CO2019009424A2 - Ligandos de cereblon y compuestos bifuncionales que comprenden el mismo - Google Patents
Ligandos de cereblon y compuestos bifuncionales que comprenden el mismoInfo
- Publication number
- CO2019009424A2 CO2019009424A2 CONC2019/0009424A CO2019009424A CO2019009424A2 CO 2019009424 A2 CO2019009424 A2 CO 2019009424A2 CO 2019009424 A CO2019009424 A CO 2019009424A CO 2019009424 A2 CO2019009424 A2 CO 2019009424A2
- Authority
- CO
- Colombia
- Prior art keywords
- compounds
- cereblon
- bifunctional compounds
- same
- binds
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 6
- 102100032783 Protein cereblon Human genes 0.000 title abstract 3
- 230000001588 bifunctional effect Effects 0.000 title abstract 3
- 239000003446 ligand Substances 0.000 title abstract 2
- 101000941994 Homo sapiens Protein cereblon Proteins 0.000 title 1
- 102000004169 proteins and genes Human genes 0.000 abstract 4
- 108090000623 proteins and genes Proteins 0.000 abstract 4
- 230000015556 catabolic process Effects 0.000 abstract 2
- 238000006731 degradation reaction Methods 0.000 abstract 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- 229920001184 polypeptide Polymers 0.000 abstract 2
- 102000004196 processed proteins & peptides Human genes 0.000 abstract 2
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 2
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 abstract 1
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 230000034512 ubiquitination Effects 0.000 abstract 1
- 238000010798 ubiquitination Methods 0.000 abstract 1
Classifications
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- 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, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
-
- 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
-
- 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
- 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
-
- 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
- C07D471/10—Spiro-condensed systems
-
- 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
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Pyridine Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762452972P | 2017-01-31 | 2017-01-31 | |
| PCT/US2018/016315 WO2018144649A1 (en) | 2017-01-31 | 2018-01-31 | Cereblon ligands and bifunctional compounds comprising the same |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO2019009424A2 true CO2019009424A2 (es) | 2020-02-28 |
Family
ID=62977181
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CONC2019/0009424A CO2019009424A2 (es) | 2017-01-31 | 2019-10-28 | Ligandos de cereblon y compuestos bifuncionales que comprenden el mismo |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US20180215731A1 (enExample) |
| EP (1) | EP3577109A4 (enExample) |
| JP (2) | JP2020506922A (enExample) |
| KR (1) | KR102747905B1 (enExample) |
| CN (2) | CN110612294B (enExample) |
| AU (3) | AU2018215212B2 (enExample) |
| BR (1) | BR112019015484A2 (enExample) |
| CA (1) | CA3050309A1 (enExample) |
| CO (1) | CO2019009424A2 (enExample) |
| IL (3) | IL312367A (enExample) |
| MX (2) | MX2019009046A (enExample) |
| WO (1) | WO2018144649A1 (enExample) |
Families Citing this family (257)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| EP3302482A4 (en) | 2015-06-05 | 2018-12-19 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| EP3337476A4 (en) | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| EP3455218A4 (en) | 2016-05-10 | 2019-12-18 | C4 Therapeutics, Inc. | C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
| WO2017197036A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| WO2017197051A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Amine-linked c3-glutarimide degronimers for target protein degradation |
| EP3454856B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| WO2018053354A1 (en) | 2016-09-15 | 2018-03-22 | Arvinas, Inc. | Indole derivatives as estrogen receptor degraders |
| MX2019004950A (es) | 2016-10-28 | 2019-09-26 | Icahn School Med Mount Sinai | Composiciones y metodos para tratar el cancer mediado por el potenciador del homologo zeste 2. |
| CA3042260C (en) * | 2016-11-01 | 2023-10-03 | Arvinas, Inc. | Tau-protein targeting protacs and associated methods of use |
| RS64976B1 (sr) | 2016-12-01 | 2024-01-31 | Arvinas Operations Inc | Derivati tetrahidronaftalena i tetrahidroizohinolina kao degradatori estrogenih receptora |
| CN110741004B (zh) | 2016-12-23 | 2023-10-17 | 阿尔维纳斯运营股份有限公司 | 用于迅速加速性纤维肉瘤多肽的靶向降解的化合物和方法 |
| JP2020505327A (ja) | 2016-12-23 | 2020-02-20 | 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. | Egfrタンパク質分解標的化キメラ分子およびその関連する使用方法 |
| WO2018118598A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| US11191741B2 (en) | 2016-12-24 | 2021-12-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
| AU2018211975B2 (en) | 2017-01-26 | 2022-05-26 | Arvinas Operations, Inc. | Modulators of estrogen receptor proteolysis and associated methods of use |
| KR102747905B1 (ko) | 2017-01-31 | 2024-12-31 | 아비나스 오퍼레이션스, 인코포레이티드 | 세레블론 리간드 및 이를 포함하는 이작용성 화합물 |
| KR102014478B1 (ko) * | 2017-05-12 | 2019-08-26 | 한국화학연구원 | 신규한 피페리딘-2,6-디온 유도체 및 이의 용도 |
| 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 |
| HRP20241553T1 (hr) | 2017-07-10 | 2025-01-17 | Celgene Corporation | 4-(4-(4-(((2-(2,6-dioksopiperidin-3-il)-l-oksoizoindolin-4-il)oksi)metil)benzil)piperazin-l-il)-3-fluorobenzonitril kao antiproliferativni spoj |
| WO2019043214A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | glutarimide |
| WO2019043208A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROQUINOLINONES |
| EP3679027A1 (en) | 2017-09-04 | 2020-07-15 | C4 Therapeutics, Inc. | Dihydrobenzimidazolones |
| US11358948B2 (en) | 2017-09-22 | 2022-06-14 | Kymera Therapeutics, Inc. | CRBN ligands and uses thereof |
| IL322809A (en) | 2017-09-22 | 2025-10-01 | Kymera Therapeutics Inc | Protein Decomposers and Their Uses |
| WO2019099868A2 (en) | 2017-11-16 | 2019-05-23 | C4 Therapeutics, Inc. | Degraders and degrons for targeted protein degradation |
| US11065231B2 (en) | 2017-11-17 | 2021-07-20 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides |
| IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| US11512080B2 (en) | 2018-01-12 | 2022-11-29 | Kymera Therapeutics, Inc. | CRBN ligands and uses thereof |
| WO2019140380A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| EP3743066A4 (en) | 2018-01-26 | 2021-09-08 | Yale University | IMIDE-BASED PROTEOLYSIS MODULATORS AND RELATED METHODS OF USE |
| US11028088B2 (en) | 2018-03-10 | 2021-06-08 | Yale University | Modulators of BTK proteolysis and methods of use |
| WO2019191112A1 (en) | 2018-03-26 | 2019-10-03 | C4 Therapeutics, Inc. | Cereblon binders for the degradation of ikaros |
| WO2019186343A1 (en) | 2018-03-26 | 2019-10-03 | Novartis Ag | N-(3-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl)benzamide derivatives |
| EP3774789B1 (en) | 2018-04-01 | 2025-03-05 | Arvinas Operations, Inc. | Brm targeting compounds and associated methods of use |
| BR112020020307A2 (pt) | 2018-04-04 | 2021-01-12 | Arvinas Operations, Inc. | Moduladores de proteólise e métodos de uso associados |
| WO2019199816A1 (en) * | 2018-04-13 | 2019-10-17 | Arvinas Operations, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| EP3781156A4 (en) | 2018-04-16 | 2022-05-18 | C4 Therapeutics, Inc. | SPIROCYCLIC COMPOUNDS |
| CA3096404A1 (en) | 2018-04-23 | 2019-10-31 | Celgene Corporation | Substituted 4-aminoisoindoline-1,3-dione compounds and their use for treating lymphoma |
| EA202092436A1 (ru) | 2018-05-14 | 2021-05-04 | Нувейшн Био Инк. | Противораковые соединения, нацеливающие на ядерные гормональные рецепторы |
| EP3578561A1 (en) | 2018-06-04 | 2019-12-11 | F. Hoffmann-La Roche AG | Spiro compounds |
| WO2020006265A1 (en) * | 2018-06-29 | 2020-01-02 | Dana-Farber Cancer Institute, Inc. | Bispecific degraders |
| AU2019293235B2 (en) | 2018-06-29 | 2025-07-03 | Dana-Farber Cancer Institute, Inc. | Immunomodulatory compounds |
| US11292792B2 (en) | 2018-07-06 | 2022-04-05 | Kymera Therapeutics, Inc. | Tricyclic CRBN ligands and uses thereof |
| EP3817822A4 (en) | 2018-07-06 | 2022-07-27 | Kymera Therapeutics, Inc. | PROTEIN DEGRADANTS AND USES THEREOF |
| AR116109A1 (es) | 2018-07-10 | 2021-03-31 | Novartis Ag | Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos |
| EP3820573B1 (en) | 2018-07-10 | 2023-08-09 | Novartis AG | 3-(5-hydroxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and their use in the treatment of ikaros family zinc finger 2 (ikzf2)-dependent diseases |
| US20200038513A1 (en) | 2018-07-26 | 2020-02-06 | Arvinas Operations, Inc. | Modulators of fak proteolysis and associated methods of use |
| EP3831811A4 (en) | 2018-07-31 | 2022-04-20 | Fimecs, Inc. | HETEROCYCLIC COMPOUND |
| CN108774215A (zh) * | 2018-08-15 | 2018-11-09 | 翟学旭 | 含氮杂环类衍生物及其在视网膜新生血管疾病中的应用 |
| US11707452B2 (en) | 2018-08-20 | 2023-07-25 | Arvinas Operations, Inc. | Modulators of alpha-synuclein proteolysis and associated methods of use |
| US11969472B2 (en) | 2018-08-22 | 2024-04-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| EP3841098A4 (en) | 2018-08-22 | 2022-05-04 | Cullgen (Shanghai), Inc. | TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHOD OF USE |
| EP3846800A4 (en) | 2018-09-04 | 2022-08-24 | C4 Therapeutics, Inc. | Compounds for the degradation of brd9 or mth1 |
| CN112654619B (zh) * | 2018-09-07 | 2022-08-30 | 南京明德新药研发有限公司 | 三环并呋喃取代哌啶二酮类化合物 |
| CA3119773A1 (en) | 2018-11-30 | 2020-06-04 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| WO2020117759A1 (en) * | 2018-12-03 | 2020-06-11 | Dana-Farber Cancer Institute, Inc. | Small molecule degraders of helios and methods of use |
| KR102864064B1 (ko) | 2018-12-19 | 2025-09-24 | 셀진 코포레이션 | 치환된 3-((3-아미노페닐)아미노)피페리딘-2,6-디온 화합물, 이의 조성물, 및 이를 사용한 치료 방법 |
| DK3897636T3 (da) | 2018-12-19 | 2025-01-13 | Celgene Corp | Substituerede 3-((3-aminophenyl)amino)piperidin-2,6-dionforbindelser, sammensætninger heraf og fremgangsmåde til behandling hermed |
| WO2020132561A1 (en) * | 2018-12-20 | 2020-06-25 | C4 Therapeutics, Inc. | Targeted protein degradation |
| EP3917916A4 (en) * | 2019-01-30 | 2022-12-14 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| WO2020162725A1 (ko) * | 2019-02-07 | 2020-08-13 | 한국화학연구원 | 표적 단백질 eed 분해 유도 데그라듀서, 이의 제조방법 및 이를 유효성분으로 함유하는 eed, ezh2, 또는 prc2 관련 질환의 예방 또는 치료용 약학적 조성물 |
| EP3924055B1 (en) | 2019-02-15 | 2024-04-03 | Novartis AG | Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| US20220143183A1 (en) * | 2019-02-23 | 2022-05-12 | New York University | Photoswitchable protacs and synthesis and uses thereof |
| CN113939300A (zh) | 2019-04-05 | 2022-01-14 | 凯麦拉医疗公司 | Stat降解剂和其用途 |
| WO2020206608A1 (en) * | 2019-04-09 | 2020-10-15 | Ranok Therapeutics (Hangzhou) Co., Ltd. | Methods and compositions for targeted protein degradation |
| WO2020214555A1 (en) | 2019-04-16 | 2020-10-22 | Northwestern University | Bifunctional compounds comprising apcin-a and their use in the treatment of cancer |
| CN119504751B (zh) * | 2019-04-18 | 2025-11-14 | 海创药业股份有限公司 | 一类靶向降解雄激素受体的双功能嵌合体杂环化合物及其用途 |
| CN118908962A (zh) | 2019-05-06 | 2024-11-08 | 西奈山伊坎医学院 | 作为hpk1的降解剂的异双功能化合物 |
| CA3138197A1 (en) | 2019-05-14 | 2020-11-19 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| US20230087825A1 (en) * | 2019-06-10 | 2023-03-23 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
| WO2020252397A1 (en) * | 2019-06-12 | 2020-12-17 | Baylor College Of Medicine | Small molecule proteolysis-targeting chimeras and methods of use thereof |
| NZ783169A (en) | 2019-06-25 | 2024-12-20 | Gilead Sciences Inc | Flt3l-fc fusion proteins and methods of use |
| CN114867727B (zh) * | 2019-07-17 | 2025-02-21 | 阿尔维纳斯运营股份有限公司 | Tau蛋白靶向化合物及相关使用方法 |
| CN114667147B (zh) * | 2019-08-26 | 2024-09-06 | 阿尔维纳斯运营股份有限公司 | 用四氢萘衍生物作为雌激素受体降解剂的治疗乳腺癌的方法 |
| WO2021041664A1 (en) * | 2019-08-27 | 2021-03-04 | The Regents Of The University Of Michigan | Cereblon e3 ligase inhibitors |
| US11905276B2 (en) * | 2019-09-12 | 2024-02-20 | Medshine Discovery Inc. | Bicyclic compound that acts as CRBN protein regulator |
| CN114401960A (zh) * | 2019-09-16 | 2022-04-26 | 诺华股份有限公司 | 胶降解剂及其使用方法 |
| PE20221417A1 (es) * | 2019-09-16 | 2022-09-20 | Novartis Ag | Degradadores bifuncionales de brd9 y sus metodos de uso |
| JP7502425B2 (ja) | 2019-10-01 | 2024-06-18 | アルヴィナス・オペレーションズ・インコーポレイテッド | Brm標的化化合物および関連使用方法 |
| EP4045496A1 (en) | 2019-10-17 | 2022-08-24 | Arvinas Operations, Inc. | Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety |
| US11952349B2 (en) | 2019-11-13 | 2024-04-09 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| 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 |
