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

Info

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
Authority
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
Application number
CN2008801260776A
Other languages
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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals Inc
Priority date (The priority date 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 date listed.)
Filing date
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

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EP2734205B1 (en) 2011-07-21 2018-03-21 Tolero Pharmaceuticals, Inc. Heterocyclic protein kinase inhibitors
EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
EP4556010A3 (en) 2011-11-30 2025-07-23 Emory University 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
DK3077397T3 (da) 2013-12-06 2019-12-16 Vertex Pharma 2-amino-6-fluor-n-[5-fluor-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamidforbindelse anvendelig som atr-kinase-inhibitor, dens fremstilling, forskellige faste former og radiomarkerede derivater deraf
WO2017013270A1 (en) 2015-07-23 2017-01-26 Universite De Strasbourg Use of leptin signaling inhibitor for protecting kidneys from patients having ciliopathy
HK1258570A1 (zh) 2015-09-30 2019-11-15 Vertex Pharmaceuticals Inc. 使用dna损伤剂及atr抑制剂的组合治疗癌症的方法
CN117838695A (zh) 2018-04-13 2024-04-09 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
NZ778055A (en) 2019-02-12 2025-11-28 Sumitomo Pharma America Inc Formulations comprising heterocyclic protein kinase inhibitors
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
EP4598539A2 (en) * 2022-10-04 2025-08-13 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
IL127566A0 (en) 1996-08-28 1999-10-28 Pfizer Substituted 6,5-hetero- bicyclic derivatives
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
DK1532145T3 (da) 2002-08-02 2007-01-15 Vertex Pharma Pyrazolpræparater der er anvendelige som inhibitorer af GSK-3
US7550470B2 (en) 2002-12-11 2009-06-23 Merck & Co. Inc. Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors
US7226919B2 (en) * 2002-12-18 2007-06-05 Vertex Pharmaceuticals Inc. Compositions useful as inhibitors of protein kinases
NZ546058A (en) * 2004-01-12 2010-09-30 Ym Biosciences Australia Pty Benzimidazole and other fused ring derivatives as selective janus kinase inhibitors
TWI372624B (en) * 2004-03-30 2012-09-21 Vertex Pharma Azaindoles useful as inhibitors of jak and other protein kinases
GB0519957D0 (en) 2005-09-30 2005-11-09 Sb Pharmco Inc Chemical compound
ATE482213T1 (de) * 2004-11-04 2010-10-15 Vertex Pharma Als inhibitoren von proteinkinasen geeignete pyrazoloä1,5-aüpyrimidine
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
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
ATE526328T1 (de) * 2007-03-09 2011-10-15 Vertex Pharma Als inhibitoren von proteinkinasen geeignete aminopyrimidine
CN101790532B (zh) 2007-07-31 2013-11-20 沃泰克斯药物股份有限公司 5-氟-1H-吡唑并[3,4-b]吡啶-3-胺及其衍生物的制备方法

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

Similar Documents

Publication Publication Date Title
CN101932583A (zh) 用作JAK2抑制剂的吡唑并[1,5-a]嘧啶类
TWI858008B (zh) 免疫調節劑、藥物組合物及其應用
CN101228161B (zh) 适用作蛋白激酶抑制剂的吡咯并吡啶类
AU2009281822B2 (en) cMET inhibitors
JP5144532B2 (ja) c−Met阻害剤及び用法
WO2007117494A1 (en) Deazapurines useful as inhibitors of janus kinases
WO2022237676A1 (zh) Shp2磷酸酶抑制剂的制备及其应用
CN101094853A (zh) 可用作蛋白激酶抑制剂的吡唑并[1,5-a]嘧啶
EP1931674A2 (en) Deazapurines useful as inhibitors of janus kinases
CN101142218A (zh) 可用作蛋白激酶抑制剂的吡咯并嘧啶
CN105473573B (zh) 用作激酶抑制剂的咔唑甲酰胺化合物
WO2018090869A1 (zh) 酰胺衍生物及其在药物中的应用
JP2010508363A (ja) ヤヌスキナーゼの阻害剤として有用な三環系ヘテロアリール化合物
CN101778825A (zh) 适用作詹纳斯激酶抑制剂的n-杂环类化合物
CN101796056A (zh) c-MET的杂环抑制剂及其用途
RU2415853C2 (ru) Бензимидазолы, применимые в качестве ингибиторов протеинкиназ
HK1147093A (en) Pyrazolo [1,5-a] pyrimidines useful as jak2 inhibitors
HK40087540A (zh) 免疫调节剂及其组合物和应用
MX2008004335A (en) Deazapurines useful as inhibitors of janus kinases

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1147093

Country of ref document: HK

C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20101229

REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1147093

Country of ref document: HK