CO5560575A2 - Compuestos derivados de dihidro-pteridinonas caracterizados por ser inhibidores de especificas cinasas del ciclo celular y preparaciones farmaceuticas que los contienen - Google Patents

Compuestos derivados de dihidro-pteridinonas caracterizados por ser inhibidores de especificas cinasas del ciclo celular y preparaciones farmaceuticas que los contienen

Info

Publication number
CO5560575A2
CO5560575A2 CO04020069A CO04020069A CO5560575A2 CO 5560575 A2 CO5560575 A2 CO 5560575A2 CO 04020069 A CO04020069 A CO 04020069A CO 04020069 A CO04020069 A CO 04020069A CO 5560575 A2 CO5560575 A2 CO 5560575A2
Authority
CO
Colombia
Prior art keywords
alkyl
group
optionally substituted
hydrogen
radical selected
Prior art date
Application number
CO04020069A
Other languages
English (en)
Inventor
Matthias Hoffmann
Matthias Grauert
Steffen Breitfelder
Christian Eickmeier
Gerald Pohl
Lehmann-Lint Thorsten
Norbert Redemann
Gisela Schnapp
Martin Steegmaier
Bauer Eckhart
Quant Jens Jurgen
Original Assignee
Boehringer Ingelheim Pharma An
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 Boehringer Ingelheim Pharma An filed Critical Boehringer Ingelheim Pharma An
Publication of CO5560575A2 publication Critical patent/CO5560575A2/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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

Abstract

1.- Compuestos de la fórmula general (I), en los que R1 significa un radical seleccionado entre el conjunto que consta de hidrógeno, NH2, XH, halógeno y un grupo alquilo C1-C3 eventualmente sustituido con uno o varios átomos de halógeno,R2 significa un radical seleccionado entre el conjunto que consta de hidrógeno, CHO, XH, -X-alquilo C1-C2 y un grupo alquilo C1-C3 eventualmente sustituido,R3 y R4 iguales o diferentes, significan un radical seleccionado entre el conjunto que consta de alquilo C1-C10, alquenilo C2-C10, alquinilo C2-C10, arilo, heteroarilo, cicloalquilo C3-C8, heterocicloalquilo C3-C8, -X-arilo, -X-heteroarilo, -X-cicloalquilo, -X-heterocicloalquilo, -NR8-arilo, -NR8-heteroarilo, -NR8-cicloalquilo, y -NR8-heterocicloalquilo, eventualmente sustituidos, o un radical seleccionado entre el conjunto que consta de hidrógeno, halógeno, COXR8, CON(R8)2, COR8 y XR8, oR3 y R4 significan en común un puente de alquilo de 2 a 5 miembros, que puede contener de 1 a 2 heteroátomos, R5 significa hidrógeno o un radical seleccionado entre el conjunto que consta de alquilo C1-C10, alquenilo C2-C10, alquinilo C2-C10, arilo, heteroarilo y cicloalquilo C3-C6, eventualmente sustituidos, o R3 y R5 ó R4 y R5 significan en común un puente de alquilo C3-C4 saturado o insaturado, que puede contener de 1 a 2 heteroátomos, R6 significa arilo o heteroarilo, eventualmente sustituido, R7 significa hidrógeno o -CO~X~alquilo C1-C4, y los X en cada caso independientemente unos de otros, significan O ó S, los R8 en cada caso independientemente unos de otros, significan hidrógeno o un radical seleccionado entre el conjunto que consta de alquilo C1-C4, alquenilo C2-C4, alquinilo C2-C4 y fenilo, eventualmente sustituidos,eventualmente en forma de sus tautómeros, sus racematos, sus enantiómeros, sus diastereoisómeros y sus mezclas, así como eventualmente de sus sales por adición de ácidos farmacológicamente inocuas.
CO04020069A 2001-09-04 2004-03-04 Compuestos derivados de dihidro-pteridinonas caracterizados por ser inhibidores de especificas cinasas del ciclo celular y preparaciones farmaceuticas que los contienen CO5560575A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10143272 2001-09-04

Publications (1)

Publication Number Publication Date
CO5560575A2 true CO5560575A2 (es) 2005-09-30

Family

ID=7697637

Family Applications (1)

Application Number Title Priority Date Filing Date
CO04020069A CO5560575A2 (es) 2001-09-04 2004-03-04 Compuestos derivados de dihidro-pteridinonas caracterizados por ser inhibidores de especificas cinasas del ciclo celular y preparaciones farmaceuticas que los contienen

Country Status (30)

Country Link
EP (1) EP1427730B1 (es)
JP (1) JP3876254B2 (es)
KR (1) KR100955589B1 (es)
CN (1) CN1551881A (es)
AR (1) AR036586A1 (es)
AT (1) ATE332898T1 (es)
AU (1) AU2002337047B2 (es)
BR (1) BRPI0212137A2 (es)
CA (1) CA2458699C (es)
CO (1) CO5560575A2 (es)
CY (1) CY1105337T1 (es)
DE (1) DE50207522D1 (es)
DK (1) DK1427730T3 (es)
EA (1) EA007062B1 (es)
EC (1) ECSP045003A (es)
ES (1) ES2268093T3 (es)
HR (1) HRP20040213A2 (es)
HU (1) HUP0401293A3 (es)
IL (2) IL160440A0 (es)
MX (1) MXPA04002067A (es)
MY (1) MY129751A (es)
NO (1) NO328804B1 (es)
NZ (1) NZ531928A (es)
PL (1) PL369740A1 (es)
PT (1) PT1427730E (es)
RS (1) RS51012B (es)
UA (1) UA76512C2 (es)
UY (1) UY27427A1 (es)
WO (1) WO2003020722A1 (es)
ZA (1) ZA200401365B (es)

Families Citing this family (106)

* 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
EP1208085B1 (en) 1999-08-04 2007-12-05 Icagen, Inc. Benzanilides as potassium channel openers
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
DE50307267D1 (de) * 2003-02-26 2007-06-21 Boehringer Ingelheim Pharma Dihydropteridinone, verfahren zu deren herstellung und deren verwendung als arzneimittel
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
US20060058311A1 (en) * 2004-08-14 2006-03-16 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation
US20060035903A1 (en) 2004-08-14 2006-02-16 Boehringer Ingelheim International Gmbh Storage stable perfusion solution for dihydropteridinones
US20060074088A1 (en) * 2004-08-14 2006-04-06 Boehringer Ingelheim International Gmbh Dihydropteridinones for the treatment of cancer diseases
US7759485B2 (en) * 2004-08-14 2010-07-20 Boehringer Ingelheim International Gmbh Process for the manufacture of dihydropteridinones
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
EP1630163A1 (de) 2004-08-25 2006-03-01 Boehringer Ingelheim Pharma GmbH & Co.KG Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
EP1632493A1 (de) 2004-08-25 2006-03-08 Boehringer Ingelheim Pharma GmbH & Co.KG Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
CA2578560A1 (en) 2004-08-27 2006-03-02 Boehringer Ingelheim International Gmbh Dihydropteridinones, method for the production thereof, and use thereof as a medicament
DE102004058337A1 (de) 2004-12-02 2006-06-14 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung von annelierten Piperazin-2-on Derivaten
CA2617589A1 (en) * 2005-08-03 2007-02-08 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
ATE479434T1 (de) 2006-02-14 2010-09-15 Vertex Pharma Als protein-kinase-inhibitoren nutzbare dyhydrodiazepine
JP2009537500A (ja) * 2006-05-19 2009-10-29 アストラゼネカ アクチボラグ 増殖抑制剤としてのジヒドロプテリジン化合物
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
EP2457913B1 (en) * 2006-10-19 2017-04-19 Signal Pharmaceuticals, LLC Heteroaryl compounds, compositions thereof, and methods of treatment therewith
EP1953163A1 (en) * 2007-02-01 2008-08-06 Boehringer Ingelheim Pharma GmbH & Co. KG Pteridinone derivatives as PI3-kinases inhibitors
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*
WO2008157235A1 (en) * 2007-06-13 2008-12-24 University Of Virginia Patent Foundation Rsk inhibitors as anti-septicemia agents
WO2009019205A1 (en) 2007-08-03 2009-02-12 Boehringer Ingelheim International Gmbh Crystalline form of a dihydropteridione derivative
JP5380447B2 (ja) * 2007-08-15 2014-01-08 バーテックス ファーマシューティカルズ インコーポレイテッド 増殖性疾患の処置のための、ヒトタンパク質キナーゼplk1ないしplk4の阻害剤としての4−(9−(3,3−ジフルオロシクロペンチル)−5,7,7−トリメチル−6−オキソ−6,7,8,9−テトラヒドロ−5h−ピリミド[4,5−b[1,4]ジアゼパン−2−イルアミノ]−3−メトキシベンザミド誘導体
KR101444924B1 (ko) 2007-09-25 2014-10-07 다케다 야쿠힌 고교 가부시키가이샤 폴로형 키나아제 억제제
JP5400791B2 (ja) * 2007-12-04 2014-01-29 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 置換ジヒドロプテリジン−6−オン誘導体、その製造方法及びキナーゼ阻害剤としてのその使用
CA2717904C (en) 2008-03-11 2016-08-30 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
AR074506A1 (es) 2008-12-09 2011-01-19 Gilead Sciences Inc Moduladores de los receptores tipo toll
NO2477987T3 (es) 2009-09-14 2018-06-09
CN102020643A (zh) * 2009-09-22 2011-04-20 上海恒瑞医药有限公司 二氢喋啶酮类衍生物、其制备方法及其在医药上的应用
BR112012006652A2 (pt) * 2009-09-25 2015-09-08 Vertex Pharma métodos para preparar os derivados de pirimidina úteis como inibidores de proteína cinase
SG179207A1 (en) 2009-09-25 2012-04-27 Vertex Pharma Methods for preparing pyrimidine derivatives useful as protein kinase inhibitors
NZ599549A (en) 2009-10-26 2013-11-29 Signal Pharm Llc Methods of synthesis and purification of heteroaryl compounds
EP2325185A1 (en) 2009-10-28 2011-05-25 GPC Biotech AG Plk inhibitor
WO2011079114A1 (en) 2009-12-23 2011-06-30 Elan Pharmaceuticals, Inc. Pteridinones as inhibitors of polo - like kinase
EP2536725B1 (en) 2010-02-17 2015-10-28 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
EP2768500B1 (en) 2011-10-19 2019-08-21 Signal Pharmaceuticals, LLC Treatment of cancer with tor kinase inhibitors
US9051269B2 (en) 2011-11-18 2015-06-09 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
EP2780014A4 (en) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc METHYLATION MODIFICATION ENZYME MODULATORS, COMPOSITIONS AND USES THEREOF
CA2857155C (en) 2011-12-02 2021-09-21 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
CA2862289C (en) 2012-02-10 2019-11-26 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US9006226B2 (en) 2012-02-23 2015-04-14 Boehringer Ingelheim International Gmbh Dihydropteridinones I
