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

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (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 (OSRAM)
EP (1) EP2938610A2 (OSRAM)
JP (1) JP2016504365A (OSRAM)
AU (1) AU2013370417A1 (OSRAM)
CA (1) CA2896731A1 (OSRAM)
WO (1) WO2014105952A2 (OSRAM)

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016504365A (ja) 2012-12-28 2016-02-12 アメリカ合衆国 Ｕｓｐ１／ｕａｆ１デユビキチナーゼ複合体阻害剤及びその使用
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
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
WO2016126929A1 (en) 2015-02-05 2016-08-11 Forma Therapeutics, Inc. Thienopyrimidinones as ubiquitin-specific protease 7 inhibitors
JP2018504432A (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阻害物質としてのイソチアゾロピリミジノン、ピラゾロピリミジノン及びピロロピリミジノン
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
JP6964343B2 (ja) * 2015-11-20 2021-11-10 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１阻害剤としてのプリノン
CN109071561B (zh) * 2016-02-12 2022-01-14 福马治疗股份有限公司 用作泛素特异性蛋白酶抑制剂的噻吩并吡嗪甲酰胺
US10913753B2 (en) 2016-02-12 2021-02-09 Valo Early Discovery, Inc. Thienopyridine carboxamides as ubiquitin-specific protease inhibitors
GB201604638D0 (en) * 2016-03-18 2016-05-04 Mission Therapeutics Ltd Novel compounds
GB201604647D0 (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
US11524966B1 (en) 2017-08-11 2022-12-13 Valo Health, Inc. Carboxamides as ubiquitin-specific protease inhibitors
EP3703669B1 (en) * 2017-11-01 2025-08-06 Dana-Farber Cancer Institute, Inc. Usp1 or uaf1 inhibitors for use in treating cancer
CA3108676A1 (en) 2018-08-09 2020-02-13 David J. Guerin Carboxamides as ubiquitin-specific protease inhibitors
JP2021534122A (ja) 2018-08-09 2021-12-09 ヴァロ アーリー ディスカバリー， インコーポレイテッド 脱ユビキチン化酵素ｕｓｐ２５及びｕｓｐ２８の阻害
JP7662519B2 (ja) 2018-12-20 2025-04-15 ケーエスキュー セラピューティクス， インコーポレイテッド 置換されたピラゾロピリミジン及び置換されたプリンならびにユビキチン特異的プロセシングプロテアーゼ１（ｕｓｐ１）阻害剤としてのそれらの使用
AU2020299526A1 (en) 2019-05-31 2022-01-20 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
IL302352A (en) 2020-10-30 2023-06-01 Ksq Therapeutics Inc Solid state forms of substituted pyrazolopyrimidines and uses thereof
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
TN2023000250A1 (en) * 2021-04-07 2025-07-02 Forma Therapeutics Inc Inhibiting ubiquitin-specific protease 1 (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
EP4430050A4 (en) 2021-11-12 2025-09-24 Insilico Medicine Ip Ltd SMALL MOLECULE INHIBITORS OF UBIQUITIN-SPECIFIC PROTEASE 1 AND THEIR USES
CN119365460A (zh) 2022-04-08 2025-01-24 尚医治疗有限责任公司 与Ras超家族蛋白相互作用以用于治疗癌症、炎性疾病、RAS病和纤维化疾病的化合物
IL316542A (en) * 2022-04-29 2024-12-01 Jiangsu Yahong Meditech Co Ltd Pyrimidine compound, method for its preparation, and pharmaceutical use thereof
WO2024086790A1 (en) 2022-10-21 2024-04-25 Exelixis, Inc. 4,5,6,7-TETRAHYDRO-1H-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
WO2024233605A1 (en) 2023-05-08 2024-11-14 Tango Therapeutics, Inc. Compounds and their use against cancer
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
WO2025007840A1 (zh) * 2023-07-05 2025-01-09 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
WO2025007777A1 (zh) * 2023-07-05 2025-01-09 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
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
DE60204509T2 (de) 2001-04-20 2006-03-16 Ciba Speciality Chemicals Holding Inc. 4-Amino-2-(2-pyridinyl)pyrimidine als mikrobizide Wirksubstanzen
EP1254903B1 (en) 2001-04-20 2005-06-08 Ciba SC Holding AG 4-Amino-2-(pyridin-2-yl)pyrimidine as microbicidal active substances
WO2003026661A1 (fr) * 2001-09-14 2003-04-03 Yamanouchi Pharmaceutical Co., Ltd. Accelerateur de secretion de l'insuline et nouveau derive de pyrimidine
MXPA04005510A (es) 2001-12-07 2006-02-24 Vertex Pharma Compuestos basados en pirimidina utiles como inhibidores de gsk-3.
CN1642422A (zh) * 2002-03-15 2005-07-20 西巴特殊化学品控股有限公司 4－氨基嘧啶及其在表面抗菌处理中的应用
JP4881558B2 (ja) * 2002-09-04 2012-02-22 シェーリング コーポレイション サイクリン依存性キナーゼインヒビターとしてのピラゾロピリミジン
US7820704B2 (en) * 2004-04-20 2010-10-26 Transtech Pharma, Inc. Substituted heteroaryl derivatives, compositions, and methods of use
CA2564996A1 (en) * 2004-05-08 2006-01-12 Taeyoung Yoon 3-aryl-5,6-disubstituted pyridazines
EP1844023A1 (en) 2004-12-31 2007-10-17 Sk Chemicals Co., Ltd. Quinazoline derivatives for the treatment and prevention of diabetes and obesity
US20070032499A1 (en) 2005-08-05 2007-02-08 Philippe Guedat Novel cysteine protease inhibitors and their therapeutic applications
MX2009003142A (es) * 2006-10-03 2009-04-06 Neurosearch As Derivados de indazolilo utiles como agentes moduladores del canal de potasio.
JP2010208945A (ja) * 2007-06-01 2010-09-24 Mitsubishi Tanabe Pharma Corp 複素環化合物
WO2009011910A2 (en) 2007-07-18 2009-01-22 Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Serices 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
CN102844313B (zh) 2010-01-28 2016-10-05 哈佛大学校长及研究员协会 提高蛋白酶体活性的组合物和方法
UY33213A (es) * 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
EP2360158A1 (en) * 2010-02-18 2011-08-24 Almirall, S.A. Pyrazole derivatives as jak inhibitors
US9518032B2 (en) 2010-04-30 2016-12-13 Dana-Farber Cancer Institute, Inc. Small molecule inhibitors of USP1 deubiquitinating enzyme activity
US8865708B2 (en) 2010-05-07 2014-10-21 California Institute Of Technology Methods and compositions for inhibition of the transitional endoplasmic reticulum ATPase
WO2012012712A2 (en) 2010-07-23 2012-01-26 President And Fellows Of Harvard College Tricyclic proteasome activity enhancing compounds
CN103261169A (zh) 2010-09-24 2013-08-21 密歇根大学董事会 脱泛素酶抑制剂及其应用方法
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
WO2013004332A1 (en) * 2011-07-07 2013-01-10 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
KR102022575B1 (ko) 2011-10-19 2019-09-18 비보룩스 아베 탈유비퀴틴화 활성의 저해 방법
JP2015513317A (ja) 2012-01-25 2015-05-07 プロテオステイシス セラピューティクス，インコーポレイテッド プロテアソーム活性を増強する化合物
WO2013112651A2 (en) 2012-01-25 2013-08-01 Proteostasis Therapeutics, Inc. Proteasome activity modulating compounds
JP2016504365A (ja) 2012-12-28 2016-02-12 アメリカ合衆国 Ｕｓｐ１／ｕａｆ１デユビキチナーゼ複合体阻害剤及びその使用

Also Published As

Publication number Publication date
US9802904B2 (en) 2017-10-31
EP2938610A2 (en) 2015-11-04
JP2016504365A (ja) 2016-02-12
WO2014105952A3 (en) 2014-10-09
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
CN112969696B (zh) 乙酰化书写器抑制剂的开发及其用途
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
KR20210098960A (ko) Helios의 소분자 분해제 및 사용 방법
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
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
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
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
KR20220044753A (ko) 아세틸 조효소 a 신테타제 단쇄 2(acss2)의 소분자 억제제
JP2022536655A (ja) キナゾリニル化合物及び使用方法
EP4333842A1 (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
TWI904095B (zh) 乙醯輔酶a合成酶短鏈2(acss2)之小分子抑制劑

Legal Events

Date Code Title Description
FZDE Dead

Effective date: 20191227