PE20221417A1 - Degradadores bifuncionales de brd9 y sus metodos de uso - Google Patents

Degradadores bifuncionales de brd9 y sus metodos de uso

Info

Publication number
PE20221417A1
PE20221417A1 PE2022000406A PE2022000406A PE20221417A1 PE 20221417 A1 PE20221417 A1 PE 20221417A1 PE 2022000406 A PE2022000406 A PE 2022000406A PE 2022000406 A PE2022000406 A PE 2022000406A PE 20221417 A1 PE20221417 A1 PE 20221417A1
Authority
PE
Peru
Prior art keywords
brd9
methods
degraders
bifunctional
bifunctional degraders
Prior art date
Application number
PE2022000406A
Other languages
English (en)
Spanish (es)
Inventor
Julien Lorber
Martin Sendzik
Xin Chen
Marie-Line Goude
Edmund Martin Harrington
Gregory John Hollingworth
Anna Vulpetti
Thomas Zoller
Original Assignee
Novartis Ag
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=72915891&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20221417(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20221417A1 publication Critical patent/PE20221417A1/es

Links

Classifications

    • 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
PE2022000406A 2019-09-16 2020-09-14 Degradadores bifuncionales de brd9 y sus metodos de uso PE20221417A1 (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962900869P 2019-09-16 2019-09-16
US201962900860P 2019-09-16 2019-09-16
US201962900863P 2019-09-16 2019-09-16
US201962900865P 2019-09-16 2019-09-16
PCT/US2020/050768 WO2021055295A1 (en) 2019-09-16 2020-09-14 Brd9 bifunctional degraders and their methods of use

Publications (1)

Publication Number Publication Date
PE20221417A1 true PE20221417A1 (es) 2022-09-20

Family

ID=72915891

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022000406A PE20221417A1 (es) 2019-09-16 2020-09-14 Degradadores bifuncionales de brd9 y sus metodos de uso

Country Status (21)

Country Link
US (1) US20220315578A1 (enExample)
EP (1) EP4041724A1 (enExample)
JP (1) JP2022547952A (enExample)
KR (1) KR20220063192A (enExample)
CN (1) CN114641473A (enExample)
AU (1) AU2020349451B2 (enExample)
BR (1) BR112022003514A2 (enExample)
CA (1) CA3153529A1 (enExample)
CO (1) CO2022002842A2 (enExample)
CR (1) CR20220105A (enExample)
DO (1) DOP2022000053A (enExample)
EC (1) ECSP22018571A (enExample)
IL (1) IL290677A (enExample)
JO (1) JOP20220069A1 (enExample)
MX (1) MX2022003102A (enExample)
PE (1) PE20221417A1 (enExample)
PH (1) PH12022550611A1 (enExample)
PY (1) PY2054376A (enExample)
TW (1) TW202123942A (enExample)
UY (1) UY38880A (enExample)
WO (1) WO2021055295A1 (enExample)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112236172A (zh) 2018-01-30 2021-01-15 福宏治疗公司 用于治疗病症的方法和化合物
EP3774804A1 (en) 2018-03-26 2021-02-17 Novartis AG N-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)benzamide derivatives
US12384776B2 (en) 2019-01-29 2025-08-12 Foghorn Therapeutics Inc. Compounds and uses thereof
WO2020160193A2 (en) 2019-01-29 2020-08-06 Foghorn Therapeutics Inc. Compounds and uses thereof
WO2020160192A1 (en) 2019-01-29 2020-08-06 Foghorn Therapeutics Inc. Compounds and uses thereof
US20230066136A1 (en) 2019-01-29 2023-03-02 Foghorn Therapeutics Inc. Compounds and uses thereof
EP3917517A4 (en) 2019-01-29 2023-01-25 Foghorn Therapeutics Inc. CONNECTIONS AND USES THEREOF
WO2021022163A2 (en) 2019-07-31 2021-02-04 Foghorn Therapeutics Inc. Compounds and uses thereof
EP4031247A1 (en) * 2019-09-16 2022-07-27 Novartis AG Bifunctional degraders and their methods of use
TWI873185B (zh) 2019-09-16 2025-02-21 日商武田藥品工業股份有限公司 唑稠合之嗒-3(2h)-酮衍生物
MX2022009308A (es) 2020-01-29 2022-08-22 Foghorn Therapeutics Inc Compuestos y usos de estos.
US12528825B2 (en) 2020-01-29 2026-01-20 Foghorn Therapeutics Inc. Compounds and uses thereof
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
US11787800B2 (en) 2020-07-29 2023-10-17 Foghorn Therapeutics Inc. BRD9 degraders and uses thereof
US11767330B2 (en) 2021-07-06 2023-09-26 Foghorn Therapeutics Inc. Citrate salt, pharmaceutical compositions, and methods of making and using the same
CN115806547A (zh) * 2021-09-09 2023-03-17 C4医药公司 选择的用于brd9的靶向降解的化合物
CN118339151A (zh) * 2021-12-15 2024-07-12 西藏海思科制药有限公司 一种抑制或降解brd9的化合物及其组合物和药学上的应用
WO2023200800A1 (en) * 2022-04-11 2023-10-19 Foghorn Therapeutics Inc. Methods of treating androgen receptor-independent prostate cancer
WO2024163609A1 (en) * 2023-02-01 2024-08-08 Foghorn Therapeutics Inc. Compositions for treating cancer
JP2026519523A (ja) 2023-05-24 2026-06-16 ビアクティカ セラピューティクス エービー Teadへの結合剤としての芳香族アミドおよびそのコンジュゲート
EP4759807A1 (en) 2023-08-11 2026-06-17 Shenzhen Zhongge Biological Technology Co., Ltd. Proteolysis targeting chimera compound for degrading irak4 and use thereof
CN117229202B (zh) * 2023-11-15 2024-01-26 苏州美诺医药科技有限公司 一种brd9靶向降解化合物的中间体的制备方法
WO2025256550A1 (zh) * 2024-06-12 2025-12-18 杭州中美华东制药有限公司 靶向降解剂配体及连接基的制备方法

Family Cites Families (15)

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US9227969B2 (en) 2013-08-14 2016-01-05 Novartis Ag Compounds and compositions as inhibitors of MEK
JP6815318B2 (ja) * 2014-12-23 2021-01-20 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 二官能性分子によって標的化タンパク質分解を誘導する方法
US9694084B2 (en) * 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
EP3265453B1 (en) * 2015-03-05 2022-06-29 Boehringer Ingelheim International GmbH New pyridinones and isoquinolinones as inhibitors of the bromodomain brd9
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
WO2018064589A1 (en) * 2016-09-29 2018-04-05 Dana-Farber Cancer Institute, Inc. Targeted protein degradation using a mutant e3 ubiquitin ligase
IL319363A (en) * 2017-01-31 2025-05-01 Arvinas Operations Inc Cervalon ligands and bifunctional compounds containing them
US11065231B2 (en) * 2017-11-17 2021-07-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
CN111491933A (zh) * 2017-12-18 2020-08-04 豪夫迈·罗氏有限公司 具有e3泛素连接酶部分的egfr双功能抑制剂
US11512080B2 (en) * 2018-01-12 2022-11-29 Kymera Therapeutics, Inc. CRBN ligands and uses thereof
CN111936501B (zh) * 2018-03-26 2023-09-22 诺华股份有限公司 布鲁顿酪氨酸激酶降解剂
EP3774804A1 (en) * 2018-03-26 2021-02-17 Novartis AG N-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)benzamide derivatives
WO2020051235A1 (en) * 2018-09-04 2020-03-12 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
EP3917517A4 (en) * 2019-01-29 2023-01-25 Foghorn Therapeutics Inc. CONNECTIONS AND USES THEREOF
WO2020160192A1 (en) * 2019-01-29 2020-08-06 Foghorn Therapeutics Inc. Compounds and uses thereof

Also Published As

Publication number Publication date
KR20220063192A (ko) 2022-05-17
CA3153529A1 (en) 2021-03-25
EP4041724A1 (en) 2022-08-17
US20220315578A1 (en) 2022-10-06
IL290677A (en) 2022-04-01
WO2021055295A1 (en) 2021-03-25
JP2022547952A (ja) 2022-11-16
MX2022003102A (es) 2022-04-06
ECSP22018571A (es) 2022-04-29
CN114641473A (zh) 2022-06-17
DOP2022000053A (es) 2023-01-31
BR112022003514A2 (pt) 2022-05-17
CR20220105A (es) 2022-06-13
CO2022002842A2 (es) 2022-04-19
UY38880A (es) 2021-04-30
JOP20220069A1 (ar) 2023-01-30
TW202123942A (zh) 2021-07-01
AU2020349451A1 (en) 2022-04-21
PY2054376A (es) 2021-09-07
AU2020349451B2 (en) 2024-02-01
PH12022550611A1 (en) 2023-03-13

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