JP2019514884A5 - - Google Patents
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- Publication number
- JP2019514884A5 JP2019514884A5 JP2018555500A JP2018555500A JP2019514884A5 JP 2019514884 A5 JP2019514884 A5 JP 2019514884A5 JP 2018555500 A JP2018555500 A JP 2018555500A JP 2018555500 A JP2018555500 A JP 2018555500A JP 2019514884 A5 JP2019514884 A5 JP 2019514884A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- alkyl
- optionally
- formula
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 69
- 125000000623 heterocyclic group Chemical group 0.000 claims 39
- 229910052739 hydrogen Inorganic materials 0.000 claims 39
- 239000001257 hydrogen Substances 0.000 claims 39
- 150000002431 hydrogen Chemical class 0.000 claims 36
- 125000001072 heteroaryl group Chemical group 0.000 claims 28
- 229910052736 halogen Inorganic materials 0.000 claims 26
- 150000002367 halogens Chemical class 0.000 claims 26
- 125000004452 carbocyclyl group Chemical group 0.000 claims 25
- 125000002252 acyl group Chemical group 0.000 claims 23
- 125000003342 alkenyl group Chemical group 0.000 claims 21
- 125000003118 aryl group Chemical group 0.000 claims 21
- 125000000304 alkynyl group Chemical group 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 20
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 19
- 229910052757 nitrogen Inorganic materials 0.000 claims 12
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 11
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 10
- 229910052717 sulfur Inorganic materials 0.000 claims 10
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 9
- 125000004429 atom Chemical group 0.000 claims 7
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 7
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 239000001301 oxygen Substances 0.000 claims 5
- 125000004430 oxygen atom Chemical group O* 0.000 claims 5
- 239000011593 sulfur Substances 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 4
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 4
- 125000004434 sulfur atom Chemical group 0.000 claims 4
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 4
- 229920002554 vinyl polymer Polymers 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 125000002837 carbocyclic group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000004193 piperazinyl group Chemical group 0.000 claims 3
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 3
- 125000000547 substituted alkyl group Chemical group 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- 108010036115 Histone Methyltransferases Proteins 0.000 claims 2
- 102000011787 Histone Methyltransferases Human genes 0.000 claims 2
- 102100038970 Histone-lysine N-methyltransferase EZH2 Human genes 0.000 claims 2
- 101000882127 Homo sapiens Histone-lysine N-methyltransferase EZH2 Proteins 0.000 claims 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 239000003623 enhancer Substances 0.000 claims 2
- QTTMOCOWZLSYSV-QWAPEVOJSA-M equilin sodium sulfate Chemical compound [Na+].[O-]S(=O)(=O)OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4C3=CCC2=C1 QTTMOCOWZLSYSV-QWAPEVOJSA-M 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 108091033319 polynucleotide Proteins 0.000 claims 2
- 102000040430 polynucleotide Human genes 0.000 claims 2
- 239000002157 polynucleotide Substances 0.000 claims 2
- 108090000765 processed proteins & peptides Proteins 0.000 claims 2
- 108090000623 proteins and genes Proteins 0.000 claims 2
- 102000004169 proteins and genes Human genes 0.000 claims 2
- 150000003384 small molecules Chemical class 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010060999 Benign neoplasm Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 101001028782 Homo sapiens Histone-lysine N-methyltransferase EZH1 Proteins 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000034038 Pathologic Neovascularization Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000003790 Weaver syndrome Diseases 0.000 claims 1
- 230000001594 aberrant effect Effects 0.000 claims 1
