CO2021001251A2 - Derivados de pirazina fusionados como inhibidores de a2a/a2b - Google Patents

Derivados de pirazina fusionados como inhibidores de a2a/a2b

Info

Publication number
CO2021001251A2
CO2021001251A2 CONC2021/0001251A CO2021001251A CO2021001251A2 CO 2021001251 A2 CO2021001251 A2 CO 2021001251A2 CO 2021001251 A CO2021001251 A CO 2021001251A CO 2021001251 A2 CO2021001251 A2 CO 2021001251A2
Authority
CO
Colombia
Prior art keywords
inhibitors
pyrazine derivatives
diseases
derivatives fused
activity
Prior art date
Application number
CONC2021/0001251A
Other languages
English (en)
Inventor
Pei Gan
Chao Qi
xiaozhao Wang
Wenqing Yao
Zhiyong Yu
Liangxing Wu
Peter Niels Carlsen
Gia Hoang
Yong Li
Wenyu Zhu
Original Assignee
Incyte Corp
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 Incyte Corp filed Critical Incyte Corp
Publication of CO2021001251A2 publication Critical patent/CO2021001251A2/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

La presente solicitud hace referencia a compuestos de Fórmula I o sales farmacéuticamente aceptable de este, los cuales modulan la actividad de receptores de adenosina, tales como los subtipos de receptores A2A y A2B, y son útiles para el tratamiento de enfermedades relacionadas con la actividad de los receptores de adenosina, lo que incluye, por ejemplo, cáncer, enfermedades inflamatorias, enfermedades cardiovasculares y enfermedades neurodegenerativas.
CONC2021/0001251A 2018-07-05 2021-02-04 Derivados de pirazina fusionados como inhibidores de a2a/a2b CO2021001251A2 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862694138P 2018-07-05 2018-07-05
US201862755845P 2018-11-05 2018-11-05
PCT/US2019/040496 WO2020010197A1 (en) 2018-07-05 2019-07-03 Fused pyrazine derivatives as a2a / a2b inhibitors

Publications (1)

Publication Number Publication Date
CO2021001251A2 true CO2021001251A2 (es) 2021-04-19

Family

ID=67470665

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2021/0001251A CO2021001251A2 (es) 2018-07-05 2021-02-04 Derivados de pirazina fusionados como inhibidores de a2a/a2b

Country Status (22)

Country Link
US (2) US11161850B2 (es)
EP (1) EP3818063A1 (es)
JP (1) JP2024012451A (es)
KR (1) KR20210049090A (es)
CN (2) CN117304191A (es)
AU (1) AU2019297361A1 (es)
BR (1) BR112021000075A2 (es)
CA (1) CA3105721A1 (es)
CL (1) CL2021000004A1 (es)
CO (1) CO2021001251A2 (es)
CR (2) CR20240054A (es)
EC (1) ECSP21007838A (es)
GE (2) GEP20237548B (es)
IL (2) IL300821A (es)
JO (1) JOP20200342A1 (es)
MA (1) MA53097A (es)
MX (2) MX2021000116A (es)
PE (1) PE20211807A1 (es)
PH (1) PH12021550019A1 (es)
SG (1) SG11202013216RA (es)
TW (2) TW202402759A (es)
WO (1) WO2020010197A1 (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CR20160395A (es) 2014-02-13 2016-12-20 Incyte Corp Ciclopropilaminas como inhibidores de lsd1
KR102421235B1 (ko) 2014-02-13 2022-07-15 인사이트 코포레이션 Lsd1 저해제로서 사이클로프로필아민
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
MY191796A (en) 2015-04-03 2022-07-15 Incyte Corp Heterocyclic compounds as lsd1 inhibitors
CN110402244B (zh) 2015-08-12 2023-02-03 因赛特公司 Lsd1抑制剂的盐
CR20200441A (es) 2018-02-27 2021-03-15 Incyte Corp Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b
MX2020012376A (es) 2018-05-18 2021-03-09 Incyte Corp Derivados de pirimidina fusionados como inhibidores de los receptores de adenosina a2a/a2b.
WO2020047198A1 (en) 2018-08-31 2020-03-05 Incyte Corporation Salts of an lsd1 inhibitor and processes for preparing the same
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
AU2020417813A1 (en) * 2020-01-03 2022-08-25 Incyte Corporation Combination therapy comprising A2A/A2B and PD-1/PD-L1 inhibitors
WO2021156439A1 (en) 2020-02-06 2021-08-12 Astrazeneca Ab Triazole compounds as adenosine receptor antagonists
AU2021241886A1 (en) * 2020-03-26 2022-10-27 Heptares Therapeutics Limited Triazolone compounds
WO2021191376A1 (en) * 2020-03-26 2021-09-30 Astrazeneca Ab Triazolone compounds
GB202011996D0 (en) * 2020-07-31 2020-09-16 Adorx Therapeutics Ltd Antagonist compounds
GB2615307A (en) * 2022-01-28 2023-08-09 Adorx Therapeutics Ltd Antagonist compounds
KR102621694B1 (ko) * 2022-09-15 2024-01-08 주식회사 스탠다임 아데노신 a2a 수용체 길항제 및 이의 용도

