TW201018685A - Pyridopyrimidinone inhibitors of PI3Kα and mTOR - Google Patents

Pyridopyrimidinone inhibitors of PI3Kα and mTOR Download PDF

Info

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
Authority
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

Links

Classifications

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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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
RS53627B1 (sr) * 2005-10-07 2015-04-30 Exelixis Inc. Derivati n-(3-amino-hinoksalin-2-il)-sulfonamida i njihova upotreba kao inhibitora fosfatidilinozitol3-kinaze
NZ594628A (en) * 2005-10-07 2013-04-26 Exelixis Inc PYRIDOPYRIMIDINONE INHIBITORS OF PI3Ka
WO2008021389A2 (en) 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
WO2008032162A1 (en) * 2006-09-15 2008-03-20 Pfizer Products Inc. Pyrido (2, 3-d) pyrimidin0ne compounds and their use as pi3 inhibitors
RS52939B (sr) * 2007-04-10 2014-02-28 Exelixis Inc. Postupci za lečenje kancera upotrebom piridopirimidinonskih inhibitora pi3k alfa
AU2008239655B2 (en) * 2007-04-11 2013-06-20 Exelixis, Inc. Pyrido (2, 3-d) pyrimidin-7-one compounds as inhibitors of PI3k-alpha for the treatment of cancer
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
JP5792819B2 (ja) 2010-09-14 2015-10-14 エクセリクシス， インク． Ｐｉ３ｋ−デルタの阻害剤ならびにそれらの使用法および製造法
TWI592411B (zh) * 2011-02-23 2017-07-21 英特爾立秦有限責任公司 激酶抑制劑之組合及其用途
EA201391606A1 (ru) * 2011-04-29 2016-01-29 Экселиксис, Инк. Способ лечения лимфомы посредством пиридопиримидиноновых ингибиторов pi3k/mtor
EA201490905A1 (ru) 2011-11-01 2014-11-28 Экселиксис, Инк. N-(3-{[(3-{[2-хлор-5-(метокси)фенил]амино}хиноксалин-2-ил)амино]сульфонил}фенил)-2-метилаланинамид как ингибитор фосфатидилинозитол-3-киназы для лечения лимфопролиферативных злокачественных заболеваний
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
EP3980010A4 (en) 2019-06-04 2023-06-07 Arcus Biosciences, Inc. 2,3,5-TRISUBSTITUTED PYRAZOLO[1,5-A]PYRIMIDINE COMPOUNDS
CN114901664B (zh) * 2020-01-10 2024-07-02 南京再明医药有限公司 吡啶酮化合物及应用
US20230165864A1 (en) * 2020-04-30 2023-06-01 Guangzhou Joyo Pharmatech Co., Ltd Application of heterocyclic compound

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
DE69839338T2 (de) 1997-02-05 2008-07-10 Warner-Lambert Company Llc Pyrido (2,3-d) pyrimidine und 4-amino-pyrimidine als inhibitoren der zellulären proliferation
KR20020070520A (ko) 2000-01-27 2002-09-09 워너-램버트 캄파니 신경퇴행성 질병의 치료를 위한 피리도피리미디논 유도체
KR20020075805A (ko) 2000-03-06 2002-10-05 워너-램버트 캄파니 5-알킬피리도[2,3-ｄ]피리미딘 타이로신 카이나제 억제제
WO2001083456A1 (en) 2000-04-27 2001-11-08 Yamanouchi Pharmaceutical Co., Ltd. Condensed heteroaryl derivatives
EP1364950A4 (en) 2001-02-26 2005-03-09 Tanabe Seiyaku Co Pyridopyrimidine and naphthyridine derivatives
US20030100572A1 (en) * 2001-06-21 2003-05-29 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
US7629350B2 (en) 2002-04-19 2009-12-08 Smithkline Beecham Corporation Compounds
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
US20050009849A1 (en) 2003-01-03 2005-01-13 Veach Darren R. Pyridopyrimidine kinase inhibitors
WO2004089930A1 (en) 2003-04-02 2004-10-21 Imclone Systems Incorporated 4-fluoroquinolone derivatives and their use as kinase inhibitors
US20070053831A1 (en) 2003-05-20 2007-03-08 Barrio Jorge R Methods for binding agents to b-amyloid plaques
BRPI0507852A (pt) 2004-02-18 2007-07-10 Warner Lambert Co 2-(piridin-3-ilamino)-pirido[2,3-d]pirimidin-7-onas
WO2005105801A1 (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
US7767687B2 (en) 2004-12-13 2010-08-03 Biogen Idec Ma Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors
CN102746298A (zh) * 2005-10-07 2012-10-24 埃克塞里艾克西斯公司 PI3Kα的吡啶并嘧啶酮抑制剂
NZ594628A (en) * 2005-10-07 2013-04-26 Exelixis Inc PYRIDOPYRIMIDINONE INHIBITORS OF PI3Ka
WO2008032162A1 (en) * 2006-09-15 2008-03-20 Pfizer Products Inc. Pyrido (2, 3-d) pyrimidin0ne compounds and their use as pi3 inhibitors
CN101711249A (zh) * 2007-04-11 2010-05-19 埃克塞里艾克西斯公司 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

Also Published As

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

Similar Documents

Publication Publication Date Title
TW201018685A (en) Pyridopyrimidinone inhibitors of PI3Kα and mTOR
EP2771342B1 (en) Purine derivatives and their use in the treatment of disease
JP4344607B2 (ja) 蛋白キナーゼ阻害剤としてのピロロピリミジン
JP5963777B2 (ja) 新規ヘテロ環誘導体
RU2637936C2 (ru) Ингибиторы активности киназы lrrk2
JP6649540B2 (ja) 置換されたヘテロアリール化合物および使用方法
CN113861188B (zh) 吡唑并[3,4-b]吡啶类衍生物及其制备方法和作为HPK1抑制剂的应用
TW201815799A (zh) 巨環激酶抑制劑
JP2010518107A (ja) Ｐｉ３−キナーゼ阻害剤およびその使用方法
CN104470923A (zh) 选择性PI3K δ抑制剂
US11304929B2 (en) Tosylacetate based compounds and derivatives thereof as PHGDH inhibitors
TW201144318A (en) Activators of AMPK and therapeutic uses thereof
TW201014841A (en) Tri-substituted pyrimidine compounds and their use as PDE10 inhibitors
JPWO2004043936A1 (ja) Ｐｌｋ阻害剤
TWI458730B (zh) 新穎２，３－二氫－１Ｈ－咪唑并｛１，２－ａ｝嘧啶－５－酮衍生物，其製法及其醫藥用途
CN102596969A (zh) 用作蛋白激酶调节剂的稠合喹啉类化合物
TW200845997A (en) 2-substituted-6-heterocyclic pyrimidone derivatives
TW201105673A (en) Novel 1,2,3,4-tetrahydropyrimido{1,2-a}pyrimidin-6-one derivatives, preparation thereof and pharmaceutical use thereof
JP2021503479A (ja) 置換ヘテロアリール化合物及び使用方法
CN110872296A (zh) 一种二氢异吲哚-1H-吡唑并[3,4-d]嘧啶酮化合物、其制备方法和应用
WO2025011444A1 (zh) 一种嘧啶胺类nuak抑制剂及其制备方法和用途
JP2008536938A (ja) Ａｋｔ活性の阻害物質
WO2022007921A1 (zh) 三嗪类化合物及其组合物和用途
JP2018527340A (ja) アリール置換ジヒドロキノリノン、その調製及び医薬品としてのその使用
WO2012083145A1 (en) Glucosamine derivatives