AU2017326171B2 - Fused 1,4-oxazepines as BET protein degraders - Google Patents

Fused 1,4-oxazepines as BET protein degraders Download PDF

Info

Publication number
AU2017326171B2
AU2017326171B2 AU2017326171A AU2017326171A AU2017326171B2 AU 2017326171 B2 AU2017326171 B2 AU 2017326171B2 AU 2017326171 A AU2017326171 A AU 2017326171A AU 2017326171 A AU2017326171 A AU 2017326171A AU 2017326171 B2 AU2017326171 B2 AU 2017326171B2
Authority
AU
Australia
Prior art keywords
optionally substituted
group
dione
benzyl
thieno
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.)
Ceased
Application number
AU2017326171A
Other languages
English (en)
Other versions
AU2017326171A1 (en
Inventor
Longchuan Bai
Zhou CHEN
Ester Fernandez-Salas
Jiantao HU
Yang Hu
Donna Mceachern
Chong QIN
Shaomeng Wang
Fuming XU
Bing Zhou
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 Michigan System
Original Assignee
University of Michigan System
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 Michigan System filed Critical University of Michigan System
Publication of AU2017326171A1 publication Critical patent/AU2017326171A1/en
Application granted granted Critical
Publication of AU2017326171B2 publication Critical patent/AU2017326171B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Virology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
AU2017326171A 2016-09-13 2017-09-13 Fused 1,4-oxazepines as BET protein degraders Ceased AU2017326171B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662393904P 2016-09-13 2016-09-13
US62/393,904 2016-09-13
PCT/US2017/051282 WO2018052945A1 (en) 2016-09-13 2017-09-13 Fused 1,4-oxazepines as bet protein degraders

Publications (2)

Publication Number Publication Date
AU2017326171A1 AU2017326171A1 (en) 2019-04-04
AU2017326171B2 true AU2017326171B2 (en) 2021-12-09

Family

ID=59955689

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2017326171A Ceased AU2017326171B2 (en) 2016-09-13 2017-09-13 Fused 1,4-oxazepines as BET protein degraders

Country Status (7)

