020279253 A1 AU2020279253 A1 AU 2020279253A1
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AU
Australia
Prior art keywords
compound
independently
proviso
alkyl
heteroatoms
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Abandoned
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AU2020279253A
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English (en)
Inventor
Michael D. Bartberger
Justin A. HILF
Oliver C. LOSON
Martina S. MCDERMOTT
Brendan M. O'boyle
Neil A. O'Brien
Corey M. Reeves
Tristin E. ROSE
Dennis Slamon
Brian M. Stoltz
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.)
California Institute of Technology
University of California San Diego UCSD
1200 Pharma LLC
Original Assignee
California Institute of Technology
University of California Berkeley
University of California San Diego UCSD
1200 Pharma LLC
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Application filed by California Institute of Technology, University of California Berkeley, University of California San Diego UCSD, 1200 Pharma LLC filed Critical California Institute of Technology
Publication of AU2020279253A1 publication Critical patent/AU2020279253A1/en
Abandoned legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/527Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems
    • 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
    • C07D487/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2020279253A 2019-05-20 2020-05-20 KRAS G12C inhibitors and uses thereof Abandoned AU2020279253A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962850289P 2019-05-20 2019-05-20
US62/850,289 2019-05-20
PCT/US2020/033816 WO2020236940A1 (en) 2019-05-20 2020-05-20 Kras g12c inhibitors and uses thereof

Publications (1)

Publication Number Publication Date
AU2020279253A1 true AU2020279253A1 (en) 2021-12-16

Family

ID=73458223

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2020279253A Abandoned AU2020279253A1 (en) 2019-05-20 2020-05-20 KRAS G12C inhibitors and uses thereof

Country Status (12)

Country Link
US (1) US20220227738A1 (https=)
EP (1) EP3972978A4 (https=)
JP (1) JP7502337B2 (https=)
KR (1) KR20220038289A (https=)
CN (1) CN114096544B (https=)
AU (1) AU2020279253A1 (https=)
BR (1) BR112021023359A2 (https=)
CA (1) CA3141604A1 (https=)
IL (1) IL288200A (https=)
MX (1) MX2021014177A (https=)
SG (1) SG11202112790SA (https=)
WO (1) WO2020236940A1 (https=)

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JP2022500385A (ja) 2018-09-10 2022-01-04 ミラティ セラピューティクス, インコーポレイテッド 組み合わせ療法
WO2020085504A1 (ja) 2018-10-26 2020-04-30 大鵬薬品工業株式会社 光照射ザンドマイヤー反応を用いたクロロアゾールカルボキシレート誘導体の製造方法
CN113164418A (zh) 2018-12-05 2021-07-23 米拉蒂治疗股份有限公司 组合疗法
WO2020146613A1 (en) 2019-01-10 2020-07-16 Mirati Therapeutics, Inc. Kras g12c inhibitors
WO2021041671A1 (en) 2019-08-29 2021-03-04 Mirati Therapeutics, Inc. Kras g12d inhibitors
CN114761012B (zh) 2019-09-24 2025-03-21 米拉蒂治疗股份有限公司 组合疗法
CN114867726B (zh) 2019-10-28 2023-11-28 默沙东有限责任公司 Kras g12c突变体的小分子抑制剂
WO2021093758A1 (zh) * 2019-11-15 2021-05-20 四川海思科制药有限公司 一种嘧啶并环衍生物及其在医药上的应用
US12479834B2 (en) 2019-11-29 2025-11-25 Taiho Pharmaceutical Co., Ltd. Phenol compound or salt thereof
PH12022551513A1 (en) 2019-12-20 2023-04-24 Mirati Therapeutics Inc Sos1 inhibitors
TWI770760B (zh) * 2020-01-08 2022-07-11 大陸商蘇州亞盛藥業有限公司 螺環四氫喹唑啉
WO2021245055A1 (en) 2020-06-02 2021-12-09 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
WO2022040469A1 (en) * 2020-08-19 2022-02-24 The Trustees Of The Stevens Institute Of Technology Spiro compounds as kras inhibitors
WO2022056307A1 (en) 2020-09-11 2022-03-17 Mirati Therapeutics, Inc. Crystalline forms of a kras g12c inhibitor
AU2021347232A1 (en) 2020-09-23 2023-04-27 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2022132200A1 (en) 2020-12-15 2022-06-23 Mirati Therapeutics, Inc. Azaquinazoline pan-kras inhibitors
EP4262803A4 (en) 2020-12-16 2025-03-12 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
WO2022133345A1 (en) 2020-12-18 2022-06-23 Erasca, Inc. Tricyclic pyridones and pyrimidones
CN114685502A (zh) * 2020-12-25 2022-07-01 由理生物医药(上海)有限公司 作为kras-g12c抑制剂的螺环类化合物
CN114805311B (zh) * 2021-01-21 2024-10-29 苏州亚盛药业有限公司 螺环茚
WO2022240971A2 (en) * 2021-05-11 2022-11-17 1200 Pharma Llc Kras g12d inhibitors and uses thereof
US20240293558A1 (en) 2021-06-16 2024-09-05 Erasca, Inc. Kras inhibitor conjugates
CA3224341A1 (en) 2021-09-01 2023-03-09 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
CN119156383A (zh) * 2021-11-09 2024-12-17 1200药业有限责任公司 选择性kras g12c抑制剂及其用途
JP2024543982A (ja) * 2021-12-01 2024-11-26 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング がんの処置のための縮環2-アミノ-3-シアノチオフェン及び誘導体
WO2023099624A1 (en) 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
AU2023218370B2 (en) * 2022-02-09 2024-11-28 Quanta Therapeutics, Inc. Kras modulators and uses thereof
IL317601A (en) 2022-05-25 2025-02-01 Quanta Therapeutics Inc Pyrimidine-based modulators and their uses
WO2024112654A1 (en) 2022-11-21 2024-05-30 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
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Also Published As

Publication number Publication date
EP3972978A1 (en) 2022-03-30
JP2022533398A (ja) 2022-07-22
KR20220038289A (ko) 2022-03-28
JP7502337B2 (ja) 2024-06-18
BR112021023359A2 (pt) 2022-02-01
CN114096544B (zh) 2025-08-12
WO2020236940A1 (en) 2020-11-26
CN114096544A (zh) 2022-02-25
EP3972978A4 (en) 2023-04-26
CA3141604A1 (en) 2020-11-26
MX2021014177A (es) 2022-04-25
IL288200A (en) 2022-01-01
US20220227738A1 (en) 2022-07-21
SG11202112790SA (en) 2021-12-30

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