AU2016270907B2 - Inhibitors of Bruton's tyrosine kinase - Google Patents

Inhibitors of Bruton's tyrosine kinase Download PDF

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Publication number
AU2016270907B2
AU2016270907B2 AU2016270907A AU2016270907A AU2016270907B2 AU 2016270907 B2 AU2016270907 B2 AU 2016270907B2 AU 2016270907 A AU2016270907 A AU 2016270907A AU 2016270907 A AU2016270907 A AU 2016270907A AU 2016270907 B2 AU2016270907 B2 AU 2016270907B2
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substituted
unsubstituted
compound
formula
pharmaceutically acceptable
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AU2016270907A
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AU2016270907A1 (en
Inventor
Gordana Babic Atallah
Wei Chen
Zhaozhong J. Jia
Alfonso Pozzan
Luca Francesco Raveglia
Riccardo Zanaletti
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Pharmacyclics LLC
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Pharmacyclics LLC
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Publication of AU2016270907B2 publication Critical patent/AU2016270907B2/en
Priority to AU2020286332A priority Critical patent/AU2020286332A1/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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 C07D415/00
    • C07D417/14—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 C07D415/00 containing three or more hetero 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/08—Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2016270907A 2015-06-02 2016-06-02 Inhibitors of Bruton's tyrosine kinase Ceased AU2016270907B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2020286332A AU2020286332A1 (en) 2015-06-02 2020-12-11 Inhibitors of Bruton's tyrosine kinase

Applications Claiming Priority (13)

Application Number Priority Date Filing Date Title
US201562169935P 2015-06-02 2015-06-02
US201562169941P 2015-06-02 2015-06-02
US201562169945P 2015-06-02 2015-06-02
US62/169,935 2015-06-02
US62/169,945 2015-06-02
US62/169,941 2015-06-02
US201562249338P 2015-11-01 2015-11-01
US201562249336P 2015-11-01 2015-11-01
US201562249340P 2015-11-01 2015-11-01
US62/249,338 2015-11-01
US62/249,336 2015-11-01
US62/249,340 2015-11-01
PCT/US2016/035489 WO2016196776A2 (en) 2015-06-02 2016-06-02 Inhibitors of bruton's tyrosine kinase

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2020286332A Division AU2020286332A1 (en) 2015-06-02 2020-12-11 Inhibitors of Bruton's tyrosine kinase

Publications (2)

Publication Number Publication Date
AU2016270907A1 AU2016270907A1 (en) 2017-12-07
AU2016270907B2 true AU2016270907B2 (en) 2020-09-17

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
AU2016270907A Ceased AU2016270907B2 (en) 2015-06-02 2016-06-02 Inhibitors of Bruton's tyrosine kinase
AU2020286332A Abandoned AU2020286332A1 (en) 2015-06-02 2020-12-11 Inhibitors of Bruton's tyrosine kinase

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU2020286332A Abandoned AU2020286332A1 (en) 2015-06-02 2020-12-11 Inhibitors of Bruton's tyrosine kinase

Country Status (14)

Country Link
US (2) US20180305348A1 (enExample)
EP (1) EP3310776A4 (enExample)
JP (1) JP2018522823A (enExample)
KR (1) KR20180021740A (enExample)
CN (1) CN107709315A (enExample)
AU (2) AU2016270907B2 (enExample)
BR (1) BR112017025986A2 (enExample)
CA (1) CA2987054A1 (enExample)
IL (1) IL255831A (enExample)
MA (1) MA42623A (enExample)
MX (1) MX2017015574A (enExample)
RU (1) RU2017145650A (enExample)
SG (1) SG10201911523YA (enExample)
WO (1) WO2016196776A2 (enExample)

