JP2012504628A - PI3KαおよびmTORのピリドピリミジノン阻害剤 - Google Patents

PI3KαおよびmTORのピリドピリミジノン阻害剤 Download PDF

Info

Publication number
JP2012504628A
JP2012504628A JP2011530150A JP2011530150A JP2012504628A JP 2012504628 A JP2012504628 A JP 2012504628A JP 2011530150 A JP2011530150 A JP 2011530150A JP 2011530150 A JP2011530150 A JP 2011530150A JP 2012504628 A JP2012504628 A JP 2012504628A
Authority
JP
Japan
Prior art keywords
formula
compound
cancer
pharmaceutically acceptable
compounds
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
JP2011530150A
Other languages
English (en)
Japanese (ja)
Other versions
JP2012504628A5 (enExample
Inventor
テ−ゴン ベク,
シュンフン マ,
クリス エー. ブーア,
ジョン エム. ナス,
Original Assignee
エグゼリクシス, インコーポレイテッド
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 エグゼリクシス, インコーポレイテッド filed Critical エグゼリクシス, インコーポレイテッド
Publication of JP2012504628A publication Critical patent/JP2012504628A/ja
Publication of JP2012504628A5 publication Critical patent/JP2012504628A5/ja
Pending legal-status Critical Current

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)
JP2011530150A 2008-09-30 2009-09-29 PI3KαおよびmTORのピリドピリミジノン阻害剤 Pending JP2012504628A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US19476108P 2008-09-30 2008-09-30
US61/194,761 2008-09-30
PCT/US2009/058881 WO2010039740A1 (en) 2008-09-30 2009-09-29 PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα AND MTOR

Publications (2)

Publication Number Publication Date
JP2012504628A true JP2012504628A (ja) 2012-02-23
JP2012504628A5 JP2012504628A5 (enExample) 2012-11-15

Family

ID=41572575

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2011530150A Pending JP2012504628A (ja) 2008-09-30 2009-09-29 PI3KαおよびmTORのピリドピリミジノン阻害剤

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
HRP20130902T1 (hr) * 2005-10-07 2013-11-08 Exelixis Inc. PIRIDOPIRIMIDINONSKI INHIBITORI PI3Kalfa
HRP20140975T1 (hr) * 2005-10-07 2014-11-21 Exelixis, Inc. Derivati n-(3-amino-hinoksalin-2-il)-sulfonamida i njihova uporaba kao inhibitora fosfatidilinozitol 3-kinaze
CA2658725A1 (en) 2006-08-16 2008-02-21 Exelixis, Inc. Using pi3k and mek modulators in treatments of cancer
CA2663401C (en) * 2006-09-15 2011-07-12 Pfizer Products Inc. Pyrido (2, 3-d) pyrimidinone compounds and their use as pi3 inhibitors
PT2139484E (pt) * 2007-04-10 2013-10-31 Exelixis Inc Métodos de tratamento de cancro usando inibidores piridopirimidinona de 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
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
TWI642670B (zh) 2010-09-14 2018-12-01 伊塞利克斯公司 Pi3k-德爾塔抑制劑以及其應用和生產方法
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
MX2013012486A (es) * 2011-04-29 2014-05-28 Exelixis Inc Metodo para tratar linfoma usando inhibidores de piridopirimidinona de fosfonio sitol 3-cinasa/diana de rapalamina en celulas de mamifero (pi3k/mtor).
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
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
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment
AU2020288610A1 (en) 2019-06-04 2022-01-27 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
CN113577080B (zh) * 2020-04-30 2022-12-09 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
ES2301194T3 (es) 1997-02-05 2008-06-16 Warner-Lambert Company Llc Pirido 2,3-d pirimidinas y 4-aminopirimidinas como inhibidores de la proliferacion celular.
SK10772002A3 (sk) 2000-01-27 2004-01-08 Warner-Lambert Company Pyridopyrimidinónové deriváty na liečbu neurodegeneratívnych ochorení
AP2002002643A0 (en) 2000-03-06 2002-12-31 Warner Lambert Co 5-alkylpyrido[2,3-d]pyrimidines tyrosine kinase inhibitors
AU5261001A (en) 2000-04-27 2001-11-12 Imperial Cancer Research Technology Ltd Condensed heteroaryl derivatives
EP1364950A4 (en) 2001-02-26 2005-03-09 Tanabe Seiyaku Co Pyridopyrimidine and naphthyridine derivatives
EP1408985A4 (en) * 2001-06-21 2006-03-22 Ariad Pharma Inc NEW PYRIDOPYRIMIDONE AND ITS USES
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
BR0309581A (pt) 2002-05-06 2005-03-29 Genelabs Tech Inc Derivados de nucleosìdeo para tratamento de infecção por vìrus de hepatite c
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
WO2005040337A2 (en) 2003-05-20 2005-05-06 The Regents Of The University Of California METHODS FOR BINDING AGENTS TO β-AMYLOID PLAQUES
CA2555724A1 (en) 2004-02-18 2005-09-09 Warner-Lambert Company Llc 2-(pyridin-3-ylamino)-pyrido[2,3-d]pyrimidin-7-ones
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
HRP20130902T1 (hr) * 2005-10-07 2013-11-08 Exelixis Inc. PIRIDOPIRIMIDINONSKI INHIBITORI PI3Kalfa
PT1940839E (pt) * 2005-10-07 2013-10-10 Exelixis Inc Inibidores de piridopirimidinona pi3k alfa
CA2663401C (en) * 2006-09-15 2011-07-12 Pfizer Products 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
US8101622B2 (en) 2012-01-24
UY32153A (es) 2011-04-29
PA8843901A1 (es) 2010-05-26
US20100087456A1 (en) 2010-04-08
EP2350070A1 (en) 2011-08-03
WO2010039740A1 (en) 2010-04-08
TW201018685A (en) 2010-05-16
AR073524A1 (es) 2010-11-10

