JP2019514883A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2019514883A5 JP2019514883A5 JP2018555281A JP2018555281A JP2019514883A5 JP 2019514883 A5 JP2019514883 A5 JP 2019514883A5 JP 2018555281 A JP2018555281 A JP 2018555281A JP 2018555281 A JP2018555281 A JP 2018555281A JP 2019514883 A5 JP2019514883 A5 JP 2019514883A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- alkyl
- disease
- independently
- formula
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 51
- 230000001588 bifunctional Effects 0.000 claims description 46
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 28
- 125000000217 alkyl group Chemical group 0.000 claims description 20
- 201000010099 disease Diseases 0.000 claims description 16
- 229910052760 oxygen Inorganic materials 0.000 claims description 16
- 230000027455 binding Effects 0.000 claims description 15
- 102000013701 Cyclin-Dependent Kinase 4 Human genes 0.000 claims description 14
- 108010025464 Cyclin-Dependent Kinase 4 Proteins 0.000 claims description 14
- 229910052799 carbon Inorganic materials 0.000 claims description 14
- 229910052736 halogen Inorganic materials 0.000 claims description 14
- 150000002367 halogens Chemical class 0.000 claims description 14
- 239000003446 ligand Substances 0.000 claims description 14
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 12
- 201000011510 cancer Diseases 0.000 claims description 12
- 125000005842 heteroatoms Chemical group 0.000 claims description 12
- 229910052717 sulfur Inorganic materials 0.000 claims description 12
- 102000013698 Cyclin-Dependent Kinase 6 Human genes 0.000 claims description 11
- 108010025468 Cyclin-Dependent Kinase 6 Proteins 0.000 claims description 11
- 150000003839 salts Chemical class 0.000 claims description 10
- 239000011780 sodium chloride Substances 0.000 claims description 10
- 206010017758 Gastric cancer Diseases 0.000 claims description 9
- 201000011549 stomach cancer Diseases 0.000 claims description 9
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims description 8
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 8
- 125000004432 carbon atoms Chemical group C* 0.000 claims description 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 8
- 206010000565 Acquired immunodeficiency syndrome Diseases 0.000 claims description 7
- 108091000081 Phosphotransferases Proteins 0.000 claims description 7
- 102000001253 Protein Kinases Human genes 0.000 claims description 7
- 206010063837 Reperfusion injury Diseases 0.000 claims description 6
- 229910052739 hydrogen Inorganic materials 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 206010006187 Breast cancer Diseases 0.000 claims description 5
- 206010009944 Colon cancer Diseases 0.000 claims description 5
- 206010025323 Lymphomas Diseases 0.000 claims description 5
- 206010025310 Other lymphomas Diseases 0.000 claims description 5
- 208000008443 Pancreatic Carcinoma Diseases 0.000 claims description 5
- 230000002401 inhibitory effect Effects 0.000 claims description 5
- 201000002528 pancreatic cancer Diseases 0.000 claims description 5
- 206010000880 Acute myeloid leukaemia Diseases 0.000 claims description 4
- 206010001019 Acute promyelocytic leukaemia Diseases 0.000 claims description 4
- 206010005949 Bone cancer Diseases 0.000 claims description 4
- 206010006895 Cachexia Diseases 0.000 claims description 4
- 206010061218 Inflammation Diseases 0.000 claims description 4
- 206010024324 Leukaemias Diseases 0.000 claims description 4
- 208000008456 Leukemia, Myelogenous, Chronic, BCR-ABL Positive Diseases 0.000 claims description 4
- 208000007046 Leukemia, Myeloid, Acute Diseases 0.000 claims description 4