Family Cites Families (146)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
JP4195729B2 (ja) 1997-03-24 2008-12-10 協和醗酵工業株式会社 [1,2,4]トリアゾロ[1,5−c]ピリミジン誘導体
DE69942097D1 (de) 1998-08-11 2010-04-15 Novartis Ag Isochinoline derivate mit angiogenesis-hemmender wirkung
AU756144B2 (en) 1998-09-22 2003-01-02 Kyowa Hakko Kogyo Co. Ltd. (1,2,4)triazolo(1,5-c)pyrimidine derivatives
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
KR100520907B1 (ko) 2000-05-26 2005-10-11 쉐링 코포레이션 아데노신 A2a수용체 길항제
PT1294358E (pt) 2000-06-28 2004-12-31 Smithkline Beecham Plc Processo de moagem por via humida
WO2002096363A2 (en) 2001-05-30 2002-12-05 Alteon, Inc. Method for treating fibrotic diseases or other indications
JP2004536807A (ja) 2001-05-30 2004-12-09 アルテオン インコーポレイテッド 緑内障vの治療方法
CA2466243A1 (en) 2001-09-19 2003-03-27 Aventis Pharma S.A. Indolizines as kinase protein inhibitors
WO2003031587A2 (en) 2001-10-09 2003-04-17 The Regents Of The University Of California Use of stat-6 inhibitors as therapeutic agents
KR20090087139A (ko) 2001-10-30 2009-08-14 노파르티스 아게 Flt3 수용체 티로신 키나아제 활성의 억제제로서의 스타우로스포린 유도체
US6921762B2 (en) 2001-11-16 2005-07-26 Amgen Inc. Substituted indolizine-like compounds and methods of use
TW200300686A (en) 2001-11-30 2003-06-16 Schering Corp Adenosine A2a receptor antagonists
CN101001857B (zh) 2002-01-22 2011-06-22 沃尼尔·朗伯有限责任公司 2-(吡啶-2-基氨基)-吡啶并[2,3-d]嘧啶-7-酮
AU2003211993A1 (en) 2002-02-15 2003-09-04 Kyowa Hakko Kogyo Co., Ltd. (1,2,4)TRIAZOLO(1,5-c)PYRIMIDINE DERIVATIVES
TW200406374A (en) 2002-05-29 2004-05-01 Novartis Ag Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
JPWO2004029056A1 (ja) 2002-09-24 2006-01-26 協和醗酵工業株式会社 [1,2,4]トリアゾロ[1,5−c]ピリミジン誘導体
AR042052A1 (es) 2002-11-15 2005-06-08 Vertex Pharma Diaminotriazoles utiles como inhibidores de proteinquinasas
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
GB0303910D0 (en) 2003-02-20 2003-03-26 Merck Sharp & Dohme Therapeutic agents
TW201018661A (en) 2003-03-14 2010-05-16 Ono Pharmaceutical Co Heterocyclic rinf having nitrogen atom derivatives and medicament containing the derivatives as active ingredient
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
AR043633A1 (es) 2003-03-20 2005-08-03 Schering Corp Ligandos de receptores de canabinoides
EP1615931A1 (en) 2003-04-09 2006-01-18 Biogen Idec MA Inc. Triazolopyrazines and methods of making and using the same
EP1633756B1 (en) 2003-04-09 2008-12-24 Biogen Idec MA Inc. A2a adenosine receptor antagonists
US20070010522A1 (en) 2003-04-09 2007-01-11 Chi Vu Triazolo[1,5-c]pyrimidines and pyrazolo[1,5-c]pyrimidines useful as a2a adenosine receptor antagonists
AU2004244906A1 (en) 2003-06-10 2004-12-16 Kyowa Hakko Kirin Co., Ltd. A method of treating an anxiety disorder
RU2376292C2 (ru) 2003-08-14 2009-12-20 Ф.Хоффманн-Ля Рош Аг Гамк-ергические модуляторы
US8362017B2 (en) 2003-08-29 2013-01-29 Exelixis, Inc. C-kit modulators and methods of use
PE20050952A1 (es) 2003-09-24 2005-12-19 Novartis Ag Derivados de isoquinolina como inhibidores de b-raf
