IL320388A - Macrocyclic KRAS inhibitors and methods of use - Google Patents

Macrocyclic KRAS inhibitors and methods of use

Info

Publication number
IL320388A
IL320388A IL320388A IL32038825A IL320388A IL 320388 A IL320388 A IL 320388A IL 320388 A IL320388 A IL 320388A IL 32038825 A IL32038825 A IL 32038825A IL 320388 A IL320388 A IL 320388A
Authority
IL
Israel
Prior art keywords
macrocyclic
methods
kras inhibitors
kras
inhibitors
Prior art date
Application number
IL320388A
Other languages
English (en)
Hebrew (he)
Inventor
Adriano Bauer
Albert Amegadzie
Andrew Smaligo
Benjamin Wigman
Brian Alan Lanman
Christopher Mohr
Fabien Emmetiere
John Charles Stellwagen
Jose M Medina
Liping H Pettus
Michael Masaharu Yamano
Ning Chen
Primali Vasundera Navaratne
Qingyian Liu
Quentin Tercenio
Rene Rahimoff
Ryan Paul Wurz
Shon Booker
Wei Zhao
Xiaofen Li
Yunxiao Li
Zhichen Wu
Aaron C Siegmund
Jeffrey Jackson
Original Assignee
Amgen Inc
Adriano Bauer
Albert Amegadzie
Andrew Smaligo
Benjamin Wigman
Brian Alan Lanman
Christopher Mohr
Fabien Emmetiere
John Charles Stellwagen
Jose M Medina
Liping H Pettus
Michael Masaharu Yamano
Ning Chen
Primali Vasundera Navaratne
Qingyian Liu
Quentin Tercenio
Rene Rahimoff
Ryan Paul Wurz
Shon Booker
Wei Zhao
Xiaofen Li
Yunxiao Li
Zhichen Wu
Aaron C Siegmund
Jeffrey Jackson
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 Amgen Inc, Adriano Bauer, Albert Amegadzie, Andrew Smaligo, Benjamin Wigman, Brian Alan Lanman, Christopher Mohr, Fabien Emmetiere, John Charles Stellwagen, Jose M Medina, Liping H Pettus, Michael Masaharu Yamano, Ning Chen, Primali Vasundera Navaratne, Qingyian Liu, Quentin Tercenio, Rene Rahimoff, Ryan Paul Wurz, Shon Booker, Wei Zhao, Xiaofen Li, Yunxiao Li, Zhichen Wu, Aaron C Siegmund, Jeffrey Jackson filed Critical Amgen Inc
Publication of IL320388A publication Critical patent/IL320388A/en

Links

Classifications

    • 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
    • C07D471/22Heterocyclic 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 systems contains four 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
    • A61K31/529Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring systems
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D498/22Heterocyclic 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 four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
IL320388A 2022-11-14 2023-11-14 Macrocyclic KRAS inhibitors and methods of use IL320388A (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US202263383674P 2022-11-14 2022-11-14
US202363497978P 2023-04-24 2023-04-24
US202363582751P 2023-09-14 2023-09-14
PCT/US2023/079582 WO2024107686A1 (en) 2022-11-14 2023-11-14 Macrocyclic kras inhibitors and methods of use

Publications (1)

Publication Number Publication Date
IL320388A true IL320388A (en) 2025-06-01

Family

ID=91085388

Family Applications (1)

Application Number Title Priority Date Filing Date
IL320388A IL320388A (en) 2022-11-14 2023-11-14 Macrocyclic KRAS inhibitors and methods of use

Country Status (15)

