AU2017250076B2 - Bet protein degraders - Google Patents

Bet protein degraders Download PDF

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Publication number
AU2017250076B2
AU2017250076B2 AU2017250076A AU2017250076A AU2017250076B2 AU 2017250076 B2 AU2017250076 B2 AU 2017250076B2 AU 2017250076 A AU2017250076 A AU 2017250076A AU 2017250076 A AU2017250076 A AU 2017250076A AU 2017250076 B2 AU2017250076 B2 AU 2017250076B2
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AU
Australia
Prior art keywords
meo
group
compound
pharmaceutically acceptable
another embodiment
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Ceased
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AU2017250076A
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English (en)
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AU2017250076A1 (en
Inventor
Longchuan Bai
Jiantao HU
Shaomeng Wang
Fuming XU
Chao-Yie Yang
Bing Zhou
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University of Michigan System
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University of Michigan System
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Publication of AU2017250076A1 publication Critical patent/AU2017250076A1/en
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Publication of AU2017250076B2 publication Critical patent/AU2017250076B2/en
Ceased legal-status Critical Current
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    • 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
    • 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
    • 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)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (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)
AU2017250076A 2016-04-12 2017-04-06 Bet protein degraders Ceased AU2017250076B2 (en)

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 (2)

Publication Number Publication Date
AU2017250076A1 AU2017250076A1 (en) 2018-11-08
AU2017250076B2 true AU2017250076B2 (en) 2021-07-22

Family

ID=58548921

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2017250076A Ceased AU2017250076B2 (en) 2016-04-12 2017-04-06 Bet protein degraders

Country Status (15)

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

Families Citing this family (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6968823B2 (ja) 2016-04-22 2021-11-17 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 Ｅｇｆｒの分解のための二官能性分子、及び使用方法
EP3455218A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
WO2017197036A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
EP4491236A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
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
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
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
WO2019043208A1 (en) 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROQUINOLINONES
CN111315735B (zh) 2017-09-04 2024-03-08 C4医药公司 二氢苯并咪唑酮
EP3679026A1 (en) 2017-09-04 2020-07-15 C4 Therapeutics, Inc. Glutarimide
US11110177B2 (en) * 2017-11-10 2021-09-07 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
CA3110267A1 (en) 2018-08-22 2020-02-27 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
CN110963994B (zh) * 2018-09-30 2022-02-08 中国科学院上海药物研究所 异吲哚啉类化合物、其制备方法、药物组合物及用途
US12161648B2 (en) 2018-10-09 2024-12-10 The Regents Of The University Of California Covalent targeting of E3 ligases
CN120698985A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
CA3126009A1 (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
US12390532B2 (en) * 2019-06-12 2025-08-19 Shanghaitech University ALK protein regulator and anti-tumor application thereof
AU2020360170A1 (en) * 2019-09-30 2022-05-19 Kyowa Kirin Co., Ltd. Bet degrader
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
CN115697989B (zh) 2020-02-26 2025-03-18 上海睿跃生物科技有限公司 原肌球蛋白受体激酶(trk)降解化合物和使用方法
AU2021231898A1 (en) 2020-03-05 2022-10-27 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
JP2023538517A (ja) 2020-08-05 2023-09-08 シーフォー セラピューティクス， インコーポレイテッド Ｒｅｔの標的分解のための化合物
WO2022051616A1 (en) * 2020-09-03 2022-03-10 Board Of Regents Of The University Of Nebraska Cdk targeted heterobifunctional small molecule proteolysis targeting chimeras
CA3217417A1 (en) 2021-05-05 2022-11-10 Kevin M. Guckian 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
US20250018046A1 (en) 2021-07-07 2025-01-16 Biogen Ma Inc Compounds for targeting degradation of irak4 proteins
AU2022308734A1 (en) 2021-07-07 2024-02-22 Biogen Ma Inc. Compounds for targeting degradation of irak4 proteins
WO2024006776A1 (en) 2022-06-27 2024-01-04 Relay Therapeutics, Inc. Estrogen receptor alpha degraders and medical use thereof
TW202417425A (zh) 2022-06-27 2024-05-01 美商傳達治療有限公司 雌激素受體α降解劑及其使用方法
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
WO2024243441A1 (en) 2023-05-24 2024-11-28 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
WO2025096855A1 (en) 2023-11-02 2025-05-08 Kumquat Biosciences Inc. Degraders and uses thereof

Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002059106A1 (en) * 2000-12-27 2002-08-01 Celgene Corporation Isoindole-imide compounds, compositions, and uses thereof
US20030096841A1 (en) * 2000-12-27 2003-05-22 Robarge Michael J. Isoindole-imide compounds, compositions, and uses thereof
WO2011153509A1 (en) * 2010-06-04 2011-12-08 Amgen Inc. Piperidinone derivatives as mdm2 inhibitors for the treatment of cancer
WO2013158644A2 (en) * 2012-04-16 2013-10-24 Synta Pharmaceuticals Corp. Targeted therapeutics
WO2014134201A1 (en) * 2013-02-28 2014-09-04 Amgen Inc. A benzoic acid derivative mdm2 inhibitor for the treatment of cancer
US20140256706A1 (en) * 2013-03-11 2014-09-11 The Regents Of The University Of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
US20150246923A1 (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
WO2017030814A1 (en) * 2015-08-19 2017-02-23 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
US20180036294A1 (en) * 2015-02-27 2018-02-08 The Regents Of The University Of Michigan 9h-pyrimido [4,5-b] indoles as bet bromodomain inhibitors
US20190119289A1 (en) * 2016-04-06 2019-04-25 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation

Family Cites Families (41)

* 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
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
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
PE20140963A1 (es) * 2008-10-29 2014-08-06 Celgene Corp Compuestos de isoindolina para el tratamiento de cancer
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
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
EP3050885B1 (en) 2009-11-05 2017-10-18 GlaxoSmithKline LLC Benzodiazepine bromodomain inhibitor
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
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
HUE031073T2 (en) 2010-05-14 2017-06-28 Dana Farber Cancer Inst Inc Thieno triazolo-diazepine compounds for the treatment of neoplasia
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
WO2011161031A1 (en) 2010-06-22 2011-12-29 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
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
KR102438072B1 (ko) 2012-01-12 2022-08-31 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
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.

Patent Citations (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002059106A1 (en) * 2000-12-27 2002-08-01 Celgene Corporation Isoindole-imide compounds, compositions, and uses thereof
US20030096841A1 (en) * 2000-12-27 2003-05-22 Robarge Michael J. Isoindole-imide compounds, compositions, and uses thereof
WO2011153509A1 (en) * 2010-06-04 2011-12-08 Amgen Inc. Piperidinone derivatives as mdm2 inhibitors for the treatment of cancer
WO2013158644A2 (en) * 2012-04-16 2013-10-24 Synta Pharmaceuticals Corp. Targeted therapeutics
WO2014134201A1 (en) * 2013-02-28 2014-09-04 Amgen Inc. A benzoic acid derivative mdm2 inhibitor for the treatment of cancer
US20170281773A1 (en) * 2013-03-11 2017-10-05 The Regents Of The University Of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
WO2014164596A1 (en) * 2013-03-11 2014-10-09 The Regents Of The University Of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
US20140256706A1 (en) * 2013-03-11 2014-09-11 The Regents Of The University Of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
US9675697B2 (en) * 2013-03-11 2017-06-13 The Regents Of The University Of Michigan BET bromodomain inhibitors and therapeutic methods using the same
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
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
US20170210761A1 (en) * 2014-02-28 2017-07-27 The Regents Of The University Of Michigan 9h-pyrimido [4,5-b]indoles and related analogs as bet bromodomain inhibitors
US20150246923A1 (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
US10253044B2 (en) * 2014-02-28 2019-04-09 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
US20150291562A1 (en) * 2014-04-14 2015-10-15 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
US20180036294A1 (en) * 2015-02-27 2018-02-08 The Regents Of The University Of Michigan 9h-pyrimido [4,5-b] indoles as bet bromodomain inhibitors
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
WO2017030814A1 (en) * 2015-08-19 2017-02-23 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
US20190119289A1 (en) * 2016-04-06 2019-04-25 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation

Also Published As

Publication number Publication date
EP3442976B1 (en) 2022-07-20
SG11201808729WA (en) 2018-11-29
RU2018139537A (ru) 2020-05-14
RU2752677C2 (ru) 2021-07-29
CN109311890A (zh) 2019-02-05
US20190169195A1 (en) 2019-06-06
AU2017250076A1 (en) 2018-11-08
IL262139A (en) 2018-11-29
ZA201806969B (en) 2019-12-18
CN109311890B (zh) 2021-08-31
JP7072519B2 (ja) 2022-05-20
JP2019511528A (ja) 2019-04-25
CA3020541A1 (en) 2017-10-19
KR20180132861A (ko) 2018-12-12
BR112018070859A2 (pt) 2019-02-05
MX384905B (es) 2025-03-14
EP3442976A1 (en) 2019-02-20
RU2018139537A3 (OSRAM) 2020-08-11
MX2018012379A (es) 2019-07-04
IL262139B (en) 2021-05-31
UA123168C2 (uk) 2021-02-24
US10633386B2 (en) 2020-04-28
WO2017180417A1 (en) 2017-10-19

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