CN109952299B - 用于制备蛋白降解靶向嵌合体的氟代羟脯氨酸衍生物 - Google Patents
用于制备蛋白降解靶向嵌合体的氟代羟脯氨酸衍生物 Download PDFInfo
- Publication number
- CN109952299B CN109952299B CN201780070023.1A CN201780070023A CN109952299B CN 109952299 B CN109952299 B CN 109952299B CN 201780070023 A CN201780070023 A CN 201780070023A CN 109952299 B CN109952299 B CN 109952299B
- Authority
- CN
- China
- Prior art keywords
- group
- compound
- formula
- compounds
- fluoro
- 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.)
- Active
Links
Images
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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further 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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/05—Dipeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61K47/545—Heterocyclic compounds
-
- 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
- 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
- A61K47/555—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 pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
-
- 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
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Molecular Biology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Pain & Pain Management (AREA)
- Virology (AREA)
- Gastroenterology & Hepatology (AREA)
- Ophthalmology & Optometry (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1615617.6 | 2016-09-14 | ||
| GB1615617.6A GB2554071A (en) | 2016-09-14 | 2016-09-14 | Small molecules |
| PCT/GB2017/052726 WO2018051107A1 (en) | 2016-09-14 | 2017-09-14 | Fluorohydroxyproline derivatives useful in the preparation of proteolysis targeted chimeras |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN109952299A CN109952299A (zh) | 2019-06-28 |
| CN109952299B true CN109952299B (zh) | 2023-04-18 |
Family
ID=57234771
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201780070023.1A Active CN109952299B (zh) | 2016-09-14 | 2017-09-14 | 用于制备蛋白降解靶向嵌合体的氟代羟脯氨酸衍生物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US11234988B2 (https=) |
| EP (1) | EP3512844A1 (https=) |
| JP (1) | JP7316932B2 (https=) |
| CN (1) | CN109952299B (https=) |
| GB (1) | GB2554071A (https=) |
| WO (1) | WO2018051107A1 (https=) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3454856B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| CN109790143A (zh) | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| ES2990061T3 (es) | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Degronímeros espirocíclicos para la degradación de proteínas diana |
| CN109641874A (zh) | 2016-05-10 | 2019-04-16 | C4医药公司 | 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体 |
| CN110573507B (zh) | 2017-04-14 | 2023-11-14 | 邓迪大学 | 小分子 |
| CN110769822A (zh) | 2017-06-20 | 2020-02-07 | C4医药公司 | 用于蛋白降解的n/o-连接的降解决定子和降解决定子体 |
| WO2019043208A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROQUINOLINONES |
| WO2019043217A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROBENZIMIDAZOLONES |
| CN118108706A (zh) | 2017-09-04 | 2024-05-31 | C4医药公司 | 戊二酰亚胺 |
