JP2020527588A - アデノシンアンタゴニストとしてのヘテロ環式化合物 - Google Patents

アデノシンアンタゴニストとしてのヘテロ環式化合物 Download PDF

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JP2020527588A
JP2020527588A JP2020502984A JP2020502984A JP2020527588A JP 2020527588 A JP2020527588 A JP 2020527588A JP 2020502984 A JP2020502984 A JP 2020502984A JP 2020502984 A JP2020502984 A JP 2020502984A JP 2020527588 A JP2020527588 A JP 2020527588A
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alkylene
optionally
alkyl
halogen
substituted
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JP2020527588A5 (enExample
Inventor
ソン・ミン・ファム
ジーユン・チェン
アマンチュラー・アンサリ
プラディープ・エス・ジャダヴァル
ヴァルシャヴェクマール・エス・パティル
ファルハ・カーン
スリーカント・エイ・ラマチャンドラン
アニル・クマール・アガルワル
サルバジット・チャクラバルティ
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Nuvation Bio Inc
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    • 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
    • C07D241/20—Nitrogen atoms
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C07D417/02—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 two hetero rings
    • C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2020502984A 2017-07-18 2018-07-18 アデノシンアンタゴニストとしてのヘテロ環式化合物 Pending JP2020527588A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762534176P 2017-07-18 2017-07-18
US62/534,176 2017-07-18
PCT/US2018/042777 WO2019018584A1 (en) 2017-07-18 2018-07-18 HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS

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JP2020527588A true JP2020527588A (ja) 2020-09-10
JP2020527588A5 JP2020527588A5 (enExample) 2021-08-26

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US (2) US11028058B2 (enExample)
EP (1) EP3654978A4 (enExample)
JP (1) JP2020527588A (enExample)
KR (1) KR20200041315A (enExample)
CN (1) CN111163780A (enExample)
AU (1) AU2018302179A1 (enExample)
CA (1) CA3070273A1 (enExample)
IL (1) IL272056A (enExample)
MX (1) MX2020000690A (enExample)
SG (1) SG11202000418XA (enExample)
WO (1) WO2019018584A1 (enExample)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3070073A1 (en) 2017-07-18 2019-01-24 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
US12030867B2 (en) 2018-05-30 2024-07-09 University Of Notre Dame Du Lac Hsp90β selective inhibitors
CN110655509B (zh) * 2018-06-29 2023-01-24 江苏恒瑞医药股份有限公司 2-胺基嘧啶类衍生物、其制备方法及其在医药上的应用
CN111094254B (zh) * 2018-07-12 2022-07-26 江苏恒瑞医药股份有限公司 杂芳基类衍生物、其制备方法及其在医药上的应用
AU2019323035B2 (en) * 2018-08-17 2024-11-07 Dizal (Jiangsu) Pharmaceutical Co., Ltd. Pyrazine compounds and uses thereof
CN112279837B (zh) * 2018-08-17 2022-08-09 迪哲(江苏)医药股份有限公司 吡嗪化合物和其用途
CN113166119B (zh) * 2018-12-28 2024-01-05 四川科伦博泰生物医药股份有限公司 取代芳基化合物及其制备方法和用途
CN111377906B (zh) * 2018-12-28 2022-09-02 四川科伦博泰生物医药股份有限公司 取代的吡嗪化合物及其制备方法和用途
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
CA3126704A1 (en) * 2019-01-18 2020-07-23 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists
US20220298141A1 (en) * 2019-08-21 2022-09-22 Kalvista Pharmaceuticals Limited Enzyme inhibitors
WO2021262596A1 (en) 2020-06-22 2021-12-30 Pmv Pharmaceuticals, Inc. Methods and compounds for restoring mutant p53 function
KR102646627B1 (ko) * 2021-03-24 2024-03-13 주식회사 스탠다임 아데노신 a2a 수용체 및 아데노신 a2b 수용체의 이중 길항제, 및 이의 용도
WO2022268520A1 (de) * 2021-06-21 2022-12-29 Bayer Aktiengesellschaft Verwendung von substituierten pyrrolidinonen oder deren salzen zur steigerung der stresstoleranz in pflanzen.
WO2023001794A1 (en) * 2021-07-20 2023-01-26 Astrazeneca Ab Substituted pyrazine-2-carboxamides as hpk1 inhibitors for the treatment of cancer
US12492178B2 (en) 2021-09-01 2025-12-09 Empathbio, Inc. Stable polymorph of R-MDMA HCl
WO2023064585A1 (en) * 2021-10-14 2023-04-20 Vanderbilt University 7,8-dihydro-5h-1,6-naphthyridine derivatives as positive allosteric modulators of the muscarinic acetylcholine receptor m4 for treating neurological and psychiatric disorders
CN113968824B (zh) * 2021-11-29 2024-01-19 郑州大学 一种2,3,5-三取代吡嗪类化合物及其制备方法和应用
US11912680B2 (en) 2021-12-28 2024-02-27 Empathbio, Inc. Nitric oxide releasing prodrugs of MDA and MDMA
AU2023397123A1 (en) * 2022-12-12 2025-02-13 Avelos Therapeutics Inc. Substituted heterocyclic compound derivatives and their pharmaceutical use
CN121399112A (zh) * 2023-04-27 2026-01-23 维泰瑞隆有限公司 Sarm1调节剂、其制备和用途
WO2025036840A1 (en) * 2023-08-11 2025-02-20 Almirall, S.A. Pyridine or pyrazine derivatives as collagen vii (c7) inducers and their use in therapy

