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PE20090210A1 - COMPOUNDS DERIVED FROM PYRAZOLO PYRIMIDINE AS INHIBITORS OF JAK QUINASE - Google Patents

COMPOUNDS DERIVED FROM PYRAZOLO PYRIMIDINE AS INHIBITORS OF JAK QUINASE

Info

Publication number
PE20090210A1
PE20090210A1 PE2008000710A PE2008000710A PE20090210A1 PE 20090210 A1 PE20090210 A1 PE 20090210A1 PE 2008000710 A PE2008000710 A PE 2008000710A PE 2008000710 A PE2008000710 A PE 2008000710A PE 20090210 A1 PE20090210 A1 PE 20090210A1
Authority
PE
Peru
Prior art keywords
alkyl
carbocyclyl
jak
pyrimidin
fluoro
Prior art date
Application number
PE2008000710A
Other languages
Spanish (es)
Inventor
Huiping Guan
Barry Raymond Hayter
Shan Huang
Stephanos Ioannidis
Jeffrey Johannes
Michelle Lamb
Bo Peng
Bin Yang
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of PE20090210A1 publication Critical patent/PE20090210A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA I, DONDE; EL ANILLO A ES FENILO Y HETEROCICLILO DE 6 MIEMBROS; X ES -NH-, -O-, -S-; R1 ES H, -CN, (C1-C6)ALQUILO, CARBOCICLILO DE 3 A 5 MIEMBROS, -N(R1a)C(O)R1b, ENTRE OTROS; R1a ES (C1-C6)ALQUILO, CARBOCICLILO DE 3 A 5 MIEMBROS, ENTRE OTROS; R1b ES (C2-C6)ALQUENILO, HETEROCICLILO DE 5 MIEMBROS, (C1-C6)ALQUILO, ENTRE OTROS; R2 ES HALO, (C2-C6)ALQUENILO, -OC(O)N(R2a)2, ENTRE OTROS; R2a ES H, (C1-C6)ALQUILO, CARBOCICLILO, ENTRE OTROS; R2 ES-CN, -OR2a, -N(R2a)N(R2a)2, ENTRE OTROS; R3 ES HALO, (C1-C6)ALQUILO, C(R3a)=N(OR3a), ENTRE OTROS; R3a ES H, (C1-C6)ALQUILO, CARBOCICLILO, ENTRE OTROS; R4 ES (C1-C6)ALQUILO, -NO2, -N(R4a)C(O)N(R4a)2; R4a ES (C1-C6)ALQUILO, CARBOCICLILO, H, ENTRE OTROS. SON SELECCIONADOS 5-FLUORO-N4-[(S)-1-(5-FLUORO-PIRIMIDIN-2-IL)-ETIL]-N2-(5-METOXI-1H-PIRAZOL-3-IL)-6-MORFOLIN-4-IL-PIRIMIDIN-2,4-DIAMINA, 1-(5-FLUORO-6-(1-(5-FLUOROPIRIMIDIN-2-IL)ETOXI)-2-(5-METIL-1H-PIRAZOL-3-ILAMINO)PIRIMIDIN-4-IL)PIPERIDIN-4-CARBONITRILO, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCESO DE PREPARACION Y COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS TIENEN ACTIVIDAD INHIBIDORA JAK QUINASA Y SON UTILES EN EL TRATAMIENTO DE DESORDENES MIELOPROLIFERATIVOS Y CANCERREFERS TO COMPOUNDS OF FORMULA I, WHERE; RING A IS PHENYL AND HETEROCYCLYL OF 6 MEMBERS; X IS -NH-, -O-, -S-; R1 IS H, -CN, (C1-C6) ALKYL, 3 TO 5-MEMBER CARBOCYCLYL, -N (R1a) C (O) R1b, AMONG OTHERS; R1a IS (C1-C6) ALKYL, CARBOCYCLYL OF 3 TO 5 MEMBERS, AMONG OTHERS; R1b IS (C2-C6) ALKENYL, 5-MEMBER HETEROCYCLYL, (C1-C6) ALKYL, AMONG OTHERS; R2 IS HALO, (C2-C6) ALKENYL, -OC (O) N (R2a) 2, AMONG OTHERS; R2a IS H, (C1-C6) ALKYL, CARBOCYCLYL, AMONG OTHERS; R2 IS-CN, -OR2a, -N (R2a) N (R2a) 2, AMONG OTHERS; R3 IS HALO, (C1-C6) ALKYL, C (R3a) = N (OR3a), AMONG OTHERS; R3a IS H, (C1-C6) ALKYL, CARBOCYCLYL, AMONG OTHERS; R4 IS (C1-C6) ALKYL, -NO2, -N (R4a) C (O) N (R4a) 2; R4a IS (C1-C6) ALKYL, CARBOCYCLYL, H, AMONG OTHERS. 5-FLUORO-N4 - [(S) -1- (5-FLUORO-PYRIMIDIN-2-IL) -ETHYL] -N2- (5-METOXY-1H-PIRAZOL-3-IL) -6-MORFOLIN- 4-IL-PYRIMIDIN-2,4-DIAMINE, 1- (5-FLUORO-6- (1- (5-FLUOROPYRIMIDIN-2-IL) ETHOXY) -2- (5-METHYL-1H-PYRAZOLE-3-ILAMINE ) PYRIMIDIN-4-IL) PIPERIDIN-4-CARBONITRILE, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL PREPARATION AND COMPOSITION PROCESS. SUCH COMPOUNDS HAVE JAK KINASE INHIBITOR ACTIVITY AND ARE USEFUL IN THE TREATMENT OF MYELOPROLIFERATIVE DISORDERS AND CANCER

