JP2017533922A5 - - Google Patents
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- Publication number
- JP2017533922A5 JP2017533922A5 JP2017525115A JP2017525115A JP2017533922A5 JP 2017533922 A5 JP2017533922 A5 JP 2017533922A5 JP 2017525115 A JP2017525115 A JP 2017525115A JP 2017525115 A JP2017525115 A JP 2017525115A JP 2017533922 A5 JP2017533922 A5 JP 2017533922A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- alkyl
- hydrogen
- halogen
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 38
- 229910052739 hydrogen Inorganic materials 0.000 claims 32
- 239000001257 hydrogen Substances 0.000 claims 32
- 150000002431 hydrogen Chemical class 0.000 claims 32
- 229910052736 halogen Inorganic materials 0.000 claims 22
- 150000002367 halogens Chemical class 0.000 claims 22
- 239000008194 pharmaceutical composition Substances 0.000 claims 21
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 12
- 125000004452 carbocyclyl group Chemical group 0.000 claims 11
- 239000003112 inhibitor Substances 0.000 claims 11
- 125000002252 acyl group Chemical group 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 125000003342 alkenyl group Chemical group 0.000 claims 8
- 125000000304 alkynyl group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- 102100029895 Bromodomain-containing protein 4 Human genes 0.000 claims 6
- 101710126815 Bromodomain-containing protein 4 Proteins 0.000 claims 6
- 102100038970 Histone-lysine N-methyltransferase EZH2 Human genes 0.000 claims 5
- 101000882127 Homo sapiens Histone-lysine N-methyltransferase EZH2 Proteins 0.000 claims 5
- 239000013078 crystal Substances 0.000 claims 4
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- 239000000651 prodrug Substances 0.000 claims 4
- 229940002612 prodrug Drugs 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 3
- 108020004707 nucleic acids Proteins 0.000 claims 3
- 102000039446 nucleic acids Human genes 0.000 claims 3
- 150000007523 nucleic acids Chemical class 0.000 claims 3
- 239000000816 peptidomimetic Substances 0.000 claims 3
- 108090000765 processed proteins & peptides Proteins 0.000 claims 3
- 102000004169 proteins and genes Human genes 0.000 claims 3
- 108090000623 proteins and genes Proteins 0.000 claims 3
- 150000003384 small molecules Chemical group 0.000 claims 3
- UMZWNADQRDCKII-UHFFFAOYSA-N 2-[5-(5-bromo-2-oxoindol-3-yl)-4-hydroxy-2-sulfanylidene-1,3-thiazol-3-yl]butanedioic acid Chemical compound OC(=O)CC(C(O)=O)n1c(O)c(sc1=S)C1=c2cc(Br)ccc2=NC1=O UMZWNADQRDCKII-UHFFFAOYSA-N 0.000 claims 2
- 229940096923 Bcl6 inhibitor Drugs 0.000 claims 2
- 101100381525 Mus musculus Bcl6 gene Proteins 0.000 claims 2
- 102000013538 Proto-Oncogene Proteins c-bcl-6 Human genes 0.000 claims 2
- 108010090920 Proto-Oncogene Proteins c-bcl-6 Proteins 0.000 claims 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 208000017760 chronic graft versus host disease Diseases 0.000 claims 2
- 239000003623 enhancer Substances 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- 210000000130 stem cell Anatomy 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000004434 sulfur atom Chemical group 0.000 claims 2
- 210000001744 T-lymphocyte Anatomy 0.000 claims 1
- 238000011316 allogeneic transplantation Methods 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 238000002513 implantation Methods 0.000 claims 1
- 230000004199 lung function Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462076358P | 2014-11-06 | 2014-11-06 | |
| US62/076,358 | 2014-11-06 | ||
| PCT/US2015/059551 WO2016073903A1 (en) | 2014-11-06 | 2015-11-06 | Use of compositions modulating chromatin structure for graft versus host disease (gvhd) |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017533922A JP2017533922A (ja) | 2017-11-16 |
| JP2017533922A5 true JP2017533922A5 (enExample) | 2018-12-13 |
Family
ID=55909890
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017525115A Pending JP2017533922A (ja) | 2014-11-06 | 2015-11-06 | 移植片対宿主病（ｇｖｈｄ）のためのクロマチン構造を調節する組成物の使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20190000860A1 (enExample) |
| EP (1) | EP3215160A4 (enExample) |
| JP (1) | JP2017533922A (enExample) |
| KR (1) | KR20170098808A (enExample) |
| CN (1) | CN107249593A (enExample) |
| AU (1) | AU2015342895A1 (enExample) |
| BR (1) | BR112017009440A2 (enExample) |
| CA (1) | CA2966336A1 (enExample) |
| WO (1) | WO2016073903A1 (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA038337B1 (ru) | 2014-06-17 | 2021-08-11 | Эпизим, Инк. | Ингибиторы ezh2 для лечения лимфомы |
| CA2964629A1 (en) | 2014-11-06 | 2016-05-12 | Dana-Farber Cancer Institute, Inc. | Ezh2 inhibitors and uses thereof |
| EA201890009A1 (ru) * | 2015-06-10 | 2018-07-31 | Эпизайм, Инк. | Ингибиторы ezh2 для лечения лимфомы |
| WO2017184999A1 (en) | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Ezh2 inhibitors and uses thereof |
| BR112019014924A2 (pt) | 2017-01-19 | 2020-03-31 | St. Marianna University School Of Medicine | Composição farmacêutica usada para o tratamento de mielopatia associada ao htlv-1 |
| US10266542B2 (en) | 2017-03-15 | 2019-04-23 | Mirati Therapeutics, Inc. | EZH2 inhibitors |
| DK3746446T3 (da) | 2018-01-31 | 2022-06-27 | Mirati Therapeutics Inc | PRC2-inhibitorer |
| CN108685880A (zh) * | 2018-04-16 | 2018-10-23 | 广东省人民医院(广东省医学科学院) | Bcl-6小分子抑制剂用于制备预防或治疗cGVHD的药物 |
| WO2020011607A1 (en) | 2018-07-09 | 2020-01-16 | Fondation Asile Des Aveugles | Inhibition of prc2 subunits to treat eye disorders |
| US20220016111A1 (en) * | 2018-12-21 | 2022-01-20 | The Walter And Eliza Hall Institute Of Medical Research | Methods of Treating Inflammation |
| US12421228B2 (en) | 2019-04-22 | 2025-09-23 | Mirati Therapeutics, Inc. | Naphthyridine derivatives as PRC2 inhibitors |
| CN114269748A (zh) | 2019-06-05 | 2022-04-01 | 米拉蒂医疗股份有限公司 | 作为用于治疗癌症的PRC2抑制剂的咪唑并[1,2-c]嘧啶衍生物 |
| CN112341390B (zh) * | 2019-08-07 | 2022-08-23 | 四川大学 | 用于制备靶向组蛋白甲基转移酶ezh2共价抑制剂的化合物及其制备方法和用途 |
| WO2021175432A1 (en) | 2020-03-04 | 2021-09-10 | Boehringer Ingelheim International Gmbh | Method for administration of an anti cancer agent |
| CA3249707A1 (en) | 2022-04-27 | 2023-11-02 | Daiichi Sankyo Company, Limited | COMBINATION OF AN ANTIBODY-DRUG CONJUGATE WITH AN EZH1 AND/OR EZH2 INHIBITOR |
| KR20250044657A (ko) * | 2022-08-09 | 2025-04-01 | 다나-파버 캔서 인스티튜트 인크. | 거대고리 bcl6 분해제 |
| WO2024211684A1 (en) * | 2023-04-06 | 2024-10-10 | Halda Therapeutics Opco, Inc. | Heterobifunctional compounds and methods of treating disease |
| WO2025085738A1 (en) | 2023-10-18 | 2025-04-24 | Halda Therapeutics Opco, Inc. | Heterobifunctional compounds and methods of treating disease |
| WO2025189056A1 (en) | 2024-03-08 | 2025-09-12 | Halda Therapeutics Opco, Inc. | Heterobifunctional compounds and their use in treating disease |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2250154T3 (es) * | 1999-07-16 | 2006-04-16 | Kissei Pharmaceutical Co., Ltd. | Agentes que inhiben las reacciones de rechazo cronico despues de un transplante de organo. |
| WO2008066887A2 (en) * | 2006-11-30 | 2008-06-05 | Albert Einstein College Of Medicine Of Yeshiva University | Small molecule inhibitors of bcl6 |
| KR20080107050A (ko) * | 2007-06-05 | 2008-12-10 | 울산대학교 산학협력단 | 항-ｃｄ１３７ 단일클론 항체를 포함하는 만성이식편대숙주 질환의 예방 또는 치료용 약학적 조성물 |
| WO2012005805A1 (en) * | 2010-05-07 | 2012-01-12 | Glaxosmithkline Llc | Azaindazoles |
| US20120014979A1 (en) * | 2010-07-16 | 2012-01-19 | Alexander Dent | Use of bcl6 inhibitors for treating autoimmune diseases |
| WO2012118812A2 (en) * | 2011-02-28 | 2012-09-07 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| US9073924B2 (en) * | 2011-09-13 | 2015-07-07 | Glaxosmithkline Llc | Azaindazoles |
| WO2013067302A1 (en) * | 2011-11-04 | 2013-05-10 | Glaxosmithkline Intellectual Property (No. 2) Limited | Method of treatment |
| AU2012332297B2 (en) * | 2011-11-04 | 2016-01-07 | Glaxosmithkline Intellectual Property (No.2) Limited | Method of treatment |
| WO2013123521A1 (en) * | 2012-02-17 | 2013-08-22 | Nexbio, Inc. | Methods, Compounds and Compositions for Treatment of Parainfluenza Virus in Immunocompromised Patients |
| WO2014155301A1 (en) * | 2013-03-26 | 2014-10-02 | Piramal Enterprises Limited | Substituted bicyclic compounds as inhibitors of ezh2 |
-
2015
- 2015-11-06 BR BR112017009440A patent/BR112017009440A2/pt not_active Application Discontinuation
- 2015-11-06 WO PCT/US2015/059551 patent/WO2016073903A1/en not_active Ceased
- 2015-11-06 CN CN201580066388.8A patent/CN107249593A/zh active Pending
- 2015-11-06 KR KR1020177014969A patent/KR20170098808A/ko not_active Withdrawn
- 2015-11-06 CA CA2966336A patent/CA2966336A1/en not_active Abandoned
- 2015-11-06 JP JP2017525115A patent/JP2017533922A/ja active Pending
- 2015-11-06 US US15/524,707 patent/US20190000860A1/en not_active Abandoned
- 2015-11-06 AU AU2015342895A patent/AU2015342895A1/en not_active Abandoned
- 2015-11-06 EP EP15856340.3A patent/EP3215160A4/en not_active Withdrawn
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