CA2703125C - Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer - Google Patents

Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer Download PDF

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Publication number
CA2703125C
CA2703125C CA2703125A CA2703125A CA2703125C CA 2703125 C CA2703125 C CA 2703125C CA 2703125 A CA2703125 A CA 2703125A CA 2703125 A CA2703125 A CA 2703125A CA 2703125 C CA2703125 C CA 2703125C
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Canada
Prior art keywords
pyrazol
pyrrolo
6alkyl
pyrazin
independently selected
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Legal status (The legal status 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 status listed.)
Expired - Fee Related
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CA2703125A
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English (en)
French (fr)
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CA2703125A1 (en
Inventor
David J. Guerin
Joon Jung
Elizabeth Stanton
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Merck Sharp and Dohme LLC
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Publication of CA2703125A1 publication Critical patent/CA2703125A1/en
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Publication of CA2703125C publication Critical patent/CA2703125C/en
Expired - Fee Related legal-status Critical Current
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2703125A 2007-10-25 2008-10-21 Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer Expired - Fee Related CA2703125C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US34307P 2007-10-25 2007-10-25
US61/000,343 2007-10-25
PCT/US2008/011971 WO2009054941A1 (en) 2007-10-25 2008-10-21 Therapeutic compounds

Publications (2)

Publication Number Publication Date
CA2703125A1 CA2703125A1 (en) 2009-04-30
CA2703125C true CA2703125C (en) 2012-08-28

Family

ID=40579830

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2703125A Expired - Fee Related CA2703125C (en) 2007-10-25 2008-10-21 Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer

Country Status (6)

Country Link
US (1) US8183245B2 (https=)
EP (1) EP2211620B1 (https=)
JP (1) JP2011500806A (https=)
AU (1) AU2008317406B2 (https=)
CA (1) CA2703125C (https=)
WO (1) WO2009054941A1 (https=)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2211620B1 (en) * 2007-10-25 2013-12-25 Merck Sharp & Dohme Corp. 3-PYRAZIN SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AS JANUS KINASE INHIBITORS FOR THE TREATMENT OF CANCER DISEASES
JP5576370B2 (ja) * 2008-08-06 2014-08-20 ファイザー・インク Chk−1阻害剤としての6置換2−ヘテロシクリルアミノピラジン化合物
WO2010068483A2 (en) 2008-11-25 2010-06-17 University Of Rochester Mlk inhibitors and methods of use
DE102009019962A1 (de) * 2009-05-05 2010-11-11 Merck Patent Gmbh 3-([1,2,3]Triazol-4-yl)-pyrrolo[2,3-b]pyridinderivate
ES2540964T3 (es) * 2009-06-08 2015-07-15 Takeda Pharmaceutical Company Limited Compuestos de dihidropirrolonaftiridinona como inhibidores de JAK
EP2338888A1 (en) * 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
SA111320200B1 (ar) 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
UY33213A (es) * 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
WO2011137022A1 (en) * 2010-04-27 2011-11-03 Merck Sharp & Dohme Corp. Azaindoles as janus kinase inhibitors
JP6086326B2 (ja) 2010-05-24 2017-03-01 ユニヴァーシティー オブ ロチェスター 二環式ヘテロアリールキナーゼ阻害剤および使用方法
WO2012054364A2 (en) * 2010-10-22 2012-04-26 Merck Sharp & Dohme Corp. Bicyclic diamines as janus kinase inhibitors
DE102010049877A1 (de) 2010-11-01 2012-05-03 Merck Patent Gmbh 7-((1,2,3)Triazol-4-yl)-pyrrolo(2,3) pyrazinderivate
KR101905927B1 (ko) 2010-11-17 2018-10-08 이도르시아 파마슈티컬스 리미티드 가교된 스피로[2.4]헵탄 에스테르 유도체
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
DE102010053347A1 (de) * 2010-12-03 2012-06-06 Merck Patent Gmbh 3-Hetaryl-substituierte Pyrrolo[2,3-b] pyridin-derivative als PDK1-Inhibitoren
DE102011008352A1 (de) 2011-01-12 2012-07-12 Merck Patent Gmbh 5-([1,2,3]Triazol-4-yl)-7H-pyrrolo-[2,3-d]pyrimidinderivate
DE102011009961A1 (de) 2011-02-01 2012-08-02 Merck Patent Gmbh 7-Azaindolderivate
CN103547580B (zh) 2011-03-22 2016-12-07 阿迪维纳斯疗法有限公司 取代的稠合三环化合物、其组合物及医药用途
DE102011105469A1 (de) * 2011-06-24 2012-12-27 Merck Patent Gmbh 7-Azaindolderivate
EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
DE102011119127A1 (de) 2011-11-22 2013-05-23 Merck Patent Gmbh 3-Cyanaryl-1H-pyrrolo[2.3-b]pyridin-Derivate
PT2796460T (pt) 2011-12-21 2018-11-05 Shanghai hengrui pharmaceutical co ltd Derivado pirrole de anel heteroarilo de seis membros, método de preparação do mesmo e suas utilizações médicas
JP6280546B2 (ja) 2012-06-26 2018-02-14 デル マー ファーマシューティカルズ ジアンヒドロガラクチトール、ジアセチルジアンヒドロガラクチトール、ジブロモズルシトール、又はこれらの類似体若しくは誘導体を用いた、遺伝子多型又はahi1の調節不全若しくは変異を有する患者におけるチロシンキナーゼインヒビター抵抗性悪性腫瘍を処置するための方法
WO2014013014A1 (en) 2012-07-18 2014-01-23 Fundació Privada Centre De Regulació Genòmica (Crg) Jak inhibitors for activation of epidermal stem cell populations
US9593115B2 (en) 2012-09-21 2017-03-14 Advinus Therapeutics Ltd. Substituted fused tricyclic compounds, compositions, and medicinal applications thereof
DE102012019369A1 (de) 2012-10-02 2014-04-03 Merck Patent Gmbh 7-Azaindolderivat
CN104884059B (zh) 2012-11-30 2018-08-10 罗切斯特大学 用于hiv/aids治疗的混合谱系激酶抑制剂
KR20160061911A (ko) 2013-04-08 2016-06-01 데니스 엠. 브라운 최적하 투여된 화학 화합물의 치료 효과
WO2015131080A1 (en) 2014-02-28 2015-09-03 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
TWI788655B (zh) 2015-02-27 2023-01-01 美商林伯士拉克許米公司 酪胺酸蛋白質激酶2(tyk2)抑制劑及其用途
TWI707852B (zh) * 2015-09-02 2020-10-21 美商林伯士拉克許米公司 Tyk2 抑制劑及其用途
MX388591B (es) 2016-06-30 2025-03-20 Daewoong Pharmaceutical Co Ltd Derivados de pirazolopirimidina como inhibidor de cinasa.
WO2018041989A1 (en) 2016-09-02 2018-03-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for diagnosing and treating refractory celiac disease type 2
KR20190084299A (ko) * 2016-11-23 2019-07-16 지앙수 헨그루이 메디슨 컴퍼니 리미티드 피롤로 6-원 헤테로방향족 고리 유도체의 제조 방법 및 그의 중간체
WO2018134352A1 (en) * 2017-01-20 2018-07-26 Leo Pharma A/S Bicyclic amines as novel jak kinase inhibitors
BR112020018094A2 (pt) 2018-03-08 2020-12-22 Incyte Corporation Compostos de aminopirazina diol como inibidores de pi3k-¿
AR117398A1 (es) * 2018-03-12 2021-08-04 Abbvie Inc Inhibidores de la señalización mediada por tirosina cinasa 2
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
EP3947737A2 (en) 2019-04-02 2022-02-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
SG11202110714VA (en) * 2019-04-09 2021-10-28 Plexxikon Inc Condensed azines for ep300 or cbp modulation and indications therefor
EP3955920A1 (en) 2019-04-16 2022-02-23 Institut National de la Santé et de la Recherche Médicale (INSERM) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
US20220372135A1 (en) 2019-09-27 2022-11-24 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
KR20230012539A (ko) 2020-05-13 2023-01-26 디스크 메디슨, 인크. 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체
WO2023222565A1 (en) 2022-05-16 2023-11-23 Institut National de la Santé et de la Recherche Médicale Methods for assessing the exhaustion of hematopoietic stems cells induced by chronic inflammation