Similar Documents

Publication Publication Date Title
US8101622B2 (en) Pyridopyrimidinone inhibitors of PI3Kα and mTOR
JP6416339B2 (ja) 選択的pi3kデルタ阻害剤
US10882858B2 (en) Imidazo[4,5-c]quinolin-2-one compounds and their use in treating cancer
EP2771342B1 (en) Purine derivatives and their use in the treatment of disease
RU2637936C2 (ru) Ингибиторы активности киназы lrrk2
JP6262245B2 (ja) オキサゾリジン−2−オンピリミジン誘導体
JP2010518107A (ja) Pi3−キナーゼ阻害剤およびその使用方法
KR20140117581A (ko) 옥사졸리딘-2-온 화합물 및 pi3k 억제제로서의 그의 용도
KR20180074788A (ko) 암의 치료에 유용한 디하이드로이미다조피라지논 유도체
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
JP2016508484A (ja) 化合物
JP2016041712A (ja) 精製されたピロロキノリニル−ピロリジン−2,5−ジオン組成物ならびにその調製方法および使用方法
TW201307344A (zh) 雜芳基並嘧啶類衍生物、其製備方法和用途
KR20120103553A (ko) 신규 1,2,3,4-테트라히드로-피리미도(1,2-a)피리미딘-6-온 유도체, 그의 제조법 및 그의 제약 용도
US20160002221A1 (en) Substituted Pyridopyrazines as Syk Inhibitors
JP2010509203A (ja) 置換されている8−ピペリジニル−2−ピリジニル−ピリミド[1,2−a]ピリミジン−6−オンおよび8−ピペリジニル−2−ピリミジニル−ピリミド[1,2−a]ピリミジン−6−オン誘導体
KR20190020122A (ko) 라파마이신 신호전달 경로 저해제의 기계적 표적 및 이의 치료학적 적용
JP6557266B2 (ja) Pi3デルタ及びガンマタンパク質キナーゼの選択的二重阻害剤としての置換クロメン誘導体
FR2947551A1 (fr) Nouveaux derives de 1,2,3,4-tetrahydro-pyrimido{1,2-a)pyrimidin-6-one, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt (pkb)
FR2951174A1 (fr) Nouveaux derives de 1,2,3,4-tetrahydro-pyrimido{1,2-a}pyrimidin-6-one, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt(pkb)
HK1236821A1 (en) Oxazolidin-2-one-pyrimidine derivatives for use in the treatment of skin fibrosis, scleroderma, hypertrophic scars or keloids
HK1209108B (en) Oxazolidin-2-one-pyrimidine derivatives

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120928

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20120928

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20140129

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20140428

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20140508

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20140805