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007510620A (ja) * 2003-10-27 2007-04-26 アステラス製薬株式会社 ピラジン誘導体およびその医薬的使用
JP2009502837A (ja) * 2005-07-29 2009-01-29 ラボラトリオス・アルミラル・ソシエダッド・アノニマ アデノシン受容体アンタゴニストとして有用なピラジン誘導体
JP2013518864A (ja) * 2010-02-05 2013-05-23 ヘプタレス セラピューティックス リミテッド １，２，４−トリアジン−４−アミン含有誘導体
CN104341386A (zh) * 2013-07-23 2015-02-11 中国科学院上海药物研究所 一类芳基杂环小分子化合物、其衍生物及其制备方法和用途
WO2016081290A1 (en) * 2014-11-18 2016-05-26 Merck Sharp & Dohme Corp. Aminopyrazine compounds with a2a antagonist properties

Family Cites Families (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
USRE47351E1 (en) 1999-06-22 2019-04-16 Gilead Sciences, Inc. 2-(N-pyrazolo)adenosines with application as adenosine A2A receptor agonists
WO2003030909A1 (en) * 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
US6992087B2 (en) 2001-11-21 2006-01-31 Pfizer Inc Substituted aryl 1,4-pyrazine derivatives
PT2476667E (pt) 2003-02-26 2014-09-18 Sugen Inc Compostos de aminoheteroarilo como inibidores da proteína quinase
WO2004084824A2 (en) 2003-03-24 2004-10-07 Merck & Co., Inc. Biaryl substituted 6-membered heterocyles as sodium channel blockers
WO2005047285A1 (en) 2003-11-04 2005-05-26 Merck & Co., Inc. Substituted naphthyridinone derivatives
GB0800741D0 (en) * 2008-01-16 2008-02-20 Univ Greenwich Cyclic triazo and diazo sodium channel blockers
US8436171B2 (en) 2008-02-01 2013-05-07 Akinion Pharmaceuticals Ab Amino substituted pyrazines as inhibitors or protein kinases
ES2480994T3 (es) 2008-03-31 2014-07-29 Genentech, Inc. Compuestos de tipo benzopirano y benzoxepina inhibidores de PI3K y métodos de uso
WO2010088177A1 (en) 2009-02-02 2010-08-05 Merck Sharp & Dohme Corp. Inhibitors of akt activity
BR112013000946B1 (pt) 2010-07-14 2020-09-08 Novartis Ag Compostos heterocíclicos agonistas de receptor de ip, seus usos, composição e combinação farmacêuticas
EP2718978B1 (en) * 2011-06-09 2018-05-16 Novaled GmbH Organic electronic device
AR089698A1 (es) 2012-01-13 2014-09-10 Novartis Ag Compuestos heterociclicos antagonistas del receptor ip
US9266891B2 (en) 2012-11-16 2016-02-23 Boehringer Ingelheim International Gmbh Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors
EP2970312B1 (en) 2013-03-11 2017-11-15 The Regents of The University of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
EP2968322B1 (en) 2013-03-15 2018-12-26 The Trustees of Columbia University in the City of New York Map kinase modulators and uses thereof
KR102307566B1 (ko) 2013-06-21 2021-10-05 제니쓰 에피제네틱스 리미티드 신규한 바이사이클릭 브로모도메인 억제제
EP3027616B1 (en) 2013-07-30 2018-01-10 Boehringer Ingelheim International GmbH Azaindole compounds as modulators of rorc
