CA2896731A1 - Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof - Google Patents

Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof Download PDF

Info

Publication number
CA2896731A1
CA2896731A1 CA2896731A CA2896731A CA2896731A1 CA 2896731 A1 CA2896731 A1 CA 2896731A1 CA 2896731 A CA2896731 A CA 2896731A CA 2896731 A CA2896731 A CA 2896731A CA 2896731 A1 CA2896731 A1 CA 2896731A1
Authority
CA
Canada
Prior art keywords
compound
salt
aryl
optionally substituted
heterocyclyl
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
CA2896731A
Other languages
English (en)
French (fr)
Inventor
David J. Maloney
Andrew S. Rosenthal
Ajit Jadhav
Thomas S. DEXHEIMER
Anton Simeonov
Zhihao ZHUANG
Qin LIANG
Diane K. Luci
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.)
University of Delaware
US Department of Health and Human Services
Original Assignee
University of Delaware
US Department of Health and Human Services
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 University of Delaware, US Department of Health and Human Services filed Critical University of Delaware
Publication of CA2896731A1 publication Critical patent/CA2896731A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • 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
    • 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
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • C07D405/02Heterocyclic 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
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CA2896731A 2012-12-28 2013-12-26 Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof Abandoned CA2896731A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261747052P 2012-12-28 2012-12-28
US61/747,052 2012-12-28
PCT/US2013/077804 WO2014105952A2 (en) 2012-12-28 2013-12-26 Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof

Publications (1)

Publication Number Publication Date
CA2896731A1 true CA2896731A1 (en) 2014-07-03

Family

ID=49958735

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2896731A Abandoned CA2896731A1 (en) 2012-12-28 2013-12-26 Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof

Country Status (6)

Country Link
US (1) US9802904B2 (enExample)
EP (1) EP2938610A2 (enExample)
JP (1) JP2016504365A (enExample)
AU (1) AU2013370417A1 (enExample)
CA (1) CA2896731A1 (enExample)
WO (1) WO2014105952A2 (enExample)

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2938610A2 (en) 2012-12-28 2015-11-04 The U.S.A. as represented by the Secretary, Department of Health and Human Services Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof
TWI698436B (zh) 2014-12-30 2020-07-11 美商佛瑪治療公司 作為泛素特異性蛋白酶7抑制劑之吡咯并及吡唑并嘧啶
MA41291A (fr) * 2014-12-30 2017-11-07 Forma Therapeutics Inc Dérivés de la pyrrolotriazinone et de l'imidazotriazinone en tant qu'inhibiteurs de la protéase spécifique de l'ubiquitine n° 7 (usp7) pour le traitement d'un cancer
EP3253759A1 (en) 2015-02-05 2017-12-13 Forma Therapeutics, Inc. Isothiazolopyrimidinones, pyrazolopyrimidinones, and pyrrolopyrimidinones as ubiquitin-specific protease 7 inhibitors
JP2018504431A (ja) 2015-02-05 2018-02-15 フォーマ セラピューティクス,インコーポレイテッド ユビキチン特異的プロテアーゼ7阻害物質としてのチエノピリミジノン
JP2018504430A (ja) 2015-02-05 2018-02-15 フォーマ セラピューティクス,インコーポレイテッド ユビキチン特異的プロテアーゼ7阻害物質としてのキナゾリノン及びアザキナゾリノン
RU2750151C2 (ru) 2015-11-20 2021-06-22 Форма Терапьютикс, Инк. Гипоксантины в качестве ингибиторов убиквитин-специфической протеазы 1
US10913753B2 (en) 2016-02-12 2021-02-09 Valo Early Discovery, Inc. Thienopyridine carboxamides as ubiquitin-specific protease inhibitors
EP3414251B1 (en) 2016-02-12 2019-10-16 Forma Therapeutics, Inc. Thienopyrazine carboxamides as ubiquitin-specific protease inhibitors
GB201604647D0 (en) * 2016-03-18 2016-05-04 Mission Therapeutics Ltd Novel compounds
GB201604638D0 (en) * 2016-03-18 2016-05-04 Mission Therapeutics Ltd Novel compounds
KR102327053B1 (ko) * 2017-03-16 2021-11-17 기초과학연구원 퀴나졸린, 퀴놀린 유도체 및 egfr 키나제 억제제로서의 용도
KR101986013B1 (ko) * 2017-08-04 2019-06-04 연세대학교 산학협력단 Ml323을 유효성분으로 포함하는 비만 예방 또는 치료용 조성물
TW201920157A (zh) 2017-08-11 2019-06-01 美商弗瑪治療公司 作為泛素–特異性蛋白酶抑制劑之甲醯胺
ES3040707T3 (en) 2017-11-01 2025-11-04 Dana Farber Cancer Inst Inc Usp1 or uaf1 inhibitors for use in treating cancer
WO2020033709A1 (en) 2018-08-09 2020-02-13 Forma Therapeutics, Inc. Inhibiting deubiquitinase usp25 and usp28
CA3108676A1 (en) 2018-08-09 2020-02-13 David J. Guerin Carboxamides as ubiquitin-specific protease inhibitors
IL284050B2 (en) 2018-12-20 2026-01-01 Ksq Therapeutics Inc Modified pyrazolopyrimidines and modified purines and their use as 1 uso inhibitors
EP3976009A4 (en) 2019-05-31 2023-07-05 Case Western Reserve University BAX INHIBITORS AND USES THEREOF
CN110699453B (zh) * 2019-10-10 2020-09-01 山东大学第二医院 一种胆管癌检测、治疗和预后靶点及应用
KR102481705B1 (ko) * 2020-08-04 2022-12-27 연세대학교 산학협력단 트리아졸 유도체를 유효성분으로 포함하는 간 섬유증의 예방 또는 치료용 조성물
KR20230098186A (ko) 2020-10-30 2023-07-03 케이에스큐 세러퓨틱스 인코포레이티드 치환된 피라졸로피리미딘의 고체 상태 형태 및 이의 용도
CN114436976B (zh) * 2021-01-29 2023-07-11 石药集团中奇制药技术(石家庄)有限公司 一种新型喹唑啉类衍生物及其制备和应用
WO2022199652A1 (en) * 2021-03-24 2022-09-29 Impact Therapeutics (Shanghai) , Inc Five-membered heteroaryl-pyrimidine compounds as usp1 inhibitors and the use thereof
MX2023011709A (es) * 2021-04-07 2023-10-12 Forma Therapeutics Inc Inhibidor de la proteasa 1 especifica de ubiquitina (usp1).
CN113368112B (zh) * 2021-05-10 2022-09-27 河南农业大学 Usp1-uaf1抑制剂在制备药物中的应用,药物组合物
WO2023083286A1 (en) 2021-11-12 2023-05-19 Insilico Medicine Ip Limited Small molecule inhibitors of ubiquitin specific protease 1 (usp1) and uses thereof
JP2025512935A (ja) 2022-04-08 2025-04-22 シャイ・セラピューティクス・エルエルシー がん、炎症性疾患、ras病、及び線維性疾患の処置のためのrasスーパーファミリータンパク質と相互作用する化合物
WO2023208130A1 (zh) * 2022-04-29 2023-11-02 江苏亚虹医药科技股份有限公司 嘧啶类化合物、其制备方法及其医药用途
EP4605391A1 (en) 2022-10-21 2025-08-27 Exelixis, Inc. 4,5,6,7-tetrahydro-1-pyrazolo[4,3-c]pyridine compounds and derivatives as usp1 inhibitors
CN120202201A (zh) * 2022-11-04 2025-06-24 深圳晶泰科技有限公司 泛素特异性蛋白酶1的抑制剂及其应用
WO2024153175A1 (en) * 2023-01-19 2024-07-25 Laekna Therapeutics Shanghai Co., Ltd. Heteroaromatic compounds and their use as usp1 inhibitors
TW202509030A (zh) * 2023-05-08 2025-03-01 美商譚格醫療公司 化合物及使用方法
WO2024233665A1 (en) * 2023-05-08 2024-11-14 Tango Therapeutics, Inc. Compounds and their use against cancer
WO2025005744A1 (ko) * 2023-06-29 2025-01-02 (주)아이젠사이언스 신규 피리미딘 유도체
CN121511238A (zh) * 2023-07-05 2026-02-10 江苏亚虹医药科技股份有限公司 嘧啶类化合物、其制备方法及其医药用途
CN121219283A (zh) * 2023-07-05 2025-12-26 江苏亚虹医药科技股份有限公司 联嘧啶化合物的晶型及其制备方法和用途
WO2025010245A1 (en) 2023-07-06 2025-01-09 Exelixis, Inc. Fused pyrazole derivatives as usp1 inhibitors
WO2025015905A1 (en) * 2023-07-14 2025-01-23 Laekna Therapeutics Shanghai Co., Ltd. Pyrimidine compounds and their use as usp1 inhibitors
WO2025102016A1 (en) * 2023-11-10 2025-05-15 Vrise Therapeutics, Inc. Novel molecules as inhibitors of dna damage repair pathway
WO2025129076A1 (en) * 2023-12-15 2025-06-19 Eikon Therapeutics, Inc. Pyridopyrimidine and quinazoline derivatives as usp1 inhibitors, compositions comprising them and methods of using the same
WO2025129135A2 (en) * 2023-12-15 2025-06-19 Eikon Therapeutics, Inc. Compositions comprising usp1 inhibitors and methods of using the same
WO2025151705A1 (en) 2024-01-10 2025-07-17 Vrise Therapeutics, Inc. Novel inhibitors of dna damage repair pathway

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT100905A (pt) 1991-09-30 1994-02-28 Eisai Co Ltd Compostos heterociclicos azotados biciclicos contendo aneis de benzeno, ciclo-hexano ou piridina e de pirimidina, piridina ou imidazol substituidos e composicoes farmaceuticas que os contem
JP2657760B2 (ja) * 1992-07-15 1997-09-24 小野薬品工業株式会社 4−アミノキナゾリン誘導体およびそれを含有する医薬品
DE19853278A1 (de) 1998-11-19 2000-05-25 Aventis Pharma Gmbh Substituierte 4-Amino-2-aryl-cyclopenta[d]pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate
ES2242839T3 (es) 2001-04-20 2005-11-16 Ciba Specialty Chemicals Holding Inc. 4-amino-2- (piridin-2-il)pirimidina como sustancias activas microbicidas.
EP1254903B1 (en) * 2001-04-20 2005-06-08 Ciba SC Holding AG 4-Amino-2-(pyridin-2-yl)pyrimidine as microbicidal active substances
JPWO2003026661A1 (ja) * 2001-09-14 2005-01-06 山之内製薬株式会社 インスリン分泌促進剤及び新規なピリミジン誘導体
JP2005516005A (ja) 2001-12-07 2005-06-02 バーテクス ファーマスーティカルズ インコーポレイテッド Gsk−3阻害剤として有用なピリミジンベースの化合物
ATE366045T1 (de) 2002-03-15 2007-07-15 Ciba Sc Holding Ag Verwendung von 4-aminopyrimidinen zur antimikrobiellen behandlung von oberflächen
EP1537116B1 (en) * 2002-09-04 2010-06-02 Schering Corporation Pyrazolopyrimidines suitable for the treatment of cancer diseases
WO2005103022A1 (en) * 2004-04-20 2005-11-03 Transtech Pharma, Inc. Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators
US8338591B2 (en) 2004-05-08 2012-12-25 Novartis International Pharmaceutical Ltd. 3-aryl-5,6-disubstituted pyridazines
JP2008526734A (ja) 2004-12-31 2008-07-24 エスケー ケミカルズ カンパニー リミテッド 糖尿及び肥満治療予防に有効なキナゾリン誘導体
US20070032499A1 (en) 2005-08-05 2007-02-08 Philippe Guedat Novel cysteine protease inhibitors and their therapeutic applications
WO2008040753A1 (en) 2006-10-03 2008-04-10 Neurosearch A/S Indazolyl derivatives useful as potassium channel modulating agents
JP2010208945A (ja) 2007-06-01 2010-09-24 Mitsubishi Tanabe Pharma Corp 複素環化合物
US8637560B2 (en) 2007-07-18 2014-01-28 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Imidazolidinone compounds, methods to inhibit deubiquitination and methods of treatment
JP2011032169A (ja) 2007-12-11 2011-02-17 Genecare Research Institute Co Ltd 4−アミノピリミジン誘導体および該化合物を含有する医薬組成物
PH12012500097A1 (en) 2009-07-21 2011-01-27 Shanghai Inst Organic Chem Potent small molecule inhibitors of autophagy, and methods of use thereof
AR077999A1 (es) * 2009-09-02 2011-10-05 Vifor Int Ag Antagonistas de pirimidin y triazin-hepcidina
US20130045992A1 (en) 2010-01-28 2013-02-21 President And Fellows Of Harvard College Compositions and Methods for Enhancing Proteasome Activity
EP2360158A1 (en) 2010-02-18 2011-08-24 Almirall, S.A. Pyrazole derivatives as jak inhibitors
UY33213A (es) * 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
WO2011137320A2 (en) 2010-04-30 2011-11-03 Dana-Farber Cancer Institute, Inc. Small molecule inhibitors of usp1 deubiquitinating enzyme activity
WO2011140527A2 (en) 2010-05-07 2011-11-10 California Institute Of Technology And The University Of Kansas Methods and compositions for inhibition of the transitional endoplasmic reticulum atpase
JP6042331B2 (ja) 2010-07-23 2016-12-14 プレジデント アンド フェローズ オブ ハーバード カレッジ プロテアソーム活性を向上させる三環系化合物
WO2012040527A2 (en) 2010-09-24 2012-03-29 The Regents Of The University Of Michigan Deubiquitinase inhibitors and methods for use of the same
WO2012061754A2 (en) 2010-11-05 2012-05-10 The Broad Institute, Inc. Compounds and methods for treating autoimmune diseases
WO2012172043A1 (en) * 2011-06-15 2012-12-20 Laboratoire Biodim Purine derivatives and their use as pharmaceuticals for prevention or treatment of bacterial infections
AU2012280725B2 (en) * 2011-07-07 2017-02-02 Merck Patent Gmbh Substituted azaheterocycles for the treatment of cancer
EP2546684A1 (fr) 2011-07-15 2013-01-16 ETA SA Manufacture Horlogère Suisse Guide de lumière pour l'éclairage d'un dispositif d'affichage d'informations
EP2565186A1 (en) 2011-09-02 2013-03-06 Hybrigenics S.A. Selective and reversible inhibitors of ubiquitin specific protease 7
JP2014237590A (ja) * 2011-09-30 2014-12-18 アステラス製薬株式会社 2−(ピリジン−2−イル)ピリミジン−4−アミン化合物又はその塩
CA2852518C (en) 2011-10-19 2019-09-24 Vivolux Ab Azepanone compounds and their use for the inhibition of deubiquitinating activity and the treatment of cancer
CA2861462A1 (en) 2012-01-25 2013-08-01 Proteostasis Therapeutics, Inc. Proteasome activity modulating tricyclic compounds
EP2806875B1 (en) 2012-01-25 2017-07-19 Proteostasis Therapeutics, Inc. Proteasome activity modulating compounds
EP2938610A2 (en) 2012-12-28 2015-11-04 The U.S.A. as represented by the Secretary, Department of Health and Human Services Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof

Also Published As

Publication number Publication date
WO2014105952A3 (en) 2014-10-09
JP2016504365A (ja) 2016-02-12
US9802904B2 (en) 2017-10-31
EP2938610A2 (en) 2015-11-04
US20150344443A1 (en) 2015-12-03
AU2013370417A1 (en) 2015-07-16
WO2014105952A2 (en) 2014-07-03

Similar Documents

Publication Publication Date Title
US9802904B2 (en) Inhibitors of the USP1/UAF1 deubiquitinase complex and uses thereof
KR102588955B1 (ko) 이환식 화합물 및 암의 치료에서의 이의 용도
EP3873898B1 (en) Histone acetylation writer inhibitor development and uses thereof
JP6790040B2 (ja) Fasnを阻害するための新規化合物および組成物
ES2897913T3 (es) Compuestos de piridona tetracíclicos como antivirales
JP2022517723A (ja) Cdk阻害剤としての大環状化合物、その製造方法及びその医薬品における応用
JP2022510313A (ja) Heliosの低分子分解誘導剤および使用方法
JP6726640B2 (ja) 腫瘍転移及び腫瘍形成の予防及び治療のための化合物並びに方法
CA3147266C (en) Imidazo[4,5-c]pyridine derivatives as toll-like receptor agonsits
JP6684831B2 (ja) 化合物
KR20140038443A (ko) 니코틴아미드 포스포리보실트랜스퍼라제 (nampt)의 억제를 위한 피페리딘 유도체 및 조성물
ES2906057T3 (es) Compuesto heterocíclico quiral con actividad antagonista de la vía Hedgehog, método y uso del mismo
TWI904095B (zh) 乙醯輔酶a合成酶短鏈2(acss2)之小分子抑制劑
JP6186440B2 (ja) キナーゼ阻害剤としてのジヒドロピロリジノピリミジン
WO2018187294A1 (en) Pyrimido-pyridazinone compound combinations, methods, kits and formulations thereof
AU2020270908B2 (en) Degradation of AKT by conjugation of ATP-competitive AKT inhibitor GDC-0068 with E3 ligase ligands and methods of use
AU2022269564A1 (en) Class iia histone deacetylase (hdac) degrader ligands and methods of use thereof
US20240150294A1 (en) Estrogen receptor alpha antagonists and uses thereof
CN119173510A (zh) 一种羟基酰胺类衍生物及其应用
CN117729921A (zh) 作为pd1/pd-l1抑制剂的化合物及其方法
US10849912B2 (en) Method of sensitizing cancer cells to the cytotoxic effects of apoptosis inducing ligands in cancer treatment
CA3165120A1 (en) Aryl hydantoin heterocycles and methods of use
KR102930506B1 (ko) 복소 고리 화합물
IL323217A (en) Selective rapamycin analogs and their uses

Legal Events

Date Code Title Description
FZDE Dead

Effective date: 20191227