AU2010238361B2 - Imidazopyrazines for use as kinase inhibitors - Google Patents

Imidazopyrazines for use as kinase inhibitors Download PDF

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Publication number
AU2010238361B2
AU2010238361B2 AU2010238361A AU2010238361A AU2010238361B2 AU 2010238361 B2 AU2010238361 B2 AU 2010238361B2 AU 2010238361 A AU2010238361 A AU 2010238361A AU 2010238361 A AU2010238361 A AU 2010238361A AU 2010238361 B2 AU2010238361 B2 AU 2010238361B2
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Prior art keywords
imidazo
morpholin
pyrazine
methyl
pyrazin
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AU2010238361A1 (en
Inventor
Sonia Martinez Gonzalez
Julen Oyarzabal Santamarina
Joaquin Pastor Fernandez
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Centro Nacional de Investigaciones Oncologicas CNIO
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Fundacion Centro Nac De Investigaciones Oncologicas Carlos Iii
Centro Nacional de Investigaciones Oncologicas CNIO
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    • C07—ORGANIC CHEMISTRY
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    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
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    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
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AU2010238361A 2009-04-16 2010-04-16 Imidazopyrazines for use as kinase inhibitors Active AU2010238361B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09380079 2009-04-16
EP09380079.5 2009-04-16
PCT/GB2010/000773 WO2010119264A1 (en) 2009-04-16 2010-04-16 Imidazopyrazines for use as kinase inhibitors

Publications (2)

Publication Number Publication Date
AU2010238361A1 AU2010238361A1 (en) 2011-11-10
AU2010238361B2 true AU2010238361B2 (en) 2015-08-06

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AU2010238361A Active AU2010238361B2 (en) 2009-04-16 2010-04-16 Imidazopyrazines for use as kinase inhibitors

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US (1) US8778935B2 (enExample)
EP (1) EP2419429B1 (enExample)
JP (1) JP5805623B2 (enExample)
KR (2) KR20120034613A (enExample)
CN (1) CN102428087B (enExample)
AU (1) AU2010238361B2 (enExample)
BR (1) BRPI1014572B8 (enExample)
CA (1) CA2756759C (enExample)
DK (1) DK2419429T3 (enExample)
EA (1) EA022629B1 (enExample)
ES (1) ES2475091T3 (enExample)
IL (1) IL215297A (enExample)
MX (1) MX2011010915A (enExample)
NZ (1) NZ596185A (enExample)
SG (1) SG175195A1 (enExample)
WO (1) WO2010119264A1 (enExample)
ZA (1) ZA201107717B (enExample)

Families Citing this family (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US8729074B2 (en) 2009-03-20 2014-05-20 Amgen Inc. Inhibitors of PI3 kinase
NZ599597A (en) 2009-10-30 2013-05-31 Janssen Pharmaceutica Nv IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS
CA2787714C (en) 2010-01-22 2019-04-09 Joaquin Pastor Fernandez Inhibitors of pi3 kinase
AR080754A1 (es) 2010-03-09 2012-05-09 Janssen Pharmaceutica Nv Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10
TW201200518A (en) * 2010-03-10 2012-01-01 Kalypsys Inc Heterocyclic inhibitors of histamine receptors for the treatment of disease
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
KR20190061096A (ko) 2010-04-22 2019-06-04 버텍스 파마슈티칼스 인코포레이티드 시클로알킬카르복스아미도-인돌 화합물의 제조 방법
WO2011141713A1 (en) 2010-05-13 2011-11-17 Centro Nacional De Investigaciones Oncologicas (Cnio) New bicyclic compounds as pi3-k and mtor inhibitors
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
EP2444084A1 (en) 2010-10-21 2012-04-25 Centro Nacional de Investigaciones Oncológicas (CNIO) Use of PI3K inibitors for the treatment of obesity
TWI617559B (zh) 2010-12-22 2018-03-11 江蘇恆瑞醫藥股份有限公司 ２－芳基咪唑并［１，２－ｂ］嗒．２－苯基咪唑并［１，２－ａ］吡啶，和２－苯基咪唑并［１，２－ａ］吡衍生物
EP2524918A1 (en) 2011-05-19 2012-11-21 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyrazines derivates as kinase inhibitors
ES2575092T3 (es) 2011-06-27 2016-06-24 Janssen Pharmaceutica, N.V. Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxalina
AU2013251475B2 (en) 2012-04-26 2018-01-04 The General Hospital Corporation Agents and methods for treating and preventing seborrheic keratosis
CN103450204B (zh) * 2012-05-31 2016-08-17 中国科学院上海药物研究所 吡咯[2，1-f][1，2，4]并三嗪类化合物，其制备方法及用途
CN102675323B (zh) * 2012-06-01 2014-04-09 南京药石药物研发有限公司 吡咯并[2,1-f][1,2,4]三嗪衍生物及其抗肿瘤用途
RU2657540C2 (ru) 2012-06-26 2018-06-14 Янссен Фармацевтика Нв Комбинации, содержащие ингибиторы pde 2, такие как 1-арил-4-метил-[1,2,4]триазоло[4,3-а]хиноксалиновые соединения, и ингибиторы pde 10, для применения в лечении неврологических или метаболических расстройств
KR102171706B1 (ko) 2012-07-09 2020-10-30 얀센 파마슈티카 엔.브이. 포스포디에스테라아제 10 효소의 억제제
WO2014022728A1 (en) 2012-08-02 2014-02-06 Endo Pharmaceuticals, Inc Substituted 5 - (quinazolin - 2 - yl) pyrimidin- 2 -amine derivatives useful as pi3k/mtor inhibitors for the treatment of cancer
US10508309B2 (en) * 2013-05-17 2019-12-17 The General Hospital Corporation Methods for detecting and treating variants of seborrheic keratoses
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
TWI720451B (zh) 2014-02-13 2021-03-01 美商英塞特控股公司 作為lsd1抑制劑之環丙胺
KR102421235B1 (ko) 2014-02-13 2022-07-15 인사이트 코포레이션 Lsd1 저해제로서 사이클로프로필아민
US9493442B2 (en) 2014-02-13 2016-11-15 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
PL3925607T3 (pl) 2014-04-15 2023-10-30 Vertex Pharmaceuticals Incorporated Kompozycje farmaceutyczne do leczenia chorób, w których pośredniczy mukowiscydozowy przezbłonowy regulator przewodnictwa
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為ｌｓｄ１抑制劑之咪唑并吡啶及咪唑并吡嗪
PL236355B1 (pl) * 2015-04-02 2021-01-11 Celon Pharma Spolka Akcyjna Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-α]pirymidyny jako inhibitory kinazy PI3
SG11201708047UA (en) 2015-04-03 2017-10-30 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
ES2928164T3 (es) 2015-10-19 2022-11-15 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
HUE060680T2 (hu) 2015-11-19 2023-04-28 Incyte Corp Heterociklusos vegyületek mint immunmodulátorok
DK3394033T3 (da) 2015-12-22 2021-01-04 Incyte Corp Heterocykliske forbindelser som immunmodulatorer
CN105622526A (zh) * 2016-02-24 2016-06-01 湖北工业大学 一种2-氨基吡嗪衍生物的制备方法
EP4285996A3 (en) * 2016-04-15 2024-01-10 Blueprint Medicines Corporation Inhibitors of activin receptor-like kinase
SG10202010414QA (en) 2016-04-22 2020-11-27 Incyte Corp Formulations of an lsd1 inhibitor
MA44860A (fr) 2016-05-06 2019-03-13 Incyte Holdings Corp Composés hétérocycliques utilisés comme immunomodulateurs
WO2017205464A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
SG11201811414TA (en) 2016-06-20 2019-01-30 Incyte Corp Heterocyclic compounds as immunomodulators
ES2930092T3 (es) 2016-07-14 2022-12-07 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
EP3504198B1 (en) 2016-08-29 2023-01-25 Incyte Corporation Heterocyclic compounds as immunomodulators
EA201991355A1 (ru) * 2016-12-07 2019-11-29 Производные имидазо[1,5-а]пиразина в качестве ингибиторов pi3kдельта
US10858364B2 (en) * 2016-12-21 2020-12-08 Acerta Pharma B.V. Imidazopyrazine inhibitors of Bruton's tyrosine kinase
EP3558989B1 (en) 2016-12-22 2021-04-14 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
CA3047991A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
US20180179179A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
MA47123A (fr) 2016-12-22 2021-03-17 Incyte Corp Dérivés de benzooxazole en tant qu'mmunomodulateurs
MD3558990T2 (ro) 2016-12-22 2023-02-28 Incyte Corp Derivați tetrahidro imidazo[4,5-c]piridină ca inductori de internalizare a PD-L1
WO2019048036A1 (en) 2017-09-06 2019-03-14 Biontech Ag SUBSTITUTED IMIDAZOQUINOLINES
TWI817956B (zh) * 2017-09-08 2023-10-11 英屬開曼群島商百濟神州有限公司 咪唑並[1,5-A]吡嗪衍生物作爲PI3Kδ 抑制劑
MX2020003862A (es) 2017-10-18 2020-08-13 Incyte Corp Derivados condensados de imidazol sustituidos por grupos hidroxi terciarios como inhibidores de fosfoinositido 3-cinasas gamma (pi3k-gamma).
WO2019226213A2 (en) * 2018-03-08 2019-11-28 Incyte Corporation AMINOPYRAZINE DIOL COMPOUNDS AS PI3K-y INHIBITORS
US10669271B2 (en) 2018-03-30 2020-06-02 Incyte Corporation Heterocyclic compounds as immunomodulators
LT3790877T (lt) 2018-05-11 2023-05-10 Incyte Corporation Tetrahidro-imidazo[4,5-c]piridino dariniai kaip pd-l1 imunomoduliatoriai
WO2020047198A1 (en) 2018-08-31 2020-03-05 Incyte Corporation Salts of an lsd1 inhibitor and processes for preparing the same
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
EP3623370A1 (en) 2018-09-13 2020-03-18 Fundación del Sector Público Estatal Centro Nacional de Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Novel trf1 modulators and analogues thereof
US20220054496A1 (en) * 2018-09-13 2022-02-24 Fundación Del Sector Público Estatal Centro Nacional De Investigaciones Oncologicas Carlos III (F.S. Modulation of trf1 for brain cancer treatment
EP3623009A1 (en) 2018-09-13 2020-03-18 Fundación del Sector Público Estatal Centro Nacional de Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Modulation of trf1 for brain cancer treatment
TW202115059A (zh) 2019-08-09 2021-04-16 美商英塞特公司 Ｐｄ—１／ｐｄ—ｌ１抑制劑之鹽
EP4037773A1 (en) 2019-09-30 2022-08-10 Incyte Corporation Pyrido[3,2-d]pyrimidine compounds as immunomodulators
PE20230407A1 (es) 2019-11-11 2023-03-07 Incyte Corp Sales y formas cristalinas de un inhibidor de pd-1/pd-l1
US11718622B2 (en) 2020-03-16 2023-08-08 Exelixis Inc. Heterocyclic adenosine receptor antagonists
CN114599653B (zh) 2020-09-28 2025-12-16 第一生物治疗股份有限公司 作为造血祖细胞激酶1(hpk1)抑制剂的吲唑及其使用方法
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
WO2022099075A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Crystalline form of a pd-1/pd-l1 inhibitor
WO2022099071A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process for making a pd-1/pd-l1 inhibitor and salts and crystalline forms thereof
WO2022140647A1 (en) * 2020-12-23 2022-06-30 Children's Hospital Medical Center Multi-cyclic irak and flt3 inhibiting compounds and uses thereof
EP4049726A1 (en) 2021-02-25 2022-08-31 Fundación del Sector Público Estatal Centro Nacional de Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Imidazo[1,2-a]pyrazines as inhibitors of haspin and therapeutic uses thereof
US20240182495A1 (en) * 2021-03-17 2024-06-06 Janssen Sciences Ireland Unlimited Company Antibacterial compounds

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002060492A1 (en) * 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
WO2004022562A1 (en) * 2002-09-09 2004-03-18 Cellular Genomics, Inc. 6-ARYL-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
WO2004072081A1 (en) * 2003-02-10 2004-08-26 Cellular Genomics, Inc. Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of kinase activity
WO2009007029A1 (de) * 2007-07-11 2009-01-15 Bayer Schering Pharma Aktiengesellschaft Imidazo-, pyrazolopyrazine und imidazotriazine zur behandlung hämatologischer erkrankungen

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2607813B1 (fr) 1986-12-05 1989-03-31 Montpellier I Universite Alkylamino-8 imidazo (1,2-a) pyrazines et derives, leur preparation et leur application en therapeutique
WO1999064401A2 (en) 1998-06-12 1999-12-16 Societe De Conseils De Recherches Et D'applications Scientifiques Sas Imidazolyl derivatives and their use as somatostatin receptor ligands
NZ523774A (en) 2000-08-01 2004-09-24 Sod Conseils Rech Applic Imidazolyl derivatives
TWI312347B (en) 2001-02-08 2009-07-21 Eisai R&D Man Co Ltd Bicyclic nitrogen-containing condensed ring compounds
IL164703A0 (en) * 2002-04-19 2005-12-18 Cellular Genomics Inc ImidazoÄ1,2-AÜpyrazin-8-ylamines method of making and method of use thereof
US20030139427A1 (en) 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
TW200413378A (en) * 2002-09-23 2004-08-01 Schering Corp Novel imidazopyrazines as cyclin dependent kinase inhibitors
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
JP2009507032A (ja) 2005-09-02 2009-02-19 アボット・ラボラトリーズ 新規なイミダゾ系複素環
CN101300233A (zh) * 2005-09-09 2008-11-05 先灵公司 氮杂稠合的细胞周期蛋白依赖性激酶抑制剂
WO2007096764A2 (en) 2006-02-27 2007-08-30 Glenmark Pharmaceuticals S.A. Bicyclic heteroaryl derivatives as cannabinoid receptor modulators
MX2008013584A (es) 2006-04-26 2009-03-23 Genentech Inc Compuestos farmaceuticos.
MX2008015747A (es) * 2006-06-06 2008-12-19 Schering Corp Imidazopirazinas como inhibidores de la proteina quinasa.
WO2008059373A1 (en) 2006-11-17 2008-05-22 Raqualia Pharma Inc. Imidazo [1, 2-a] pyrazine derivatives and their use as acid pump antagonists
CA2690557A1 (en) 2007-06-14 2008-12-24 Schering Corporation Imidazopyrazines as protein kinase inhibitors

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002060492A1 (en) * 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
WO2004022562A1 (en) * 2002-09-09 2004-03-18 Cellular Genomics, Inc. 6-ARYL-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
WO2004072081A1 (en) * 2003-02-10 2004-08-26 Cellular Genomics, Inc. Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of kinase activity
WO2009007029A1 (de) * 2007-07-11 2009-01-15 Bayer Schering Pharma Aktiengesellschaft Imidazo-, pyrazolopyrazine und imidazotriazine zur behandlung hämatologischer erkrankungen

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