GB0403819D0 (en) 2004-02-20 2004-03-24 Merck Sharp & Dohme New compounds
JP2007529496A (ja) 2004-03-19 2007-10-25 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー 抗菌剤としてのイミダゾピリジン及びイミダゾピリミジン誘導体
US7306631B2 (en) 2004-03-30 2007-12-11 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
US7687638B2 (en) 2004-06-04 2010-03-30 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
MY144044A (en) 2004-06-10 2011-07-29 Irm Llc Compounds and compositions as protein kinase inhibitors
JP2008503562A (ja) 2004-06-23 2008-02-07 イデニクス(ケイマン)リミテツド フラビウイルス科による感染症を治療するための5−アザ−7−デアザプリン誘導体
US20050288502A1 (en) 2004-06-25 2005-12-29 Andersen Denise L Substituted heterocyclic compounds and methods of use
US7713973B2 (en) 2004-10-15 2010-05-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
US20060211739A1 (en) 2005-02-08 2006-09-21 Arturo Perez-Medrano Use of selective P2X7 receptor antagonists
WO2006129626A1 (ja) 2005-05-30 2006-12-07 Kyowa Hakko Kogyo Co., Ltd. [1,2,4]トリアゾロ[1,5-c]ピリミジン誘導体の製造法
US7851478B2 (en) 2005-06-07 2010-12-14 Kyowa Hakko Kirin Co., Ltd. Agent for preventing and/or treating movement disorder
US7452892B2 (en) 2005-06-17 2008-11-18 Bristol-Myers Squibb Company Triazolopyrimidine cannabinoid receptor 1 antagonists
JP4986451B2 (ja) 2005-06-30 2012-07-25 信一郎 礒部 マーキング剤
WO2007011759A2 (en) 2005-07-15 2007-01-25 Kalypsys, Inc. Inhibitors of mitotic kinesin
CA2620223A1 (en) 2005-09-02 2007-03-08 Abbott Laboratories Novel imidazo based heterocycles
AU2006315718B2 (en) 2005-11-10 2012-10-04 Merck Sharp & Dohme Corp. Imidazopyrazines as protein kinase inhibitors
ES2436877T3 (es) 2005-11-17 2014-01-07 OSI Pharmaceuticals, LLC Intermedios para la preparación de inhibidores de mTOR bicíclicos condensados
US8349850B2 (en) 2006-03-28 2013-01-08 Atir Holding S.A. Heterocyclic compounds and uses thereof in the treatment of sexual disorders
WO2007138072A2 (en) 2006-05-31 2007-12-06 Galapagos N.V. Triazolopyrazine compounds useful for the treatment of degenerative & inflammatory diseases
EP2049518B1 (en) 2006-05-31 2011-08-31 Takeda San Diego, Inc. Indazole and isoindole derivatives as glucokinase activating agents.
KR20090025261A (ko) 2006-06-23 2009-03-10 인사이트 코포레이션 Hm74a 아고니스트로서의 퓨리논 유도체
EP2037905B1 (en) 2006-06-23 2013-05-01 Radius Health, Inc. Treatment of vasomotor symptoms with selective estrogen receptor modulators
WO2008011560A2 (en) 2006-07-20 2008-01-24 Mehmet Kahraman Benzothiophene inhibitors of rho kinase
DE102006041292A1 (de) 2006-09-01 2008-03-06 Henkel Kgaa Wasserstoffperoxid-Aktivierung mit N-Heterocyclen
WO2008037607A1 (de) 2006-09-25 2008-04-03 Basf Se Carbonylgruppen-enthaltende heterocyclische verbindungen und deren verwendung zur bekämpfung von phytopathogenen pilzen
WO2008056176A1 (en) 2006-11-10 2008-05-15 Scottish Biomedical Limited Pyrazolopyrimidines as phosphodiesterase inhibitors
WO2008070599A1 (en) 2006-12-05 2008-06-12 Chung-Ming Sun Indazole compounds
