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

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic 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
    • C07D498/14—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (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 (https=)
EP (1) EP3512855B1 (https=)
JP (1) JP6961684B2 (https=)
CN (1) CN110062759B (https=)
AU (1) AU2017326171B2 (https=)
CA (1) CA3036834A1 (https=)
WO (1) WO2018052945A1 (https=)

Families Citing this family (38)

* 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
EP3454862B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
EP4491236A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
CN109641874A (zh) 2016-05-10 2019-04-16 C4医药公司 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
CN109790143A (zh) 2016-05-10 2019-05-21 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
EP4717317A2 (en) 2017-06-20 2026-04-01 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
CN118108706A (zh) 2017-09-04 2024-05-31 C4医药公司 戊二酰亚胺
CN118206529A (zh) 2017-09-04 2024-06-18 C4医药公司 二氢苯并咪唑酮
CN111278816B (zh) 2017-09-04 2024-03-15 C4医药公司 二氢喹啉酮
WO2019055444A1 (en) * 2017-09-13 2019-03-21 The Regents Of The University Of Michigan DEGRADATION AGENTS OF BROMODOMAIN BET PROTEIN WITH CLEAR BINDERS
EP3710002A4 (en) 2017-11-16 2021-07-07 C4 Therapeutics, Inc. DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION
JP2021519337A (ja) 2018-03-26 2021-08-10 シー４ セラピューティクス， インコーポレイテッド Ｉｋａｒｏｓの分解のためのセレブロン結合剤
US12539292B2 (en) 2018-04-01 2026-02-03 Arvinas Operations, Inc. BRM targeting compounds and associated methods of use
CN110357889B (zh) * 2018-04-09 2022-03-15 上海科技大学 蛋白降解靶向化合物、其抗肿瘤应用、其中间体及中间体应用
CA3095912A1 (en) * 2018-04-13 2019-10-17 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
CN119751456A (zh) 2018-04-16 2025-04-04 C4医药公司 螺环化合物
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
EP3841100A1 (en) 2018-08-20 2021-06-30 Arvinas Operations, Inc. Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases
EP3863642A4 (en) * 2018-10-09 2022-06-29 The Regents of the University of California Covalent targeting of e3 ligases
JP2022507267A (ja) 2018-11-13 2022-01-18 バイオセリックス， インコーポレイテッド 置換イソインドリノン
CN120698983A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
EP3932922A4 (en) 2019-02-25 2022-05-11 ShanghaiTech University SULPHUR-CONTAINING COMPOUND BASED ON A GLUTARIMIDE FRAMEWORK AND ITS USE
WO2020181232A1 (en) 2019-03-06 2020-09-10 C4 Therapeutics, Inc. Heterocyclic compounds for medical treatment
CN119954801A (zh) 2019-07-17 2025-05-09 阿尔维纳斯运营股份有限公司 Tau蛋白靶向化合物及相关使用方法
WO2021023233A1 (zh) 2019-08-05 2021-02-11 上海科技大学 Egfr蛋白降解剂及其抗肿瘤应用
CN115397821B (zh) 2019-10-17 2024-09-03 阿尔维纳斯运营股份有限公司 含有与bcl6靶向部分连接的e3泛素连接酶结合部分的双官能分子
AU2020387392B2 (en) 2019-11-19 2025-09-11 Bristol-Myers Squibb Company Compounds useful as inhibitors of Helios protein
JP2023507590A (ja) * 2019-12-17 2023-02-24 オリオニス バイオサイエンシズ，インコーポレイテッド タンパク質の動員および／または分解を調節する化合物
AU2021231898A1 (en) 2020-03-05 2022-10-27 C4 Therapeutics, Inc. Compounds for targeted degradation of BRD9
TW202140441A (zh) 2020-03-23 2021-11-01 美商必治妥美雅史谷比公司 經取代之側氧基異吲哚啉化合物
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
JP2024504932A (ja) 2021-01-13 2024-02-02 モンテ ローザ セラピューティクス， インコーポレイテッド イソインドリノン化合物
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
BR112023020077A2 (pt) 2021-04-06 2023-11-14 Bristol Myers Squibb Co Compostos de oxoisoindolina substituída por piridinila
CN117279910A (zh) 2021-04-16 2023-12-22 阿尔维纳斯运营股份有限公司 Bcl6蛋白水解的调节剂和其相关使用方法
KR20240035820A (ko) 2021-07-09 2024-03-18 플렉시움 인코포레이티드 Ikzf2를 조절하는 아릴 화합물 및 약학 조성물
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
IL63907A0 (en) 1980-09-24 1981-12-31 Cetus Corp Diagnostic method and antibody probe for use therein
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"
EP1887008B1 (en) 2005-05-30 2021-04-21 Mitsubishi Tanabe Pharma Corporation Thienotriazolodiazepine compound and a medicinal use thereof
WO2008092231A1 (en) 2007-02-01 2008-08-07 Resverlogix Corp. Compounds for the prevention and treatment of cardiovascular diseases
WO2009084693A1 (ja) 2007-12-28 2009-07-09 Mitsubishi Tanabe Pharma Corporation 抗癌剤
KR101629356B1 (ko) 2008-06-26 2016-06-13 리스버로직스 코퍼레이션 퀴나졸리논 유도체의 제조방법
KR20190091564A (ko) 2009-04-22 2019-08-06 리스버로직스 코퍼레이션 신규한 소염제
DE102009051823A1 (de) 2009-11-04 2011-05-05 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. Einkristallines Schweißen von direktional verfestigten Werkstoffen
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
RS54645B1 (sr) 2009-11-05 2016-08-31 Glaxosmithkline Llc Benzodiazepin kao inhibitor bromodomena
MX354217B (es) 2010-05-14 2018-02-19 Dana Farber Cancer Inst Inc Composiciones y metodos para el tratamiento de leucemia.
PL2902030T3 (pl) 2010-05-14 2017-07-31 Dana-Farber Cancer Institute, Inc. Związki tienotriazolodiazepinowe do leczenia nowotworu
WO2011143651A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for modulating metabolism
US9085582B2 (en) 2010-06-22 2015-07-21 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
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
EP2677865A4 (en) 2011-02-23 2015-04-22 Icahn School Med Mount Sinai BROMODOMAIN INHIBITORS AS MODULATORS OF GENE EXPRESSION
WO2012151512A2 (en) 2011-05-04 2012-11-08 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
EP2838881B1 (en) 2012-04-20 2018-08-08 AbbVie Inc. Isoindolone derivatives
JP6215315B2 (ja) 2012-06-12 2017-10-18 アッヴィ・インコーポレイテッド ピリジノンおよびピリダジノン誘導体
EP2970312B1 (en) 2013-03-11 2017-11-15 The Regents of The University of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
US9714946B2 (en) * 2013-03-14 2017-07-25 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
US9580430B2 (en) 2014-02-28 2017-02-28 The Regents Of The University Of Michigan 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors
AU2015247817C1 (en) * 2014-04-14 2022-02-10 Arvinas Operations, Inc. Imide-based modulators of proteolysis and associated methods of use
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
EP3454862B1 (en) 2016-05-10 2024-09-11 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
US11466028B2 (en) 2022-10-11
JP6961684B2 (ja) 2021-11-05
EP3512855B1 (en) 2022-07-27
CN110062759A (zh) 2019-07-26
US20210284657A1 (en) 2021-09-16
JP2019526615A (ja) 2019-09-19
EP3512855A1 (en) 2019-07-24
AU2017326171A1 (en) 2019-04-04
CN110062759B (zh) 2022-05-24
CA3036834A1 (en) 2018-03-22
WO2018052945A1 (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
EP3416969B1 (en) Fused 1,4-oxazepines and related analogs as bet bromodomain inhibitors
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
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