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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English (en)
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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    • 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)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Mycology (AREA)
  • Immunology (AREA)
  • Radiology & Medical Imaging (AREA)
  • Microbiology (AREA)
  • Inorganic Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Pathology (AREA)
  • Oncology (AREA)
  • Hematology (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)

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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
JP5111113B2 (ja) * 2004-12-13 2012-12-26 サネシス ファーマシューティカルズ, インコーポレイテッド Rafキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン
EP2364974A1 (en) * 2005-10-07 2011-09-14 Exelixis, Inc. N-(3-Phenylamino-quinoxalin-2-yl)-benzenesulfonamide derivatives as phosphatidylinositol 3-kinase inhibitors
HRP20130902T1 (hr) * 2005-10-07 2013-11-08 Exelixis Inc. PIRIDOPIRIMIDINONSKI INHIBITORI PI3Kalfa
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
HRP20110621T2 (hr) 2006-09-15 2013-12-06 Pfizer Products Inc. SPOJEVI PIRIDO[2,3-d]PIRIMIDINONA I NJIHOVA UPOTREBA KAO INHIBITORI PI3
ES2430614T3 (es) 2007-04-10 2013-11-21 Exelixis, Inc. Métodos de tratamiento del cáncer usando inhibidores de piridopirimidinona de PI3K alfa
US20100150827A1 (en) * 2007-04-11 2010-06-17 Exelixis, Inc Pyrido [2, 3-d] pyrimidin-7-one compounds as inhibitors of p13k-alpha for the treatment of cancer
US8101622B2 (en) * 2008-09-30 2012-01-24 Exelixis, Inc. Pyridopyrimidinone inhibitors of PI3Kα and mTOR
AU2010341573B2 (en) * 2009-12-22 2016-10-13 Vertex Pharmaceuticals Incorporated Isoindolinone inhibitors of phosphatidylinositol 3-kinase
WO2011100319A1 (en) 2010-02-09 2011-08-18 Exelixis, Inc. Methods of treating cancer using pyridopyrimidinone inhibitors of pi3k and mtor in combination with autophagy inhibitors
AR082985A1 (es) 2010-09-14 2013-01-23 Exelixis Inc INHIBIDORES DE PI3K-d Y METODOS DE SU USO Y PREPARACION
WO2013056067A1 (en) * 2011-10-13 2013-04-18 Exelixis, Inc. Compounds for use in the treatment of basal cell carcinoma
MX2014005249A (es) 2011-11-01 2015-03-05 Exelixis Inc N-(3-{[(3-{[2-cloro-5-(metoxi)fenil]amino}quinoxalin-2-il)amino]s ulfonil}fenil)-2-metilalaninamida como inhibidor de fosfatidilinositol 3-cinasa para el tratamiento de neoplasias malignas 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
DE602005002562T2 (de) * 2004-05-04 2008-01-31 Warner-Lambert Company Llc Pyrrolylsubstituierte pyridoä2,3-düpyrimidin-7-one und derivate davon als therapeutische mittel
JP5480503B2 (ja) * 2005-10-07 2014-04-23 エクセリクシス, インク. PI3Kαのピリドピリミジノン型阻害剤
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
HRP20110621T2 (hr) * 2006-09-15 2013-12-06 Pfizer Products Inc. SPOJEVI PIRIDO[2,3-d]PIRIMIDINONA I NJIHOVA UPOTREBA KAO INHIBITORI PI3

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

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Application publication date: 20100519