DE102007012645A1 (de) 2007-03-16 2008-09-18 Bayer Healthcare Ag Substituierte Imidazo- und Triazolopyrimidine
KR20090130109A (ko) 2007-04-10 2009-12-17 하. 룬트벡 아크티에 셀스카브 P2x7 길항제로서의 헤테로아릴 아미드 유사체
US8039505B2 (en) 2007-04-11 2011-10-18 University Of Utah Research Foundation Compounds for modulating T-cells
WO2008141249A1 (en) 2007-05-10 2008-11-20 Acadia Pharmaceuticals Inc. Imidazol (1,2-a)pyridines and related compounds with activity at cannabinoid cb2 receptors
WO2008138843A1 (en) 2007-05-10 2008-11-20 Galapagos N.V. Imidazopyridines and triazolopyrimidines useful for the treatment of joint degenerative & inflammatory diseases
AU2008277628B2 (en) 2007-07-18 2012-03-15 Novartis Ag Bicyclic heteroaryl compounds and their use as kinase inhibitors
GB0715087D0 (en) 2007-08-03 2007-09-12 Summit Corp Plc Drug combinations for the treatment of duchenne muscular dystrophy
EP2187883A2 (en) 2007-08-10 2010-05-26 Genelabs Technologies, Inc. Nitrogen containing bicyclic chemical entities for treating viral infections
GB0719803D0 (en) 2007-10-10 2007-11-21 Cancer Rec Tech Ltd Therapeutic compounds and their use
CN101801379A (zh) 2007-10-18 2010-08-11 诺瓦提斯公司 治疗癌症和骨疾病的csf-1r抑制剂
US20090118301A1 (en) 2007-11-02 2009-05-07 Arbor Vita Corporation Compositions and Methods for Treating Cancer
US20100292232A1 (en) 2007-11-09 2010-11-18 Daniel Elleder Non-nucleoside reverse transcriptase inhibitors
PE20091074A1 (es) 2007-12-13 2009-07-26 Bayer Healthcare Ag Triazolotriazinas y triazolopirazinas y su uso
KR20100095020A (ko) 2007-12-19 2010-08-27 암젠 인크 세포 주기 억제제로서의 융합된 피리딘, 피리미딘 및 트리아진 화합물
US7820665B2 (en) 2007-12-19 2010-10-26 Amgen Inc. Imidazopyridazine inhibitors of PI3 kinase for cancer treatment
JP5547099B2 (ja) 2008-03-14 2014-07-09 インテリカイン, エルエルシー キナーゼ阻害剤および使用方法
WO2009117421A2 (en) 2008-03-17 2009-09-24 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
KR101632450B1 (ko) 2008-03-21 2016-06-21 엔쏜 인코포레이티드 다작용기성 화합물을 이용한 적층체에 대한 금속의 접착 촉진
US20090281089A1 (en) 2008-04-11 2009-11-12 Genentech, Inc. Pyridyl inhibitors of hedgehog signalling
EP2444403A1 (en) 2008-04-18 2012-04-25 Shionogi Co., Ltd. Heterocyclic compound having inhibitory activity on PI3K
TWI473614B (zh) 2008-05-29 2015-02-21 Kyowa Hakko Kirin Co Ltd Anti-analgesic inhibitors
US9254283B2 (en) 2008-07-23 2016-02-09 Kyowa Hakko Kirin Co., Ltd. Therapeutic agent for migraine
WO2010032874A1 (ja) 2008-09-19 2010-03-25 住友化学株式会社 農業用組成物
US20120021519A1 (en) 2008-09-19 2012-01-26 Presidents And Fellows Of Harvard College Efficient induction of pluripotent stem cells using small molecule compounds
PA8852901A1 (es) 2008-12-22 2010-07-27 Lilly Co Eli Inhibidores de proteina cinasa
MX2011006332A (es) 2008-12-23 2011-06-27 Abbott Lab Compuestos antivirales.
US8546405B2 (en) 2008-12-23 2013-10-01 Abbott Laboratories Anti-viral compounds
EP2210891A1 (en) 2009-01-26 2010-07-28 Domain Therapeutics New adenosine receptor ligands and uses thereof
WO2010104306A2 (ko) 2009-03-07 2010-09-16 주식회사 메디젠텍 세포핵에서 세포질로의 gsk3의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 gsk3 이동에 의해 발생되는 질환의 치료 또는 예방용 약학적 조성물
