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

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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 (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7989622B2 (en) * 2005-10-07 2011-08-02 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors and methods of their use
EA016945B1 (ru) * 2005-10-07 2012-08-30 Экселиксис, Инк. ПИРИДОПИРИМИДИНОНОВЫЕ ИНГИБИТОРЫ PI3Kα
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
PT2074122E (pt) * 2006-09-15 2011-08-24 Pfizer Prod Inc Compostos de pirido(2,3-d)-pirimidinona e sua utilização como inibidores de pi3
MY150697A (en) * 2007-04-10 2014-02-28 Exelixis Inc Methods of treating cancer using pyridopyrimdinone inhibitors of p13k alpha
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
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
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
CN103635183A (zh) * 2011-04-29 2014-03-12 埃克塞利希斯股份有限公司 使用pi3k/mtor的吡啶并嘧啶抑制剂来治疗淋巴瘤的方法
CN107375289A (zh) 2011-11-01 2017-11-24 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‑激酶抑制剂的化合物
EP3266455B1 (en) 2015-03-06 2020-12-30 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
CN114206332B (zh) 2019-06-04 2024-08-23 艾库斯生物科学有限公司 2,3,5-三取代吡唑并[1,5-a]嘧啶化合物
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
GB202415232D0 (en) 2024-10-16 2024-11-27 Nacamed As Composition

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
JP2003523358A (ja) 2000-01-27 2003-08-05 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー 神経変性疾患の治療のためのピリドピリミジノン誘導体
AP2002002643A0 (en) 2000-03-06 2002-12-31 Warner Lambert Co 5-alkylpyrido[2,3-d]pyrimidines tyrosine kinase inhibitors
KR100774855B1 (ko) 2000-04-27 2007-11-08 아스텔라스세이야쿠 가부시키가이샤 축합 헤테로아릴 유도체
JP4166991B2 (ja) 2001-02-26 2008-10-15 田辺三菱製薬株式会社 ピリドピリミジンまたはナフチリジン誘導体
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
KR20040103972A (ko) 2002-04-19 2004-12-09 스미스클라인 비참 코포레이션 신규 화합물
US20040063658A1 (en) 2002-05-06 2004-04-01 Roberts Christopher Don 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
JP2007504283A (ja) 2003-05-20 2007-03-01 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア β−アミロイド斑に作用物質を結合させる方法
BRPI0507852A (pt) 2004-02-18 2007-07-10 Warner Lambert Co 2-(piridin-3-ilamino)-pirido[2,3-d]pirimidin-7-onas
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
US7767687B2 (en) 2004-12-13 2010-08-03 Biogen Idec Ma Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors
EA016945B1 (ru) * 2005-10-07 2012-08-30 Экселиксис, Инк. ПИРИДОПИРИМИДИНОНОВЫЕ ИНГИБИТОРЫ PI3Kα
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
PT2074122E (pt) * 2006-09-15 2011-08-24 Pfizer Prod Inc Compostos de pirido(2,3-d)-pirimidinona e sua utilização como inibidores de pi3
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
EP2350070A1 (en) 2011-08-03
US8101622B2 (en) 2012-01-24
PA8843901A1 (es) 2010-05-26
JP2012504628A (ja) 2012-02-23
US20100087456A1 (en) 2010-04-08
WO2010039740A1 (en) 2010-04-08
AR073524A1 (es) 2010-11-10
UY32153A (es) 2011-04-29

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
JP2026053668A (ja) Tyk2阻害剤およびその使用
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
US11304929B2 (en) Tosylacetate based compounds and derivatives thereof as PHGDH inhibitors
JPWO2004043936A1 (ja) Plk阻害剤
TW201144318A (en) Activators of AMPK and therapeutic uses thereof
TW201014841A (en) Tri-substituted pyrimidine compounds and their use as PDE10 inhibitors
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
TW200845997A (en) 2-substituted-6-heterocyclic pyrimidone derivatives
JP2021503479A (ja) 置換ヘテロアリール化合物及び使用方法
TW201105673A (en) Novel 1,2,3,4-tetrahydropyrimido{1,2-a}pyrimidin-6-one derivatives, preparation thereof and pharmaceutical use thereof
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
WO2022007921A1 (zh) 三嗪类化合物及其组合物和用途
CN116947764A (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
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
CN103384667A (zh) 作为PI3K/mTOR抑制剂的苯并氧氮杂卓及其使用和生产方法
TW202448451A (zh) 新穎噻吩并[3,2—b]吡啶衍生物