AU2003268385B2 - Pyrazolopyrimidines as cyclin dependent kinase inhibitors - Google Patents

Pyrazolopyrimidines as cyclin dependent kinase inhibitors Download PDF

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Publication number
AU2003268385B2
AU2003268385B2 AU2003268385A AU2003268385A AU2003268385B2 AU 2003268385 B2 AU2003268385 B2 AU 2003268385B2 AU 2003268385 A AU2003268385 A AU 2003268385A AU 2003268385 A AU2003268385 A AU 2003268385A AU 2003268385 B2 AU2003268385 B2 AU 2003268385B2
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AU
Australia
Prior art keywords
compound
group
aryl
alkyl
cycloalkyl
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.)
Ceased
Application number
AU2003268385A
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English (en)
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AU2003268385A1 (en
Inventor
Lawrence W. Dillard
Ronald J. Doll
Michael P. Dwyer
Viyyoor Moopil Girijavallabhan
Timothy J. Guzi
Zhen Min He
Ray Anthony James
Haengsoon Park
Kamil Paruch
Vinh D. Tran
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 & 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
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Application filed by Pharmacopeia Inc, Schering Corp filed Critical Pharmacopeia Inc
Publication of AU2003268385A1 publication Critical patent/AU2003268385A1/en
Application granted granted Critical
Publication of AU2003268385B2 publication Critical patent/AU2003268385B2/en
Assigned to PHARMACOPEIA, INC., SCHERING CORPORATION reassignment PHARMACOPEIA, INC. Request for Assignment Assignors: PHARMACOPEIA DRUG DISCOVERY, INC., SCHERING CORPORATION
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds 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
    • A61K31/7064—Compounds 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
    • A61K31/7068—Compounds 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
    • A61K31/7072—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P43/00—Drugs 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Hematology (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)
AU2003268385A 2002-09-04 2003-09-03 Pyrazolopyrimidines as cyclin dependent kinase inhibitors Ceased AU2003268385B2 (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
AU2003268385A1 AU2003268385A1 (en) 2004-03-29
AU2003268385B2 true AU2003268385B2 (en) 2006-12-21

Family

ID=31978544

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2003268385A Ceased AU2003268385B2 (en) 2002-09-04 2003-09-03 Pyrazolopyrimidines as cyclin dependent kinase inhibitors

Country Status (19)

Country Link
US (3) US7074924B2 (cg-RX-API-DMAC10.html)
EP (1) EP1534710B1 (cg-RX-API-DMAC10.html)
JP (2) JP4700344B2 (cg-RX-API-DMAC10.html)
KR (1) KR20050057139A (cg-RX-API-DMAC10.html)
CN (1) CN1701074A (cg-RX-API-DMAC10.html)
AR (1) AR041136A1 (cg-RX-API-DMAC10.html)
AT (1) ATE376548T1 (cg-RX-API-DMAC10.html)
AU (1) AU2003268385B2 (cg-RX-API-DMAC10.html)
CA (1) CA2497450C (cg-RX-API-DMAC10.html)
DE (1) DE60317077T2 (cg-RX-API-DMAC10.html)
ES (1) ES2291665T3 (cg-RX-API-DMAC10.html)
IL (1) IL167088A (cg-RX-API-DMAC10.html)
MX (1) MXPA05002570A (cg-RX-API-DMAC10.html)
MY (2) MY141978A (cg-RX-API-DMAC10.html)
NZ (1) NZ539164A (cg-RX-API-DMAC10.html)
PE (1) PE20040999A1 (cg-RX-API-DMAC10.html)
TW (1) TWI335919B (cg-RX-API-DMAC10.html)
WO (1) WO2004022560A1 (cg-RX-API-DMAC10.html)
ZA (1) ZA200501852B (cg-RX-API-DMAC10.html)

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US7196078B2 (en) * 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
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LT3418281T (lt) 2012-12-07 2021-01-11 Vertex Pharmaceuticals Inc. Pirazolo[1,5-a]pirimidinai, naudotini kaip atr kinazės inhibitoriai, skirti vėžinių ligų gydymui
RU2015143517A (ru) * 2013-03-13 2017-04-19 Дженентек, Инк. Пиразолсодержащие соединения и их применения
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
EP2970289A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
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HUE046727T2 (hu) 2013-12-06 2020-03-30 Vertex Pharma Az ATR-kináz inhibitoraként használható vegyület, 2-amino-6-fluoro-N-[5-fluoro-piridin-3-IL]-pirazolo-[1,5-A]-pirimidin-3-karboxamid, ennek elõállítása, különbözõ szilárd formái és ezek radioaktív nyomjelzett származékai
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
ES2777608T3 (es) 2014-06-05 2020-08-05 Vertex Pharma Derivados radiomarcados de un compuesto de 2-amino-6-fluoro-N-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útiles como inhibidores de ATR cinasa, la preparación de dicho compuesto y diferentes formas sólidas del mismo
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Also Published As

Publication number Publication date
DE60317077T2 (de) 2008-07-24
US7511049B2 (en) 2009-03-31
US20040116442A1 (en) 2004-06-17
JP2006502161A (ja) 2006-01-19
ATE376548T1 (de) 2007-11-15
ES2291665T3 (es) 2008-03-01
WO2004022560A9 (en) 2005-07-07
IL167088A (en) 2010-12-30
JP4700344B2 (ja) 2011-06-15
NZ539164A (en) 2006-04-28
MY141978A (en) 2010-08-16
US20070275983A1 (en) 2007-11-29
TWI335919B (en) 2011-01-11
KR20050057139A (ko) 2005-06-16
HK1071569A1 (en) 2005-07-22
CA2497450A1 (en) 2004-03-18
US20060173016A1 (en) 2006-08-03
AR041136A1 (es) 2005-05-04
TW200420564A (en) 2004-10-16
EP1534710B1 (en) 2007-10-24
WO2004022560A1 (en) 2004-03-18
US7074924B2 (en) 2006-07-11
AU2003268385A1 (en) 2004-03-29
MXPA05002570A (es) 2005-09-08
DE60317077D1 (de) 2007-12-06
CA2497450C (en) 2011-05-31
MY137888A (en) 2009-03-31
ZA200501852B (en) 2005-09-08
US7309705B2 (en) 2007-12-18
PE20040999A1 (es) 2004-12-28
EP1534710A1 (en) 2005-06-01
JP2010168406A (ja) 2010-08-05
CN1701074A (zh) 2005-11-23

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MK25 Application lapsed reg. 22.2i(2) - failure to pay acceptance fee
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Free format text: IN VOL 21, NO 15, PAGE(S) 1652 UNDER THE HEADING APPLICATIONS LAPSED, REFUSED OR WITHDRAWN, PATENTSCEASED OR EXPIRED - 2003 DELETE ALL REFERENCE TO 2003268385

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