CN113490669A - 一类具有降解Btk活性的化合物 - Google Patents
一类具有降解Btk活性的化合物 Download PDFInfo
- Publication number
- CN113490669A CN113490669A CN202080018195.6A CN202080018195A CN113490669A CN 113490669 A CN113490669 A CN 113490669A CN 202080018195 A CN202080018195 A CN 202080018195A CN 113490669 A CN113490669 A CN 113490669A
- Authority
- CN
- China
- Prior art keywords
- compound
- absent
- pharmaceutically acceptable
- integer
- acceptable salt
- 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.)
- Granted
Links
Classifications
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
本发明提供了一类具有降解Btk活性的化合物，具体地，本发明提供了一种如下式I所示的化合物；其中，各基团的定义如说明书中所述。本发明的化合物具有很好的Btk抑制活性并能将Btk降解，可以用于制备治疗Btk活性相关的疾病的药物。
Description
PCT国内申请，说明书已公开。
Claims (14)
- PCT国内申请，权利要求书已公开。
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2019101580204 | 2019-03-02 | ||
| CN201910158020 | 2019-03-02 | ||
| CN201910161658.3A CN111662294A (zh) | 2019-03-05 | 2019-03-05 | 一类具有降解Btk活性的化合物 |
| CN2019101616583 | 2019-03-05 | ||
| PCT/CN2020/077404 WO2020177657A1 (zh) | 2019-03-02 | 2020-03-02 | 一类具有降解Btk活性的化合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN113490669A true CN113490669A (zh) | 2021-10-08 |
| CN113490669B CN113490669B (zh) | 2022-12-30 |
Family
ID=72337613
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202080018195.6A Active CN113490669B (zh) | 2019-03-02 | 2020-03-02 | 一类具有降解Btk活性的化合物 |
Country Status (2)
| Country | Link |
|---|---|
| CN (1) | CN113490669B (zh) |
| WO (1) | WO2020177657A1 (zh) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2023284703A1 (zh) * | 2021-07-15 | 2023-01-19 | 标新生物医药科技(上海)有限公司 | 基于布鲁顿酪氨酸激酶配体设计的蛋白降解化合物及其应用 |
| CN114409658B (zh) * | 2022-04-02 | 2022-06-07 | 水木未来(北京)科技有限公司 | 一种同时调节btk和ikzf3的双功能化合物 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109422752B (zh) * | 2017-09-03 | 2023-04-07 | 上海美志医药科技有限公司 | 一类具有抑制并降解布鲁顿酪氨酸蛋白激酶Btk活性的化合物 |
| WO2019127008A1 (zh) * | 2017-12-26 | 2019-07-04 | 清华大学 | 一种靶向降解btk的化合物及其应用 |
| CA3085457C (en) * | 2018-01-29 | 2023-05-23 | Dana-Farber Cancer Institute, Inc. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
| EP3765026A4 (en) * | 2018-03-10 | 2021-12-22 | Yale University | BTK PROTEOLYSIS MODULATORS AND METHODS FOR USE |
-
2020
- 2020-03-02 CN CN202080018195.6A patent/CN113490669B/zh active Active
- 2020-03-02 WO PCT/CN2020/077404 patent/WO2020177657A1/zh active Application Filing
Non-Patent Citations (3)
| Title |
|---|
| CHRISTOPHER P. TINWORTH ET AL: ""PROTAC-Mediated Degradation of Bruton’s Tyrosine Kinase Is Inhibited by Covalent Binding"", 《AMERICAN CHEMICAL SOCIETY》 * |
| S. KRAJCOVICOVA ET AL: ""Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC)"", 《THE ROYAL SOCIETY OF CHEMISTRY》 * |
| Y. SUN ET AL: ""PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies"", 《CELL RESEARCH》 * |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2020177657A1 (zh) | 2020-09-10 |
| CN113490669B (zh) | 2022-12-30 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN110461846B (zh) | 一类具有抑制并降解布鲁顿酪氨酸蛋白激酶Btk活性的化合物 | |
| CN109963844B (zh) | 一类抑制并降解酪氨酸蛋白激酶alk的化合物 | |
| CN110724174B (zh) | 吡咯并三嗪类化合物、组合物及其应用 | |
| WO2021027911A1 (zh) | 新型螺环类K-Ras G12C抑制剂 | |
| CN111662294A (zh) | 一类具有降解Btk活性的化合物 | |
| CN109516989B (zh) | 一类抑制并降解cdk的化合物 | |
| KR20120083492A (ko) | 신규 5-플루오로우라실 유도체 | |
| CN113490669B (zh) | 一类具有降解Btk活性的化合物 | |
| CN112979656A (zh) | 一类靶向降解btk蛋白的化合物 | |
| US20160340321A1 (en) | Substituted 1,2,3-Triazoles as Antitumor Agents | |
| CN109937203B (zh) | 一类具有抑制并降解酪氨酸蛋白激酶jak1或jak2活性的化合物 | |
| CN109422751B (zh) | 一类具有降解酪氨酸蛋白激酶jak3活性的化合物 | |
| CN115708410B (zh) | 靶向降解Btk的化合物及其抗肿瘤用途 | |
| WO2023030335A1 (zh) | 作为tyk2/jak1假激酶结构域抑制剂的化合物及合成和使用方法 | |
| RU2768451C1 (ru) | Селективный антагонист рецепторов типа A2A | |
| CN114149435A (zh) | 靶向降解Btk的化合物及其应用 | |
| CN114539229A (zh) | 嘧啶二酮类衍生物、其制备方法及其在医药上的应用 | |
| JP2023511222A (ja) | 置換ピリダジノン類化合物とその用途 | |
| CN113214230B (zh) | 2-取代吡唑氨基-4-取代氨基-5-嘧啶甲酰胺类化合物、组合物及其应用 | |
| CN114573459B (zh) | β-榄香烯双胺基取代衍生物及其制备方法和应用 | |
| CN112480100B (zh) | 吡咯烷酮衍生物 | |
| CN116120327A (zh) | β-榄香烯13,14-位对称的双取代衍生物及其制备方法和应用 | |
| CN117384153A (zh) | 一类甲基转移酶抑制剂及其用途 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant |