CO2022002842A2 - Degradadores bifuncionales de brd9 y sus métodos de uso - Google Patents
Degradadores bifuncionales de brd9 y sus métodos de usoInfo
- Publication number
- CO2022002842A2 CO2022002842A2 CONC2022/0002842A CO2022002842A CO2022002842A2 CO 2022002842 A2 CO2022002842 A2 CO 2022002842A2 CO 2022002842 A CO2022002842 A CO 2022002842A CO 2022002842 A2 CO2022002842 A2 CO 2022002842A2
- Authority
- CO
- Colombia
- Prior art keywords
- brd9
- methods
- degraders
- bifunctional
- bromodomain protein
- Prior art date
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)
- 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)
Applications Claiming Priority (5)
| 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 | |
| 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 |
|---|---|
| CO2022002842A2 true CO2022002842A2 (es) | 2022-04-19 |
Family
ID=72915891
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CONC2022/0002842A CO2022002842A2 (es) | 2019-09-16 | 2022-03-11 | Degradadores bifuncionales de brd9 y sus métodos de uso |
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=) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9227969B2 (en) | 2013-08-14 | 2016-01-05 | Novartis Ag | Compounds and compositions as inhibitors of MEK |
| WO2016105518A1 (en) * | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| US9694084B2 (en) * | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| US11319318B2 (en) * | 2015-03-05 | 2022-05-03 | Boehringer Ingelheim International Gmbh | Pyridinones and isoquinolinones as inhibitors of the bromodomain BRD9 |
| 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 |
| WO2018064589A1 (en) * | 2016-09-29 | 2018-04-05 | Dana-Farber Cancer Institute, Inc. | Targeted protein degradation using a mutant e3 ubiquitin ligase |
| IL312367A (en) * | 2017-01-31 | 2024-06-01 | Arvinas Operations Inc | Cereblon ligands and bifunctional compounds comprising the same |
| EP3710443A1 (en) * | 2017-11-17 | 2020-09-23 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides |
| JP2021506848A (ja) * | 2017-12-18 | 2021-02-22 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | Ｅ３ユビキチンリガーゼ部分を持つｅｇｆｒを有する二官能性阻害剤 |
| WO2019140387A1 (en) * | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Crbn ligands and uses thereof |
| EP3774808A1 (en) * | 2018-03-26 | 2021-02-17 | Novartis AG | 3-hydroxy-n-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)pyrrolidine-1-carboxamide derivatives |
| 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 |
| 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 |
| CN113874016A (zh) * | 2019-01-29 | 2021-12-31 | 福宏治疗公司 | 化合物及其用途 |
-
2020
- 2020-09-14 JP JP2022515701A patent/JP2022547952A/ja active Pending
- 2020-09-14 WO PCT/US2020/050768 patent/WO2021055295A1/en not_active Ceased
- 2020-09-14 PE PE2022000406A patent/PE20221417A1/es unknown
- 2020-09-14 AU AU2020349451A patent/AU2020349451B2/en not_active Ceased
- 2020-09-14 TW TW109131573A patent/TW202123942A/zh unknown
- 2020-09-14 CN CN202080061458.1A patent/CN114641473A/zh active Pending
- 2020-09-14 EP EP20793192.4A patent/EP4041724A1/en active Pending
- 2020-09-14 PY PY202002054376A patent/PY2054376A/es unknown
- 2020-09-14 CR CR20220105A patent/CR20220105A/es unknown
- 2020-09-14 PH PH1/2022/550611A patent/PH12022550611A1/en unknown
- 2020-09-14 CA CA3153529A patent/CA3153529A1/en active Pending
- 2020-09-14 BR BR112022003514A patent/BR112022003514A2/pt unknown
- 2020-09-14 MX MX2022003102A patent/MX2022003102A/es unknown
- 2020-09-14 KR KR1020227010572A patent/KR20220063192A/ko not_active Ceased
- 2020-09-14 US US17/020,114 patent/US20220315578A1/en active Pending
- 2020-09-14 UY UY0001038880A patent/UY38880A/es not_active Application Discontinuation
-
2022
- 2022-02-16 IL IL290677A patent/IL290677A/en unknown
- 2022-03-10 DO DO2022000053A patent/DOP2022000053A/es unknown
- 2022-03-11 CO CONC2022/0002842A patent/CO2022002842A2/es unknown
- 2022-03-11 EC ECSENADI202218571A patent/ECSP22018571A/es unknown
- 2022-03-15 JO JOP/2022/0069A patent/JOP20220069A1/ar unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2020349451B2 (en) | 2024-02-01 |
| 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 |
| UY38880A (es) | 2021-04-30 |
| TW202123942A (zh) | 2021-07-01 |
| CA3153529A1 (en) | 2021-03-25 |
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