JP2011529920A - ピリミジン化合物、組成物及び使用方法 - Google Patents

ピリミジン化合物、組成物及び使用方法 Download PDF

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JP2011529920A
JP2011529920A JP2011521363A JP2011521363A JP2011529920A JP 2011529920 A JP2011529920 A JP 2011529920A JP 2011521363 A JP2011521363 A JP 2011521363A JP 2011521363 A JP2011521363 A JP 2011521363A JP 2011529920 A JP2011529920 A JP 2011529920A
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phenyl
pyrimidin
group
tetrahydropyrido
cancer
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JP2011529920A5 (https=
Inventor
フィリップ ベルジュロン，
フレデリック コーエン，
アンソニー エストラーダ，
マイケル， エフ． ティー． コーラー，
ケヴィン， ホン ルーエン ラウ，
クォン リ，
ジョゼフ， ピー． リッシカトス，
ダニエル， フレッド オートワイン，
チョンファ ペイ，
シャンルイ チャオ，
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ジェネンテック， インコーポレイテッド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/18—Bridged 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2011521363A 2008-07-31 2009-07-31 ピリミジン化合物、組成物及び使用方法 Pending JP2011529920A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US8530908P 2008-07-31 2008-07-31
US61/085,309 2008-07-31
PCT/US2009/052469 WO2010014939A1 (en) 2008-07-31 2009-07-31 Pyrimidine compounds, compositions and methods of use

Publications (2)

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JP2011529920A true JP2011529920A (ja) 2011-12-15
JP2011529920A5 JP2011529920A5 (https=) 2012-09-13

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US (2) US8163763B2 (https=)
EP (1) EP2318377B1 (https=)
JP (1) JP2011529920A (https=)
KR (1) KR20110046514A (https=)
CN (1) CN102171194A (https=)
AR (1) AR073354A1 (https=)
AU (1) AU2009276339B2 (https=)
BR (1) BRPI0911688A2 (https=)
CA (1) CA2729045A1 (https=)
CL (1) CL2011000191A1 (https=)
CO (1) CO6311051A2 (https=)
EC (1) ECSP11010796A (https=)
ES (1) ES2432821T3 (https=)
IL (1) IL210462A0 (https=)
MA (1) MA32580B1 (https=)
MX (1) MX2011001196A (https=)
NZ (1) NZ590777A (https=)
PE (1) PE20110403A1 (https=)
RU (1) RU2473549C2 (https=)
TW (1) TW201018681A (https=)
UA (1) UA101676C2 (https=)
WO (1) WO2010014939A1 (https=)
ZA (1) ZA201100110B (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2020517698A (ja) * 2017-04-28 2020-06-18 ノバルティス アーゲー ６−６縮合二環式ヘテロアリール化合物及びｌａｔｓ阻害剤としてのその使用
JP2021502993A (ja) * 2017-11-15 2021-02-04 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｃ阻害剤

Families Citing this family (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2264819C (en) * 1996-09-04 2010-03-23 Intertrust Technologies Corp. Trusted infrastructure support systems, methods and techniques for secure electronic commerce, electronic transactions, commerce process control and automation, distributed computing, and rights management
CA2725014C (en) 2008-05-30 2014-06-17 Amgen Inc. Inhibitors of pi3 kinase
CA2729045A1 (en) 2008-07-31 2010-02-04 Philippe Bergeron Pyrimidine compounds, compositions and methods of use
JP5579724B2 (ja) * 2008-10-17 2014-08-27 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ホスファチジルイノシトール−３−キナーゼ（ｐｉ−３キナーゼ）阻害剤としてのテトラ−アザ−複素環
ES2529205T3 (es) 2009-03-13 2015-02-17 Cellzome Limited Derivados de pirimidina como inhibidores de mTOR
WO2010120991A1 (en) * 2009-04-17 2010-10-21 Wyeth Llc 5, 6, 7, 8-tetrahydropyrido[4,3-d]pyrimidine compounds, their use as mtor, pi3, and hsmg-1 kinase inhibitors, and their syntheses
WO2010120996A1 (en) * 2009-04-17 2010-10-21 Wyeth Llc 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
UY32582A (es) 2009-04-28 2010-11-30 Amgen Inc Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero
US20100331305A1 (en) * 2009-06-24 2010-12-30 Genentech, Inc. Oxo-heterocycle fused pyrimidine compounds, compositions and methods of use
JP5579864B2 (ja) * 2009-11-12 2014-08-27 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト Ｎ−９−置換プリン化合物、組成物及び使用の方法
EP2499143B1 (en) * 2009-11-12 2016-03-16 F.Hoffmann-La Roche Ag N7-substituted purine and pyrazolopyrimidine compounds, compositions and methods of use
EP2542536B1 (en) 2010-03-04 2015-01-21 Cellzome Limited Morpholino substituted urea derivatives as mtor inhibitors
BR112012022868A2 (pt) * 2010-03-16 2018-06-05 Merck Patent Gmbh morfolinilquinazolinas
ES2577829T3 (es) 2010-06-04 2016-07-19 F. Hoffmann-La Roche Ag Derivados de aminopirimidina como moduladores de la LRRK2
EP2608668B1 (en) * 2010-08-23 2016-06-01 Merck Sharp & Dohme Corp. Fused tricyclic inhibitors of mammalian target of rapamycin
NO2638031T3 (https=) 2010-11-10 2018-03-10
TW201500358A (zh) 2010-12-16 2015-01-01 赫夫門羅氏藥廠股份有限公司 三環ｐｉ３ｋ抑制劑化合物及其使用方法
WO2012135781A1 (en) * 2011-04-01 2012-10-04 Genentech, Inc. Combinations of akt inhibitor compounds and chemotherapeutic agents, and methods of use
RU2013148817A (ru) * 2011-04-01 2015-05-10 Дженентек, Инк. Комбинации соединений-ингибиторов акт и мек и способы их применения
WO2012136622A1 (en) 2011-04-04 2012-10-11 Cellzome Limited Dihydropyrrolo pyrimidine derivatives as mtor inhibitors
US8846656B2 (en) * 2011-07-22 2014-09-30 Novartis Ag Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators
US9101900B2 (en) 2011-07-27 2015-08-11 Res Usa, Llc Gasification system and method
WO2013041652A1 (en) 2011-09-21 2013-03-28 Cellzome Limited Morpholino substituted urea or carbamate derivatives as mtor inhibitors
KR20140084130A (ko) 2011-10-07 2014-07-04 셀좀 리미티드 Mtor 억제제로서의 모르폴리노 치환된 바이사이클릭 피리미딘 우레아 또는 카르바메이트 유도체
AR089284A1 (es) 2011-12-22 2014-08-13 Galapagos Nv Dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios
WO2013134518A1 (en) 2012-03-09 2013-09-12 Amgen Inc. Sulfamide sodium channel inhibitors
KR20160027219A (ko) 2012-05-23 2016-03-09 에프. 호프만-라 로슈 아게 내배엽 및 간세포를 수득하고 사용하는 조성물 및 방법
CA2904089C (en) * 2013-03-08 2017-05-02 Wockhardt Limited A process for sodium salt of (2s, 5r)-2-carboxamido-7-oxo-6-sulfooxy -1,6-diaza-bicyclo[3.2.1]octane
RU2649141C2 (ru) * 2015-04-20 2018-03-30 государственное бюджетное образовательное учреждение высшего профессионального образования "Пермская государственная фармацевтическая академия" Министерства здравоохранения Российской Федерации (ГБОУ ВПО ПГФА Минздрава России) 3,4-диметил-6-(3-пиридил)-N-фенил-2-оксо-1,2,3,6-тетрагидропиримидин-5-карбоксамид, проявляющий противогрибковое действие в отношении штамма Candida albicans
CN106467538B (zh) * 2015-08-14 2019-03-05 沈阳中化农药化工研发有限公司 一种取代的四氢异喹啉化合物与用途
WO2017164705A1 (ko) * 2016-03-24 2017-09-28 재단법인 대구경북첨단의료산업진흥재단 신규한 피리딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 fgfr 관련 질환의 예방 또는 치료용 약학적 조성물
KR102444509B1 (ko) 2016-05-18 2022-09-19 미라티 테라퓨틱스, 인크. Kras g12c 억제제
JP7340519B2 (ja) * 2017-11-06 2023-09-07 メッドシャイン ディスカバリー インコーポレイテッド ｍＴＯＲＣ１／２二重阻害剤としてのピリドピリミジン系化合物
US10647715B2 (en) 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
WO2019126731A1 (en) 2017-12-22 2019-06-27 Petra Pharma Corporation Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
HRP20241163T1 (hr) 2018-04-24 2024-11-22 Merck Patent Gmbh Antiproliferacijski spojevi i njihova uporaba
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
EP3849535A4 (en) 2018-09-10 2022-06-29 Mirati Therapeutics, Inc. Combination therapies
JP2022500385A (ja) 2018-09-10 2022-01-04 ミラティ セラピューティクス， インコーポレイテッド 組み合わせ療法
EP3849537B1 (en) 2018-09-10 2024-10-23 Mirati Therapeutics, Inc. Combination therapies
EA202190749A1 (ru) 2018-09-10 2021-07-09 Мирати Терапьютикс, Инк. Способы комбинированной терапии
MX2021002804A (es) 2018-12-05 2021-07-15 Mirati Therapeutics Inc Terapias de combinacion.
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
GB201905222D0 (en) * 2019-04-12 2019-05-29 Airspan Networks Inc Air-to-ground (ATG) communication technologies
TW202112767A (zh) 2019-06-17 2021-04-01 美商佩特拉製藥公司 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物
MX2022002465A (es) 2019-08-29 2022-05-19 Mirati Therapeutics Inc Inhibidores de kras g12d.
WO2021061749A1 (en) 2019-09-24 2021-04-01 Mirati Therapeutics, Inc. Combination therapies
PH12022551513A1 (en) 2019-12-20 2023-04-24 Mirati Therapeutics Inc Sos1 inhibitors
EP4210833A4 (en) 2020-09-11 2024-09-11 Mirati Therapeutics, Inc. CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR
US20230357239A1 (en) 2020-09-18 2023-11-09 Bayer Aktiengesellschaft Pyrido[2,3-d]pyrimidin-4-amines as sos1 inhibitors
JP2023553492A (ja) 2020-12-15 2023-12-21 ミラティ セラピューティクス， インコーポレイテッド アザキナゾリン汎ＫＲａｓ阻害剤
EP4262803A4 (en) 2020-12-16 2025-03-12 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
EP4074317A1 (en) 2021-04-14 2022-10-19 Bayer AG Phosphorus derivatives as novel sos1 inhibitors
CN115466258A (zh) * 2021-06-11 2022-12-13 成都苑东生物制药股份有限公司 Atr抑制剂及其用途
CN117164590B (zh) * 2022-05-25 2026-03-17 沈阳药科大学 稠合嘧啶类衍生物及其应用
CN118538308B (zh) * 2024-07-12 2024-11-22 碳氢数科(成都)信息技术有限公司 化学反应数据挖掘方法、系统、存储介质及终端

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3248395A (en) * 1962-03-22 1966-04-26 Boehringer Sohn Ingelheim 4-amino-5, 6, 7, 8-tetrahydro-pyrido-[4, 3-d]-pyrimidine substitution products
JPH10508875A (ja) * 1995-06-07 1998-09-02 ファイザー・インコーポレーテッド 複素環式の縮合環ピリミジン誘導体
US20040043986A1 (en) * 2002-08-13 2004-03-04 Joe Nahra 5,6-Fused 3,4-dihydropyrimidine-2-one derivatives as matrix metalloproteinase inhibitors
JP2005120102A (ja) * 2000-04-27 2005-05-12 Yamanouchi Pharmaceut Co Ltd 縮合ヘテロアリール誘導体
WO2006043490A1 (ja) * 2004-10-20 2006-04-27 Astellas Pharma Inc. 非芳香環縮合ピリミジン誘導体
US20060258658A1 (en) * 2000-09-15 2006-11-16 David Bebbington Triazole compounds useful as protein kinase inhibitors
WO2007060404A1 (en) * 2005-11-22 2007-05-31 Kudos Pharmaceuticals Limited PYRIDO-,PYRAZO- AND PYRIMIDO-PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
WO2007106503A2 (en) * 2006-03-13 2007-09-20 Osi Pharmaceuticals, Inc. Combined treatment with an egfr kinase inhibitor and an agent that sensitizes tumor cells to the effects of egfr kinase inhibitors
WO2008023161A1 (en) * 2006-08-23 2008-02-28 Kudos Pharmaceuticals Limited 2-methylmorpholine pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as mtor inhibitors
GB2444853A (en) * 2006-12-14 2008-06-18 Medical Res Council Production of regulatory T cells