US8865716B2 (en) 2012-02-23 2014-10-21 Boehringer Ingelheim International Gmbh Dihydropteridinones II
EA028462B1 (ru) 2012-02-24 2017-11-30 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Способы лечения немелкоклеточного рака легких на поздних стадиях c применением комбинированного лечения с ингибитором киназы tor
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
AR094494A1 (es) 2013-01-16 2015-08-05 Signal Pharm Llc Pirrolopirimidinas sustituidas, sus composiciones, y sus métodos de tratamiento
WO2014127815A1 (en) * 2013-02-21 2014-08-28 Boehringer Ingelheim International Gmbh Dihydropteridinones i
EP2958918B1 (en) * 2013-02-21 2016-12-07 Boehringer Ingelheim International GmbH Dihydropteridinones ii
EP2970305B1 (en) 2013-03-15 2017-02-22 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
EP2986319A1 (en) 2013-04-17 2016-02-24 Signal Pharmaceuticals, LLC Combination therapy comprising a tor kinase inhibitor and n-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer
US9359364B2 (en) 2013-04-17 2016-06-07 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
CA2909625C (en) 2013-04-17 2021-06-01 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer
NZ629332A (en) 2013-04-17 2017-05-26 Signal Pharm Llc Treatment of cancer with dihydropyrazino-pyrazines
WO2014172426A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
NZ631082A (en) 2013-04-17 2017-06-30 Signal Pharm Llc Methods for treating cancer using tor kinase inhibitor combination therapy
SG10201708111YA (en) 2013-04-17 2017-11-29 Signal Pharm Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
CA2912627C (en) 2013-05-29 2022-03-15 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
WO2015004075A1 (de) * 2013-07-09 2015-01-15 Bayer Pharma Aktiengesellschaft Modifizierte bet-proteininhibitorische dihydrochinoxalinone und dihydropyridopyrazinone
BR112016001457A2 (pt) 2013-07-25 2017-08-29 Dana Farber Cancer Inst Inc Inibidores de fatores de transcrição e usos dos mesmos
US20150031699A1 (en) 2013-07-26 2015-01-29 Boehringer Ingelheim International Gmbh Treatment of myelodysplastic syndrome
WO2015023915A1 (en) 2013-08-15 2015-02-19 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
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
EP3099693A4 (en) 2014-01-31 2017-08-16 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
EP3099677A4 (en) 2014-01-31 2017-07-26 Dana-Farber Cancer Institute, Inc. Diaminopyrimidine benzenesulfone derivatives and uses thereof
JP2017514806A (ja) 2014-04-16 2017-06-08 シグナル ファーマシューティカルズ,エルエルシー Torキナーゼ阻害剤組み合わせ療法を使用して癌を治療する方法
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
WO2015160882A1 (en) 2014-04-16 2015-10-22 Signal Pharmaceuticals, Llc SOLID FORMS COMPRISING 7-(6-(2-HYDROXYPROPAN-2YL) 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
WO2015160880A1 (en) 2014-04-16 2015-10-22 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
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
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
ES2930667T3 (es) 2014-07-11 2022-12-21 Gilead Sciences Inc Moduladores de receptores de tipo Toll para el tratamiento de VIH
JP2017520603A (ja) 2014-07-14 2017-07-27 シグナル ファーマシューティカルズ,エルエルシー 置換ピロロピリミジン化合物を使用するがんの治療方法及びその組成物
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
CN106715437A (zh) 2014-08-08 2017-05-24 达纳-法伯癌症研究所股份有限公司 二氮杂环庚烷衍生物及其用途
MX2017003284A (es) 2014-09-16 2017-06-28 Gilead Sciences Inc Formas solidas de modulador de receptor tipo toll.
ES2706527T3 (es) 2014-09-16 2019-03-29 Gilead Sciences Inc Métodos para preparar moduladores de receptores tipo Toll
US9867831B2 (en) 2014-10-01 2018-01-16 Boehringer Ingelheim International Gmbh Combination treatment of acute myeloid leukemia and myelodysplastic syndrome
JP6815318B2 (ja) * 2014-12-23 2021-01-20 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 二官能性分子によって標的化タンパク質分解を誘導する方法
EP3307728A4 (en) 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. ASSOCIATION THERAPY USING TRANSCRIPTION INHIBITORS AND KINASE INHIBITORS
US10577350B2 (en) 2015-08-28 2020-03-03 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
AU2016319116B2 (en) 2015-09-11 2020-10-01 Dana-Farber Cancer Institute, Inc. Cyano thienotriazolodiazepines and uses thereof
KR20180051576A (ko) 2015-09-11 2018-05-16 다나-파버 캔서 인스티튜트 인크. 아세트아미드 티에노트리아졸로디아제핀 및 그의 용도
US10913752B2 (en) 2015-11-25 2021-02-09 Dana-Farber Cancer Institute, Inc. Bivalent bromodomain inhibitors and uses thereof
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
BR112019027402A2 (pt) 2017-06-22 2020-07-07 Celgene Corporation tratamento de carcinoma hepatocelular caracterizado por infecção pelo vírus da hepatite b
WO2019126696A1 (en) * 2017-12-22 2019-06-27 Dana-Farber Cancer Institute, Inc. Nek inhibitors and methods of use
CN112218865B (zh) * 2018-04-24 2024-03-12 沃泰克斯药物股份有限公司 喋啶酮化合物及其用途
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
EP3833353A4 (en) * 2018-08-10 2022-08-24 Yale University SMALL MOLECULAR PI5P4K ALPHA/BETA INHIBITORS AND METHODS OF TREATMENT THEREOF
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
CN113637017B (zh) * 2021-08-12 2024-03-26 中国药科大学 含二氢喋呤结构的化合物及其制备方法与用途

