JP5805623B2 - キナーゼ阻害剤として使用するためのイミダゾピラジン類 - Google Patents

キナーゼ阻害剤として使用するためのイミダゾピラジン類 Download PDF

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JP5805623B2
JP5805623B2 JP2012505227A JP2012505227A JP5805623B2 JP 5805623 B2 JP5805623 B2 JP 5805623B2 JP 2012505227 A JP2012505227 A JP 2012505227A JP 2012505227 A JP2012505227 A JP 2012505227A JP 5805623 B2 JP5805623 B2 JP 5805623B2
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JP2012524053A (ja
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フェルナンデス， ホアキン パストル
フェルナンデス， ホアキン パストル
ゴンサレス， ソニア マルティネス
ゴンサレス， ソニア マルティネス
サンタマリナ， フレン オイアルサバル
サンタマリナ， フレン オイアルサバル
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Centro Nacional de Investigaciones Oncologicas CNIO
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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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    • A61K31/00—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic 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
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
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    • 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

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  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Immunology (AREA)
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  • Communicable Diseases (AREA)
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  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
JP2012505227A 2009-04-16 2010-04-16 キナーゼ阻害剤として使用するためのイミダゾピラジン類 Active JP5805623B2 (ja)

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 (3)

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JP2012524053A JP2012524053A (ja) 2012-10-11
JP2012524053A5 JP2012524053A5 (https=) 2013-05-30
JP5805623B2 true JP5805623B2 (ja) 2015-11-04

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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=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11267813B2 (en) 2017-09-06 2022-03-08 BioNTech SE Substituted imidazoquinolines

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
JP2012521354A (ja) 2009-03-20 2012-09-13 アムジエン・インコーポレーテツド Ｐｉ３キナーゼの阻害薬
KR101774035B1 (ko) 2009-10-30 2017-09-01 얀센 파마슈티카 엔.브이. 이미다조［１，２―ｂ］피리다진 유도체 및 ＰＤＥ１０ 저해제로서의 그의 용도
US9073927B2 (en) 2010-01-22 2015-07-07 Fundacion Centro Nacional De Investigaciones Oncologicas 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
ES2608474T3 (es) 2010-04-22 2017-04-11 Vertex Pharmaceuticals Incorporated Proceso de producción de compuestos indol cycloalkylcarboxamido
WO2011141713A1 (en) 2010-05-13 2011-11-17 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
WO2013000924A1 (en) 2011-06-27 2013-01-03 Janssen Pharmaceutica Nv 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES
HUE051096T2 (hu) 2012-04-26 2021-03-01 Massachusetts Gen Hospital Ágensek és módszerek a sebészeti keratózis kezelésére és megelõzésére
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
WO2014001314A1 (en) 2012-06-26 2014-01-03 Janssen Pharmaceutica Nv Combinations comprising pde 2 inhibitors such as 1-aryl-4-methyl- [1,2,4] triazolo [4,3-a] quinoxaline compounds and pde 10 inhibitors for use in the treatment of neurological or metabolic disorders
AU2013289284B2 (en) 2012-07-09 2017-03-30 Janssen Pharmaceutica Nv Inhibitors of phosphodiesterase 10 enzyme
US9145411B2 (en) 2012-08-02 2015-09-29 Asana Biosciences, Llc Substituted amino-pyrimidine derivatives
US10508309B2 (en) * 2013-05-17 2019-12-17 The General Hospital Corporation Methods for detecting and treating variants of seborrheic keratoses
EP3105219B9 (en) 2014-02-13 2018-10-03 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
EP3105218B1 (en) 2014-02-13 2019-09-25 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
JP6602779B2 (ja) 2014-02-13 2019-11-06 インサイト・コーポレイション Ｌｓｄ１阻害剤としてのシクロプロピルアミン類
ES2885181T3 (es) 2014-04-15 2021-12-13 Vertex Pharma Composiciones farmacéuticas para el tratamiento de enfermedades mediadas por el regulador de la conductancia transmembrana de fibrosis quística
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
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines 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
MY189367A (en) 2015-08-12 2022-02-08 Incyte Corp Salts of an lsd1 inhibitor
WO2017070089A1 (en) 2015-10-19 2017-04-27 Incyte Corporation Heterocyclic compounds as immunomodulators
SG10202004618TA (en) 2015-11-19 2020-06-29 Incyte Corp Heterocyclic compounds as immunomodulators
MA44075A (fr) 2015-12-17 2021-05-19 Incyte Corp Dérivés de n-phényl-pyridine-2-carboxamide et leur utilisation en tant que modulateurs des interactions protéine/protéine 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
CN109311889B (zh) * 2016-04-15 2021-11-16 缆图药品公司 激活素受体样激酶抑制剂
TWI833686B (zh) 2016-04-22 2024-03-01 美商英塞特公司 Lsd1 抑制劑之調配物
AR108396A1 (es) 2016-05-06 2018-08-15 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
WO2017205464A1 (en) 2016-05-26 2017-11-30 Incyte Corporation Heterocyclic compounds as immunomodulators
HUE060256T2 (hu) 2016-06-20 2023-02-28 Incyte Corp Heterociklusos vegyületek mint immunmodulátorok
EP3484866B1 (en) 2016-07-14 2022-09-07 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2018044783A1 (en) 2016-08-29 2018-03-08 Incyte Corporation Heterocyclic compounds as immunomodulators
CA3045959A1 (en) * 2016-12-07 2018-06-14 Beigene, Ltd. Imidazo [1,5-a] pyrazine derivatives as pi3kdelta inhibitors
AU2017383236B2 (en) * 2016-12-21 2022-02-10 Acerta Pharma B.V. Imidazopyrazine inhibitors of Bruton's tyrosine kinase
WO2018119221A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Pyridine derivatives as immunomodulators
US20180179202A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
ES2874756T3 (es) 2016-12-22 2021-11-05 Incyte Corp Derivados de triazolo[1,5-A]piridina como inmunomoduladores
JP7101678B2 (ja) 2016-12-22 2022-07-15 インサイト・コーポレイション 免疫調節剤としての複素環式化合物
LT3558990T (lt) 2016-12-22 2022-12-27 Incyte Corporation Tetrahidroimidazo[4,5-c]piridino dariniai kaip pd-l1 internalizavimo induktoriai
BR112020004500A2 (pt) * 2017-09-08 2020-12-01 Beigene, Ltd. derivados de imidazo [1,5-a] pirazina como inibidores de pi3kdelta
KR102717072B1 (ko) 2017-10-18 2024-10-15 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-¿
SMT202500157T1 (it) 2018-03-30 2025-05-12 Incyte Corp Composti eterociclici come immunomodulatori
HUE061503T2 (hu) 2018-05-11 2023-07-28 Incyte Corp Tetrahidro-imidazo[4,5-C]piridin-származékok mint PD-L1 immunmodulátorok
US10968200B2 (en) 2018-08-31 2021-04-06 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
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
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
JP7665593B2 (ja) 2019-08-09 2025-04-21 インサイト・コーポレイション Ｐｄ－１／ｐｄ－ｌ１阻害剤の塩
PE20221038A1 (es) 2019-09-30 2022-06-17 Incyte Corp Compuestos de pirido[3,2-d] pirimidina como inmunomoduladores
CA3160131A1 (en) 2019-11-11 2021-05-20 Incyte Corporation Salts and crystalline forms of a pd-1/pd-l1 inhibitor
US11718622B2 (en) 2020-03-16 2023-08-08 Exelixis Inc. Heterocyclic adenosine receptor antagonists
WO2022064459A1 (en) 2020-09-28 2022-03-31 1ST Biotherapeutics, Inc. Indazoles as hematopoietic progenitor kinase 1 (hpk1) inhibitors and methods of using same
CR20230230A (es) 2020-11-06 2023-07-27 Incyte Corp Proceso para hacer un inhibidor de pd-1/pdl1 y sales y formas cristalinas del mismo
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor
TW202233615A (zh) 2020-11-06 2022-09-01 美商英塞特公司 Ｐｄ—１／ｐｄ—ｌ１抑制劑之結晶形式
CA3201841A1 (en) * 2020-12-23 2022-06-30 Scott Bryan HOYT 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
CN117440958A (zh) * 2021-03-17 2024-01-23 爱尔兰詹森科学公司 抗菌化合物

