TW201018685A - Pyridopyrimidinone inhibitors of PI3Kα and mTOR - Google Patents

Pyridopyrimidinone inhibitors of PI3Kα and mTOR Download PDF

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Publication number
TW201018685A
TW201018685A TW098133017A TW98133017A TW201018685A TW 201018685 A TW201018685 A TW 201018685A TW 098133017 A TW098133017 A TW 098133017A TW 98133017 A TW98133017 A TW 98133017A TW 201018685 A TW201018685 A TW 201018685A
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TW
Taiwan
Prior art keywords
compound
formula
cancer
pharmaceutically acceptable
optionally
Prior art date
Application number
TW098133017A
Other languages
English (en)
Chinese (zh)
Inventor
Tae-Gon Baik
Sung-Hoon Ma
Chris A Buhr
John M Nuss
Original Assignee
Exelixis Inc
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 Exelixis Inc filed Critical Exelixis Inc
Publication of TW201018685A publication Critical patent/TW201018685A/zh

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Classifications

    • 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
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW098133017A 2008-09-30 2009-09-29 Pyridopyrimidinone inhibitors of PI3Kα and mTOR TW201018685A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US19476108P 2008-09-30 2008-09-30

Publications (1)

Publication Number Publication Date
TW201018685A true TW201018685A (en) 2010-05-16

Family

ID=41572575

Family Applications (1)

Application Number Title Priority Date Filing Date
TW098133017A TW201018685A (en) 2008-09-30 2009-09-29 Pyridopyrimidinone inhibitors of PI3Kα and mTOR

Country Status (8)

Country Link
US (1) US8101622B2 (enExample)
EP (1) EP2350070A1 (enExample)
JP (1) JP2012504628A (enExample)
AR (1) AR073524A1 (enExample)
PA (1) PA8843901A1 (enExample)
TW (1) TW201018685A (enExample)
UY (1) UY32153A (enExample)
WO (1) WO2010039740A1 (enExample)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GEP20115304B (en) * 2005-10-07 2011-10-10 Exelixis Inc PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα
WO2007044729A2 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
ATE539752T1 (de) 2006-08-16 2012-01-15 Exelixis Inc Verwendung von pi3k- und mek-modulatoren bei der krebsbehandlung
MY146420A (en) * 2006-09-15 2012-08-15 Pfizer Prod Inc Pyrido (2, 3-d) pyrimidinone compounds and their use as pi3 inhibitors
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
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
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
AU2011302196B2 (en) 2010-09-14 2016-04-28 Exelixis, Inc. Inhibitors of PI3K-delta and methods of their use and manufacture
JP6130305B2 (ja) * 2011-02-23 2017-05-17 インテリカイン, エルエルシー キナーゼ阻害剤の組み合わせおよびそれらの使用
JP2014513104A (ja) * 2011-04-29 2014-05-29 エクセリクシス, インク. Pi3k/mtorのピリドピリミジノン阻害剤を用いたリンパ腫の治療方法
SG11201401961UA (en) 2011-11-01 2014-05-29 Exelixis Inc N- (3- { [ (3- { [2-chloro-5- (methoxy) phenyl] amino} quinoxalin- 2 -yl) amino] sulfonyl} phe nyl) - 2 -methylalaninamide as phosphatidylinositol 3 - kinase inhibitor for the treatment of lymphoproliferative malignancies
US20180214452A1 (en) 2015-03-06 2018-08-02 Korea Advanced Institute Of Science And Technology COMPOSITION FOR PREVENTION OR TREATMENT OF INTRACTABLE EPILEPSY COMPRISING mTOR INHIBITOR
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
CA3142712A1 (en) 2019-06-04 2020-12-10 Arcus Biosciences, Inc. 2,3,5-trisubstituted pyrazolo[1,5-a]pyrimidine compounds
WO2021139775A1 (zh) * 2020-01-10 2021-07-15 江苏先声药业有限公司 吡啶酮化合物及应用
WO2021219101A1 (zh) * 2020-04-30 2021-11-04 广州嘉越医药科技有限公司 一种含杂环的化合物的应用

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL117923A (en) 1995-05-03 2000-06-01 Warner Lambert Co Anti-cancer pharmaceutical compositions containing polysubstituted pyrido¬2,3-d¾pyrimidine derivatives and certain such novel compounds
WO1998033798A2 (en) 1997-02-05 1998-08-06 Warner Lambert Company Pyrido[2,3-d]pyrimidines and 4-amino-pyrimidines as inhibitors of cell proliferation
PL357634A1 (en) 2000-01-27 2004-07-26 Warner-Lambert Company Pyridopyrimidinone derivatives for treatment of neurodegenerative disease
EA200200802A1 (ru) 2000-03-06 2003-02-27 Уорнер-Ламберт Компани 5-АЛКИЛПИРИДО[2.3-d]ПИРИМИДИНОВЫЕ ИНГИБИТОРЫ ТИРОЗИНКИНАЗЫ
EP1277738B1 (en) 2000-04-27 2011-03-30 Astellas Pharma Inc. Condensed heteroaryl derivatives
NZ527741A (en) 2001-02-26 2005-02-25 Tanabe Seiyaku Co Pyridopyrimidine or naphthyridine derivative
WO2003000270A1 (en) * 2001-06-21 2003-01-03 Ariad Pharmaceuticals, Inc. Novel pyridopyrimidones and uses thereof
US7019002B2 (en) 2001-12-11 2006-03-28 Pharmacia & Upjohn, S.P.A. Pyridopyrimidinones derivatives as telomerase inhibitors
KR20040103972A (ko) 2002-04-19 2004-12-09 스미스클라인 비참 코포레이션 신규 화합물
CA2484921A1 (en) 2002-05-06 2003-11-13 Genelabs Technologies, Inc. Nucleoside derivatives for treating hepatitis c virus infection
JP2004083587A (ja) 2002-08-06 2004-03-18 Tanabe Seiyaku Co Ltd 医薬組成物
WO2004063195A1 (en) 2003-01-03 2004-07-29 Sloan-Kettering Institute For Cancer Research Pyridopyrimidine kinase inhibitors
WO2004089930A1 (en) 2003-04-02 2004-10-21 Imclone Systems Incorporated 4-fluoroquinolone derivatives and their use as kinase inhibitors
EP1624900A4 (en) 2003-05-20 2007-05-02 Univ California METHOD OF BINDING AGENTS AT BETA AMYLOID PLAQUE
EP1718645A1 (en) 2004-02-18 2006-11-08 Warner-Lambert Company LLC 2-(pyridin-3-ylamino)-pyrido 2,3-d pyrimidin-7-ones
CA2563669A1 (en) * 2004-05-04 2005-11-10 Warner-Lambert Company Llc Pyrrolyl substituted pyrido[2,3-d]pyrimidin-7-ones and derivatives thereof as therapeutic agents
AU2005316668B2 (en) 2004-12-13 2012-09-06 Millennium Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors
GEP20115304B (en) * 2005-10-07 2011-10-10 Exelixis Inc PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα
EA201200669A1 (ru) * 2005-10-07 2012-11-30 Экселиксис, Инк. ПИРИДОПИРИМИДИНОНОВЫЕ ИНГИБИТОРЫ PI3Kα
MY146420A (en) * 2006-09-15 2012-08-15 Pfizer Prod Inc Pyrido (2, 3-d) pyrimidinone compounds and their use as pi3 inhibitors
CA2683820A1 (en) * 2007-04-11 2008-10-23 Exelixis, Inc. Pyrido [2, 3-d] pyrimidin-7-one compounds as inhibitors of p13k-alpha for the treatment of cancer

Also Published As

Publication number Publication date
WO2010039740A1 (en) 2010-04-08
EP2350070A1 (en) 2011-08-03
US20100087456A1 (en) 2010-04-08
JP2012504628A (ja) 2012-02-23
UY32153A (es) 2011-04-29
PA8843901A1 (es) 2010-05-26
US8101622B2 (en) 2012-01-24
AR073524A1 (es) 2010-11-10

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