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
CZ2002846A3 (cs) * 1999-09-15 2003-02-12 Warner-Lambert Company Pteridinony, jako inhibitory kinasy
WO2002076954A1 (en) * 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases

Also Published As

Publication number Publication date
CN1551881A (zh) 2004-12-01
PL369740A1 (en) 2005-05-02
NO328804B1 (no) 2010-05-18
EP1427730A1 (de) 2004-06-16
MY129751A (en) 2007-04-30
NZ531928A (en) 2005-10-28
IL160440A0 (en) 2004-07-25
PT1427730E (pt) 2006-11-30
YU27304A (sh) 2006-08-17
JP3876254B2 (ja) 2007-01-31
ZA200401365B (en) 2005-05-27
WO2003020722A1 (de) 2003-03-13
UY27427A1 (es) 2003-03-31
ATE332898T1 (de) 2006-08-15
BRPI0212137A2 (pt) 2016-06-28
AR036586A1 (es) 2004-09-22
IL160440A (en) 2009-09-01
UA76512C2 (en) 2006-08-15
NO20040680L (no) 2004-02-16
KR100955589B1 (ko) 2010-04-30
CY1105337T1 (el) 2010-03-03
KR20040029465A (ko) 2004-04-06
ECSP045003A (es) 2004-04-28
JP2005501904A (ja) 2005-01-20
EA007062B1 (ru) 2006-06-30
EA200400368A1 (ru) 2004-12-30
HRP20040213A2 (en) 2005-02-28
AU2002337047B2 (en) 2008-01-10
DK1427730T3 (da) 2006-11-06
HUP0401293A3 (en) 2008-03-28
EP1427730B1 (de) 2006-07-12
ES2268093T3 (es) 2007-03-16
HUP0401293A2 (hu) 2004-10-28
CA2458699C (en) 2010-10-19
DE50207522D1 (de) 2006-08-24
CA2458699A1 (en) 2003-03-13
AU2002337047B8 (en) 2003-03-18
RS51012B (sr) 2010-10-31
NO20040680D0 (no) 2004-02-16
MXPA04002067A (es) 2004-06-07

