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IL281802B2 - Use of an inhibitor of an ent family transporter in the treatment of cancer and combination thereof with an adenosine receptor antagonist - Google Patents

Use of an inhibitor of an ent family transporter in the treatment of cancer and combination thereof with an adenosine receptor antagonist

Info

Publication number
IL281802B2
IL281802B2 IL281802A IL28180221A IL281802B2 IL 281802 B2 IL281802 B2 IL 281802B2 IL 281802 A IL281802 A IL 281802A IL 28180221 A IL28180221 A IL 28180221A IL 281802 B2 IL281802 B2 IL 281802B2
Authority
IL
Israel
Prior art keywords
cancer
inhibitor
treatment
combination
receptor antagonist
Prior art date
Application number
IL281802A
Other languages
Hebrew (he)
Other versions
IL281802A (en
IL281802B1 (en
Original Assignee
iTeos Belgium SA
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
Priority claimed from BE20180115A external-priority patent/BE1026612B1/en
Application filed by iTeos Belgium SA filed Critical iTeos Belgium SA
Publication of IL281802A publication Critical patent/IL281802A/en
Publication of IL281802B1 publication Critical patent/IL281802B1/en
Publication of IL281802B2 publication Critical patent/IL281802B2/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/49—Cinchonan derivatives, e.g. quinine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/4965—Non-condensed pyrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
IL281802A 2018-09-27 2021-03-25 Use of an inhibitor of an ent family transporter in the treatment of cancer and combination thereof with an adenosine receptor antagonist IL281802B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862737717P 2018-09-27 2018-09-27
BE20180115A BE1026612B1 (en) 2018-09-27 2018-09-27 USE OF AN ENT FAMILY CARRIER INHIBITOR IN THE TREATMENT OF CANCER AND COMBINATION THEREOF WITH AN ADENOSINE RECEPTOR ANTAGONIST
PCT/EP2019/076244 WO2020065036A1 (en) 2018-09-27 2019-09-27 Use of an inhibitor of an ent family transporter in the treatment of cancer and combination thereof with an adenosine receptor antagonist

Publications (3)

Publication Number Publication Date
IL281802A IL281802A (en) 2021-05-31
IL281802B1 IL281802B1 (en) 2025-06-01
IL281802B2 true IL281802B2 (en) 2025-10-01

Family

ID=68109305

Family Applications (1)

Application Number Title Priority Date Filing Date
IL281802A IL281802B2 (en) 2018-09-27 2021-03-25 Use of an inhibitor of an ent family transporter in the treatment of cancer and combination thereof with an adenosine receptor antagonist

Country Status (4)

Country Link
JP (1) JP7641894B2 (en)
BR (1) BR112021006033A2 (en)
IL (1) IL281802B2 (en)
WO (1) WO2020065036A1 (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102640927B1 (en) 2017-03-30 2024-02-27 아이테오스 벨지움 에스에이 2-Oxo-thiazole derivatives as A2A inhibitors and compounds for use in cancer treatment
US11376255B2 (en) 2018-09-11 2022-07-05 iTeos Belgium SA Thiocarbamate derivatives as A2A inhibitors, pharmaceutical composition thereof and combinations with anticancer agents
WO2020053263A1 (en) * 2018-09-11 2020-03-19 Iteos Therapeutics S.A. Thiocarbamate derivatives as a2a inhibitors, pharmaceutical composition thereof and combinations with anticancer agents
AU2020395495B2 (en) * 2019-12-02 2024-05-09 Astrazeneca Ab Solid pharmaceutical formulations of 6-(2-chloro-6-methylpyridin-4-yl)-5-(-4-fluorophenyl)-1,2,4-triazin-3-amine
CN117136242A (en) 2021-02-17 2023-11-28 Iteos比利时公司 Compounds, compositions and methods of treatment thereof
JP2024537110A (en) * 2021-10-06 2024-10-10 アイテオ ベルギウム エスエー Macrocyclic compounds having ENT1 inhibitory activity
JP2024535501A (en) * 2021-10-06 2024-09-30 アイテオ ベルギウム エスエー Methods for producing macrocyclic compounds with ENT1 inhibitory activity
WO2025104613A1 (en) 2023-11-14 2025-05-22 iTeos Belgium SA Ent1 inhibitors in combination with checkpoint inhibitors
WO2025163520A1 (en) * 2024-01-30 2025-08-07 iTeos Belgium SA Ent1 inhibitors for use in the treatment of diseases with increased adenosine levels
WO2025202864A1 (en) 2024-03-25 2025-10-02 iTeos Belgium SA Ent1 inhibitors in combination with oncolytic viruses and their use in the treatment of cancer