Family Cites Families (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH04224580A (ja) 1990-12-25 1992-08-13 Nippon Soda Co Ltd ピリミジン誘導体、その製造方法及び農園芸用殺菌剤
US5338740A (en) 1993-07-13 1994-08-16 Pfizer Inc. Angiotensin II receptor antagonists
US5942508A (en) 1997-02-04 1999-08-24 Senju Pharmaceutical Co., Ltd. Method for solubilizing pyridonecarboxylic acid solubilizer thereof and aqueous solution containing solubilized pyridonecarboxylic acid
US6187777B1 (en) 1998-02-06 2001-02-13 Amgen Inc. Compounds and methods which modulate feeding behavior and related diseases
JP4611524B2 (ja) 1998-06-02 2011-01-12 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド ピロロ［２，３ｄ］ピリミジン組成物およびその使用
KR100774855B1 (ko) * 2000-04-27 2007-11-08 아스텔라스세이야쿠 가부시키가이샤 축합 헤테로아릴 유도체
US6608053B2 (en) 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
US6989385B2 (en) * 2000-12-21 2006-01-24 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
WO2002088079A2 (en) 2001-05-01 2002-11-07 Bristol-Myers Squibb Company Dual inhibitors of pde 7 and pde 4
US7105667B2 (en) 2001-05-01 2006-09-12 Bristol-Myers Squibb Co. Fused heterocyclic compounds and use thereof
PE20030008A1 (es) 2001-06-19 2003-01-22 Bristol Myers Squibb Co Inhibidores duales de pde 7 y pde 4
ATE466581T1 (de) 2001-12-07 2010-05-15 Vertex Pharma Verbindungen auf pyrimidin-basis als gsk-3-hemmer
DE60332433D1 (de) 2002-03-15 2010-06-17 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
JPWO2003104230A1 (ja) 2002-06-07 2005-10-06 協和醗酵工業株式会社 二環性ピリミジン誘導体
US7208498B2 (en) 2002-07-15 2007-04-24 Merck & Co., Inc. Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
US7112676B2 (en) * 2002-11-04 2006-09-26 Hoffmann-La Roche Inc. Pyrimido compounds having antiproliferative activity
US7223766B2 (en) 2003-03-28 2007-05-29 Scios, Inc. Bi-cyclic pyrimidine inhibitors of TGFβ
EP1646615B1 (en) 2003-06-06 2009-08-26 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives as modulators of atp-binding cassette transporters
CN1894222A (zh) 2003-08-05 2007-01-10 沃泰克斯药物股份有限公司 作为电压门控离子通道抑制剂的稠合嘧啶化合物
TW200530235A (en) 2003-12-24 2005-09-16 Renovis Inc Bicycloheteroarylamine compounds as ion channel ligands and uses thereof
US7312330B2 (en) 2003-12-24 2007-12-25 Renovis, Inc. Bicycloheteroarylamine compounds as ion channel ligands and uses thereof
US20050239806A1 (en) 2004-01-13 2005-10-27 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
KR20070058602A (ko) 2004-09-30 2007-06-08 티보텍 파마슈티칼즈 리미티드 Ｈｃｖ 저해 바이-사이클릭 피리미딘
WO2006042102A2 (en) 2004-10-05 2006-04-20 Neurogen Corporation Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds
US7557112B2 (en) * 2004-10-08 2009-07-07 Astellas Pharma Inc. Aromatic-ring-fused pyrimidine derivative
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
US20060128710A1 (en) 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
JP2008525422A (ja) 2004-12-23 2008-07-17 ファイザー・プロダクツ・インク 抗癌剤として有用な複素芳香族誘導体
JP2008531538A (ja) 2005-02-25 2008-08-14 クドス ファーマシューティカルズ リミテッド ２，４−ジアミノ−ピリドピリミジン誘導体とｍＴＯＲ阻害剤としてのその使用
GB0520657D0 (en) 2005-10-11 2005-11-16 Ludwig Inst Cancer Res Pharmaceutical compounds
GB2431156A (en) 2005-10-11 2007-04-18 Piramed Ltd 1-cyclyl-3-substituted- -benzenes and -azines as inhibitors of phosphatidylinositol 3-kinase
EP1979325A1 (en) 2006-01-11 2008-10-15 AstraZeneca AB Morpholino pyrimidine derivatives and their use in therapy
PE20080145A1 (es) 2006-03-21 2008-02-11 Janssen Pharmaceutica Nv Tetrahidro-pirimidoazepinas como moduladores de trpv1
TWI498332B (zh) 2006-04-26 2015-09-01 Hoffmann La Roche 作為pi3k抑制劑之嘧啶衍生物及相關製備方法、醫藥組合物、用途、套組及產物
WO2007129161A2 (en) 2006-04-26 2007-11-15 F. Hoffmann-La Roche Ag Thieno [3, 2-d] pyrimidine derivative useful as pi3k inhibitor
TW200801012A (en) 2006-04-26 2008-01-01 Piramed Ltd Phosphoinositide 3-kinase inhibitor compounds and methods of use
KR20090021155A (ko) 2006-04-26 2009-02-27 에프. 호프만-라 로슈 아게 Ｐｉ3ｋ 억제제로서의 피리미딘 유도체
GB0608820D0 (en) 2006-05-04 2006-06-14 Piramed Ltd Pharmaceutical compounds
CA2656566C (en) 2006-07-06 2014-06-17 Array Biopharma Inc. Dihydrofuro pyrimidines as akt protein kinase inhibitors
WO2008021456A2 (en) 2006-08-16 2008-02-21 Cytovia, Inc. N-aryl-5,7-dihydrofuro[3,4-d]pyrimidin-4-amines and analogs as activators of caspases and inducers of apoptosis and the use thereof
AU2007287428B2 (en) 2006-08-24 2011-08-11 Astrazeneca Ab Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders
WO2008032089A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidaz0lyl-2-m0rph0lin0-6-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
CN101535296A (zh) 2006-09-14 2009-09-16 阿斯利康(瑞典)有限公司 作为p13k和mtor抑制剂用于治疗增殖性疾病的2-苯并咪唑基-6-吗啉代-4-苯基嘧啶衍生物
EP2064203A1 (en) 2006-09-14 2009-06-03 AstraZeneca AB 2-benzimidaz0lyl-6-m0rph0lin0-4-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
JP2010503648A (ja) 2006-09-14 2010-02-04 アストラゼネカ アクチボラグ 増殖性疾患の治療のためのｐｉ３ｋ及びｍｔｏｒ阻害剤としての２−ベンゾイミダゾリル−６−モルホリノ−４−（アゼチジン、ピロリジン、ピペリジン、又はアゼピン）ピリミジン誘導体
WO2008032033A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidazolyl-2-morpholino-6-piperazinylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032060A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidaz0lyl-6-m0rph0lin0-2-piperazinylpyrimidine derivatives as p13k and mtor inhibitors for the treatment of proliferative disorders
WO2008032036A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 6-benzimidaz0lyl-2-m0rph0lin0-4- (azetidine, pyrrolidine, piperidine or azepine) pyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
MX2009005950A (es) 2006-12-07 2009-10-12 Genentech Inc Compuestos inhibidores de fosfoinositido 3-quinasas y metodos de uso.
RU2470936C2 (ru) 2006-12-07 2012-12-27 Дженентек, Инк. Соединения-ингибиторы фосфоинозитид 3-киназы и способы применения
US20080233127A1 (en) * 2007-03-21 2008-09-25 Wyeth Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors
US20080234262A1 (en) * 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
EP2146981A1 (en) 2007-04-12 2010-01-27 F. Hoffmann-Roche AG Pharmaceutical compounds
GB0707087D0 (en) 2007-04-12 2007-05-23 Piramed Ltd Pharmaceutical compounds
JP2010523639A (ja) 2007-04-12 2010-07-15 エフ．ホフマン−ラ ロシュ アーゲー 医薬化合物
WO2008152387A1 (en) 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Quinazoline derivatives as pi3 kinase inhibitors
US7893060B2 (en) 2007-06-12 2011-02-22 F. Hoffmann-La Roche Ag Thiazolopyrimidines and their use as inhibitors of phosphatidylinositol-3 kinase
WO2008152394A1 (en) 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Pharmaceutical compounds
CA2704711C (en) 2007-09-24 2016-07-05 Genentech, Inc. Thiazolopyrimidine p13k inhibitor compounds and methods of use
EA201000484A1 (ru) 2007-10-16 2010-12-30 ВАЙЕТ ЭлЭлСи Тиенопиримидиновые и пиразолопиримидиновые соединения и их применение в качестве ингибиторов киназы mtor и киназы pi3
US20090149458A1 (en) 2007-11-27 2009-06-11 Wyeth PYRROLO[3,2-d]PYRIMIDINE COMPOUNDS AND THEIR USE AS PI3 KINASE AND mTOR KINASE INHIBITORS
CA2729045A1 (en) 2008-07-31 2010-02-04 Philippe Bergeron Pyrimidine compounds, compositions and methods of use

