PE20252237A1 - Inhibidores macrociclicos de kras y metodos de uso - Google Patents

Inhibidores macrociclicos de kras y metodos de uso

Info

Publication number
PE20252237A1
PE20252237A1 PE2025001022A PE2025001022A PE20252237A1 PE 20252237 A1 PE20252237 A1 PE 20252237A1 PE 2025001022 A PE2025001022 A PE 2025001022A PE 2025001022 A PE2025001022 A PE 2025001022A PE 20252237 A1 PE20252237 A1 PE 20252237A1
Authority
PE
Peru
Prior art keywords
alkylene
compound
salt
macrocyclic
methods
Prior art date
Application number
PE2025001022A
Other languages
English (en)
Spanish (es)
Inventor
Albert Amegadzie
Ning Chen
Qingyian Liu
Ryan Paul Wurz
Christopher Mohr
Shon Booker
Liping H Pettus
Jose M Medina
Primali Vasundera Navaratne
Rene Rahimoff
Brian Alan Lanman
Fabien Emmetiere
Andrew Smaligo
Michael Masaharu Yamano
Adriano Bauer
Benjamin Wigman
John Charles Stellwagen
Kexue Li
Quentin Tercenio
Wei Zhao
Xiaofen Li
Yunxiao Li
Zhichen Wu
Aaron C Siegmund
Jeffrey Jackson
Original Assignee
Amgen Inc
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 filed Critical Amgen Inc
Publication of PE20252237A1 publication Critical patent/PE20252237A1/es

Links

Classifications

    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or 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
    • A61K31/55Heterocyclic 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
    • 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
    • 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

  • Health & Medical Sciences (AREA)
  • Chemical & Material 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)
PE2025001022A 2022-11-14 2023-11-14 Inhibidores macrociclicos de kras y metodos de uso PE20252237A1 (es)

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
PE20252237A1 true PE20252237A1 (es) 2025-09-15

Family

ID=91085388

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2025001022A PE20252237A1 (es) 2022-11-14 2023-11-14 Inhibidores macrociclicos de kras y metodos de uso

Country Status (13)

Country Link
US (3) US20240294551A1 (enExample)
EP (1) EP4598921A1 (enExample)
JP (3) JP7743484B2 (enExample)
KR (1) KR20250095749A (enExample)
CN (1) CN120500482A (enExample)
AU (1) AU2023382606A1 (enExample)
CL (1) CL2025001425A1 (enExample)
CO (1) CO2025006813A2 (enExample)
IL (1) IL320388A (enExample)
MX (1) MX2025005539A (enExample)
PE (1) PE20252237A1 (enExample)
TW (1) TW202430532A (enExample)
WO (1) WO2024107686A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4469164A1 (en) 2023-02-14 2024-12-04 F. Hoffmann-La Roche AG Tricyclic compounds for the treatment of cancer
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. 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
WO2025194057A1 (en) * 2024-03-14 2025-09-18 Amgen Inc. Macrocyclic compounds as modulators of kras and uses thereof
WO2025194054A1 (en) * 2024-03-14 2025-09-18 Amgen Inc. Spirocyclic compounds as modulators of kras and uses thereof
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
WO2025240582A1 (en) * 2024-05-14 2025-11-20 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
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021041671A1 (en) * 2019-08-29 2021-03-04 Mirati Therapeutics, Inc. Kras g12d inhibitors
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
EP4262807A4 (en) * 2020-12-15 2025-04-23 Mirati Therapeutics, Inc. Azachinazoline pan-KRAS inhibitors
US11999753B2 (en) * 2020-12-16 2024-06-04 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-KRas inhibitors
MX2023008463A (es) * 2021-02-16 2023-12-07 Leidos Biomedical Res Inc Composiciones y métodos para la inhibición del gen del virus de sarcoma de rata kirsten (kras).
US20240174691A1 (en) * 2021-03-17 2024-05-30 Genfleet Therapeutics (Shanghai) Inc. Pyrimidine-fused cyclic compound, preparation method therefor and use thereof
WO2022214102A1 (zh) * 2021-04-09 2022-10-13 杭州英创医药科技有限公司 作为kras g12d抑制剂的杂环化合物
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

