CA2999523A1 - Combination therapy of bromodomain inhibitors and checkpoint blockade - Google Patents

Combination therapy of bromodomain inhibitors and checkpoint blockade Download PDF

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Publication number
CA2999523A1
CA2999523A1 CA2999523A CA2999523A CA2999523A1 CA 2999523 A1 CA2999523 A1 CA 2999523A1 CA 2999523 A CA2999523 A CA 2999523A CA 2999523 A CA2999523 A CA 2999523A CA 2999523 A1 CA2999523 A1 CA 2999523A1
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CA
Canada
Prior art keywords
substituted
unsubstituted
alkyl
protecting group
carbocyclyl
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.)
Abandoned
Application number
CA2999523A
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English (en)
French (fr)
Inventor
James E. Bradner
Simon John Hogg
Ricky Wayne Johnston
Jake Shortt
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.)
Peter MacCallum Cancer Institute
Dana Farber Cancer Institute Inc
Original Assignee
Peter MacCallum Cancer Institute
Dana Farber Cancer Institute 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 Peter MacCallum Cancer Institute, Dana Farber Cancer Institute Inc filed Critical Peter MacCallum Cancer Institute
Publication of CA2999523A1 publication Critical patent/CA2999523A1/en
Abandoned legal-status Critical Current

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    • 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
    • A61K31/495Heterocyclic 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
    • 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
    • A61K31/55Heterocyclic 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
    • A61K31/551Heterocyclic 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
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/55171,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2827Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against B7 molecules, e.g. CD80, CD86
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2878Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the NGF-receptor/TNF-receptor superfamily, e.g. CD27, CD30, CD40, CD95
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K2039/505Medicinal preparations containing antigens or antibodies comprising antibodies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/20Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/24Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Endocrinology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CA2999523A 2015-10-02 2016-09-30 Combination therapy of bromodomain inhibitors and checkpoint blockade Abandoned CA2999523A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562236280P 2015-10-02 2015-10-02
US62/236,280 2015-10-02
PCT/US2016/054924 WO2017059319A2 (en) 2015-10-02 2016-09-30 Combination therapy of bromodomain inhibitors and checkpoint blockade

Publications (1)

Publication Number Publication Date
CA2999523A1 true CA2999523A1 (en) 2017-04-06

Family

ID=57137298

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2999523A Abandoned CA2999523A1 (en) 2015-10-02 2016-09-30 Combination therapy of bromodomain inhibitors and checkpoint blockade

Country Status (16)

Country Link
US (1) US20190192532A1 (enExample)
EP (1) EP3355922A2 (enExample)
JP (1) JP2018530554A (enExample)
KR (1) KR20180081507A (enExample)
CN (1) CN108289957A (enExample)
AR (1) AR107500A1 (enExample)
AU (1) AU2016331190A1 (enExample)
BR (1) BR112018006689A2 (enExample)
CA (1) CA2999523A1 (enExample)
CL (1) CL2018000853A1 (enExample)
HK (1) HK1256269A1 (enExample)
IL (1) IL258212A (enExample)
MA (1) MA43037A (enExample)
MX (1) MX2018003824A (enExample)
PE (1) PE20181068A1 (enExample)
WO (1) WO2017059319A2 (enExample)

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BR112012029005A2 (pt) 2010-05-14 2016-07-26 Dana Farber Cancer Inst Inc composições e métodos de tratamento de neoplasia, doença inflamatória e outros distúrbios
CA2799403C (en) 2010-05-14 2020-01-21 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
EP3868387A1 (en) 2012-07-20 2021-08-25 Taiga Biotechnologies, Inc. Enhanced reconstitution and autoreconstitution of the hematopoietic compartment
CN105849110B (zh) 2013-11-08 2019-08-02 达纳-法伯癌症研究所有限公司 使用溴结构域和额外终端(bet)蛋白抑制剂的用于癌症的组合疗法
MX377534B (es) 2014-02-28 2025-03-10 Tensha Therapeutics Inc Compuestos para usarse en el tratamiento de hiperinsulinemia.
WO2016069578A1 (en) 2014-10-27 2016-05-06 Tensha Therapeutics, Inc. Bromodomain inhibitors
MY195089A (en) 2016-05-27 2023-01-10 Agenus Inc Anti-Tim-3 Antibodies and Methods of use thereof
WO2018102678A1 (en) 2016-12-02 2018-06-07 Taiga Biotechnologies, Inc. Nanoparticle formulations
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
WO2019140953A1 (zh) * 2018-01-16 2019-07-25 深圳市塔吉瑞生物医药有限公司 用于抑制激酶活性的二苯氨基嘧啶类化合物
US12454520B2 (en) 2018-07-06 2025-10-28 Kymera Therapeutics, Inc. Protein degraders and uses thereof
US12187686B2 (en) * 2018-09-07 2025-01-07 H. Lee Moffitt Cancer Center And Research Institute, Inc. BRD4-JAK2 inhibitors
TWI816881B (zh) * 2018-09-13 2023-10-01 大陸商恒翼生物醫藥(上海)股份有限公司 用於治療三陰性乳癌之組合療法
KR102891608B1 (ko) 2018-11-30 2025-11-28 카이메라 쎄라퓨틱스 인코포레이티드 Irak 분해제 및 이의 용도
CN109666723B (zh) * 2019-01-22 2022-04-15 南通大学 一种基于pdl1/pdl2超增强子的免疫检测点抑制剂的应用
CN113874033A (zh) 2019-04-08 2021-12-31 泰加生物工艺学公司 用于冷冻保存免疫细胞的组合物和方法
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WO2021090061A1 (en) * 2019-11-05 2021-05-14 Resverlogix Corp. Methods of treatment and/or prevention of major adverse cardiovascular events (mace) with a combination of a bet bromodomain inhibitor and a sodium dependent glucose transport 2 inhibitor
KR102420262B1 (ko) * 2019-11-26 2022-07-13 주식회사 베노바이오 신규한 퀘르세틴 리독스 유도체 및 bet 억제제로서의 용도
EP4076520A4 (en) 2019-12-17 2024-03-27 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2021175432A1 (en) 2020-03-04 2021-09-10 Boehringer Ingelheim International Gmbh Method for administration of an anti cancer agent
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
WO2021257857A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Naphthyridinone compounds as jak2 v617f inhibitors
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Also Published As

Publication number Publication date
MA43037A (fr) 2018-08-08
CN108289957A (zh) 2018-07-17
IL258212A (en) 2018-05-31
EP3355922A2 (en) 2018-08-08
US20190192532A1 (en) 2019-06-27
HK1256269A1 (zh) 2019-09-20
WO2017059319A3 (en) 2017-10-12
WO2017059319A2 (en) 2017-04-06
BR112018006689A2 (pt) 2018-10-09
AR107500A1 (es) 2018-05-09
PE20181068A1 (es) 2018-07-04
JP2018530554A (ja) 2018-10-18
AU2016331190A1 (en) 2018-04-12
CL2018000853A1 (es) 2018-08-31
KR20180081507A (ko) 2018-07-16
MX2018003824A (es) 2019-04-01

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Legal Events

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FZDE Discontinued

Effective date: 20221222

FZDE Discontinued

Effective date: 20221222