JP5587206B2 - ＪＡＫ２阻害剤として有用なピラゾロ［１，５−ａ］ピリミジン - Google Patents

ＪＡＫ２阻害剤として有用なピラゾロ［１，５−ａ］ピリミジン Download PDF

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Publication number
JP5587206B2
JP5587206B2 JP2010539781A JP2010539781A JP5587206B2 JP 5587206 B2 JP5587206 B2 JP 5587206B2 JP 2010539781 A JP2010539781 A JP 2010539781A JP 2010539781 A JP2010539781 A JP 2010539781A JP 5587206 B2 JP5587206 B2 JP 5587206B2
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Japan
Prior art keywords
aliphatic
ring
membered
nhc
compound
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JP2010539781A
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English (en)
Japanese (ja)
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JP2011507881A5 (enExample
JP2011507881A (ja
Inventor
マーク レデボアー，
マイケル スチュワート，
デイビッド メッサースミス，
ジョン ダッフィー，
ガブリエル マルチネス−ボテッラ，
ジョン カム，
ファイ ガオ，
フランチェスコ サリトゥロ，
バレリー マロン，
アルバート ピアース，
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2010539781A 2007-12-19 2008-12-18 ＪＡＫ２阻害剤として有用なピラゾロ［１，５−ａ］ピリミジン Expired - Fee Related JP5587206B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US1482407P 2007-12-19 2007-12-19
US61/014,824 2007-12-19
PCT/US2008/087362 WO2009085913A1 (en) 2007-12-19 2008-12-18 PYRAZOLO [1,5-a] PYRIMIDINES USEFUL AS JAK2 INHIBITORS

Publications (3)

Publication Number Publication Date
JP2011507881A JP2011507881A (ja) 2011-03-10
JP2011507881A5 JP2011507881A5 (enExample) 2013-01-31
JP5587206B2 true JP5587206B2 (ja) 2014-09-10

Family

ID=40431839

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2010539781A Expired - Fee Related JP5587206B2 (ja) 2007-12-19 2008-12-18 ＪＡＫ２阻害剤として有用なピラゾロ［１，５−ａ］ピリミジン

Country Status (13)

Country Link
US (1) US8937064B2 (enExample)
EP (1) EP2252618A1 (enExample)
JP (1) JP5587206B2 (enExample)
KR (1) KR20100108390A (enExample)
CN (1) CN101932583A (enExample)
AU (1) AU2008343173A1 (enExample)
CA (1) CA2709710A1 (enExample)
IL (1) IL206466A0 (enExample)
MX (1) MX2010006748A (enExample)
NZ (1) NZ586662A (enExample)
RU (1) RU2010129928A (enExample)
WO (1) WO2009085913A1 (enExample)
ZA (1) ZA201004368B (enExample)

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AR077999A1 (es) * 2009-09-02 2011-10-05 Vifor Int Ag Antagonistas de pirimidin y triazin-hepcidina
EP2338888A1 (en) * 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
UY33213A (es) * 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
US8785467B2 (en) * 2010-09-30 2014-07-22 Merck Sharp & Dohme Corp. Alkoxy pyrimidine PDE10 inhibitors
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
JP6105578B2 (ja) 2011-07-21 2017-03-29 トレロ ファーマシューティカルズ， インコーポレイテッド 複素環式プロテインキナーゼ阻害剤
EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
CA2856722C (en) 2011-11-30 2022-11-22 Emory University Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections
CN102887858B (zh) * 2012-09-07 2014-11-19 苏州康润医药有限公司 3-氯-5-氨基-1h-吡唑-4-甲酸乙酯的合成方法
CN103073549A (zh) * 2012-09-07 2013-05-01 苏州康润医药有限公司 3-溴吡唑啉[1,5-α]吡嘧啶-2-甲酸的合成工艺
SMT202000713T1 (it) 2012-12-07 2021-03-15 Vertex Pharma Pirazolo [1,5-a] pirimidine utili come inibitori dell'atr chinasi per il trattamento di malattie del cancro
ES2768678T3 (es) 2013-12-06 2020-06-23 Vertex Pharma Compuesto de 2-amino-6-fluoro-N-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-carboxamida útil como inhibidor de la ATR quinasa, su preparación, diferentes formas sólidas y derivados radiomarcados de las mismas
WO2017013270A1 (en) 2015-07-23 2017-01-26 Universite De Strasbourg Use of leptin signaling inhibitor for protecting kidneys from patients having ciliopathy
RU2768621C1 (ru) 2015-09-30 2022-03-24 Вертекс Фармасьютикалз Инкорпорейтед Способ лечения рака с использованием комбинации повреждающих днк средств и ингибиторов atr
CN112236139A (zh) 2018-04-13 2021-01-15 大日本住友制药肿瘤公司 用于治疗骨髓增殖性肿瘤和与癌症相关的纤维化的pim激酶抑制剂
JP7662528B2 (ja) 2019-02-12 2025-04-15 スミトモ ファーマ アメリカ， インコーポレイテッド 複素環式タンパク質キナーゼ阻害剤を含む製剤
KR20220088699A (ko) 2019-09-27 2022-06-28 디스크 메디슨, 인크. 골수섬유증 및 관련 상태의 치료 방법
JP2023528223A (ja) 2020-05-13 2023-07-04 ディスク・メディシン・インコーポレイテッド 骨髄線維症を処置するための抗ヘモジュベリン（ｈｊｖ）抗体
WO2024076614A2 (en) * 2022-10-04 2024-04-11 Children's Hospital Medical Center Multi-cyclic irak and flt3 inhibiting compounds and uses thereof
EP4611753A1 (en) 2022-10-31 2025-09-10 Sumitomo Pharma America, Inc. Pim1 inhibitor for treating myeloproliferative neoplasms