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
DK1086086T3 (da) 1998-06-12 2005-01-24 Sod Conseils Rech Applic Imidazolylderivater og anvendelse deraf som somatostatinreceptorligander
ATE360620T1 (de) 2000-08-01 2007-05-15 Sod Conseils Rech Applic Imidazolderivate
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
KR20050008691A (ko) * 2002-04-19 2005-01-21 셀룰러 지노믹스 아이엔씨 이미다조[1,2-ａ]피라진-8-일 아민, 그의 제조방법 및사용방법
US20030139427A1 (en) 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
AU2003270489A1 (en) * 2002-09-09 2004-03-29 Cellular Genomics, Inc. 6-ARYL-IMIDAZO(1,2-a)PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
NZ538685A (en) * 2002-09-23 2008-02-29 Schering Corp Imidazopyrazines as cyclin dependent kinase inhibitors
WO2004072080A1 (en) 2003-02-10 2004-08-26 Cellular Genomics, Inc. Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of hsp90 complex activity
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
JP2009507843A (ja) * 2005-09-09 2009-02-26 シェーリング コーポレイション アザ縮合サイクリン依存性キナーゼ阻害剤
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
EP2029605A1 (en) * 2006-06-06 2009-03-04 Schering Corporation Imidazopyrazines as protein kinase inhibitors
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
DE102007032349A1 (de) * 2007-07-11 2009-01-15 Bayer Healthcare Ag Imidazo-, Pyrazolopyrazine und Imidazotriazine und ihre Verwendung

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11267813B2 (en) 2017-09-06 2022-03-08 BioNTech SE Substituted imidazoquinolines
US12054485B2 (en) 2017-09-06 2024-08-06 BioNTech SE Substituted imidazoquinolines

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