Also Published As

Publication number Publication date
JP2024071370A (ja) 2024-05-24
WO2024107686A1 (en) 2024-05-23
TW202430532A (zh) 2024-08-01
CL2025001425A1 (es) 2025-08-29
KR20250095749A (ko) 2025-06-26
AU2023382606A1 (en) 2025-05-08
US20250304599A1 (en) 2025-10-02
JP7743484B2 (ja) 2025-09-24
JP2025539080A (ja) 2025-12-03
US20240294551A1 (en) 2024-09-05
JP2025179208A (ja) 2025-12-09
US20250236631A1 (en) 2025-07-24
CN120500482A (zh) 2025-08-15
MX2025005539A (es) 2025-06-02
IL320388A (en) 2025-06-01
EP4598921A1 (en) 2025-08-13
CO2025006813A2 (es) 2025-06-06

Similar Documents

Publication Publication Date Title
PE20252237A1 (es) Inhibidores macrociclicos de kras y metodos de uso
PE20251288A1 (es) Compuestos heterociclicos como inmunomoduladores
CO5700774A2 (es) Derivados de triazol como inhibidores de 11-beta-hidroxiesteroide deshidrogenasa-1
AR034390A1 (es) Derivados de 1-sulfonil-tetrahidro quinolinas sustituidas, composiciones farmaceuticas y el uso de las mismas para la elaboracion de medicamentos como inhibidores de la gama secretasa
AR110153A1 (es) ÁCIDOS PROPIÓNICOS 3-SUSTITUIDOS COMO INHIBIDORES DE LA INTEGRINA aV
PE20212303A1 (es) Inhibidores aza-heterobiciclicos de mat2a y metodos de uso en el tratamiento de cancer
AR046297A1 (es) Inhibidores de la dpp - iv metodos para prepararlos y composiciones farmaceuticas que los contienen como agente activo
PE20240327A1 (es) Heterociclos con sustitucion amino para tratar canceres con mutaciones de egfr
KR940701264A (ko) 안과질환에 대한 마크로라이드 화합물의 용도
AR053652A1 (es) Derivados de indol como inhibidores de proteina quinasas. composiciones farmaceuticas
AR064304A1 (es) Formulaciones de ansamicina y sus metodos de uso
RU2008116844A (ru) Ацилированные производные спиропиперидина как модуляторы рецептора меланокортина-4
AR079231A1 (es) Derivados de imidazoquinolina
PE20090630A1 (es) Derivados de indol 2-carboxi sustituidos y metodos para su utilizacion
AR038235A1 (es) Compuestos de espiropiperidina n-sustituidos como ligandos para el receptor orl-1
AR037534A1 (es) Derivado de adamantano, su uso en la fabricacion de un medicamento para usar en terapia, composicion farmaceutica, proceso para la preparacion de dicho compuesto y dicha composicion y compuestos intermediarios
AR054090A1 (es) Derivados de quinuclidina como antagonistas del receptor muscarinico m3. composiciones farmaceuticas y proceso de obtencion
AR036391A1 (es) Uso de un compuesto de prostaglandina para preparar una composicion farmaceutica para abrir los canales de cic en un mamifero y compuestos de prostaglandina
PE20230177A1 (es) COMPUESTOS HETEROCICLICOS DE ARILMETILENO COMO BLOQUEADORES DEL CANAL SHAKER DE POTASIO Kv1.3
AR123648A1 (es) Compuestos de carbamoilpiridona tricíclicos puenteados y sus usos
PE20242099A1 (es) Compuestos de piridotriazina sustituidos y usos de estos
PE20060483A1 (es) Compuestos heterociclicos como antagonistas de nk1
RU2013146659A (ru) Способы лечения рака
PE20220169A1 (es) Compuestos macrociclicos como agonistas de sting
AR123049A1 (es) Compuestos terapéuticos y modos de uso