KR20230003161A - 브루톤의 티로신 키나제(btk) 억제제와 e3 리가제 리간드의 접합에 의한 btk의 분해 및 사용 방법 - Google Patents

브루톤의 티로신 키나제(btk) 억제제와 e3 리가제 리간드의 접합에 의한 btk의 분해 및 사용 방법 Download PDF

Info

Publication number
KR20230003161A
KR20230003161A KR1020227041734A KR20227041734A KR20230003161A KR 20230003161 A KR20230003161 A KR 20230003161A KR 1020227041734 A KR1020227041734 A KR 1020227041734A KR 20227041734 A KR20227041734 A KR 20227041734A KR 20230003161 A KR20230003161 A KR 20230003161A
Authority
KR
South Korea
Prior art keywords
mmol
phenyl
tert
methyl
butyl
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
KR1020227041734A
Other languages
English (en)
Korean (ko)
Inventor
헤샹 왕
바일린 레이
창신 후오
동큉 순
지에 첸
즈위 왕
유쳉 왕
Original Assignee
베이진 엘티디
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 베이진 엘티디 filed Critical 베이진 엘티디
Publication of KR20230003161A publication Critical patent/KR20230003161A/ko
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicinal Preparation (AREA)
KR1020227041734A 2020-04-30 2021-04-29 브루톤의 티로신 키나제(btk) 억제제와 e3 리가제 리간드의 접합에 의한 btk의 분해 및 사용 방법 Pending KR20230003161A (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN2020088322 2020-04-30
CNPCT/CN2020/088322 2020-04-30
CN2021085369 2021-04-02
CNPCT/CN2021/085369 2021-04-02
PCT/CN2021/090898 WO2021219070A1 (en) 2020-04-30 2021-04-29 Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use

Publications (1)

Publication Number Publication Date
KR20230003161A true KR20230003161A (ko) 2023-01-05

Family

ID=78374077

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020227041734A Pending KR20230003161A (ko) 2020-04-30 2021-04-29 브루톤의 티로신 키나제(btk) 억제제와 e3 리가제 리간드의 접합에 의한 btk의 분해 및 사용 방법

Country Status (13)

Country Link
US (1) US20230167118A1 (https=)
EP (1) EP4146655A4 (https=)
JP (2) JP7681038B2 (https=)
KR (1) KR20230003161A (https=)
CN (4) CN116589466B (https=)
AU (1) AU2021264916A1 (https=)
BR (1) BR112022019014A2 (https=)
CA (1) CA3172498A1 (https=)
IL (1) IL297664A (https=)
MX (1) MX2022013407A (https=)
TW (1) TWI902789B (https=)
WO (1) WO2021219070A1 (https=)
ZA (1) ZA202209962B (https=)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116589466B (zh) * 2020-04-30 2025-08-15 百济神州有限公司 通过缀合btk抑制剂与e3连接酶配体降解布鲁顿氏酪氨酸激酶(btk)及其使用方法
CN116981675A (zh) * 2020-12-31 2023-10-31 百济神州有限公司 通过布鲁顿氏酪氨酸激酶（btk）抑制剂与e3连接酶配体的缀合降解btk和使用方法
AU2022270089A1 (en) * 2021-05-03 2023-11-16 Nurix Therapeutics, Inc. Compounds for inhibiting or degrading target proteins, compositions, comprising the same, methods of their making, and methods of their use
TW202309039A (zh) * 2021-05-05 2023-03-01 美商百健Ｍａ公司 用於靶向布魯頓氏酪胺酸激酶降解之化合物
KR20240020735A (ko) 2021-05-07 2024-02-15 카이메라 쎄라퓨틱스 인코포레이티드 Cdk2 분해제 및 그 용도
JP2024525181A (ja) * 2021-06-21 2024-07-10 ベイジーン スウィッツァーランド ゲーエムベーハー （ｒ）－グルタルイミドｃｒｂｎリガンド及び使用方法
KR20240128831A (ko) 2021-12-30 2024-08-27 베이진 스위찰랜드 게엠베하 브루톤 티로신 키나아제(btk) 억제제와 e3 리가아제 리간드의 접합에 의한 btk의 분해 및 사용 방법
WO2023125907A1 (en) * 2021-12-30 2023-07-06 Beigene, Ltd. Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use
JP7805983B2 (ja) 2022-03-22 2026-01-26 アッヴィ・インコーポレイテッド ブルトン型チロシンキナーゼを分解するためのピリミジン
WO2024169871A1 (zh) * 2023-02-17 2024-08-22 江苏威凯尔医药科技有限公司 Btk抑制剂及其用途
CN118946561A (zh) * 2023-03-10 2024-11-12 标新生物医药科技(上海)有限公司 新颖的e3泛素连接酶配体、蛋白降解剂及其应用
CN117126133A (zh) * 2023-08-14 2023-11-28 中国海洋大学 一种化合物及其用途
TW202532078A (zh) * 2024-02-09 2025-08-16 瑞士商百濟神州瑞士有限責任公司 用嵌合降解活化化合物治療b細胞增殖性病症
CN120623148A (zh) * 2024-03-11 2025-09-12 北京深势科技有限公司 一种c-Myc降解剂及其制备方法和用途
WO2025218772A1 (en) * 2024-04-19 2025-10-23 Beigene (Suzhou) Co., Ltd. Solid forms comprising a bruton's tyrosine kinase degrader and uses therefor
WO2025232885A1 (en) * 2024-05-10 2025-11-13 Beigene (Suzhou) Co., Ltd. Preparation method of a bruton's tyrosine kinase degrader thereof
WO2026012424A1 (zh) * 2024-07-10 2026-01-15 江苏恒瑞医药股份有限公司 一种杂芳基类化合物、其制备方法及其在医药上的应用
CN121405700A (zh) * 2024-07-26 2026-01-27 苏州亚盛药业有限公司 Btk降解剂及其用途

