CA2497450C - Pyrazolopyrimidines as cyclin dependent kinase inhibitors - Google Patents

Pyrazolopyrimidines as cyclin dependent kinase inhibitors Download PDF

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Publication number
CA2497450C
CA2497450C CA2497450A CA2497450A CA2497450C CA 2497450 C CA2497450 C CA 2497450C CA 2497450 A CA2497450 A CA 2497450A CA 2497450 A CA2497450 A CA 2497450A CA 2497450 C CA2497450 C CA 2497450C
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CA
Canada
Prior art keywords
compound
group
pharmaceutically acceptable
solvate
acceptable salt
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.)
Expired - Fee Related
Application number
CA2497450A
Other languages
English (en)
French (fr)
Other versions
CA2497450A1 (en
Inventor
Timothy J. Guzi
Kamil Paruch
Michael P. Dwyer
Ronald J. Doll
Viyyoor Moopil Girijavallabhan
Lawrence W. Dillard
Vinh D. Tran
Zhen Min He
Ray Anthony James
Haengsoon Park
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.)
Merck Sharp and Dohme LLC
Pharmacopeia LLC
Original Assignee
Pharmacopeia Inc
Schering Corp
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 Pharmacopeia Inc, Schering Corp filed Critical Pharmacopeia Inc
Publication of CA2497450A1 publication Critical patent/CA2497450A1/en
Application granted granted Critical
Publication of CA2497450C publication Critical patent/CA2497450C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2497450A 2002-09-04 2003-09-03 Pyrazolopyrimidines as cyclin dependent kinase inhibitors Expired - Fee Related CA2497450C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US40799902P 2002-09-04 2002-09-04
US60/407,999 2002-09-04
PCT/US2003/027502 WO2004022560A1 (en) 2002-09-04 2003-09-03 Pyrazolopyrimidines as cyclin dependent kinase inhibitors

Publications (2)

Publication Number Publication Date
CA2497450A1 CA2497450A1 (en) 2004-03-18
CA2497450C true CA2497450C (en) 2011-05-31

Family

ID=31978544

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2497450A Expired - Fee Related CA2497450C (en) 2002-09-04 2003-09-03 Pyrazolopyrimidines as cyclin dependent kinase inhibitors

Country Status (19)

Country Link
US (3) US7074924B2 (cg-RX-API-DMAC7.html)
EP (1) EP1534710B1 (cg-RX-API-DMAC7.html)
JP (2) JP4700344B2 (cg-RX-API-DMAC7.html)
KR (1) KR20050057139A (cg-RX-API-DMAC7.html)
CN (1) CN1701074A (cg-RX-API-DMAC7.html)
AR (1) AR041136A1 (cg-RX-API-DMAC7.html)
AT (1) ATE376548T1 (cg-RX-API-DMAC7.html)
AU (1) AU2003268385B2 (cg-RX-API-DMAC7.html)
CA (1) CA2497450C (cg-RX-API-DMAC7.html)
DE (1) DE60317077T2 (cg-RX-API-DMAC7.html)
ES (1) ES2291665T3 (cg-RX-API-DMAC7.html)
IL (1) IL167088A (cg-RX-API-DMAC7.html)
MX (1) MXPA05002570A (cg-RX-API-DMAC7.html)
MY (2) MY141978A (cg-RX-API-DMAC7.html)
NZ (1) NZ539164A (cg-RX-API-DMAC7.html)
PE (1) PE20040999A1 (cg-RX-API-DMAC7.html)
TW (1) TWI335919B (cg-RX-API-DMAC7.html)
WO (1) WO2004022560A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA200501852B (cg-RX-API-DMAC7.html)

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WO2011028638A1 (en) 2009-09-04 2011-03-10 Schering Corporation Modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors
RU2543386C2 (ru) * 2010-02-26 2015-02-27 Мицубиси Танабе Фарма Коропорейшн Производные пиразолопиримидина и их применение в качестве ингибиторов pde10
US10953012B2 (en) 2011-04-26 2021-03-23 Bioenergenix Llc Heterocyclic compounds for the inhibition of pask
EP2723746A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
US9278973B2 (en) 2012-10-25 2016-03-08 Bioenergenix Llc Heterocyclic compounds for the inhibition of PASK
US10392389B2 (en) 2012-10-25 2019-08-27 Bioenergenix Llc Heterocyclic compounds for the inhibition of PASK
EP4534538A3 (en) 2012-12-07 2025-06-11 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
MX2015011898A (es) * 2013-03-13 2016-05-05 Genentech Inc Compuestos de pirazolo y usos de los mismos.
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
US8969360B2 (en) 2013-03-15 2015-03-03 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
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CA2932757C (en) 2013-12-06 2023-10-31 Vertex Pharmaceuticals Incorporated 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof
JP2017501145A (ja) 2013-12-23 2017-01-12 ノージン ビーブイ Ccr9調節因子として有用な化合物
RU2719583C2 (ru) 2014-06-05 2020-04-21 Вертекс Фармасьютикалз Инкорпорейтед Радиоактивно меченные производные 2-амино-6-фтор-n-[5-фтор-пиридин-3-ил]-пиразоло[1, 5-а]пиримидин-3-карбоксамида, используемые в качестве ингибитора atr киназы, препараты на основе этого соединения и его различные твердые формы
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Also Published As

Publication number Publication date
CN1701074A (zh) 2005-11-23
US7309705B2 (en) 2007-12-18
MY141978A (en) 2010-08-16
AU2003268385B2 (en) 2006-12-21
KR20050057139A (ko) 2005-06-16
AU2003268385A1 (en) 2004-03-29
NZ539164A (en) 2006-04-28
EP1534710B1 (en) 2007-10-24
IL167088A (en) 2010-12-30
JP4700344B2 (ja) 2011-06-15
ZA200501852B (en) 2005-09-08
WO2004022560A1 (en) 2004-03-18
AR041136A1 (es) 2005-05-04
PE20040999A1 (es) 2004-12-28
JP2010168406A (ja) 2010-08-05
ATE376548T1 (de) 2007-11-15
US7074924B2 (en) 2006-07-11
MXPA05002570A (es) 2005-09-08
EP1534710A1 (en) 2005-06-01
US7511049B2 (en) 2009-03-31
JP2006502161A (ja) 2006-01-19
DE60317077T2 (de) 2008-07-24
US20070275983A1 (en) 2007-11-29
US20040116442A1 (en) 2004-06-17
MY137888A (en) 2009-03-31
US20060173016A1 (en) 2006-08-03
ES2291665T3 (es) 2008-03-01
HK1071569A1 (en) 2005-07-22
DE60317077D1 (de) 2007-12-06
CA2497450A1 (en) 2004-03-18
TW200420564A (en) 2004-10-16
TWI335919B (en) 2011-01-11
WO2004022560A9 (en) 2005-07-07

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