AU2020349451B2 - BRD9 bifunctional degraders and their methods of use - Google Patents

BRD9 bifunctional degraders and their methods of use Download PDF

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Publication number
AU2020349451B2
AU2020349451B2 AU2020349451A AU2020349451A AU2020349451B2 AU 2020349451 B2 AU2020349451 B2 AU 2020349451B2 AU 2020349451 A AU2020349451 A AU 2020349451A AU 2020349451 A AU2020349451 A AU 2020349451A AU 2020349451 B2 AU2020349451 B2 AU 2020349451B2
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AU
Australia
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compound
group
formula
alkyl
alkylene
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Ceased
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AU2020349451A
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English (en)
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AU2020349451A1 (en
Inventor
Xin Chen
Marie-Line GOUDE
Edmund Martin Harrington
Gregory John Hollingworth
Julien LORBER
Martin Sendzik
Anna Vulpetti
Thomas Zoller
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Novartis AG
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Novartis AG
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    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2020349451A 2019-09-16 2020-09-14 BRD9 bifunctional degraders and their methods of use Ceased AU2020349451B2 (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201962900869P 2019-09-16 2019-09-16
US201962900865P 2019-09-16 2019-09-16
US201962900863P 2019-09-16 2019-09-16
US201962900860P 2019-09-16 2019-09-16
US62/900,863 2019-09-16
US62/900,860 2019-09-16
US62/900,865 2019-09-16
US62/900,869 2019-09-16
PCT/US2020/050768 WO2021055295A1 (en) 2019-09-16 2020-09-14 Brd9 bifunctional degraders and their methods of use

Publications (2)

Publication Number Publication Date
AU2020349451A1 AU2020349451A1 (en) 2022-04-21
AU2020349451B2 true AU2020349451B2 (en) 2024-02-01

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ID=72915891

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Application Number Title Priority Date Filing Date
AU2020349451A Ceased AU2020349451B2 (en) 2019-09-16 2020-09-14 BRD9 bifunctional degraders and their methods of use

Country Status (21)

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

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EP3746135A4 (en) 2018-01-30 2022-03-09 Foghorn Therapeutics Inc. METHODS AND COMPOUNDS FOR TREATMENT OF DISEASE
CN111936498B (zh) 2018-03-26 2024-04-16 诺华股份有限公司 N-(3-(7H-吡咯并[2,3-d]嘧啶-4-基)苯基)苯甲酰胺衍生物
US12384776B2 (en) 2019-01-29 2025-08-12 Foghorn Therapeutics Inc. Compounds and uses thereof
EP3917517A4 (en) 2019-01-29 2023-01-25 Foghorn Therapeutics Inc. CONNECTIONS AND USES THEREOF
CN113874016A (zh) 2019-01-29 2021-12-31 福宏治疗公司 化合物及其用途
US20230066136A1 (en) 2019-01-29 2023-03-02 Foghorn Therapeutics Inc. Compounds and uses thereof
WO2021022163A2 (en) 2019-07-31 2021-02-04 Foghorn Therapeutics Inc. Compounds and uses thereof
CN114521196A (zh) * 2019-09-16 2022-05-20 诺华股份有限公司 双官能团降解剂及其使用方法
CR20220160A (es) 2019-09-16 2022-06-16 Takeda Pharmaceuticals Co Derivados de piridazin-3(2h)-ona fusionados con azol
EP4096651A4 (en) * 2020-01-29 2024-01-24 Foghorn Therapeutics Inc. COMPOUNDS AND THEIR USES
US12528825B2 (en) 2020-01-29 2026-01-20 Foghorn Therapeutics Inc. Compounds and uses thereof
TW202146412A (zh) 2020-03-05 2021-12-16 美商Ｃ４醫藥公司 用於標靶降解brd9之化合物
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
WO2023039208A1 (en) * 2021-09-09 2023-03-16 C4 Therapeutics, Inc. Selected compounds for targeted degradation of brd9
WO2023109892A1 (zh) * 2021-12-15 2023-06-22 海思科医药集团股份有限公司 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
KR20260029501A (ko) 2023-05-24 2026-03-04 베액티카 테라퓨틱스 아베 Tead에 대한 결합제로서의 방향족 아미드 및 이의 접합체
CN121816348A (zh) 2023-08-11 2026-04-07 深圳众格生物科技有限公司 一种降解irak4的蛋白降解靶向嵌合体化合物及其应用
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

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WO2017223452A1 (en) * 2016-06-23 2017-12-28 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
WO2020051235A1 (en) * 2018-09-04 2020-03-12 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
WO2020160198A1 (en) * 2019-01-29 2020-08-06 Foghorn Therapeutics Inc. Compounds and uses thereof

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Also Published As

Publication number Publication date
CN114641473A (zh) 2022-06-17
EP4041724A1 (en) 2022-08-17
KR20220063192A (ko) 2022-05-17
PY2054376A (es) 2021-09-07
PH12022550611A1 (en) 2023-03-13
BR112022003514A2 (pt) 2022-05-17
WO2021055295A1 (en) 2021-03-25
ECSP22018571A (es) 2022-04-29
US20220315578A1 (en) 2022-10-06
JOP20220069A1 (ar) 2023-01-30
AU2020349451A1 (en) 2022-04-21
MX2022003102A (es) 2022-04-06
JP2022547952A (ja) 2022-11-16
PE20221417A1 (es) 2022-09-20
IL290677A (en) 2022-04-01
DOP2022000053A (es) 2023-01-31
CR20220105A (es) 2022-06-13
CO2022002842A2 (es) 2022-04-19
UY38880A (es) 2021-04-30
TW202123942A (zh) 2021-07-01
CA3153529A1 (en) 2021-03-25

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