CA3153529A1 - Brd9 bifunctional degraders and their methods of use - Google Patents

Brd9 bifunctional degraders and their methods of use Download PDF

Info

Publication number
CA3153529A1
CA3153529A1 CA3153529A CA3153529A CA3153529A1 CA 3153529 A1 CA3153529 A1 CA 3153529A1 CA 3153529 A CA3153529 A CA 3153529A CA 3153529 A CA3153529 A CA 3153529A CA 3153529 A1 CA3153529 A1 CA 3153529A1
Authority
CA
Canada
Prior art keywords
group
compound
alkyl
alkylene
formula
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CA3153529A
Other languages
English (en)
French (fr)
Inventor
Julien LORBER
Martin Sendzik
Xin Chen
Marie-Line GOUDE
Edmund Martin Harrington
Gregory John Hollingworth
Anna Vulpetti
Thomas Zoller
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
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=CA3153529(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 CA3153529A1 publication Critical patent/CA3153529A1/en
Pending legal-status Critical Current

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)
CA3153529A 2019-09-16 2020-09-14 Brd9 bifunctional degraders and their methods of use Pending CA3153529A1 (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 (1)

Publication Number Publication Date
CA3153529A1 true CA3153529A1 (en) 2021-03-25

Family

ID=72915891

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3153529A Pending CA3153529A1 (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=)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

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
CO2022002842A2 (es) 2022-04-19
UY38880A (es) 2021-04-30
TW202123942A (zh) 2021-07-01

Similar Documents

Publication Publication Date Title
CA3153529A1 (en) Brd9 bifunctional degraders and their methods of use
CN113717156B (zh) Egfr抑制剂、其制备方法及用途
US12459921B2 (en) Isoindoline compound, preparation method, pharmaceutical composition and use thereof
US20250122202A1 (en) Egfr inhibitor, preparation method therefor and use thereof
TW202311260A (zh) 含有亞磺醯亞胺基的atr抑制劑化合物
AU2015266453C1 (en) Alk kinase inhibitor, and preparation method and use thereof
CA2787248C (en) Piperazine compound having a pgds inhibitory effect
EP3828174A1 (en) Pyridazinone derivative
WO2017129116A1 (zh) 吡咯嘧啶五元氮杂环衍生物及其应用
JP7439018B2 (ja) 置換アリールエーテル系化合物、その調製方法、医薬組成物およびその応用
US12428373B2 (en) Dopamine D2 receptor ligands
JP7030776B2 (ja) アミノピリジン誘導体およびそれらの選択的ａｌｋ－２阻害剤としての使用
CA2875494A1 (en) 2h-imidazol-4-amine compounds and their use as bace inhibitors
JP7853957B2 (ja) ピラゾールボロン酸化合物、それを含有する医薬組成物、及びそれらの使用
JP2024510778A (ja) １，３－置換シクロブチル誘導体及びその使用
KR20250055509A (ko) 치료에 사용하기 위한 parp14의 표적 단백질 분해
TW202325305A (zh) ２－（芳基－２－基）嗎啉及其氘代衍生物、製備方法和應用
EP4206184A1 (en) Phenol derivative
CN115381824B (zh) 周期蛋白依赖性激酶9抑制剂的用途
RU2823231C1 (ru) Соединение-антагонист PD-L1
JP2024105489A (ja) Μｇａτ２阻害活性を有する縮合環誘導体の製造方法
WO2025121362A1 (ja) ジオキソピペリジン誘導体およびその用途
HK40087772A (en) Phenol derivative
KR20260053336A (ko) Erk의 활성 조절을 위한 화합물 및 조성물
BR122025005591A2 (pt) Uso de e processo para preparação de derivados de ciclobutila 1,3-substituída, combinação farmacêutica, e kit

Legal Events

Date Code Title Description
MFA Maintenance fee for application paid

Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 4TH ANNIV.) - STANDARD

Year of fee payment: 4

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-1-1-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20240823

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-1-1-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT DETERMINED COMPLIANT

Effective date: 20240823

Free format text: ST27 STATUS EVENT CODE: A-1-1-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20240823

D11 Substantive examination requested

Free format text: ST27 STATUS EVENT CODE: A-1-1-D10-D11-D117 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: REQUEST FOR EXAMINATION RECEIVED

Effective date: 20240916

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-1-1-P10-P11-P101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT RECEIVED - VOLUNTARY AMENDMENT

Effective date: 20240916

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-1-1-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20241120

D00 Search and/or examination requested or commenced

Free format text: ST27 STATUS EVENT CODE: A-1-1-D10-D00-D118 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: REQUEST FOR EXAMINATION REQUIREMENTS DETERMINED COMPLIANT

Effective date: 20241203

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-1-1-P10-P11-P102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT DETERMINED COMPLIANT

Effective date: 20241203

P13 Application amended

Free format text: ST27 STATUS EVENT CODE: A-1-1-P10-P13-X000 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: APPLICATION AMENDED

Effective date: 20241203

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-1-1-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20241203

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-1-1-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT

Effective date: 20250415

D11 Substantive examination requested

Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D11-D155 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: ALL REQUIREMENTS FOR EXAMINATION DETERMINED COMPLIANT

Effective date: 20250429

D15 Examination report completed

Free format text: ST27 STATUS EVENT CODE: A-2-2-D10-D15-D126 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: EXAMINER'S REPORT

Effective date: 20251015

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT

Effective date: 20260304