JP2019510801A5 - - Google Patents
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- JP2019510801A5 JP2019510801A5 JP2018552857A JP2018552857A JP2019510801A5 JP 2019510801 A5 JP2019510801 A5 JP 2019510801A5 JP 2018552857 A JP2018552857 A JP 2018552857A JP 2018552857 A JP2018552857 A JP 2018552857A JP 2019510801 A5 JP2019510801 A5 JP 2019510801A5
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- Prior art keywords
- alkyl
- optionally substituted
- hydrogen
- formula
- aryl
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims 47
- 229910052739 hydrogen Inorganic materials 0.000 claims 44
- 239000001257 hydrogen Substances 0.000 claims 44
- 125000000547 substituted alkyl group Chemical group 0.000 claims 32
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 29
- 125000003118 aryl group Chemical group 0.000 claims 25
- 125000000623 heterocyclic group Chemical group 0.000 claims 22
- 150000002148 esters Chemical class 0.000 claims 20
- 239000000651 prodrug Substances 0.000 claims 20
- 229940002612 prodrug Drugs 0.000 claims 20
- 150000003839 salts Chemical class 0.000 claims 20
- 150000002431 hydrogen Chemical class 0.000 claims 15
- 125000001072 heteroaryl group Chemical group 0.000 claims 13
- 125000003710 aryl alkyl group Chemical group 0.000 claims 12
- 125000002837 carbocyclic group Chemical group 0.000 claims 12
- 125000003342 alkenyl group Chemical group 0.000 claims 11
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 108030003690 Phosphatidylinositol-4,5-bisphosphate 3-kinases Proteins 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 6
- 125000004429 atom Chemical group 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 208000030507 AIDS Diseases 0.000 claims 3
- 206010063837 Reperfusion injury Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 208000028867 ischemia Diseases 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims 2
- 101100459319 Arabidopsis thaliana VIII-2 gene Proteins 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
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- 201000004624 Dermatitis Diseases 0.000 claims 2
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- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 206010035664 Pneumonia Diseases 0.000 claims 2
- 208000033826 Promyelocytic Acute Leukemia Diseases 0.000 claims 2
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 2
- 206010040047 Sepsis Diseases 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 2
- 230000000747 cardiac effect Effects 0.000 claims 2
- 208000015114 central nervous system disease Diseases 0.000 claims 2
- 201000003444 follicular lymphoma Diseases 0.000 claims 2
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- 208000011580 syndromic disease Diseases 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- KPPVNWGJXFMGAM-UUILKARUSA-N (e)-2-methyl-1-(6-methyl-3,4-dihydro-2h-quinolin-1-yl)but-2-en-1-one Chemical compound CC1=CC=C2N(C(=O)C(/C)=C/C)CCCC2=C1 KPPVNWGJXFMGAM-UUILKARUSA-N 0.000 claims 1
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
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- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 208000035143 Bacterial infection Diseases 0.000 claims 1
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 201000006474 Brain Ischemia Diseases 0.000 claims 1
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- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 241000282465 Canis Species 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000031229 Cardiomyopathies Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000007882 Gastritis Diseases 0.000 claims 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 201000005569 Gout Diseases 0.000 claims 1
- 206010018634 Gouty Arthritis Diseases 0.000 claims 1
- 208000031886 HIV Infections Diseases 0.000 claims 1
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- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 206010062038 Lip neoplasm Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 201000009906 Meningitis Diseases 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 208000003445 Mouth Neoplasms Diseases 0.000 claims 1
- 208000000112 Myalgia Diseases 0.000 claims 1
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
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- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010037660 Pyrexia Diseases 0.000 claims 1
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- 206010040070 Septic Shock Diseases 0.000 claims 1
- 201000010001 Silicosis Diseases 0.000 claims 1
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- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000006045 Spondylarthropathies Diseases 0.000 claims 1
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000007107 Stomach Ulcer Diseases 0.000 claims 1
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical group C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 208000025865 Ulcer Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 208000009956 adenocarcinoma Diseases 0.000 claims 1
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 1
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 230000003110 anti-inflammatory effect Effects 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 230000001640 apoptogenic effect Effects 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
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- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 208000019664 bone resorption disease Diseases 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 206010008118 cerebral infarction Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 210000004351 coronary vessel Anatomy 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 210000002919 epithelial cell Anatomy 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- 201000005917 gastric ulcer Diseases 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 206010022000 influenza Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
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- 210000003734 kidney Anatomy 0.000 claims 1
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- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 201000004792 malaria Diseases 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- LOTBYPQQWICYBB-UHFFFAOYSA-N methyl n-hexyl-n-[2-(hexylamino)ethyl]carbamate Chemical group CCCCCCNCCN(C(=O)OC)CCCCCC LOTBYPQQWICYBB-UHFFFAOYSA-N 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 230000009826 neoplastic cell growth Effects 0.000 claims 1
- 230000001613 neoplastic effect Effects 0.000 claims 1
- 201000008383 nephritis Diseases 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 230000003959 neuroinflammation Effects 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 230000008816 organ damage Effects 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 201000010279 papillary renal cell carcinoma Diseases 0.000 claims 1
- 230000007170 pathology Effects 0.000 claims 1
- 210000000578 peripheral nerve Anatomy 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 230000002685 pulmonary effect Effects 0.000 claims 1
- 201000003651 pulmonary sarcoidosis Diseases 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 208000020352 skin basal cell carcinoma Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 201000010106 skin squamous cell carcinoma Diseases 0.000 claims 1
- 201000002314 small intestine cancer Diseases 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- 241001529453 unidentified herpesvirus Species 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
- 0 *c1nc(*)nc(N(C2CCCC2)C2C3CCC2)c1N(*)C3=O Chemical compound *c1nc(*)nc(N(C2CCCC2)C2C3CCC2)c1N(*)C3=O 0.000 description 3
- UZEKOJOSBVTNSU-UHFFFAOYSA-N CC(C)c1cccc(S(Nc(cc2)ccc2NC(C=C)=O)(=O)=O)c1 Chemical compound CC(C)c1cccc(S(Nc(cc2)ccc2NC(C=C)=O)(=O)=O)c1 UZEKOJOSBVTNSU-UHFFFAOYSA-N 0.000 description 2
- BWAXSJKHZWUQQZ-UHFFFAOYSA-N CCC(N(CC1)CCN1S(c1cc(C)ccc1)(=O)=O)=O Chemical compound CCC(N(CC1)CCN1S(c1cc(C)ccc1)(=O)=O)=O BWAXSJKHZWUQQZ-UHFFFAOYSA-N 0.000 description 2
- BWXKCOZXTDTDMP-UHFFFAOYSA-N Cc1cccc(S(N(CC2)CCC2NC(C=C)=O)(=O)=O)c1 Chemical compound Cc1cccc(S(N(CC2)CCC2NC(C=C)=O)(=O)=O)c1 BWXKCOZXTDTDMP-UHFFFAOYSA-N 0.000 description 2
- BIPZVWKVPTVORW-UHFFFAOYSA-N Cc1cccc(S(N(CC2)CCC2O)(=O)=O)c1 Chemical compound Cc1cccc(S(N(CC2)CCC2O)(=O)=O)c1 BIPZVWKVPTVORW-UHFFFAOYSA-N 0.000 description 2
- ODUZJPLGAILSDK-UHFFFAOYSA-N Cc1cccc(S(N(CC2)CCN2C(C=C)=O)(=O)=O)c1 Chemical compound Cc1cccc(S(N(CC2)CCN2C(C=C)=O)(=O)=O)c1 ODUZJPLGAILSDK-UHFFFAOYSA-N 0.000 description 2
- JZLSGOTZKRYLLY-UHFFFAOYSA-N Cc1cccc(S(N2CCN(C)CC2)(=O)=O)c1 Chemical compound Cc1cccc(S(N2CCN(C)CC2)(=O)=O)c1 JZLSGOTZKRYLLY-UHFFFAOYSA-N 0.000 description 2
- HRPVXLWXLXDGHG-UHFFFAOYSA-N Acrylamide Chemical compound NC(=O)C=C HRPVXLWXLXDGHG-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662319459P | 2016-04-07 | 2016-04-07 | |
| US62/319,459 | 2016-04-07 | ||
| PCT/US2017/026522 WO2017177092A1 (en) | 2016-04-07 | 2017-04-07 | Pyrimido-diazepinone kinase scaffold compounds and methods of treating pi3k-mediated disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019510801A JP2019510801A (ja) | 2019-04-18 |
| JP2019510801A5 true JP2019510801A5 (enExample) | 2020-05-21 |
| JP6968819B2 JP6968819B2 (ja) | 2021-11-17 |
Family
ID=60001546
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018552857A Active JP6968819B2 (ja) | 2016-04-07 | 2017-04-07 | ピリミド−ジアゼピノンキナーゼ骨格化合物およびｐｉ３ｋ媒介性障害の治療方法 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US11155556B2 (enExample) |
| EP (1) | EP3440084B1 (enExample) |
| JP (1) | JP6968819B2 (enExample) |
| KR (1) | KR20180132812A (enExample) |
| CN (1) | CN109311901A (enExample) |
| AU (1) | AU2017248186B2 (enExample) |
| WO (1) | WO2017177092A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20200390783A1 (en) * | 2018-02-20 | 2020-12-17 | Dana-Farber Cancer Institute, Inc. | Inhibitors of egfr and methods of use thereof |
| EP3755337A4 (en) * | 2018-02-20 | 2021-11-03 | Dana-Farber Cancer Institute, Inc. | EGFR INHIBITOR PHARMACEUTICAL COMBINATIONS AND METHODS OF USE |
| CA3087716A1 (en) * | 2018-02-20 | 2019-08-29 | Dana-Farber Cancer Institute, Inc. | Inhibitors of egfr and methods of use thereof |
| CN110787168B (zh) * | 2019-11-06 | 2022-06-24 | 中国医科大学 | 一种小分子化合物C29H28Cl2N6O在大肠杆菌性脑膜炎中的应用 |
| US12195490B2 (en) * | 2020-01-30 | 2025-01-14 | The Regents Of The University Of California | STRAD-binding agents and uses thereof |
| CN114539263B (zh) * | 2020-11-11 | 2023-04-25 | 暨南大学 | 一类含氮并杂环化合物及其药用组合物和应用 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6667300B2 (en) | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
| TW200808325A (en) * | 2006-07-06 | 2008-02-16 | Astrazeneca Ab | Novel compounds |
| WO2008040951A1 (en) * | 2006-10-03 | 2008-04-10 | Astrazeneca Ab | Compounds |
| EP1953163A1 (en) * | 2007-02-01 | 2008-08-06 | Boehringer Ingelheim Pharma GmbH & Co. KG | Pteridinone derivatives as PI3-kinases inhibitors |
| EP2139892B1 (en) * | 2007-03-22 | 2011-09-14 | Takeda Pharmaceutical Company Limited | Substituted pyrimidodiazepines useful as plk1 inhibitors |
| PL2205603T3 (pl) * | 2007-09-28 | 2014-07-31 | Cyclacel Ltd | Pochodne pirymidyny jako inhibitory kinaz białkowych |
| CA2748181C (en) * | 2009-01-06 | 2019-07-16 | Nathanael S. Gray | Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders |
| US9126948B2 (en) | 2011-03-25 | 2015-09-08 | Incyte Holdings Corporation | Pyrimidine-4,6-diamine derivatives as PI3K inhibitors |
| EP2970317A4 (en) * | 2013-03-15 | 2016-11-02 | Dana Farber Cancer Inst Inc | PYRIMIDODIAZEPINONE COMPOUNDS AND METHOD FOR THE TREATMENT OF DISEASES |
| JP2017504651A (ja) * | 2014-01-31 | 2017-02-09 | 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 | ジアゼパン誘導体の使用 |
| EP3307728A4 (en) * | 2015-06-12 | 2019-07-17 | Dana Farber Cancer Institute, Inc. | COMBINATION THERAPY OF TRANSCRIPTION INHIBITORS AND CHINESE INHIBITORS |
| CA3012516A1 (en) * | 2016-03-04 | 2017-09-08 | Anhui New Star Pharmaceutical Development Co., Ltd | Pyrimidine seven-membered-ring compounds, preparation method therefor, pharmaceutical composition therefor, and uses thereof |
| WO2018075608A1 (en) * | 2016-10-18 | 2018-04-26 | Dana-Farber Cancer Institute, Inc. | Pyrimido-diazepinone kinase scaffold compounds and methods of treating dclk1/2-mediated disorders |
-
2017
- 2017-04-07 EP EP17779885.7A patent/EP3440084B1/en active Active
- 2017-04-07 AU AU2017248186A patent/AU2017248186B2/en active Active
- 2017-04-07 JP JP2018552857A patent/JP6968819B2/ja active Active
- 2017-04-07 KR KR1020187031991A patent/KR20180132812A/ko not_active Ceased
- 2017-04-07 WO PCT/US2017/026522 patent/WO2017177092A1/en not_active Ceased
- 2017-04-07 US US16/090,869 patent/US11155556B2/en active Active
- 2017-04-07 CN CN201780035745.3A patent/CN109311901A/zh active Pending
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