1. WO2026085629 - SUBSTITUTED HETEROCYCLIC COMPOUNDS, COMPOSITIONS COMPRISING THEM AND USES THEREOF

Publication Number WO/2026/085629

Publication Date 30.04.2026

International Application No. PCT/CA2025/051411

International Filing Date 24.10.2025

IPC

C07D 513/04 2006.1

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
513	Heterocyclic 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/, C07D477/232
02	in which the condensed system contains two hetero rings
04	Ortho-condensed systems

A61K 31/428 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41	having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425	Thiazoles
428	condensed with carbocyclic rings

A61K 31/429 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41	having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425	Thiazoles
429	condensed with heterocyclic ring systems

A61K 31/438 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435	having six-membered rings with one nitrogen as the only ring hetero atom
438	the ring being spiro-condensed with carbocyclic or heterocyclic ring systems

A61K 31/439 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435	having six-membered rings with one nitrogen as the only ring hetero atom
439	the ring forming part of a bridged ring system, e.g. quinuclidine

A61K 31/454 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435	having six-membered rings with one nitrogen as the only ring hetero atom
44	Non-condensed pyridines; Hydrogenated derivatives thereof
445	Non-condensed piperidines, e.g. piperocaine
4523	containing further heterocyclic ring systems
454	containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone

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C07D 513/04 2006.1

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
513	Heterocyclic 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/, C07D477/232
02	in which the condensed system contains two hetero rings
04	Ortho-condensed systems

A61K 31/428 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41	having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425	Thiazoles
428	condensed with carbocyclic rings

A61K 31/429 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41	having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425	Thiazoles
429	condensed with heterocyclic ring systems

A61K 31/438 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435	having six-membered rings with one nitrogen as the only ring hetero atom
438	the ring being spiro-condensed with carbocyclic or heterocyclic ring systems

A61K 31/439 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435	having six-membered rings with one nitrogen as the only ring hetero atom
439	the ring forming part of a bridged ring system, e.g. quinuclidine

A61K 31/454 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435	having six-membered rings with one nitrogen as the only ring hetero atom
44	Non-condensed pyridines; Hydrogenated derivatives thereof
445	Non-condensed piperidines, e.g. piperocaine
4523	containing further heterocyclic ring systems
454	containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone

A61K 31/496 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495	having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
496	Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin

A61K 31/499 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495	having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
499	Spiro-condensed pyrazines or piperazines

A61K 31/551 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
55	having seven-membered rings, e.g. azelastine, pentylenetetrazole
551	having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep

A61K 31/4184 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41	having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4164	1,3-Diazoles
4184	condensed with carbocyclic rings, e.g. benzimidazoles

A61K 31/4985 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495	having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4985	Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems

A61K 31/4995 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495	having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4995	Pyrazines or piperazines forming part of bridged ring systems

A61K 31/5377 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535	having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5375	1,4-Oxazines, e.g. morpholine
5377	not condensed and containing further heterocyclic rings, e.g. timolol

A61K 31/5383 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535	having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5375	1,4-Oxazines, e.g. morpholine
5383	ortho- or peri-condensed with heterocyclic ring systems

A61K 31/5386 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535	having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5375	1,4-Oxazines, e.g. morpholine
5386	spiro-condensed or forming part of bridged ring systems

A61P 35/00 2006.1

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35	Antineoplastic agents

C07D 409/04 2006.1

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
409	Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02	containing two hetero rings
04	directly linked by a ring-member-to-ring- member bond

C07D 409/14 2006.1

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
409	Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
14	containing three or more hetero rings

C07D 413/12 2006.1

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
413	Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02	containing two hetero rings
12	linked by a chain containing hetero atoms as chain links

C07D 417/04 2006.1

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
417	Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02	containing two hetero rings
04	directly linked by a ring-member-to-ring- member bond

C07D 417/14 2006.1

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
417	Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
14	containing three or more hetero rings

C07D 451/02 2006.1

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
451	Heterocyclic compounds containing 8-azabicyclo octane, 9-azabicyclo nonane, or 3-oxa-9-azatricyclo nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
02	containing not further condensed 8-azabicyclo octane or 3-oxa-9-azatricyclo nonane ring systems, e.g. tropane; Cyclic acetals thereof

C07D 487/04 2006.1

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
487	Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02	in which the condensed system contains two hetero rings
04	Ortho-condensed systems

C07D 491/048 2006.1

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
491	Heterocyclic 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/-C07D459/290
02	in which the condensed system contains two hetero rings
04	Ortho-condensed systems
044	with only one oxygen atom as ring hetero atom in the oxygen-containing ring
048	the oxygen-containing ring being five-membered

C07D 519/00 2006.1

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
519	Heterocyclic 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/ or C07D455/257

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Applicants

• UNIVERSITÉ DE MONTRÉAL [CA]/[CA]

Inventors

• BEAULIEU, Pierre Louis
• BEAULIEU, Eric
• CHACON-HUETE, Franklin
• DANESHMANDKASHANI, Pargol
• JARVIS, Scott
• MESSINA, Cynthia
• REDDY, Thumkunta Jagadeeswar
• WAHHAB, Amal
• GHAVRE, Mukund
• SCHUETZ, Doris
• TRUDEL, Vincent
• VAILLANCOURT, Mick
• SAYES, Morgane
• LY, Vu Linh
• TREMBLAY, Maxime
• DORE, Michaël
• LAVOIE, Hugo

Agents

• ROBIC AGENCE PI S.E.C. / ROBIC IP AGENCY LP

Priority Data

114141218		23.10.2025		TW
63/711,451		24.10.2024		US

Publication Language English (en)

Filing Language English (en)

Designated States

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AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CV, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IQ, IR, IS, IT, JM, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, MG, MK, MN, MU, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UY, UZ, VC, VN, WS, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, CV, GH, GM, KE, LR, LS, MU, MW, MZ, NA, RW, SC, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, ME, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)

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Title

(EN) SUBSTITUTED HETEROCYCLIC COMPOUNDS, COMPOSITIONS COMPRISING THEM AND USES THEREOF

(FR) COMPOSÉS HÉTÉROCYCLIQUES SUBSTITUÉS, COMPOSITIONS LES COMPRENANT ET LEURS UTILISATIONS

Abstract

(EN) Compounds, compositions, and their use in the treatment of a proliferative disease or condition such as a said proliferative disease or disorder characterized by dysregulation of the RAS-ERK pathway (e.g. cancer, RASopathies), for instance a disease or disorder associated with a KRAS gene mutation or an amplification of the KRAS locus. The compounds disclosed are of Formula (I) as defined herein, or a pharmaceutically acceptable salt and/or solvate thereof.

(FR) L'invention concerne des composés, des compositions et leur utilisation dans le traitement d'une maladie ou d'un état prolifératif tel qu'une maladie ou un trouble prolifératif caractérisé par une dysrégulation de la voie RAS-ERK (par exemple, le cancer, les RASopathies), par exemple une maladie ou un trouble associé à une mutation du gène KRAS ou une amplification du locus KRAS. Les composés divulgués sont de formule (I) telle que définie dans la description, ou un sel et/ou solvate pharmaceutiquement acceptable de ceux-ci.

Latest bibliographic data on file with the International Bureau

The publication of an international application under the Patent Cooperation Treaty in PATENTSCOPE (which constitutes an element of the Gazette) does not imply the expression of any opinion whatsoever on the part of the International Bureau of WIPO concerning the legal status of any country, territory, city or area or of its authorities, or concerning the delimitation of its frontiers or boundaries.