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)
  • 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 (Direct)
EP (1) EP2938610A2 (Direct)
JP (1) JP2016504365A (Direct)
AU (1) AU2013370417A1 (Direct)
CA (1) CA2896731A1 (Direct)
WO (1) WO2014105952A2 (Direct)

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
AR103297A1 (es) 2014-12-30 2017-05-03 Forma Therapeutics Inc Pirrolo y pirazolopirimidinas como inhibidores de la proteasa 7 específica de ubiquitina
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
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
WO2016126929A1 (en) 2015-02-05 2016-08-11 Forma Therapeutics, Inc. Thienopyrimidinones as ubiquitin-specific protease 7 inhibitors
US9938300B2 (en) 2015-02-05 2018-04-10 Forma Therapeutics, Inc. Isothiazolopyrimidinones, pyrazolopyrimidinones, and pyrrolopyrimidinones as ubiquitin-specific protease 7 inhibitors
SG11201804098TA (en) 2015-11-20 2018-06-28 Forma Therapeutics Inc Purinones as ubiquitin-specific protease 1 inhibitors
CN109071560B (zh) * 2016-02-12 2022-01-14 瓦洛健康公司 用作泛素特异性蛋白酶抑制剂的噻吩并吡啶甲酰胺
ES2763274T3 (es) 2016-02-12 2020-05-27 Forma Therapeutics Inc Carboxamidas de tienopirazina como inhibidores de la proteasa específica de la ubiquitina
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
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
WO2019089216A1 (en) 2017-11-01 2019-05-09 Dana-Farber Cancer Institute, Inc. Methods of treating cancers
EP3833661A1 (en) 2018-08-09 2021-06-16 Valo Early Discovery, Inc. Carboxamides as ubiquitin-specific protease inhibitors
EP3833441A1 (en) 2018-08-09 2021-06-16 Valo Early Discovery, Inc. Inhibiting deubiquitinase usp25 and usp28
TWI895986B (zh) 2018-12-20 2025-09-01 美商Ｋｓｑ治療公司 經取代之吡唑并嘧啶及經取代之嘌呤以及其作為泛素特異性加工蛋白酶１（ｕｓｐ１）抑制劑的用途
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
JP2023548148A (ja) 2020-10-30 2023-11-15 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 置換ピラゾロピリミジンの固体形態及びその使用
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
CN117241801A (zh) * 2021-04-07 2023-12-15 福马治疗有限公司 抑制泛素特异性蛋白酶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
GEAP202416532A (en) 2021-11-12 2024-08-12 Insilico Medicine Ip Ltd Small molecule inhibitors of ubiquitin specific protease 1 (usp1) and uses thereof
KR20250007533A (ko) 2022-04-08 2025-01-14 샤이 테라퓨틱스 엘엘씨 암, 염증성 질환, ras질환 및 섬유성 질환의 치료를 위한 ras 슈퍼패밀리 단백질과 상호작용하는 화합물
JP2025515319A (ja) * 2022-04-29 2025-05-14 江▲蘇▼▲亞▼虹医▲薬▼科技股▲フン▼有限公司 ピリミジン化合物、それを調製するための方法、及びその薬学的使用
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
ATE297390T1 (de) 2001-04-20 2005-06-15 Ciba Sc Holding Ag 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
CA2469316A1 (en) 2001-12-07 2003-06-19 Vertex Pharmaceuticals, Inc. Pyrimidine-based compounds useful as gsk-3 inhibitors
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
ATE469903T1 (de) 2002-09-04 2010-06-15 Schering Corp Zur behandlung von krebserkrankungen geeignete pyrazolopyrimidine
MXPA06012130A (es) * 2004-04-20 2007-01-31 Transtech Pharma Inc Derivados de tiazol y pirimidina substituidos como moduladores del receptor de melanocortina.
WO2006004589A2 (en) * 2004-05-08 2006-01-12 Neurogen Corporation 3-aryl-5,6-disubstituted pyridazines
KR20060079121A (ko) 2004-12-31 2006-07-05 에스케이케미칼주식회사 당뇨 및 비만 치료예방에 유효한 퀴나졸린 유도체
US20070032499A1 (en) 2005-08-05 2007-02-08 Philippe Guedat Novel cysteine protease inhibitors and their therapeutic applications
JP2010505794A (ja) 2006-10-03 2010-02-25 ノイロサーチ アクティーゼルスカブ カリウムチャネル調節剤として有用なインダゾリル誘導体
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
BR112012018631A8 (pt) 2010-01-28 2017-12-19 President And Fellows Of Harvard Colege composições e métodos para intensificação da atividade do proteassoma
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
EP2566480A4 (en) 2010-05-07 2014-03-19 California Inst Of Techn METHOD AND COMPOSITIONS FOR INHIBITING THE VALOSIN-CONTAINING PROTEIN
CA2808432C (en) 2010-07-23 2019-06-04 President And Fellows Of Harvard College Tricyclic proteasome activity enhancing compounds with thieno[2,3-d]pyrimidine core
EP2619184B1 (en) 2010-09-24 2018-05-23 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
CA2840883C (en) 2011-07-07 2019-07-16 Merck Patent Gmbh Substituted azaheterocycles
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
WO2013058691A1 (en) 2011-10-19 2013-04-25 Vivolux Ab Method for inhibition of deubiquitinating activity
CA2861462A1 (en) 2012-01-25 2013-08-01 Proteostasis Therapeutics, Inc. Proteasome activity modulating tricyclic compounds
JP2015504919A (ja) 2012-01-25 2015-02-16 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調節する化合物
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
WO2014105952A2 (en) 2014-07-03
EP2938610A2 (en) 2015-11-04
US20150344443A1 (en) 2015-12-03
WO2014105952A3 (en) 2014-10-09
AU2013370417A1 (en) 2015-07-16
JP2016504365A (ja) 2016-02-12

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
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
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
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
KR20220044753A (ko) 아세틸 조효소 a 신테타제 단쇄 2(acss2)의 소분자 억제제
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
IL323217A (en) Selective rapamycin analogs and their uses

Legal Events

Date Code Title Description
FZDE Dead

Effective date: 20191227