EP2464647B1 (en) 2009-08-11 2016-09-21 Bristol-Myers Squibb Company Azaindazoles as btk kinase modulators and use thereof
CA2771532C (en) 2009-08-17 2021-03-23 Intellikine, Inc. Heterocyclic compounds and uses thereof
US8435994B2 (en) 2009-11-16 2013-05-07 Merck Sharp & Dohme Corp. Substituted [1,2,4]triazolo[4,3-alpha]quinoxalines as adenosine A2a receptor antagonists
WO2011078143A1 (ja) 2009-12-22 2011-06-30 塩野義製薬株式会社 ピリミジン誘導体およびそれらを含有する医薬組成物
US20110190269A1 (en) 2010-02-01 2011-08-04 Karlheinz Baumann Gamma secretase modulators
UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
TW201200518A (en) 2010-03-10 2012-01-01 Kalypsys Inc Heterocyclic inhibitors of histamine receptors for the treatment of disease
KR101732212B1 (ko) 2010-03-18 2017-05-02 재단법인 한국파스퇴르연구소 항감염성 화합물
UY33304A (es) 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
GB201007187D0 (en) 2010-04-29 2010-06-09 Iti Scotland Ltd Ubiquitination modulators
WO2011153588A1 (en) 2010-06-10 2011-12-15 Biota Scientific Management Pty Ltd Viral polymerase inhibitors
US20120083498A1 (en) 2010-06-17 2012-04-05 Fatah Kashanchi Modulators of Viral Transcription, and Methods and Compositions Therewith
ES2614128T3 (es) 2010-08-27 2017-05-29 Merck Patent Gmbh Derivados de triazolopirazina
DK2632467T3 (en) 2010-10-25 2016-08-15 G1 Therapeutics Inc CDK inhibitors
CN104906103B (zh) 2010-12-14 2018-05-18 电泳有限公司 酪蛋白激酶1δ(CK1δ)抑制剂
EP2663565B1 (en) 2011-01-11 2017-03-15 Sunovion Pharmaceuticals Inc. Heteroaryl compounds and methods of use thereof
WO2012116237A2 (en) 2011-02-23 2012-08-30 Intellikine, Llc Heterocyclic compounds and uses thereof
PT2688887E (pt) 2011-03-23 2015-07-06 Amgen Inc Inibidores duais tricíclicos fusionados de cdk 4/6 e flt3
US9029389B2 (en) 2011-04-21 2015-05-12 Institut Pasteur Korea Anti-inflammation compounds
WO2012147890A1 (ja) 2011-04-27 2012-11-01 持田製薬株式会社 新規アゾール誘導体
DE102011111400A1 (de) 2011-08-23 2013-02-28 Merck Patent Gmbh Bicyclische heteroaromatische Verbindungen
EP2604265A1 (en) 2011-12-17 2013-06-19 Royal College of Surgeons in Ireland (RCSI) P2x7 antagonists as frontline or adjunctive treatment against status epilepticus
WO2013106254A1 (en) 2012-01-11 2013-07-18 Dow Agrosciences Llc Pesticidal compositions and processes related thereto
WO2013178572A1 (en) 2012-05-30 2013-12-05 F. Hoffmann-La Roche Ag Triazolo compounds as pde10 inhibitors
WO2013191112A1 (ja) 2012-06-22 2013-12-27 住友化学株式会社 縮合複素環化合物
JP2015528013A (ja) 2012-07-27 2015-09-24 ビアル−ポルテラ エ コンパニア,ソシエダッド アノニマ 置換ウレア化合物の合成方法
EP2919770A4 (en) 2012-11-14 2017-03-08 The Board of Regents of The University of Texas System Inhibition of hif-2 heterodimerization with hif1 (arnt)
WO2014126580A1 (en) 2013-02-15 2014-08-21 Dow Agrosciences Llc Pesticidal compositions and processes related thereto
EP2968304B1 (en) 2013-03-14 2018-10-10 The Trustees of Columbia University in the City of New York 4-phenylpiperidines, their preparation and use