- 125000004057 biotinyl group Chemical class [H]N1C(=O)N([H])[C@]2([H])[C@@]([H])(SC([H])([H])[C@]12[H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C(*)=O 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 206010020718 hyperplasia Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 125000003566 oxetanyl group Chemical group 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662326036P | 2016-04-22 | 2016-04-22 | |
| US62/326,036 | 2016-04-22 | ||
| PCT/US2017/028885 WO2017184999A1 (en) | 2016-04-22 | 2017-04-21 | Ezh2 inhibitors and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019514884A JP2019514884A (ja) | 2019-06-06 |
| JP2019514884A5 true JP2019514884A5 (enExample) | 2020-06-11 |
| JP7493304B2 JP7493304B2 (ja) | 2024-05-31 |
Family
ID=60116436
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018555500A Active JP7493304B2 (ja) | 2016-04-22 | 2017-04-21 | Ｅｚｈ２インヒビターおよびそれらの使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10633371B2 (enExample) |
| EP (1) | EP3445365A4 (enExample) |
| JP (1) | JP7493304B2 (enExample) |
| CN (1) | CN109069508A (enExample) |
| AU (1) | AU2017252460B2 (enExample) |
| CA (1) | CA3018270A1 (enExample) |
| WO (1) | WO2017184999A1 (enExample) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2964629A1 (en) | 2014-11-06 | 2016-05-12 | Dana-Farber Cancer Institute, Inc. | Ezh2 inhibitors and uses thereof |
| 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 |
| CN108314677B (zh) * | 2017-01-17 | 2020-06-30 | 安徽中科拓苒药物科学研究有限公司 | 一种ezh2抑制剂及其用途 |
| US10266542B2 (en) | 2017-03-15 | 2019-04-23 | Mirati Therapeutics, Inc. | EZH2 inhibitors |
| CN109942556A (zh) * | 2017-12-21 | 2019-06-28 | 上海青煜医药科技有限公司 | 嘧啶酮化合物及其应用 |
| DK3746446T3 (da) | 2018-01-31 | 2022-06-27 | Mirati Therapeutics Inc | PRC2-inhibitorer |
| CN110229151B (zh) * | 2018-03-06 | 2021-09-10 | 上海海和药物研究开发股份有限公司 | 吲嗪类化合物、其制备方法及用途 |
| WO2020011607A1 (en) | 2018-07-09 | 2020-01-16 | Fondation Asile Des Aveugles | Inhibition of prc2 subunits to treat eye disorders |
| US12421228B2 (en) | 2019-04-22 | 2025-09-23 | Mirati Therapeutics, Inc. | Naphthyridine derivatives as PRC2 inhibitors |
| TWI747121B (zh) * | 2019-05-21 | 2021-11-21 | 大江生醫股份有限公司 | 茶樹葉的發酵物用於調控ＣＣＴ基因、Ｐｉｎｋ１基因、ＰＡＲＰ２基因、ＭＩＴＦ基因、ＵＮＧ基因、ＥＲＣＣ６基因、ＴＥＲＣ基因、ＣＤ４０基因、ＤＹＮＬＬ２基因、ＧＲＫ５基因、ＲＥＬＢ基因、ＴＮＦＳＦ１４基因、ＩＬ４Ｒ基因與ＲＥＬＡ基因的表現量及抗老化、美白、提升免疫力與降低脂肪累積之用途 |
| 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 |
| UY39882A (es) * | 2021-08-02 | 2023-06-15 | Eurofarma Laboratorios S A | COMPUESTOS NACILHIDRAZÓNICOS INHIBIDORES DE Nav 1.7 Y/O Nav 1.8, SUS PROCESOS DE OBTENCIÓN, COMPOSICIONES, USOS, MÉTODOS DE TRATAMIENTO DE ESTOS Y KITS |
| CN115197202B (zh) * | 2022-07-15 | 2024-01-26 | 四川大学 | 一种ezh2共价抑制剂及其制备方法和应用 |
| PY2404093A (es) * | 2023-01-30 | 2024-10-03 | Eurofarma Laboratorios S A | Hidrazidas bloqueadoras de nav 1.7 y/o nav 1.8, sus procesos de obtención, composiciones, usos, métodos de tratamiento de los mismos y kits |
| KR20260019479A (ko) | 2023-05-04 | 2026-02-10 | 레볼루션 메디슨즈, 인크. | Ras 관련 질환 또는 장애를 위한 병용 요법 |
| CN121889155A (zh) | 2023-08-07 | 2026-04-17 | 锐新医药公司 | 用于治疗ras蛋白相关疾病或病症的rmc-6291 |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250313530A1 (en) * | 2024-04-05 | 2025-10-09 | Trustees Of Boston University | Small molecule inhibitors of interleukin-4 and uses thereof |
| 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 |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
| WO2026090116A2 (en) | 2024-10-21 | 2026-04-30 | Revolution Medicines, Inc. | Ras inhibitors |
| US20260108528A1 (en) | 2024-10-22 | 2026-04-23 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2026090245A1 (en) | 2024-10-22 | 2026-04-30 | Revolution Medicines, Inc. | Use of ras inhibitors for treating cancer |
| WO2026106912A1 (en) | 2024-11-12 | 2026-05-21 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026112260A1 (en) | 2024-11-21 | 2026-05-28 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026122764A2 (en) | 2024-12-06 | 2026-06-11 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026128688A2 (en) | 2024-12-13 | 2026-06-18 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026161839A1 (en) | 2025-01-27 | 2026-07-30 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US7989465B2 (en) | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| WO2010008436A1 (en) | 2008-06-24 | 2010-01-21 | Albert Einstein College Of Medicine Of Yeshiva University | Methods and compositions for inhibition of bcl6 repression |
| WO2011014032A2 (en) | 2009-07-31 | 2011-02-03 | Lg Electronics Inc. | Washing machine |
| US9423331B2 (en) * | 2010-04-14 | 2016-08-23 | Mobrey Limited | Method of determining the energy content of a methane-rich gas mixture |
| MX2012012966A (es) | 2010-05-07 | 2013-01-22 | Glaxosmithkline Llc | Indoles. |
| WO2012005805A1 (en) | 2010-05-07 | 2012-01-12 | Glaxosmithkline Llc | Azaindazoles |
| ES2606958T3 (es) | 2010-05-14 | 2017-03-28 | Dana-Farber Cancer Institute, Inc. | Compuestos de tienotriazolodiazepina para tratar una neoplasia |
| US20120014979A1 (en) | 2010-07-16 | 2012-01-19 | Alexander Dent | Use of bcl6 inhibitors for treating autoimmune diseases |
| 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 |
| JO3363B1 (ar) | 2011-04-13 | 2019-03-13 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| US9073924B2 (en) | 2011-09-13 | 2015-07-07 | Glaxosmithkline Llc | Azaindazoles |
| US9730925B2 (en) | 2011-09-30 | 2017-08-15 | Glaxomithkline Llc | Methods of treating cancer |
| WO2013067300A1 (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 |
| WO2013067302A1 (en) | 2011-11-04 | 2013-05-10 | Glaxosmithkline Intellectual Property (No. 2) Limited | Method of treatment |
| JP6106685B2 (ja) | 2011-11-17 | 2017-04-05 | 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 | Ｃ−ｊｕｎ−ｎ−末端キナーゼ（ｊｎｋ）の阻害剤 |
| US10579982B2 (en) * | 2012-01-03 | 2020-03-03 | International Business Machines Corporation | Identifying money laundering in micro-commerce |
| WO2013123521A1 (en) | 2012-02-17 | 2013-08-22 | Nexbio, Inc. | Methods, Compounds and Compositions for Treatment of Parainfluenza Virus in Immunocompromised Patients |
| CA3177515A1 (en) * | 2012-03-12 | 2013-09-19 | Epizyme, Inc. | Inhibitors of human ezh2, and methods of use thereof |
| EP2836216B1 (en) * | 2012-04-13 | 2022-06-08 | Epizyme, Inc. | Combination therapy for treating cancer |
| US9562041B2 (en) * | 2012-05-16 | 2017-02-07 | Glaxosmithkline Llc | Enhancer of zeste homolog 2 inhibitors |
| DE102012011464A1 (de) * | 2012-06-12 | 2013-12-12 | Merck Patent Gmbh | Verfahren zur Erzeugung von dreidimensionalen Mustern in flüssigkristallinen Beschichtungen |
| BR112015008480A2 (pt) | 2012-10-15 | 2017-07-04 | Epizyme Inc | compostos de benzeno substituído |
| RU2015127822A (ru) | 2012-12-13 | 2017-01-16 | ГЛЭКСОСМИТКЛАЙН ЭлЭлСи | Ингибиторы энхансера гомолога 2 белка zeste |
| EP2934531A4 (en) | 2012-12-19 | 2016-06-15 | Glaxosmithkline Llc | COMBINATION |
| CA2894216A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | 1,4-pyridone compounds |
| CA2894222A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | 1,4-pyridone bicyclic heteroaryl compounds |
| US20160031907A1 (en) | 2013-03-15 | 2016-02-04 | Epizyme, Inc. | Substituted Benzene Compounds |
| WO2014155301A1 (en) | 2013-03-26 | 2014-10-02 | Piramal Enterprises Limited | Substituted bicyclic compounds as inhibitors of ezh2 |
| EP3022184B1 (en) * | 2013-07-19 | 2017-09-27 | Epizyme, Inc. | Substituted benzene compounds |
| US9738630B2 (en) | 2013-11-19 | 2017-08-22 | Bristol-Myers Squibb Company | Inhibitors of lysine methyl transferase |
| WO2015110999A1 (en) * | 2014-01-24 | 2015-07-30 | Piramal Enterprises Limited | Ezh2 inhibitors and uses thereof |
| CA2964629A1 (en) | 2014-11-06 | 2016-05-12 | Dana-Farber Cancer Institute, Inc. | Ezh2 inhibitors and uses thereof |
| BR112017009440A2 (pt) | 2014-11-06 | 2017-12-19 | Dana Farber Cancer Inst Inc | uso de composições que modulam a estrutura de cromatina quanto à doença do enxerto versus hospedeiro (gvhd) |
-
2017
- 2017-04-21 WO PCT/US2017/028885 patent/WO2017184999A1/en not_active Ceased
- 2017-04-21 AU AU2017252460A patent/AU2017252460B2/en not_active Ceased
- 2017-04-21 EP EP17786731.4A patent/EP3445365A4/en not_active Withdrawn
- 2017-04-21 CN CN201780025008.5A patent/CN109069508A/zh active Pending
- 2017-04-21 CA CA3018270A patent/CA3018270A1/en active Pending
- 2017-04-21 US US16/095,188 patent/US10633371B2/en active Active
- 2017-04-21 JP JP2018555500A patent/JP7493304B2/ja active Active
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