CA2756759C - Imidazopyrazines for use as kinase inhibitors - Google Patents

Imidazopyrazines for use as kinase inhibitors Download PDF

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Publication number
CA2756759C
CA2756759C CA2756759A CA2756759A CA2756759C CA 2756759 C CA2756759 C CA 2756759C CA 2756759 A CA2756759 A CA 2756759A CA 2756759 A CA2756759 A CA 2756759A CA 2756759 C CA2756759 C CA 2756759C
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Prior art keywords
morpholin
imidazo
pyrazine
methyl
pyrazin
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CA2756759A
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English (en)
French (fr)
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CA2756759A1 (en
Inventor
Joaquin Pastor Fernandez
Sonia Martinez Gonzalez
Julen Oyarzabal Santamarina
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Fundacion del Sector Publico Estatal Centro Nacional de Investigaciones Oncologicas Carlos III FSP CNIO
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Centro Nacional de Investigaciones Oncologicas CNIO
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    • 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
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    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/161,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/181,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/20Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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

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  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Physical Education & Sports Medicine (AREA)
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  • Rheumatology (AREA)
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  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Molecular Biology (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Surgery (AREA)
  • AIDS & HIV (AREA)
CA2756759A 2009-04-16 2010-04-16 Imidazopyrazines for use as kinase inhibitors Active CA2756759C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09380079.5 2009-04-16
EP09380079 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
CA2756759A1 CA2756759A1 (en) 2010-10-21
CA2756759C true CA2756759C (en) 2017-11-07

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Application Number Title Priority Date Filing Date
CA2756759A Active CA2756759C (en) 2009-04-16 2010-04-16 Imidazopyrazines for use as kinase inhibitors

Country Status (17)

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US (1) US8778935B2 (https=)
EP (1) EP2419429B1 (https=)
JP (1) JP5805623B2 (https=)
KR (2) KR101792837B1 (https=)
CN (1) CN102428087B (https=)
AU (1) AU2010238361B2 (https=)
BR (1) BRPI1014572B8 (https=)
CA (1) CA2756759C (https=)
DK (1) DK2419429T3 (https=)
EA (1) EA022629B1 (https=)
ES (1) ES2475091T3 (https=)
IL (1) IL215297A (https=)
MX (1) MX2011010915A (https=)
NZ (1) NZ596185A (https=)
SG (1) SG175195A1 (https=)
WO (1) WO2010119264A1 (https=)
ZA (1) ZA201107717B (https=)

Families Citing this family (74)

