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PE20250162A1 - Inhibidores de ripk1 y metodos de uso - Google Patents

Inhibidores de ripk1 y metodos de uso

Info

Publication number
PE20250162A1
PE20250162A1 PE2024002605A PE2024002605A PE20250162A1 PE 20250162 A1 PE20250162 A1 PE 20250162A1 PE 2024002605 A PE2024002605 A PE 2024002605A PE 2024002605 A PE2024002605 A PE 2024002605A PE 20250162 A1 PE20250162 A1 PE 20250162A1
Authority
PE
Peru
Prior art keywords
ripk1
halogen
optionally substituted
substituents independently
independently selected
Prior art date
Application number
PE2024002605A
Other languages
English (en)
Inventor
Joanna L Chen
Yi-Heng Chen
Erin F Dimauro
Min Lu
Joey L Methot
Andrew J Musacchio
Anandan Palani
Barbara Pio
Duque Lorena Rico
Phieng Siliphaivanh
Brandon A Vara
Xavier Fradera
Original Assignee
Merck Sharp And Dohme Llc
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 Merck Sharp And Dohme Llc filed Critical Merck Sharp And Dohme Llc
Publication of PE20250162A1 publication Critical patent/PE20250162A1/es

Links

Classifications

    • 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
    • C07D487/04Ortho-condensed 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41961,2,4-Triazoles
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/429Thiazoles 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further 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
    • A61K31/535Heterocyclic 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • C07D471/04Ortho-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
    • C07D498/04Ortho-condensed systems
    • 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
    • C07D513/02Heterocyclic 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 two hetero rings
    • C07D513/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente invencion proporciona compuestos de formula I, o una sal farmaceuticamente aceptable de los mismos, en donde R1 se selecciona entre cicloalquilo C3-C6, arilo y heteroarilo, donde cada uno de estos esta opcionalmente sustituido con uno a cuatro sustituyentes seleccionados independientemente entre halogeno, -CN, entre otros. R2 se selecciona entre cicloalquilo C3-C10, heterocicloalquilo, arilo y heteroarilo, donde cada uno de estos esta opcionalmente sustituido con uno a cuatro sustituyentes seleccionados independientemente entre halogeno, -CN, entre otros. R3 y R4, junto con los atomos a los que estan unidos, forman un anillo de 5 o 6 miembros condensado con el anillo triazol, en donde el anillo de 5 o 6 miembros comprende opcionalmente heteroatomos seleccionados entre N, O, o S y esta opcionalmente sustituido con uno a cuatro sustituyentes seleccionados independientemente entre halogeno, -OH y alquilo C1-C6. Los compuestos de la formula I actuan como inhibidores de la proteina quinasa serina/treonina que interactua con el receptor 1 (RIPK1). RIPK1 funciona en una variedad de vias celulares relacionadas como la senalizacion inmunitaria innata, muerte celular, ante ello los compuestos de la invencion permitirian contrarrestar a RIPK1.
PE2024002605A 2022-05-19 2023-05-17 Inhibidores de ripk1 y metodos de uso PE20250162A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202263343591P 2022-05-19 2022-05-19
US202363491422P 2023-03-21 2023-03-21
PCT/US2023/022462 WO2023225041A1 (en) 2022-05-19 2023-05-17 Ripk1 inhibitors and methods of use

Publications (1)

Publication Number Publication Date
PE20250162A1 true PE20250162A1 (es) 2025-01-22

Family

ID=86771477

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2024002605A PE20250162A1 (es) 2022-05-19 2023-05-17 Inhibidores de ripk1 y metodos de uso

Country Status (17)

Country Link
US (2) US20250326766A1 (es)
EP (1) EP4526300A1 (es)
JP (1) JP7680639B1 (es)
KR (1) KR20250012616A (es)
CN (1) CN119585270A (es)
AU (1) AU2023273636A1 (es)
CA (1) CA3256884A1 (es)
CL (1) CL2024003468A1 (es)
CO (1) CO2024015538A2 (es)
CR (1) CR20240506A (es)
DO (1) DOP2024000236A (es)
GE (1) GEAP202516658A (es)
IL (1) IL317043A (es)
MX (1) MX2024014166A (es)
PE (1) PE20250162A1 (es)
TW (1) TWI878888B (es)
WO (1) WO2023225041A1 (es)

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101171211B1 (ko) * 2004-03-10 2012-08-07 얀센 파마슈티카 엔.브이. Mtp를 저해하는 5-원 헤테로사이클에 의해 치환된 아릴 피페리딘 또는 피페라진
RS63203B1 (sr) * 2016-12-09 2022-06-30 Denali Therapeutics Inc Jedinjenja korisna kao inhibitori ripk1
RS65308B1 (sr) * 2017-07-14 2024-04-30 Hoffmann La Roche Biciklična ketonska jedinjenja i postupci za njihovu upotrebu
EP3908586B1 (en) * 2019-01-11 2022-12-21 F. Hoffmann-La Roche AG Bicyclic pyrrolotriazolr ketone compounds and methods of use thereof

Also Published As

Publication number Publication date
MX2024014166A (es) 2024-12-06
US20250326766A1 (en) 2025-10-23
US20240025912A1 (en) 2024-01-25
WO2023225041A1 (en) 2023-11-23
JP2025521068A (ja) 2025-07-08
TW202406906A (zh) 2024-02-16
KR20250012616A (ko) 2025-01-24
IL317043A (en) 2025-01-01
CA3256884A1 (en) 2023-11-23
AU2023273636A1 (en) 2024-12-05
TWI878888B (zh) 2025-04-01
EP4526300A1 (en) 2025-03-26
CN119585270A (zh) 2025-03-07
CL2024003468A1 (es) 2025-04-11
CO2024015538A2 (es) 2024-12-30
CR20240506A (es) 2025-01-07
GEAP202516658A (en) 2025-03-25
DOP2024000236A (es) 2024-12-15
JP7680639B1 (ja) 2025-05-20

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