JP6961684B2 - Betタンパク質分解物質としての縮合1,4−オキサゼピン - Google Patents

Betタンパク質分解物質としての縮合1,4−オキサゼピン Download PDF

Info

Publication number
JP6961684B2
JP6961684B2 JP2019513957A JP2019513957A JP6961684B2 JP 6961684 B2 JP6961684 B2 JP 6961684B2 JP 2019513957 A JP2019513957 A JP 2019513957A JP 2019513957 A JP2019513957 A JP 2019513957A JP 6961684 B2 JP6961684 B2 JP 6961684B2
Authority
JP
Japan
Prior art keywords
group
oxazepine
benzyl
thieno
triazolo
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.)
Expired - Fee Related
Application number
JP2019513957A
Other languages
English (en)
Japanese (ja)
Other versions
JP2019526615A (ja
JP2019526615A5 (enExample
Inventor
シャオメン ワン
ヤン フー
チョン チン
フーミン スー
ジャンタオ フー
ビン チョウ
チョウ チェン
エステル フェルナンデスーサラス
ロンチュアン バイ
ドナ マケカーン
Original Assignee
ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン
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 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン filed Critical ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン
Publication of JP2019526615A publication Critical patent/JP2019526615A/ja
Publication of JP2019526615A5 publication Critical patent/JP2019526615A5/ja
Application granted granted Critical
Publication of JP6961684B2 publication Critical patent/JP6961684B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

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)
  • 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)
JP2019513957A 2016-09-13 2017-09-13 Betタンパク質分解物質としての縮合1,4−オキサゼピン Expired - Fee Related JP6961684B2 (ja)

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 (3)

Publication Number Publication Date
JP2019526615A JP2019526615A (ja) 2019-09-19
JP2019526615A5 JP2019526615A5 (enExample) 2020-10-22
JP6961684B2 true JP6961684B2 (ja) 2021-11-05

Family

ID=59955689

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2019513957A Expired - Fee Related JP6961684B2 (ja) 2016-09-13 2017-09-13 Betタンパク質分解物質としての縮合1,4−オキサゼピン

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 (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
WO2017197046A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation
CN109562107A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的杂环降解决定子体
CN109562113A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的螺环降解决定子体
CN121974842A (zh) 2016-05-10 2026-05-05 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
EP4717317A3 (en) 2017-06-20 2026-06-03 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
WO2019043217A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROBENZIMIDAZOLONES
CN118108706A (zh) 2017-09-04 2024-05-31 C4医药公司 戊二酰亚胺
WO2019043208A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROQUINOLINONES
US11267822B2 (en) 2017-09-13 2022-03-08 The Regents Of The University Of Michigan BET bromodomain protein degraders with cleavable linkers
EP3710002A4 (en) 2017-11-16 2021-07-07 C4 Therapeutics, Inc. DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION
CN111902141A (zh) 2018-03-26 2020-11-06 C4医药公司 用于ikaros降解的羟脑苷脂结合剂
US12539292B2 (en) 2018-04-01 2026-02-03 Arvinas Operations, Inc. BRM targeting compounds and associated methods of use
EP3778590A4 (en) 2018-04-09 2021-12-22 ShanghaiTech University ANTI PROTEIN DEGRADATION COMPOUND, ANTITUMOR APPLICATION, INTERMEDIATE THEREOF, AND INTERMEDIATE USE
CA3095912A1 (en) * 2018-04-13 2019-10-17 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
US11707452B2 (en) 2018-08-20 2023-07-25 Arvinas Operations, Inc. Modulators of alpha-synuclein proteolysis and associated methods of use
CN120468320A (zh) * 2018-10-09 2025-08-12 加利福尼亚大学董事会 E3连接酶的共价靶向
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
EP3897631A4 (en) 2018-12-20 2022-11-23 C4 Therapeutics, Inc. TARGETED PROTEIN BREAKDOWN
EP3932922A4 (en) 2019-02-25 2022-05-11 ShanghaiTech University SULPHUR-CONTAINING COMPOUND BASED ON A GLUTARIMIDE FRAMEWORK AND ITS USE
ES2995214T3 (en) 2019-03-06 2025-02-07 C4 Therapeutics Inc Heterocyclic compounds for medical treatment
EP3999182A1 (en) 2019-07-17 2022-05-25 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
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
MX2022004526A (es) 2019-10-17 2022-07-21 Arvinas Operations Inc Moléculas bifuncionales que contienen una porción de unión a la ligasa de ubiquitina e3 unida a una porción de direccionamiento a bcl6.
JP7629459B2 (ja) 2019-11-19 2025-02-13 ブリストル-マイヤーズ スクイブ カンパニー Heliosタンパク質の阻害剤として有用な化合物
JP7871189B2 (ja) * 2019-12-17 2026-06-08 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
CN119823124A (zh) 2020-03-05 2025-04-15 C4医药公司 用于brd9的靶向降解的化合物
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
CN117242060B (zh) 2021-01-13 2026-07-17 蒙特罗莎治疗股份有限公司 异吲哚啉酮化合物
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
PE20231941A1 (es) 2021-04-06 2023-12-05 Bristol Myers Squibb Co Compuestos de oxoisoindolina sustituidos con piridinilo
CN118388454A (zh) 2021-04-16 2024-07-26 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
TW202317546A (zh) 2021-07-09 2023-05-01 美商普萊克斯姆公司 調節ikzf2之芳基化合物及醫藥組合物
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