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3248395A (en) * 1962-03-22 1966-04-26 Boehringer Sohn Ingelheim 4-amino-5, 6, 7, 8-tetrahydro-pyrido-[4, 3-d]-pyrimidine substitution products
JPH10508875A (ja) * 1995-06-07 1998-09-02 ファイザー・インコーポレーテッド 複素環式の縮合環ピリミジン誘導体
JP2005120102A (ja) * 2000-04-27 2005-05-12 Yamanouchi Pharmaceut Co Ltd 縮合ヘテロアリール誘導体
US20060258658A1 (en) * 2000-09-15 2006-11-16 David Bebbington Triazole compounds useful as protein kinase inhibitors
US20040043986A1 (en) * 2002-08-13 2004-03-04 Joe Nahra 5,6-Fused 3,4-dihydropyrimidine-2-one derivatives as matrix metalloproteinase inhibitors
WO2006043490A1 (ja) * 2004-10-20 2006-04-27 Astellas Pharma Inc. 非芳香環縮合ピリミジン誘導体
WO2007060404A1 (en) * 2005-11-22 2007-05-31 Kudos Pharmaceuticals Limited PYRIDO-,PYRAZO- AND PYRIMIDO-PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
WO2007106503A2 (en) * 2006-03-13 2007-09-20 Osi Pharmaceuticals, Inc. Combined treatment with an egfr kinase inhibitor and an agent that sensitizes tumor cells to the effects of egfr kinase inhibitors
WO2008023161A1 (en) * 2006-08-23 2008-02-28 Kudos Pharmaceuticals Limited 2-methylmorpholine pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as mtor inhibitors
GB2444853A (en) * 2006-12-14 2008-06-18 Medical Res Council Production of regulatory T cells

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2020517698A (ja) * 2017-04-28 2020-06-18 ノバルティス アーゲー ６−６縮合二環式ヘテロアリール化合物及びｌａｔｓ阻害剤としてのその使用
US11458138B2 (en) 2017-04-28 2022-10-04 Novartis Ag 6-6 fused bicyclic heteroaryl compounds and their use as LATS inhibitors
JP7247102B2 (ja) 2017-04-28 2023-03-28 ノバルティス アーゲー ６－６縮合二環式ヘテロアリール化合物及びｌａｔｓ阻害剤としてのその使用
JP2021502993A (ja) * 2017-11-15 2021-02-04 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｃ阻害剤
JP7322019B2 (ja) 2017-11-15 2023-08-07 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｃ阻害剤

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