BR122019007990B1 (pt) 2013-11-18 2021-05-04 Forma Therapeutics, Inc Composto, e, composição farmacêutica
RU2720237C2 (ru) 2013-11-18 2020-04-28 Форма Терапеутикс, Инк. Композиции, содержащие бензопиперазин, в качестве ингибиторов бромодоменов вет
US9580430B2 (en) 2014-02-28 2017-02-28 The Regents Of The University Of Michigan 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors
SMT202000133T1 (it) 2014-04-23 2020-05-08 Incyte Corp 1h-pirrolo[2,3-c]piridin-7(6h)-oni e pirazolo[3,4-c]piridin-7(6h)-oni come inibitori di proteine bet
WO2016092375A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Corp. Substituted heterocycles as bromodomain inhibitors
EP3262045A1 (en) 2015-02-27 2018-01-03 The Regents of The University of Michigan 9h-pyrimido [4,5-b]indoles as bet bromodomain inhibitors
KR20180012861A (ko) 2015-06-16 2018-02-06 오리온 코포레이션 브로모도메인 억제제로서의 스피로[사이클로부탄-1,3'-인돌린]-2'-온 유도체
WO2017025918A1 (en) 2015-08-11 2017-02-16 Novartis Ag 5-bromo-2,6-di-(lh-pyrazol-l-yl)pyrimidin-4-amine for use in the treatment of cancer
HK1255102A1 (zh) 2015-09-21 2019-08-02 Plexxikon Inc. 杂环化合物及其应用
EP3353162A1 (en) 2015-09-22 2018-08-01 Glaxosmithkline Intellectual Property (No. 2) Limited Pyridinone dicarboxamide for use as bromodomain inhibitors
AU2016379425B2 (en) 2015-12-24 2021-11-11 Corvus Pharmaceuticals, Inc. Methods of treating cancer
AU2017290362B2 (en) 2016-07-01 2021-08-05 Pharmacosmos Holding A/S Synthesis of N-(heteroaryl)-pyrrolo[3,2-d]pyrimidin-2-amines
WO2018005533A1 (en) 2016-07-01 2018-01-04 G1 Therapeutics, Inc. Antiproliferative pyrimidine-based compounds
CN109789143A (zh) 2016-07-01 2019-05-21 G1治疗公司 基于嘧啶的抗增殖剂
GB201612092D0 (en) 2016-07-12 2016-08-24 Almac Discovery Ltd Pharmaceutical compounds
WO2018081863A1 (en) 2016-11-04 2018-05-11 University Of Wollongong 6-SUBSTITUTED DERIVATIVES OF HEXAMETHYLENE AMILORIDE AS INHIBITORS OF uPA AND USES THEREOF
MX389798B (es) 2017-01-20 2025-03-20 Arcus Biosciences Inc Azolopirimidina para el tratamiento de trastornos relacionados con el cáncer.
AU2018246355B2 (en) 2017-03-30 2021-12-09 iTeos Belgium SA 2-oxo-thiazole derivatives as A2A inhibitors and compounds for use in the treatment of cancers
TWI801372B (zh) 2017-03-30 2023-05-11 比利時商艾特歐斯比利時有限公司 作為a2a抑制劑的硫胺甲酸酯衍生物以及用於癌症治療的方法
CN107221611B (zh) 2017-06-15 2019-02-05 江西冠能光电材料有限公司 一种稳定易加工有机半导体材料及其有机发光器件应用
AU2018294557A1 (en) 2017-06-30 2020-01-02 Ryvu Therapeutics S.A. Imidazo(1,2-a)pyrazine modulators of the adenosine A2A receptor
CA3070073A1 (en) 2017-07-18 2019-01-24 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
CA3080976A1 (en) 2017-11-06 2019-05-09 Corvus Pharmaceuticals, Inc. Adenosine pathway inhibitors for cancer treatment
WO2019096322A1 (zh) 2017-11-20 2019-05-23 上海医药集团股份有限公司 一种吡唑酮并嘧啶类化合物、其制备方法及应用
