CN102171194A - 嘧啶化合物、组合物和使用方法 - Google Patents

嘧啶化合物、组合物和使用方法 Download PDF

Info

Publication number
CN102171194A
CN102171194A CN200980139005XA CN200980139005A CN102171194A CN 102171194 A CN102171194 A CN 102171194A CN 200980139005X A CN200980139005X A CN 200980139005XA CN 200980139005 A CN200980139005 A CN 200980139005A CN 102171194 A CN102171194 A CN 102171194A
Authority
CN
China
Prior art keywords
phenyl
pyrimidin
tetrahydropyrido
urea
methylmorpholino
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
CN200980139005XA
Other languages
English (en)
Chinese (zh)
Inventor
菲利普·伯杰龙
弗雷德里克·科恩
安东尼·埃斯特拉达
迈克尔·F·T·凯勒
凯文·H·L·劳
C·李
约瑟夫·P·利西卡托斯
丹尼尔·F·奥特瓦恩
裴中华
赵宪瑞
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Genentech Inc
Original Assignee
Genentech 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 Genentech Inc filed Critical Genentech Inc
Publication of CN102171194A publication Critical patent/CN102171194A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
CN200980139005XA 2008-07-31 2009-07-31 嘧啶化合物、组合物和使用方法 Pending CN102171194A (zh)

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 (1)

Publication Number Publication Date
CN102171194A true CN102171194A (zh) 2011-08-31

Family

ID=41610758

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200980139005XA Pending CN102171194A (zh) 2008-07-31 2009-07-31 嘧啶化合物、组合物和使用方法

Country Status (23)

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

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105143226A (zh) * 2013-03-08 2015-12-09 沃克哈特有限公司 制备(2s,5r)-2-甲酰胺基-7-氧代-6-磺酰氧基-1,6-二氮杂-双环[3.2.1]辛烷的钠盐的方法
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
CN117164590A (zh) * 2022-05-25 2023-12-05 沈阳药科大学 稠合嘧啶类衍生物及其应用
CN118538308A (zh) * 2024-07-12 2024-08-23 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

Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0974129B1 (en) * 1996-09-04 2006-08-16 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
EP2318377B1 (en) 2008-07-31 2013-08-21 Genentech, Inc. 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
BR112012011188A2 (pt) * 2009-11-12 2021-06-29 F.Hoffmann - La Roche Ag ''composto,composição farmacêutica e uso de um composto"
US8828990B2 (en) * 2009-11-12 2014-09-09 Genentech, Inc. N-7 substituted purine and pyrazolopyrimine compounds, compositions and methods of use
ES2535116T3 (es) 2010-03-04 2015-05-05 Cellzome Limited Derivados de urea sustituida con morfolino como inhibidores de mtor
WO2011113512A1 (de) 2010-03-16 2011-09-22 Merck Patent Gmbh Morpholinylchinazoline
HUE029196T2 (en) 2010-06-04 2017-02-28 Hoffmann La Roche Aminoprimidine derivatives as LRRK2 modulators
EP2608668B1 (en) * 2010-08-23 2016-06-01 Merck Sharp & Dohme Corp. Fused tricyclic inhibitors of mammalian target of rapamycin
BR112013011600B1 (pt) 2010-11-10 2022-01-11 Genentech, Inc Derivados de pirazol aminopirimidina, seu uso e composição que os compreende
MX2013006858A (es) 2010-12-16 2013-07-29 Hoffmann La Roche Compuesto triciclicos inhibidores de la pi3k y metodos de uso.
TR201815685T4 (tr) * 2011-04-01 2018-11-21 Genentech Inc Kanser tedavisi için akt ve mek inhibe edici bileşiklerin kombinasyonları.
SG10201504303SA (en) 2011-04-01 2015-07-30 Genentech Inc Combinations Of AKT Inhibitor Compounds And Chemotherapeutic Agents, And Methods Of Use
EP2694511A1 (en) * 2011-04-04 2014-02-12 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
US20130025281A1 (en) 2011-07-27 2013-01-31 Rentech, Inc. Gasification system and method
JP5995975B2 (ja) 2011-09-21 2016-09-21 セルゾーム リミテッド Ｍｔｏｒ阻害剤としてのモルホリノ置換尿素またはカルバメート誘導体
WO2013050508A1 (en) 2011-10-07 2013-04-11 Cellzome Limited Morpholino substituted bicyclic pyrimidine urea or carbamate derivatives as mtor inhibitors
AR089284A1 (es) 2011-12-22 2014-08-13 Galapagos Nv Dihidropirimidinoisoquinolinonas y composiciones farmaceuticas de las mismas para el tratamiento de trastornos inflamatorios
US9051311B2 (en) 2012-03-09 2015-06-09 Amgen Inc. Sulfamide sodium channel inhibitors
RU2014149145A (ru) 2012-05-23 2016-07-20 Ф. Хоффманн-Ля Рош Аг Композиции и способы получения и применения эндодермальных клеток и гепатоцитов
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
AU2017266911B2 (en) 2016-05-18 2021-09-02 Array Biopharma, Inc. KRas G12C inhibitors
JOP20190257A1 (ar) * 2017-04-28 2019-10-28 Novartis Ag مركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 واستخدامها كمثبطات lats
CN111315750B (zh) 2017-11-06 2022-12-23 南京明德新药研发有限公司 作为mTORC1/2双激酶抑制剂的吡啶并嘧啶类化合物
SI3710439T1 (sl) * 2017-11-15 2023-06-30 Mirati Therapeutics, Inc., Zaviralci mutacije kras g12c
US10647715B2 (en) 2017-11-15 2020-05-12 Mirati Therapeutics, Inc. KRas G12C inhibitors
JP7569688B2 (ja) 2017-12-22 2024-10-18 ハイバーセル，インコーポレイテッド ホスファチジルイノシトールリン酸キナーゼ阻害剤としてのアミノピリジン誘導体
PT3784666T (pt) 2018-04-24 2022-06-06 Merck Patent Gmbh Compostos antiproliferação e utilizações dos mesmos
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
EP3849536A4 (en) 2018-09-10 2022-06-29 Mirati Therapeutics, Inc. Combination therapies
EP3849538A4 (en) 2018-09-10 2022-06-29 Mirati Therapeutics, Inc. Combination therapies
HRP20250059T1 (hr) 2018-09-10 2025-03-28 Mirati Therapeutics, Inc. Kombinirane terapije
EA202190630A1 (ru) 2018-12-05 2021-10-11 Мирати Терапьютикс, Инк. Способы комбинированной терапии
WO2020146613A1 (en) 2019-01-10 2020-07-16 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
JP7622043B2 (ja) 2019-08-29 2025-01-27 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｄ阻害剤
CA3152025A1 (en) 2019-09-24 2021-04-01 David BRIERE Combination therapies
EP4076418A4 (en) 2019-12-20 2024-01-24 Mirati Therapeutics, Inc. Sos1 inhibitors
JP2023540809A (ja) 2020-09-11 2023-09-26 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阻害剤の結晶形態
CN116323623B (zh) 2020-09-18 2025-09-26 拜耳公司 作为SOS1抑制剂的吡啶并[2,3-d]嘧啶-4-胺
IL303446A (en) 2020-12-15 2023-08-01 Mirati Therapeutics Inc Azaquinazoline compounds as PAN-KRas inhibitors
WO2022133038A1 (en) 2020-12-16 2022-06-23 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
EP4074317A1 (en) 2021-04-14 2022-10-19 Bayer AG Phosphorus derivatives as novel sos1 inhibitors

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1141298A (zh) * 1995-06-07 1997-01-29 美国辉瑞有限公司 杂环稠合嘧啶衍生物
US20040043986A1 (en) * 2002-08-13 2004-03-04 Joe Nahra 5,6-Fused 3,4-dihydropyrimidine-2-one derivatives as matrix metalloproteinase inhibitors
CN1486312A (zh) * 2000-12-21 2004-03-31 ��̩��˹ҩ��ɷ����޹�˾ 可用作蛋白激酶抑制剂的吡唑化合物
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

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1197466B (de) 1962-03-22 1965-07-29 Thomae Gmbh Dr K Verfahren zur Herstellung von neuen 5, 6, 7, 8-Tetrahydropyrido-[4, 3-d]pyrimidinen
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
PL204628B1 (pl) * 1998-06-02 2010-01-29 Osi Pharmaceuticals Pochodna pirolo[2,3d]pirymidyny, jej zastosowanie i sposoby wytwarzania tej pochodnej i preparaty farmaceutyczne
JP3810017B2 (ja) * 2000-04-27 2006-08-16 アステラス製薬株式会社 縮合ヘテロアリール誘導体
US6608053B2 (en) * 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
WO2001083456A1 (en) * 2000-04-27 2001-11-08 Yamanouchi Pharmaceutical Co., Ltd. Condensed heteroaryl derivatives
ATE346064T1 (de) 2000-09-15 2006-12-15 Vertex Pharma Pyrazolverbindungen als protein-kinasehemmer
US7105667B2 (en) * 2001-05-01 2006-09-12 Bristol-Myers Squibb Co. Fused heterocyclic compounds and use thereof
WO2002088079A2 (en) 2001-05-01 2002-11-07 Bristol-Myers Squibb Company Dual inhibitors of pde 7 and pde 4
PE20030008A1 (es) * 2001-06-19 2003-01-22 Bristol Myers Squibb Co Inhibidores duales de pde 7 y pde 4
DE60236322D1 (de) * 2001-12-07 2010-06-17 Vertex Pharma Verbindungen auf pyrimidin-basis als gsk-3-hemmer
US7091343B2 (en) * 2002-03-15 2006-08-15 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
EP1552842A1 (en) * 2002-06-07 2005-07-13 Kyowa Hakko Kogyo Co., Ltd. Bicyclic pyrimidine derivatives
US7208498B2 (en) * 2002-07-15 2007-04-24 Merck & Co., Inc. Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
US7129351B2 (en) * 2002-11-04 2006-10-31 Hoffmann-La Roche Inc. Pyrimido compounds having antiproliferative activity
EP1608631A4 (en) * 2003-03-28 2008-08-20 Scios Inc BICYCLIC PYRIMIDININHIBITORS OF TGF BETA
ATE440825T1 (de) * 2003-06-06 2009-09-15 Vertex Pharma Pyrimidin-derivate zur verwendung als modulatoren von atp-bindende kassette transportern
EP1663994B1 (en) * 2003-08-05 2012-03-07 Vertex Pharmaceuticals Incorporated Tetrahydroquinazoline compounds as inhibitors of voltage-gated ion channels
US7312330B2 (en) 2003-12-24 2007-12-25 Renovis, Inc. Bicycloheteroarylamine compounds as ion channel ligands and uses thereof
TW200530235A (en) 2003-12-24 2005-09-16 Renovis Inc Bicycloheteroarylamine compounds as ion channel ligands and uses thereof
US20050187389A1 (en) * 2004-01-13 2005-08-25 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
EP1799218A1 (en) 2004-09-30 2007-06-27 Tibotec Pharmaceuticals Ltd. Hcv inhibiting bi-cyclic pyrimidines
WO2006042102A2 (en) * 2004-10-05 2006-04-20 Neurogen Corporation Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds
EP1806347A4 (en) * 2004-10-08 2009-07-01 Astellas Pharma Inc PYRIMIDINE DERIVATIVES FUSED WITH AN AROMATIC RING
TW200621257A (en) * 2004-10-20 2006-07-01 Astellas Pharma Inc Pyrimidine derivative fused with nonaromatic ring
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
CA2588220A1 (en) 2004-12-23 2006-06-29 Pfizer Products Inc. Heteroaromatic derivatives useful as anticancer agents
KR20070113252A (ko) 2005-02-25 2007-11-28 쿠도스 파마슈티칼스 리미티드 2,4-디아미노-피리도피리미딘 유도체 및 이의 ｍＴＯＲ억제제로서의 용도
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
HRP20120963T1 (hr) * 2005-11-22 2012-12-31 Kudos Pharmaceuticals Ltd PIRIDO-, PIRAZO- I PIRIMIDOPIRIMIDINSKI DERIVATI KAO mTOR INHIBITORI
US20110034454A1 (en) 2006-01-11 2011-02-10 Allan Paul Dishington 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
KR101402474B1 (ko) * 2006-04-26 2014-06-19 제넨테크, 인크. 포스포이노시티드 3-키나제 억제제 화합물 및 이를 포함하는 약학적 조성물
BRPI0710874A2 (pt) * 2006-04-26 2012-02-14 Hoffmann La Roche compostos de tienopirimidina, processos de produção dos referidos compostos, composições farmacêuticas contendo os mesmos, kit, produto, e usos dos compostos
MX2008013582A (es) 2006-04-26 2009-01-19 Hoffmann La Roche Derivados de pirimidina como inhibidores de fosfatidilinositol-3-c inasa.
EP2041139B1 (en) * 2006-04-26 2011-11-09 F. Hoffmann-La Roche AG Pharmaceutical compounds
GB0608820D0 (en) 2006-05-04 2006-06-14 Piramed Ltd Pharmaceutical compounds
US8329701B2 (en) 2006-07-06 2012-12-11 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
MX2009002046A (es) 2006-08-24 2009-03-06 Astrazeneca Ab Derivados de morfolino pirimidina utiles en el tratamiento de trastornos proliferativos.
US20090325954A1 (en) 2006-09-14 2009-12-31 Sam Butterworth 2-benzimidazolyl-6-morpholino-4-phenylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
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
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
CN101563340A (zh) 2006-09-14 2009-10-21 阿斯利康(瑞典)有限公司 用作pi3k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-哌啶-4-基嘧啶衍生物
EP2069330A1 (en) 2006-09-14 2009-06-17 AstraZeneca AB 2 -benzimidazolyl- 6 -morpholino-4- (azetidine, pyrrolidine, piperidine or azepine) pyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
KR101507182B1 (ko) * 2006-12-07 2015-03-30 제넨테크, 인크. 포스포이노시타이드 3-키나제 억제제 화합물 및 그의 사용 방법
TWI499420B (zh) * 2006-12-07 2015-09-11 Hoffmann La Roche 肌醇磷脂３-激酶抑制劑化合物及使用方法
EP2094837B1 (en) * 2006-12-14 2012-04-25 Medical Research Council Use of pi3k, m-tor and akt inhibitors to induce foxp3 expression and generate regulatory t cells
US20080234262A1 (en) * 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
US20080233127A1 (en) * 2007-03-21 2008-09-25 Wyeth Imidazolopyrimidine analogs and their use as pi3 kinase and mtor 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
WO2008125839A2 (en) 2007-04-12 2008-10-23 Piramed Limited Pyrimidine derivatives as inhibitors of phosphatidylinositol-3-kinase
WO2008152387A1 (en) 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Quinazoline derivatives as pi3 kinase inhibitors
WO2008152394A1 (en) 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Pharmaceutical compounds
JP5539190B2 (ja) 2007-06-12 2014-07-02 エフ．ホフマン−ラ ロシュ アーゲー チアゾロピリミジン類及びホスファチジルイノシトール−３キナーゼのインヒビターとしてのそれらの使用
CA2704711C (en) * 2007-09-24 2016-07-05 Genentech, Inc. Thiazolopyrimidine p13k inhibitor compounds and methods of use
AU2008312631A1 (en) * 2007-10-16 2009-04-23 Wyeth Llc Thienopyrimidine and pyrazolopyrimidine compounds and their use as mTOR kinase and PI3 kinase inhibitors
WO2009070524A1 (en) 2007-11-27 2009-06-04 Wyeth Pyrrolo[3,2-d]pyrimidine compounds and their use as pi3 kinase and mtor kinase inhibitors
EP2318377B1 (en) 2008-07-31 2013-08-21 Genentech, Inc. Pyrimidine compounds, compositions and methods of use

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1141298A (zh) * 1995-06-07 1997-01-29 美国辉瑞有限公司 杂环稠合嘧啶衍生物
CN1486312A (zh) * 2000-12-21 2004-03-31 ��̩��˹ҩ��ɷ����޹�˾ 可用作蛋白激酶抑制剂的吡唑化合物
US20040043986A1 (en) * 2002-08-13 2004-03-04 Joe Nahra 5,6-Fused 3,4-dihydropyrimidine-2-one derivatives as matrix metalloproteinase 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

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105143226A (zh) * 2013-03-08 2015-12-09 沃克哈特有限公司 制备(2s,5r)-2-甲酰胺基-7-氧代-6-磺酰氧基-1,6-二氮杂-双环[3.2.1]辛烷的钠盐的方法
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
CN117164590A (zh) * 2022-05-25 2023-12-05 沈阳药科大学 稠合嘧啶类衍生物及其应用
CN118538308A (zh) * 2024-07-12 2024-08-23 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
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

Also Published As

Publication number Publication date
ES2432821T3 (es) 2013-12-05
CA2729045A1 (en) 2010-02-04
EP2318377B1 (en) 2013-08-21
EP2318377A4 (en) 2012-05-09
US20120165313A1 (en) 2012-06-28
IL210462A0 (en) 2011-03-31
JP2011529920A (ja) 2011-12-15
NZ590777A (en) 2012-11-30
RU2473549C2 (ru) 2013-01-27
AU2009276339A1 (en) 2010-02-04
CO6311051A2 (es) 2011-08-22
CL2011000191A1 (es) 2011-05-20
MX2011001196A (es) 2011-05-30
PE20110403A1 (es) 2011-07-04
ECSP11010796A (es) 2011-02-28
US20100069357A1 (en) 2010-03-18
ZA201100110B (en) 2012-04-25
WO2010014939A1 (en) 2010-02-04
UA101676C2 (uk) 2013-04-25
AU2009276339B2 (en) 2012-06-07
AR073354A1 (es) 2010-11-03
TW201018681A (en) 2010-05-16
KR20110046514A (ko) 2011-05-04
RU2011107278A (ru) 2012-09-10
US8163763B2 (en) 2012-04-24
BRPI0911688A2 (pt) 2015-07-28
EP2318377A1 (en) 2011-05-11
MA32580B1 (fr) 2011-08-01
AU2009276339A8 (en) 2011-03-03

Similar Documents

Publication Publication Date Title
EP2318377B1 (en) Pyrimidine compounds, compositions and methods of use
TWI891666B (zh) 作為ｆｇｆｒ抑制劑之雙環雜環
JP6496376B2 (ja) 阻害剤化合物
EP3774817B1 (en) Bcl6 inhibitors
KR101469334B1 (ko) Ｎ-9-치환된 퓨린 화합물, 조성물 및 사용 방법
CN115151540A (zh) 作为mettl3抑制剂的多杂环化合物
JP2018150358A (ja) Ｔａｎｋ結合キナーゼインヒビター化合物
CN106459035B (zh) N2‑苯基‑吡啶并[3,4‑d]嘧啶‑2,8‑二胺衍生物及其作为mps1抑制剂的用途
JP2012531422A (ja) オキソ−複素環縮合ピリミジン化合物、組成物及び使用方法
JP2021506979A (ja) ホスファチジルイノシトールリン酸キナーゼ阻害剤としてのアリール−ビピリジンアミン誘導体
CN106188038A (zh) 一类具有激酶抑制活性的化合物、制备方法和用途
CN102712642A (zh) N-7 取代的嘌呤和吡唑并嘧啶化合物、组合物和使用方法
TW202327592A (zh) Cdk9抑制劑及其用途
HK1160466A (en) Pyrimidine compounds, compositions and methods of use
EA050300B1 (ru) Ингибиторы bcl6
HK40046058B (en) Bcl6 inhibitors
HK40046058A (en) Bcl6 inhibitors
HK1172328B (en) N-7 substituted purine and pyrazolopyrimidine compounds, compositions and methods of use
HK1176556B (en) N-9-substituted purine compounds, compositions and methods of use

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1160466

Country of ref document: HK

C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20110831

REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1160466

Country of ref document: HK