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
US5886026A (en) 1993-07-19 1999-03-23 Angiotech Pharmaceuticals Inc. Anti-angiogenic compositions and methods of use
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
BR9711970A (pt) 1996-08-28 1999-08-24 Pfizer Derivados 6,5-substitu¡do-heterobic¡clicos
CA2291709A1 (en) 1997-05-30 1998-12-03 Merck & Co., Inc. Novel angiogenesis inhibitors
US6245759B1 (en) 1999-03-11 2001-06-12 Merck & Co., Inc. Tyrosine kinase inhibitors
US7713989B2 (en) 2000-04-27 2010-05-11 Dow Robert L Glucocorticoid receptor modulators
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
ATE339419T1 (de) 2002-08-02 2006-10-15 Vertex Pharma Pyrazolenthaltende zusammensetzungen und ihre verwendung als gsk-3 inhibitoren
US7550470B2 (en) 2002-12-11 2009-06-23 Merck & Co. Inc. Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors
DE60326646D1 (de) 2002-12-18 2009-04-23 Vertex Pharma Benzisoxazolderivate, die sich als inhibitoren von proteinkinasen eigen
GB2432834A (en) * 2004-01-12 2007-06-06 Cytopia Res Pty Ltd Selective Kinase Inhibitors
EP2332940B1 (en) * 2004-03-30 2012-10-31 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of JAK and other protein kinases
GB0519957D0 (en) 2005-09-30 2005-11-09 Sb Pharmco Inc Chemical compound
DK1812440T3 (da) * 2004-11-04 2011-01-31 Vertex Pharma Pyrazolo[1,5-a]pyrimidiner, der kan anvendes som inhibistorer af proteinkinaser
EP1922321A1 (en) 2005-08-09 2008-05-21 Eirx Therapeutics Ltd Pyrazoloý1,5-a¨pyrimidine compounds and pharmaceutical compositions containing them
CN101801971A (zh) * 2005-09-30 2010-08-11 沃泰克斯药物股份有限公司 可用作janus激酶抑制剂的脱氮嘌呤
CN101679409B (zh) * 2006-12-22 2014-11-26 Astex治疗学有限公司 双环杂环衍生化合物、其医药组合物和其用途
AU2008226466B2 (en) 2007-03-09 2013-06-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
NZ582879A (en) 2007-07-31 2012-03-30 Vertex Pharma Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof

Also Published As

Publication number Publication date
CN101932583A (zh) 2010-12-29
RU2010129928A (ru) 2012-01-27
IL206466A0 (en) 2010-12-30
AU2008343173A1 (en) 2009-07-09
ZA201004368B (en) 2013-01-30
NZ586662A (en) 2012-08-31
MX2010006748A (es) 2010-08-18
US8937064B2 (en) 2015-01-20
CA2709710A1 (en) 2009-07-09
EP2252618A1 (en) 2010-11-24
US20110118255A1 (en) 2011-05-19
JP2011507881A (ja) 2011-03-10
KR20100108390A (ko) 2010-10-06
WO2009085913A1 (en) 2009-07-09

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