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MY203083A (en) * 2016-12-21 2024-06-07 Acerta Pharma Bv Imidazopyrazine inhibitors of bruton's tyrosine kinase
KR101956815B1 (ko) * 2017-02-14 2019-03-12 한국화학연구원 트리아졸로피리다진 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 브루톤티로신 키나제 활성 관련 질환의 예방 또는 치료용 약학적 조성물
CN109384774B (zh) * 2017-08-11 2023-02-17 中国科学院上海药物研究所 一类多取代的吡嗪/三嗪酰胺类化合物及其制备方法和应用
CN108530450B (zh) * 2018-05-03 2021-03-30 赖建智 具有egfr抑制活性的化合物、制备方法及其在疾病治疗中的应用
KR102797697B1 (ko) 2018-05-25 2025-04-22 에이2에이 파마수티칼스, 잉크. 신종 항암제 후보로서, 매우 강력한 tacc3 억제제
CN113412259B (zh) 2018-10-15 2024-07-16 紐力克斯治疗公司 通过泛素蛋白酶体途径降解btk的双官能化合物
HRP20250048T1 (hr) 2018-10-22 2025-03-28 Alumis Inc. Inhibitori tyk2 i njihova uporaba
WO2020167518A1 (en) * 2019-02-13 2020-08-20 Nurix Therapeutics, Inc. Bifunctional compounds for degrading btk via ubiquitin proteosome pathway
EP3942045A1 (en) 2019-03-21 2022-01-26 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
AU2020272937B2 (en) 2019-04-09 2024-09-26 Nurix Therapeutics, Inc. 3-substituted piperidine compounds for Cbl-b inhibition, and use of a Cbl-b inhibitor in combination with a cancer vaccine and/or oncolytic virus
JP7587528B2 (ja) 2019-05-17 2024-11-20 ニューリックス セラピューティクス，インコーポレイテッド Ｃｂｌ－ｂ阻害のためのシアノシクロブチル化合物及びその使用
CA3144450A1 (en) 2019-06-26 2020-12-30 Nurix Therapeutics, Inc. Substituted benzyl-triazole compounds for cbl-b inhibition, and further uses thereof
US12121540B2 (en) 2019-09-24 2024-10-22 Nurix Therapeutics, Inc. CBL inhibitors and compositions for use in adoptive cell therapy
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
MX2022006672A (es) 2019-12-04 2022-08-08 Nurix Therapeutics Inc Compuestos bifuncionales para la degradacion de btk a traves de la via de proteosomas de ubiquitina.
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
BR112022022220A2 (pt) * 2020-06-01 2022-12-13 Wigen Biomedicine Tech Shanghai Co Ltd Composto, composição farmacêutica, uso do composto, e método para tratar, regular e/ou prevenir uma doença relacionada a uma proteína mutante de egfr
WO2022071772A1 (ko) * 2020-09-29 2022-04-07 (주)메디톡스 단백질 키나제 저해제 및 그의 용도
MX2023011883A (es) 2021-04-08 2023-11-09 Nurix Therapeutics Inc Terapias combinadas con compuestos inhibidores de cbl-b.
WO2022221194A1 (en) * 2021-04-12 2022-10-20 A2A Pharmaceuticals, Inc. Compositions and methods for treating cancer
CA3223769A1 (en) * 2021-07-01 2023-01-05 Xinglu ZHOU Bruton's tyrosine kinase and mutant degrader, composition and application thereof
WO2023076303A1 (en) 2021-10-26 2023-05-04 Nurix Therapeutics, Inc. Piperidinylpyrazine-carboxamide compounds for treating and preventing cancer and for degrading btk
WO2023088477A1 (zh) * 2021-11-22 2023-05-25 杭州和正医药有限公司 一种可降解btk激酶的多功能化合物、组合物及应用
EP4499625A4 (en) 2022-03-24 2026-03-18 A2A Pharmaceuticals Inc CANCER COMPOSITIONS AND TREATMENT METHODS

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WO2013052394A1 (en) * 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
WO2013104573A1 (en) * 2012-01-10 2013-07-18 F. Hoffmann-La Roche Ag Pyridazine amide compounds and their use as syk inhibitors
WO2014153280A1 (en) * 2013-03-22 2014-09-25 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors

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WO2013052394A1 (en) * 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
WO2013104573A1 (en) * 2012-01-10 2013-07-18 F. Hoffmann-La Roche Ag Pyridazine amide compounds and their use as syk inhibitors
WO2014153280A1 (en) * 2013-03-22 2014-09-25 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors

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Also Published As

Publication number Publication date
KR20180021740A (ko) 2018-03-05
MA42623A (fr) 2018-06-20
WO2016196776A3 (en) 2017-01-05
CN107709315A (zh) 2018-02-16
RU2017145650A3 (enExample) 2019-11-22
EP3310776A4 (en) 2019-01-16
SG10201911523YA (en) 2020-02-27
WO2016196776A2 (en) 2016-12-08
US20210070748A1 (en) 2021-03-11
BR112017025986A2 (pt) 2018-08-14
MX2017015574A (es) 2018-08-09
JP2018522823A (ja) 2018-08-16
IL255831A (en) 2018-01-31
EP3310776A2 (en) 2018-04-25
RU2017145650A (ru) 2019-07-15
AU2016270907A1 (en) 2017-12-07
CA2987054A1 (en) 2016-12-08
AU2020286332A1 (en) 2021-01-21
US20180305348A1 (en) 2018-10-25

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