Similar Documents

Publication Publication Date Title
CO5560575A2 (es) Compuestos derivados de dihidro-pteridinonas caracterizados por ser inhibidores de especificas cinasas del ciclo celular y preparaciones farmaceuticas que los contienen
CO5650164A2 (es) Hetrociclil-3-sulfonilindazoles como ligandos de 5-hidroxitriptamina-6
CO5680412A2 (es) Agonistas del receptor adrenergico etilamino beta 2 sustituido con amino
CO5680430A2 (es) Derivados de 1-benzol-piperazina como inhibidores de la captacion de glicina para el ratamiento de psicosis
CO5640136A2 (es) Derivados de hexahidropiridoisoquinolinas inhibidores de dpp-iv y composiciones farmaceuticas que los contienen
ES2189726T3 (es) Isoxazolidinas sustituidas con heterociclo y su uso como fungicidas.
ES2571779T3 (es) Inhibidores de cinasa a base de nicotinamida
AR049346A1 (es) 3-amino-1-arilpropil-indoles como inhibidores de reabsorcion de monoaminas
AR082826A2 (es) Inhibidores heterociclicos de mek, composiciones farmaceuticas que los contienen, usos, y metodos de preparacion de los mismos
AR053149A1 (es) Uso de compuestos de diosmetina para la obtencion de composiciones farmaceuticas destinadas a la prevencion y/o tratamiento de patologias tromboticas y patologias que conlleven el riesgo de producir trombosis
AR050153A1 (es) Beta-agonistas, procedimiento para su preparacion y su uso como medicamentos
ECSP088731A (es) Derivados de 1,2,4,5-tetrahidro-3h-benzazepinas, su procedimiento de preparación y las composiciones farmacéuticas que las contienen
ES2247527T3 (es) Inhibidores de metaloproteinasa de triaril-oxi-aril-espiro-pirimidina-2,4,6-triona.
AR056860A1 (es) Derivados de triazol inhibidores de receptores de quinasa tgf-beta1, composiciones farmaceuticas que los contienen y usos para el tratamiento de tumores
AR072819A1 (es) Derivados de triazolo[4,3-a]piridina,procedimiento de preparacion,intermediarios de dicho proceso,composiciones farmaceuticas que los comprenden y uso de los mismos, como inhibidores de la proteinquinasa met,para el tratamiento de canceres,psoriasis,enfermedades del sistema nervioso central y otras
AR020165A1 (es) Derivados de pirimidinas sustituidas, su procedimiento de preparacion, composiciones farmaceuticas que las contienen y el uso de los mismos para la preparacion de medicamentos
AR037907A1 (es) Derivados de azaindolilalquilamina como ligandos de 5-hidroxitriptamina-6
AR054813A1 (es) Derivados de pirroloquinolinas y sus usos como inhibidores de proteinas quinasas
AR057681A1 (es) Moduladores de interleuquina-1 y factor-alfa de necrosis tumoral; sintesis y metodos de uso de dichos moduladores
AR064729A1 (es) Derivados de 2,4-dianilinopirimidinas, su preparacion, composiciones farmaceuticas y usos como inhibidores de ikk
AR077364A1 (es) Derivados de 6-oxo-1,6- dihidro -pirimidin-2-il-) amida, su preparacion y su utilizacion farmaceutica como inhibidores de fosforilacion de akt (pkb)
CO5631442A2 (es) Nuevos derivados de indolizina 1,2,3 sustituida, inhibidores de los fgfs, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen
AR045949A1 (es) Derivados de piridina, inhibidores de urotensina ii
AR077446A1 (es) Derivados de 2,3-dihidro-1h-imidazo(1,2-a) pirimidin-5-ona. su preparacion y su utilizacion farmaceutica
CO5650235A2 (es) Derivados de imidazol

Legal Events

Date Code Title Description
FG Application granted
FD Application lapsed