JP2018507191A5 - - Google Patents
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- JP2018507191A5 JP2018507191A5 JP2017539592A JP2017539592A JP2018507191A5 JP 2018507191 A5 JP2018507191 A5 JP 2018507191A5 JP 2017539592 A JP2017539592 A JP 2017539592A JP 2017539592 A JP2017539592 A JP 2017539592A JP 2018507191 A5 JP2018507191 A5 JP 2018507191A5
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- JP
- Japan
- Prior art keywords
- carbocyclyl
- alkyl
- group
- independently selected
- optionally substituted
- 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.)
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- 125000004452 carbocyclyl group Chemical group 0.000 claims description 130
- 125000000217 alkyl group Chemical group 0.000 claims description 124
- 125000001475 halogen functional group Chemical group 0.000 claims description 116
- 150000001875 compounds Chemical class 0.000 claims description 94
- 125000000623 heterocyclic group Chemical group 0.000 claims description 92
- 125000004043 oxo group Chemical group O=* 0.000 claims description 62
- 150000003839 salts Chemical class 0.000 claims description 62
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 54
- 125000003545 alkoxy group Chemical group 0.000 claims description 52
- 206010028980 Neoplasm Diseases 0.000 claims description 40
- 125000000304 alkynyl group Chemical group 0.000 claims description 35
- 125000003342 alkenyl group Chemical group 0.000 claims description 32
- 102100035222 Transcription initiation factor TFIID subunit 1 Human genes 0.000 claims description 26
- 201000009030 Carcinoma Diseases 0.000 claims description 24
- 101000596093 Homo sapiens Transcription initiation factor TFIID subunit 1 Proteins 0.000 claims description 24
- 201000011510 cancer Diseases 0.000 claims description 24
- 206010039491 Sarcoma Diseases 0.000 claims description 20
- 239000000203 mixture Substances 0.000 claims description 19
- 229910052799 carbon Inorganic materials 0.000 claims description 17
- -1 R f Chemical group 0.000 claims description 15
- 229910052739 hydrogen Inorganic materials 0.000 claims description 14
- 239000003814 drug Substances 0.000 claims description 11
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 10
- 206010009944 Colon cancer Diseases 0.000 claims description 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
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- 239000001257 hydrogen Substances 0.000 claims description 10
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- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 8
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 8
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- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 8
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- 229910052757 nitrogen Inorganic materials 0.000 claims description 8
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 8
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 8
- 208000000587 small cell lung carcinoma Diseases 0.000 claims description 8
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- 125000003118 aryl group Chemical group 0.000 claims description 6
- 230000002401 inhibitory effect Effects 0.000 claims description 6
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- 208000031637 Erythroblastic Acute Leukemia Diseases 0.000 claims description 4
- 208000036566 Erythroleukaemia Diseases 0.000 claims description 4
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims description 4
- 208000006168 Ewing Sarcoma Diseases 0.000 claims description 4
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- 208000007054 Medullary Carcinoma Diseases 0.000 claims description 4
- 208000000172 Medulloblastoma Diseases 0.000 claims description 4
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- 208000008601 Polycythemia Diseases 0.000 claims description 4
- 208000009052 Precursor T-Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims description 4
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- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 4
- 201000000582 Retinoblastoma Diseases 0.000 claims description 4
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- 208000000453 Skin Neoplasms Diseases 0.000 claims description 4
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 4
- 208000029052 T-cell acute lymphoblastic leukemia Diseases 0.000 claims description 4
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- 208000014070 Vestibular schwannoma Diseases 0.000 claims description 4
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims description 4
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- 208000037828 epithelial carcinoma Diseases 0.000 claims description 4
- 201000005619 esophageal carcinoma Diseases 0.000 claims description 4
- 201000007281 estrogen-receptor positive breast cancer Diseases 0.000 claims description 4
- 230000001605 fetal effect Effects 0.000 claims description 4
- 239000000835 fiber Substances 0.000 claims description 4
- 201000003444 follicular lymphoma Diseases 0.000 claims description 4
- 206010017758 gastric cancer Diseases 0.000 claims description 4
- 210000004602 germ cell Anatomy 0.000 claims description 4
- 208000005017 glioblastoma Diseases 0.000 claims description 4
- 208000002409 gliosarcoma Diseases 0.000 claims description 4
- 201000010536 head and neck cancer Diseases 0.000 claims description 4
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 4
- 208000025750 heavy chain disease Diseases 0.000 claims description 4
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- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 4
- 239000005556 hormone Substances 0.000 claims description 4
- 229940088597 hormone Drugs 0.000 claims description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 4
- 230000005764 inhibitory process Effects 0.000 claims description 4
- 208000032839 leukemia Diseases 0.000 claims description 4
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- 208000012804 lymphangiosarcoma Diseases 0.000 claims description 4
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- 235000013372 meat Nutrition 0.000 claims description 4
- 208000023356 medullary thyroid gland carcinoma Diseases 0.000 claims description 4
- 206010027191 meningioma Diseases 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 208000025113 myeloid leukemia Diseases 0.000 claims description 4
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 4
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- 201000008026 nephroblastoma Diseases 0.000 claims description 4
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 4
- 201000008968 osteosarcoma Diseases 0.000 claims description 4
- 208000004019 papillary adenocarcinoma Diseases 0.000 claims description 4
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- 208000024724 pineal body neoplasm Diseases 0.000 claims description 4
- 230000002062 proliferating effect Effects 0.000 claims description 4
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- 201000008753 synovium neoplasm Diseases 0.000 claims description 4
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- 238000000034 method Methods 0.000 description 10
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| JP6639497B2 (ja) | 2014-11-10 | 2020-02-05 | ジェネンテック， インコーポレイテッド | ブロモドメインインヒビターおよびその使用 |
| CN109641894B (zh) * | 2016-08-24 | 2022-09-09 | 豪夫迈·罗氏有限公司 | 2-氮杂双环[3.1.0]己烷-3-酮衍生物及使用方法 |
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| US11171132B2 (en) * | 2019-10-03 | 2021-11-09 | Globalfoundries U.S. Inc. | Bi-directional breakdown silicon controlled rectifiers |
| CN112625036A (zh) * | 2019-10-08 | 2021-04-09 | 上海海和药物研究开发股份有限公司 | 一类具有brd4抑制活性的化合物、其制备方法及用途 |
| CN114591338B (zh) * | 2022-03-31 | 2023-05-09 | 苏州欧康维视生物科技有限公司 | 一种Syk和VEGFR2双靶点抑制剂的制备方法及其用途 |
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2016
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- 2016-01-28 EP EP16704984.0A patent/EP3250571B1/en active Active
- 2016-01-28 JP JP2017539592A patent/JP6709792B2/ja active Active
- 2016-01-28 WO PCT/US2016/015450 patent/WO2016123391A1/en not_active Ceased
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2017
- 2017-07-24 US US15/658,213 patent/US10202378B2/en active Active