IL262139B - Bet protein degraders - Google Patents

Bet protein degraders

Info

Publication number
IL262139B
IL262139B IL262139A IL26213918A IL262139B IL 262139 B IL262139 B IL 262139B IL 262139 A IL262139 A IL 262139A IL 26213918 A IL26213918 A IL 26213918A IL 262139 B IL262139 B IL 262139B
Authority
IL
Israel
Prior art keywords
bet protein
protein degraders
degraders
bet
protein
Prior art date
Application number
IL262139A
Other languages
English (en)
Hebrew (he)
Other versions
IL262139A (en
Original Assignee
Univ Michigan Regents
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 Univ Michigan Regents filed Critical Univ Michigan Regents
Publication of IL262139A publication Critical patent/IL262139A/en
Publication of IL262139B publication Critical patent/IL262139B/en

Links

Classifications

    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4738Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
IL262139A 2016-04-12 2018-10-04 Bet protein degraders IL262139B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662321499P 2016-04-12 2016-04-12
US201662393888P 2016-09-13 2016-09-13
PCT/US2017/026278 WO2017180417A1 (en) 2016-04-12 2017-04-06 Bet protein degraders

Publications (2)

Publication Number Publication Date
IL262139A IL262139A (en) 2018-11-29
IL262139B true IL262139B (en) 2021-05-31

Family

ID=58548921

Family Applications (1)

Application Number Title Priority Date Filing Date
IL262139A IL262139B (en) 2016-04-12 2018-10-04 Bet protein degraders

Country Status (15)

Country Link
US (1) US10633386B2 (enExample)
EP (1) EP3442976B1 (enExample)
JP (1) JP7072519B2 (enExample)
KR (1) KR20180132861A (enExample)
CN (1) CN109311890B (enExample)
AU (1) AU2017250076B2 (enExample)
BR (1) BR112018070859A2 (enExample)
CA (1) CA3020541A1 (enExample)
IL (1) IL262139B (enExample)
MX (1) MX384905B (enExample)
RU (1) RU2752677C2 (enExample)
SG (1) SG11201808729WA (enExample)
UA (1) UA123168C2 (enExample)
WO (1) WO2017180417A1 (enExample)
ZA (1) ZA201806969B (enExample)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3892272B1 (en) 2016-04-22 2024-07-24 Dana-Farber Cancer Institute, Inc. Bifunctional molecules for degradation of egfr and methods of use
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
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
EP4483875A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Spirocyclic 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
CA3025806C (en) * 2016-06-23 2023-04-04 Dana-Farber Cancer Institute, Inc. Degradation of bromodomain-containing protein 9 (brd9) by conjugation of brd9 inhibitors with e3 ligase ligand and methods of use
EP3641762B1 (en) 2017-06-20 2026-02-18 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
CN109422751B (zh) * 2017-09-03 2022-04-22 上海美志医药科技有限公司 一类具有降解酪氨酸蛋白激酶jak3活性的化合物
CN111315735B (zh) 2017-09-04 2024-03-08 C4医药公司 二氢苯并咪唑酮
EP3679028A1 (en) 2017-09-04 2020-07-15 C4 Therapeutics, Inc. Dihydroquinolinones
EP3679026A1 (en) 2017-09-04 2020-07-15 C4 Therapeutics, Inc. Glutarimide
WO2019094772A1 (en) * 2017-11-10 2019-05-16 The Regents Of The University Of Michigan Ash1l degraders and methods of treatment therewith
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
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
AU2019323446B2 (en) 2018-08-22 2025-01-30 Cullgen (Shanghai), Inc. Tropomyosin receptor kinase (TRK) degradation compounds and methods of use
US11969472B2 (en) 2018-08-22 2024-04-30 Cullgen (Shanghai), Inc. Tropomyosin receptor kinase (TRK) degradation compounds and methods of use
EP3846800A4 (en) 2018-09-04 2022-08-24 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
US12459921B2 (en) * 2018-09-30 2025-11-04 Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Isoindoline compound, preparation method, pharmaceutical composition and use thereof
EP3863642A4 (en) * 2018-10-09 2022-06-29 The Regents of the University of California Covalent targeting of e3 ligases
CN120698983A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
EP3908291A4 (en) * 2019-01-07 2023-01-11 Dana-Farber Cancer Institute, Inc. SMALL MOLECULAR DEGRADERS OF FKBP12 VIA RECRUITMENT OF THE VON HIPPEL-LINDAU E3 UBIQUITIN LIGASE (VHL) AND USE IN DTAG SYSTEMS
BR112021014220A2 (pt) * 2019-01-22 2022-01-18 Merck Patent Gmbh Derivados heterocíclicos
ES2995214T3 (en) 2019-03-06 2025-02-07 C4 Therapeutics Inc Heterocyclic compounds for medical treatment
WO2020249048A1 (zh) * 2019-06-12 2020-12-17 上海科技大学 Alk蛋白调节剂及其抗肿瘤应用
TW202126638A (zh) * 2019-09-30 2021-07-16 日商協和麒麟股份有限公司 Bet分解劑
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
JP7692924B2 (ja) 2020-02-26 2025-06-16 クルゲン(シャンハイ),インク. トロポミオシン受容体キナーゼ(trk)分解化合物とその使用方法
IL295709A (en) 2020-03-05 2022-10-01 C4 Therapeutics Inc Compounds for targeted degradation of brd9
CN113387932B (zh) * 2020-03-14 2023-05-09 成都先导药物开发股份有限公司 一种诱导brd4蛋白降解的双功能化合物
CN112920176B (zh) * 2020-05-25 2022-11-04 四川大学华西医院 可诱导prc2蛋白复合物核心亚基降解的双功能化合物和药物组合物及应用
EP4192458A4 (en) 2020-08-05 2024-09-04 C4 Therapeutics, Inc. COMPOUNDS FOR TARGETED DEGRADATION OF RET
WO2022051616A1 (en) * 2020-09-03 2022-03-10 Board Of Regents Of The University Of Nebraska Cdk targeted heterobifunctional small molecule proteolysis targeting chimeras
BR112023023065A2 (pt) 2021-05-05 2024-01-30 Biogen Ma Inc Compostos para direcionar a degradação da tirosina quinase de bruton
CN113336801B (zh) * 2021-06-08 2023-08-22 中国人民解放军空军军医大学 含有bet抑制剂的四价铂配合物与应用
KR20240035526A (ko) 2021-07-07 2024-03-15 바이오젠 엠에이 인코포레이티드 Irak4 단백질의 분해를 표적하는 화합물
JP2024525580A (ja) 2021-07-07 2024-07-12 バイオジェン・エムエイ・インコーポレイテッド Irak4タンパク質の分解をターゲティングするための化合物
WO2024006776A1 (en) 2022-06-27 2024-01-04 Relay Therapeutics, Inc. Estrogen receptor alpha degraders and medical use thereof
AU2023298115A1 (en) 2022-06-27 2025-01-16 Relay Therapeutics, Inc. Estrogen receptor alpha degraders and use thereof
WO2024050016A1 (en) 2022-08-31 2024-03-07 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell
CN116585322B (zh) * 2023-01-16 2023-10-13 中山大学中山眼科中心 Bet蛋白降解剂在预防和治疗视网膜退行性改变相关疾病中的应用
EP4720059A1 (en) 2023-05-24 2026-04-08 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
WO2025007000A1 (en) 2023-06-30 2025-01-02 Kumquat Biosciences Inc. Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors
WO2025049555A1 (en) 2023-08-31 2025-03-06 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell
TW202523291A (zh) 2023-11-02 2025-06-16 美商金橘生物科技公司 降解劑及其用途

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS57501692A (enExample) 1980-09-24 1982-09-16
ATE53862T1 (de) 1982-01-22 1990-06-15 Cetus Corp Verfahren zur charakterisierung von hla und die darin benutzten cdns-testmittel.
US4582788A (en) 1982-01-22 1986-04-15 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
DE69717160T2 (de) 1996-09-13 2003-05-08 Mitsubishi Pharma Corp., Osaka Thienotriazolodiazepinverbindungen und ihre medizinischen anwendungen
US20030045552A1 (en) * 2000-12-27 2003-03-06 Robarge Michael J. Isoindole-imide compounds, compositions, and uses thereof
US7091353B2 (en) * 2000-12-27 2006-08-15 Celgene Corporation Isoindole-imide compounds, compositions, and 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
DK2118074T3 (en) 2007-02-01 2014-03-10 Resverlogix Corp Compounds for the prevention and treatment of cardiovascular diseases
US8476260B2 (en) 2007-12-28 2013-07-02 Mitsubishi Tanabe Pharma Corporation Antitumor agent
KR101629356B1 (ko) 2008-06-26 2016-06-13 리스버로직스 코퍼레이션 퀴나졸리논 유도체의 제조방법
EP2358697B1 (en) * 2008-10-29 2015-10-21 Celgene Corporation Isoindoline compounds for use in the treatment of cancer.
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
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
SI2496582T1 (sl) 2009-11-05 2016-04-29 Glaxosmithkline Llc Corporation Service Company Benzodiazepinski inhibitor bromodomene
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
SG10201501062SA (en) * 2010-02-11 2015-04-29 Celgene Corp Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
MX373121B (es) 2010-05-14 2020-04-30 Dana Farber Cancer Inst Inc Composiciones y metodos para el tratamiento de leucemia.
JP5913292B2 (ja) 2010-05-14 2016-04-27 ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド 代謝を調節する組成物および方法
MX384074B (es) 2010-05-14 2025-03-12 Dana Farber Cancer Inst Inc Composiciones y métodos para tratar neoplasias, enfermedades inflamatorias y otros trastornos.
JO2998B1 (ar) * 2010-06-04 2016-09-05 Amgen Inc مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان
ES2526671T3 (es) 2010-06-22 2015-01-14 Glaxosmithkline Llc Compuestos de benzotriazoldiazepina inhibidores de bromodominios
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
CA2828212A1 (en) 2011-02-23 2012-08-30 Shiraz Mujtaba Inhibitors of bromodomains as modulators of gene expression
EP2705039B1 (en) 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
US9328117B2 (en) 2011-06-17 2016-05-03 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
JP2015508414A (ja) * 2012-01-12 2015-03-19 イエール ユニバーシティ E3ユビキチンリガーゼによる標的タンパク質および他のポリペプチドの分解増強のための化合物および方法
US20140079636A1 (en) * 2012-04-16 2014-03-20 Dinesh U. Chimmanamada Targeted therapeutics
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
WO2013185284A1 (en) 2012-06-12 2013-12-19 Abbott Laboratories Pyridinone and pyridazinone derivatives
CA2902856C (en) * 2013-02-28 2021-02-16 Amgen Inc. A benzoic acid derivative mdm2 inhibitor for the treatment of cancer
JP6401773B2 (ja) * 2013-03-11 2018-10-10 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン Betブロモドメイン阻害剤およびこれを用いる治療方法
JP2017511801A (ja) * 2014-02-28 2017-04-27 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン BETブロモドメイン阻害剤としての9H−ピリミド[4,5−b]インドールおよび関連類似体
US20160058872A1 (en) * 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
CN119591582A (zh) * 2014-04-14 2025-03-11 阿尔维纳斯运营股份有限公司 基于酰亚胺的蛋白水解调节剂和相关使用方法
US10307407B2 (en) * 2015-02-27 2019-06-04 The Regents Of The University Of Michigan 9H-pyrimido [4,5-B] indoles as BET bromodomain inhibitors
EP3337476A4 (en) * 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
AU2017246453A1 (en) * 2016-04-06 2018-11-08 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation

Also Published As

Publication number Publication date
AU2017250076A1 (en) 2018-11-08
BR112018070859A2 (pt) 2019-02-05
RU2018139537A3 (enExample) 2020-08-11
EP3442976B1 (en) 2022-07-20
EP3442976A1 (en) 2019-02-20
MX2018012379A (es) 2019-07-04
IL262139A (en) 2018-11-29
CN109311890B (zh) 2021-08-31
RU2018139537A (ru) 2020-05-14
SG11201808729WA (en) 2018-11-29
CA3020541A1 (en) 2017-10-19
JP7072519B2 (ja) 2022-05-20
ZA201806969B (en) 2019-12-18
MX384905B (es) 2025-03-14
US20190169195A1 (en) 2019-06-06
RU2752677C2 (ru) 2021-07-29
UA123168C2 (uk) 2021-02-24
JP2019511528A (ja) 2019-04-25
KR20180132861A (ko) 2018-12-12
CN109311890A (zh) 2019-02-05
US10633386B2 (en) 2020-04-28
WO2017180417A1 (en) 2017-10-19
AU2017250076B2 (en) 2021-07-22

Similar Documents

Publication Publication Date Title
ZA201806969B (en) Bet protein degraders
GB201502305D0 (en) Protein
GB201502306D0 (en) Protein
GB201608885D0 (en) Treatment
GB201415344D0 (en) Protein
HUE050893T2 (hu) Protein
GB201609597D0 (en) Therapy
GB201515745D0 (en) Proteins
GB201511787D0 (en) Proteins
GB201513033D0 (en) Proteins
PL3099793T3 (pl) Białko
GB2558968B (en) G Proteins
PL3469691T3 (pl) Konfiguracja szyku halbacha
GB201522610D0 (en) Protein
GB201618477D0 (en) Therapy
TWM532803U (en) Walker
GB201609610D0 (en) N7
GB201621467D0 (en) Modified bulgeomers
GB201620166D0 (en) Concept four
GB201615923D0 (en) Macrophage-based therapy
GB201607497D0 (en) Antidate v2
PH32016001296S1 (en) Hand lamp
PH32016001297S1 (en) Hand lamp
GB201617107D0 (en) Treatment
GB201616374D0 (en) Modified bulgeomers

Legal Events

Date Code Title Description
FF Patent granted