AU2013370417A1 - 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
AU2013370417A1
AU2013370417A1 AU2013370417A AU2013370417A AU2013370417A1 AU 2013370417 A1 AU2013370417 A1 AU 2013370417A1 AU 2013370417 A AU2013370417 A AU 2013370417A AU 2013370417 A AU2013370417 A AU 2013370417A AU 2013370417 A1 AU2013370417 A1 AU 2013370417A1
Authority
AU
Australia
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
AU2013370417A
Other languages
English (en)
Inventor
Thomas S. DEXHEIMER
Ajit Jadhav
Qin LIANG
Diane K. Luci
David J. Maloney
Andrew S. Rosenthal
Anton Simeonov
Zhihao ZHUANG
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
Government of the United States of America
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, Government of the United States of America filed Critical University of Delaware
Publication of AU2013370417A1 publication Critical patent/AU2013370417A1/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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)
AU2013370417A 2012-12-28 2013-12-26 Inhibitors of the USP1/UAF1 deubiquitinase complex and uses thereof Abandoned AU2013370417A1 (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
AU2013370417A1 true AU2013370417A1 (en) 2015-07-16

Family

ID=49958735

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2013370417A Abandoned AU2013370417A1 (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 (https=)
EP (1) EP2938610A2 (https=)
JP (1) JP2016504365A (https=)
AU (1) AU2013370417A1 (https=)
CA (1) CA2896731A1 (https=)
WO (1) WO2014105952A2 (https=)

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
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
EP3253765A1 (en) 2015-02-05 2017-12-13 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
US9840491B2 (en) 2015-02-05 2017-12-12 Forma Therapeutics, Inc. Quinazolinones and azaquinazolinones as ubiquitin-specific protease 7 inhibitors
CN108473495B (zh) * 2015-11-20 2022-04-12 福马治疗有限公司 作为泛素-特异性蛋白酶1抑制剂的嘌呤酮
CA3014192A1 (en) 2016-02-12 2017-08-17 Forma Therapeutics, Inc. Thienopyridine carboxamides as ubiquitin-specific protease inhibitors
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
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
AR112468A1 (es) 2017-08-11 2019-10-30 Forma Therapeutics Inc Carboxamidas como inhibidores de proteasa específicos de ubiquitina
US11413288B2 (en) 2017-11-01 2022-08-16 Dana-Farber Cancer Institute, Inc. Methods of treating cancers
AU2019319907B2 (en) 2018-08-09 2024-09-05 Valo Health, Inc. Carboxamides as ubiquitin-specific protease inhibitors
EP3833441A1 (en) 2018-08-09 2021-06-16 Valo Early Discovery, Inc. Inhibiting deubiquitinase usp25 and usp28
US11485736B2 (en) 2018-12-20 2022-11-01 KSQ Therapeutics, Inc. Substituted pyrazolopyrimidines and substituted purines and their use as ubiquitin-specific-processing protease 1 (USP1) inhibitors
AU2020299526B2 (en) 2019-05-31 2026-01-29 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
CA3214040A1 (en) * 2021-04-07 2022-10-13 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
IL312642A (en) 2021-11-12 2024-07-01 Insilico Medicine Ip Ltd Small molecule inhibitors of ubiquitin specific protease 1 (usp1) and uses thereof
IL315733A (en) 2022-04-08 2024-11-01 SHY Therapeutics LLC Compounds that Interact with RAS Superfamily Proteins for the Treatment of Cancer, Inflammatory, Basoplastic, and Fibrotic Diseases
KR20250004854A (ko) * 2022-04-29 2025-01-08 장슈 야홍 메디텍 코퍼레이션 리미티드 피리미딘 화합물, 이의 제조 방법 및 이의 약학적 용도
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
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
KR20260033560A (ko) * 2023-07-05 2026-03-10 장슈 야홍 메디텍 코퍼레이션 리미티드 피리미딘 화합물, 이의 제조 방법 및 이의 의학적 용도
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
WO2025129135A2 (en) * 2023-12-15 2025-06-19 Eikon Therapeutics, Inc. Compositions comprising usp1 inhibitors and methods of using the same
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
TW202539659A (zh) 2024-01-10 2025-10-16 美商維瑞斯治療股份有限公司 Dna損傷修復途徑的新穎抑制劑