| CN111372585A (zh) | 2017-11-16 | 2020-07-03 | C4医药公司 | 用于靶蛋白降解的降解剂和降解决定子 |
| WO2019183523A1 (en) * | 2018-03-23 | 2019-09-26 | Genentech, Inc. | Hetero-bifunctional degrader compounds and their use as modulators of targeted ubiquination (vhl) |
| EP3773576A4 (en) | 2018-03-26 | 2021-12-29 | C4 Therapeutics, Inc. | Cereblon binders for the degradation of ikaros |
| EP3781156A4 (en) | 2018-04-16 | 2022-05-18 | C4 Therapeutics, Inc. | SPIROCYCLIC COMPOUNDS |
| EP3578561A1 (en) | 2018-06-04 | 2019-12-11 | F. Hoffmann-La Roche AG | Spiro compounds |
| US20210283139A1 (en) * | 2018-06-13 | 2021-09-16 | Amphista Therapeutics Ltd | Bifunctional molecules for targeting uchl5 |
| WO2020027225A1 (ja) | 2018-07-31 | 2020-02-06 | ファイメクス株式会社 | 複素環化合物 |
| CN120698983A (zh) | 2018-12-20 | 2025-09-26 | C4医药公司 | 靶向蛋白降解 |
| ES2995214T3 (en) | 2019-03-06 | 2025-02-07 | C4 Therapeutics Inc | Heterocyclic compounds for medical treatment |
| EP3941607A1 (en) | 2019-03-21 | 2022-01-26 | Codiak BioSciences, Inc. | Process for preparing extracellular vesicles |
| US20240108747A1 (en) | 2019-03-21 | 2024-04-04 | Lonza Sales Ag | Extracellular vesicle conjugates and uses thereof |
| WO2020206608A1 (en) * | 2019-04-09 | 2020-10-15 | Ranok Therapeutics (Hangzhou) Co., Ltd. | Methods and compositions for targeted protein degradation |
| CN110885332B (zh) * | 2019-12-06 | 2022-03-18 | 中国人民解放军第二军医大学 | 一种PDEδ蛋白降解靶向嵌合体及其制备方法和应用 |
| US20230099727A1 (en) * | 2020-01-13 | 2023-03-30 | January Therapeutics, Inc. | Nanoparticle compositions |
| WO2021237100A1 (en) | 2020-05-21 | 2021-11-25 | Codiak Biosciences, Inc. | Methods of targeting extracellular vesicles to lung |
| CN113321700B (zh) * | 2020-06-02 | 2022-07-01 | 泰比瑞医药科技(石家庄)有限公司 | 一种降解靶蛋白的双功能化合物及其用途 |
| CN115867554B (zh) | 2020-06-09 | 2025-09-02 | 普莱鲁德疗法有限公司 | Brm靶向化合物和相关使用方法 |
| WO2022066928A2 (en) | 2020-09-23 | 2022-03-31 | Codiak Biosciences, Inc. | Process for preparing extracellular vesicles |
| WO2022099117A1 (en) | 2020-11-06 | 2022-05-12 | Prelude Therapeutics Incorporated | Brm targeting compounds and associated methods of use |
| KR20230106637A (ko) * | 2020-11-11 | 2023-07-13 | 제넨테크, 인크. | 빈혈 및 암 치료용 vhl 억제제로서의 1-(2-(4-시클로프로필-1h-1,2,3-트리아졸-1-일)아세틸)-4-히드록시-n-(벤질)피롤리딘 e-2-카르복사미드 유도체 |
| CN115154419B (zh) * | 2021-04-02 | 2023-11-28 | 中国科学院上海药物研究所 | 一种纳米胶束前体和纳米胶束,其制备方法及应用 |
| CN113651835A (zh) * | 2021-06-04 | 2021-11-16 | 上海大学 | 一种bethdac双靶向protac的制备方法和应用 |
| US20240336612A1 (en) | 2021-07-13 | 2024-10-10 | Prelude Therapeutics Incorporated | BRM Targeting Compounds And Associated Methods Of Use |
| CN115109047B (zh) * | 2021-09-08 | 2024-02-20 | 中国科学院化学研究所 | 一种基于protac设计的铁死亡诱导剂 |
| CN114288422B (zh) * | 2022-01-21 | 2023-04-28 | 陕西科技大学 | 一种化学靶向降解目标蛋白的脂质体及其制备方法 |
| CN114907386B (zh) * | 2022-03-11 | 2023-03-31 | 山东大学 | 一种hemtac小分子降解剂及其应用 |
| CN114560908B (zh) * | 2022-03-11 | 2024-10-25 | 国家纳米科学中心 | 一种多肽protac分子及其制备方法和应用 |
| CN119836416A (zh) | 2022-06-16 | 2025-04-15 | 普莱鲁德疗法有限公司 | 具有泛素连接酶结合部分的靶向kat6的化合物 |
| CN115057909A (zh) * | 2022-07-13 | 2022-09-16 | 浙江工业大学 | 一种基于化合物pacma31的蛋白降解靶向嵌合体及其制备方法与应用 |
