KR20200018503A - 5-브로모-2,6-디(1h-피라졸-1-일)피리미딘-4-아민 및 새로운 염의 결정질 형태 - Google Patents

5-브로모-2,6-디(1h-피라졸-1-일)피리미딘-4-아민 및 새로운 염의 결정질 형태 Download PDF

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KR20200018503A
KR20200018503A KR1020197038580A KR20197038580A KR20200018503A KR 20200018503 A KR20200018503 A KR 20200018503A KR 1020197038580 A KR1020197038580 A KR 1020197038580A KR 20197038580 A KR20197038580 A KR 20197038580A KR 20200018503 A KR20200018503 A KR 20200018503A
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amino acid
seq
acid sequence
ser
thr
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카이 추이
웨이융 쿵
훌리오 세자르 카스트로-팔로미노 라리아
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노파르티스 아게
팔로바이오파마, 에스.엘.
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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
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • 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
    • 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
    • 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
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • 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
    • A61K2039/545—Medicinal preparations containing antigens or antibodies characterised by the dose, timing or administration schedule
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • 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)
  • Immunology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Mycology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Microbiology (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
KR1020197038580A 2017-05-31 2018-05-30 5-브로모-2,6-디(1h-피라졸-1-일)피리미딘-4-아민 및 새로운 염의 결정질 형태 Ceased KR20200018503A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2017/086624 2017-05-31
CN2017086624 2017-05-31
PCT/IB2018/053839 WO2018220546A1 (en) 2017-05-31 2018-05-30 Crystalline forms of 5-bromo-2,6-di(1 h-pyrazol-1-yl)pyrimidin-4-amine and new salts

Publications (1)

Publication Number Publication Date
KR20200018503A true KR20200018503A (ko) 2020-02-19

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KR1020197038580A Ceased KR20200018503A (ko) 2017-05-31 2018-05-30 5-브로모-2,6-디(1h-피라졸-1-일)피리미딘-4-아민 및 새로운 염의 결정질 형태

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Country Link
US (2) US10933064B2 (https=)
EP (1) EP3630751B1 (https=)
JP (1) JP7273732B2 (https=)
KR (1) KR20200018503A (https=)
CN (1) CN110944995B (https=)
AR (1) AR111906A1 (https=)
AU (1) AU2018277241B2 (https=)
BR (1) BR112019025149A2 (https=)
CA (1) CA3065475A1 (https=)
CL (2) CL2019003468A1 (https=)
IL (2) IL270795B2 (https=)
JO (1) JOP20190279B1 (https=)
MX (1) MX2021014104A (https=)
PH (1) PH12019502703A1 (https=)
RU (2) RU2019138329A (https=)
TW (1) TWI814725B (https=)
WO (1) WO2018220546A1 (https=)
ZA (1) ZA201907610B (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
MY204234A (en) 2018-08-27 2024-08-16 Regeneron Pharma Use of raman spectroscopy in downstream purification