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
WO2003026661A1 (fr) * 2001-09-14 2003-04-03 Yamanouchi Pharmaceutical Co., Ltd. Accelerateur de secretion de l'insuline et nouveau derive de pyrimidine
ATE466581T1 (de) 2001-12-07 2010-05-15 Vertex Pharma Verbindungen auf pyrimidin-basis als gsk-3-hemmer
US7731985B2 (en) 2002-03-15 2010-06-08 Ciba Specialty Chemicals Corporation 4-aminopyrimidines and their use for the antimicrobial treatment of surfaces
MXPA05002571A (es) * 2002-09-04 2005-09-08 Schering Corp Pirazolopirimidinas como inhibidores de cinasa dependientes de ciclina.
AU2005236055B2 (en) * 2004-04-20 2011-10-06 Transtech Pharma, Llc Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators
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
KR20120117905A (ko) 2010-01-28 2012-10-24 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 프로테아좀 활성을 향상시키는 조성물 및 방법
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
CA2797719C (en) 2010-04-30 2019-11-26 Dana-Farber Cancer Institute, Inc. Small molecule inhibitors of usp1 deubiquitinating enzyme activity
JP2013530942A (ja) 2010-05-07 2013-08-01 カリフォルニア・インスティチュート・オブ・テクノロジー 移行型小胞体atpアーゼの阻害のための方法および組成物
EP2595993B1 (en) 2010-07-23 2018-04-18 President and Fellows of Harvard College Tricyclic proteasome activity enhancing compounds
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
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
SG11201401608PA (en) 2011-10-19 2014-07-30 Vivolux Ab Method for inhibition of deubiquitinating activity
EP2806875B1 (en) 2012-01-25 2017-07-19 Proteostasis Therapeutics, Inc. Proteasome activity modulating compounds
AU2013202373B2 (en) 2012-01-25 2016-04-14 Proteostasis Therapeutics, Inc. Proteasome activity enhancing 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
JP2016504365A (ja) 2016-02-12
CA2896731A1 (en) 2014-07-03
WO2014105952A2 (en) 2014-07-03
EP2938610A2 (en) 2015-11-04
WO2014105952A3 (en) 2014-10-09
US9802904B2 (en) 2017-10-31
US20150344443A1 (en) 2015-12-03

Similar Documents

Publication Publication Date Title
US9802904B2 (en) Inhibitors of the USP1/UAF1 deubiquitinase complex and uses thereof
EP3873898B1 (en) Histone acetylation writer inhibitor development and uses thereof
KR102588955B1 (ko) 이환식 화합물 및 암의 치료에서의 이의 용도
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
KR20210098960A (ko) Helios의 소분자 분해제 및 사용 방법
JP6139782B2 (ja) 置換ピラゾロピリミジン化合物、及びその薬学的に許容される塩、並びにこれらの溶媒和物、立体異性体、及び互変異性体、並びにこれらを含む医薬組成物
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
AU2019316858B2 (en) Smad3 inhibitors
US11014902B2 (en) MYC G-quadruplex stabilizing small molecules and their use
ES2906057T3 (es) Compuesto heterocíclico quiral con actividad antagonista de la vía Hedgehog, método y uso del mismo
WO2021041976A1 (en) Perk inhibiting indolinyl compounds
KR20220153581A (ko) Ulk1/2 의 억제제 및 이의 사용 방법
KR20220044753A (ko) 아세틸 조효소 a 신테타제 단쇄 2(acss2)의 소분자 억제제
AU2020270908B2 (en) Degradation of AKT by conjugation of ATP-competitive AKT inhibitor GDC-0068 with E3 ligase ligands and methods of use
CN119173510A (zh) 一种羟基酰胺类衍生物及其应用
US8710062B2 (en) Piperazinedione compounds
JP2024516194A (ja) Pd1/pd-l1阻害剤としての化合物及びその方法
US10849912B2 (en) Method of sensitizing cancer cells to the cytotoxic effects of apoptosis inducing ligands in cancer treatment
WO2025101912A1 (en) Hells helicase degraders and uses thereof
HK40055968B (en) Histone acetylation writer inhibitor development and uses thereof
HK40055968A (en) Histone acetylation writer inhibitor development and uses thereof
HK40001081A (en) Substituted 2, 4-diamino-quinoline derivatives for use in the treatment of proliferative diseases

Legal Events

Date Code Title Description
MK4 Application lapsed section 142(2)(d) - no continuation fee paid for the application