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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Prior art keywords
methyl
pyrazine
amino
carboxamide
oxazole
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Expired - Fee Related
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Japanese (ja)
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JP2017533946A5 (enExample
JP2017533946A (ja
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 & Dohme LLC
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Merck Sharp & Dohme LLC
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic 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
    • C07D241/14—Heterocyclic 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-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

Related Child Applications (1)

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JP2020138418A Division JP2020193211A (ja) 2014-11-18 2020-08-19 A2a拮抗薬特性を有するアミノピラジン化合物

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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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JP2017526527A Expired - Fee Related JP6779204B2 (ja) 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
JP2020138418A Withdrawn JP2020193211A (ja) 2014-11-18 2020-08-19 A2a拮抗薬特性を有するアミノピラジン化合物

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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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CN110446709B (zh) 2017-01-23 2023-09-12 锐新医药公司 作为变构shp2抑制剂的二环化合物
CN108570054B (zh) * 2017-03-07 2021-07-16 广州再极医药科技有限公司 氨基嘧啶并五元杂环化合物、其中间体、制备方法、药物组合物及应用
CA3070073A1 (en) 2017-07-18 2019-01-24 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
JP2020527588A (ja) * 2017-07-18 2020-09-10 ニューベイション・バイオ・インコーポレイテッドNuvation Bio Inc. アデノシンアンタゴニストとしてのヘテロ環式化合物
JP2020532541A (ja) 2017-08-31 2020-11-12 コーバス・ファーマシューティカルズ・インコーポレイテッド アデノシンa2b受容体およびアデノシンa2a受容体を調節するための化合物および方法
BR112020007058A2 (pt) 2017-10-12 2020-10-06 Revolution Medicines, Inc. compostos de piridina, pirazina, e triazina como inibidores de shp2 alostéricos
US11498923B2 (en) 2017-12-13 2022-11-15 Merck Sharp & Dohme Llc Substituted imidazo[1,2-c]quinazolines as A2A antagonists
BR112020009757A2 (pt) 2017-12-15 2020-11-03 Revolution Medicines, Inc. compostos policíclicos como inibidores alostéricos de shp2
SG11202101486RA (en) 2018-08-16 2021-03-30 Innate Tumor Immunity Inc Substitued 4-amino-1h-imidazo[4,5-c]quinoline compounds and improved methods for their preparation
US20200079793A1 (en) * 2018-08-31 2020-03-12 Corvus Pharmaceuticals, Inc. Compounds and methods for modulating adenosine a2b receptor and adenosine a2a receptor
JP2022507734A (ja) 2018-11-20 2022-01-18 メルク・シャープ・アンド・ドーム・コーポレーション 置換アミノトリアゾロピリミジン及びアミノトリアゾロピラジンアデノシン受容体アンタゴニスト、医薬組成物及びそれらの使用
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
JP2022511778A (ja) 2018-11-30 2022-02-01 メルク・シャープ・アンド・ドーム・コーポレーション アデノシン受容体拮抗薬としての7-、8-及び10-置換されたアミノトリアゾロキナゾリン誘導体、医薬組成物及びそれらの使用
AR117164A1 (es) 2018-11-30 2021-07-14 Merck Sharp & Dohme Derivados de amino-triazoloquinazolina 9-sustituidos como antagonistas del receptor de adenosina, composiciones farmacéuticas y su uso para el tratamiento de diversos tipos de cáncer
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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
CN111423364A (zh) * 2020-05-19 2020-07-17 阿里生物新材料(常州)有限公司 一种(3-环丙基吡啶-2-基)甲胺的合成方法
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US10472347B2 (en) 2019-11-12
WO2016081290A1 (en) 2016-05-26
BR112017010261A2 (pt) 2018-02-06
RU2727805C2 (ru) 2020-07-24
CA2967944A1 (en) 2016-05-26
EP3220910A4 (en) 2018-04-25
CN107106558A (zh) 2017-08-29
MX381180B (es) 2025-03-12
CA2967944C (en) 2020-11-17
EP3220910B1 (en) 2020-01-15
RU2017120853A (ru) 2018-12-19
JP2020193211A (ja) 2020-12-03
MX2017006483A (es) 2017-09-12
RU2017120853A3 (enExample) 2019-06-17
EP3220910A1 (en) 2017-09-27
AU2015350315A1 (en) 2017-05-18
AU2015350315B2 (en) 2020-06-25
KR20170083136A (ko) 2017-07-17
JP2017533946A (ja) 2017-11-16
US20180327385A1 (en) 2018-11-15

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