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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Expired - Fee Related legal-status Critical Current
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (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
US8183245B2 (en) * 2007-10-25 2012-05-22 Merck Sharp & Dohme Corp. Pyrazine substituted pyrrolopyridines as inhibitors of JAK and PDK1
ES2378513T3 (es) * 2008-08-06 2012-04-13 Pfizer Inc. Compuestos 2-heterociclilamino piracinas sustituidas en posición 6 como inhibidores de CHK-1
CA2744498C (en) 2008-11-25 2017-10-24 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
US20130040933A1 (en) * 2010-04-27 2013-02-14 Brandon Cash Azaindoles as janus kinase inhibitors
AU2011258465B2 (en) 2010-05-24 2016-12-15 University Of Rochester Bicyclic heteroaryl kinase inhibitors and methods of use
EP2629777B1 (en) * 2010-10-22 2018-12-19 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
CN103221392B (zh) 2010-11-17 2015-06-03 埃科特莱茵药品有限公司 桥联螺[2.4]庚酯衍生物
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
WO2012127506A1 (en) 2011-03-22 2012-09-27 Advinus Therapeutics Limited Substituted fused tricyclic compounds, compositions and medicinal applications thereof
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
KR102032934B1 (ko) 2011-12-21 2019-10-16 지앙수 헨그루이 메디슨 컴퍼니 리미티드 피롤 6원 헤테로아릴 고리 유도체, 그의 제조 방법, 및 그의 의약 용도
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
IN2015DN02008A (https=) 2012-09-21 2015-08-14 Advinus Therapeutics Ltd
DE102012019369A1 (de) 2012-10-02 2014-04-03 Merck Patent Gmbh 7-Azaindolderivat
EP2925319B1 (en) 2012-11-30 2019-01-09 University Of Rochester Mixed lineage kinase inhibitors for hiv/aids therapies
EP2983674A4 (en) 2013-04-08 2017-05-10 Dennis M. Brown Therapeutic benefit of suboptimally administered chemical compounds
WO2015131080A1 (en) * 2014-02-28 2015-09-03 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
EP3262049B1 (en) 2015-02-27 2022-07-20 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
EP4327809A3 (en) * 2015-09-02 2024-04-17 Takeda Pharmaceutical Company Limited Tyk2 inhibitors and uses thereof
RU2714206C1 (ru) 2016-06-30 2020-02-13 Даевунг Фармасьютикал Ко., Лтд. Пиразолопиримидиновые производные в качестве ингибитора киназы
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
MX391179B (es) * 2016-11-23 2025-03-21 Jiangsu Hengrui Medicine Co Método de preparación e intermediario de derivado de un anillo heteroaromático de seis miembros pirrolo
CN110291090A (zh) * 2017-01-20 2019-09-27 利奥制药有限公司 作为新型jak激酶抑制剂的双环胺
BR112020018094A2 (pt) 2018-03-08 2020-12-22 Incyte Corporation Compostos de aminopirazina diol como inibidores de pi3k-¿
AU2019234574A1 (en) * 2018-03-12 2020-09-03 Abbvie Inc. Inhibitors of tyrosine kinase 2 mediated signaling
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
JP2022527972A (ja) 2019-04-02 2022-06-07 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル 前悪性病変を有する患者において癌を予測及び予防する方法
KR20220018475A (ko) * 2019-04-09 2022-02-15 플렉시콘 인코퍼레이티드 Ep300 또는 cbp 조절 및 이의 표시를 위한 응축 아진
US20220202820A1 (en) 2019-04-16 2022-06-30 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
CN114761013A (zh) 2019-09-27 2022-07-15 迪斯克医药公司 治疗骨髓纤维化和相关病症的方法
WO2021231798A1 (en) 2020-05-13 2021-11-18 Disc Medicine, Inc. Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis
EP4526469A1 (en) 2022-05-16 2025-03-26 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
JP4787150B2 (ja) * 2003-03-06 2011-10-05 エーザイ・アール・アンド・ディー・マネジメント株式会社 Ｊｎｋ阻害剤
TWI372624B (en) * 2004-03-30 2012-09-21 Vertex Pharma Azaindoles useful as inhibitors of jak and other protein kinases
EP1781654A1 (en) * 2004-07-27 2007-05-09 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
CN102206216B (zh) 2005-06-22 2014-11-12 普莱希科公司 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物
WO2007007919A2 (en) * 2005-07-14 2007-01-18 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
EP2455382B1 (en) * 2005-12-13 2016-10-26 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
US8183245B2 (en) * 2007-10-25 2012-05-22 Merck Sharp & Dohme Corp. Pyrazine substituted pyrrolopyridines as inhibitors of JAK and PDK1

Also Published As

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

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