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL129299A0 (en) 1999-03-31 2000-02-17 Mor Research Applic Ltd Monoclonal antibodies antigens and diagnosis of malignant diseases
JP4064671B2 (ja) * 2000-02-25 2008-03-19 エフ．ホフマン−ラ ロシュ アーゲー アデノシン受容体モジュレーター
IL149820A0 (en) 2002-05-23 2002-11-10 Curetech Ltd Humanized immunomodulatory monoclonal antibodies for the treatment of neoplastic disease or immunodeficiency
ES2350687T3 (es) 2002-07-03 2011-01-26 Ono Pharmaceutical Co., Ltd. Composiciones de inmunopotenciación.
CN1753912B (zh) 2002-12-23 2011-11-02 惠氏公司 抗pd-1抗体及其用途
JP2007514003A (ja) 2003-12-15 2007-05-31 アルミラル プロデスファルマ アーゲー アデノシン受容体アンタゴニストとしての２，６−ビスヘテロアリール−４−アミノピリミジン
RU2494107C2 (ru) 2005-05-09 2013-09-27 Оно Фармасьютикал Ко., Лтд. Моноклональные антитела человека к белку программируемой смерти 1 (pd-1) и способы лечения рака с использованием анти-pd-1-антител самостоятельно или в комбинации с другими иммунотерапевтическими средствами
CN104356236B (zh) 2005-07-01 2020-07-03 E.R.施贵宝&圣斯有限责任公司 抗程序性死亡配体1(pd-l1)的人单克隆抗体
CA2644996A1 (en) * 2006-03-02 2007-09-13 Cv Therapeutics, Inc. A2a adenosine receptor antagonists
WO2008110891A2 (en) 2007-03-09 2008-09-18 Orchid Research Laboratories Limited, New heterocyclic compounds
US8153064B2 (en) 2007-03-22 2012-04-10 Doebler Ii Robert W Systems and devices for isothermal biochemical reactions and/or analysis
HRP20131167T1 (hr) 2007-06-18 2014-01-03 Merck Sharp & Dohme B.V. Antitijela za humani receptor programirane smrti pd-1
WO2009114335A2 (en) 2008-03-12 2009-09-17 Merck & Co., Inc. Pd-1 binding proteins
WO2010098788A2 (en) 2008-08-25 2010-09-02 Amplimmune, Inc. Pd-i antagonists and methods for treating infectious disease
US8927697B2 (en) 2008-09-12 2015-01-06 Isis Innovation Limited PD-1 specific antibodies and uses thereof
KR101814408B1 (ko) 2008-09-26 2018-01-04 다나-파버 캔서 인스티튜트 인크. 인간 항-ｐｄ-１, ｐｄ-ｌ１, 및 ｐｄ-ｌ2 항체 및 그의 용도
AU2009333580B2 (en) 2008-12-09 2016-07-07 Genentech, Inc. Anti-PD-L1 antibodies and their use to enhance T-cell function
WO2010089411A2 (en) 2009-02-09 2010-08-12 Universite De La Mediterranee Pd-1 antibodies and pd-l1 antibodies and uses thereof
WO2011066342A2 (en) 2009-11-24 2011-06-03 Amplimmune, Inc. Simultaneous inhibition of pd-l1/pd-l2
CN102892786B (zh) 2010-03-11 2016-03-16 Ucb医药有限公司 Pd-1抗体
ES2365960B1 (es) 2010-03-31 2012-06-04 Palobiofarma, S.L Nuevos antagonistas de los receptores de adenosina.
US8907053B2 (en) 2010-06-25 2014-12-09 Aurigene Discovery Technologies Limited Immunosuppression modulating compounds
KR101970025B1 (ko) 2011-04-20 2019-04-17 메디뮨 엘엘씨 Ｂ7-ｈ1 및 ｐｄ-1과 결합하는 항체 및 다른 분자들
JP6240600B2 (ja) 2011-07-24 2017-11-29 キュアテク リミテッド ヒト化免疫モノクローナル抗体の変異体
HRP20201595T1 (hr) 2011-11-28 2020-12-11 Merck Patent Gmbh Anti-pd-l1 protutijela i njihova uporaba
JP6742903B2 (ja) 2013-05-02 2020-08-19 アナプティスバイオ インコーポレイティッド プログラム死−１（ｐｄ−１）に対する抗体
US9676853B2 (en) 2013-05-31 2017-06-13 Sorrento Therapeutics, Inc. Antigen binding proteins that bind PD-1
WO2014209804A1 (en) 2013-06-24 2014-12-31 Biomed Valley Discoveries, Inc. Bispecific antibodies
EA034666B1 (ru) 2013-09-13 2020-03-04 Бейджин Свитзерланд Гмбх Антитело против pd-1 и его применение для лечения рака или вирусной инфекции и фрагмент антитела
MY184154A (en) 2013-12-12 2021-03-23 Shanghai hengrui pharmaceutical co ltd Pd-1 antibody, antigen-binding fragment thereof, and medical application thereof
TWI681969B (zh) 2014-01-23 2020-01-11 美商再生元醫藥公司 針對ｐｄ-１的人類抗體
SG10201900002QA (en) 2014-01-24 2019-02-27 Dana Farber Cancer Institue Inc Antibody molecules to pd-1 and uses thereof
TWI693232B (zh) 2014-06-26 2020-05-11 美商宏觀基因股份有限公司 與pd-1和lag-3具有免疫反應性的共價結合的雙抗體和其使用方法
TWI716362B (zh) 2014-10-14 2021-01-21 瑞士商諾華公司 針對ｐｄ－ｌ１之抗體分子及其用途
TWI595006B (zh) 2014-12-09 2017-08-11 禮納特神經系統科學公司 抗ｐｄ－１抗體類和使用彼等之方法
SI3334431T1 (sl) * 2015-08-11 2020-01-31 Novartis Ag 5-bromo-2,6-di-(1h-pirazol-l-il)pyrimidin-4-amin za uporabo v zdravljenju raka
DK3579874T3 (da) * 2017-02-10 2021-10-11 Novartis Ag 1-(4-amino-5-brom-6-(1h-pyrazol-1-yl)pyrimidin-2-yl)-1h-pyrazol-4-ol og anvendelse deraf til behandling af cancer
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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Publication number Publication date
IL291721A (en) 2022-05-01
TWI814725B (zh) 2023-09-11
CA3065475A1 (en) 2018-12-06
AU2018277241B2 (en) 2021-03-04
IL270795B2 (en) 2023-12-01
JP7273732B2 (ja) 2023-05-15
ZA201907610B (en) 2021-10-27
CL2019003468A1 (es) 2020-08-14
US20200163963A1 (en) 2020-05-28
AU2018277241A1 (en) 2019-12-12
WO2018220546A1 (en) 2018-12-06
RU2019138329A3 (https=) 2022-02-17
CN110944995B (zh) 2024-03-12
EP3630751B1 (en) 2024-03-27
RU2022102355A (ru) 2022-03-30
EP3630751A1 (en) 2020-04-08
CL2021002667A1 (es) 2022-07-01
IL291721B2 (en) 2024-07-01
JP2020521774A (ja) 2020-07-27
RU2019138329A (ru) 2021-07-01
JOP20190279A1 (ar) 2019-11-28
IL270795A (en) 2020-01-30
US11654144B2 (en) 2023-05-23
PH12019502703A1 (en) 2020-10-26
CN110944995A (zh) 2020-03-31
IL291721B1 (en) 2024-03-01
BR112019025149A2 (pt) 2020-06-23
JOP20190279B1 (ar) 2024-04-18
AR111906A1 (es) 2019-08-28
IL270795B1 (en) 2023-08-01
MX2021014104A (es) 2021-12-10
US20210145831A1 (en) 2021-05-20
TW201920152A (zh) 2019-06-01
US10933064B2 (en) 2021-03-02

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