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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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.)
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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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 (enExample)
EP (1) EP3972978A4 (enExample)
JP (1) JP7502337B2 (enExample)
KR (1) KR20220038289A (enExample)
CN (1) CN114096544B (enExample)
AU (1) AU2020279253A1 (enExample)
BR (1) BR112021023359A2 (enExample)
CA (1) CA3141604A1 (enExample)
IL (1) IL288200A (enExample)
MX (1) MX2021014177A (enExample)
SG (1) SG11202112790SA (enExample)
WO (1) WO2020236940A1 (enExample)

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EP3849535A4 (en) 2018-09-10 2022-06-29 Mirati Therapeutics, Inc. Combination therapies
EP3849537B1 (en) 2018-09-10 2024-10-23 Mirati Therapeutics, Inc. Combination therapies
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
MX2021002804A (es) 2018-12-05 2021-07-15 Mirati Therapeutics Inc Terapias de combinacion.
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
MX2022002465A (es) 2019-08-29 2022-05-19 Mirati Therapeutics Inc Inhibidores de kras g12d.
WO2021061749A1 (en) 2019-09-24 2021-04-01 Mirati Therapeutics, Inc. Combination therapies
UA129778C2 (uk) 2019-10-28 2025-07-30 Мерк Шарп Енд Доум Елелсі Низькомолекулярні інгібітори g12c-мутантного kras
CN114630832A (zh) * 2019-11-15 2022-06-14 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
EP4067343A4 (en) 2019-11-29 2024-01-03 Taiho Pharmaceutical Co., Ltd. NEW PHENOLIC COMPOUND OR SALT THEREOF
PH12022551513A1 (en) 2019-12-20 2023-04-24 Mirati Therapeutics Inc Sos1 inhibitors
WO2021139748A1 (en) * 2020-01-08 2021-07-15 Ascentage Pharma (Suzhou) Co., Ltd. Spirocyclic tetrahydroquinazolines
JP7808058B2 (ja) 2020-06-02 2026-01-28 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 がんを治療するための縮合環化2-アミノ-3-シアノチオフェン及び誘導体
WO2022040469A1 (en) * 2020-08-19 2022-02-24 The Trustees Of The Stevens Institute Of Technology Spiro compounds as kras inhibitors
EP4210833A4 (en) 2020-09-11 2024-09-11 Mirati Therapeutics, Inc. CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR
JP2023544450A (ja) 2020-09-23 2023-10-23 エラスカ・インコーポレイテッド 三環式ピリドン及びピリミドン
JP2023553492A (ja) 2020-12-15 2023-12-21 ミラティ セラピューティクス, インコーポレイテッド アザキナゾリン汎KRas阻害剤
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
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
KR20240055778A (ko) 2021-09-01 2024-04-29 노파르티스 아게 Tead 억제제를 포함하는 제약 조합물 및 암의 치료를 위한 이의 용도
CA3237274A1 (en) * 2021-11-09 2023-05-19 1200 Pharma Llc Select kras g12c inhibitors and uses thereof
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
WO2023099608A1 (en) * 2021-12-01 2023-06-08 Boehringer Ingelheim International Gmbh Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer
CA3243798A1 (en) * 2022-02-09 2023-08-17 Quanta Therapeutics, Inc. Kras Modulators and Their Uses
WO2023230190A1 (en) 2022-05-25 2023-11-30 Quanta Therapeutics, Inc. Pyrimidine based modulators and uses thereof
TW202430179A (zh) 2022-11-21 2024-08-01 美商樹線生物科學公司 螺環二氫哌喃并嘧啶KRas抑制劑
KR20260041941A (ko) 2023-03-15 2026-03-27 콴타 테라퓨틱스, 인크. Kras 조절 인자 및 이의 용도
WO2025038936A1 (en) 2023-08-17 2025-02-20 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
TW202528315A (zh) 2023-09-21 2025-07-16 美商樹線生物科學公司 螺環二氫哌喃并吡啶KRas抑制劑
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Also Published As

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

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