JP2017504650A5 - - Google Patents
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- JP2017504650A5 JP2017504650A5 JP2016549416A JP2016549416A JP2017504650A5 JP 2017504650 A5 JP2017504650 A5 JP 2017504650A5 JP 2016549416 A JP2016549416 A JP 2016549416A JP 2016549416 A JP2016549416 A JP 2016549416A JP 2017504650 A5 JP2017504650 A5 JP 2017504650A5
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- Prior art keywords
- substituted
- unsubstituted
- disease
- alkyl
- protecting group
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 54
- 229910052739 hydrogen Inorganic materials 0.000 claims 51
- 239000001257 hydrogen Substances 0.000 claims 51
- 150000002431 hydrogen Chemical class 0.000 claims 51
- 125000001072 heteroaryl group Chemical group 0.000 claims 47
- 125000000623 heterocyclic group Chemical group 0.000 claims 47
- 150000003839 salts Chemical class 0.000 claims 45
- 201000010099 disease Diseases 0.000 claims 41
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 41
- 125000003342 alkenyl group Chemical group 0.000 claims 34
- 125000000304 alkynyl group Chemical group 0.000 claims 34
- 125000003118 aryl group Chemical group 0.000 claims 34
- 125000004452 carbocyclyl group Chemical group 0.000 claims 34
- 150000001875 compounds Chemical class 0.000 claims 30
- 229910052736 halogen Inorganic materials 0.000 claims 25
- 150000002367 halogens Chemical group 0.000 claims 25
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 24
- 229910052757 nitrogen Inorganic materials 0.000 claims 22
- 125000002252 acyl group Chemical group 0.000 claims 18
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 18
- 102000001805 Bromodomains Human genes 0.000 claims 17
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 17
- 238000000034 method Methods 0.000 claims 15
- 108090000623 proteins and genes Proteins 0.000 claims 14
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 13
- 239000008194 pharmaceutical composition Substances 0.000 claims 13
- 229910052717 sulfur Inorganic materials 0.000 claims 13
- 125000004430 oxygen atom Chemical group O* 0.000 claims 12
- 108091005575 Bromodomain-containing proteins Proteins 0.000 claims 11
- 102000004169 proteins and genes Human genes 0.000 claims 11
- 125000004434 sulfur atom Chemical group 0.000 claims 11
- 230000000694 effects Effects 0.000 claims 9
- 208000015181 infectious disease Diseases 0.000 claims 8
- 108050009021 Bromodomains Proteins 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 239000001301 oxygen Substances 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 208000030507 AIDS Diseases 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 4
- 241000711549 Hepacivirus C Species 0.000 claims 4
- 241000725303 Human immunodeficiency virus Species 0.000 claims 4
- 201000003176 Severe Acute Respiratory Syndrome Diseases 0.000 claims 4
- 230000002159 abnormal effect Effects 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 208000024908 graft versus host disease Diseases 0.000 claims 4
- 125000006239 protecting group Chemical group 0.000 claims 4
- 201000001320 Atherosclerosis Diseases 0.000 claims 3
- 241000701806 Human papillomavirus Species 0.000 claims 3
- VEYYWZRYIYDQJM-ZETCQYMHSA-N N(2)-acetyl-L-lysine Chemical group CC(=O)N[C@H](C([O-])=O)CCCC[NH3+] VEYYWZRYIYDQJM-ZETCQYMHSA-N 0.000 claims 3
- 241000700584 Simplexvirus Species 0.000 claims 3
- 125000002837 carbocyclic group Chemical group 0.000 claims 3
- 238000000338 in vitro Methods 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 230000001105 regulatory effect Effects 0.000 claims 3
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 206010060999 Benign neoplasm Diseases 0.000 claims 2
- 102100033641 Bromodomain-containing protein 2 Human genes 0.000 claims 2
- 101710126816 Bromodomain-containing protein 2 Proteins 0.000 claims 2
- 102100033642 Bromodomain-containing protein 3 Human genes 0.000 claims 2
- 101710126814 Bromodomain-containing protein 3 Proteins 0.000 claims 2
- 102100029895 Bromodomain-containing protein 4 Human genes 0.000 claims 2
- 101710126815 Bromodomain-containing protein 4 Proteins 0.000 claims 2
- 108010040163 CREB-Binding Protein Proteins 0.000 claims 2
- 102100021975 CREB-binding protein Human genes 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 201000011001 Ebola Hemorrhagic Fever Diseases 0.000 claims 2
- 208000017701 Endocrine disease Diseases 0.000 claims 2
- 102100038885 Histone acetyltransferase p300 Human genes 0.000 claims 2
- 108010033040 Histones Proteins 0.000 claims 2
- 101000882390 Homo sapiens Histone acetyltransferase p300 Proteins 0.000 claims 2
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 206010029260 Neuroblastoma Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 208000034038 Pathologic Neovascularization Diseases 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 206010039710 Scleroderma Diseases 0.000 claims 2
- 206010040047 Sepsis Diseases 0.000 claims 2
- 102000006467 TATA-Box Binding Protein Human genes 0.000 claims 2
- 108010044281 TATA-Box Binding Protein Proteins 0.000 claims 2
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 2
- 206010057644 Testis cancer Diseases 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000001246 bromo group Chemical group Br* 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 208000016097 disease of metabolism Diseases 0.000 claims 2
- 208000030172 endocrine system disease Diseases 0.000 claims 2
- 230000003176 fibrotic effect Effects 0.000 claims 2
- 208000004104 gestational diabetes Diseases 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 206010022000 influenza Diseases 0.000 claims 2
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000030159 metabolic disease Diseases 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 102000020233 phosphotransferase Human genes 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 230000005855 radiation Effects 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 239000011593 sulfur Substances 0.000 claims 2
- 201000003120 testicular cancer Diseases 0.000 claims 2
- 231100000419 toxicity Toxicity 0.000 claims 2
- 230000001988 toxicity Effects 0.000 claims 2
- 238000013518 transcription Methods 0.000 claims 2
- 230000035897 transcription Effects 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 208000037260 Atherosclerotic Plaque Diseases 0.000 claims 1
- 101000596093 Homo sapiens Transcription initiation factor TFIID subunit 1 Proteins 0.000 claims 1
- 101000596092 Homo sapiens Transcription initiation factor TFIID subunit 1-like Proteins 0.000 claims 1
- 241000726306 Irus Species 0.000 claims 1
- 102100035222 Transcription initiation factor TFIID subunit 1 Human genes 0.000 claims 1
- 102100035238 Transcription initiation factor TFIID subunit 1-like Human genes 0.000 claims 1
- 230000036523 atherogenesis Effects 0.000 claims 1
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 1
- 208000003154 papilloma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 241001529453 unidentified herpesvirus Species 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461934668P | 2014-01-31 | 2014-01-31 | |
| US61/934,668 | 2014-01-31 | ||
| PCT/US2015/014109 WO2015117083A1 (en) | 2014-01-31 | 2015-02-02 | Diazepane derivatives and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017504650A JP2017504650A (ja) | 2017-02-09 |
| JP2017504650A5 true JP2017504650A5 (OSRAM) | 2018-08-30 |
Family
ID=53757810
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016549416A Pending JP2017504650A (ja) | 2014-01-31 | 2015-02-02 | ジアゼパン誘導体およびその使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9695172B2 (OSRAM) |
| EP (1) | EP3099696A4 (OSRAM) |
| JP (1) | JP2017504650A (OSRAM) |
| KR (1) | KR20160111036A (OSRAM) |
| CN (1) | CN105940005A (OSRAM) |
| BR (1) | BR112016017045A2 (OSRAM) |
| CA (1) | CA2936256A1 (OSRAM) |
| HK (1) | HK1225383A1 (OSRAM) |
| MX (1) | MX2016009976A (OSRAM) |
| RU (1) | RU2016134941A (OSRAM) |
| WO (1) | WO2015117083A1 (OSRAM) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CA2784807C (en) | 2009-12-29 | 2021-12-14 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
| HUE031073T2 (en) | 2010-05-14 | 2017-06-28 | Dana Farber Cancer Inst Inc | Thieno triazolo-diazepine compounds for the treatment of neoplasia |
| WO2011143657A1 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Male contraceptive compositions and methods of use |
| CA2799403C (en) | 2010-05-14 | 2020-01-21 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for treating leukemia |
| WO2013074986A1 (en) | 2011-11-17 | 2013-05-23 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| US10112927B2 (en) | 2012-10-18 | 2018-10-30 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| US9758522B2 (en) | 2012-10-19 | 2017-09-12 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| US10000483B2 (en) | 2012-10-19 | 2018-06-19 | Dana-Farber Cancer Institute, Inc. | Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof |
| KR20160034379A (ko) | 2013-07-25 | 2016-03-29 | 다나-파버 캔서 인스티튜트 인크. | 전사 인자의 억제제 및 그의 용도 |
| CA2927917C (en) | 2013-10-18 | 2022-08-09 | Syros Pharmaceuticals, Inc. | Heteroaromatic compounds useful for the treatment of proliferative diseases |
| JP6491202B2 (ja) | 2013-10-18 | 2019-03-27 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | サイクリン依存性キナーゼ７（ｃｄｋ７）の多環阻害剤 |
| RU2016122654A (ru) | 2013-11-08 | 2017-12-14 | Дана-Фарбер Кэнсер Инститьют, Инк. | Комбинированная терапия злокачественной опухоли с использованием ингибиторов бромодоменового и экстратерминального (вет) белка |
| US10150756B2 (en) | 2014-01-31 | 2018-12-11 | Dana-Farber Cancer Institute, Inc. | Diaminopyrimidine benzenesulfone derivatives and uses thereof |
| US10793571B2 (en) | 2014-01-31 | 2020-10-06 | Dana-Farber Cancer Institute, Inc. | Uses of diazepane derivatives |
| CA2940472A1 (en) | 2014-02-28 | 2015-09-03 | Tensha Therapeutics, Inc. | Treatment of conditions associated with hyperinsulinaemia |
| US10017477B2 (en) | 2014-04-23 | 2018-07-10 | Dana-Farber Cancer Institute, Inc. | Janus kinase inhibitors and uses thereof |
| US9862688B2 (en) | 2014-04-23 | 2018-01-09 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged janus kinase inhibitors and uses thereof |
| EP3177147A4 (en) | 2014-08-08 | 2018-01-24 | Dana-Farber Cancer Institute, Inc. | Dihydropteridinone derivatives and uses thereof |
| RU2017104897A (ru) | 2014-08-08 | 2018-09-10 | Дана-Фарбер Кэнсер Инститьют, Инк. | Производные диазепана и их применения |
| EA033325B1 (ru) | 2014-10-27 | 2019-09-30 | Тэнша Терапеутикс, Инк. | Ингибиторы бромодомена |
| EP3236959B1 (en) | 2014-12-23 | 2025-09-24 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| CA2978518C (en) | 2015-03-27 | 2023-11-21 | Nathanael S. Gray | Inhibitors of cyclin-dependent kinases |
| CA2986441A1 (en) | 2015-06-12 | 2016-12-15 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| JP7028766B2 (ja) | 2015-09-09 | 2022-03-02 | 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の阻害剤 |
| KR20180051576A (ko) | 2015-09-11 | 2018-05-16 | 다나-파버 캔서 인스티튜트 인크. | 아세트아미드 티에노트리아졸로디아제핀 및 그의 용도 |
| CN108472300A (zh) | 2015-09-11 | 2018-08-31 | 达纳-法伯癌症研究所股份有限公司 | 氰基噻吩并三唑并二氮杂环庚三烯及其用途 |
| PE20181298A1 (es) | 2015-11-25 | 2018-08-07 | Dana Farber Cancer Inst Inc | Inhibidores de bromodominio bivalentes y usos de los mismos |
| AU2017346845B2 (en) * | 2016-10-18 | 2021-12-02 | Dana-Farber Cancer Institute, Inc. | Pyrimido-diazepinone kinase scaffold compounds and methods of treating DCLK1/2-mediated disorders |
| RU2664331C1 (ru) * | 2017-10-23 | 2018-08-16 | Федеральное государственное бюджетное учреждение науки Новосибирский институт органической химии им. Н.Н. Ворожцова Сибирского отделения Российской академии наук (НИОХ СО РАН) | 6,13,13-ТРИМЕТИЛ-6,8,9,12-ТЕТРАГИДРО-6,9-МЕТАНОАЗЕПИНО[2,1-b]ХИНАЗОЛИН-10(7Н)-ОН В КАЧЕСТВЕ ИНГИБИТОРА ВИРУСОВ ГРИППА А |
| US11110177B2 (en) * | 2017-11-10 | 2021-09-07 | The Regents Of The University Of Michigan | ASH1L degraders and methods of treatment therewith |
| WO2020005807A1 (en) | 2018-06-25 | 2020-01-02 | Dana-Farber Cancer Institute, Inc. | Taire family kinase inhibitors and uses thereof |
| WO2020093162A1 (en) * | 2018-11-07 | 2020-05-14 | Neomed Institute | Treatment of bet inhibitor-resistant cancers and other diseases responsive to dual bet and cbp/ep300 inhibition therapy |
| GB202202199D0 (en) * | 2022-02-18 | 2022-04-06 | Cancer Research Tech Ltd | Compounds |
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-
2015
- 2015-02-02 KR KR1020167023460A patent/KR20160111036A/ko not_active Withdrawn
- 2015-02-02 CA CA2936256A patent/CA2936256A1/en not_active Abandoned
- 2015-02-02 HK HK16113707.9A patent/HK1225383A1/zh unknown
- 2015-02-02 CN CN201580006614.3A patent/CN105940005A/zh active Pending
- 2015-02-02 JP JP2016549416A patent/JP2017504650A/ja active Pending
- 2015-02-02 EP EP15744026.4A patent/EP3099696A4/en not_active Ceased
- 2015-02-02 WO PCT/US2015/014109 patent/WO2015117083A1/en not_active Ceased
- 2015-02-02 RU RU2016134941A patent/RU2016134941A/ru not_active Application Discontinuation
- 2015-02-02 BR BR112016017045A patent/BR112016017045A2/pt active Search and Examination
- 2015-02-02 MX MX2016009976A patent/MX2016009976A/es unknown
- 2015-02-02 US US15/114,895 patent/US9695172B2/en active Active