PE2008000710A 2007-04-25 2008-04-25 COMPOUNDS DERIVED FROM PYRAZOLO PYRIMIDINE AS INHIBITORS OF JAK QUINASE PE20090210A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US91401707P 2007-04-25 2007-04-25

Publications (1)

Publication Number Publication Date
PE20090210A1 true PE20090210A1 (en) 2009-04-01

Family

ID=39618922

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008000710A PE20090210A1 (en) 2007-04-25 2008-04-25 COMPOUNDS DERIVED FROM PYRAZOLO PYRIMIDINE AS INHIBITORS OF JAK QUINASE

Country Status (5)

Country Link
AR (1) AR066147A1 (en)
PE (1) PE20090210A1 (en)
TW (1) TW200846344A (en)
UY (1) UY31048A1 (en)
WO (1) WO2008132502A1 (en)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2012014158A (en) 2010-06-04 2013-02-07 Hoffmann La Roche Aminopyrimidine derivatives as lrrk2 modulators.
ES2653967T3 (en) 2010-11-10 2018-02-09 Genentech, Inc. Pyrazole aminopyrimidine derivatives as modulators of LRRK2
ITMI20110472A1 (en) * 2011-03-24 2012-09-25 Erregierre Spa PROCEDURE FOR THE PREPARATION OF ZILEUTON AT HIGH PURITY
AU2012288892B2 (en) * 2011-07-28 2016-04-21 Cellzome Limited Heterocyclyl pyrimidine analogues as JAK inhibitors
EP2554544A1 (en) * 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
ES2633793T3 (en) * 2011-09-22 2017-09-25 Merck Sharp & Dohme Corp. Pyrazole carboxamides as Janus kinase inhibitors
CA2875990A1 (en) * 2012-05-24 2013-11-28 Cellzome Limited Heterocyclyl pyrimidine analogues as tyk2 inhibitors
KR20220143164A (en) 2012-11-21 2022-10-24 피티씨 테라퓨틱스, 인크. Substituted reverse pyrimidine bmi-1 inhibitors
CA2922657C (en) 2013-08-30 2022-04-12 Ptc Therapeutics, Inc. Substituted pyrimidine bmi-1 inhibitors
US10584115B2 (en) 2013-11-21 2020-03-10 Ptc Therapeutics, Inc. Substituted pyridine and pyrazine BMI-1 inhibitors
EP3359154B1 (en) * 2015-10-08 2021-05-26 Suzhou Yunxuan Yiyao Keji Youxian Gongsi Wnt signaling pathway inhibitors and therapeutic applications thereof
CN105254613A (en) * 2015-10-08 2016-01-20 苏州云轩医药科技有限公司 Heterocyclic compound with Wnt signal path inhibitory activity and application thereof
WO2018112843A1 (en) * 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. Heteroaryl piperidine ether allosteric modulators of the m4 muscarinic acetylcholine receptor
KR20210029790A (en) * 2018-07-05 2021-03-16 메이오 파운데이션 포 메디칼 에쥬케이션 앤드 리써치 PIKfyve inhibitor
BR112021002630A2 (en) 2018-08-17 2021-05-11 Ptc Therapeutics, Inc. method to treat pancreatic cancer
KR20220088699A (en) 2019-09-27 2022-06-28 디스크 메디슨, 인크. Methods of treating myelofibrosis and related conditions
MX2022008627A (en) 2020-01-13 2022-11-08 Verge Analytics Inc PYRAZOLO-SUBSTITUTED PYRIMIDINES AND USES THEREOF.
KR20230012539A (en) 2020-05-13 2023-01-26 디스크 메디슨, 인크. Anti-hemojuvelin (HJV) antibodies to treat myelofibrosis
CN111454214B (en) * 2020-05-27 2023-04-07 龙曦宁（上海）医药科技有限公司 Synthetic method of 2-methoxy-1-pyrimidineethylamine hydrochloride
IL309892A (en) * 2021-07-01 2024-03-01 Aerie Pharmaceuticals Inc Azatidinylpyrimidine-type substances, preparations containing them and their use
AU2023298142A1 (en) * 2022-06-29 2025-01-09 Alcon Inc. Azetidinyl pyrimidines and uses thereof as jak inhibitors
TW202409017A (en) 2022-08-24 2024-03-01 大陸商江蘇恆瑞醫藥股份有限公司 Heterocyclic compounds, preparation method and medical use thereof

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY141220A (en) * 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
JP2008540391A (en) * 2005-05-05 2008-11-20 アストラゼネカ アクチボラグ Pyrazolylamino substituted pyrimidines and their use in the treatment of cancer
AU2006248780B2 (en) * 2005-05-16 2010-06-03 Astrazeneca Ab Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors

Also Published As

Publication number Publication date
AR066147A1 (en) 2009-07-29
TW200846344A (en) 2008-12-01
WO2008132502A1 (en) 2008-11-06
UY31048A1 (en) 2008-11-28

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