JP2015506985A5 - - Google Patents
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- Publication number
- JP2015506985A5 JP2015506985A5 JP2014556793A JP2014556793A JP2015506985A5 JP 2015506985 A5 JP2015506985 A5 JP 2015506985A5 JP 2014556793 A JP2014556793 A JP 2014556793A JP 2014556793 A JP2014556793 A JP 2014556793A JP 2015506985 A5 JP2015506985 A5 JP 2015506985A5
- Authority
- JP
- Japan
- Prior art keywords
- alkylene
- piperidin
- alkyl
- ring
- heteroaryl
- 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
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- -1 (cyclopropyl)- Chemical class 0.000 claims 23
- 150000001875 compounds Chemical group 0.000 claims 11
- 125000002947 alkylene group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000004452 carbocyclyl group Chemical group 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 125000001153 fluoro group Chemical group F* 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 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
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000004484 1-methylpiperidin-4-yl group Chemical group CN1CCC(CC1)* 0.000 claims 1
- 125000004201 2,4-dichlorophenyl group Chemical group [H]C1=C([H])C(*)=C(Cl)C([H])=C1Cl 0.000 claims 1
- 125000004215 2,4-difluorophenyl group Chemical group [H]C1=C([H])C(*)=C(F)C([H])=C1F 0.000 claims 1
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 108010033040 Histones Proteins 0.000 claims 1
- 102000006947 Histones Human genes 0.000 claims 1
- 108010039491 Ricin Proteins 0.000 claims 1
- 125000003342 alkenyl 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
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000000040 m-tolyl group Chemical group [H]C1=C([H])C(*)=C([H])C(=C1[H])C([H])([H])[H] 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- CMWTZPSULFXXJA-VIFPVBQESA-N naproxen Chemical group C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-N 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 1
- AHIHJODVQGBOND-UHFFFAOYSA-M propan-2-yl carbonate Chemical compound CC(C)OC([O-])=O AHIHJODVQGBOND-UHFFFAOYSA-M 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 0 C*(CCC1=Cc(cccc2)c2NC1=O)c(cc1C=C2*)ccc1NC2=O Chemical compound C*(CCC1=Cc(cccc2)c2NC1=O)c(cc1C=C2*)ccc1NC2=O 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261597695P | 2012-02-10 | 2012-02-10 | |
| US61/597,695 | 2012-02-10 | ||
| US201261667821P | 2012-07-03 | 2012-07-03 | |
| US61/667,821 | 2012-07-03 | ||
| PCT/US2013/025639 WO2013120104A2 (en) | 2012-02-10 | 2013-02-11 | Modulators of methyl modifying enzymes, compositions and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015506985A JP2015506985A (ja) | 2015-03-05 |
| JP2015506985A5 true JP2015506985A5 (enExample) | 2016-03-31 |
| JP5989805B2 JP5989805B2 (ja) | 2016-09-07 |
Family
ID=48948171
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014556793A Active JP5989805B2 (ja) | 2012-02-10 | 2013-02-11 | メチル基変更酵素の調節物質、組成物及びその使用 |
| JP2015557190A Active JP5989923B2 (ja) | 2012-02-10 | 2014-02-11 | メチル基変更酵素の調節物質、組成物及びその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015557190A Active JP5989923B2 (ja) | 2012-02-10 | 2014-02-11 | メチル基変更酵素の調節物質、組成物及びその使用 |
Country Status (20)
| Country | Link |
|---|---|
| US (8) | US9085583B2 (enExample) |
| EP (1) | EP2812001B1 (enExample) |
| JP (2) | JP5989805B2 (enExample) |
| AR (1) | AR094755A1 (enExample) |