* 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
MX2011009796A (es) 2009-03-20 2011-12-14 Amgen Inc Inhibidores de la cinasa pi3.
PH12012500778A1 (en) 2009-10-30 2012-11-26 Janssen Pharmaceutica Nv IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS
EP2526102B1 (en) * 2010-01-22 2017-03-08 Fundación Centro Nacional de Investigaciones Oncológicas Carlos III 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
MX353408B (es) 2010-04-22 2018-01-11 Vertex Pharma Proceso para producir compuestos de cicloalquilcarboxamido-indol.
US20130131057A1 (en) 2010-05-13 2013-05-23 Centro Nacional De Investigaciones Oncologicas (Cnio New bicyclic compounds as pi3-k and mtor inhibitors
EP2444084A1 (en) 2010-10-21 2012-04-25 Centro Nacional de Investigaciones Oncológicas (CNIO) Use of PI3K inibitors for the treatment of obesity
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
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
BR112013033375B1 (pt) 2011-06-27 2022-05-10 Janssen Pharmaceutica N.V Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxa-lina, seu uso, composição farmacêutica que os compreende, processo de preparação dos mesmos, solução estéril e composto intermediário
DK2841075T3 (da) 2012-04-26 2020-06-22 Massachusetts Gen Hospital Midler og fremgangsmåder til behandling og forebyggelse af seboroisk keratose
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
HK1206250A1 (en) 2012-06-26 2016-01-08 Janssen Pharmaceutica Nv Combinations comprising pde 2 inhibitors such as 1-aryl-4-methyl-[1,2,4] triazolo [4,3-a] quinoxaline compounds and ped 10 inhibitors for use in the treatment of neurological or metabolic disorders
WO2014009305A1 (en) 2012-07-09 2014-01-16 Janssen Pharmaceutica Nv Inhibitors of phosphodiesterase 10 enzyme
US9145411B2 (en) 2012-08-02 2015-09-29 Asana Biosciences, Llc Substituted amino-pyrimidine derivatives
WO2014186663A2 (en) * 2013-05-17 2014-11-20 The General Hospital Corporation Methods for detecting and treating variants of seborrheic keratoses
MX373103B (es) 2014-02-13 2020-04-17 Incyte Holdings Corp Ciclopropilaminas como inhibidores de desmetilasa específica de lisina 1 (lsd1).
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
EP3105219B9 (en) 2014-02-13 2018-10-03 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
SI3105218T1 (sl) 2014-02-13 2019-11-29 Incyte Corp Ciklopropilamini kot inhibitorji LSD1
RU2744460C2 (ru) 2014-04-15 2021-03-09 Вертекс Фармасьютикалз Инкорпорейтед Фармацевтические композиции для лечения заболеваний, опосредованных муковисцидозным трансмембранным регулятором проводимости
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines 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
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
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
EP3277689B1 (en) 2015-04-03 2019-09-04 Incyte Corporation Heterocyclic compounds as lsd1 inhibitors
LT3334709T (lt) 2015-08-12 2025-03-10 Incyte Holdings Corporation Lsd1 inhibitoriaus druskos
EP3365340B1 (en) 2015-10-19 2022-08-10 Incyte Corporation Heterocyclic compounds as immunomodulators
US20170145025A1 (en) 2015-11-19 2017-05-25 Incyte Corporation Heterocyclic compounds as immunomodulators
ES2916874T3 (es) 2015-12-17 2022-07-06 Incyte Corp Derivados de N-fenil-piridina-2-carboxamida y su uso como moduladores de la interacción proteína/proteína PD-1/PD-L1
AU2016379372A1 (en) 2015-12-22 2018-08-02 Incyte Corporation Heterocyclic compounds as immunomodulators
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
SG11201808907PA (en) * 2016-04-15 2018-11-29 Blueprint Medicines Corp Inhibitors of activin receptor-like kinase
JP6999574B2 (ja) 2016-04-22 2022-01-18 インサイト・コーポレイション Lsd1阻害剤の製剤
ES2906460T3 (es) 2016-05-06 2022-04-18 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
ES2905980T3 (es) 2016-05-26 2022-04-12 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
BR112018076534A2 (pt) 2016-06-20 2019-04-02 Incyte Corporation compostos heterocíclicos como imunomoduladores
MA45669A (fr) 2016-07-14 2019-05-22 Incyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
ES2941716T3 (es) 2016-08-29 2023-05-25 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
TW202233190A (zh) * 2016-12-07 2022-09-01 英屬開曼群島商百濟神州有限公司 作為PI3Kδ抑制劑的咪唑並[1,5-A]吡衍生物
ES2856248T3 (es) * 2016-12-21 2021-09-27 Acerta Pharma Bv Inhibidores de imidazopirazina de la tirosina quinasa de Bruton
WO2018119286A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
ES2899402T3 (es) 2016-12-22 2022-03-11 Incyte Corp Derivados de piridina como inmunomoduladores
ES2874756T3 (es) 2016-12-22 2021-11-05 Incyte Corp Derivados de triazolo[1,5-A]piridina como inmunomoduladores
AU2017382870B2 (en) 2016-12-22 2022-03-24 Incyte Corporation Benzooxazole derivatives as immunomodulators
EP3558990B1 (en) 2016-12-22 2022-08-10 Incyte Corporation Tetrahydro imidazo[4,5-c]pyridine derivatives as pd-l1 internalization inducers
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
KR20240152947A (ko) 2017-10-18 2024-10-22 인사이트 코포레이션 Pi3k-감마 저해제로서의 3차 하이드록시기로 치환된 축합된 이미다졸 유도체
BR112020018094A2 (pt) 2018-03-08 2020-12-22 Incyte Corporation Compostos de aminopirazina diol como inibidores de pi3k-¿
CR20200520A (es) 2018-03-30 2021-03-09 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
WO2019217821A1 (en) 2018-05-11 2019-11-14 Incyte Corporation Tetrahydro-imidazo[4,5-c]pyridine derivatives as pd-l1 immunomodulators
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)
WO2020052772A1 (en) 2018-09-13 2020-03-19 Fundación Del Sector Público Estatal Centro Nacional De Investigaciones Oncológicas Carlos III (F.S.P. CNIO) 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
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
EP4010342A1 (en) 2019-08-09 2022-06-15 Incyte Corporation Salts of a pd-1/pd-l1 inhibitor
WO2021067217A1 (en) 2019-09-30 2021-04-08 Incyte Corporation Pyrido[3,2-d]pyrimidine compounds as immunomodulators
BR112022009031A2 (pt) 2019-11-11 2022-10-11 Incyte Corp Sais e formas cristalinas de um inibidor de pd-1/pd-l1
US11718622B2 (en) 2020-03-16 2023-08-08 Exelixis Inc. Heterocyclic adenosine receptor antagonists
IL301244A (en) 2020-09-28 2023-05-01 1St Biotherapeutics Inc INDOLES AS HEMATOPOIETIC PROGENITOR KINASE 1 (HPK1) INHIBITORS AND METHODS OF USING THEM
WO2022099075A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Crystalline form of a pd-1/pd-l1 inhibitor
US11866434B2 (en) 2020-11-06 2024-01-09 Incyte Corporation Process for making a PD-1/PD-L1 inhibitor and salts and crystalline forms thereof
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
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
MX2023010941A (es) * 2021-03-17 2023-11-28 Janssen Sciences Ireland Unlimited Co Compuestos antibacterianos.