Citations (3)

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Publication number Priority date Publication date Assignee Title
WO2007140181A2 (en) * 2006-05-26 2007-12-06 King Pharmaceuticals Research And Development, Inc. Combination therapy comprising an adenosine uptake inhibitor and a non-selective adenosine receptor antagonist
WO2009011897A1 (en) * 2007-07-17 2009-01-22 Combinatorx, Incorporated Combinations for the treatment of b-cell proliferative disorders
WO2012055015A1 (en) * 2010-10-26 2012-05-03 Alberta Health Services Combination comprising an atp analog and an adenosine receptor antagonist or a nucleobase/nucleoside analog for the treatment of cancer

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EP0295317A1 (en) * 1987-06-16 1988-12-21 BOEHRINGER INGELHEIM INTERNATIONAL GmbH Pharmaceutical composition for the treatment of tumors
GB8819626D0 (en) * 1988-08-18 1988-09-21 Boehringer Ingelheim Int Pharmaceutical composition for treatment of tumours
GB0906579D0 (en) 2009-04-16 2009-05-20 Vernalis R&D Ltd Pharmaceuticals, compositions and methods of making and using the same
US9291747B2 (en) 2010-02-08 2016-03-22 Essilor International (Compagnie Generale D'optique) Optical article comprising an anti-reflecting coating having anti-fogging properties
ES2365960B1 (en) * 2010-03-31 2012-06-04 Palobiofarma, S.L NEW ANTAGONISTS OF ADENOSINE RECEPTORS.
CN116768859A (en) 2017-01-20 2023-09-19 艾库斯生物科学有限公司 Azolopyrimidines for the treatment of cancer related disorders
TWI801372B (en) 2017-03-30 2023-05-11 比利時商艾特歐斯比利時有限公司 Thiocarbamate derivatives as a2a inhibitors and methods for use in the treatment of cancers

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007140181A2 (en) * 2006-05-26 2007-12-06 King Pharmaceuticals Research And Development, Inc. Combination therapy comprising an adenosine uptake inhibitor and a non-selective adenosine receptor antagonist
WO2009011897A1 (en) * 2007-07-17 2009-01-22 Combinatorx, Incorporated Combinations for the treatment of b-cell proliferative disorders
WO2012055015A1 (en) * 2010-10-26 2012-05-03 Alberta Health Services Combination comprising an atp analog and an adenosine receptor antagonist or a nucleobase/nucleoside analog for the treatment of cancer

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
BARBARA CACCIARI ET AL,, A2A ADENOSINE RECEPTOR ANTAGONISTS AS THERAPEUTIC CANDIDATES: ARE THEY STILL AN INTERESTING CHALLENGE?, 9 July 2018 (2018-07-09) *
NAKAGAWA H ET AL,, BASIS FOR DOSING TIME-DEPENDENT CHANGE IN THE ANTI-TUMOR EFFECT OF IMATINIB IN MICE, 31 December 2006 (2006-12-31) *
STEPHEN B. WILLINGHAM ET AL,, A2AR ANTAGONISM WITH CPI-444 INDUCES ANTITUMOR RESPONSES AND AUGMENTS EFFICACY TO ANTI-PD-(L)1 AND ANTI-CTLA-4 IN PRECLINICAL MODELS, 21 August 2018 (2018-08-21) *

Also Published As

Publication number Publication date
JP2022503879A (en) 2022-01-12
WO2020065036A1 (en) 2020-04-02
BR112021006033A2 (en) 2021-09-08
JP7641894B2 (en) 2025-03-07
IL281802A (en) 2021-05-31
IL281802B1 (en) 2025-06-01

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