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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CN
China
Prior art keywords
compound
methyl
formula
amino
pyrido
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Pending
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CN200880018758A
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English (en)
Chinese (zh)
Inventor
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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—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
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations 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
    • A61K51/025—Preparations 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • A61N5/1001—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy using radiation sources introduced into or applied onto the body; brachytherapy
    • 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

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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)
  • Radiology & Medical Imaging (AREA)
  • Inorganic Chemistry (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (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)

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

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2005316668B2 (en) * 2004-12-13 2012-09-06 Millennium Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors
BRPI0617162B8 (pt) * 2005-10-07 2021-05-25 Exelixis Inc compostos inibidores de fosfatidilinositol 3-quinase composições farmacêuticas que os contem e métodos de uso dos mesmos
CN101395155A (zh) * 2005-10-07 2009-03-25 埃克塞里艾克西斯公司 PI3Kα的吡啶并嘧啶酮抑制剂
CN101528231A (zh) 2006-08-16 2009-09-09 埃克塞利希斯股份有限公司 在癌症的治疗中使用pi3k和mek调控剂
DK2074122T5 (da) * 2006-09-15 2014-03-17 Pfizer Prod Inc Pyrido (2, 3-d) pyrimidin0n-forbindelser og anvendelse deraf som pi3 inhibitorer
JP2010523670A (ja) 2007-04-10 2010-07-15 エクセリクシス， インク． Ｐｉ３ｋアルファのピリドピリミジノン阻害剤を使用した治療方法
EP2142543B8 (en) * 2007-04-11 2013-07-03 Exelixis, Inc. Pyrido [2, 3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer
WO2010039740A1 (en) * 2008-09-30 2010-04-08 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
UY33221A (es) 2010-02-09 2011-09-30 Univ California MÉTODOS PARA TRATAR CÁNCER USANDO INHIBIDORES DE PI3K Y mTOR EN COMBINACIÓN CON INHIBIDORES DE AUTOFAGIA
EP2616442B8 (en) 2010-09-14 2018-10-17 Exelixis, Inc. Inhibitors of pi3k-delta and methods of their use and manufacture
WO2013056067A1 (en) * 2011-10-13 2013-04-18 Exelixis, Inc. Compounds for use in the treatment of basal cell carcinoma
CN104302294A (zh) 2011-11-01 2015-01-21 埃克塞利希斯股份有限公司 用于治疗淋巴组织增生性恶性肿瘤的作为磷脂酰肌醇3-激酶抑制剂的n-(3-{[(3-{[2-氯-5-(甲氧基)苯基]氨基}喹喔啉-2-基)氨基]磺酰基}苯基)-2-甲基丙氨酰胺

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
ATE373659T1 (de) * 2004-05-04 2007-10-15 Warner Lambert Co Pyrrolylsubstituierte pyrido(2,3-d)pyrimidin-7- one und derivate davon als therapeutische mittel
US8247408B2 (en) * 2005-10-07 2012-08-21 Exelixis, Inc. Pyridopyrimidinone inhibitors of PI3Kα for the treatment of cancer
CN101528231A (zh) * 2006-08-16 2009-09-09 埃克塞利希斯股份有限公司 在癌症的治疗中使用pi3k和mek调控剂
DK2074122T5 (da) * 2006-09-15 2014-03-17 Pfizer Prod Inc Pyrido (2, 3-d) pyrimidin0n-forbindelser og anvendelse deraf som pi3 inhibitorer

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

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Application publication date: 20100519