Country Link
US (3) US12570672B2 (https=)
EP (1) EP4598921A1 (https=)
JP (3) JP7743484B2 (https=)
KR (2) KR102919887B1 (https=)
CN (1) CN120500482A (https=)
AU (1) AU2023382606A1 (https=)
CL (1) CL2025001425A1 (https=)
CO (1) CO2025006813A2 (https=)
IL (1) IL320388A (https=)
JO (1) JOP20250111A1 (https=)
MX (1) MX2025005539A (https=)
PE (1) PE20252237A1 (https=)
TW (1) TW202430532A (https=)
UY (1) UY40522A (https=)
WO (1) WO2024107686A1 (https=)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN120813588A (zh) 2023-02-14 2025-10-17 豪夫迈·罗氏有限公司 用于治疗癌症的三环化合物
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2025123007A1 (en) * 2023-12-08 2025-06-12 Kestrel Therapeutics Inc. Ras inhibitors and methods of use thereof
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025194054A1 (en) * 2024-03-14 2025-09-18 Amgen Inc. Spirocyclic compounds as modulators of kras and uses thereof
TW202602882A (zh) * 2024-03-14 2026-01-16 美商安進公司 作為kras調節劑的大環化合物及其用途
WO2025230862A1 (en) * 2024-04-29 2025-11-06 Amgen Inc. Macrocyclic amino compounds as modulators of kras and uses therof
WO2025230860A1 (en) * 2024-04-29 2025-11-06 Amgen Inc. Solid forms of macrocyclic compounds and uses thereof
WO2025230878A1 (en) * 2024-04-29 2025-11-06 Amgen Inc. Macrocyclic compounds as modulators of kras and uses thereof
WO2025240465A1 (en) * 2024-05-14 2025-11-20 Amgen Inc. Processes for preparing macrocyclic compounds
WO2025240582A1 (en) * 2024-05-14 2025-11-20 Amgen Inc. Macrocyclic compounds as modulators of kras and uses thereof
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ras抑制劑
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026035947A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload
WO2026035945A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026055477A1 (en) * 2024-09-06 2026-03-12 Amgen Inc. Macrocyclic compounds as modulators of kras and uses thereof
WO2026064527A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload
WO2026064520A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4302834A3 (en) 2016-07-12 2024-07-17 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
JP7240319B2 (ja) 2017-01-23 2023-03-15 レヴォリューション・メディスンズ,インコーポレイテッド アロステリックshp2阻害剤としての二環式化合物
AU2018273356B2 (en) 2017-05-22 2021-09-16 Amgen Inc. KRAS G12C inhibitors and methods of using the same
AU2018329920B2 (en) 2017-09-08 2022-12-01 Amgen Inc. Inhibitors of KRAS G12C and methods of using the same
TW201930292A (zh) 2017-10-12 2019-08-01 美商銳新醫藥公司 作為變構shp2抑制劑的吡啶、吡嗪和三嗪化合物
JP2022513967A (ja) 2018-12-20 2022-02-09 アムジエン・インコーポレーテツド Kif18a阻害剤として有用なヘテロアリールアミド
JP7686559B2 (ja) 2018-12-20 2025-06-02 アムジエン・インコーポレーテツド Kif18a阻害剤
AU2019401495B2 (en) 2018-12-20 2025-06-26 Amgen Inc. Heteroaryl amides useful as KIF18A inhibitors
MA54543A (fr) 2018-12-20 2022-03-30 Amgen Inc Inhibiteurs de kif18a
MX2022002465A (es) * 2019-08-29 2022-05-19 Mirati Therapeutics Inc Inhibidores de kras g12d.
CN115003668A (zh) * 2020-01-21 2022-09-02 南京明德新药研发有限公司 作为kras抑制剂的大环类化合物
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
BR112023016299A2 (pt) * 2021-02-16 2023-11-28 L Livermore Nat Security Llc Composições e métodos para inibir kras
CA3211725A1 (en) * 2021-03-17 2022-09-22 Tao Jiang Pyrimidine-fused cyclic compound, preparation method therefor and use thereof
US20250255868A1 (en) * 2021-04-09 2025-08-14 Hangzhou Innogate Pharma Co., Ltd. Heterocyclic compound acting as kras g12d inhibitor
CN115304623A (zh) * 2021-04-30 2022-11-08 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
WO2022246092A1 (en) 2021-05-21 2022-11-24 Blossomhill Therapeutics, Inc. Macrocyclic compounds for treating disease
WO2023040989A1 (en) 2021-09-16 2023-03-23 Suzhou Zanrong Pharma Limited Kras g12c inhibitors and uses thereof
EP4573095A1 (en) 2022-08-17 2025-06-25 Treeline Biosciences, Inc. Pyridopyrimidine kras inhibitors

Also Published As

Publication number Publication date
CN120500482A (zh) 2025-08-15
PE20252237A1 (es) 2025-09-15
US12570672B2 (en) 2026-03-10
CL2025001425A1 (es) 2025-08-29
US20250304599A1 (en) 2025-10-02
JOP20250111A1 (ar) 2025-05-13
TW202430532A (zh) 2024-08-01
UY40522A (es) 2024-05-15
JP2025539080A (ja) 2025-12-03
US20240294551A1 (en) 2024-09-05
JP2025179208A (ja) 2025-12-09
JP7743484B2 (ja) 2025-09-24
MX2025005539A (es) 2025-06-02
CO2025006813A2 (es) 2025-06-06
JP2024071370A (ja) 2024-05-24
KR20250095749A (ko) 2025-06-26
WO2024107686A1 (en) 2024-05-23
EP4598921A1 (en) 2025-08-13
KR102919887B1 (ko) 2026-01-29
KR20260017504A (ko) 2026-02-05
AU2023382606A1 (en) 2025-05-08
US20250236631A1 (en) 2025-07-24

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