- 208000005749 Leukemia, Promyelocytic, Acute Diseases 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 206010033128 Ovarian cancer Diseases 0.000 claims description 4
- 206010060862 Prostate cancer Diseases 0.000 claims description 4
- 206010038389 Renal cancer Diseases 0.000 claims description 4
- 201000005216 brain cancer Diseases 0.000 claims description 4
- 201000006934 chronic myeloid leukemia Diseases 0.000 claims description 4
- 201000004624 dermatitis Diseases 0.000 claims description 4
- 230000002496 gastric Effects 0.000 claims description 4
- 125000001072 heteroaryl group Chemical group 0.000 claims description 4
- 230000004054 inflammatory process Effects 0.000 claims description 4
- 201000007270 liver cancer Diseases 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 201000000849 skin cancer Diseases 0.000 claims description 4
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims description 4
- 206010004146 Basal cell carcinoma Diseases 0.000 claims description 3
- 206010061255 Ischaemia Diseases 0.000 claims description 3
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 3
- 208000006011 Stroke Diseases 0.000 claims description 3
- 230000000747 cardiac effect Effects 0.000 claims description 3
- 201000008779 central nervous system disease Diseases 0.000 claims description 3
- 125000006448 cycloalkyl cycloalkyl group Chemical group 0.000 claims description 3
- 210000002919 epithelial cells Anatomy 0.000 claims description 3
- 230000002062 proliferating Effects 0.000 claims description 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims description 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 2
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims description 2
- 208000009956 Adenocarcinoma Diseases 0.000 claims description 2
- 206010001897 Alzheimer's disease Diseases 0.000 claims description 2
- 206010002026 Amyotrophic lateral sclerosis Diseases 0.000 claims description 2
- 206010003210 Arteriosclerosis Diseases 0.000 claims description 2
- 206010003246 Arthritis Diseases 0.000 claims description 2
- 208000006673 Asthma Diseases 0.000 claims description 2
- 206010003816 Autoimmune disease Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 2
- 206010007559 Cardiac failure congestive Diseases 0.000 claims description 2
- 208000005846 Cardiomyopathy Diseases 0.000 claims description 2
- 208000008787 Cardiovascular Disease Diseases 0.000 claims description 2
- 206010008120 Cerebral ischaemia Diseases 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 2
- 206010011401 Crohn's disease Diseases 0.000 claims description 2
- 208000005679 Eczema Diseases 0.000 claims description 2
- 208000007882 Gastritis Diseases 0.000 claims description 2
- 208000005017 Glioblastoma Diseases 0.000 claims description 2
- 206010018634 Gouty arthritis Diseases 0.000 claims description 2
- 208000005721 HIV Infections Diseases 0.000 claims description 2
- 206010019016 Haemorrhagic stroke Diseases 0.000 claims description 2
- 108009000344 Head and Neck Squamous Cell Carcinoma Proteins 0.000 claims description 2
- 206010073071 Hepatocellular carcinoma Diseases 0.000 claims description 2
- 208000006572 Human Influenza Diseases 0.000 claims description 2
- 201000001971 Huntington's disease Diseases 0.000 claims description 2
- 206010020751 Hypersensitivity Diseases 0.000 claims description 2
- 206010021972 Inflammatory bowel disease Diseases 0.000 claims description 2
- 206010022000 Influenza Diseases 0.000 claims description 2
- 208000002551 Irritable Bowel Syndrome Diseases 0.000 claims description 2