Country Link
US (1) US11466028B2 (enExample)
EP (1) EP3512855B1 (enExample)
JP (1) JP6961684B2 (enExample)
CN (1) CN110062759B (enExample)
AU (1) AU2017326171B2 (enExample)
CA (1) CA3036834A1 (enExample)
WO (1) WO2018052945A1 (enExample)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
EP3455218A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
EP4491236A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
WO2017197036A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
CN118440096A (zh) 2017-06-20 2024-08-06 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
CN111315735B (zh) 2017-09-04 2024-03-08 C4医药公司 二氢苯并咪唑酮
WO2019043208A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROQUINOLINONES
EP3679026A1 (en) 2017-09-04 2020-07-15 C4 Therapeutics, Inc. Glutarimide
US11267822B2 (en) 2017-09-13 2022-03-08 The Regents Of The University Of Michigan BET bromodomain protein degraders with cleavable linkers
CN111372585A (zh) 2017-11-16 2020-07-03 C4医药公司 用于靶蛋白降解的降解剂和降解决定子
KR20210018199A (ko) 2018-03-26 2021-02-17 씨4 테라퓨틱스, 인코포레이티드 이카로스의 분해를 위한 세레블론 결합제
JP7367908B2 (ja) * 2018-04-09 2023-10-24 上海科技大学 標的タンパク質分解化合物、その抗腫瘍応用、その中間体および中間体の応用
EP3774772A1 (en) * 2018-04-13 2021-02-17 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2019204354A1 (en) 2018-04-16 2019-10-24 C4 Therapeutics, Inc. Spirocyclic compounds
EP3578561A1 (en) 2018-06-04 2019-12-11 F. Hoffmann-La Roche AG Spiro compounds
CN110407854B (zh) * 2018-08-17 2020-09-15 北京加科思新药研发有限公司 新的四环化合物
CN112912376A (zh) 2018-08-20 2021-06-04 阿尔维纳斯运营股份有限公司 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物
US12161648B2 (en) 2018-10-09 2024-12-10 The Regents Of The University Of California Covalent targeting of E3 ligases
CA3119343C (en) 2018-11-13 2024-01-16 Biotheryx, Inc. Substituted isoindolinones
CN120698985A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
US11912699B2 (en) 2019-07-17 2024-02-27 Arvinas Operations, Inc. Tau-protein targeting compounds and associated
AU2020368542B2 (en) 2019-10-17 2024-02-29 Arvinas Operations, Inc. Bifunctional molecules containing an E3 ubiquitine ligase binding moiety linked to a BCL6 targeting moiety
IL293027A (en) 2019-11-19 2022-07-01 Bristol Myers Squibb Co Compounds useful as inhibitors of Helios protein
EP4076464A4 (en) * 2019-12-17 2024-06-12 Orionis Biosciences, Inc. COMPOUNDS FOR MODULATION OF PROTEIN RECRUITMENT AND/OR DEGRADATION
AU2021231898A1 (en) 2020-03-05 2022-10-27 C4 Therapeutics, Inc. Compounds for targeted degradation of BRD9
CN111499644B (zh) * 2020-04-24 2021-07-20 苏州大学 咪唑并[1,5-a]喹唑啉-5(4H)-酮类衍生物及其制备方法和用途
WO2022152821A1 (en) 2021-01-13 2022-07-21 Monte Rosa Therapeutics Ag Isoindolinone compounds
CN112979657A (zh) * 2021-02-03 2021-06-18 福建医科大学 一种靶向降解Hsp90蛋白的化合物及其制备方法与应用
RS66982B1 (sr) 2021-04-06 2025-07-31 Bristol Myers Squibb Co Piridinil supstituisana oksoizoindolinska jedinjenja
EP4323352A1 (en) 2021-04-16 2024-02-21 Arvinas Operations, Inc. Modulators of bcl6 proteolysis and associated methods of use
WO2023283425A1 (en) 2021-07-09 2023-01-12 Plexium, Inc. Aryl compounds and pharmaceutical compositions that modulate ikzf2
CN116410205B (zh) * 2021-12-29 2024-07-05 上海皓元生物医药科技有限公司 一种3-取代-9-甲基-噻吩并三唑并噁嗪类化合物的制备方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160058872A1 (en) * 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
WO2017142881A1 (en) * 2016-02-15 2017-08-24 The Regents Of The University Of Michigan Fused 1,4-oxazepines and related analogs as bet bromodomain inhibitors

