AU2017226005A1 - Inhibitors of WDR5 protein-protein binding - Google Patents

Inhibitors of WDR5 protein-protein binding Download PDF

Info

Publication number
AU2017226005A1
AU2017226005A1 AU2017226005A AU2017226005A AU2017226005A1 AU 2017226005 A1 AU2017226005 A1 AU 2017226005A1 AU 2017226005 A AU2017226005 A AU 2017226005A AU 2017226005 A AU2017226005 A AU 2017226005A AU 2017226005 A1 AU2017226005 A1 AU 2017226005A1
Authority
AU
Australia
Prior art keywords
phenyl
6alkyl
carboxamide
trifluoromethyl
fluoro
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.)
Abandoned
Application number
AU2017226005A
Other languages
English (en)
Inventor
Rima AL-AWAR
Methvin Isaac
Babu Joseph
Yong Liu
Ahmed Mamai
Gennady PODA
Pandiaraju SUBRAMANIAN
David UEHLING
Brian Wilson
Carlos Armando ZEPEDA-VELAZQUEZ
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.)
Propellon Therapeutics Inc
Original Assignee
Propellon Therapeutics 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 Propellon Therapeutics Inc filed Critical Propellon Therapeutics Inc
Publication of AU2017226005A1 publication Critical patent/AU2017226005A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08Radicals containing only hydrogen and carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/14Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08Bridged systems

Landscapes

  • 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)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
AU2017226005A 2016-03-01 2017-03-01 Inhibitors of WDR5 protein-protein binding Abandoned AU2017226005A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662301678P 2016-03-01 2016-03-01
US62/301,678 2016-03-01
PCT/CA2017/050271 WO2017147701A1 (en) 2016-03-01 2017-03-01 Inhibitors of wdr5 protein-protein binding

Publications (1)

Publication Number Publication Date
AU2017226005A1 true AU2017226005A1 (en) 2018-09-06

Family

ID=59743040

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2017226005A Abandoned AU2017226005A1 (en) 2016-03-01 2017-03-01 Inhibitors of WDR5 protein-protein binding

Country Status (6)

Country Link
US (1) US11174250B2 (https=)
EP (1) EP3423437A4 (https=)
JP (1) JP2019507179A (https=)
AU (1) AU2017226005A1 (https=)
CA (1) CA3015417A1 (https=)
WO (1) WO2017147701A1 (https=)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11319299B2 (en) 2016-03-01 2022-05-03 Propellon Therapeutics Inc. Substituted carboxamides as inhibitors of WDR5 protein-protein binding
KR20190084063A (ko) 2016-10-28 2019-07-15 이칸 스쿨 오브 메디슨 엣 마운트 시나이 Ezh2-매개성 암 치료용 조성물 및 방법
WO2018106870A1 (en) 2016-12-08 2018-06-14 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating cdk4/6-mediated cancer
WO2019046944A1 (en) * 2017-09-06 2019-03-14 Propellon Therapeutics Inc. INHIBITORS OF PROTEIN BINDING WDR5-PROTEIN
US10501466B2 (en) 2017-09-19 2019-12-10 Vanderbilt University WDR5 inhibitors and modulators
JP2021515013A (ja) 2018-03-06 2021-06-17 アイカーン スクール オブ メディスン アット マウント シナイ セリンスレオニンキナーゼ(akt)分解/破壊化合物および使用方法
CN108715585A (zh) * 2018-04-23 2018-10-30 中国药科大学 苯基联三氮唑类mll1-wdr5蛋白-蛋白相互作用抑制剂
US10844044B2 (en) 2018-06-14 2020-11-24 Vanderbilt University WDR5 inhibitors and modulators
EP3810145A4 (en) * 2018-06-21 2022-06-01 Icahn School of Medicine at Mount Sinai Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use
US10807959B2 (en) 2018-08-16 2020-10-20 Vanderbilt University WDR5-MLL1 inhibitors and modulators
CN109734674B (zh) 2019-02-26 2022-08-26 中国药科大学 苯胺类wdr5蛋白-蛋白相互作用抑制剂及其制法和用途
JP7503851B2 (ja) 2019-05-06 2024-06-21 アイカーン スクール オブ メディスン アット マウント シナイ Hpk1の分解剤としてのヘテロ二官能性化合物
US12103924B2 (en) 2020-06-01 2024-10-01 Icahn School Of Medicine At Mount Sinai Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use
US20230286948A1 (en) * 2022-03-14 2023-09-14 Huyabio International, Llc Haloalkylpyridyl triazole mll1-wdr5 protein-protein interaction inhibitor
CN119365449A (zh) * 2022-07-01 2025-01-24 甘李药业股份有限公司 一种用作wdr5抑制剂的化合物或其可药用盐及其应用
CN117486791A (zh) * 2023-10-18 2024-02-02 南通敏言生物医药科技有限公司 一种5-甲氧基-4-(三氟甲基)吡啶-2-甲酸甲酯的合成方法
WO2026058961A1 (en) 2024-09-13 2026-03-19 Alivexis, Inc. Wdr5 inhibitors, compounds, pharmaceutical compositions, and methods of use thereof

Family Cites Families (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100354309B1 (ko) 1993-11-12 2003-01-06 파마시아 앤드 업존 캄파니 피리미딘-티오알킬및알킬에테르화합물
JPH0959236A (ja) 1995-08-23 1997-03-04 Dai Ichi Seiyaku Co Ltd ベンズアミド化合物
US20010051719A1 (en) 1996-12-19 2001-12-13 Smithkline Beecham P.L.C. Novel compounds
US6541669B1 (en) 1998-06-08 2003-04-01 Theravance, Inc. β2-adrenergic receptor agonists
DE19952146A1 (de) 1999-10-29 2001-06-07 Boehringer Ingelheim Pharma Arylalkane, Arylalkene und Aryl-azaalkane, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
CN100355751C (zh) 2000-03-29 2007-12-19 西克拉塞尔有限公司 2-取代的4-杂芳基-嘧啶、其组合物及其用途
JP2002193938A (ja) * 2000-12-01 2002-07-10 Bayer Ag 4−アリールピリジン誘導体
EP1389194A2 (en) 2001-04-27 2004-02-18 Vertex Pharmaceuticals Incorporated Inhibitors of bace
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
CN1681487A (zh) 2002-07-15 2005-10-12 美瑞德生物工程公司 化合物、组合物及其使用方法
AU2003270489A1 (en) 2002-09-09 2004-03-29 Cellular Genomics, Inc. 6-ARYL-IMIDAZO(1,2-a)PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
GB0412072D0 (en) 2004-05-28 2004-06-30 Syngenta Participations Ag Chemical compounds
RU2401265C2 (ru) 2004-06-10 2010-10-10 Айрм Ллк Соединения и композиции в качестве ингибиторов протеинкиназы
WO2006081172A2 (en) 2005-01-26 2006-08-03 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2006124731A2 (en) 2005-05-12 2006-11-23 Irm Llc Compounds and compositions as protein kinase inhibitors
DE102005022977A1 (de) 2005-05-19 2006-12-07 Merck Patent Gmbh Phenylchinazolinderivate
US20070254894A1 (en) 2006-01-10 2007-11-01 Kane John L Jr Novel small molecules with selective cytotoxicity against human microvascular endothelial cell proliferation
KR20080092412A (ko) 2006-02-06 2008-10-15 아이알엠 엘엘씨 단백질 키나제 억제제로서의 화합물 및 조성물
CA2644143C (en) 2006-04-05 2013-10-01 Novartis Ag Combinations comprising bcr-abl/c-kit/pdgf-r tk inhibitors for treating cancer
CA2679659C (en) 2007-03-01 2016-01-19 Novartis Ag Pim kinase inhibitors and methods of their use
BRPI0813356A2 (pt) 2007-06-15 2014-12-30 Irm Llc Inibidores de proteína quinase e métodos para uso dos mesmos
CN101875617B (zh) 2009-03-23 2015-05-20 中国医学科学院药物研究所 烷氧基取代芳环的氨甲酰基类芳酸化合物及其制法和用途
MX2011011661A (es) 2009-05-07 2011-11-18 Astrazeneca Ab Compuestos 1-cianoetilheterociclilcarboxamida sustituidos 750.
WO2011129936A2 (en) 2010-04-16 2011-10-20 Kinex Pharmaceuticals, Llc Compositions and methods for the prevention and treatment of cancer
WO2011149874A2 (en) 2010-05-26 2011-12-01 Schering Corporation N-phenyl imidazole carboxamide inhibitors of 3-phosphoinositide-dependent protein kinase-1
WO2011156557A2 (en) 2010-06-11 2011-12-15 Thomas James B Compounds active at the neurotensin receptor
WO2011159685A2 (en) 2010-06-16 2011-12-22 The Regents Of The University Of Michigan Inhibition of wdr5 interaction with its binding partners and therapeutic methods
CN201802360U (zh) 2010-06-29 2011-04-20 中国石油化工股份有限公司胜利油田分公司采油工艺研究院 曲柄无游梁抽油机
WO2012066065A1 (en) 2010-11-17 2012-05-24 Novartis Ag Phenyl-heteroaryl amine compounds and their uses
TW201406736A (zh) * 2012-06-28 2014-02-16 Fujifilm Corp 新穎的醯胺衍生物或其鹽
WO2014048878A1 (en) 2012-09-26 2014-04-03 Evotec (Uk) Ltd. Phenyl- or pyridyl- pyrrolo[2,3b]pyrazine derivatives useful in the treatment or prevention of proliferative disorders or dysplasia
CA2887598A1 (en) 2012-10-12 2014-04-17 Takeda Pharmaceutical Company Limited Cyclopropanamine compound and use thereof
US9079866B2 (en) 2013-02-04 2015-07-14 Janssen Pharmaceutica Nv Flap modulators
CA2932353A1 (en) 2013-12-13 2015-06-18 Steven P. Treon Methods to treat lymphoplasmacytic lymphoma
EP3079683A4 (en) 2013-12-13 2017-12-20 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
CN104926801B (zh) 2014-03-22 2019-06-04 浙江大学 取代氮杂环类衍生物、含其的药物组合物及其在抗肿瘤中的应用
CN105585565B (zh) 2014-10-23 2019-10-01 中国医学科学院药物研究所 含2-苯胺基-4-噻唑基吡啶衍生物及其制法和药物组合物与用途
CN105837575B (zh) 2015-01-13 2019-01-15 四川大学 3-乙炔基吡唑并嘧啶衍生物及其制备方法和用途
CN105175284B (zh) * 2015-07-21 2017-06-16 中国药科大学 酰胺类化合物、制备方法及其医药用途
US11319299B2 (en) 2016-03-01 2022-05-03 Propellon Therapeutics Inc. Substituted carboxamides as inhibitors of WDR5 protein-protein binding
IL302705A (en) 2016-03-01 2023-07-01 Immatics Biotechnologies Gmbh Peptides, combinations of peptides, cell-based drugs for use in immunotherapy against bladder cancer and other types of cancer
WO2017221092A1 (en) 2016-06-20 2017-12-28 Novartis Ag Triazolopyridine compounds and uses thereof
US10160763B2 (en) 2016-09-13 2018-12-25 Vanderbilt University WDR5 inhibitors and modulators
WO2019046944A1 (en) 2017-09-06 2019-03-14 Propellon Therapeutics Inc. INHIBITORS OF PROTEIN BINDING WDR5-PROTEIN
US10501466B2 (en) 2017-09-19 2019-12-10 Vanderbilt University WDR5 inhibitors and modulators
WO2020086857A1 (en) 2018-10-24 2020-04-30 Vanderbilt University Wdr5 inhibitors and modulators
WO2021026672A1 (en) 2019-08-09 2021-02-18 Novartis Ag Heterocyclic wdr5 inhibitors as anti-cancer compounds

Also Published As

Publication number Publication date
US20190119264A1 (en) 2019-04-25
EP3423437A1 (en) 2019-01-09
EP3423437A4 (en) 2019-07-24
JP2019507179A (ja) 2019-03-14
WO2017147701A1 (en) 2017-09-08
US11174250B2 (en) 2021-11-16
CA3015417A1 (en) 2017-09-08

Similar Documents

Publication Publication Date Title
US12264147B2 (en) Substituted carboxamides as inhibitors of WDR5 protein-protein binding
US11174250B2 (en) Substituted carboxamides as inhibitors of WDR5 protein-protein binding
JP6759514B2 (ja) ブロモドメインに対して活性な化合物
JP5976778B2 (ja) キナーゼ阻害剤としてのピラゾリル−ピリミジン誘導体
JP5931926B2 (ja) 医薬としてのアザインダゾールまたはジアザインダゾール型の誘導体
AU2018328768A1 (en) Inhibitors of WDR5 protein-protein binding
AU2014351413B2 (en) Pyrrolopyrrolone derivatives and their use as BET inhibitors
CN113773257A (zh) 用作cdk抑制剂的经过取代的杂环衍生物
US20130143896A1 (en) Isoxazolo-quinazolines as modulators of protein kinase activity
JP7189153B2 (ja) Plk1阻害剤としてのピロール誘導体
JP6257835B2 (ja) 新規なトリアゾロピリミジノン又はトリアゾロピリジノン誘導体、及びこれらの用途
KR20160012197A (ko) 피라졸로-피롤리딘-4-온 유도체 및 질환의 치료에서의 그의 용도
CN107531683A (zh) Usp7抑制剂化合物及使用方法
JP2021500334A (ja) Ehmt2阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法
CN109641909B (zh) 雷帕霉素信号通路抑制剂的机理靶标及其治疗应用
WO2017034377A1 (en) Pyridopyrimidinone compounds for modulating the catalytic activity of histone lysine demethylases (kdms)
JP2026511081A (ja) Atmキナーゼ阻害剤
HK40065957A (zh) 用作cdk抑制剂的经过取代的杂环衍生物
HK1255239B (zh) 用作cdk抑制剂的经过取代的杂环衍生物

Legal Events

Date Code Title Description
MK1 Application lapsed section 142(2)(a) - no request for examination in relevant period