- 206010061256 Ischaemic stroke Diseases 0.000 claims description 2
- 208000003456 Juvenile Arthritis Diseases 0.000 claims description 2
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims description 2
- 210000004072 Lung Anatomy 0.000 claims description 2
- 206010027476 Metastasis Diseases 0.000 claims description 2
- 208000000112 Myalgia Diseases 0.000 claims description 2
- 208000010125 Myocardial Infarction Diseases 0.000 claims description 2
- 208000004296 Neuralgia Diseases 0.000 claims description 2
- 206010053643 Neurodegenerative disease Diseases 0.000 claims description 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
- 208000002193 Pain Diseases 0.000 claims description 2
- 206010061536 Parkinson's disease Diseases 0.000 claims description 2
- 206010035664 Pneumonia Diseases 0.000 claims description 2
- 206010037660 Pyrexia Diseases 0.000 claims description 2
- 208000006265 Renal Cell Carcinoma Diseases 0.000 claims description 2
- 206010039073 Rheumatoid arthritis Diseases 0.000 claims description 2
- 206010040070 Septic shock Diseases 0.000 claims description 2
- 210000003491 Skin Anatomy 0.000 claims description 2
- 208000008513 Spinal Cord Injury Diseases 0.000 claims description 2
- 208000006045 Spondylarthropathy Diseases 0.000 claims description 2
- 206010052775 Spondyloarthropathy Diseases 0.000 claims description 2
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims description 2
- 206010041823 Squamous cell carcinoma Diseases 0.000 claims description 2
- 208000007107 Stomach Ulcer Diseases 0.000 claims description 2
- 208000007536 Thrombosis Diseases 0.000 claims description 2
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 claims description 2
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 claims description 2
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims description 2
- 125000003545 alkoxy group Chemical group 0.000 claims description 2
- 201000005794 allergic hypersensitivity disease Diseases 0.000 claims description 2
- 125000005418 aryl aryl group Chemical group 0.000 claims description 2
- 201000009596 autoimmune hypersensitivity disease Diseases 0.000 claims description 2
- 201000006474 brain ischemia Diseases 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 201000008031 cardiomyopathy Diseases 0.000 claims description 2
- 210000004027 cells Anatomy 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 230000001684 chronic Effects 0.000 claims description 2
- 201000006233 congestive heart failure Diseases 0.000 claims description 2
- 229910052805 deuterium Inorganic materials 0.000 claims description 2
- YZCKVEUIGOORGS-OUBTZVSYSA-N deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 231100001003 eczema Toxicity 0.000 claims description 2
- 201000004101 esophageal cancer Diseases 0.000 claims description 2
- 201000005917 gastric ulcer Diseases 0.000 claims description 2
- 201000005569 gout Diseases 0.000 claims description 2
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 2
- 201000001820 human immunodeficiency virus infectious disease Diseases 0.000 claims description 2
- 200000000018 inflammatory disease Diseases 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 201000006721 lip cancer Diseases 0.000 claims description 2
- 201000004792 malaria Diseases 0.000 claims description 2
- 201000009906 meningitis Diseases 0.000 claims description 2
- 125000002950 monocyclic group Chemical group 0.000 claims description 2
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 2
- 201000008383 nephritis Diseases 0.000 claims description 2
- 230000003959 neuroinflammation Effects 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims description 2
- 201000008482 osteoarthritis Diseases 0.000 claims description 2
- 201000004681 psoriasis Diseases 0.000 claims description 2
- 230000002685 pulmonary Effects 0.000 claims description 2
- 201000003651 pulmonary sarcoidosis Diseases 0.000 claims description 2
- 201000010174 renal carcinoma Diseases 0.000 claims description 2
- 230000000268 renotropic Effects 0.000 claims description 2
- 200000000008 restenosis Diseases 0.000 claims description 2
- 230000036303 septic shock Effects 0.000 claims description 2
- 201000002314 small intestine cancer Diseases 0.000 claims description 2
- 201000006704 ulcerative colitis Diseases 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- 208000009856 Lung Disease Diseases 0.000 claims 2
- 208000003950 B-Cell Lymphoma Diseases 0.000 claims 1
- 210000004204 Blood Vessels Anatomy 0.000 claims 1
- 210000000988 Bone and Bones Anatomy 0.000 claims 1
- 206010028323 Muscle pain Diseases 0.000 claims 1
- 206010068760 Ulcers Diseases 0.000 claims 1
- 201000009030 carcinoma Diseases 0.000 claims 1
- 201000011231 colorectal cancer Diseases 0.000 claims 1
- 231100000406 dermatitis Toxicity 0.000 claims 1
- 201000008325 diseases of cellular proliferation Diseases 0.000 claims 1
- 201000009673 liver disease Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 201000009251 multiple myeloma Diseases 0.000 claims 1
- 230000000926 neurological Effects 0.000 claims 1
- 231100000397 ulcer Toxicity 0.000 claims 1
- 230000000051 modifying Effects 0.000 description 4
- 239000003814 drug Substances 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 0 **c1c(C(N([C@](CCC(N2)=N)C2=*)C2=O)=*)c2ccc1 Chemical compound **c1c(C(N([C@](CCC(N2)=N)C2=*)C2=O)=*)c2ccc1 0.000 description 2
- 201000009910 diseases by infectious agent Diseases 0.000 description 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 description 1
- 108009000283 Allograft Rejection Proteins 0.000 description 1
- 206010060945 Bacterial infection Diseases 0.000 description 1
- 206010007554 Cardiac failure Diseases 0.000 description 1
- 210000004351 Coronary Vessels Anatomy 0.000 description 1
- 206010013637 Dressler's syndrome Diseases 0.000 description 1
- 206010018338 Glioma Diseases 0.000 description 1
- 206010018651 Graft versus host disease Diseases 0.000 description 1
- 206010019280 Heart failure Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 206010061523 Lip and/or oral cavity cancer Diseases 0.000 description 1
- 210000004185 Liver Anatomy 0.000 description 1
- 208000004852 Lung Injury Diseases 0.000 description 1
- 208000001388 Opportunistic Infections Diseases 0.000 description 1
- 208000001132 Osteoporosis Diseases 0.000 description 1
- 208000001293 Peripheral Nervous System Disease Diseases 0.000 description 1
- 206010034606 Peripheral neuropathy Diseases 0.000 description 1
- 206010069363 Traumatic lung injury Diseases 0.000 description 1
- 206010047461 Viral infection Diseases 0.000 description 1
- 208000001756 Virus Disease Diseases 0.000 description 1
- 230000033115 angiogenesis Effects 0.000 description 1
- 230000001640 apoptogenic Effects 0.000 description 1
- 230000002917 arthritic Effects 0.000 description 1
- 201000010816 bone resorption disease Diseases 0.000 description 1
- 230000002757 inflammatory Effects 0.000 description 1
- 231100000515 lung injury Toxicity 0.000 description 1
- 230000036210 malignancy Effects 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 201000006417 multiple sclerosis Diseases 0.000 description 1
- 210000000056 organs Anatomy 0.000 description 1
- 201000010001 silicosis Diseases 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 201000005671 spondyloarthropathy Diseases 0.000 description 1
- 201000010874 syndrome Diseases 0.000 description 1
- 241001529453 unidentified herpesvirus Species 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662326571P | 2016-04-22 | 2016-04-22 | |
| US62/326,571 | 2016-04-22 | ||
| PCT/US2017/028941 WO2017185031A1 (en) | 2016-04-22 | 2017-04-21 | Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019514883A JP2019514883A (ja) | 2019-06-06 |
| JP2019514883A5 true JP2019514883A5 (US20040106767A1-20040603-C00005.png) | 2020-05-28 |
| JP6921115B2 JP6921115B2 (ja) | 2021-08-18 |
Family
ID=60116458
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018555281A Active JP6921115B2 (ja) | 2016-04-22 | 2017-04-21 | サイクリン依存性キナーゼ４／６（ｃｄｋ４／６）阻害剤のｅ３リガーゼリガンドとのコンジュゲーションによるｃｄｋ４／６の分解および使用法 |
Country Status (7)
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3445760B1 (en) * | 2016-04-22 | 2022-02-23 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 9 (cdk9) by conjugation of cdk9 inhibitors with e3 ligase ligand and methods of use |
| US10584101B2 (en) * | 2016-10-11 | 2020-03-10 | Arvinas, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| 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. |
| CN110267659A (zh) * | 2016-12-08 | 2019-09-20 | 西奈山伊坎医学院 | 用于治疗cdk4/6介导的癌症的组合物和方法 |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| CN109516989B (zh) * | 2017-09-17 | 2021-12-31 | 上海美志医药科技有限公司 | 一类抑制并降解cdk的化合物 |
| JP2021506978A (ja) | 2017-12-22 | 2021-02-22 | ラヴェンナ ファーマシューティカルズ，インコーポレイテッド | ホスファチジルイノシトールリン酸キナーゼ阻害剤としてのアミノピリジン誘導体 |
| WO2019160890A1 (en) * | 2018-02-13 | 2019-08-22 | Dana-Farber Cancer Institute, Inc. | Cyclin-dependent kinase degraders and methods of use |
| CN112334451A (zh) | 2018-02-15 | 2021-02-05 | 诺维逊生物股份有限公司 | 作为激酶抑制剂的杂环化合物 |
| CA3091041A1 (en) * | 2018-02-22 | 2019-08-29 | Ichan School Of Medicine At Mount Sinai | Protein arginine methyltransferase 5 (prmt5) degradation / disruption compounds and methods of use |
| CN112154146A (zh) * | 2018-03-06 | 2020-12-29 | 西奈山伊坎医学院 | 丝氨酸苏氨酸激酶(akt)降解/破坏化合物和使用方法 |
| KR102548191B1 (ko) * | 2018-04-09 | 2023-06-28 | 상하이테크 유니버시티 | 표적 단백질 분해 화합물, 이의 항종양 응용, 이의 중간체 및 중간체의 응용 |
| CN112996518A (zh) * | 2018-06-21 | 2021-06-18 | 西奈山伊坎医学院 | Wd40重复结构域蛋白5(wdr5)降解/破坏化合物和使用方法 |
| US20230070613A1 (en) * | 2018-07-05 | 2023-03-09 | Icahn School Of Medicine At Mount Sinai | Protein tyrosine kinase 6 (ptk6) degradation / disruption compounds and methods of use |
| US20210340140A1 (en) * | 2018-07-23 | 2021-11-04 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use |
| JP7297053B2 (ja) | 2018-08-20 | 2023-06-23 | アルビナス・オペレーションズ・インコーポレイテッド | 神経変性疾患を治療するためのｅ３ユビキチンリガーゼ結合活性を有するキメラ（ｐｒｏｔａｃ）化合物を標的とし、アルファ－シヌクレインタンパク質を標的とするタンパク質分解 |
| EP3873906A4 (en) * | 2018-11-02 | 2022-07-27 | The Wistar Institute of Anatomy and Biology | PROTEOLYSIS-TARGETED CHIMERAS |
| AU2019381688A1 (en) | 2018-11-13 | 2021-06-03 | Biotheryx, Inc. | Substituted isoindolinones |
| EP3941607A1 (en) | 2019-03-21 | 2022-01-26 | Codiak BioSciences, Inc. | Process for preparing extracellular vesicles |
| CN113747925A (zh) | 2019-03-21 | 2021-12-03 | 科迪亚克生物科学公司 | 胞外囊泡缀合物及其用途 |
| WO2020206137A1 (en) | 2019-04-04 | 2020-10-08 | Dana-Farber Cancer Institute, Inc. | Cdk2/5 degraders and uses thereof |
| CN113645972A (zh) * | 2019-04-09 | 2021-11-12 | 达纳-法伯癌症研究所有限公司 | 通过atp-竞争性akt抑制剂gdc-0068与e3连接酶配体的接合降解akt及使用方法 |
| JP2022529700A (ja) * | 2019-04-23 | 2022-06-23 | 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 | サイクリン依存性キナーゼ１２（ｃｄｋ１２）の分解剤およびその使用 |
| CA3142713A1 (en) * | 2019-06-03 | 2020-12-10 | Regents Of The University Of Minnesota | Compounds that degrade kinases and uses thereof |
| TW202112767A (zh) | 2019-06-17 | 2021-04-01 | 美商佩特拉製藥公司 | 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物 |
| CN110143948B (zh) * | 2019-06-21 | 2021-05-14 | 上海博悦生物科技有限公司 | Cdk4/6抑制剂、其药物组合物、制备方法及应用 |
| TWI769382B (zh) * | 2019-06-21 | 2022-07-01 | 長庚大學 | 利博西林用於製備治療罹患磷酸二酯酶４介導疾病的患者的醫藥組合物及用途 |
| WO2021011913A1 (en) | 2019-07-17 | 2021-01-21 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
| EP4031247A1 (en) * | 2019-09-16 | 2022-07-27 | Novartis AG | Bifunctional degraders and their methods of use |
| JOP20220152A1 (ar) | 2019-12-18 | 2023-01-30 | Novartis Ag | مشتقات 3-(5- ميثوكسي -1- أوكسو أيزو إندولين -2- يل) بيبريدين -2، 6- دايون واستخداماتها |
| 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 |
| TW202208381A (zh) * | 2020-05-06 | 2022-03-01 | 美商紐力克斯醫療股份有限公司 | 造血前驅細胞激酶之雙官能降解劑及其治療用途 |
| WO2021237100A1 (en) | 2020-05-21 | 2021-11-25 | Codiak Biosciences, Inc. | Methods of targeting extracellular vesicles to lung |
| CN111909155B (zh) * | 2020-08-21 | 2022-10-18 | 东莞理工学院 | 蛋白水解靶向嵌合体、提高其口服生物利用度的前药分子及应用 |
| WO2022066928A2 (en) | 2020-09-23 | 2022-03-31 | Codiak Biosciences, Inc. | Process for preparing extracellular vesicles |
| CN114349738B (zh) * | 2020-10-14 | 2023-05-05 | 清华大学 | 一类靶向降解cdk2的小分子缀合物及其应用 |
| CR20230516A (es) | 2021-04-16 | 2024-01-23 | Arvinas Operations Inc | Moduladores de la proteólisis bcl6 y métodos de uso asociados |
| WO2023061440A1 (en) * | 2021-10-14 | 2023-04-20 | Cullgen (Shanghai), Inc. | Modified proteins and protein degraders |
| WO2023178130A1 (en) * | 2022-03-16 | 2023-09-21 | Biotheryx, Inc. | Sos1 protein degraders, pharmaceutical compositions, and therapeutic applications |
| TW202406904A (zh) * | 2022-04-25 | 2024-02-16 | 大陸商上海岸闊醫藥科技有限公司 | Ｃｄｋ抑制劑、醫藥組成物及其治療應用 |
| CN115364100B (zh) * | 2022-08-25 | 2023-08-29 | 杭州天玑济世生物科技有限公司 | Ly2835219作为线粒体自噬诱导剂的用途 |
| US11957759B1 (en) | 2022-09-07 | 2024-04-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use |
| WO2024083257A1 (zh) * | 2022-10-21 | 2024-04-25 | 上海领泰生物医药科技有限公司 | Sos1蛋白降解剂及其应用 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20060111716A (ko) | 2002-01-22 | 2006-10-27 | 워너-램버트 캄파니 엘엘씨 | 2-(피리딘-2-일아미노)-피리도[2,3-ｄ]피리미딘-7-온 |
| KR101353857B1 (ko) * | 2008-08-22 | 2014-01-21 | 노파르티스 아게 | Ｃｄｋ 억제제로서 피롤로피리미딘 화합물 |
| PA8852901A1 (es) | 2008-12-22 | 2010-07-27 | Lilly Co Eli | Inhibidores de proteina cinasa |
| KR20210132233A (ko) * | 2014-04-14 | 2021-11-03 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법 |
| CN105294655B (zh) * | 2014-07-26 | 2019-03-15 | 广东东阳光药业有限公司 | Cdk类小分子抑制剂的化合物及其用途 |
| WO2016040858A1 (en) * | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| WO2016040848A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors |
| 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 |
| CA3020543A1 (en) * | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 8 (cdk8) by conjugation of cdk8 inhibitors with e3 ligase ligand and methods of use |
| US20210340140A1 (en) * | 2018-07-23 | 2021-11-04 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use |
-
2017
- 2017-04-21 CA CA3018434A patent/CA3018434A1/en active Pending
- 2017-04-21 EP EP17786755.3A patent/EP3445765A4/en active Pending
- 2017-04-21 CN CN201780024853.0A patent/CN109071552B/zh active Active
- 2017-04-21 US US16/094,098 patent/US10865204B2/en active Active
- 2017-04-21 AU AU2017254708A patent/AU2017254708B2/en active Active
- 2017-04-21 WO PCT/US2017/028941 patent/WO2017185031A1/en active Application Filing
- 2017-04-21 JP JP2018555281A patent/JP6921115B2/ja active Active