Family Cites Families (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR8108820A (pt) 1980-09-24 1982-08-24 Cetus Corp Processo e sonda de diagnostico
US4582788A (en) 1982-01-22 1986-04-15 Cetus Corporation HLA typing method and cDNA probes used therein
ATE53862T1 (de) 1982-01-22 1990-06-15 Cetus Corp Verfahren zur charakterisierung von hla und die darin benutzten cdns-testmittel.
US4683194A (en) 1984-05-29 1987-07-28 Cetus Corporation Method for detection of polymorphic restriction sites and nucleic acid sequences
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
CA1284931C (en) 1986-03-13 1991-06-18 Henry A. Erlich Process for detecting specific nucleotide variations and genetic polymorphisms present in nucleic acids
CA1338457C (en) 1986-08-22 1996-07-16 Henry A. Erlich Purified thermostable enzyme
US5093330A (en) 1987-06-15 1992-03-03 Ciba-Geigy Corporation Staurosporine derivatives substituted at methylamino nitrogen
JPH05345785A (ja) * 1992-01-16 1993-12-27 Yoshitomi Pharmaceut Ind Ltd トリアゾロオキサゼピン化合物
DE69717160T2 (de) 1996-09-13 2003-05-08 Mitsubishi Pharma Corp., Osaka Thienotriazolodiazepinverbindungen und ihre medizinischen anwendungen
FR2843126B1 (fr) 2002-08-01 2006-01-27 Cis Bio Int "methode de determination d'une activite enzymatique endoglycosidase"
WO2006129623A1 (ja) 2005-05-30 2006-12-07 Mitsubishi Tanabe Pharma Corporation チエノトリアゾロジアゼピン化合物及びその医薬としての用途
DK2118074T3 (en) 2007-02-01 2014-03-10 Resverlogix Corp Compounds for the prevention and treatment of cardiovascular diseases
CN101910182B (zh) 2007-12-28 2013-07-17 田边三菱制药株式会社 抗癌剂
ES2532402T3 (es) 2008-06-26 2015-03-26 Resverlogix Corporation Métodos de preparación de derivados de quinazolinona
CN107252429B (zh) 2009-04-22 2023-06-16 雷斯韦洛吉克斯公司 新抗炎剂
DE102009051823A1 (de) 2009-11-04 2011-05-05 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. Einkristallines Schweißen von direktional verfestigten Werkstoffen
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
EP3050885B1 (en) 2009-11-05 2017-10-18 GlaxoSmithKline LLC Benzodiazepine bromodomain inhibitor
CA2799403C (en) 2010-05-14 2020-01-21 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
CN103119160B (zh) 2010-05-14 2016-06-01 达那-法伯癌症研究所 用于调节代谢的组合物和方法
HUE031073T2 (en) 2010-05-14 2017-06-28 Dana Farber Cancer Inst Inc Thieno triazolo-diazepine compounds for the treatment of neoplasia
WO2011161031A1 (en) 2010-06-22 2011-12-29 Glaxosmithkline Llc Benzotriazolodiazepine compounds inhibitors of bromodomains
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
AU2012220620A1 (en) 2011-02-23 2013-10-03 Icahn School Of Medicine At Mount Sinai Inhibitors of bromodomains as modulators of gene expression
EP2705039B1 (en) * 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
EP2721031B1 (en) 2011-06-17 2016-01-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2013033270A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same
DE102011082013A1 (de) 2011-09-01 2013-03-07 Bayer Pharma AG 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
US20130281399A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
HK1206744A1 (en) 2012-04-20 2016-01-15 Abbvie Inc. Isoindolone derivatives
MX2014015156A (es) 2012-06-12 2015-08-06 Abbvie Inc Derivados de piridinona y piridazinona.
CN105377851B (zh) 2013-03-11 2018-07-20 密执安州立大学董事会 Bet布罗莫结构域抑制剂和使用这些抑制剂的治疗方法
WO2014159392A1 (en) * 2013-03-14 2014-10-02 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
WO2015131005A1 (en) 2014-02-28 2015-09-03 The Regents Of The University Of Michigan 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors
KR20250127179A (ko) * 2014-04-14 2025-08-26 아비나스 오퍼레이션스, 인코포레이티드 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법
GB201504314D0 (en) 2015-03-13 2015-04-29 Univ Dundee Small molecules
WO2017176958A1 (en) * 2016-04-06 2017-10-12 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
WO2017197036A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160058872A1 (en) * 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
WO2017142881A1 (en) * 2016-02-15 2017-08-24 The Regents Of The University Of Michigan Fused 1,4-oxazepines and related analogs as bet bromodomain inhibitors

Also Published As

Publication number Publication date
AU2017326171A1 (en) 2019-04-04
CN110062759B (zh) 2022-05-24
US11466028B2 (en) 2022-10-11
CN110062759A (zh) 2019-07-26
US20210284657A1 (en) 2021-09-16
EP3512855A1 (en) 2019-07-24
WO2018052945A1 (en) 2018-03-22
JP6961684B2 (ja) 2021-11-05
JP2019526615A (ja) 2019-09-19
EP3512855B1 (en) 2022-07-27
CA3036834A1 (en) 2018-03-22

Similar Documents

Publication Publication Date Title
AU2017326171B2 (en) Fused 1,4-oxazepines as BET protein degraders
AU2017326175B2 (en) Fused 1,4-diazepines as BET protein degraders
EP3442976B1 (en) Bet protein degraders
EP3440066B1 (en) Mdm2 protein degraders
EP3110818B1 (en) 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors
US11045448B2 (en) Piperidines as covalent menin inhibitors
EP3628044B1 (en) Pyrrolo[2,3-c]pyridines and related analogs as lsd-1 inhibitors
US10307407B2 (en) 9H-pyrimido [4,5-B] indoles as BET bromodomain inhibitors
EP3416969B1 (en) Fused 1,4-oxazepines and related analogs as bet bromodomain inhibitors
US11267822B2 (en) BET bromodomain protein degraders with cleavable linkers
HK40004858A (en) Bet protein degraders
HK40004858B (en) Bet protein degraders

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired