CN110290808B - 1-(4-氨基-5-溴-6-(1h-吡唑-1-基)嘧啶-2-基)-1h-吡唑-4-醇及其在治疗癌症中的用途 - Google Patents

1-(4-氨基-5-溴-6-(1h-吡唑-1-基)嘧啶-2-基)-1h-吡唑-4-醇及其在治疗癌症中的用途 Download PDF

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Publication number
CN110290808B
CN110290808B CN201880011779.3A CN201880011779A CN110290808B CN 110290808 B CN110290808 B CN 110290808B CN 201880011779 A CN201880011779 A CN 201880011779A CN 110290808 B CN110290808 B CN 110290808B
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amino acid
seq
acid sequence
pyrazol
cancer
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Expired - Fee Related
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Chinese (zh)
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CN110290808A (zh
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S·比里克
J·A·卡马乔戈麦斯
J·S·卡梅伦
J·C·卡斯特罗-帕罗米诺拉里亚
D·R·小霍华德
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Novartis AG
Palobiofarma SL
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Palobiofarma SL
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    • 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
    • C07D403/14—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 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
    • A61K31/505—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
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/39558—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IG], 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
    • C07K16/2818—Immunoglobulins [IG], 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 CD28 or CD152
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IG], 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
    • C07K16/2827—Immunoglobulins [IG], 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/56—Immunoglobulins specific features characterized by immunoglobulin fragments variable (Fv) region, i.e. VH and/or VL
    • C07K2317/565—Complementarity determining region [CDR]

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Mycology (AREA)
  • Microbiology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201880011779.3A 2017-02-10 2018-02-08 1-(4-氨基-5-溴-6-(1h-吡唑-1-基)嘧啶-2-基)-1h-吡唑-4-醇及其在治疗癌症中的用途 Expired - Fee Related CN110290808B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762457219P 2017-02-10 2017-02-10
US62/457,219 2017-02-10
PCT/IB2018/050783 WO2018146612A1 (en) 2017-02-10 2018-02-08 1-(4-amino-5-bromo-6-(1 h-pyrazol-1-yl)pyrimidin-2-yl)-1 h-pyrazol-4-ol and use thereof in the treatment of cancer

Publications (2)

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CN110290808A CN110290808A (zh) 2019-09-27
CN110290808B true CN110290808B (zh) 2023-07-11

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US (1) US11078191B2 (https=)
EP (1) EP3579874B1 (https=)
JP (1) JP7161481B2 (https=)
KR (1) KR20190115053A (https=)
CN (1) CN110290808B (https=)
AU (2) AU2018217963B2 (https=)
CA (1) CA3051986A1 (https=)
DK (1) DK3579874T3 (https=)
ES (1) ES2893006T3 (https=)
HU (1) HUE057337T2 (https=)
IL (1) IL268549B (https=)
PL (1) PL3579874T3 (https=)
PT (1) PT3579874T (https=)
SI (1) SI3579874T1 (https=)
WO (1) WO2018146612A1 (https=)

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* Cited by examiner, † Cited by third party
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WO2017106656A1 (en) * 2015-12-17 2017-06-22 Novartis Ag Antibody molecules to pd-1 and uses thereof
AU2018277241B2 (en) * 2017-05-31 2021-03-04 Novartis Ag Crystalline forms of 5-bromo-2,6-di(1H-pyrazol-1- yl)pyrimidin-4-amine and new salts

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NZ590480A (en) * 2004-02-11 2012-05-25 Schering Corp 7-Amino-pyrazolo[1,5-a]pyrimidine derivatives as cyclin dependent kinase inhibitors
CN105658206A (zh) * 2013-06-03 2016-06-08 诺华股份有限公司 抗pd-l1抗体与mek抑制剂和/或braf抑制剂的组合
CN105793260A (zh) * 2013-11-25 2016-07-20 癌症研究技术有限公司 作为用于治疗癌症的raf抑制剂的1-(5-叔丁基-2-芳基-吡唑-3-基)-3-[2-氟-4-[(3-氧代-4h-吡啶并[2，3-b]吡嗪-8-基)氧基]苯基]脲衍生物

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NZ590480A (en) * 2004-02-11 2012-05-25 Schering Corp 7-Amino-pyrazolo[1,5-a]pyrimidine derivatives as cyclin dependent kinase inhibitors
WO2011121418A1 (en) * 2010-03-31 2011-10-06 Palobiofarma, S.L. 4 - aminopyrimidine derivatives and their as as adenosine a2a receptor antagonists
CN105658206A (zh) * 2013-06-03 2016-06-08 诺华股份有限公司 抗pd-l1抗体与mek抑制剂和/或braf抑制剂的组合
CN105793260A (zh) * 2013-11-25 2016-07-20 癌症研究技术有限公司 作为用于治疗癌症的raf抑制剂的1-(5-叔丁基-2-芳基-吡唑-3-基)-3-[2-氟-4-[(3-氧代-4h-吡啶并[2，3-b]吡嗪-8-基)氧基]苯基]脲衍生物

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Publication number Publication date
JP2020507569A (ja) 2020-03-12
HUE057337T2 (hu) 2022-05-28
US20190359600A1 (en) 2019-11-28
RU2019128199A3 (https=) 2021-05-14
IL268549B (en) 2021-10-31
AU2020256467A1 (en) 2020-11-12
WO2018146612A1 (en) 2018-08-16
AU2018217963B2 (en) 2020-11-19
DK3579874T3 (da) 2021-10-11
CA3051986A1 (en) 2018-08-16
EP3579874B1 (en) 2021-07-21
PL3579874T3 (pl) 2022-02-28
EP3579874A1 (en) 2019-12-18
AU2020256467B2 (en) 2022-03-03
PT3579874T (pt) 2021-10-07
AU2018217963A1 (en) 2019-08-08
KR20190115053A (ko) 2019-10-10
JP7161481B2 (ja) 2022-10-26
IL268549A (en) 2019-09-26
CN110290808A (zh) 2019-09-27
ES2893006T3 (es) 2022-02-07
SI3579874T1 (sl) 2021-11-30
US11078191B2 (en) 2021-08-03
RU2019128199A (ru) 2021-03-10

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