Family Cites Families (48)

* 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
EP0084796B1 (en) 1982-01-22 1990-05-02 Cetus Corporation Hla typing method and cdna probes used therein
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
WO1998011111A1 (en) 1996-09-13 1998-03-19 Yoshitomi Pharmaceutical Industries, Ltd. Thienotriazolodiazepine compounds and medicinal uses thereof
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
PT2118074E (pt) 2007-02-01 2014-03-20 Resverlogix Corp Compostos para a prevenção e tratamento de doenças cardiovasculares
CN101910182B (zh) 2007-12-28 2013-07-17 田边三菱制药株式会社 抗癌剂
US8114995B2 (en) 2008-06-26 2012-02-14 Resverlogix Corp. Methods of preparing quinazolinone derivatives
US9757368B2 (en) 2009-04-22 2017-09-12 Resverlogix Corp. Anti-inflammatory agents
DE102009051823A1 (de) 2009-11-04 2011-05-05 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. Einkristallines Schweißen von direktional verfestigten Werkstoffen
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
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
AU2010317096B2 (en) 2009-11-05 2015-03-26 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
ES2606958T3 (es) 2010-05-14 2017-03-28 Dana-Farber Cancer Institute, Inc. Compuestos de tienotriazolodiazepina para tratar una neoplasia
CN103154246B (zh) 2010-05-14 2015-11-25 达那-法伯癌症研究所 用于治疗白血病的组合物和方法
WO2011143651A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for modulating metabolism
EP2585465B1 (en) 2010-06-22 2014-11-12 GlaxoSmithKline LLC Benzotriazolodiazepine compounds inhibitors of bromodomains
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
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
WO2012174487A2 (en) 2011-06-17 2012-12-20 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
WO2013033268A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bivalent bromodomain ligands, 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
WO2013155695A1 (en) 2012-04-20 2013-10-24 Abbott Laboratories Isoindolone derivatives
HK1208681A1 (en) 2012-06-12 2016-03-11 Abbvie Inc. Pyridinone and pyridazinone derivatives
EP2970312B1 (en) 2013-03-11 2017-11-15 The Regents of The University of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
WO2014159392A1 (en) * 2013-03-14 2014-10-02 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
US20160058872A1 (en) * 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
EP4649963A3 (en) * 2014-04-14 2026-05-13 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
CA3014644A1 (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
EP3440082A1 (en) * 2016-04-06 2019-02-13 The Regents of The University of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
CN109562113A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的螺环降解决定子体

Also Published As

Publication number Publication date
EP3512855B1 (en) 2022-07-27
US11466028B2 (en) 2022-10-11
US20210284657A1 (en) 2021-09-16
JP2019526615A (ja) 2019-09-19
CN110062759A (zh) 2019-07-26
AU2017326171B2 (en) 2021-12-09
WO2018052945A1 (en) 2018-03-22
EP3512855A1 (en) 2019-07-24
CA3036834A1 (en) 2018-03-22
CN110062759B (zh) 2022-05-24
AU2017326171A1 (en) 2019-04-04

Similar Documents

Publication Publication Date Title
JP7035027B2 (ja) Betタンパク質分解物質としての縮合1,4-ジアゼピン
CN110062759B (zh) 作为bet蛋白降解剂的稠合的1,4-氧氮杂䓬
JP7072519B2 (ja) Betタンパク質分解剤
JP6967522B2 (ja) Betブロモドメイン阻害剤としての融合1,4−オキサゼピンおよび関連類似体
JP2022078201A (ja) Mdm2タンパク質分解剤
JP6991585B2 (ja) メニン阻害剤としてのピペリジン
EP3110818B1 (en) 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors
WO2016145045A1 (en) Compositions for use in treating glioblastoma
JP2020515571A (ja) 共有結合性メニン阻害剤としてのピペリジン
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
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200911

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20200911

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20210219

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20210715

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20210819

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20210917

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20211013

R150 Certificate of patent or registration of utility model

Ref document number: 6961684

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees