JP6779204B2 - A2a拮抗薬特性を有するアミノピラジン化合物 - Google Patents

A2a拮抗薬特性を有するアミノピラジン化合物 Download PDF

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Publication number
JP6779204B2
JP6779204B2 JP2017526527A JP2017526527A JP6779204B2 JP 6779204 B2 JP6779204 B2 JP 6779204B2 JP 2017526527 A JP2017526527 A JP 2017526527A JP 2017526527 A JP2017526527 A JP 2017526527A JP 6779204 B2 JP6779204 B2 JP 6779204B2
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methyl
pyrazine
amino
carboxamide
oxazole
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JP2017533946A (ja
JP2017533946A5 (enExample
Inventor
クアン,ロンジー
ティン,ポーリーン
アリ,アムジャド
ウー,ホーピン
バーリン,マイケル
スタンフォード,アンドリュー
ウォン,ホンウー
シュー,ギャン
キム,デヴィッド
デン,シャオリン
リム,ヨン−ヒ
ユ,ヨウノン
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Merck Sharp and Dohme LLC
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2017526527A 2014-11-18 2015-11-13 A2a拮抗薬特性を有するアミノピラジン化合物 Expired - Fee Related JP6779204B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462081262P 2014-11-18 2014-11-18
US62/081,262 2014-11-18
PCT/US2015/060509 WO2016081290A1 (en) 2014-11-18 2015-11-13 Aminopyrazine compounds with a2a antagonist properties

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JP2017533946A JP2017533946A (ja) 2017-11-16
JP2017533946A5 JP2017533946A5 (enExample) 2018-12-20
JP6779204B2 true JP6779204B2 (ja) 2020-11-04

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US (1) US10472347B2 (enExample)
EP (1) EP3220910B1 (enExample)
JP (2) JP6779204B2 (enExample)
KR (1) KR20170083136A (enExample)
CN (1) CN107106558A (enExample)
AU (1) AU2015350315B2 (enExample)
BR (1) BR112017010261A2 (enExample)
CA (1) CA2967944C (enExample)
MX (1) MX381180B (enExample)
RU (1) RU2727805C2 (enExample)
WO (1) WO2016081290A1 (enExample)

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EP3594216B1 (en) * 2017-03-07 2022-04-06 Guangzhou Maxinovel Pharmaceuticals Co., Ltd. Aminopyrimidine five-membered heterocyclic compound, and intermediate, preparation method, pharmaceutical composition and application thereof
KR20200040764A (ko) 2017-07-18 2020-04-20 누베이션 바이오 인크. 1,8-나프티리디논 화합물 및 그의 용도
WO2019018584A1 (en) 2017-07-18 2019-01-24 GiraFpharma LLC HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS
CN111629728A (zh) 2017-08-31 2020-09-04 科尔沃斯制药股份有限公司 用于调节腺苷a2b受体和腺苷a2a受体的化合物和方法
JP2020536881A (ja) 2017-10-12 2020-12-17 レヴォリューション・メディスンズ,インコーポレイテッド アロステリックshp2阻害剤としてのピリジン、ピラジンおよびトリアジン化合物
EP3723754A4 (en) 2017-12-13 2021-05-19 Merck Sharp & Dohme Corp. IMIDAZO [1,2-C] QUINAZOLINE-5-AMINE COMPOUNDS WITH PROPERTIES OF A2A ANTAGONIST
CA3084058A1 (en) 2017-12-15 2019-06-20 Revolution Medicines, Inc. Polycyclic compounds as allosteric shp2 inhibitors
WO2020037094A1 (en) 2018-08-16 2020-02-20 Innate Tumor Immunity, Inc. Substitued 4-amino-1h-imidazo[4,5-c]quinoline compounds and improved methods for their preparation
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CA3119774A1 (en) 2018-11-20 2020-05-28 Merck Sharp & Dohme Corp. Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use
US12414952B2 (en) 2018-11-20 2025-09-16 Merck Sharp & Dohme Llc Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use
AU2019388872A1 (en) 2018-11-30 2021-05-27 Merck Sharp & Dohme Llc 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use
JOP20210117A1 (ar) 2018-11-30 2023-01-30 Merck Sharp & Dohme مشتقات أمينو ترايازولو كوينازولين بها استبدال في الموضع-9 كمضادات مستقبل أدينوزين، تركيبات صيدلانية واستخدامها
BR112021012685A2 (pt) 2019-01-11 2021-12-28 Omeros Corp Métodos para tratar câncer, para aumentar o nível de citocinas th1 nas células mononucleares de sangue periférico humanas, para realçar uma resposta imune antitumoral e para estimular e/ou amplificar uma resposta imune em um sujeito mamífero sofrendo de ou em risco de desenvolver câncer ou metástase de câncer, e, composição farmacêutica
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TW202128650A (zh) * 2019-10-11 2021-08-01 德商拜耳動物保健有限公司 作為殺蟲劑之新穎的雜芳基取代之吡𠯤衍生物
CN111285798A (zh) * 2020-04-09 2020-06-16 阿里生物新材料(常州)有限公司 一种(3-环丙基吡啶-2-基)甲胺盐酸盐的合成方法
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EP3220910A1 (en) 2017-09-27
MX2017006483A (es) 2017-09-12
US10472347B2 (en) 2019-11-12
JP2017533946A (ja) 2017-11-16
JP2020193211A (ja) 2020-12-03
RU2727805C2 (ru) 2020-07-24
KR20170083136A (ko) 2017-07-17
MX381180B (es) 2025-03-12
CN107106558A (zh) 2017-08-29
CA2967944C (en) 2020-11-17
WO2016081290A1 (en) 2016-05-26
AU2015350315A1 (en) 2017-05-18
RU2017120853A3 (enExample) 2019-06-17
AU2015350315B2 (en) 2020-06-25
EP3220910A4 (en) 2018-04-25
US20180327385A1 (en) 2018-11-15
BR112017010261A2 (pt) 2018-02-06
EP3220910B1 (en) 2020-01-15
RU2017120853A (ru) 2018-12-19
CA2967944A1 (en) 2016-05-26

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