WO2015013635A2 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
WO2015157955A1 (en) 2014-04-17 2015-10-22 Abbvie Inc. Heterocyclic btk inhibit ors
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
EP3204007B1 (en) 2014-10-06 2023-12-20 Apm Therapeutics 1, Inc. Triazolopyridine compounds and methods for the treatment of cystic fibrosis
PL3257853T3 (pl) 2015-02-12 2022-03-21 Nissan Chemical Corporation Skondensowany związek heterocykliczny i środek zwalczający szkodliwe organizmy
EP3795568A1 (en) 2015-03-06 2021-03-24 Pharmakea, Inc. Fluorinated lysyl oxidase-like 2 inhibitors and uses thereof
MY191796A (en) 2015-04-03 2022-07-15 Incyte Corp Heterocyclic compounds as lsd1 inhibitors
EP3393475A4 (en) 2015-12-24 2019-08-14 Corvus Pharmaceuticals, Inc. METHOD FOR THE TREATMENT OF CANCER
IL261606B (en) 2016-03-16 2022-09-01 Kura Oncology Inc Inhibitors of converted menin-mll and methods of use
WO2017223414A1 (en) 2016-06-24 2017-12-28 Incyte Corporation HETEROCYCLIC COMPOUNDS AS PI3K-γ INHIBITORS
JP7240319B2 (ja) 2017-01-23 2023-03-15 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阻害剤としての二環式化合物
EP3575301A4 (en) 2017-03-16 2020-08-05 Jiangsu Hengrui Medicine Co., Ltd. HETEROARYL [4,3-C] PYRIMIDINE-5-AMINE DERIVATIVE, PROCESS FOR PREPARATION AND MEDICAL USES
PT3611174T (pt) * 2017-04-07 2022-07-07 Medshine Discovery Inc Derivado de [1,2,4]triazolo[1,5-c]pirimidina como inibidor do recetor a2a
US11542248B2 (en) 2017-06-08 2023-01-03 Kura Oncology, Inc. Methods and compositions for inhibiting the interaction of menin with MLL proteins
WO2019002606A1 (en) * 2017-06-30 2019-01-03 Selvita S.A. ADENOSINE A2A RECEPTOR 5,6-BICYCLO-IMIDAZO [1,2-A] PYRAZINE MODULATORS
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
WO2019079469A1 (en) 2017-10-18 2019-04-25 Incyte Corporation CONDENSED IMIDAZOLE DERIVATIVES SUBSTITUTED WITH HYDROXY TERTIARY GROUPS AS INHIBITORS OF PI3K-GAMMA
SG11202003641RA (en) 2017-10-24 2020-05-28 Bayer Ag Substituted imidazopyridine amides and use thereof
CR20200441A (es) * 2018-02-27 2021-03-15 Incyte Corp Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b
MX2020012376A (es) 2018-05-18 2021-03-09 Incyte Corp Derivados de pirimidina fusionados como inhibidores de los receptores de adenosina a2a/a2b.
AR116315A1 (es) 2018-09-12 2021-04-21 Dizal Jiangsu Pharmaceutical Co Ltd Compuestos de triazolo-pirimidina y usos de los mismos
EP3856173A4 (en) 2018-09-26 2022-07-06 Kura Oncology, Inc. TREATMENT OF HEMATOLOGICAL MALIGNITIES WITH MENIN INHIBITORS
CN111295384B (zh) 2018-10-10 2022-08-12 江苏豪森药业集团有限公司 双环类衍生物抑制剂、其制备方法和应用
WO2020106560A1 (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
EP3889152A4 (en) 2018-11-30 2022-09-07 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. HETEROAROMATIC DERIVATIVES FOR USE AS REGULATORS, PROCESS FOR THEIR PREPARATION AND THEIR USE
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
CA3150766A1 (en) 2019-08-26 2021-03-04 Incyte Corporation Triazolopyrimidines as a2a / a2b inhibitors

Also Published As

Publication number Publication date
CL2021000004A1 (es) 2021-05-14
JP2024012451A (ja) 2024-01-30
JP2021529804A (ja) 2021-11-04
KR20210049090A (ko) 2021-05-04
MA53097A (fr) 2021-05-12
SG11202013216RA (en) 2021-01-28
GEP20237548B (en) 2023-10-10
TWI829716B (zh) 2024-01-21
PE20211807A1 (es) 2021-09-14
MX2023008994A (es) 2023-08-08
US11161850B2 (en) 2021-11-02
IL300821A (en) 2023-04-01
CN117304191A (zh) 2023-12-29
CN113166153A (zh) 2021-07-23
TW202012409A (zh) 2020-04-01
IL279829A (en) 2021-03-01
US20220135570A1 (en) 2022-05-05
PH12021550019A1 (en) 2021-09-13
CR20240054A (es) 2024-02-26
AU2019297361A1 (en) 2021-02-25
EP3818063A1 (en) 2021-05-12
ECSP21007838A (es) 2021-04-29
TW202402759A (zh) 2024-01-16
CA3105721A1 (en) 2020-01-09
GEP20237560B (en) 2023-10-25
BR112021000075A2 (pt) 2021-04-06
CR20210071A (es) 2021-06-10
MX2021000116A (es) 2021-03-29
WO2020010197A1 (en) 2020-01-09
JOP20200342A1 (ar) 2020-12-30
US20200031835A1 (en) 2020-01-30

Similar Documents

Publication Publication Date Title
CO2021001251A2 (es) Derivados de pirazina fusionados como inhibidores de a2a/a2b
ECSP20060827A (es) Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b
ECSP21008112A (es) Compuestos de pirrolotriazina como inhibidores de tam
CO2022003457A2 (es) Triazolopirimidinas como inhibidores de a2a/a2b
CL2021001984A1 (es) Pirazolopiridinas y triazolopiridinas como inhibidores de a2a / a2b.
UY37124A (es) Nuevos compuestos de 6,7-dihidro-5h-benzo[7]anuleno sustituidos, procesos para su preparación y usos terapéuticos de los mismos
CR20150633A (es) Derivados del bipirazol como inhibidores jak
UY35898A (es) ?compuestos inhibidores de syk y composiciones que los comprenden?.
ECSP17021897A (es) Compuestos y composiciones como inhibidores de quinasa raf
AR094964A1 (es) USO DE DERIVADOS DE PIRAZOLOPIRIMIDINA PARA EL TRATAMIENTO DE TRASTORNOS RELACIONADOS CON LA FOSFOINOSITIDA 3-CINASA d (PI3Kd)
ECSP20061378A (es) COMPUESTOS DIÓLICOS DE AMINOPIRAZINA COMO INHIBIDORES DE PI3K-gamma
UY36875A (es) Composiciones inhibidoras de bromodominios para el tratamiento de diversas enfermedades
CL2020001047A1 (es) Derivados de imidazol condensado sustituidos por grupos de hidroxia terciaria como inhibidores pi3k-gamma.
CR20170513A (es) Derivados de pirazol útiles como inhibidores de proteína activadora de 5-li-poxigenasa (flap).
ECSP18056196A (es) Derivados de indano
AR117605A1 (es) Derivados de pirazina fusionados como inhibidores de a2a / a2b
UY36608A (es) Derivados de indol
EA202190204A1 (ru) Производные конденсированных пиразинов как ингибиторы a2a/a2b
CU20140107A7 (es) Derivados macrocíclicos para el tratamiento de enfermedades
EA202092016A1 (ru) Имидазопиримидины и триазолопиримидины в качестве ингибиторов a2a/a2b