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013157021A1 (en) * 2012-04-20 2013-10-24 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
KR20150060839A (ko) * 2012-10-26 2015-06-03 에프. 호프만-라 로슈 아게 브루톤 티로신 키나아제의 억제제
EP3444251B1 (en) * 2013-12-11 2023-06-07 Biogen MA Inc. Biaryl compounds useful for the treatment of human diseases in oncology, neurology and immunology
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
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
CN116589466B (zh) * 2020-04-30 2025-08-15 百济神州有限公司 通过缀合btk抑制剂与e3连接酶配体降解布鲁顿氏酪氨酸激酶(btk)及其使用方法

Also Published As

Publication number Publication date
IL297664A (en) 2022-12-01
CA3172498A1 (en) 2021-11-04
CN115485278A (zh) 2022-12-16
TWI902789B (zh) 2025-11-01
JP2023523130A (ja) 2023-06-02
MX2022013407A (es) 2022-11-14
EP4146655A1 (en) 2023-03-15
BR112022019014A2 (pt) 2022-11-29
EP4146655A4 (en) 2024-07-31
ZA202209962B (en) 2023-05-31
JP7681038B2 (ja) 2025-05-21
JP2025122005A (ja) 2025-08-20
CN121159541A (zh) 2025-12-19
TW202142542A (zh) 2021-11-16
WO2021219070A1 (en) 2021-11-04
CN116589467A (zh) 2023-08-15
CN116589466A (zh) 2023-08-15
AU2021264916A1 (en) 2022-11-03
CN116589466B (zh) 2025-08-15
US20230167118A1 (en) 2023-06-01

Similar Documents

Publication Publication Date Title
JP7681038B2 (ja) Ｂｔｋ阻害因子とｅ３リガーゼリガンドとのコンジュゲーションによるブルトンチロシンキナーゼ（ｂｔｋ）の分解及び使用方法
CN114127067B (zh) 作为hpk1抑制剂的三环化合物及其用途
JP7579816B2 (ja) ＨＰＫ１阻害剤としてのピロロ［２，３－ｂ］ピラジン及びその使用
CN114929689B (zh) Bcl-2抑制剂
CN114341127B (zh) 作为hpk1抑制剂的氨基吡嗪化合物及其用途
JP2022517222A (ja) Ｋｒａｓ ｇ１２ｃ阻害剤
WO2020103896A1 (en) Pyrrolo[2,3-b]pyridines as hpk1 inhibitor and uses thereof
CN114174299A (zh) 通过btk抑制剂与e3连接酶配体缀合对布鲁顿氏酪氨酸激酶(btk)的降解以及使用方法
CN113423708B (zh) 作为tlr7激动剂的咪唑并[2,1-f][1,2,4]三嗪-4-胺衍生物
CN115335376A (zh) 通过缀合btk抑制剂与e3连接酶配体降解布鲁顿氏酪氨酸激酶（btk）及其使用方法
US20240246977A1 (en) Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and method of use
JP2025503463A (ja) ブルトン型チロシンキナーゼ（ｂｔｋ）阻害剤をｅ３リガーゼリガンドにコンジュゲートすることによるｂｔｋの分解及び使用方法
JP2025501082A (ja) ブルトン型チロシンキナーゼ（ｂｔｋ）阻害剤をｅ３リガーゼリガンドにコンジュゲートすることによるｂｔｋの分解及び使用方法
EA050708B1 (ru) Деградация тирозинкиназы брутона (btk) посредством конъюгации ингибиторов btk с лигандом лигазы е3 и способы применения
TW202608884A (zh) 藉由軛合btk抑制劑與e3連接酶配位基降解布魯頓氏酪胺酸激酶（btk）及其使用方法
HK40098887A (zh) 通过缀合btk抑制剂与e3连接酶配体降解布鲁顿氏酪氨酸激酶(btk)及其使用方法
HK40098888B (zh) 通过缀合btk抑制剂与e3连接酶配体降解布鲁顿氏酪氨酸激酶(btk)及其使用方法
HK40098888A (zh) 通过缀合btk抑制剂与e3连接酶配体降解布鲁顿氏酪氨酸激酶(btk)及其使用方法
HK40076737A (en) Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use
EA046667B1 (ru) ПИРРОЛО[2,3-b]ПИРАЗИНЫ В КАЧЕСТВЕ ИНГИБИТОРА HPK1 И ИХ ПРИМЕНЕНИЕ

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

A201 Request for examination
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

D21 Rejection of application intended

Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D21-EXM-PE0902 (AS PROVIDED BY THE NATIONAL OFFICE)

PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

R18 Changes to party contact information recorded

Free format text: ST27 STATUS EVENT CODE: A-3-3-R10-R18-OTH-X000 (AS PROVIDED BY THE NATIONAL OFFICE)

R18-X000 Changes to party contact information recorded

St.27 status event code: A-3-3-R10-R18-oth-X000

PN2301 Change of applicant

St.27 status event code: A-3-3-R10-R11-asn-PN2301

R11 Change to the name of applicant or owner or transfer of ownership requested

Free format text: ST27 STATUS EVENT CODE: A-3-3-R10-R11-ASN-PN2301 (AS PROVIDED BY THE NATIONAL OFFICE)

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-NAP-X000 (AS PROVIDED BY THE NATIONAL OFFICE)

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000