JP7072519B2 - Ｂｅｔタンパク質分解剤 - Google Patents

Ｂｅｔタンパク質分解剤 Download PDF

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JP7072519B2
JP7072519B2 JP2018553365A JP2018553365A JP7072519B2 JP 7072519 B2 JP7072519 B2 JP 7072519B2 JP 2018553365 A JP2018553365 A JP 2018553365A JP 2018553365 A JP2018553365 A JP 2018553365A JP 7072519 B2 JP7072519 B2 JP 7072519B2
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compound
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pharmaceutically acceptable
solvate
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JP2019511528A (ja
JP2019511528A5 (enExample
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シャオメン ワン
ビン チョウ
フーミン スー
ジャンタオ フー
ロンチュアン バイ
チャオ－イエ ヤン
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ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu

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  • 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)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
JP2018553365A 2016-04-12 2017-04-06 Ｂｅｔタンパク質分解剤 Expired - Fee Related JP7072519B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662321499P 2016-04-12 2016-04-12
US62/321,499 2016-04-12
US201662393888P 2016-09-13 2016-09-13
US62/393,888 2016-09-13
PCT/US2017/026278 WO2017180417A1 (en) 2016-04-12 2017-04-06 Bet protein degraders

Publications (3)

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JP2019511528A JP2019511528A (ja) 2019-04-25
JP2019511528A5 JP2019511528A5 (enExample) 2020-05-14
JP7072519B2 true JP7072519B2 (ja) 2022-05-20

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JP2018553365A Expired - Fee Related JP7072519B2 (ja) 2016-04-12 2017-04-06 Ｂｅｔタンパク質分解剤

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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 (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017185036A1 (en) 2016-04-22 2017-10-26 Dana Farber Cancer Institute, Inc. Bifunctional molecules for degradation of egfr and methods of use
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
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
WO2017197046A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for 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
US11285218B2 (en) * 2016-06-23 2022-03-29 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
EP4717317A3 (en) 2017-06-20 2026-06-03 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
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
WO2019043217A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROBENZIMIDAZOLONES
US10632209B2 (en) * 2017-11-10 2020-04-28 The Regents Of The University Of Michigan ASH1L inhibitors and methods of treatment therewith
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
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
US11969472B2 (en) 2018-08-22 2024-04-30 Cullgen (Shanghai), Inc. Tropomyosin receptor kinase (TRK) degradation compounds and methods of use
MX2021001957A (es) 2018-08-22 2021-07-15 Cullgen Shanghai Inc Compuestos de degradacion y metodos de uso del receptor de tropomiosina quinasa (trk).
WO2020051235A1 (en) 2018-09-04 2020-03-12 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
CA3121667A1 (en) * 2018-09-30 2020-04-02 Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Isoindoline compound, preparation method, pharmaceutical composition and use thereof
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
EP3897631A4 (en) 2018-12-20 2022-11-23 C4 Therapeutics, Inc. TARGETED PROTEIN BREAKDOWN
WO2020146250A1 (en) * 2019-01-07 2020-07-16 Dana-Farber Cancer Institute, Inc. SMALL MOLECULE DEGRADERS OF FKBP12 VIA RECRUITMENT OF VON HIPPEL-LINDAU E3 UBIQUITIN LIGASE (VHL) E3 UBIQUITIN LIGASE, AND USES 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
EP4029499A4 (en) * 2019-06-12 2023-07-26 Shanghaitech University Alk protein regulator and anti-tumor application thereof
CN114502534A (zh) * 2019-09-30 2022-05-13 协和麒麟株式会社 Bet降解剂
BR112022016901A2 (pt) 2020-02-26 2022-12-06 Cullgen Shanghai Inc Compostos de degradação do receptor de tropomiosina quinase (trk) e métodos de uso
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
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
CN116490186B (zh) 2020-08-05 2025-10-31 C4医药公司 用于ret的靶向降解的化合物
WO2022051616A1 (en) * 2020-09-03 2022-03-10 Board Of Regents Of The University Of Nebraska Cdk targeted heterobifunctional small molecule proteolysis targeting chimeras
US20240287076A1 (en) 2021-05-05 2024-08-29 Biogen Ma Inc. Compounds for targeting degradation of bruton's tyrosine kinase
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
CA3224732A1 (en) 2021-07-07 2023-01-12 Kevin M. Guckian Compounds for targeting degradation of irak4 proteins
WO2023283372A1 (en) 2021-07-07 2023-01-12 Biogen Ma Inc. Compounds for targeting degradation of irak4 proteins
EP4511128A1 (en) 2022-04-20 2025-02-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
CA3260847A1 (en) 2022-06-27 2024-01-04 Relay Therapeutics, Inc. Estrogen Alpha Receptor Degrading Agents and Their Uses
WO2024006776A1 (en) 2022-06-27 2024-01-04 Relay Therapeutics, Inc. Estrogen receptor alpha degraders and medical 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
US20240383910A1 (en) * 2023-05-15 2024-11-21 Baylor College Of Medicine Small molecule btk degraders and methods of use thereof
WO2024243441A1 (en) 2023-05-24 2024-11-28 Kumquat Biosciences Inc. Heterocyclic compounds and uses thereof
EP4735451A1 (en) 2023-06-30 2026-05-06 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
CN122228262A (zh) 2023-11-02 2026-06-16 金橘生物科技公司 降解剂及其用途
WO2026151924A1 (en) * 2025-01-09 2026-07-16 Triana Biomedicines, Inc. 2-(2, 6-dioxopiperidine-3-yl)-1, 3-dioxoisoindoline derivatives bearing an heteroaryl group as anaplastic lymphoma kinase (alk) degraders and uses thereof

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014164596A1 (en) 2013-03-11 2014-10-09 The Regents Of The University Of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
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
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
US20150291562A1 (en) 2014-04-14 2015-10-15 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
US20160058872A1 (en) 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use

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
WO1998011111A1 (en) 1996-09-13 1998-03-19 Yoshitomi Pharmaceutical Industries, Ltd. Thienotriazolodiazepine compounds and medicinal uses thereof
US7091353B2 (en) * 2000-12-27 2006-08-15 Celgene Corporation Isoindole-imide compounds, compositions, and uses thereof
US20030045552A1 (en) * 2000-12-27 2003-03-06 Robarge Michael J. 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
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
CA2957226C (en) * 2008-10-29 2018-08-14 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
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
AU2010317096B2 (en) 2009-11-05 2015-03-26 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
SG183257A1 (en) * 2010-02-11 2012-09-27 Celgene Corp Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
ES2606958T3 (es) 2010-05-14 2017-03-28 Dana-Farber Cancer Institute, Inc. Compuestos de tienotriazolodiazepina para tratar una neoplasia
WO2011143651A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for modulating metabolism
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
JO2998B1 (ar) * 2010-06-04 2016-09-05 Amgen Inc مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان
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
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
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
WO2014134201A1 (en) * 2013-02-28 2014-09-04 Amgen Inc. A benzoic acid derivative mdm2 inhibitor for the treatment of cancer
EP3262045A1 (en) * 2015-02-27 2018-01-03 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
EP3440082A1 (en) * 2016-04-06 2019-02-13 The Regents of The University of Michigan Monofunctional intermediates for ligand-dependent target protein degradation

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2014164596A1 (en) 2013-03-11 2014-10-09 The Regents Of The University Of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
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
US20150291562A1 (en) 2014-04-14 2015-10-15 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
US20160058872A1 (en) 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Winter, Georg E. et al，Phthalimide conjugation as a strategy for in vivo target protein degradation，Science，2015年，348 (6241)，1376-1381
Zengerle, Michael; Chan, Kwok-Ho; Ciulli, Alessio，Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4，ACS Chemical Biology，2015年，10 (8)，1770-1777

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RU2018139537A (ru) 2020-05-14
RU2018139537A3 (enExample) 2020-08-11
JP2019511528A (ja) 2019-04-25
RU2752677C2 (ru) 2021-07-29
IL262139A (en) 2018-11-29
KR20180132861A (ko) 2018-12-12
AU2017250076A1 (en) 2018-11-08
UA123168C2 (uk) 2021-02-24
MX2018012379A (es) 2019-07-04
EP3442976A1 (en) 2019-02-20
US20190169195A1 (en) 2019-06-06
CN109311890A (zh) 2019-02-05
US10633386B2 (en) 2020-04-28
AU2017250076B2 (en) 2021-07-22
SG11201808729WA (en) 2018-11-29
CA3020541A1 (en) 2017-10-19
ZA201806969B (en) 2019-12-18
IL262139B (en) 2021-05-31
EP3442976B1 (en) 2022-07-20
WO2017180417A1 (en) 2017-10-19
BR112018070859A2 (pt) 2019-02-05
CN109311890B (zh) 2021-08-31
MX384905B (es) 2025-03-14

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