CN1551881A - 新颖二氢喋啶酮,其制备方法及作为药物组合物的用途 - Google Patents

新颖二氢喋啶酮,其制备方法及作为药物组合物的用途 Download PDF

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Publication number
CN1551881A
CN1551881A CNA028172884A CN02817288A CN1551881A CN 1551881 A CN1551881 A CN 1551881A CN A028172884 A CNA028172884 A CN A028172884A CN 02817288 A CN02817288 A CN 02817288A CN 1551881 A CN1551881 A CN 1551881A
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Chinese (zh)
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马赛厄斯·霍夫曼
马赛厄斯·格劳尔特
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斯蒂芬·布赖特费尔德
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克里斯琴·艾克迈克
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杰拉尔德·波尔
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索尔斯坦·莱曼－林茨
诺伯特·雷德曼
吉塞拉·施纳普
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马丁·斯蒂格梅尔
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埃克哈特·鲍尔
J
詹斯·J·匡特
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Boehringer Ingelheim Pharma GmbH and Co KG
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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Transplantation (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
CNA028172884A 2001-09-04 2002-08-30 新颖二氢喋啶酮,其制备方法及作为药物组合物的用途 Pending CN1551881A (zh)

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DE10143272.0 2001-09-04
DE10143272 2001-09-04

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EP (1) EP1427730B1 (enExample)
JP (1) JP3876254B2 (enExample)
KR (1) KR100955589B1 (enExample)
CN (1) CN1551881A (enExample)
AR (1) AR036586A1 (enExample)
AT (1) ATE332898T1 (enExample)
AU (1) AU2002337047B2 (enExample)
BR (1) BRPI0212137A2 (enExample)
CA (1) CA2458699C (enExample)
CO (1) CO5560575A2 (enExample)
CY (1) CY1105337T1 (enExample)
DE (1) DE50207522D1 (enExample)
DK (1) DK1427730T3 (enExample)
EA (1) EA007062B1 (enExample)
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Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101065381B (zh) * 2004-12-02 2011-03-30 贝林格尔·英格海姆国际有限公司 稠合的哌嗪-2-酮衍生物的制备方法及所述方法的中间体
WO2011035534A1 (zh) * 2009-09-22 2011-03-31 江苏恒瑞医药股份有限公司 二氢喋啶酮类衍生物、其制备方法及其在医药上的应用
CN101636399B (zh) * 2007-03-22 2012-04-18 武田药品工业株式会社 可用作plk1抑制剂的取代的嘧啶并二氮杂*
CN103664845A (zh) * 2013-12-27 2014-03-26 湖南欧亚生物有限公司 一种Plk激酶抑制剂药物中间体7-氨基-2,3-二氢苯并呋喃-4-甲酸的制备方法
CN108610343A (zh) * 2018-06-12 2018-10-02 杨文思 一种用于治疗癌症的表皮生长因子受体抑制剂及其合成方法
CN112218865A (zh) * 2018-04-24 2021-01-12 沃泰克斯药物股份有限公司 喋啶酮化合物及其用途
CN113637017A (zh) * 2021-08-12 2021-11-12 中国药科大学 含四氢喋呤结构的化合物及其制备方法与用途

Families Citing this family (99)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6495550B2 (en) * 1999-08-04 2002-12-17 Icagen, Inc. Pyridine-substituted benzanilides as potassium ion channel openers
AU779034B2 (en) 1999-08-04 2005-01-06 Icagen, Inc. Benzanilides as potassium channel openers
ES2287583T3 (es) * 2003-02-26 2007-12-16 BOEHRINGER INGELHEIM PHARMA GMBH & CO.KG Dihidropteridinonas, procedimiento para su preparacion y su uso como medicamenteos.
