ZA201806969B - Bet protein degraders - Google Patents

Bet protein degraders

Info

Publication number
ZA201806969B
ZA201806969B ZA2018/06969A ZA201806969A ZA201806969B ZA 201806969 B ZA201806969 B ZA 201806969B ZA 2018/06969 A ZA2018/06969 A ZA 2018/06969A ZA 201806969 A ZA201806969 A ZA 201806969A ZA 201806969 B ZA201806969 B ZA 201806969B
Authority
ZA
South Africa
Prior art keywords
bet protein
protein degraders
degraders
bet
protein
Prior art date
Application number
ZA2018/06969A
Other languages
English (en)
Inventor
Wang Shaomeng
Zhou Bing
Xu Fuming
Hu Jiantao
Bai Longchuan
Yang Chao-Yie
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 ZA201806969B publication Critical patent/ZA201806969B/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)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
ZA2018/06969A 2016-04-12 2018-10-18 Bet protein degraders ZA201806969B (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 (1)

Publication Number Publication Date
ZA201806969B true ZA201806969B (en) 2019-12-18

Family

ID=58548921

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA2018/06969A ZA201806969B (en) 2016-04-12 2018-10-18 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 (45)

* 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
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
WO2017197046A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation
WO2017197051A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Amine-linked c3-glutarimide degronimers for target protein degradation
EP3474900A4 (en) * 2016-06-23 2020-03-11 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
EP3679026A1 (en) 2017-09-04 2020-07-15 C4 Therapeutics, Inc. Glutarimide
CN111278816B (zh) 2017-09-04 2024-03-15 C4医药公司 二氢喹啉酮
CN118206529A (zh) 2017-09-04 2024-06-18 C4医药公司 二氢苯并咪唑酮
JP2021502388A (ja) * 2017-11-10 2021-01-28 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン Ash1l阻害剤及びそれを用いた治療方法
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
WO2019191112A1 (en) 2018-03-26 2019-10-03 C4 Therapeutics, Inc. Cereblon binders for the degradation of ikaros
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
IL280984B2 (en) 2018-08-22 2025-02-01 Cullgen Shanghai Inc Tropomyosin receptor kinase (TRK) inhibitor 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
CN114085212B (zh) * 2018-09-30 2023-05-02 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
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
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
CN113348168A (zh) * 2019-01-22 2021-09-03 默克专利有限公司 杂环衍生物
CA3141413C (en) * 2019-06-12 2024-05-14 Xiaobao Yang Alk protein regulator and anti-tumor application thereof
WO2021065980A1 (ja) * 2019-09-30 2021-04-08 協和キリン株式会社 Bet分解剤
WO2023205701A1 (en) 2022-04-20 2023-10-26 Kumquat Biosciences Inc. Macrocyclic heterocycles and uses thereof
US12410171B2 (en) 2020-02-26 2025-09-09 Cullgen (Shanghai), Inc. Tropomyosin receptor kinase (TRK) degradation compounds and methods of use
JP7746278B2 (ja) 2020-03-05 2025-09-30 シーフォー セラピューティクス, インコーポレイテッド Brd9の標的分解のための化合物
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
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
UY39756A (es) 2021-05-05 2022-11-30 Biogen Ma Inc Compuestos para la degradación dirigida de la tirosina cinasa 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
WO2023283372A1 (en) 2021-07-07 2023-01-12 Biogen Ma Inc. Compounds for targeting degradation of irak4 proteins
IL309941A (en) 2021-07-07 2024-03-01 Biogen Ma Inc Compounds to target degradation of IRAK4 proteins
JP2025521686A (ja) 2022-06-27 2025-07-10 リレー セラピューティクス, インコーポレイテッド エストロゲン受容体アルファ分解剤及びその使用
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
AU2024276994A1 (en) 2023-05-24 2025-10-23 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
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
WO1998011111A1 (en) 1996-09-13 1998-03-19 Yoshitomi Pharmaceutical Industries, Ltd. Thienotriazolodiazepine compounds and medicinal uses thereof
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"
US8044042B2 (en) 2005-05-30 2011-10-25 Mitsubishi Tanabe Pharma Corporation Thienotriazolodiazepine compound and medicinal use thereof
NZ579355A (en) 2007-02-01 2012-03-30 Resverlogix Corp 2-(Aryl)-4-oxo-quinazoline derivatives
CN101910182B (zh) 2007-12-28 2013-07-17 田边三菱制药株式会社 抗癌剂
SI2346837T1 (sl) 2008-06-26 2015-05-29 Resverlogix Corporation Postopki pripravljanja kinazolinonskih derivatov
EP3354646A1 (en) * 2008-10-29 2018-08-01 Celgene Corporation Isoindoline compounds for use in the treatment of cancer
JP5813626B2 (ja) 2009-04-22 2015-11-17 レスバーロジックス コーポレイション 新規抗炎症剤
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
GB0919423D0 (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
WO2011054845A1 (en) 2009-11-05 2011-05-12 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
TR201903027T4 (tr) * 2010-02-11 2019-03-21 Celgene Corp Arilmetoksi izoindolin türevleri ve bunları içeren kompozisyonlar ve bunları kullanma yöntemleri.
BR112012029005A2 (pt) 2010-05-14 2016-07-26 Dana Farber Cancer Inst Inc composições e métodos de tratamento de neoplasia, doença inflamatória e outros distúrbios
US20130252331A1 (en) 2010-05-14 2013-09-26 James Elliott Bradner Compositions and methods for modulating metabolism
CA2799403C (en) 2010-05-14 2020-01-21 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating leukemia
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
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
US20140066410A1 (en) 2011-02-23 2014-03-06 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
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
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
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
MX2014012635A (es) 2012-04-20 2015-05-15 Abbvie Inc Derivados de isoindolona.
BR112014031068A2 (pt) 2012-06-12 2017-06-27 Abbvie Inc derivados piridinona e piridazinona
JP6266659B2 (ja) * 2013-02-28 2018-01-24 アムジエン・インコーポレーテツド 癌の治療のための安息香酸誘導体mdm2阻害剤
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
EP3110818B1 (en) * 2014-02-28 2019-10-23 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
EP3131588B1 (en) 2014-04-14 2025-11-05 Arvinas Operations, Inc. Imide-based modulators of proteolysis and associated methods of use
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
UA123168C2 (uk) 2021-02-24
AU2017250076B2 (en) 2021-07-22
RU2018139537A3 (enExample) 2020-08-11
MX2018012379A (es) 2019-07-04
RU2752677C2 (ru) 2021-07-29
BR112018070859A2 (pt) 2019-02-05
AU2017250076A1 (en) 2018-11-08
WO2017180417A1 (en) 2017-10-19
IL262139A (en) 2018-11-29
CA3020541A1 (en) 2017-10-19
MX384905B (es) 2025-03-14
CN109311890B (zh) 2021-08-31
KR20180132861A (ko) 2018-12-12
SG11201808729WA (en) 2018-11-29
EP3442976B1 (en) 2022-07-20
US10633386B2 (en) 2020-04-28
EP3442976A1 (en) 2019-02-20
RU2018139537A (ru) 2020-05-14
IL262139B (en) 2021-05-31
US20190169195A1 (en) 2019-06-06
JP7072519B2 (ja) 2022-05-20
CN109311890A (zh) 2019-02-05
JP2019511528A (ja) 2019-04-25

Similar Documents

Publication Publication Date Title
ZA201806969B (en) Bet protein degraders
GB201502305D0 (en) Protein
GB201502306D0 (en) Protein
GB201608885D0 (en) Treatment
GB201415344D0 (en) Protein
PL3702450T3 (pl) Białko
GB201515745D0 (en) Proteins
GB201511787D0 (en) Proteins
GB201609597D0 (en) Therapy
GB2558968B (en) G Proteins
GB201513033D0 (en) Proteins
PL3099793T3 (pl) Białko
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
PH32016001297S1 (en) Hand lamp
PH32016001296S1 (en) Hand lamp
GB201617107D0 (en) Treatment
GB201616374D0 (en) Modified bulgeomers