Family Cites Families (19)

* 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
US6852725B1 (en) 1998-06-12 2005-02-08 Societe De Conseils De Recherches Et D'applications Scientifiques, S. A. S. Imidazolyl derivatives
WO2002010140A2 (en) 2000-08-01 2002-02-07 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) Imidazolyl derivatives
US20040102455A1 (en) * 2001-01-30 2004-05-27 Burns Christopher John Method of inhibiting kinases
TWI312347B (en) 2001-02-08 2009-07-21 Eisai R&D Man Co Ltd Bicyclic nitrogen-containing condensed ring compounds
CA2482991A1 (en) * 2002-04-19 2003-10-30 Cellular Genomics, Inc. Imidazo[1,2-a]pyrazin-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
US7312341B2 (en) 2002-09-09 2007-12-25 Cgi Pharmaceuticals, Inc. 6-aryl-imidazo[1,2-a] pyrazin-8-ylamines, method of making, and method of use thereof
TW200413378A (en) * 2002-09-23 2004-08-01 Schering Corp Novel imidazopyrazines as cyclin dependent kinase inhibitors
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
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
US7709468B2 (en) 2005-09-02 2010-05-04 Abbott Laboratories Imidazo based heterocycles
CA2621983A1 (en) * 2005-09-09 2007-03-22 Schering Corporation Azafused cyclin dependent kinase inhibitors
WO2007096764A2 (en) 2006-02-27 2007-08-30 Glenmark Pharmaceuticals S.A. Bicyclic heteroaryl derivatives as cannabinoid receptor modulators
TWI498332B (zh) 2006-04-26 2015-09-01 Hoffmann La Roche 作為pi3k抑制劑之嘧啶衍生物及相關製備方法、醫藥組合物、用途、套組及產物
AR061229A1 (es) * 2006-06-06 2008-08-13 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
MX2009013729A (es) 2007-06-14 2010-01-25 Schering Corp Imidazopirazinas como inhibidores de proteina quinasa.
DE102007032349A1 (de) 2007-07-11 2009-01-15 Bayer Healthcare Ag Imidazo-, Pyrazolopyrazine und Imidazotriazine und ihre Verwendung

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