CN101711249A - 作为PI3K-α的抑制剂用于治疗癌症的吡啶并[2,3-D]嘧啶-7-酮化合物 - Google Patents

作为PI3K-α的抑制剂用于治疗癌症的吡啶并[2,3-D]嘧啶-7-酮化合物 Download PDF

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Publication number
CN101711249A
CN101711249A CN200880018758A CN200880018758A CN101711249A CN 101711249 A CN101711249 A CN 101711249A CN 200880018758 A CN200880018758 A CN 200880018758A CN 200880018758 A CN200880018758 A CN 200880018758A CN 101711249 A CN101711249 A CN 101711249A
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China
Prior art keywords
compound
methyl
formula
amino
pyrido
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CN200880018758A
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Chinese (zh)
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C·A·布尔
L·王
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Exelixis Inc
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Exelixis Inc
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Publication of CN101711249A publication Critical patent/CN101711249A/zh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-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
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/025Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus inorganic Tc complexes or compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61NELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00Radiation therapy
    • A61N5/10X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • A61N5/1001X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy using radiation sources introduced into or applied onto the body; brachytherapy
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Radiology & Medical Imaging (AREA)
  • Inorganic Chemistry (AREA)
  • Mycology (AREA)
  • Optics & Photonics (AREA)
  • Microbiology (AREA)
  • Immunology (AREA)
  • Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Hematology (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)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN200880018758A 2007-04-11 2008-04-11 作为PI3K-α的抑制剂用于治疗癌症的吡啶并[2,3-D]嘧啶-7-酮化合物 Pending CN101711249A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US91116007P 2007-04-11 2007-04-11
US60/911,160 2007-04-11
PCT/US2008/004807 WO2008127712A1 (en) 2007-04-11 2008-04-11 Pyrido [2, 3-d] pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer

Publications (1)

Publication Number Publication Date
CN101711249A true CN101711249A (zh) 2010-05-19

Family

ID=39642739

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200880018758A Pending CN101711249A (zh) 2007-04-11 2008-04-11 作为PI3K-α的抑制剂用于治疗癌症的吡啶并[2,3-D]嘧啶-7-酮化合物

Country Status (25)

Country Link
US (2) US20100209340A1 (enExample)
EP (1) EP2142544B8 (enExample)
JP (1) JP2010523681A (enExample)
KR (1) KR20090130104A (enExample)
CN (1) CN101711249A (enExample)
AU (1) AU2008239596B2 (enExample)
BR (1) BRPI0810175A2 (enExample)
CA (1) CA2683820A1 (enExample)
CO (1) CO6241119A2 (enExample)
CR (1) CR11098A (enExample)
DO (1) DOP2009000242A (enExample)
EA (1) EA018964B1 (enExample)
EC (1) ECSP099722A (enExample)
ES (1) ES2425068T3 (enExample)
IL (1) IL201209A0 (enExample)
MA (1) MA31336B1 (enExample)
MX (1) MX2009010815A (enExample)
MY (1) MY150747A (enExample)
NI (1) NI200900183A (enExample)
NZ (1) NZ579945A (enExample)
SV (1) SV2009003389A (enExample)
TN (1) TN2009000389A1 (enExample)
UA (1) UA101315C2 (enExample)
WO (1) WO2008127712A1 (enExample)
ZA (1) ZA200906648B (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1828186A1 (en) * 2004-12-13 2007-09-05 Sunesis Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors
US8044062B2 (en) * 2005-10-07 2011-10-25 Exelixis, Inc. Substituted pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors of phospatidylinositol 3-kinase alpha
ES2513165T3 (es) * 2005-10-07 2014-10-24 Exelixis, Inc. Derivados de N-(3-amino-quinoxalin-2-il)-sulfonamida y su uso como inhibidores de la fosfatidilinositol-3-quinasa
JP2010500994A (ja) 2006-08-16 2010-01-14 エグゼリクシス, インコーポレイテッド Pi3kおよびmekモジュレーターを使用する方法
GEP20115306B (enExample) 2006-09-15 2011-10-10 Pfizer Prod Inc
UA100979C2 (ru) 2007-04-10 2013-02-25 Экселиксис, Инк. Применение пиридопиримидиноновых ингибиторов pi3k альфа для лечения рака
CA2683784A1 (en) * 2007-04-11 2008-10-23 Exelixis, Inc. Pyrido[2,3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer
AR073524A1 (es) * 2008-09-30 2010-11-10 Exelixis Inc Piridopirimidinonas inhibidores de pi3k a y m tor
NZ600954A (en) * 2009-12-22 2013-11-29 Isoindolinone inhibitors of phosphatidylinositol 3-kinase
AR080151A1 (es) 2010-02-09 2012-03-14 Exelixis Inc Metodos para tratar cancer usando inhibidores de piridopirimidinona de pi 3k y mtor en combinacion con inhibidores de autofagia
TWI642670B (zh) 2010-09-14 2018-12-01 伊塞利克斯公司 Pi3k-德爾塔抑制劑以及其應用和生產方法
WO2013056067A1 (en) * 2011-10-13 2013-04-18 Exelixis, Inc. Compounds for use in the treatment of basal cell carcinoma
PE20141794A1 (es) 2011-11-01 2014-12-17 Exelixis Inc N-(3-{[(3-{[2-cloro-5-(metoxi)fenil]amino}quinoxalin-2-il)amino]sulfonil}fenil)-2-metilalaninamida como inhibidor de fosfatidilinositol 3-quinasa para el tratamiento de neoplasias linfoproliferativas

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1183099A (zh) * 1995-05-03 1998-05-27 沃尼尔·朗伯公司 抑制蛋白质酪氨酸激酶介导的细胞增殖的吡啶并[2,3-d]嘧啶
WO2007044813A1 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2937284A (en) * 1958-05-01 1960-05-17 Burroughs Wellcome Co 2, 4-diamino-5, 6-dialkylpyrido (2, 3-d) pyrimidines and method
US7019002B2 (en) * 2001-12-11 2006-03-28 Pharmacia & Upjohn, S.P.A. Pyridopyrimidinones derivatives as telomerase inhibitors
BRPI0510560A (pt) * 2004-05-04 2007-11-20 Warner Lambert Co pirido[2,3-d] pirimidin-7-onas pirrolil substituìdas e seus derivados como agentes terapêuticos
US8247408B2 (en) * 2005-10-07 2012-08-21 Exelixis, Inc. Pyridopyrimidinone inhibitors of PI3Kα for the treatment of cancer
JP2010500994A (ja) * 2006-08-16 2010-01-14 エグゼリクシス, インコーポレイテッド Pi3kおよびmekモジュレーターを使用する方法
GEP20115306B (enExample) * 2006-09-15 2011-10-10 Pfizer Prod Inc

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1183099A (zh) * 1995-05-03 1998-05-27 沃尼尔·朗伯公司 抑制蛋白质酪氨酸激酶介导的细胞增殖的吡啶并[2,3-d]嘧啶
WO2007044813A1 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα

Also Published As

Publication number Publication date
MX2009010815A (es) 2009-10-29
HK1139941A1 (en) 2010-09-30
NZ579945A (en) 2012-05-25
CO6241119A2 (es) 2011-01-20
DOP2009000242A (es) 2010-04-30
US20100209340A1 (en) 2010-08-19
CR11098A (es) 2010-01-27
SV2009003389A (es) 2010-04-27
TN2009000389A1 (en) 2010-12-31
EP2142544B8 (en) 2013-07-03
US20130343988A1 (en) 2013-12-26
EP2142544A1 (en) 2010-01-13
CA2683820A1 (en) 2008-10-23
NI200900183A (es) 2010-10-05
AU2008239596B2 (en) 2013-08-15
EP2142544B1 (en) 2013-05-22
EA200970936A1 (ru) 2010-02-26
ECSP099722A (es) 2009-12-28
AU2008239596A1 (en) 2008-10-23
WO2008127712A1 (en) 2008-10-23
ZA200906648B (en) 2010-04-28
IL201209A0 (en) 2010-05-31
UA101315C2 (ru) 2013-03-25
MA31336B1 (fr) 2010-04-01
JP2010523681A (ja) 2010-07-15
MY150747A (en) 2014-02-28
ES2425068T3 (es) 2013-10-11
BRPI0810175A2 (pt) 2014-12-30
EA018964B1 (ru) 2013-12-30
KR20090130104A (ko) 2009-12-17

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Application publication date: 20100519