US6861422B2 (en) 2003-02-26 2005-03-01 Boehringer Ingelheim Pharma Gmbh & Co. Kg Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
DE102004029784A1 (de) 2004-06-21 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel
DE102004033670A1 (de) * 2004-07-09 2006-02-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Pyridodihydropyrazinone, Verfahren zu Ihrer Herstellung und Ihre Verwendung als Arzneimittel
US20060074088A1 (en) * 2004-08-14 2006-04-06 Boehringer Ingelheim International Gmbh Dihydropteridinones for the treatment of cancer diseases
US20060035903A1 (en) 2004-08-14 2006-02-16 Boehringer Ingelheim International Gmbh Storage stable perfusion solution for dihydropteridinones
US7759485B2 (en) 2004-08-14 2010-07-20 Boehringer Ingelheim International Gmbh Process for the manufacture of dihydropteridinones
US20060058311A1 (en) 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
US7728134B2 (en) * 2004-08-14 2010-06-01 Boehringer Ingelheim International Gmbh Hydrates and polymorphs of 4[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament
EP1632493A1 (de) 2004-08-25 2006-03-08 Boehringer Ingelheim Pharma GmbH & Co.KG Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
EP1630163A1 (de) 2004-08-25 2006-03-01 Boehringer Ingelheim Pharma GmbH & Co.KG Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
JP2008510771A (ja) * 2004-08-27 2008-04-10 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 ジヒドロプテリジノン、その製造方法および医薬薬剤としてのその使用
EP1915155A1 (en) * 2005-08-03 2008-04-30 Boehringer Ingelheim International GmbH Dihydropteridinones in the treatment of respiratory diseases
US7439358B2 (en) * 2006-02-08 2008-10-21 Boehringer Ingelheim International Gmbh Specific salt, anhydrous and crystalline form of a dihydropteridione derivative
NZ570530A (en) 2006-02-14 2011-09-30 Vertex Pharma Pharmaceutical compositions comprising 6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4)diazepine derivatives
US20090312336A1 (en) * 2006-05-19 2009-12-17 Astrazeneca Ab Dihydropteridine compounds as anti proliferative agents
TW200808325A (en) * 2006-07-06 2008-02-16 Astrazeneca Ab Novel compounds
WO2008009909A1 (en) * 2006-07-17 2008-01-24 Astrazeneca Ab Pteridimones as modulators of polo-like kinase
WO2008040951A1 (en) * 2006-10-03 2008-04-10 Astrazeneca Ab Compounds
MX337906B (es) 2006-10-19 2016-03-28 Signal Pharm Llc Compuestos de heteroarilo, composiciones de los mismos, y su uso como inhibidores de proteina cinasas.
EP1953163A1 (en) * 2007-02-01 2008-08-06 Boehringer Ingelheim Pharma GmbH & Co. KG Pteridinone derivatives as PI3-kinases inhibitors
WO2008157235A1 (en) * 2007-06-13 2008-12-24 University Of Virginia Patent Foundation Rsk inhibitors as anti-septicemia agents
JP5261487B2 (ja) 2007-08-03 2013-08-14 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 ジヒドロプテリジノン誘導体の結晶形
AU2008287339A1 (en) * 2007-08-15 2009-02-19 Vertex Pharmaceuticals Incorporated 4-(9-(3, 3-difluorocyclopentyl) -5, 7, 7-trimethyl-6-oxo-6, 7, 8, 9-tetrahydro-5H-pyrimido [4, 5-b][1, 4] diazepin-2-ylamino)-3-methoxybenzamide Derivatives as Inhibitors of the Human Protein Kinases PLK1 to PLK4 for the Treatment of Proliferative Diseases
NZ584760A (en) 2007-09-25 2012-03-30 Takeda Pharmaceutical Polo-like kinase inhibitors
US8598172B2 (en) 2007-12-04 2013-12-03 Nerviano Medical Sciences S.R.L. Substituted dihydropteridin-6-one derivatives, process for their preparation and their use as kinase inhibitors
US8765791B2 (en) 2008-03-11 2014-07-01 University Health Network Method of treating cancer using a neuropeptide Y 5R (NP Y5R) antagonist
EP2100894A1 (en) 2008-03-12 2009-09-16 4Sc Ag Pyridopyrimidines used as Plk1 (polo-like kinase) inhibitors
EP2112152A1 (en) 2008-04-22 2009-10-28 GPC Biotech AG Dihydropteridinones as Plk Inhibitors
GB0807452D0 (en) * 2008-04-24 2008-05-28 Chroma Therapeutics Ltd PLK inhibitors
US8093043B2 (en) 2008-06-04 2012-01-10 New York University β-TrCP1, β-TrCP2 and RSK1 or RSK2 inhibitors and methods for sensitizing target cells to apoptosis
WO2009153197A1 (en) 2008-06-18 2009-12-23 F. Hoffmann-La Roche Ag Halo-substituted pyrimidodiazepines as plkl inhibitors
US8110578B2 (en) 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
TWI534136B (zh) 2008-12-09 2016-05-21 吉李德科學股份有限公司 用於製備可用作類鐸受體調節劑之化合物的中間體化合物
SI2477987T1 (en) 2009-09-14 2018-03-30 Gilead Sciences, Inc. MODULATORS TO TOLL OF LIKE RECEPTORS
KR20120096474A (ko) 2009-09-25 2012-08-30 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제로서 유용한 피리미딘 유도체의 제조 방법
CA2773742C (en) 2009-09-25 2017-12-05 Vertex Pharmaceuticals Incorporated Methods for preparing pyrimidine derivatives useful as protein kinase inhibitors
CN102686225A (zh) 2009-10-26 2012-09-19 西格诺药品有限公司 杂芳基化合物的合成和纯化方法
EP2325185A1 (en) 2009-10-28 2011-05-25 GPC Biotech AG Plk inhibitor
MX2012007273A (es) 2009-12-23 2012-12-17 Elan Pharm Inc Pteridinonas como inhibidores de la quinasa tipo polo.
WO2011101369A1 (en) 2010-02-17 2011-08-25 Boehringer Ingelheim International Gmbh Dihydropteridinones, method for production and use thereof
US8546566B2 (en) 2010-10-12 2013-10-01 Boehringer Ingelheim International Gmbh Process for manufacturing dihydropteridinones and intermediates thereof
US9358233B2 (en) 2010-11-29 2016-06-07 Boehringer Ingelheim International Gmbh Method for treating acute myeloid leukemia
US9370535B2 (en) 2011-05-17 2016-06-21 Boehringer Ingelheim International Gmbh Method for treatment of advanced solid tumors
SG10201912850WA (en) 2011-10-19 2020-02-27 Signal Pharm Llc Treatment Of Cancer With TOR Kinase Inhibitors
EP2780013A4 (en) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
US9206128B2 (en) 2011-11-18 2015-12-08 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
WO2013082344A1 (en) 2011-12-02 2013-06-06 Signal Pharmaceuticals, Llc Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use
JP5989805B2 (ja) 2012-02-10 2016-09-07 コンステレーション・ファーマシューティカルズ・インコーポレイテッドＣｏｎｓｔｅｌｌａｔｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． メチル基変更酵素の調節物質、組成物及びその使用
US8865716B2 (en) 2012-02-23 2014-10-21 Boehringer Ingelheim International Gmbh Dihydropteridinones II
US9006226B2 (en) 2012-02-23 2015-04-14 Boehringer Ingelheim International Gmbh Dihydropteridinones I
MX358303B (es) 2012-02-24 2018-08-14 Signal Pharm Llc Uso de 7-(6-(2-hidroxipropan-2il) piridin-3-il)-1-((1r,4r)4-metoxi ciclohexil)-3, 4-dihidropirazin-[2,3-b] pirazin-2(1h)-ona o una sal, estereoisómero o tautómero aceptable farmaceuticamente del mismo, en combinación con una cantidad efectiva de erlotinib o azacitidina para preparar un composición farmacéutica en el tratamiento de cáncer de pulmón de cédula no pequeña, avanzado.
AU2013203714B2 (en) 2012-10-18 2015-12-03 Signal Pharmaceuticals, Llc Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity
AU2014207641A1 (en) 2013-01-16 2015-08-06 Signal Pharmaceuticals, Llc Substituted Pyrrolopyrimidine Compounds, compositions thereof, and methods of treatment therewith
JP6052527B2 (ja) * 2013-02-21 2016-12-27 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 ジヒドロプテリジノンｉ
EP2958918B1 (en) * 2013-02-21 2016-12-07 Boehringer Ingelheim International GmbH Dihydropteridinones ii
US9745305B2 (en) 2013-03-15 2017-08-29 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US9474757B2 (en) 2013-04-17 2016-10-25 Signal Pharmaceuticals, Llc Methods for treating cancer using TOR kinase inhibitor combination therapy
EP2986609B1 (en) 2013-04-17 2019-06-19 Signal Pharmaceuticals, LLC Pharmaceutical formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl) pyridin-3-yl) -3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one
EA030808B1 (ru) 2013-04-17 2018-09-28 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи ПРИМЕНЕНИЕ 1-ЭТИЛ-7-(2-МЕТИЛ-6-(1Н-1,2,4-ТРИАЗОЛ-3-ИЛ)ПИРИДИН-3-ИЛ)-3,4-ДИГИДРОПИРАЗИНО[2,3-b]ПИРАЗИН-2(1Н)-ОНА В ЛЕЧЕНИИ МУЛЬТИФОРМНОЙ ГЛИОБЛАСТОМЫ
NZ631082A (en) 2013-04-17 2017-06-30 Signal Pharm Llc Methods for treating cancer using tor kinase inhibitor combination therapy
BR112015026292B1 (pt) 2013-04-17 2022-04-12 Signal Pharmaceuticals, Llc Uso de 1-etil-7-(2-metil-6-(1h-1,2,4-triazol-3-il)piridin-3-il)-3,4-dihidropirazino [2,3-b]pirazin-2(1h)- ona e métodos in vitro
MX2015014455A (es) 2013-04-17 2016-07-21 Signal Pharm Llc Terapia de combinacion que comprende un inhibidor de tor cinasa y n-(3-(5-fluoro-2-(4-(2-metoxietoxi)fenilamino)pirimidin-4-ilamino )fenil)acrilamida para tratar cancer.
MY189663A (en) 2013-04-17 2022-02-23 Signal Pharm Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
JP6401250B2 (ja) 2013-05-29 2018-10-10 シグナル ファーマシューティカルズ，エルエルシー ７−（６−（２−ヒドロキシプロパン−２−イル）ピリジン−３−イル）−１−（（ｔｒａｎｓ）−４−メトキシシクロヘキシル）−３，４−ジヒドロピラジノ［２，３−ｂ］ピラジン−２（１Ｈ）−オン、その固体形態の医薬組成物、及びその使用方法
HK1221721A1 (zh) * 2013-07-09 2017-06-09 Bayer Pharma Aktiengesellschaft Bet蛋白抑制性的改性的二氢喹喔啉酮类化合物和二氢吡啶并吡嗪酮类化合物
JP2016531113A (ja) 2013-07-25 2016-10-06 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド 転写因子の阻害剤およびその使用
US20150031699A1 (en) 2013-07-26 2015-01-29 Boehringer Ingelheim International Gmbh Treatment of myelodysplastic syndrome
US9969716B2 (en) 2013-08-15 2018-05-15 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
CA2936865A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
EP3099693A4 (en) 2014-01-31 2017-08-16 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
NZ714742A (en) 2014-04-16 2017-04-28 Signal Pharm Llc Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use
US9718824B2 (en) 2014-04-16 2017-08-01 Signal Pharmaceuticals, Llc Solid forms comprising 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, and a coformer, compositions and methods of use thereof
EP3131551A4 (en) 2014-04-16 2017-09-20 Signal Pharmaceuticals, LLC SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF
EP3131552B1 (en) 2014-04-16 2020-07-15 Signal Pharmaceuticals, LLC Methods for treating cancer using tor kinase inhibitor combination therapy
WO2015193228A1 (de) * 2014-06-19 2015-12-23 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische 1,4-dihydropyrido[3,4-b]pyrazinone mit para-substituierter aromatischer amino- oder ethergruppe
WO2015193229A1 (de) * 2014-06-19 2015-12-23 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische 1,4-dihydropyrido[3,4-b]pyrazinone mit meta-substituierter aromatischer amino- oder ethergruppe
JP6522732B2 (ja) 2014-07-11 2019-05-29 ギリアード サイエンシーズ， インコーポレイテッド Ｈｉｖを治療するためのトール様受容体の調節因子
NZ629796A (en) 2014-07-14 2015-12-24 Signal Pharm Llc Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use
AU2015289929A1 (en) 2014-07-14 2017-03-02 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
BR112017002369A2 (pt) 2014-08-08 2017-12-05 Dana Farber Cancer Inst Inc derivados de diazepana e usos dos mesmos
KR20190125537A (ko) 2014-09-16 2019-11-06 길리애드 사이언시즈, 인코포레이티드 톨-유사 수용체 조정제의 고체 형태
PT3194402T (pt) 2014-09-16 2019-02-11 Gilead Sciences Inc Métodos de preparação de moduladores dos recetores tipo toll
US9867831B2 (en) 2014-10-01 2018-01-16 Boehringer Ingelheim International Gmbh Combination treatment of acute myeloid leukemia and myelodysplastic syndrome
EP3256470B1 (en) * 2014-12-23 2023-07-26 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
WO2017040190A1 (en) 2015-08-28 2017-03-09 Constellation Pharmaceuticals, Inc. Crystalline forms of (r)-n-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1h-indole-3-carboxamide
JP2018526421A (ja) 2015-09-11 2018-09-13 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド シアノチエノトリアゾロジアゼピンおよびこれらの使用
BR112018004617A2 (pt) 2015-09-11 2018-09-25 Dana Farber Cancer Inst Inc acetamida tienotriazoldiazepinas e usos das mesmas
CN108472295B (zh) 2015-11-25 2022-04-15 达纳-法伯癌症研究所股份有限公司 二价溴结构域抑制剂及其用途
DE102017005091A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substituierte 3,4-Dihydropyrido[2,3-b]pyrazin-2(1H)-one
DE102017005089A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substitulerte 3,4-Dihydrochinoxalin-2(1H)-one
US10457640B2 (en) 2016-10-19 2019-10-29 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of EZH2
MX2019015731A (es) 2017-06-22 2020-08-03 Celgene Corp Tratamiento de carcinoma hepatocelular caracterizado por infeccion por virus de hepatitis b.
US11279707B2 (en) * 2017-12-22 2022-03-22 Dana-Farber Cancer Institute, Inc. NEK inhibitors and methods of use
US11773096B2 (en) 2018-08-10 2023-10-03 Yale University Small-molecule PI5P4K alpha/beta inhibitors and methods of treatment using same
CN111039944B (zh) 2018-10-12 2021-11-23 中国科学院合肥物质科学研究院 Mst1激酶抑制剂及其用途

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2645152B1 (fr) * 1989-03-30 1991-05-31 Lipha 3h-pteridinones-4, procedes de preparation et medicaments les contenant
CA2029651C (en) * 1989-11-17 2000-06-06 David D. Davey Tricyclic pteridinones and a process for their preparation
US5698556A (en) * 1995-06-07 1997-12-16 Chan; Carcy L. Methotrexate analogs and methods of using same
NZ516872A (en) * 1999-09-15 2003-10-31 Warner Lambert Co Pteridinones as kinase inhibitors
WO2002076954A1 (en) * 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases

Cited By (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102093361A (zh) * 2004-12-02 2011-06-15 贝林格尔.英格海姆国际有限公司 稠合的哌嗪-2-酮衍生物的制备方法
CN101065381B (zh) * 2004-12-02 2011-03-30 贝林格尔·英格海姆国际有限公司 稠合的哌嗪-2-酮衍生物的制备方法及所述方法的中间体
CN101636399B (zh) * 2007-03-22 2012-04-18 武田药品工业株式会社 可用作plk1抑制剂的取代的嘧啶并二氮杂*
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RU2559881C2 (ru) * 2009-09-22 2015-08-20 Цзянсу Хансох Фармасьютикал Ко.,Лтд. Производные дигидроптеридинона, способ их получения и фармацевтическое применение
WO2011035534A1 (zh) * 2009-09-22 2011-03-31 江苏恒瑞医药股份有限公司 二氢喋啶酮类衍生物、其制备方法及其在医药上的应用
CN102421778A (zh) * 2009-09-22 2012-04-18 江苏恒瑞医药股份有限公司 二氢喋啶酮类衍生物、其制备方法及其在医药上的应用
CN102421778B (zh) * 2009-09-22 2013-10-16 江苏恒瑞医药股份有限公司 二氢喋啶酮类衍生物、其制备方法及其在医药上的应用
US8691822B2 (en) 2009-09-22 2014-04-08 Jiangsu Hengrui Medicine Co., Ltd. Dihydropteridinone derivatives, preparation process and pharmaceutical use thereof
AU2010297921B2 (en) * 2009-09-22 2014-12-11 Jiangsu Hansoh Pharmaceutical Co., Ltd. Dihydropteridinone derivatives, preparation process and pharmaceutical use thereof
CN103664845A (zh) * 2013-12-27 2014-03-26 湖南欧亚生物有限公司 一种Plk激酶抑制剂药物中间体7-氨基-2,3-二氢苯并呋喃-4-甲酸的制备方法
CN103664845B (zh) * 2013-12-27 2016-02-10 湖南欧亚生物有限公司 一种Plk激酶抑制剂药物中间体7-氨基-2,3-二氢苯并呋喃-4-甲酸的制备方法
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