JP2018524298A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2018524298A5 JP2018524298A5 JP2017564058A JP2017564058A JP2018524298A5 JP 2018524298 A5 JP2018524298 A5 JP 2018524298A5 JP 2017564058 A JP2017564058 A JP 2017564058A JP 2017564058 A JP2017564058 A JP 2017564058A JP 2018524298 A5 JP2018524298 A5 JP 2018524298A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- ezh2 inhibitor
- ezh2
- inhibitor according
- lymphoma
- 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
- 102100038970 Histone-lysine N-methyltransferase EZH2 Human genes 0.000 claims 29
- 101000882127 Homo sapiens Histone-lysine N-methyltransferase EZH2 Proteins 0.000 claims 29
- 239000003112 inhibitor Substances 0.000 claims 25
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 206010025323 Lymphomas Diseases 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- 229940124597 therapeutic agent Drugs 0.000 claims 5
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 210000001280 germinal center Anatomy 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 3
- 208000003950 B-cell lymphoma Diseases 0.000 claims 2
- 108010033040 Histones Proteins 0.000 claims 2
- 210000001102 germinal center b cell Anatomy 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 230000011987 methylation Effects 0.000 claims 2
- 238000007069 methylation reaction Methods 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- GRZXWCHAXNAUHY-NSISKUIASA-N (2S)-2-(4-chlorophenyl)-1-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]-1-piperazinyl]-3-(propan-2-ylamino)-1-propanone Chemical group C1([C@H](C(=O)N2CCN(CC2)C=2C=3[C@H](C)C[C@@H](O)C=3N=CN=2)CNC(C)C)=CC=C(Cl)C=C1 GRZXWCHAXNAUHY-NSISKUIASA-N 0.000 claims 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- QTBWCSQGBMPECM-UHFFFAOYSA-N 3-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethyl-3-pyrazolyl]phenyl]-1,1-dimethylurea Chemical compound N=1N(CC)C=C(C=2C=3C=C(NC=3N=CC=2)C=2C=C(CN(C)C)C=CC=2)C=1C1=CC=C(NC(=O)N(C)C)C=C1 QTBWCSQGBMPECM-UHFFFAOYSA-N 0.000 claims 1
- 102100021569 Apoptosis regulator Bcl-2 Human genes 0.000 claims 1
- 102100021631 B-cell lymphoma 6 protein Human genes 0.000 claims 1
- 108091012583 BCL2 Proteins 0.000 claims 1
- 229940124130 Bcl inhibitor Drugs 0.000 claims 1
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- KGPGFQWBCSZGEL-ZDUSSCGKSA-N GSK690693 Chemical compound C=12N(CC)C(C=3C(=NON=3)N)=NC2=C(C#CC(C)(C)O)N=CC=1OC[C@H]1CCCNC1 KGPGFQWBCSZGEL-ZDUSSCGKSA-N 0.000 claims 1
- 101000971234 Homo sapiens B-cell lymphoma 6 protein Proteins 0.000 claims 1
- DNVXATUJJDPFDM-KRWDZBQOSA-N JQ1 Chemical compound N([C@@H](CC(=O)OC(C)(C)C)C1=NN=C(N1C=1SC(C)=C(C)C=11)C)=C1C1=CC=C(Cl)C=C1 DNVXATUJJDPFDM-KRWDZBQOSA-N 0.000 claims 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- NSQSAUGJQHDYNO-UHFFFAOYSA-N n-[(4,6-dimethyl-2-oxo-1h-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide Chemical group C=1C(C=2C=CC(CN3CCOCC3)=CC=2)=CC(C(=O)NCC=2C(NC(C)=CC=2C)=O)=C(C)C=1N(CC)C1CCOCC1 NSQSAUGJQHDYNO-UHFFFAOYSA-N 0.000 claims 1
- CGBJSGAELGCMKE-UHFFFAOYSA-N omipalisib Chemical compound COC1=NC=C(C=2C=C3C(C=4C=NN=CC=4)=CC=NC3=CC=2)C=C1NS(=O)(=O)C1=CC=C(F)C=C1F CGBJSGAELGCMKE-UHFFFAOYSA-N 0.000 claims 1
- 239000006186 oral dosage form Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 238000007390 skin biopsy Methods 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- OCGCJISPOYIXKL-MGCOHNPYSA-N CCN[C@H](CC1)CC[C@@H]1N(C)C Chemical compound CCN[C@H](CC1)CC[C@@H]1N(C)C OCGCJISPOYIXKL-MGCOHNPYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562173685P | 2015-06-10 | 2015-06-10 | |
| US62/173,685 | 2015-06-10 | ||
| PCT/US2016/037024 WO2016201328A1 (en) | 2015-06-10 | 2016-06-10 | Ezh2 inhibitors for treating lymphoma |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018524298A JP2018524298A (ja) | 2018-08-30 |
| JP2018524298A5 true JP2018524298A5 (enExample) | 2019-07-11 |
| JP6890097B2 JP6890097B2 (ja) | 2021-06-18 |
Family
ID=57504554
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017564058A Active JP6890097B2 (ja) | 2015-06-10 | 2016-06-10 | リンパ腫を処置するためのｅｚｈ２阻害剤 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US20180311251A1 (enExample) |
| EP (1) | EP3307713A4 (enExample) |
| JP (1) | JP6890097B2 (enExample) |
| CN (1) | CN107635965A (enExample) |
| AU (2) | AU2016275051A1 (enExample) |
| CA (1) | CA2988816A1 (enExample) |
| EA (1) | EA201890009A1 (enExample) |
| IL (1) | IL256056A (enExample) |
| MX (2) | MX387885B (enExample) |
| WO (1) | WO2016201328A1 (enExample) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20130102477A1 (en) | 2010-06-23 | 2013-04-25 | Ryan D. Morin | Biomarkers for non-hodgkin lymphomas and uses thereof |
| JO3438B1 (ar) | 2011-04-13 | 2019-10-20 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| MX376008B (es) | 2012-10-15 | 2025-03-07 | Epizyme Inc | Inhibidor de ezh2 para usarse en el tratamiento de sarcoma epiteloide. |
| ES2863996T3 (es) | 2013-12-06 | 2021-10-13 | Epizyme Inc | Terapia de combinación para el tratamiento del cáncer |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| CA2952074C (en) | 2014-06-17 | 2022-08-30 | Epizyme, Inc. | Ezh2 inhibitors for treating lymphoma |
| IL296080B2 (en) * | 2014-11-17 | 2023-12-01 | Eisai R&D Man Co Ltd | Method for treating cancer |
| CN107635965A (zh) | 2015-06-10 | 2018-01-26 | Epizyme股份有限公司 | 用于治疗淋巴瘤的ezh2抑制剂 |
| EA201890567A1 (ru) | 2015-08-24 | 2018-08-31 | Эпизайм, Инк. | Способ лечения рака |
| JP2019503391A (ja) | 2016-01-29 | 2019-02-07 | エピザイム，インコーポレイティド | 癌を処置するための併用療法 |
| US11786533B2 (en) | 2016-06-01 | 2023-10-17 | Epizyme, Inc. | Use of EZH2 inhibitors for treating cancer |
| US11147819B2 (en) | 2016-06-17 | 2021-10-19 | Epizyme, Inc. | EZH2 inhibitors for treating cancer |
| US11191741B2 (en) | 2016-12-24 | 2021-12-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
| EP3571200B8 (en) | 2017-01-17 | 2022-08-03 | HepaRegeniX GmbH | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| WO2018183885A1 (en) | 2017-03-31 | 2018-10-04 | Epizyme, Inc. | Combination therapy for treating cancer |
| WO2018223030A1 (en) | 2017-06-02 | 2018-12-06 | Epizyme, Inc. | Use of ezh2 inhibitors for treating cancer |
| CA3074720A1 (en) | 2017-09-05 | 2019-03-14 | Epizyme, Inc. | Combination therapy for treating cancer |
| US20210000815A1 (en) * | 2017-12-28 | 2021-01-07 | Constellation Pharmaceuticals, Inc. | Pharmacokinetic enhancement of ezh2 inhibitors through combination therapies |
| US11220515B2 (en) | 2018-01-26 | 2022-01-11 | Yale University | Imide-based modulators of proteolysis and associated methods of use |
| US11969472B2 (en) | 2018-08-22 | 2024-04-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| BR112021003098A2 (pt) | 2018-08-22 | 2021-05-11 | Cullgen (Shanghai), Inc. | compostos de degradação de receptor de tropomiosina quinase (trk) e métodos de uso |
| TWI837231B (zh) * | 2018-11-29 | 2024-04-01 | 日商第一三共股份有限公司 | 含有ｅｚｈ１／２雙重抑制劑之醫藥組合及其用途 |
| WO2020165402A1 (en) * | 2019-02-14 | 2020-08-20 | Westfälische Wilhelms-Universität Münster | Gd2-upregulation by ezh2 inhibition in cancer therapy |
| EP4017527A1 (en) | 2019-08-22 | 2022-06-29 | Juno Therapeutics, Inc. | Combination therapy of a t cell therapy and an enhancer of zeste homolog 2 (ezh2) inhibitor and related methods |
| CN110960525A (zh) * | 2019-11-26 | 2020-04-07 | 济南大学 | 新型eed-ezh2相互作用抑制剂的确定和评价 |
| CN110950834A (zh) * | 2019-11-26 | 2020-04-03 | 济南大学 | 新型eed-ezh2相互作用小分子抑制剂的确定和评价 |
| US12410171B2 (en) | 2020-02-26 | 2025-09-09 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| CN111303133A (zh) * | 2020-03-25 | 2020-06-19 | 清华大学 | 降解ezh2蛋白的小分子化合物 |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112012028556A2 (pt) * | 2010-05-07 | 2014-04-01 | Glaxosmithkline Llc | Indóis |
| BR112013005806B1 (pt) | 2010-09-10 | 2022-05-10 | Epizyme, Inc | Métodos para detectar se um indivíduo é um candidato para o tratamento com ou responsivo a um inibidor de ezh2 e usos terapêuticos do dito inibidor de ezh2 |
| US9175331B2 (en) | 2010-09-10 | 2015-11-03 | Epizyme, Inc. | Inhibitors of human EZH2, and methods of use thereof |
| WO2012118812A2 (en) | 2011-02-28 | 2012-09-07 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| TW201733984A (zh) | 2011-04-13 | 2017-10-01 | 雅酶股份有限公司 | 經取代之苯化合物 |
| JO3438B1 (ar) | 2011-04-13 | 2019-10-20 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| BR112014007603A2 (pt) * | 2011-09-30 | 2017-06-13 | Glaxosmithkline Llc | métodos de tratamento do câncer |
| KR102453519B1 (ko) | 2012-03-12 | 2022-10-11 | 에피자임, 인코포레이티드 | 인간 ｅｚｈ2의 억제제 및 이의 사용 방법 |
| HUE045353T2 (hu) | 2012-04-13 | 2019-12-30 | Epizyme Inc | N-((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)-metil)-5-(etil-(tetrahidro-2H-pirán-4-il) -amino)-4-metil-4'-(morfolino-metil)-[1,1'-bifenil]-3-karboxamid-hidrobromid a hematológiai rendszer egy sejtszaporodásos rendellenességének kezelésében való alkalmazásra |
| NZ729643A (en) | 2012-04-13 | 2018-02-23 | Epizyme Inc | Combination therapy for treating cancer |
| WO2013173441A2 (en) | 2012-05-16 | 2013-11-21 | Glaxosmithkline Llc | Enhancer of zeste homolog 2 inhibitors |
| MX376008B (es) * | 2012-10-15 | 2025-03-07 | Epizyme Inc | Inhibidor de ezh2 para usarse en el tratamiento de sarcoma epiteloide. |
| CA2887562C (en) * | 2012-10-15 | 2021-01-12 | Epizyme, Inc. | Substituted benzene compounds |
| US20150283142A1 (en) * | 2013-03-15 | 2015-10-08 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using pi3 kinase isoform modulators |
| US20140120083A1 (en) | 2012-11-01 | 2014-05-01 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using pi3 kinase isoform modulators |
| DK2914296T4 (da) | 2012-11-01 | 2022-01-03 | Infinity Pharmaceuticals Inc | Behandling af cancere under anvendelse af PI3-kinase-isoform-modulatorer |
| EP2934531A4 (en) | 2012-12-19 | 2016-06-15 | Glaxosmithkline Llc | COMBINATION |
| WO2014100665A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | 1,4-pyridone bicyclic heteroaryl compounds |
| EP2935214B1 (en) | 2012-12-21 | 2019-02-20 | Epizyme, Inc. | 1,4-pyridone compounds |
| EP2970281A4 (en) | 2013-03-15 | 2016-08-03 | Epizyme Inc | SUBSTITUTED BENZOL COMPOUNDS |
| US9776996B2 (en) | 2013-03-15 | 2017-10-03 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| SG10201709926VA (en) * | 2013-05-30 | 2017-12-28 | Infinity Pharmaceuticals Inc | Treatment of cancers using pi3 kinase isoform modulators |
| US10150764B2 (en) | 2013-07-19 | 2018-12-11 | Epizyme, Inc. | Substituted benzene compounds |
| WO2015010078A2 (en) | 2013-07-19 | 2015-01-22 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| SG11201602269QA (en) | 2013-10-16 | 2016-04-28 | Epizyme Inc | Hydrochloride salt form for ezh2 inhibition |
| AU2014337121A1 (en) | 2013-10-18 | 2016-04-14 | Epizyme, Inc. | Method of treating cancer |
| ES2863996T3 (es) | 2013-12-06 | 2021-10-13 | Epizyme Inc | Terapia de combinación para el tratamiento del cáncer |
| CA2952074C (en) * | 2014-06-17 | 2022-08-30 | Epizyme, Inc. | Ezh2 inhibitors for treating lymphoma |
| WO2015200650A1 (en) | 2014-06-25 | 2015-12-30 | Epizyme, Inc. | Substituted benzene and 6,5-fused bicyclic heteroaryl compounds |
| CN112168967A (zh) | 2014-10-16 | 2021-01-05 | Epizyme股份有限公司 | 治疗癌症的方法 |
| JP2017533922A (ja) * | 2014-11-06 | 2017-11-16 | 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 | 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 |
| IL296080B2 (en) | 2014-11-17 | 2023-12-01 | Eisai R&D Man Co Ltd | Method for treating cancer |
| JP6544507B2 (ja) | 2015-02-09 | 2019-07-17 | 日本精機株式会社 | ヘッドアップディスプレイ装置 |
| AU2016252546A1 (en) | 2015-04-20 | 2017-11-02 | Epizyme, Inc. | Combination therapy for treating cancer |
| CN107635965A (zh) | 2015-06-10 | 2018-01-26 | Epizyme股份有限公司 | 用于治疗淋巴瘤的ezh2抑制剂 |
| KR20170095656A (ko) | 2016-02-15 | 2017-08-23 | 동부대우전자 주식회사 | 방열구조를 갖는 세탁기 |
-
2016
- 2016-06-10 CN CN201680032950.XA patent/CN107635965A/zh active Pending
- 2016-06-10 WO PCT/US2016/037024 patent/WO2016201328A1/en not_active Ceased
- 2016-06-10 CA CA2988816A patent/CA2988816A1/en active Pending
- 2016-06-10 AU AU2016275051A patent/AU2016275051A1/en not_active Abandoned
- 2016-06-10 US US15/580,908 patent/US20180311251A1/en not_active Abandoned
- 2016-06-10 JP JP2017564058A patent/JP6890097B2/ja active Active
- 2016-06-10 EP EP16808443.2A patent/EP3307713A4/en not_active Withdrawn
- 2016-06-10 MX MX2017015938A patent/MX387885B/es unknown
- 2016-06-10 EA EA201890009A patent/EA201890009A1/ru unknown
-
2017
- 2017-12-03 IL IL256056A patent/IL256056A/en unknown
- 2017-12-07 MX MX2021013830A patent/MX2021013830A/es unknown
-
2019
- 2019-01-17 US US16/250,211 patent/US11202781B2/en active Active
-
2021
- 2021-03-18 AU AU2021201705A patent/AU2021201705A1/en not_active Abandoned
- 2021-11-15 US US17/526,307 patent/US11951109B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2018524298A5 (enExample) | ||
| JP2019521988A5 (enExample) | ||
| JP2011505347A5 (enExample) | ||
| JP2019514854A5 (enExample) | ||
| JP2009504763A5 (enExample) | ||
| JP2017518334A5 (enExample) | ||
| JP2018021051A5 (enExample) | ||
| RU2018106453A (ru) | Соединения | |
| RU2006109467A (ru) | Способы лечения рака с использованием ингибиторов hdac | |
| JP2005506352A5 (enExample) | ||
| CA2883751A1 (en) | Methods of treating alzheimer's disease and pharmaceutical compositions thereof | |
| RU2013124824A (ru) | Твердые дисперсии, содержащие средства, вызывающие апоптоз | |
| JP2016539134A5 (enExample) | ||
| JP2008509187A5 (enExample) | ||
| RU2013137452A (ru) | Композиции, содержащие расщепляемое ферментами пролекарство оксикодона | |
| JP2018524390A5 (enExample) | ||
| JP2016534063A5 (enExample) | ||
| RU2019141734A (ru) | Терапевтические соединения и композиции и способы их применения | |
| RU2014152790A (ru) | Пирролопиразоновые ингибиторы танкиразы | |
| ES2698363T3 (es) | Composiciones de oxprenolol para tratar el cáncer | |
| JP2018090566A5 (enExample) | ||
| JP2008534453A5 (enExample) | ||
| RU2008139195A (ru) | Замещенные арилсульфанамиды как противовирусные средства | |
| RU99101081A (ru) | Режим введения ингибиторов н+, к+-атфазы | |
| JP2015522033A5 (enExample) |