CN101932583A - 用作JAK2抑制剂的吡唑并[1,5-a]嘧啶类 - Google Patents

用作JAK2抑制剂的吡唑并[1,5-a]嘧啶类 Download PDF

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Publication number
CN101932583A
CN101932583A CN2008801260776A CN200880126077A CN101932583A CN 101932583 A CN101932583 A CN 101932583A CN 2008801260776 A CN2008801260776 A CN 2008801260776A CN 200880126077 A CN200880126077 A CN 200880126077A CN 101932583 A CN101932583 A CN 101932583A
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CN
China
Prior art keywords
group
unit
compound
aliphatic group
nhc
Prior art date
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.)
Pending
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CN2008801260776A
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English (en)
Chinese (zh)
Inventor
M·莱德博尔
M·斯图尔特
D·梅瑟史密斯
J·达菲
G·马丁内斯-博特利亚
J·科姆
高淮
F·萨里图罗
V·马罗内
A·皮尔斯
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Publication date
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of CN101932583A publication Critical patent/CN101932583A/zh
Pending legal-status Critical Current

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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)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (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)
CN2008801260776A 2007-12-19 2008-12-18 用作JAK2抑制剂的吡唑并[1,5-a]嘧啶类 Pending CN101932583A (zh)

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 (1)

Publication Number Publication Date
CN101932583A true CN101932583A (zh) 2010-12-29

Family

ID=40431839

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2008801260776A Pending CN101932583A (zh) 2007-12-19 2008-12-18 用作JAK2抑制剂的吡唑并[1,5-a]嘧啶类

Country Status (13)

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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102887858A (zh) * 2012-09-07 2013-01-23 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

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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
WO2012044561A2 (en) * 2010-09-30 2012-04-05 Merck Sharp & Dohme Corp. 2-alkoxy pyrimidine pde10 inhibitors
EP2463289A1 (en) 2010-11-26 2012-06-13 Almirall, S.A. Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors
EP3812387A1 (en) 2011-07-21 2021-04-28 Sumitomo Dainippon Pharma Oncology, Inc. Heterocyclic protein kinase inhibitors
EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
ES3018133T3 (en) 2011-11-30 2025-05-14 Univ Emory Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae
SI2941432T1 (en) 2012-12-07 2018-07-31 Vertex Pharmaceuticals Incorporated 2-AMINO-6-FLUORO-N- (5-FLUORO-4- (4- (4- (OXETHAN-3-YL) PIPERAZIN-1-CARBONYL) PIPERIDIN-1-YLIPRIDIN-3-YL) 1,5 ALFA) PYRIMIDINE-3-CARBOXAMIDE AS ATR KINAZE INHIBITOR
PT3077397T (pt) * 2013-12-06 2020-01-22 Vertex Pharma Composto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-carboxamida útil como inibidor da atr quinase, a sua preparação, diferentes formas sólidas e derivados radiomarcados do mesmo
WO2017013270A1 (en) 2015-07-23 2017-01-26 Universite De Strasbourg Use of leptin signaling inhibitor for protecting kidneys from patients having ciliopathy
AU2016331955B2 (en) 2015-09-30 2022-07-21 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors
JP2021521170A (ja) 2018-04-13 2021-08-26 スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド 骨髄増殖性新生物およびがんに関連する線維症の処置のためのｐｉｍキナーゼ阻害剤
KR20260008165A (ko) 2019-02-12 2026-01-15 스미토모 파마 아메리카, 인크. 헤테로시클릭 단백질 키나제 억제제를 포함하는 제제
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
EP4598539A2 (en) * 2022-10-04 2025-08-13 Children's Hospital Medical Center Multi-cyclic irak and flt3 inhibiting compounds and uses thereof
CN120302975A (zh) 2022-10-31 2025-07-11 住友制药美国公司 治疗骨髓增生性肿瘤的pim1抑制剂

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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
JP3621706B2 (ja) 1996-08-28 2005-02-16 ファイザー・インク 置換された６，５―ヘテロ―二環式誘導体
JP2002501532A (ja) 1997-05-30 2002-01-15 メルク エンド カンパニー インコーポレーテッド 新規血管形成阻害薬
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
CN1319968C (zh) 2002-08-02 2007-06-06 沃泰克斯药物股份有限公司 用作gsk－3的抑制剂的吡唑组合物
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
DK1704145T3 (da) * 2004-01-12 2012-09-24 Ym Biosciences Australia Pty Selektive kinaseinhibitorer
ES2364340T3 (es) * 2004-03-30 2011-08-31 Vertex Pharmaceuticals Incorporated Azaindoles útiles como inhibidores de jak y otras proteína quinasas.
GB0519957D0 (en) 2005-09-30 2005-11-09 Sb Pharmco Inc Chemical compound
PT1812440E (pt) * 2004-11-04 2011-01-25 Vertex Pharma Pirazolo[1,5-a]pirimidinas úteis enquanto inibidores de proteínas cinases
WO2007017678A1 (en) 2005-08-09 2007-02-15 Eirx Therapeutics Limited Pyrazolo[1,5-a] pyrimidine compounds and pharmaceutical compositions containing them
ZA200802685B (en) * 2005-09-30 2009-10-28 Vertex Pharma Deazapurines useful as inhibitors of janus kinases
US8513276B2 (en) * 2006-12-22 2013-08-20 Astex Therapeutics Limited Imidazo[1,2-a]pyridine compounds for use in treating cancer
EP2137183B1 (en) * 2007-03-09 2011-09-28 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

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102887858A (zh) * 2012-09-07 2013-01-23 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
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

Also Published As

Publication number Publication date
US8937064B2 (en) 2015-01-20
US20110118255A1 (en) 2011-05-19
EP2252618A1 (en) 2010-11-24
WO2009085913A1 (en) 2009-07-09
ZA201004368B (en) 2013-01-30
NZ586662A (en) 2012-08-31
MX2010006748A (es) 2010-08-18
JP2011507881A (ja) 2011-03-10
RU2010129928A (ru) 2012-01-27
AU2008343173A1 (en) 2009-07-09
CA2709710A1 (en) 2009-07-09
IL206466A0 (en) 2010-12-30
KR20100108390A (ko) 2010-10-06
JP5587206B2 (ja) 2014-09-10

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