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 effect 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
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 16
- 229910052760 oxygen Inorganic materials 0.000 claims description 16
- 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
- 201000010099 disease Diseases 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
- 230000008685 targeting Effects 0.000 claims description 14
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 12
- 206010028980 Neoplasm Diseases 0.000 claims description 12
- 125000005842 heteroatom 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
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 9
- 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
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 8
- 208000030507 AIDS Diseases 0.000 claims description 7
- 108091000080 Phosphotransferase Proteins 0.000 claims description 7
- 201000011510 cancer Diseases 0.000 claims description 7
- 102000020233 phosphotransferase Human genes 0.000 claims description 7
- 206010009944 Colon cancer Diseases 0.000 claims description 6
- 206010063837 Reperfusion injury Diseases 0.000 claims description 6
- 150000001721 carbon Chemical group 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
- 208000026310 Breast neoplasm Diseases 0.000 claims description 5
- 206010025323 Lymphomas Diseases 0.000 claims description 5
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 5
- 208000029742 colonic neoplasm Diseases 0.000 claims description 5
- 230000002401 inhibitory effect Effects 0.000 claims description 5
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 5
- 201000002528 pancreatic cancer Diseases 0.000 claims description 5
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 5
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims description 4
- 206010005949 Bone cancer Diseases 0.000 claims description 4
- 208000018084 Bone neoplasm Diseases 0.000 claims description 4
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 4
- 206010006895 Cachexia Diseases 0.000 claims description 4
- 201000004624 Dermatitis Diseases 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
- 206010033128 Ovarian cancer Diseases 0.000 claims description 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 4
- 206010035664 Pneumonia Diseases 0.000 claims description 4
- 208000033826 Promyelocytic Acute Leukemia Diseases 0.000 claims description 4
- 206010060862 Prostate cancer Diseases 0.000 claims description 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 4
- 206010038389 Renal cancer Diseases 0.000 claims description 4
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 4
- 206010040047 Sepsis Diseases 0.000 claims description 4
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 4
- 125000001072 heteroaryl group Chemical group 0.000 claims description 4
- 208000032839 leukemia Diseases 0.000 claims description 4
- 201000007270 liver cancer Diseases 0.000 claims description 4
- 208000014018 liver neoplasm Diseases 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000020816 lung neoplasm 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
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 3
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 3
- 208000005440 Basal Cell Neoplasms Diseases 0.000 claims description 3
- 206010004146 Basal cell carcinoma Diseases 0.000 claims description 3
- 206010019280 Heart failures 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
- 208000015114 central nervous system disease Diseases 0.000 claims description 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 3
- 210000002919 epithelial cell Anatomy 0.000 claims description 3
- 208000028867 ischemia Diseases 0.000 claims description 3
- 230000002062 proliferating effect 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
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 206010003210 Arteriosclerosis Diseases 0.000 claims description 2
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 201000006474 Brain Ischemia Diseases 0.000 claims description 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 201000009030 Carcinoma Diseases 0.000 claims description 2
- 206010007559 Cardiac failure congestive Diseases 0.000 claims description 2
- 208000031229 Cardiomyopathies Diseases 0.000 claims description 2
- 208000024172 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
- 208000011231 Crohn disease Diseases 0.000 claims description 2
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 2
- 208000007882 Gastritis Diseases 0.000 claims description 2
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims description 2
- 201000005569 Gout Diseases 0.000 claims description 2
- 206010018634 Gouty Arthritis Diseases 0.000 claims description 2
- 208000031886 HIV Infections Diseases 0.000 claims description 2
- 208000037357 HIV infectious disease Diseases 0.000 claims description 2
- 208000016988 Hemorrhagic Stroke Diseases 0.000 claims description 2
- 208000023105 Huntington disease Diseases 0.000 claims description 2
- 206010020751 Hypersensitivity Diseases 0.000 claims description 2
- 206010061218 Inflammation Diseases 0.000 claims description 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 2
- 208000032382 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
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 206010062038 Lip neoplasm Diseases 0.000 claims description 2
- 201000009906 Meningitis Diseases 0.000 claims description 2
- 206010027476 Metastases Diseases 0.000 claims description 2
- 208000003445 Mouth Neoplasms Diseases 0.000 claims description 2
- 208000000112 Myalgia Diseases 0.000 claims description 2
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims description 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
- 208000002193 Pain Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 206010037660 Pyrexia Diseases 0.000 claims description 2
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims description 2
- 206010040070 Septic Shock Diseases 0.000 claims description 2
- 208000006045 Spondylarthropathies Diseases 0.000 claims description 2
- 208000000102 Squamous Cell Carcinoma of Head and Neck 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
- 208000025865 Ulcer Diseases 0.000 claims description 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 208000009956 adenocarcinoma Diseases 0.000 claims description 2
- 208000011341 adult acute respiratory distress syndrome Diseases 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
- 208000026935 allergic disease Diseases 0.000 claims description 2
- 230000007815 allergy Effects 0.000 claims description 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 2
- 208000011775 arteriosclerosis disease Diseases 0.000 claims description 2
- 206010003246 arthritis Diseases 0.000 claims description 2
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 208000006673 asthma Diseases 0.000 claims description 2
- 208000010668 atopic eczema Diseases 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 210000004027 cell Anatomy 0.000 claims description 2
- 206010008118 cerebral infarction Diseases 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 230000001684 chronic effect Effects 0.000 claims description 2
- 229910052805 deuterium Inorganic materials 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 201000004101 esophageal cancer Diseases 0.000 claims description 2
- 230000002496 gastric effect Effects 0.000 claims description 2
- 201000005917 gastric ulcer Diseases 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims description 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 2
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims description 2
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 230000004054 inflammatory process Effects 0.000 claims description 2
- 206010022000 influenza Diseases 0.000 claims description 2
- 208000020658 intracerebral hemorrhage Diseases 0.000 claims description 2
- 208000002551 irritable bowel syndrome 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
- 230000009401 metastasis Effects 0.000 claims description 2
- 125000002950 monocyclic group Chemical group 0.000 claims description 2
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 2
- 208000010125 myocardial infarction Diseases 0.000 claims description 2
- 201000008383 nephritis Diseases 0.000 claims description 2
- 208000004296 neuralgia Diseases 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- 230000003959 neuroinflammation Effects 0.000 claims description 2
- 208000021722 neuropathic pain Diseases 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims description 2
- 201000008482 osteoarthritis Diseases 0.000 claims description 2
- 230000036407 pain Effects 0.000 claims description 2
- 230000002685 pulmonary effect Effects 0.000 claims description 2
- 201000003651 pulmonary sarcoidosis Diseases 0.000 claims description 2
- 201000010174 renal carcinoma Diseases 0.000 claims description 2
- 208000037803 restenosis Diseases 0.000 claims description 2
- 206010039073 rheumatoid arthritis 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
- 208000020431 spinal cord injury Diseases 0.000 claims description 2
- 201000005671 spondyloarthropathy Diseases 0.000 claims description 2
- 206010041823 squamous cell carcinoma Diseases 0.000 claims description 2
- 208000017572 squamous cell neoplasm Diseases 0.000 claims description 2
- 208000024891 symptom Diseases 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 208000019693 Lung disease Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000034189 Sclerosis Diseases 0.000 claims 1
- 210000004204 blood vessel Anatomy 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 208000035269 cancer or benign tumor Diseases 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000013465 muscle pain Diseases 0.000 claims 1
- 210000004788 neurological cell Anatomy 0.000 claims 1
- 230000000926 neurological effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 14
- 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
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 description 2
- 208000015181 infectious disease Diseases 0.000 description 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 description 1
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 208000021866 Dressler syndrome Diseases 0.000 description 1
- 208000032612 Glial tumor Diseases 0.000 description 1
- 206010018338 Glioma Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 206010061523 Lip and/or oral cavity cancer Diseases 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
- 201000010001 Silicosis Diseases 0.000 description 1
- 206010069363 Traumatic lung injury Diseases 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- 230000033115 angiogenesis Effects 0.000 description 1
- 230000001640 apoptogenic effect Effects 0.000 description 1
- 230000002917 arthritic effect Effects 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 208000019664 bone resorption disease Diseases 0.000 description 1
- 210000004351 coronary vessel Anatomy 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 208000024908 graft versus host disease Diseases 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 210000004185 liver Anatomy 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
- 230000009826 neoplastic cell growth Effects 0.000 description 1
- 230000008816 organ damage Effects 0.000 description 1
- 208000033808 peripheral neuropathy Diseases 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 241001529453 unidentified herpesvirus Species 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 230000003612 virological effect 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 (OSRAM) | 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)
| Country | Link |
|---|---|
| US (1) | US10865204B2 (OSRAM) |
| EP (1) | EP3445765A4 (OSRAM) |
| JP (1) | JP6921115B2 (OSRAM) |
| CN (1) | CN109071552B (OSRAM) |
| AU (1) | AU2017254708B2 (OSRAM) |
| CA (1) | CA3018434A1 (OSRAM) |
| WO (1) | WO2017185031A1 (OSRAM) |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017185023A1 (en) * | 2016-04-22 | 2017-10-26 | 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 |
| KR20250044800A (ko) | 2016-10-11 | 2025-04-01 | 아비나스 오퍼레이션스, 인코포레이티드 | 안드로겐 수용체의 표적 분해용 화합물 및 방법 |
| EP3532464A4 (en) | 2016-10-28 | 2020-07-08 | Icahn School of Medicine at Mount Sinai | COMPOSITIONS AND METHODS FOR THE TREATMENT OF EZH2 MEDIATION CANCER |
| AU2017370694A1 (en) * | 2016-12-08 | 2019-07-25 | Icahn School Of Medicine At Mount Sinai | Compositions and methods for treating CDK4/6-mediated cancer |
| 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 |
| MX2020006587A (es) | 2017-12-22 | 2020-12-10 | Ravenna Pharmaceuticals Inc | Derivados de aminopiridina como inhibidores de fosfatidilinositol fosfato cinasa. |
| WO2019160890A1 (en) | 2018-02-13 | 2019-08-22 | Dana-Farber Cancer Institute, Inc. | Cyclin-dependent kinase degraders and methods of use |
| AU2019220746A1 (en) | 2018-02-15 | 2020-08-27 | Nuvation Bio Inc. | Heterocyclic compounds as kinase inhibitors |
| WO2019165189A1 (en) * | 2018-02-22 | 2019-08-29 | Icahn School Of Medicine At Mount Sinai | Protein arginine methyltransferase 5 (prmt5) degradation / disruption compounds and methods of use |
| AU2019231689A1 (en) * | 2018-03-06 | 2020-09-24 | Icahn School Of Medicine At Mount Sinai | Serine threonine kinase (AKT) degradation / disruption compounds and methods of use |
| CN111936498B (zh) | 2018-03-26 | 2024-04-16 | 诺华股份有限公司 | N-(3-(7H-吡咯并[2,3-d]嘧啶-4-基)苯基)苯甲酰胺衍生物 |
| WO2019196812A1 (zh) * | 2018-04-09 | 2019-10-17 | 上海科技大学 | 蛋白降解靶向化合物、其抗肿瘤应用、其中间体及中间体应用 |
| CA3104298A1 (en) * | 2018-06-21 | 2019-12-26 | Icahn School Of Medicine At Mount Sinai | Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use |
| 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 |
| AU2019309909A1 (en) * | 2018-07-23 | 2021-02-04 | 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 |
| CN112912376A (zh) | 2018-08-20 | 2021-06-04 | 阿尔维纳斯运营股份有限公司 | 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物 |
| WO2020092662A1 (en) * | 2018-11-02 | 2020-05-07 | The Wistar Institute Of Anatomy And Biology | Proteolysis-targeting chimeras |
| CA3119343C (en) | 2018-11-13 | 2024-01-16 | Biotheryx, Inc. | Substituted isoindolinones |
| US12233356B2 (en) | 2019-03-21 | 2025-02-25 | Lonza Sales Ag | Process for preparing extracellular vesicles |
| JP2022525924A (ja) | 2019-03-21 | 2022-05-20 | コディアック バイオサイエンシーズ, インコーポレイテッド | 細胞外小胞コンジュゲート及びその使用 |
| CN114269331A (zh) * | 2019-03-28 | 2022-04-01 | 埃萨制药股份有限公司 | 雄激素受体调节剂和用作蛋白水解靶向嵌合体配体的方法 |
| US12466809B2 (en) * | 2019-04-04 | 2025-11-11 | Dana-Farber Cancer Institute, Inc. | CDK2/5 degraders and uses thereof |
| US20220226481A1 (en) * | 2019-04-09 | 2022-07-21 | Dana-Farber Cancer Institute, Inc. | Degradation of akt by conjugation of atp-competitive akt inhibitor gdc-0068 with e3 ligase ligands and methods of use |
| WO2020219650A1 (en) * | 2019-04-23 | 2020-10-29 | Dana-Farber Cancer Institute, Inc. | Degraders of cyclin-dependent kinase 12 (cdk12) and uses thereof |
| CA3137916A1 (en) | 2019-05-06 | 2020-11-12 | Ichan School Of Medicine At Mount Sinai | Heterobifunctional compounds as degraders of hpk1 |
| US20220233702A1 (en) * | 2019-06-03 | 2022-07-28 | 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 |
| 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 |
| 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 |
| CN119954801A (zh) | 2019-07-17 | 2025-05-09 | 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 |
| WO2021053495A1 (en) * | 2019-09-16 | 2021-03-25 | Novartis Ag | Bifunctional degraders and their methods of use |
| CN119019369A (zh) | 2019-10-17 | 2024-11-26 | 阿尔维纳斯运营股份有限公司 | 含有与bcl6靶向部分连接的e3泛素连接酶结合部分的双官能分子 |
| AU2020410514A1 (en) | 2019-12-18 | 2022-06-30 | Novartis Ag | 3-(5-methoxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| US20230158152A1 (en) * | 2020-03-17 | 2023-05-25 | Medshine Discovery Inc. | Proteolysis regulator and method for using same |
| KR20230008176A (ko) * | 2020-05-06 | 2023-01-13 | 누릭스 테라퓨틱스 인코포레이티드 | 조혈 전구세포 키나아제의 이작용성 분해제 및 이의 치료적 용도 |
| EP4146642A1 (en) | 2020-05-09 | 2023-03-15 | Arvinas Operations, Inc. | Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same |
| WO2021237100A1 (en) | 2020-05-21 | 2021-11-25 | Codiak Biosciences, Inc. | Methods of targeting extracellular vesicles to lung |
| US12103924B2 (en) | 2020-06-01 | 2024-10-01 | Icahn School Of Medicine At Mount Sinai | Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use |
| 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 |
| JP2023539663A (ja) | 2020-08-28 | 2023-09-15 | アルビナス・オペレーションズ・インコーポレイテッド | 急速進行性線維肉腫タンパク質分解化合物及び関連する使用方法 |
| US20240241020A1 (en) | 2020-09-23 | 2024-07-18 | Lonza Sales Ag | 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 |
| CA3200608A1 (en) * | 2020-12-09 | 2022-06-16 | Xiaozhang Zheng | Irak degraders and uses thereof |
| WO2022221673A1 (en) | 2021-04-16 | 2022-10-20 | Arvinas Operations, Inc. | Modulators of bcl6 proteolysis and associated methods of use |
| AU2022284366A1 (en) | 2021-06-03 | 2023-10-26 | Novartis Ag | 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and medical uses thereof |
| WO2023061440A1 (en) * | 2021-10-14 | 2023-04-20 | Cullgen (Shanghai), Inc. | Modified proteins and protein degraders |
| US20250186434A1 (en) * | 2022-03-16 | 2025-06-12 | Biotheryx, Inc. | Sos1 protein degraders, pharmaceutical compositions thereof, and their 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 |
| WO2024054591A1 (en) | 2022-09-07 | 2024-03-14 | 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 |
| WO2024183798A1 (en) * | 2023-03-07 | 2024-09-12 | Cullgen Inc. | Compounds and methods of treating cancers |
| US12496301B2 (en) | 2023-12-08 | 2025-12-16 | Arvinas Operations, Inc. | Use of androgen receptor degrader for the treatment of spinal and bulbar muscular atrophy |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL218692B1 (pl) * | 2002-01-22 | 2015-01-30 | Warner Lambert Co | Podstawiony 2-(pirydyn-2-yloamino)pirydo[2,3-d]pirymidyn-7-on oraz jego zastosowanie do leczenia zaburzenia lub stanu spowodowanego nieprawidłową proliferacją komórek |
| BRPI0917791B1 (pt) * | 2008-08-22 | 2022-03-22 | Novartis Ag | Compostos de pirrolopirimidina como inibidores de cdk, bem como composição farmacêutica e combinação |
| JO2885B1 (en) * | 2008-12-22 | 2015-03-15 | ايلي ليلي اند كومباني | Protein kinase inhibitors |
| KR20250127179A (ko) * | 2014-04-14 | 2025-08-26 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해의 이미드-기초된 조절인자 및 연관된 이용 방법 |
| WO2016015604A1 (en) | 2014-07-26 | 2016-02-04 | Sunshine Lake Pharma Co., Ltd. | Compounds as cdk small-molecule inhibitors and uses thereof |
| 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 |
| WO2016040858A1 (en) * | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| WO2016105518A1 (en) * | 2014-12-23 | 2016-06-30 | Dana-Farber Cancer Institute, Inc. | Methods to induce targeted protein degradation through bifunctional molecules |
| US10865205B2 (en) * | 2016-04-22 | 2020-12-15 | 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 |
| AU2019309909A1 (en) * | 2018-07-23 | 2021-02-04 | 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 AU AU2017254708A patent/AU2017254708B2/en active Active
- 2017-04-21 EP EP17786755.3A patent/EP3445765A4/en active Pending
- 2017-04-21 US US16/094,098 patent/US10865204B2/en active Active
- 2017-04-21 CA CA3018434A patent/CA3018434A1/en active Pending
- 2017-04-21 CN CN201780024853.0A patent/CN109071552B/zh active Active
- 2017-04-21 WO PCT/US2017/028941 patent/WO2017185031A1/en not_active Ceased
- 2017-04-21 JP JP2018555281A patent/JP6921115B2/ja active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2019514883A5 (OSRAM) | ||
| JP2019514882A5 (OSRAM) | ||
| JP2019514876A5 (OSRAM) | ||
| JP2019519476A5 (OSRAM) | ||
| JP2016523973A5 (OSRAM) | ||
| KR102093608B1 (ko) | 이미다조피리딘 화합물 | |
| JP2019535744A5 (OSRAM) | ||
| JP7371221B2 (ja) | Irak4キナーゼ阻害剤及びその調製方法 | |
| JP2019535746A5 (OSRAM) | ||
| JP6592512B2 (ja) | 三環式アトロプ異性体の化合物 | |
| EP3013815B1 (en) | Carbazole carboxamide compounds useful as kinase inhibitors | |
| JP2016053042A5 (OSRAM) | ||
| JP2014193925A5 (OSRAM) | ||
| JP2019524883A5 (OSRAM) | ||
| JP2014503567A5 (OSRAM) | ||
| JP2018515490A5 (OSRAM) | ||
| JP2013525363A5 (OSRAM) | ||
| JP2019510801A5 (OSRAM) | ||
| JP2010509284A5 (OSRAM) | ||
| JP2020525512A (ja) | 癌および他の疾患を処置するためのATF4阻害剤としての2−(4−クロロフェノキシ)−N−((1−(2−(4−クロロフェノキシ)エチンアゼチジン(ethynazetidin)−3−イル)メチル)アセトアミド誘導体および関連化合物 | |
| JP2018527412A (ja) | Perk阻害剤としての1−フェニルピロリジン−2−オン誘導体 | |
| KR102142797B1 (ko) | 피리디닐아미노피리미딘 유도체의 메실레이트 염의 결정질 형태, 그의 제조 방법, 및 그의 용도 | |
| JP2017534653A (ja) | ブロモドメイン及びエキストラ末端タンパク質の阻害のための方法及び組成物 | |
| JP2014520153A5 (OSRAM) | ||
| CN114026068A (zh) | Ep2拮抗剂 |