| WO2024027792A1 (en) * | 2022-08-05 | 2024-02-08 | Shenzhen Newdel Biotech Co., Ltd. | Protein kinase degrading agent, medicament and use |
| CN115028681B (zh) * | 2022-08-11 | 2022-11-15 | 中国科学院微生物研究所 | 一种降解亲环素a的嵌合体化合物及其制备方法与应用 |
| JP2025538228A (ja) | 2022-11-15 | 2025-11-26 | プレリュード・セラピューティクス・インコーポレイテッド | Brm標的化化合物及び関連する使用方法 |
| WO2024240078A1 (en) * | 2023-05-19 | 2024-11-28 | The Chinese University Of Hong Kong | Compositions and methods related to protein labeling |
| WO2025049555A1 (en) | 2023-08-31 | 2025-03-06 | Oerth Bio Llc | Compositions and methods for targeted inhibition and degradation of proteins in an insect cell |
| CN116855471B (zh) * | 2023-09-04 | 2023-11-28 | 江苏申基生物科技有限公司 | 一种嘌呤核苷磷酸化酶突变体及其应用 |
| TW202530189A (zh) | 2023-09-29 | 2025-08-01 | 日商第一三共股份有限公司 | 3-苯基丙基胺衍生物 |
| WO2025101942A1 (en) | 2023-11-10 | 2025-05-15 | Prelude Therapeutics Incorporated | Kat6 targeting compounds |
| CN117756883B (zh) * | 2023-12-18 | 2024-10-11 | 江苏海洋大学 | 一种靶向乙酰胆碱酯酶的化合物及其制备方法和应用 |
| US20250276074A1 (en) | 2024-03-01 | 2025-09-04 | Prelude Therapeutics Incorporated | Brm and brg1 targeting antibody-drug conjugates and methods of use thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103402996A (zh) * | 2011-01-04 | 2013-11-20 | 诺瓦提斯公司 | 可用于治疗年龄相关性黄斑变性(amd)的吲哚化合物或其类似物 |
| CN104583193A (zh) * | 2012-06-28 | 2015-04-29 | 诺华股份有限公司 | 吡咯烷衍生物及其作为补体途径调节剂的用途 |
| CN104736569A (zh) * | 2012-01-12 | 2015-06-24 | 耶鲁大学 | 通过e3泛素连接酶增强靶蛋白质及其他多肽降解的化合物和方法 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009014730A1 (en) * | 2007-07-26 | 2009-01-29 | Idenix Pharmaceuticals, Inc. | Macrocyclic serine protease inhibitors |
| WO2013106646A2 (en) * | 2012-01-12 | 2013-07-18 | Yale University | Compounds and methods for the inhibition of vcb e3 ubiquitin ligase |
| GB201311891D0 (en) * | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| GB201311888D0 (en) * | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| RU2738833C9 (ru) * | 2014-04-14 | 2022-02-28 | Арвинас, Оперэйшнз, Инк. | Имидные модуляторы протеолиза и способы их применения |
| US10071164B2 (en) * | 2014-08-11 | 2018-09-11 | Yale University | Estrogen-related receptor alpha based protac compounds and associated methods of use |
| JP6817962B2 (ja) * | 2015-01-20 | 2021-01-20 | アルビナス・オペレーションズ・インコーポレイテッドArvinas Operations, Inc. | ターゲティングされたアンドロゲン受容体分解のための化合物および方法 |
| GB201504314D0 (en) * | 2015-03-13 | 2015-04-29 | Univ Dundee | Small molecules |
| EP3270917A4 (en) | 2015-03-18 | 2018-08-08 | Arvinas, Inc. | Compounds and methods for the enhanced degradation of targeted proteins |
-
2016
- 2016-09-14 GB GB1615617.6A patent/GB2554071A/en not_active Withdrawn
-
2017
- 2017-09-14 US US16/333,454 patent/US11234988B2/en not_active Expired - Fee Related
- 2017-09-14 WO PCT/GB2017/052726 patent/WO2018051107A1/en not_active Ceased
- 2017-09-14 EP EP17771547.1A patent/EP3512844A1/en not_active Withdrawn
- 2017-09-14 CN CN201780070023.1A patent/CN109952299B/zh active Active
- 2017-09-14 JP JP2019514814A patent/JP7316932B2/ja active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103402996A (zh) * | 2011-01-04 | 2013-11-20 | 诺瓦提斯公司 | 可用于治疗年龄相关性黄斑变性(amd)的吲哚化合物或其类似物 |
| CN104736569A (zh) * | 2012-01-12 | 2015-06-24 | 耶鲁大学 | 通过e3泛素连接酶增强靶蛋白质及其他多肽降解的化合物和方法 |
| CN104583193A (zh) * | 2012-06-28 | 2015-04-29 | 诺华股份有限公司 | 吡咯烷衍生物及其作为补体途径调节剂的用途 |
Non-Patent Citations (3)
| Title |
|---|
| "Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4";Michael Zengerle et al.;《ACS Chem. Biol》;20150602;第10卷;第1770-1777页 * |
| 3-Fluoroazetidinecarboxylic Acids and trans,trans-3,4-Difluoroproline as Peptide Scaffolds: Inhibition of Pancreatic;Zilei Liu et al.;《J. Org. Chem.》;20150410;第80卷;第4244-4258页 * |
| PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer;Kanak Raina et al.;《PNAS》;20160606;第113卷;第7124-7129页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| GB2554071A (en) | 2018-03-28 |
| JP2019531290A (ja) | 2019-10-31 |
| EP3512844A1 (en) | 2019-07-24 |
| JP7316932B2 (ja) | 2023-07-28 |
| US20190255066A1 (en) | 2019-08-22 |
| WO2018051107A1 (en) | 2018-03-22 |
| CN109952299A (zh) | 2019-06-28 |
| US11234988B2 (en) | 2022-02-01 |
| GB201615617D0 (en) | 2016-10-26 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN109952299B (zh) | 用于制备蛋白降解靶向嵌合体的氟代羟脯氨酸衍生物 | |
| ES2866152T3 (es) | Derivados de tirosina amida como inhibidores de la Rho-quinasa | |
| EP3268363B1 (en) | Derivatives of 1-[(cyclopentyl or 2-pyrrolidinyl)carbonylaminomethyl]-4-(1,3-thiazol-5-yl) benzene which are useful for the treatment of proliferative, autoimmune or inflammatory diseases | |
| ES2648228T3 (es) | Derivados de imidazo[1,2-b]piridazina como inhibidores de cinasa | |
| AU2012204920B2 (en) | Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (AMD) | |
| AU2017348826B2 (en) | Amino pyrazolopyrimidine compound used as neurotrophic factor tyrosine kinase receptor inhibitor | |
| IL294048A (en) | sos1 inhibitors | |
| ES2761903T3 (es) | Derivados de carbazol | |
| EP3710431A1 (en) | Substituted pyrrolopyrimidine jak inhibitors and methods of making and using the same | |
| ES2956090T3 (es) | Inhibidores de bencimidazol de enzimas PAD | |
| CA3005741A1 (en) | Compounds and compositions useful for treating disorders related to ntrk | |
| JP2024089673A (ja) | ピラゾリル-アミノ-ピリミジニル誘導体のベンズアミド、およびその組成物ならびに方法 | |
| CN115867346B (zh) | 激酶抑制剂 | |
| AU2022284939A1 (en) | Pyridazinone compound as parp7 inhibitor | |
| AU2017239295B2 (en) | Compound having mutant IDH inhibitory activity, preparation method and use thereof | |
| CN116635398A (zh) | 改进的小分子 | |
| AU2020328707A1 (en) | Bridged heterocyclyl-substituted pyrimidine compound, preparation method therefor, and pharmaceutical use thereof | |
| JP7764479B2 (ja) | H4アンタゴニスト化合物 | |
| AU2014259534B2 (en) | Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (AMD) | |
| WO2026075941A1 (en) | Pyridazinone derivatives as pad4 inhibitors | |
| WO2026021342A1 (zh) | 一种杂环类化合物及其在医药上的应用 | |
| EA048017B1 (ru) | Бензамиды производных пиразолил-амино-пиримидинила, композиции на их основе и способы применения | |
| HK1226736A1 (en) | 2,6-substituted purine derivatives and their use in the treatment of proliferative disorders |
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 |