CA3051986A1 - 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 - Google Patents

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 Download PDF

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Publication number
CA3051986A1
CA3051986A1 CA3051986A CA3051986A CA3051986A1 CA 3051986 A1 CA3051986 A1 CA 3051986A1 CA 3051986 A CA3051986 A CA 3051986A CA 3051986 A CA3051986 A CA 3051986A CA 3051986 A1 CA3051986 A1 CA 3051986A1
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CA
Canada
Prior art keywords
seq
amino acid
acid sequence
pyrazol
cancer
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
CA3051986A
Other languages
English (en)
French (fr)
Inventor
Sanela Bilic
Juan Alberto Camacho Gomez
John Scott CAMERON
Julio Cesar Castro-Palomino Laria
Danny Roland Howard Jr.
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.)
Novartis AG
Palobiofarma SL
Original Assignee
Novartis AG
Palobiofarma SL
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Filing date
Publication date
Application filed by Novartis AG, Palobiofarma SL filed Critical Novartis AG
Publication of CA3051986A1 publication Critical patent/CA3051986A1/en
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61K39/39558Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • C07K16/00Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803Immunoglobulins [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
    • C07K16/2818Immunoglobulins [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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803Immunoglobulins [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
    • C07K16/2827Immunoglobulins [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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/50Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/56Immunoglobulins specific features characterized by immunoglobulin fragments variable (Fv) region, i.e. VH and/or VL
    • C07K2317/565Complementarity determining region [CDR]

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
CA3051986A 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 Pending CA3051986A1 (en)

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 (1)

Publication Number Publication Date
CA3051986A1 true CA3051986A1 (en) 2018-08-16

Family

ID=61274309

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3051986A Pending CA3051986A1 (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

Country Status (15)

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

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2986067T3 (es) * 2015-12-17 2024-11-08 Novartis Ag Moléculas de anticuerpos frente a PD-1 y usos de las mismas
JP7273732B2 (ja) * 2017-05-31 2023-05-15 ノバルティス アーゲー 5-ブロモ-2,6-ジ(1h-ピラゾール-1-イル)ピリミジン-4-アミン及び新たな塩の結晶形

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IL129299A0 (en) 1999-03-31 2000-02-17 Mor Research Applic Ltd Monoclonal antibodies antigens and diagnosis of malignant diseases
IL149820A0 (en) 2002-05-23 2002-11-10 Curetech Ltd Humanized immunomodulatory monoclonal antibodies for the treatment of neoplastic disease or immunodeficiency
US7119200B2 (en) * 2002-09-04 2006-10-10 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
CN101899114A (zh) 2002-12-23 2010-12-01 惠氏公司 抗pd-1抗体及其用途
DK2439273T3 (da) 2005-05-09 2019-06-03 Ono Pharmaceutical Co Humane monoklonale antistoffer til programmeret død-1(pd-1) og fremgangsmåder til behandling af cancer ved anvendelse af anti-pd-1- antistoffer alene eller i kombination med andre immunterapeutika
PT1907424E (pt) 2005-07-01 2015-10-09 Squibb & Sons Llc Anticorpos monoclonais humanos para o ligando 1 de morte programada (pd-l1)
BR122017025062B8 (pt) 2007-06-18 2021-07-27 Merck Sharp & Dohme anticorpo monoclonal ou fragmento de anticorpo para o receptor de morte programada humano pd-1, polinucleotídeo e composição compreendendo o referido anticorpo ou fragmento
EP2262837A4 (en) 2008-03-12 2011-04-06 Merck Sharp & Dohme PD-1 BINDING PROTEINS
JP2012500855A (ja) 2008-08-25 2012-01-12 アンプリミューン、インコーポレーテッド Pd−1アンタゴニストおよび感染性疾患を処置するための方法
AU2009290544B2 (en) 2008-09-12 2015-07-16 Oxford University Innovation Limited PD-1 specific antibodies and uses thereof
US8552154B2 (en) 2008-09-26 2013-10-08 Emory University Anti-PD-L1 antibodies and uses therefor
EP3255060A1 (en) 2008-12-09 2017-12-13 F. Hoffmann-La Roche AG Anti-pd-l1 antibodies and their use to enhance t-cell function
JP5844159B2 (ja) 2009-02-09 2016-01-13 ユニヴェルシテ デクス−マルセイユUniversite D’Aix−Marseille Pd−1抗体およびpd−l1抗体ならびにその使用
WO2011066342A2 (en) 2009-11-24 2011-06-03 Amplimmune, Inc. Simultaneous inhibition of pd-l1/pd-l2
EP2545078A1 (en) 2010-03-11 2013-01-16 UCB Pharma, S.A. Pd-1 antibody
ES2365960B1 (es) 2010-03-31 2012-06-04 Palobiofarma, S.L Nuevos antagonistas de los receptores de adenosina.
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JP6072771B2 (ja) 2011-04-20 2017-02-01 メディミューン,エルエルシー B7−h1およびpd−1に結合する抗体およびその他の分子
CA2840018C (en) 2011-07-24 2019-07-16 Curetech Ltd. Variants of humanized immunomodulatory monoclonal antibodies
KR101764096B1 (ko) 2011-11-28 2017-08-02 메르크 파텐트 게엠베하 항-pd-l1 항체 및 그의 용도
SMT202100065T1 (it) 2013-05-02 2021-03-15 Anaptysbio Inc Anticorpi diretti contro la proteina della morte programmata (pd-1)
WO2014194302A2 (en) 2013-05-31 2014-12-04 Sorrento Therapeutics, Inc. Antigen binding proteins that bind pd-1
TN2015000444A1 (en) * 2013-06-03 2017-04-06 Novartis Ag Combinations of an anti-pd-l1 antibody and a mek inhibitor and/or a braf inhibitor
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CN112552401B (zh) 2013-09-13 2023-08-25 广州百济神州生物制药有限公司 抗pd1抗体及其作为治疗剂与诊断剂的用途
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Also Published As

Publication number Publication date
KR20190115053A (ko) 2019-10-10
JP2020507569A (ja) 2020-03-12
PT3579874T (pt) 2021-10-07
EP3579874B1 (en) 2021-07-21
DK3579874T3 (da) 2021-10-11
IL268549A (en) 2019-09-26
AU2020256467A1 (en) 2020-11-12
HUE057337T2 (hu) 2022-05-28
CN110290808A (zh) 2019-09-27
AU2018217963B2 (en) 2020-11-19
EP3579874A1 (en) 2019-12-18
AU2020256467B2 (en) 2022-03-03
WO2018146612A1 (en) 2018-08-16
PL3579874T3 (pl) 2022-02-28
US11078191B2 (en) 2021-08-03
JP7161481B2 (ja) 2022-10-26
US20190359600A1 (en) 2019-11-28
RU2019128199A (ru) 2021-03-10
AU2018217963A1 (en) 2019-08-08
IL268549B (en) 2021-10-31
SI3579874T1 (sl) 2021-11-30
CN110290808B (zh) 2023-07-11
RU2019128199A3 (enExample) 2021-05-14
ES2893006T3 (es) 2022-02-07

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