RU2727805C2 - Аминопиразиновые соединения со свойствами антагониста a2a - Google Patents

Аминопиразиновые соединения со свойствами антагониста a2a Download PDF

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Publication number
RU2727805C2
RU2727805C2 RU2017120853A RU2017120853A RU2727805C2 RU 2727805 C2 RU2727805 C2 RU 2727805C2 RU 2017120853 A RU2017120853 A RU 2017120853A RU 2017120853 A RU2017120853 A RU 2017120853A RU 2727805 C2 RU2727805 C2 RU 2727805C2
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Russia
Prior art keywords
methyl
amino
carboxamide
pyrazine
oxazol
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RU2017120853A
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English (en)
Russian (ru)
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RU2017120853A (ru
RU2017120853A3 (enExample
Inventor
Жунцзе КУАН
Полин ТИНГ
Амджад Али
Хэпин У
Майкл БЕРЛИН
Эндрю СТЭМФОРД
Хунву ВАН
Ган ЧЖОУ
Дэвид Ким
Цяолинь ДЭН
Йеон-Хее ЛИМ
Юнун ЮЙ
Original Assignee
Мерк Шарп И Доум Корп.
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    • 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
    • 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
    • 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
    • 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
    • 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

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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)
RU2017120853A 2014-11-18 2015-11-13 Аминопиразиновые соединения со свойствами антагониста a2a RU2727805C2 (ru)

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

Publications (3)

Publication Number Publication Date
RU2017120853A RU2017120853A (ru) 2018-12-19
RU2017120853A3 RU2017120853A3 (enExample) 2019-06-17
RU2727805C2 true RU2727805C2 (ru) 2020-07-24

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RU2017120853A RU2727805C2 (ru) 2014-11-18 2015-11-13 Аминопиразиновые соединения со свойствами антагониста a2a

Country Status (11)

Country Link
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
WO2020146795A1 (en) 2019-01-11 2020-07-16 Omeros Corporation Methods and compositions for treating cancer
WO2020150674A1 (en) 2019-01-18 2020-07-23 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
US11254670B2 (en) 2019-01-18 2022-02-22 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
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
EP3929189A1 (en) * 2020-06-25 2021-12-29 Bayer Animal Health GmbH Novel heteroaryl-substituted pyrazine derivatives as pesticides
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CN117157278A (zh) * 2021-03-23 2023-12-01 柏奥艾奇实验室公司 Nlrp3炎性体的抑制剂
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US20250230168A1 (en) 2023-12-22 2025-07-17 Gilead Sciences, Inc. Azaspiro wrn inhibitors
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Also Published As

Publication number Publication date
US10472347B2 (en) 2019-11-12
WO2016081290A1 (en) 2016-05-26
BR112017010261A2 (pt) 2018-02-06
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
JP6779204B2 (ja) 2020-11-04

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