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BR112021009078A8 - Antagonistas substituídos de receptor de adenosina de aminotriazolopirimidina e aminotriazolopirazina, composições farmacêuticas e seus usos - Google Patents

Antagonistas substituídos de receptor de adenosina de aminotriazolopirimidina e aminotriazolopirazina, composições farmacêuticas e seus usos

Info

Publication number
BR112021009078A8
BR112021009078A8 BR112021009078A BR112021009078A BR112021009078A8 BR 112021009078 A8 BR112021009078 A8 BR 112021009078A8 BR 112021009078 A BR112021009078 A BR 112021009078A BR 112021009078 A BR112021009078 A BR 112021009078A BR 112021009078 A8 BR112021009078 A8 BR 112021009078A8
Authority
BR
Brazil
Prior art keywords
adenosine receptor
aminotriazolopyrazine
aminotriazolopyrimidine
pharmaceutical compositions
receptor antagonists
Prior art date
Application number
BR112021009078A
Other languages
English (en)
Other versions
BR112021009078A2 (pt
Inventor
G Brill Zachary
Ali Amjad
Cumming Jared
Demong Duane
Deng Qiaolin
H Graham Thomas
Kuang Rongze
Lim Yeon-Hee
W Plummer Christopher
Lorena Rico Duque Jenny
Wang Huijun
Zhang Yonglian
Zhao Kake
Original Assignee
Merck Sharp & Dohme
Merck Sharp & Dohme Llc
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 Merck Sharp & Dohme, Merck Sharp & Dohme Llc filed Critical Merck Sharp & Dohme
Publication of BR112021009078A2 publication Critical patent/BR112021009078A2/pt
Publication of BR112021009078A8 publication Critical patent/BR112021009078A8/pt

Links

Classifications

    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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 [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [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
    • C07K16/2818—Immunoglobulins [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 CD28 or CD152
    • 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
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

ANTAGONISTAS SUBSTITUÍDOS DE RECEPTOR DE ADENOSINA DE AMINOTRIAZOLOPIRIMIDINA E AMINOTRIAZOLOPIRAZINA, COMPOSIÇÕES FARMACÊUTICAS E SEUS USOS. Em suas muitas modalidades, a presente invenção fornece certos compostos substituídos de aminotriazolopirimidina e aminotriazolopirazina de Fórmula (IA) e Fórmula (IB) ou e sais farmaceuticamente aceitáveis dos mesmos, em que, R1, R2, e R3 são como definidos na presente invenção, composições farmacêuticas compreendendo um ou mais de tais compostos (sozinhos e em combinação com um ou mais outros agentes terapeuticamente ativos), e métodos para a sua preparação e uso, sozinhos e em combinação com outros agentes terapêuticos, como antagonistas de A2a e/ou receptores A2b, e seu uso no tratamento de uma variedade de doenças, condições ou distúrbios que são mediados, pelo menos em parte, pelo receptor de adenosina A2a e/ou receptor de adenosina A2b.
BR112021009078A 2018-11-20 2019-11-15 Antagonistas substituídos de receptor de adenosina de aminotriazolopirimidina e aminotriazolopirazina, composições farmacêuticas e seus usos BR112021009078A8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862769843P 2018-11-20 2018-11-20
US62/769,843 2018-11-20
PCT/US2019/061622 WO2020106558A1 (en) 2018-11-20 2019-11-15 Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use

Publications (2)

Publication Number Publication Date
BR112021009078A2 BR112021009078A2 (pt) 2021-08-10
BR112021009078A8 true BR112021009078A8 (pt) 2023-02-07

Family

ID=70774154

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112021009078A BR112021009078A8 (pt) 2018-11-20 2019-11-15 Antagonistas substituídos de receptor de adenosina de aminotriazolopirimidina e aminotriazolopirazina, composições farmacêuticas e seus usos

Country Status (11)

Country Link
US (1) US20210395255A1 (pt)
EP (1) EP3883575A4 (pt)
JP (1) JP2022507734A (pt)
KR (1) KR20210093964A (pt)
CN (1) CN113015530A (pt)
AU (1) AU2019383948A1 (pt)
BR (1) BR112021009078A8 (pt)
CA (1) CA3119774A1 (pt)
MA (1) MA55142A (pt)
MX (1) MX2021005839A (pt)
WO (1) WO2020106558A1 (pt)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2019385905B2 (en) 2018-11-30 2023-01-12 Merck Sharp & Dohme Llc 9-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use
CA3150766A1 (en) * 2019-08-26 2021-03-04 Incyte Corporation Triazolopyrimidines as a2a / a2b inhibitors
AU2023252914A1 (en) 2022-04-13 2024-10-17 Arcus Biosciences, Inc. Combination therapy for treating trop-2 expressing cancers

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EP0976753B1 (en) * 1997-03-24 2004-01-02 Kyowa Hakko Kogyo Co., Ltd. [1,2,4]TRIAZOLO[1,5-c]PYRIMIDINE DERIVATIVES
JPWO2003028732A1 (ja) * 2001-09-28 2005-01-13 協和醗酵工業株式会社 受容体拮抗剤
AR038366A1 (es) * 2001-11-30 2005-01-12 Schering Corp Compuestos de 1,2,4-triazolo [1,5-c] pirimidinas sustituidas, antagonistas del receptor de adenosina a2a, composiciones farmaceuticas, el uso de dichos compuestos para la manufactura de un medicamento para el tratamiento de enfermedades del sistema nervioso central y un kit que comprende combinacion
AU2003211993A1 (en) * 2002-02-15 2003-09-04 Kyowa Hakko Kogyo Co., Ltd. (1,2,4)TRIAZOLO(1,5-c)PYRIMIDINE DERIVATIVES
DE60334303D1 (de) 2002-07-03 2010-11-04 Tasuku Honjo Immunpotenzierende zusammensetzungen
WO2004029056A1 (ja) * 2002-09-24 2004-04-08 Kyowa Hakko Kogyo Co., Ltd. [１，２，４]トリアゾロ[１，５−ｃ]ピリミジン誘導体
AU2003288675B2 (en) 2002-12-23 2010-07-22 Medimmune Limited Antibodies against PD-1 and uses therefor
ES2729974T3 (es) 2003-01-23 2019-11-07 Ono Pharmaceutical Co Anticuerpo específico de PD-1 y CD3 humanas
EP1615931A1 (en) * 2003-04-09 2006-01-18 Biogen Idec MA Inc. Triazolopyrazines and methods of making and using the same
WO2006121168A1 (en) 2005-05-09 2006-11-16 Ono Pharmaceutical Co., Ltd. Human monoclonal antibodies to programmed death 1(pd-1) and methods for treating cancer using anti-pd-1 antibodies alone or in combination with other immunotherapeutics
PT1907424E (pt) 2005-07-01 2015-10-09 Squibb & Sons Llc Anticorpos monoclonais humanos para o ligando 1 de morte programada (pd-l1)
NZ582150A (en) 2007-06-18 2012-08-31 Msd Oss Bv Antibodies to human programmed death receptor pd-1
WO2009114335A2 (en) 2008-03-12 2009-09-17 Merck & Co., Inc. Pd-1 binding proteins
DE102008023801A1 (de) * 2008-05-15 2009-11-19 Bayer Schering Pharma Aktiengesellschaft Substituierte Imidazo- und Triazolopyrimidine, Imidazo- und Pyrazolopyrazine und Imidazotriazine
GB0906579D0 (en) * 2009-04-16 2009-05-20 Vernalis R&D Ltd Pharmaceuticals, compositions and methods of making and using the same
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
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HUE034832T2 (hu) 2008-12-09 2021-12-28 Hoffmann La Roche Anti-PD-L1 antitestek és alkalmazásuk T-sejt-funkció fokozására
WO2011066342A2 (en) 2009-11-24 2011-06-03 Amplimmune, Inc. Simultaneous inhibition of pd-l1/pd-l2
MX368257B (es) 2011-08-01 2019-09-26 Genentech Inc Antagonistas de unión al eje pd-1e inhibidores de mek y sus usos en el tratamiento de cáncer.
AR108875A1 (es) * 2016-06-24 2018-10-03 Incyte Corp COMPUESTOS HETEROCÍCLICOS COMO INHIBIDORES DE PI3K-g
ES2919474T3 (es) 2017-04-07 2022-07-26 Medshine Discovery Inc Derivado de [1,2,4]triazolo[1,5-c]pirimidina como inhibidor del receptor A2A
CN109535161B (zh) * 2017-09-22 2021-09-03 江苏恒瑞医药股份有限公司 三唑并嘧啶类衍生物、其制备方法及其在医药上的应用
CR20230030A (es) 2018-02-27 2023-03-10 Incyte Corp Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b (divisional 2020-0441)

Also Published As

Publication number Publication date
KR20210093964A (ko) 2021-07-28
AU2019383948A1 (en) 2021-05-20
WO2020106558A1 (en) 2020-05-28
US20210395255A1 (en) 2021-12-23
CN113015530A (zh) 2021-06-22
EP3883575A4 (en) 2022-06-15
MX2021005839A (es) 2021-07-15
MA55142A (fr) 2022-02-23
JP2022507734A (ja) 2022-01-18
CA3119774A1 (en) 2020-05-28
EP3883575A1 (en) 2021-09-29
BR112021009078A2 (pt) 2021-08-10

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Legal Events

Date Code Title Description
B25A Requested transfer of rights approved

Owner name: MERCK SHARP AND DOHME LLC (US)

B11A Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing
B11Y Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette]