CA3180686A1 - Novel small molecules for targeted degradation of untargetable kras in cancer therapy - Google Patents

Novel small molecules for targeted degradation of untargetable kras in cancer therapy Download PDF

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Publication number
CA3180686A1
CA3180686A1 CA3180686A CA3180686A CA3180686A1 CA 3180686 A1 CA3180686 A1 CA 3180686A1 CA 3180686 A CA3180686 A CA 3180686A CA 3180686 A CA3180686 A CA 3180686A CA 3180686 A1 CA3180686 A1 CA 3180686A1
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CA
Canada
Prior art keywords
compound
kras
group bonded
cancer
group
Prior art date
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.)
Pending
Application number
CA3180686A
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English (en)
French (fr)
Inventor
Baskaran Pillai
Dinesh M.G.
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.)
Pillai Universal LLC
Original Assignee
Pillai Universal 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 Pillai Universal LLC filed Critical Pillai Universal LLC
Publication of CA3180686A1 publication Critical patent/CA3180686A1/en
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA3180686A 2020-06-04 2021-05-26 Novel small molecules for targeted degradation of untargetable kras in cancer therapy Pending CA3180686A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN202041023434 2020-06-04
IN202041023434 2020-06-04
PCT/IB2021/054591 WO2021245499A1 (en) 2020-06-04 2021-05-26 Novel small molecules for targeted degradation of untargetable kras in cancer therapy

Publications (1)

Publication Number Publication Date
CA3180686A1 true CA3180686A1 (en) 2021-12-09

Family

ID=78830675

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3180686A Pending CA3180686A1 (en) 2020-06-04 2021-05-26 Novel small molecules for targeted degradation of untargetable kras in cancer therapy

Country Status (11)

Country Link
US (1) US20230202981A1 (https=)
EP (1) EP4161511B1 (https=)
JP (1) JP7789016B2 (https=)
KR (1) KR20230019937A (https=)
CN (2) CN115768427B (https=)
AU (1) AU2021284517A1 (https=)
BR (1) BR112022024300A2 (https=)
CA (1) CA3180686A1 (https=)
IL (1) IL298672A (https=)
MX (1) MX2022015253A (https=)
WO (1) WO2021245499A1 (https=)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
EA202190749A1 (ru) 2018-09-10 2021-07-09 Мирати Терапьютикс, Инк. Способы комбинированной терапии
EP3849535A4 (en) 2018-09-10 2022-06-29 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
EP3849537B1 (en) 2018-09-10 2024-10-23 Mirati Therapeutics, Inc. Combination therapies
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
PH12022551513A1 (en) 2019-12-20 2023-04-24 Mirati Therapeutics Inc Sos1 inhibitors
EP4210833A4 (en) 2020-09-11 2024-09-11 Mirati Therapeutics, Inc. CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR
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
WO2025083563A1 (en) * 2023-10-18 2025-04-24 Pillai Universal Llc Effective therapeutic small-molecule inhibitors for metastatic cancer
WO2025083561A1 (en) * 2023-10-18 2025-04-24 Pillai Universal Llc Novel lead small molecule inhibitors on undruggable target towards anticancer activity
WO2025083564A1 (en) * 2023-10-18 2025-04-24 Pillai Universal Llc Novel small molecule degrader as a potential anticancer
WO2025083568A1 (en) * 2023-10-18 2025-04-24 Pillai Universal Llc Novel small-molecule protein kinase inhibitors for implications in cancer treatment
WO2025083570A1 (en) * 2023-10-18 2025-04-24 Pillai Universal Llc Novel small-molecule agents in overcoming tumor regression in cancers

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
OA12274A (en) * 2000-05-22 2006-05-09 Aventis Pharma Inc Arylmethylamine derivatives for use as tryptase inhibitors.
GB0012362D0 (en) * 2000-05-22 2000-07-12 Aventis Pharma Ltd Chemical compounds
HUP0402106A3 (en) * 2001-11-01 2009-07-28 Janssen Pharmaceutica Nv Heteroaryl amines as glycogen synthase kinase 3 beta inhibitors, process for their preparation and pharmaceutical compositions containing them
WO2007075896A2 (en) * 2005-12-22 2007-07-05 Kemia, Inc. Heterocyclic cytokine inhibitors
JP2013525308A (ja) * 2010-04-16 2013-06-20 キュリス,インコーポレイテッド K−ras変異を有する癌の治療
US20190284149A1 (en) * 2014-09-12 2019-09-19 Ariagen, Inc. Aryl hydrocarbon receptor modulator
CN106317055A (zh) * 2015-07-02 2017-01-11 中国科学院上海药物研究所 一类具有激酶抑制活性的化合物、制备方法和用途
WO2018140513A1 (en) * 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
CN110885332B (zh) * 2019-12-06 2022-03-18 中国人民解放军第二军医大学 一种PDEδ蛋白降解靶向嵌合体及其制备方法和应用

Also Published As

Publication number Publication date
EP4161511A1 (en) 2023-04-12
JP7789016B2 (ja) 2025-12-19
KR20230019937A (ko) 2023-02-09
MX2022015253A (es) 2023-03-14
IL298672A (en) 2023-01-01
BR112022024300A2 (pt) 2023-01-24
TW202210465A (zh) 2022-03-16
CN115768427B (zh) 2025-03-28
WO2021245499A1 (en) 2021-12-09
CN115768427A (zh) 2023-03-07
EP4161511B1 (en) 2026-04-29
AU2021284517A1 (en) 2023-01-05
JP2023529354A (ja) 2023-07-10
EP4161511A4 (en) 2024-07-17
CN120208921A (zh) 2025-06-27
US20230202981A1 (en) 2023-06-29

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