US11498923B2 (en) 2017-12-13 2022-11-15 Merck Sharp & Dohme Llc Substituted imidazo[1,2-c]quinazolines as A2A antagonists
TWI713952B (zh) 2017-12-20 2020-12-21 大陸商貝達藥業股份有限公司 作為溴結構域蛋白質抑制劑的化合物和組合物
WO2019134539A1 (zh) 2018-01-05 2019-07-11 四川科伦博泰生物医药股份有限公司 二氢吡唑酮并嘧啶类化合物及其制备方法和用途
US11427593B2 (en) 2018-01-16 2022-08-30 Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Bromodomain inhibitor compound and use thereof
WO2019148161A1 (en) 2018-01-29 2019-08-01 Beta Pharma, Inc. 2h-indazole derivatives as cdk4 and cdk6 inhibitors and therapeutic uses thereof
CN111511745B (zh) 2018-02-06 2022-05-27 江苏恒瑞医药股份有限公司 吡唑并[1，5-a][1，3，5]三嗪-2-胺类衍生物、其制备方法及其应用
CA3090795A1 (en) 2018-02-13 2019-08-22 Iovance Biotherapeutics, Inc. Expansion of tumor infiltrating lymphocytes (tils) with adenosine a2a receptor antagonists and therapeutic combinations of tils and adenosine a2a receptor antagonists
WO2019158070A1 (zh) 2018-02-15 2019-08-22 杭州阿诺生物医药科技有限公司 A2a和/或a2b受体拮抗剂
US11479555B2 (en) 2018-02-23 2022-10-25 Newave Pharmaceutical Inc. Substituted 1,2-dihydro-3H-pyrazolo[3,4-D]pyrimidin-3-ones as inhibitors of WEE-1 kinase
AU2019227607C1 (en) 2018-02-27 2023-07-20 Incyte Corporation Imidazopyrimidines and triazolopyrimidines as A2A / A2B inhibitors
CA3088997A1 (en) 2018-02-28 2019-09-06 The Regents Of The University Of Colorado, A Body Corporate Wee1 kinase inhibitors and methods of treating cancer using the same
BR112020018286A2 (pt) 2018-03-09 2020-12-29 Recurium Ip Holdings, Llc 1,2-di-hidro-3h-pirazolo[3,4-d]pirimidin-3-onas substituídas
US11220510B2 (en) 2018-04-09 2022-01-11 Incyte Corporation Pyrrole tricyclic compounds as A2A / A2B inhibitors
AU2019323035B2 (en) 2018-08-17 2024-11-07 Dizal (Jiangsu) Pharmaceutical Co., Ltd. Pyrazine compounds and uses thereof
AR116315A1 (es) 2018-09-12 2021-04-21 Dizal Jiangsu Pharmaceutical Co Ltd Compuestos de triazolo-pirimidina y usos de los mismos
US11254670B2 (en) 2019-01-18 2022-02-22 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
WO2020150674A1 (en) 2019-01-18 2020-07-23 Nuvation Bio Inc. Heterocyclic compounds as adenosine antagonists

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007510620A (ja) * 2003-10-27 2007-04-26 アステラス製薬株式会社 ピラジン誘導体およびその医薬的使用
JP2009502837A (ja) * 2005-07-29 2009-01-29 ラボラトリオス・アルミラル・ソシエダッド・アノニマ アデノシン受容体アンタゴニストとして有用なピラジン誘導体
JP2013518864A (ja) * 2010-02-05 2013-05-23 ヘプタレス セラピューティックス リミテッド １，２，４−トリアジン−４−アミン含有誘導体
CN104341386A (zh) * 2013-07-23 2015-02-11 中国科学院上海药物研究所 一类芳基杂环小分子化合物、其衍生物及其制备方法和用途
WO2016081290A1 (en) * 2014-11-18 2016-05-26 Merck Sharp & Dohme Corp. Aminopyrazine compounds with a2a antagonist properties

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