| GB201918414D0 (en) | 2019-12-13 | 2020-01-29 | Z Factor Ltd | Compounds and their use for the treatment of Alpha1-Antitrypsin deficiency |
| JP2023507172A (ja) * | 2019-12-17 | 2023-02-21 | オリオニス バイオサイエンシズ,インコーポレイテッド | タンパク質分解の調節 |
| US11591332B2 (en) | 2019-12-17 | 2023-02-28 | Kymera Therapeutics, Inc. | IRAK degraders and uses thereof |
| JP2023509366A (ja) | 2019-12-17 | 2023-03-08 | カイメラ セラピューティクス, インコーポレイテッド | Irak分解剤およびそれらの使用 |
| PH12022551486A1 (en) | 2019-12-19 | 2023-11-13 | Arvinas Operations Inc | Compounds and methods for the targeted degradation of androgen receptor |
| MX2022007659A (es) | 2019-12-20 | 2022-07-19 | C4 Therapeutics Inc | Compuestos de isoindolinona e indazol para la degradacion del receptor del factor de crecimiento epidermico (egfr). |
| US11679109B2 (en) | 2019-12-23 | 2023-06-20 | Kymera Therapeutics, Inc. | SMARCA degraders and uses thereof |
| CN113087704B (zh) | 2019-12-23 | 2023-09-08 | 上海济煜医药科技有限公司 | 一种蛋白降解剂化合物的制备方法和应用 |
| CA3164578A1 (en) * | 2020-01-14 | 2021-07-22 | Scott KANNER | Compositions and methods for targeted protein stabilization by redirecting endogenous deubiquitinases |
| TW202140475A (zh) * | 2020-01-16 | 2021-11-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 稠合醯亞胺類衍生物、其製備方法及其在醫藥上的應用 |
| WO2021143822A1 (zh) * | 2020-01-16 | 2021-07-22 | 江苏恒瑞医药股份有限公司 | 并环酰亚胺类衍生物、其制备方法及其在医药上的应用 |
| US11618751B1 (en) | 2022-03-25 | 2023-04-04 | Ventus Therapeutics U.S., Inc. | Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 derivatives |
| TWI832035B (zh) | 2020-02-14 | 2024-02-11 | 美商基利科學股份有限公司 | 結合ccr8之抗體及融合蛋白及其用途 |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| CN115697989B (zh) | 2020-02-26 | 2025-03-18 | 上海睿跃生物科技有限公司 | 原肌球蛋白受体激酶(trk)降解化合物和使用方法 |
| EP3875456A1 (en) * | 2020-03-02 | 2021-09-08 | Technische Universität Darmstadt | Hetero-bifunctional proteolysis-targeting chimeras (protacs) for the selective degradation of fk506-binding proteins (fkbps) |
| CN111249276B (zh) * | 2020-03-05 | 2021-07-13 | 南京巴傲得生物科技有限公司 | 吲哚布洛芬制备cbp溴区抑制试剂的用途 |
| CN115279370B (zh) | 2020-03-05 | 2025-01-10 | C4医药公司 | 用于brd9的靶向降解的化合物 |
| US20230123104A1 (en) * | 2020-03-06 | 2023-04-20 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Crystal of tricyclic compound acting on crbn protein and preparation method therefor |
| CN113387931A (zh) * | 2020-03-13 | 2021-09-14 | 四川海思科制药有限公司 | 一种具有抑制或降解蛋白激酶的化合物及其制备方法和药学上的应用 |
| CN115380026B (zh) * | 2020-03-17 | 2023-11-07 | 南京明德新药研发有限公司 | 蛋白降解调节剂与其使用方法 |
| JP2023518202A (ja) * | 2020-03-18 | 2023-04-28 | ダナ-ファーバー キャンサー インスティテュート,インコーポレイテッド | Petトレーサーpbb3に基づく異常タウの標的化ディグレーダー |
| PH12022552458A1 (en) | 2020-03-19 | 2024-01-22 | Kymera Therapeutics Inc | Mdm2 degraders and uses thereof |
| KR20210122163A (ko) * | 2020-03-27 | 2021-10-08 | (주) 업테라 | Plk1의 선택적 분해를 유도하는 피라졸로퀴나졸린 유도체 화합물 |
| WO2021210878A1 (ko) * | 2020-04-17 | 2021-10-21 | 광주과학기술원 | Crbn 결합 펩티드 및 이를 이용한 알츠하이머 병 예방 또는 치료용 조성물 |
| WO2021219077A1 (zh) * | 2020-04-29 | 2021-11-04 | 泰比棣医药科技(石家庄)有限公司 | 一种组织靶向的蛋白靶向降解化合物及其用途 |
| CN113582974B (zh) * | 2020-04-30 | 2022-05-17 | 江西济民可信集团有限公司 | 一类作为蛋白降解剂的化合物及其制备方法和医药用途 |
| US20230357249A1 (en) * | 2020-05-14 | 2023-11-09 | The Regents Of The University Of Michigan | Androgen receptor protein degraders with a tricyclic cereblon ligand |
| WO2021236885A1 (en) * | 2020-05-21 | 2021-11-25 | Dana-Farber Cancer Institute, Inc. | Piperidine-2,6-diones as small molecule degraders of helios and methods of use |
| TW202210483A (zh) | 2020-06-03 | 2022-03-16 | 美商凱麥拉醫療公司 | Irak降解劑之結晶型 |
| CR20230007A (es) | 2020-06-12 | 2023-06-01 | Shanghai Jemincare Pharmaceuticals Co Ltd | Compuesto de ftalazinona, y método de preparación y uso médico de este. |
| WO2021262591A1 (en) * | 2020-06-22 | 2021-12-30 | Dana-Farber Cancer Institute, Inc. | Protein tag to induce ligand dependent degradation of protein/protein-fusions |
| KR102559329B1 (ko) * | 2020-07-02 | 2023-07-25 | 포항공과대학교 산학협력단 | 신규한 프로탁 키메라 화합물, 이를 포함하는 표적 단백질 분해를 통한 질환의 예방, 개선 또는 치료용 약학적 조성물 |
| WO2022007903A1 (zh) * | 2020-07-09 | 2022-01-13 | 四川海思科制药有限公司 | 一种能够抑制并降解雄激素受体的化合物及其药物组合物和药学上的应用 |
| KR102646850B1 (ko) * | 2020-07-21 | 2024-03-13 | 주식회사 유빅스테라퓨틱스 | 안드로겐 수용체 분해용 화합물 및 이들의 의약 용도 |
| KR20220014952A (ko) * | 2020-07-29 | 2022-02-08 | 한국화학연구원 | 안드로겐 수용체의 저해 또는 분해용 화합물 및 이들의 의약 용도 |
| AU2021319847A1 (en) * | 2020-08-03 | 2023-03-02 | Captor Therapeutics S.A. | Low molecular weight protein degraders and their applications |
| KR20230050375A (ko) * | 2020-08-05 | 2023-04-14 | 상하이 리딩택 파마슈티컬 코., 엘티디. | 단백질 표적화 및 분해용 화합물, 이의 제조방법 및 용도 |
| WO2022032026A1 (en) | 2020-08-05 | 2022-02-10 | C4 Therapeutics, Inc. | Compounds for targeted degradation of ret |
| US12180193B2 (en) | 2020-08-28 | 2024-12-31 | Arvinas Operations, Inc. | Accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| CN114133379B (zh) * | 2020-09-04 | 2024-02-13 | 南京奥瑞药业有限公司 | 一种杂环化合物、其制备方法、中间体、组合物以及应用 |
| CN114163444B (zh) * | 2020-09-11 | 2023-07-14 | 江苏恒瑞医药股份有限公司 | 一种用于雄激素受体蛋白靶向降解的嵌合体化合物、其制备方法及其在医药上的应用 |
| CR20230162A (es) | 2020-09-14 | 2023-06-02 | Arvinas Operations Inc | Formas cristalinas y amorfas de un compuesto para la degradación dirigida del receptor de estrógenos |
| CN114181277A (zh) * | 2020-09-15 | 2022-03-15 | 江苏恒瑞医药股份有限公司 | 一种用于雄激素受体蛋白靶向降解的嵌合体化合物、其制备方法及其在医药上的应用 |
| EP4217352A4 (en) | 2020-09-23 | 2024-04-10 | St. Jude Children's Research Hospital, Inc. | Substituted n-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)arylsulfonamide analogs as modulators of cereblon protein |
| IL301626A (en) * | 2020-09-30 | 2023-05-01 | Astrazeneca Ab | Compounds and their use in treating cancer |
| JP2023545509A (ja) * | 2020-10-14 | 2023-10-30 | シーフォー セラピューティクス, インコーポレイテッド | 医学的療法のための、ネオ基質を分解する三環式化合物 |
| WO2022087125A1 (en) | 2020-10-21 | 2022-04-28 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor protein |
| CN114621231B (zh) * | 2020-12-14 | 2025-09-12 | 杭州中美华东制药有限公司 | 一种靶向降解/抑制活性的嵌合化合物及其制备方法和用途 |
| MX2023007852A (es) | 2020-12-30 | 2023-07-07 | Kymera Therapeutics Inc | Degradadores de cinasas asociadas al receptor de interleucina-1 (irak) y usos de los mismos. |
| EP4277901A1 (en) | 2021-01-13 | 2023-11-22 | Monte Rosa Therapeutics, Inc. | Isoindolinone compounds |
| CN116867778A (zh) * | 2021-02-04 | 2023-10-10 | 正大天晴药业集团股份有限公司 | 苯并七元环类双功能化合物及其应用 |
| EP4291187A4 (en) | 2021-02-15 | 2025-01-15 | Kymera Therapeutics, Inc. | Irak4 degraders and uses thereof |
| AU2022220869A1 (en) | 2021-02-15 | 2023-08-24 | Kymera Therapeutics, Inc. | Irak4 degraders and uses thereof |
| WO2022178532A1 (en) * | 2021-02-19 | 2022-08-25 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
| US20250276964A1 (en) * | 2021-03-15 | 2025-09-04 | Novartis Ag | Benzisoxazole Derivatives and Uses thereof |
| IL306010A (en) | 2021-03-23 | 2023-11-01 | Nuvation Bio Inc | Anticancer compounds against the nuclear hormone receptor |
| US20250099596A1 (en) * | 2021-03-29 | 2025-03-27 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Tetrahydronaphthalene compound, and preparation method therefor and use thereof in medicine |
| CN115141179B (zh) * | 2021-03-31 | 2024-09-13 | 江苏恒瑞医药股份有限公司 | 一种新型苯并杂环基类衍生物、其制备方法及其在医药上的应用 |
| JP7768592B2 (ja) * | 2021-03-31 | 2025-11-12 | デューク ストリート バイオ リミテッド | 医薬化合物 |
| US11319319B1 (en) | 2021-04-07 | 2022-05-03 | Ventus Therapeutics U.S., Inc. | Compounds for inhibiting NLRP3 and uses thereof |
| AU2022259683A1 (en) | 2021-04-16 | 2023-10-19 | Arvinas Operations, Inc. | Modulators of bcl6 proteolysis and associated methods of use |
| CN113603676B (zh) * | 2021-04-28 | 2022-05-24 | 浙江工业大学 | 基于厄洛替尼靶向降解egfr蛋白小分子化合物及其制备方法和应用 |
| JP2024516024A (ja) * | 2021-05-03 | 2024-04-11 | ニューベイション・バイオ・インコーポレイテッド | 抗がん核内ホルモン受容体標的化化合物 |
| IL308219A (en) | 2021-05-05 | 2024-01-01 | Biogen Ma Inc | Compounds to Target Broton Tyrosine Kinase Degradation |
| CN117715904A (zh) | 2021-05-07 | 2024-03-15 | 凯麦拉医疗公司 | Cdk2降解剂和其用途 |
| US20220389394A1 (en) | 2021-05-18 | 2022-12-08 | Gilead Sciences, Inc. | METHODS OF USING FLT3L-Fc FUSION PROTEINS |
| WO2022250224A1 (ko) * | 2021-05-26 | 2022-12-01 | 주식회사 이노큐어테라퓨틱스 | 피페리딘디온 유도체 |
| WO2022250350A1 (ko) * | 2021-05-26 | 2022-12-01 | 주식회사 이노큐어테라퓨틱스 | 피페리딘디온 유도체 |
| KR102474999B1 (ko) * | 2021-05-26 | 2022-12-07 | 주식회사 이노큐어테라퓨틱스 | 피페리딘디온 유도체 |
| KR102489160B1 (ko) * | 2021-05-26 | 2023-01-18 | 주식회사 이노큐어테라퓨틱스 | 피페리딘디온 유도체 |
| WO2022255889A1 (en) * | 2021-06-01 | 2022-12-08 | Captor Therapeutics S.A. | Compounds which bind to cereblon, and use thereof |
| WO2022255888A1 (en) * | 2021-06-01 | 2022-12-08 | Captor Therapeutics S.A. | Targeted protein degradation using bifunctional compounds that bind ubiquitin ligase and target mcl-1 protein |
| WO2022255890A1 (en) * | 2021-06-01 | 2022-12-08 | Captor Therapeutics S.A. | Compounds which bind to cereblon, and use thereof |
| EP4351583A4 (en) | 2021-06-08 | 2025-06-04 | C4 Therapeutics, Inc. | THERAPEUTICS TO DEGRADE MUTANT BRAF |
| CN117561249A (zh) * | 2021-06-25 | 2024-02-13 | 细胞基因公司 | Cereblon结合化合物、其组合物及其用于治疗的方法 |
| US20240374591A1 (en) * | 2021-06-25 | 2024-11-14 | Celgene Corporation | Cereblon binding compounds, compositions thereof, and methods of treatment therewith |
| EP4359406A4 (en) * | 2021-06-25 | 2025-05-21 | Celgene Corporation | CEREBLON-BINDING COMPOUNDS, COMPOSITIONS THEREOF AND METHODS OF TREATMENT USING THEM |
| US20250129047A1 (en) | 2021-07-04 | 2025-04-24 | Newave Pharmaceutical Inc. | Isoquinoline derivatives as mutant egfr modulators and uses thereof |
| US20250018046A1 (en) | 2021-07-07 | 2025-01-16 | Biogen Ma Inc | Compounds for targeting degradation of irak4 proteins |
| IL309941A (en) | 2021-07-07 | 2024-03-01 | Biogen Ma Inc | Compounds to target degradation of IRAK4 proteins |
| KR20240035820A (ko) | 2021-07-09 | 2024-03-18 | 플렉시움 인코포레이티드 | Ikzf2를 조절하는 아릴 화합물 및 약학 조성물 |
| WO2023017442A1 (en) * | 2021-08-10 | 2023-02-16 | Uppthera, Inc. | Novel plk1 degradation inducing compound |
| CN118475567A (zh) * | 2021-08-11 | 2024-08-09 | 西藏海思科制药有限公司 | 一种杂环衍生物及其组合物和药学上的应用 |
| EP4367118B1 (en) | 2021-08-18 | 2025-01-29 | Nurix Therapeutics, Inc. | Bifunctional degraders of interleukin-1 receptor-associated kinases and therapeutic use thereof |
| WO2023025159A1 (zh) * | 2021-08-23 | 2023-03-02 | 上海领泰生物医药科技有限公司 | Irak4降解剂及其制备方法和应用 |
| EP4395549A1 (en) | 2021-09-01 | 2024-07-10 | Oerth Bio LLC | Compositions and methods for targeted degradation of proteins in a plant cell |
| CN115746058A (zh) * | 2021-09-03 | 2023-03-07 | 南京知和医药科技有限公司 | 一种多环化合物在制备抗肿瘤药物方面的用途 |
| WO2023056443A1 (en) * | 2021-10-01 | 2023-04-06 | Dana-Farber Cancer Institute, Inc. | Binders of cereblon and methods of use thereof |
| TW202322799A (zh) * | 2021-10-06 | 2023-06-16 | 美商C4醫藥公司 | 冠狀病毒非結構性蛋白3降解化合物 |
| CN116003418A (zh) * | 2021-10-22 | 2023-04-25 | 标新生物医药科技(上海)有限公司 | Crbn e3连接酶配体化合物、基于该配体化合物开发的蛋白降解剂及它们的应用 |
| KR20240091056A (ko) | 2021-10-28 | 2024-06-21 | 길리애드 사이언시즈, 인코포레이티드 | 피리디진-3(2h)-온 유도체 |
| WO2023077030A1 (en) | 2021-10-29 | 2023-05-04 | Gilead Sciences, Inc. | Cd73 compounds |
| EP4422635A4 (en) | 2021-10-29 | 2025-11-26 | Kymera Therapeutics Inc | IRAQ4 DEGRADATION AGENTS AND THEIR SYNTHESIS |
| WO2023081224A1 (en) * | 2021-11-03 | 2023-05-11 | St. Jude Children's Research Hospital, Inc. | Substituted n-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4- yl)methyl)benzamide analogs as modulators of cereblon protein |
| US20250127906A1 (en) * | 2021-11-05 | 2025-04-24 | University Of South Carolina | Small-molecule degraders of cdk8 and cdk19 |
| CN118574827A (zh) | 2021-11-24 | 2024-08-30 | 阿维纳斯运营公司 | Brm靶向化合物和相关的使用方法 |
| CN118679160A (zh) | 2021-11-24 | 2024-09-20 | 阿维纳斯运营公司 | Brm靶向化合物和相关的使用方法 |
| AU2022397695A1 (en) | 2021-11-25 | 2024-06-06 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Chimeric compound for targeted degradation of androgen receptor protein, preparation method therefor, and medical use thereof |
| EP4452414A2 (en) | 2021-12-22 | 2024-10-30 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| JP2024545193A (ja) | 2021-12-22 | 2024-12-05 | ギリアード サイエンシーズ, インコーポレイテッド | Ikarosジンクフィンガーファミリー分解剤及びその使用 |
| CN114085213B (zh) * | 2022-01-20 | 2022-03-25 | 苏州国匡医药科技有限公司 | 一种arv-471的制备方法 |
| TW202340168A (zh) | 2022-01-28 | 2023-10-16 | 美商基利科學股份有限公司 | Parp7抑制劑 |
| AU2023214044A1 (en) | 2022-01-31 | 2024-08-08 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| US12358887B2 (en) | 2022-03-17 | 2025-07-15 | Gilead Sciences, Inc. | IKAROS Zinc Finger Family degraders and uses thereof |
| EP4499628A1 (en) * | 2022-03-24 | 2025-02-05 | GlaxoSmithKline Intellectual Property Development Limited | 2,4-dioxotetrahydropyrimidinyl derivatives as degrons in protacs |
| CN119487038A (zh) | 2022-04-21 | 2025-02-18 | 吉利德科学公司 | Kras g12d调节化合物 |
| WO2023212599A2 (en) * | 2022-04-26 | 2023-11-02 | Endotarget Inc. | Compounds and methods for targeted degradation of estrogen receptors |
| KR20250021314A (ko) | 2022-06-06 | 2025-02-12 | 씨4 테라퓨틱스, 인코포레이티드 | 비시클릭-치환된 글루타르이미드 세레블론 결합제 |
| CN119487035A (zh) * | 2022-06-30 | 2025-02-18 | 安宏生医股份有限公司 | 双官能基化合物及包含所述双官能基化合物的医药组合物及其用于治疗雄激素受体相关疾病的方法 |
| WO2024006929A1 (en) | 2022-07-01 | 2024-01-04 | Gilead Sciences, Inc. | Cd73 compounds |
| WO2024015412A1 (en) * | 2022-07-12 | 2024-01-18 | Regents Of The University Of Michigan | Tetrahydronaphthalene derivatives as estrogen receptor degraders |
| CN116496253B (zh) * | 2022-08-19 | 2024-10-11 | 中国人民解放军军事科学院军事医学研究院 | c-MET蛋白靶向降解剂及其医药应用 |
| CN115089588A (zh) * | 2022-08-22 | 2022-09-23 | 云南大学 | 达沙布韦作为e3连接酶新型配体构建protac的应用 |
| WO2024050016A1 (en) | 2022-08-31 | 2024-03-07 | Oerth Bio Llc | Compositions and methods for targeted inhibition and degradation of proteins in an insect cell |
| US11957759B1 (en) | 2022-09-07 | 2024-04-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use |
| WO2024054953A1 (en) * | 2022-09-08 | 2024-03-14 | Halda Therapeutics Opco, Inc. | Heterobifunctional compounds and methods of treating disease |
| WO2024054954A1 (en) * | 2022-09-08 | 2024-03-14 | Halda Therapeutics Opco, Inc. | Heterobifunctional compounds and methods of treating disease |
| WO2024054955A1 (en) * | 2022-09-08 | 2024-03-14 | Halda Therapeutics Opco, Inc. | Heterobifunctional compounds and methods of treating disease |
| CN118019736A (zh) * | 2022-09-08 | 2024-05-10 | 标新生物医药科技(上海)有限公司 | 基于cereblon蛋白设计的分子胶化合物及其应用 |
| AU2023338217A1 (en) | 2022-09-09 | 2025-04-03 | Innovo Therapeutics, Inc. | CK1α AND DUAL CK1α / GSPT1 DEGRADING COMPOUNDS |
| CN119855812A (zh) * | 2022-09-14 | 2025-04-18 | 海南先声再明医药股份有限公司 | 多并环类化合物及其用途 |
| WO2024064316A1 (en) | 2022-09-23 | 2024-03-28 | Regents Of The University Of Michigan | Compounds and compositions as smarca2/4 inhibitors and uses thereof |
| WO2024073475A1 (en) * | 2022-09-27 | 2024-04-04 | Oncopia Therapeutics, Inc. D/B/A Proteovant Therapeutics, Inc. | Cereblon ligands and uses thereof |
| CN119998300A (zh) * | 2022-09-29 | 2025-05-13 | 海南先声再明医药股份有限公司 | 一类稠环化合物及其用途 |
| EP4596538A4 (en) * | 2022-09-29 | 2025-12-31 | Jiangsu Hengrui Pharmaceuticals Co Ltd | PHARMACEUTICALLY ACCEPTABLE SALT AND CRYSTALLINE FORM OF TETRAHYDRONAPHTALENE DERIVATIVE, AND PROCESS OF PREPARATION |
| CN117801051A (zh) * | 2022-09-30 | 2024-04-02 | 苏州德亘生物医药有限公司 | 一类eRF3a靶向蛋白降解机制治疗人类肿瘤的药物 |
| US20240180900A1 (en) | 2022-10-24 | 2024-06-06 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| US12331048B2 (en) | 2022-10-31 | 2025-06-17 | Ventus Therapeutics U.S., Inc. | Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 inhibitors |
| KR20240076745A (ko) * | 2022-11-22 | 2024-05-30 | 주식회사 이노큐어테라퓨틱스 | 신규한 c-MET 단백질 리간드를 포함하는 디그레이더 및 이를 포함하는 약학 조성물 |
| JP2025538554A (ja) * | 2022-11-22 | 2025-11-28 | イノキュア セラピューティクス,インコーポレイテッド | Brdタンパク質を分解するための分解剤およびそれを含有する薬学的組成物 |
| KR20240075764A (ko) * | 2022-11-22 | 2024-05-29 | 주식회사 이노큐어테라퓨틱스 | cMET 단백질을 분해하는 디그레이더 및 이를 포함하는 약학 조성물 |
| CN120641411A (zh) * | 2022-12-06 | 2025-09-12 | 凯普托尔治疗学股份有限公司 | 使用结合泛素连接酶和靶mcl-1蛋白的双功能化合物的靶向蛋白降解 |
| WO2024123195A1 (en) * | 2022-12-06 | 2024-06-13 | Captor Therapeutics S.A. | Targeted protein degradation using prodrugs of bifunctional compounds that bind ubiquitin ligase and target mcl-1 protein |
| EP4638436A1 (en) | 2022-12-22 | 2025-10-29 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| WO2024153025A1 (zh) * | 2023-01-16 | 2024-07-25 | 南京明德新药研发有限公司 | 取代的苯并七元环化合物及其应用 |
| EP4655073A2 (en) | 2023-01-26 | 2025-12-03 | Arvinas Operations, Inc. | Cereblon-based kras degrading protacs ans uses related thereto |
| EP4665720A2 (en) * | 2023-02-16 | 2025-12-24 | Bristol-Myers Squibb Company | Isoindolinone glutarimide and phenyl glutarimide analogs as degraders of ret kinase |
| CN116253719B (zh) * | 2023-03-06 | 2025-04-01 | 苏州国匡医药科技有限公司 | 一种雌激素和雄激素受体双重降解剂及其应用 |
| US20240374588A1 (en) | 2023-04-07 | 2024-11-14 | Astrazeneca Ab | Irak4 protacs |
| WO2024215754A1 (en) | 2023-04-11 | 2024-10-17 | Gilead Sciences, Inc. | Kras modulating compounds |
| TW202448467A (zh) * | 2023-04-20 | 2024-12-16 | 美商奧榮醫療公司 | 靶記細胞狀態之技術 |
| CN121079300A (zh) | 2023-04-21 | 2025-12-05 | 吉利德科学公司 | Prmt5抑制剂及其用途 |
| AU2024276994A1 (en) | 2023-05-24 | 2025-10-23 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| CN120202200A (zh) * | 2023-06-01 | 2025-06-24 | 标新生物医药科技(上海)有限公司 | 基于氧代异吲哚啉基取代的四氢嘧啶二酮的化合物及其应用 |
| WO2024245408A1 (zh) * | 2023-06-01 | 2024-12-05 | 上海海和药物研究开发股份有限公司 | 用于雄激素受体依赖性疾病的苯并(杂)环烷基化合物 |
| WO2024245444A1 (zh) * | 2023-06-01 | 2024-12-05 | 标新生物医药科技(上海)有限公司 | 氧代异吲哚啉基取代的四氢嘧啶二酮衍生物及其应用 |
| WO2024256988A1 (en) | 2023-06-14 | 2024-12-19 | Astrazeneca Ab | Smarca2 degraders and uses thereof |
| TW202515566A (zh) | 2023-06-14 | 2025-04-16 | 瑞典商阿斯特捷利康公司 | Smarca2降解劑及其用途 |
| WO2024263781A1 (en) * | 2023-06-23 | 2024-12-26 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | Targeted degraders of hiv-1 nef for the treatment of hiv disease |
| WO2025006753A2 (en) | 2023-06-30 | 2025-01-02 | Merck Patent Gmbh | Heterobifunctional compounds for the degradation of kras protein |
| WO2025006783A2 (en) | 2023-06-30 | 2025-01-02 | Merck Patent Gmbh | Heterobifunctional compounds for the degradation of kras |
| WO2025007000A1 (en) | 2023-06-30 | 2025-01-02 | Kumquat Biosciences Inc. | Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors |
| US20250042922A1 (en) | 2023-06-30 | 2025-02-06 | Gilead Sciences, Inc. | Kras modulating compounds |
| WO2025011623A1 (zh) * | 2023-07-12 | 2025-01-16 | 上海壹迪生物技术有限公司 | 氰基喹啉类靶向蛋白降解分子、其制备方法和应用 |
| US20250066328A1 (en) | 2023-07-26 | 2025-02-27 | Gilead Sciences, Inc. | Parp7 inhibitors |
| WO2025024811A1 (en) | 2023-07-26 | 2025-01-30 | Gilead Sciences, Inc. | Parp7 inhibitors |
| 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 |
| WO2025054530A1 (en) | 2023-09-08 | 2025-03-13 | Gilead Sciences, Inc. | Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds |
| WO2025054347A1 (en) | 2023-09-08 | 2025-03-13 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| CN119613374A (zh) * | 2023-09-14 | 2025-03-14 | 中国科学院上海药物研究所 | 吲唑酮类化合物、其制备方法、药物组合物及其应用 |
| WO2025063888A1 (en) | 2023-09-19 | 2025-03-27 | Kancure Pte. Ltd. | Survivin-targeted compounds |
| TW202530192A (zh) * | 2023-09-22 | 2025-08-01 | 英商葛蘭素史密斯克藍智慧財產發展有限公司 | 新穎化合物 |
| WO2025075693A1 (en) * | 2023-10-02 | 2025-04-10 | Purdue Research Foundation | Shp2 degraders for cancer therapy |
| TW202523291A (zh) | 2023-11-02 | 2025-06-16 | 美商金橘生物科技公司 | 降解劑及其用途 |
| US20250154172A1 (en) | 2023-11-03 | 2025-05-15 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| US20250177539A1 (en) * | 2023-12-01 | 2025-06-05 | Astrazeneca Ab | Er degraders and uses thereof |
| US20250230168A1 (en) | 2023-12-22 | 2025-07-17 | Gilead Sciences, Inc. | Azaspiro wrn inhibitors |
| WO2025136129A1 (en) * | 2023-12-22 | 2025-06-26 | Captor Therapeutics S.A. | Targeted protein degradation using bifunctional compounds that bind ubiquitin ligase and target protein kinase c |
| WO2025179161A1 (en) | 2024-02-21 | 2025-08-28 | Innovo Therapeutics, Inc. | Protein degrading compounds |
| WO2025212557A1 (en) * | 2024-04-01 | 2025-10-09 | The Johns Hopkins University | Delivery of aurora kinase inhibitors using nano-scale drug delivery platforms by covalent conjugation |
| WO2025245003A1 (en) | 2024-05-21 | 2025-11-27 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
Family Cites Families (142)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2460304C2 (de) | 1974-12-20 | 1983-08-04 | Grünenthal GmbH, 5190 Stolberg | 1-n-Propyl-4-phthalimido-piperidin-2,6-dion, Verfahren zu seiner Herstellung und dieses enthaltende Arzneimittel |
| US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
| US5510357A (en) | 1995-02-28 | 1996-04-23 | Eli Lilly And Company | Benzothiophene compounds as anti-estrogenic agents |
| CZ302378B6 (cs) | 1996-07-24 | 2011-04-20 | Celgene Corporation | Optický izomer (S)-1,3-dioxo-2-(2,6-dioxopiperidin-3-yl)-4-aminoisoindolin a farmaceutická kompozice s jeho obsahem |
| CA2287387C (en) | 1997-05-14 | 2010-02-16 | Sloan-Kettering Institute For Cancer Research | Methods and compositions for destruction of selected proteins |
| WO1999015521A1 (en) | 1997-09-23 | 1999-04-01 | Eli Lilly And Company | Benzothiophenes |
| ATE294163T1 (de) | 1997-12-17 | 2005-05-15 | Merck & Co Inc | Integrin-rezeptor-antagonisten |
| CA2342222A1 (en) * | 1998-08-31 | 2000-03-09 | Sugen, Inc. | Geometrically restricted 2-indolinone derivatives as modulators of protein kinase activity |
| US6306663B1 (en) | 1999-02-12 | 2001-10-23 | Proteinex, Inc. | Controlling protein levels in eucaryotic organisms |
| CA2372176A1 (en) | 1999-05-05 | 2000-11-09 | Merck & Co., Inc. | Novel prolines as antimicrobial agents |
| AU2001288213B2 (en) | 2000-06-28 | 2005-04-14 | Bristol-Myers Squibb Company | Selective androgen receptor modulators and methods for their identification, design and use |
| PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| US7208157B2 (en) | 2000-09-08 | 2007-04-24 | California Institute Of Technology | Proteolysis targeting chimeric pharmaceutical |
| WO2002020740A2 (en) | 2000-09-08 | 2002-03-14 | California Institute Of Technology | Proteolysis targeting chimeric pharmaceutical |
| US20030045552A1 (en) | 2000-12-27 | 2003-03-06 | Robarge Michael J. | Isoindole-imide compounds, compositions, and uses thereof |
| CA2432932A1 (en) | 2001-02-16 | 2002-08-29 | Mark A. Scialdone | Angiogenesis-inhibitory tripeptides, compositions and their methods of use |
| GB0106953D0 (en) | 2001-03-20 | 2001-05-09 | Univ Aberdeen | Neufofibrillary labels |
| HN2002000136A (es) | 2001-06-11 | 2003-07-31 | Basf Ag | Inhibidores de la proteasa del virus hiv, compuestos que contienen a los mismos, sus usos farmaceuticos y los materiales para su sintesis |
| US7030141B2 (en) | 2001-11-29 | 2006-04-18 | Christopher Franklin Bigge | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade |
| SI1505973T1 (sl) | 2002-05-17 | 2010-06-30 | Celgene Corp | Kombinacija za zdravljenje multiplega mieloma |
| RU2310651C2 (ru) | 2002-08-30 | 2007-11-20 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Азотсодержащие ароматические производные, фармацевтическая композиция, их содержащая, способ лечения и применение |
| WO2005007141A2 (en) * | 2003-07-11 | 2005-01-27 | Proteologics, Inc. | Ubiquitin ligase inhibitors and methods related thereto |
| WO2006006065A1 (en) | 2004-07-08 | 2006-01-19 | Warner-Lambert Company Llc | Androgen modulators |
| CN100383139C (zh) | 2005-04-07 | 2008-04-23 | 天津和美生物技术有限公司 | 可抑制细胞释放肿瘤坏死因子的哌啶-2,6-二酮衍生物 |
| WO2006113942A2 (en) | 2005-04-20 | 2006-10-26 | Schering Corporation | Method of inhibiting cathepsin activity |
| AU2007245022A1 (en) | 2006-03-29 | 2007-11-08 | The Regents Of The University Of California | Diarylthiohydantoin compounds |
| TWI473808B (zh) | 2005-06-22 | 2015-02-21 | Plexxikon Inc | 用於激酶調節的化合物及方法及其適應症 |
| CA2822094C (en) | 2005-08-31 | 2015-10-27 | Celgene Corporation | Isoindole-imide compounds and compositions comprising and methods of using the same |
| JP2009529008A (ja) | 2006-03-03 | 2009-08-13 | ノバルティス アクチエンゲゼルシャフト | N−ホルミルヒドロキシルアミン化合物 |
| AU2007275415A1 (en) | 2006-07-20 | 2008-01-24 | Ligand Pharmaceuticals Incorporated | Proline urea CCR1 antagonists for the treatment of autoimmune diseases or inflammation |
| RU2448101C2 (ru) | 2006-08-30 | 2012-04-20 | Селджин Корпорейшн | 5-замещенные изоиндолиновые соединения |
| JP5523831B2 (ja) | 2006-08-30 | 2014-06-18 | セルジーン コーポレイション | 5−置換イソインドリン化合物 |
| US8877780B2 (en) | 2006-08-30 | 2014-11-04 | Celgene Corporation | 5-substituted isoindoline compounds |
| WO2008054827A2 (en) | 2006-11-03 | 2008-05-08 | Pharmacyclics, Inc. | Bruton's tyrosine kinase activity probe and method of using |
| AU2008206695A1 (en) * | 2007-01-16 | 2008-07-24 | Proteologics Ltd | Methods for enhancing the therapeutic efficacy of topoisomerase inhibitors |
| KR20100038108A (ko) | 2007-07-25 | 2010-04-12 | 브리스톨-마이어스 스큅 컴퍼니 | 트리아진 키나제 억제제 |
| JP2010535213A (ja) | 2007-07-31 | 2010-11-18 | アンドロサイエンス コーポレーション | アンドロゲン受容体分解(ard)エンハンサーを含む組成物ならびに皮膚疾患および脱毛の予防的または治療的処理方法 |
| EP2239264A4 (en) | 2007-12-28 | 2012-01-11 | Mitsubishi Tanabe Pharma Corp | ANTITUMORAL MEDIUM |
| EP3354646A1 (en) | 2008-10-29 | 2018-08-01 | Celgene Corporation | Isoindoline compounds for use in the treatment of cancer |
| US8691187B2 (en) | 2009-03-23 | 2014-04-08 | Eli Lilly And Company | Imaging agents for detecting neurological disorders |
| WO2010141805A1 (en) | 2009-06-05 | 2010-12-09 | Janssen Pharmaceutica Nv | Heterocyclic amides as modulators of trpa1 |
| EP2453908B1 (en) | 2009-07-13 | 2018-03-14 | President and Fellows of Harvard College | Bifunctional stapled polypeptides and uses thereof |
| SG10201501062SA (en) | 2010-02-11 | 2015-04-29 | Celgene Corp | Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same |
| US8198300B2 (en) | 2010-04-29 | 2012-06-12 | Universidad De Chile | Method for preventing tau protein aggregation and treating Alzheimer's disease with a quinoline derivative compound |
| CA2799403C (en) | 2010-05-14 | 2020-01-21 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for treating leukemia |
| US8981083B2 (en) | 2010-05-14 | 2015-03-17 | Dana Farber Cancer Institute, Inc. | Compositions and methods for treating neoplasia, inflammatory disease and other disorders |
| AU2011272860A1 (en) | 2010-06-30 | 2013-02-07 | Brandeis University | Small-molecule-targeted protein degradation |
| US8822520B2 (en) | 2010-09-22 | 2014-09-02 | Presidio Pharmaceuticals, Inc. | Substituted bicyclic HCV inhibitors |
| AU2011305315A1 (en) | 2010-09-24 | 2013-03-28 | The Regents Of The University Of Michigan | Deubiquitinase inhibitors and methods for use of the same |
| CN102477033A (zh) | 2010-11-23 | 2012-05-30 | 苏州波锐生物医药科技有限公司 | 苯并噻酚类化合物及其在制备预防和/或治疗乳腺癌骨质疏松症药物中的用途 |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| EP2649099A4 (en) | 2010-12-07 | 2016-10-19 | Univ Yale | SMALL MOLECULAR HYDROPHOBIC LABELING OF FUSION PROTEINS AND INDUCED REMOVAL FROM THIS |
| US20140243282A1 (en) | 2010-12-31 | 2014-08-28 | Satish Reddy Kallam | Methods and compositions for designing novel conjugate therapeutics |
| US9365640B2 (en) | 2011-04-29 | 2016-06-14 | Celgene Corporation | Methods for the treatment of cancer and inflammatory diseases using cereblon as a predictor |
| DK2797888T3 (en) | 2011-12-31 | 2016-09-19 | Beigene Ltd | Fused tricyclic compounds as RAF kinase inhibitors |
| WO2013106646A2 (en) | 2012-01-12 | 2013-07-18 | Yale University | Compounds and methods for the inhibition of vcb e3 ubiquitin ligase |
| EP3608317A1 (en) * | 2012-01-12 | 2020-02-12 | Yale University | Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase |
| US20150141470A1 (en) | 2012-05-08 | 2015-05-21 | The Broad Institute, Inc. | Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy |
| US20150119435A1 (en) | 2012-05-11 | 2015-04-30 | Yale University | Compounds useful for promoting protein degradation and methods using same |
| BR112014032105A2 (pt) | 2012-06-25 | 2017-08-01 | Oncoethix Sa | método para o tratamento de câncer |
| CA2879454A1 (en) | 2012-07-19 | 2014-01-23 | Drexel University | Novel sigma receptor ligands and methods of modulating cellular protein homeostasis using same |
| KR101738063B1 (ko) | 2012-09-21 | 2017-05-19 | 아로그 파마슈티칼스, 인코퍼레이티드 | 구조적으로 활성인 인산화된 flt3 키나제의 억제 방법 |
| GB201311910D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel Compounds |
| NL2011274C2 (en) | 2013-08-06 | 2015-02-09 | Illumicare Ip B V 51 | Groundbreaking platform technology for specific binding to necrotic cells. |
| CN105164135A (zh) | 2013-02-22 | 2015-12-16 | 拜耳医药股份有限公司 | 4-取代的吡咯并二氮杂卓和吡唑并二氮杂卓 |
| US9492460B2 (en) | 2013-02-27 | 2016-11-15 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
| 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 |
| EP3027614B1 (de) | 2013-07-23 | 2017-08-23 | Bayer Pharma Aktiengesellschaft | Substituierte dihydropyrido[3,4-b]pyrazinone als duale inhibitoren von bet-proteinen und polo-like kinasen |
| WO2015015318A2 (en) | 2013-07-31 | 2015-02-05 | Zenith Epigenetics Corp. | Novel quinazolinones as bromodomain inhibitors |
| US20150051208A1 (en) | 2013-08-14 | 2015-02-19 | Boehringer Ingelheim International Gmbh | Pyridinones |
| US9428513B2 (en) | 2013-11-07 | 2016-08-30 | Boehringer Ingelheim International Gmbh | Triazolopyrazine |
| CN105934246B (zh) | 2013-11-18 | 2019-10-22 | 福马疗法公司 | 作为bet溴域抑制剂的四氢喹啉组成物 |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9458156B2 (en) | 2014-12-23 | 2016-10-04 | Bristol-Myers Squibb Company | Tricyclic compounds as anticancer agents |
| US20150259288A1 (en) | 2014-03-14 | 2015-09-17 | City Of Hope | 5-bromo-indirubins |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| US20160058872A1 (en) | 2014-04-14 | 2016-03-03 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| KR20250127179A (ko) * | 2014-04-14 | 2025-08-26 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법 |
| TW201613916A (en) | 2014-06-03 | 2016-04-16 | Gilead Sciences Inc | TANK-binding kinase inhibitor compounds |
| WO2015188120A1 (en) | 2014-06-06 | 2015-12-10 | The Scripps Research Institute | Sulfur(vi) fluoride compounds and methods for the preparation thereof |
| WO2015195863A1 (en) | 2014-06-20 | 2015-12-23 | Constellation Pharmaceuticals, Inc. | Hydrated 2-((4s)-6-(4-chlorophenyl)-1 -methyl-4h-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide |
| US20160022642A1 (en) | 2014-07-25 | 2016-01-28 | Yale University | Compounds Useful for Promoting Protein Degradation and Methods Using Same |
| US10071164B2 (en) | 2014-08-11 | 2018-09-11 | Yale University | Estrogen-related receptor alpha based protac compounds and associated methods of use |
| EP3201199A1 (en) | 2014-10-02 | 2017-08-09 | Glaxosmithkline Intellectual Property (No. 2) Limited | Compound |
| EP3212654B1 (en) | 2014-10-27 | 2020-04-08 | Tensha Therapeutics, Inc. | Bromodomain inhibitors |
| WO2016097071A1 (en) | 2014-12-18 | 2016-06-23 | F. Hoffmann-La Roche Ag | Estrogen receptor modulators and uses thereof |
| JP6815318B2 (ja) * | 2014-12-23 | 2021-01-20 | ダナ−ファーバー キャンサー インスティテュート,インコーポレイテッド | 二官能性分子によって標的化タンパク質分解を誘導する方法 |
| US9694084B2 (en) | 2014-12-23 | 2017-07-04 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| KR102564925B1 (ko) | 2015-01-20 | 2023-08-07 | 아비나스 오퍼레이션스, 인코포레이티드 | 안드로겐 수용체의 표적화된 분해를 위한 화합물 및 방법 |
| US12312316B2 (en) | 2015-01-20 | 2025-05-27 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| 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 |
| GB201506872D0 (en) | 2015-04-22 | 2015-06-03 | Ge Oil & Gas Uk Ltd | Novel compounds |
| GB201506871D0 (en) * | 2015-04-22 | 2015-06-03 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| CA2988414C (en) * | 2015-06-04 | 2023-09-26 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| EP3302482A4 (en) | 2015-06-05 | 2018-12-19 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| WO2017007612A1 (en) * | 2015-07-07 | 2017-01-12 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| US20170008904A1 (en) * | 2015-07-10 | 2017-01-12 | Arvinas, Inc. | Mdm2-based modulators of proteolysis and associated methods of use |
| CA2988436A1 (en) * | 2015-07-13 | 2017-01-19 | Arvinas, Inc. | Alanine-based modulators of proteolysis and associated methods of use |
| WO2017024319A1 (en) | 2015-08-06 | 2017-02-09 | Dana-Farber Cancer Institute, Inc. | Tunable endogenous protein degradation |
| EP3337476A4 (en) | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| GB201516243D0 (en) | 2015-09-14 | 2015-10-28 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| RU2018120330A (ru) * | 2015-11-02 | 2019-12-04 | Йейл Юниверсити | Химерные соединения, осуществляющие нацеливание для протеолиза, и способы их получения и применения |
| JP7264642B2 (ja) | 2016-03-16 | 2023-04-25 | エイチ リー モフィット キャンサー センター アンド リサーチ インスティテュート インコーポレイテッド | エフェクターt細胞機能を増進するための、セレブロンを標的とする小分子 |
| US20170281784A1 (en) | 2016-04-05 | 2017-10-05 | Arvinas, Inc. | Protein-protein interaction inducing technology |
| CN113788818A (zh) | 2016-04-06 | 2021-12-14 | 密执安大学评议会 | Mdm2蛋白质降解剂 |
| JP6968823B2 (ja) | 2016-04-22 | 2021-11-17 | ダナ−ファーバー キャンサー インスティテュート,インコーポレイテッド | Egfrの分解のための二官能性分子、及び使用方法 |
| WO2017197051A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Amine-linked c3-glutarimide degronimers for target protein degradation |
| EP3455218A4 (en) | 2016-05-10 | 2019-12-18 | C4 Therapeutics, Inc. | C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| WO2018053354A1 (en) | 2016-09-15 | 2018-03-22 | Arvinas, Inc. | Indole derivatives as estrogen receptor degraders |
| HUE061847T2 (hu) | 2016-10-11 | 2023-08-28 | Arvinas Operations Inc | Androgén receptor célzott degradálására alkalmas vegyületek és eljárások |
| CA3042260C (en) | 2016-11-01 | 2023-10-03 | Arvinas, Inc. | Tau-protein targeting protacs and associated methods of use |
| CA3042301A1 (en) | 2016-11-22 | 2018-05-31 | Dana-Farber Cancer Institute, Inc. | Degradation of protein kinases by conjugation of protein kinase inhibitors with e3 ligase ligand and methods of use |
| RS64976B1 (sr) | 2016-12-01 | 2024-01-31 | Arvinas Operations Inc | Derivati tetrahidronaftalena i tetrahidroizohinolina kao degradatori estrogenih receptora |
| CN110741004B (zh) | 2016-12-23 | 2023-10-17 | 阿尔维纳斯运营股份有限公司 | 用于迅速加速性纤维肉瘤多肽的靶向降解的化合物和方法 |
| WO2018118598A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, Inc. | Compounds and methods for the targeted degradation of fetal liver kinase polypeptides |
| JP2020505327A (ja) | 2016-12-23 | 2020-02-20 | 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. | Egfrタンパク質分解標的化キメラ分子およびその関連する使用方法 |
| US11191741B2 (en) | 2016-12-24 | 2021-12-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
| AU2018211975B2 (en) | 2017-01-26 | 2022-05-26 | Arvinas Operations, Inc. | Modulators of estrogen receptor proteolysis and associated methods of use |
| KR102747905B1 (ko) | 2017-01-31 | 2024-12-31 | 아비나스 오퍼레이션스, 인코포레이티드 | 세레블론 리간드 및 이를 포함하는 이작용성 화합물 |
| CN110545853A (zh) | 2017-04-28 | 2019-12-06 | 石英治疗有限公司 | Raf降解偶联化合物 |
| AU2018261331C1 (en) | 2017-05-01 | 2022-08-04 | Spg Therapeutics, Inc. | Tripartite androgen receptor eliminators, methods and uses thereof |
| US11505560B2 (en) | 2017-10-20 | 2022-11-22 | Dana-Farber Cancer Institute, Inc. | Heterobifunctional compounds with improved specificity |
| EP3743066A4 (en) | 2018-01-26 | 2021-09-08 | Yale University | IMIDE-BASED PROTEOLYSIS MODULATORS AND RELATED METHODS OF USE |
| BR112020018006A2 (pt) | 2018-04-12 | 2021-01-12 | Bayer Aktiengesellschaft | Derivados de n-(ciclopropilmetil)-5-(metilsulfonil)-n-{1-[1-(pirimidin-2-il)-1h-1,2,4-triazol-5-il]etil}benzamida e os derivados correspondentes de piridina-carboxamida como pesticidas |
| AU2020404305A1 (en) | 2019-12-19 | 2022-08-04 | Janssen Pharmaceutica Nv | Substituted straight chain spiro derivatives |
| US20230087008A1 (en) | 2019-12-19 | 2023-03-23 | Skinosive | Adhesive photoprotective compounds and uses thereof |
| PH12022551486A1 (en) | 2019-12-19 | 2023-11-13 | Arvinas Operations Inc | Compounds and methods for the targeted degradation of androgen receptor |
| BR112022012020A2 (pt) | 2019-12-19 | 2022-09-20 | Debiopharm Int Sa | Novos compostos e seu uso |
| JOP20220156A1 (ar) | 2019-12-19 | 2023-01-30 | Bayer Ag | مشتقات فوروإندازول |
| JP7644517B2 (ja) | 2019-12-19 | 2025-03-12 | ジャコバイオ ファーマスーティカルズ カンパニー リミテッド | Kras突然変異型タンパク質阻害剤 |
| CN113087704B (zh) | 2019-12-23 | 2023-09-08 | 上海济煜医药科技有限公司 | 一种蛋白降解剂化合物的制备方法和应用 |
| PH12022551585A1 (en) | 2019-12-27 | 2023-11-29 | Lupin Ltd | Substituted tricyclic compounds |
| IL298525A (en) | 2020-05-29 | 2023-01-01 | Blueprint Medicines Corp | Pralsetinib pharmaceutical compositions |
| PH12022553222A1 (en) | 2020-05-29 | 2024-02-12 | Boehringer Ingelheim Animal Health Usa Inc | Anthelmintic heterocyclic compounds |
| MX2023006883A (es) | 2020-12-11 | 2023-06-23 | Arvinas Operations Inc | Metodos para tratar el cancer de prostata. |
| EP4291159A1 (en) | 2021-02-15 | 2023-12-20 | Propella Therapeutics, Inc. | Abiraterone prodrugs |
| US20240180900A1 (en) | 2022-10-24 | 2024-06-06 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| AU2024245334A1 (en) | 2023-03-30 | 2025-10-02 | Arvinas Operations, Inc. | Crystalline forms of a compound for the targeted degradation of the androgen receptor |
| US20250009737A1 (en) | 2023-06-30 | 2025-01-09 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
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2018
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| US20250313547A1 (en) | 2025-10-09 |
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| WO2018144649A8 (en) | 2019-08-22 |
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| MX2023008056A (es) | 2023-09-12 |
| CN110612294B (zh) | 2024-01-16 |
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| MX2019009046A (es) | 2019-10-30 |
| CN115974840A (zh) | 2023-04-18 |
| US20180215731A1 (en) | 2018-08-02 |
| IL268069A (en) | 2019-09-26 |
| KR20190116315A (ko) | 2019-10-14 |
| RU2019123462A (ru) | 2021-01-27 |
| RU2019123462A3 (enExample) | 2021-05-24 |
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| CA3050309A1 (en) | 2018-08-09 |
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