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2295433A3 (en) * 2003-03-06 2011-07-06 Eisai R&D Management Co., Ltd. JNK inhibitors
ES2364340T3 (es) * 2004-03-30 2011-08-31 Vertex Pharmaceuticals Incorporated Azaindoles útiles como inhibidores de jak y otras proteína quinasas.
WO2006015123A1 (en) * 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
US7361764B2 (en) * 2004-07-27 2008-04-22 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
EP1828180A4 (en) 2004-12-08 2010-09-15 Glaxosmithkline Llc 1H-pyrrolo [2,3-BETA] PYRIDINE
US20060264442A1 (en) 2005-05-18 2006-11-23 Allergan, Inc. Methods for the treatment of ocular and neurodegenerative conditions in a mammal
UA95244C2 (ru) 2005-06-22 2011-07-25 Плексикон, Инк. Соединения и способ модулирования активности киназ, и показания для их применения
WO2007007919A2 (en) * 2005-07-14 2007-01-18 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
SG10202003901UA (en) * 2005-12-13 2020-05-28 Incyte Holdings Corp Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
EP2211620B1 (en) * 2007-10-25 2013-12-25 Merck Sharp & Dohme Corp. 3-PYRAZIN SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AS JANUS KINASE INHIBITORS FOR THE TREATMENT OF CANCER DISEASES

Also Published As

Publication number Publication date
EP2211620A4 (en) 2012-06-06
US20100210623A1 (en) 2010-08-19
WO2009054941A1 (en) 2009-04-30
JP2011500806A (ja) 2011-01-06
EP2211620B1 (en) 2013-12-25
US8183245B2 (en) 2012-05-22
AU2008317406A1 (en) 2009-04-30
EP2211620A1 (en) 2010-08-04
CA2703125A1 (en) 2009-04-30
AU2008317406B2 (en) 2013-07-18

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