| AU (1) | AU2013216721B2 (enExample) |
| BR (1) | BR112015018508B1 (enExample) |
| CA (1) | CA2862289C (enExample) |
| CY (1) | CY1119060T1 (enExample) |
| DK (1) | DK2953941T3 (enExample) |
| EA (1) | EA029089B9 (enExample) |
| ES (1) | ES2632241T3 (enExample) |
| HR (1) | HRP20171030T1 (enExample) |
| LT (1) | LT2953941T (enExample) |
| MX (1) | MX363392B (enExample) |
| MY (1) | MY172156A (enExample) |
| NZ (1) | NZ628762A (enExample) |
| PT (1) | PT2953941T (enExample) |
| SM (1) | SMT201700340T1 (enExample) |
| UA (1) | UA117362C2 (enExample) |
| WO (1) | WO2013120104A2 (enExample) |
Families Citing this family (64)
| 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 |
| EP2780013A4 (en) | 2011-11-18 | 2015-07-01 | Constellation Pharmaceuticals Inc | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF |
| EP2812001B1 (en) * | 2012-02-10 | 2017-06-14 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| BR112015008447A2 (pt) | 2012-10-15 | 2017-07-04 | Epizyme Inc | métodos para tratar câncer |
| RS56207B1 (sr) * | 2013-02-11 | 2017-11-30 | Constellation Pharmaceuticals Inc | Modulatori enzima koji modifikuju metil, njihove kompozicije i upotreba |
| EP2970305B1 (en) | 2013-03-15 | 2017-02-22 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| CA2910873A1 (en) | 2013-04-30 | 2014-11-06 | Glaxosmithkline Intellectual Property (No.2) Limited | Enhancer of zeste homolog 2 inhibitors |
| JP2016523955A (ja) | 2013-07-10 | 2016-08-12 | グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｎｏ．２ Ｌｉｍｉｔｅｄ | Ｚｅｓｔｅホモログ２エンハンサー阻害剤 |
| TWI636047B (zh) | 2013-08-14 | 2018-09-21 | 英商卡爾維斯塔製藥有限公司 | 雜環衍生物 |
| EP3033334A1 (en) * | 2013-08-15 | 2016-06-22 | Constellation Pharmaceuticals, Inc. | Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof |
| WO2015078417A1 (zh) * | 2013-11-29 | 2015-06-04 | 四川好医生药业集团有限公司 | 吡咯并嘧啶化合物及其在制备降血糖药物中的用途 |
| WO2015200650A1 (en) * | 2014-06-25 | 2015-12-30 | Epizyme, Inc. | Substituted benzene and 6,5-fused bicyclic heteroaryl compounds |
| KR20170068603A (ko) * | 2014-10-28 | 2017-06-19 | 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 | 제스트 인핸서 상동체 2 억제제 |
| GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | Enzyme inhibitors |
| GB201421085D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| TW201636344A (zh) | 2014-12-05 | 2016-10-16 | 美國禮來大藥廠 | Ｅｚｈ２抑制劑 |
| US20180037568A1 (en) * | 2015-02-13 | 2018-02-08 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| UY36758A (es) * | 2015-06-30 | 2016-12-30 | Glaxosmithkline Ip No 2 Ltd | Inhibidores del potenciador del homólogo zeste 2 |
| WO2017018975A1 (en) | 2015-07-24 | 2017-02-02 | Constellation Pharmaceuticals, Inc. | Combination therapies for modulation of histone methyl modifying enzymes |
| JP2018522045A (ja) | 2015-08-03 | 2018-08-09 | コンステレーション・ファーマシューティカルズ・インコーポレイテッドＣｏｎｓｔｅｌｌａｔｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | Ｅｚｈ２阻害剤および制御性ｔ細胞機能の調節 |
| WO2017025493A1 (en) * | 2015-08-12 | 2017-02-16 | Bayer Pharma Aktiengesellschaft | Quinoline ezh2 inhibitors |
| US10493076B2 (en) | 2015-08-24 | 2019-12-03 | Epizyme, Inc. | Method for treating cancer |
| TW201718598A (zh) | 2015-08-27 | 2017-06-01 | 美國禮來大藥廠 | Ｅｚｈ２抑制劑 |
| WO2017040190A1 (en) | 2015-08-28 | 2017-03-09 | Constellation Pharmaceuticals, Inc. | Crystalline forms of (r)-n-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1h-indole-3-carboxamide |
| EP4309738A3 (en) | 2015-10-06 | 2024-07-17 | Epizyme, Inc. | Method of treating medulloblastoma with an ezh2 inhibitor |
| EP3674709A1 (en) | 2015-11-05 | 2020-07-01 | Epizyme Inc | Flow cytometry for monitoring histone h3 methylation status |
| US11951108B2 (en) | 2016-01-29 | 2024-04-09 | Epizyme, Inc. | Combination therapy for treating cancer |
| AU2017233898B2 (en) | 2016-03-15 | 2022-12-15 | Oryzon Genomics, S.A. | Combinations of LSD1 inhibitors for use in the treatment of solid tumors |
| SG10201913616UA (en) | 2016-05-31 | 2020-03-30 | Kalvista Pharmaceuticals Ltd | Pyrazole derivatives as plasma kallikrein inhibitors |
| GB201609607D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts |
| GB201609603D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide |
| MA45406A (fr) | 2016-06-17 | 2019-04-24 | Epizyme Inc | Inhibiteurs d'ezh2 pour traiter le cancer |
| EP3529242A1 (en) * | 2016-10-19 | 2019-08-28 | Constellation Pharmaceuticals, Inc. | Synthesis of inhibitors of ezh2 |
| AU2017367768A1 (en) | 2016-12-02 | 2019-07-18 | Epizyme, Inc. | Combination therapy for treating cancer |
| WO2018136596A1 (en) | 2017-01-20 | 2018-07-26 | Constellation Pharmaceuticals, Inc. | Solid dispersions of (r)-n-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1h-indole-3-carboxamide |
| US10266542B2 (en) | 2017-03-15 | 2019-04-23 | Mirati Therapeutics, Inc. | EZH2 inhibitors |
| WO2018183885A1 (en) | 2017-03-31 | 2018-10-04 | Epizyme, Inc. | Combination therapy for treating cancer |
| WO2018231973A1 (en) | 2017-06-13 | 2018-12-20 | Epizyme, Inc. | Inhibitors of ezh2 and methods of use thereof |
| US20210161883A1 (en) | 2017-07-10 | 2021-06-03 | Constellation Pharmaceuticals, Inc. | Ezh2 inhibitor-induced gene expression |
| WO2019094552A1 (en) | 2017-11-09 | 2019-05-16 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| TWI698238B (zh) | 2017-11-14 | 2020-07-11 | 美商輝瑞股份有限公司 | Ｅｚｈ２抑制劑組合治療 |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| MX2020005168A (es) | 2017-11-29 | 2020-08-20 | Kalvista Pharmaceuticals Ltd | Formas de dosificacion que contienen un inhibidor calicreina de plasma. |
| CN111757734A (zh) | 2017-12-28 | 2020-10-09 | 星座制药公司 | 通过组合疗法的ezh2抑制剂的药代动力学增强 |
| FI4043466T3 (fi) | 2018-01-31 | 2024-10-30 | Mirati Therapeutics Inc | Prc2:n estäjiä |
| WO2019178191A1 (en) | 2018-03-14 | 2019-09-19 | Biogen Ma Inc. | O-glycoprotein-2-acetamido-2-deoxy-3-d-glycopyranosidase inhibitors |
| HUE066783T2 (hu) * | 2018-04-18 | 2024-09-28 | Constellation Pharmaceuticals Inc | Metil módosító enzimek modulátorai, ezek készítményei és alkalmazásuk |
| CA3104209A1 (en) | 2018-07-09 | 2020-01-16 | Fondation Asile Des Aveugles | Inhibition of prc2 subunits to treat eye disorders |
| AU2019344922B2 (en) | 2018-09-19 | 2025-02-06 | Biogen Ma Inc. | O-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors |
| TW202031645A (zh) * | 2018-10-30 | 2020-09-01 | 丹麥商Ｈ 朗德貝克公司 | 作為Kv3鉀通道激活劑之芳基磺醯基吡咯甲醯胺衍生物 |
| TW202039482A (zh) | 2018-12-05 | 2020-11-01 | 美商百健Ｍａ公司 | 嗎啉基、哌嗪基、氧氮雜環庚烷基及二氮雜環庚烷基o-醣蛋白-2-乙醯胺基-2-去氧-3-d-葡萄哌喃醣苷酶抑制劑 |
| WO2020139339A1 (en) | 2018-12-27 | 2020-07-02 | Constellation Pharmaceuticals, Inc. | Ezh2 and androgen receptor signaling inhibitors as tools for targeting prostate cancer |
| CN110357840B (zh) * | 2019-01-22 | 2022-04-12 | 石家庄和中科技有限公司 | 4-糠硫基戊酮-2的制备方法 |
| US20220106305A1 (en) | 2019-02-04 | 2022-04-07 | Biogen Ma Inc. | Bicyclic ether o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors |
| WO2020185593A1 (en) | 2019-03-08 | 2020-09-17 | Biogen Ma Inc. | Azetidinyl 0-glyc0pr0tein-2-acetamid0-2-deoxy-3-d-gluc0pyran0sidase inhibitors |
| JP7624404B2 (ja) | 2019-04-22 | 2025-01-30 | ミラティ セラピューティクス，インク． | Ｐｒｃ２阻害剤としてのナフチリジン誘導体 |
| WO2020247475A1 (en) | 2019-06-05 | 2020-12-10 | Mirati Therapeutics, Inc. | Imidazo[1,2-c]pyrimidine derivatives as prc2 inhibitors for treating cancer |
| KR20220041130A (ko) * | 2019-07-24 | 2022-03-31 | 콘스텔레이션 파마슈티칼스, 인크. | 암 치료를 위한 병용 요법에서의 ezh2 억제 |
| WO2021028645A1 (en) | 2019-08-09 | 2021-02-18 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
| JP2022545467A (ja) | 2019-08-22 | 2022-10-27 | ジュノー セラピューティクス インコーポレイテッド | Ｔ細胞療法とｚｅｓｔｅホモログ２エンハンサー（ＥＺＨ２）阻害剤との併用療法および関連方法 |
| UY38934A (es) | 2019-10-29 | 2021-05-31 | Biogen Ma Inc | Inhibidores de o-glucoproteína-2-acetamido-2-deoxi-3-d-glucopiranosidasa espirocíclica |
| PE20231168A1 (es) | 2020-08-03 | 2023-07-26 | Biogen Ma Inc | Formas cristalinas de un inhibidor de la o-glucoproteina-2-acetamido-2-desoxi-3-d-glucopiranosidasa |
| WO2022150962A1 (en) | 2021-01-12 | 2022-07-21 | Westlake Pharmaceutical (Hangzhou) Co., Ltd. | Protease inhibitors, preparation, and uses thereof |
| CN118026860A (zh) * | 2024-02-05 | 2024-05-14 | 福建福瑞明德药业有限公司 | 一种3-[1-(二甲基氨基)乙基]苯酚的制备方法 |
Family Cites Families (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IE52670B1 (en) | 1981-03-03 | 1988-01-20 | Leo Ab | Heterocyclic carboxamides,compositions containing such compounds,and processes for their preparation |
| US5308854A (en) | 1990-06-18 | 1994-05-03 | Merck & Co., Inc. | Inhibitors of HIV reverse transcriptase |
| EP0867183B1 (en) | 1996-07-22 | 2004-10-06 | Daiichi Suntory Pharma Co., Ltd. | Arylpiperidinol and arylpiperidine derivatives and drugs containing the same |
| NZ531928A (en) | 2001-09-04 | 2005-10-28 | Boehringer Ingelheim Pharma | Novel dihydropteridinones, method for producing the same and the use thereof as medicaments |
| US6897220B2 (en) | 2001-09-14 | 2005-05-24 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| MXPA03000145A (es) | 2002-01-07 | 2003-07-15 | Pfizer | Compuestos de oxo u oxi-piridina como moduladores de receptores 5-ht4. |
| AU2003220401A1 (en) | 2002-03-18 | 2003-10-08 | Bristol-Myers Squibb Company | Uracil derivatives as inhibitors of tnf-alpha converting enzyme (tace) and matrix metalloproteinases |
| TWI319387B (en) | 2002-04-05 | 2010-01-11 | Astrazeneca Ab | Benzamide derivatives |
| TW200500341A (en) * | 2002-11-12 | 2005-01-01 | Astrazeneca Ab | Novel compounds |
| JP2007519735A (ja) | 2004-01-30 | 2007-07-19 | メルク エンド カムパニー インコーポレーテッド | Ｈｉｖインテグラーゼ阻害剤として有用であるｎ−ベンジル−３，４−ジヒドロキシピリジン−２−カルボキサミド及びｎ−ベンジル−２，３−ジヒドロキシピリジン−４−カルボキサミド化合物 |
| US9212149B2 (en) | 2004-04-30 | 2015-12-15 | Takeda Pharmaceutical Company Limited | Substituted 2-amidoquinazol-4-ones as matrix metalloproteinase-13 inhibitors |
| WO2005118796A2 (en) | 2004-06-01 | 2005-12-15 | The University Of North Carolina At Chapel Hill | Reconstituted histone methyltransferase complex and methods of identifying modulators thereof |
| US7732475B2 (en) * | 2005-07-14 | 2010-06-08 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| EP1915155A1 (en) | 2005-08-03 | 2008-04-30 | Boehringer Ingelheim International GmbH | Dihydropteridinones in the treatment of respiratory diseases |
| RU2008127252A (ru) | 2005-12-08 | 2010-01-20 | Новартис АГ (CH) | Эффекты ингибиторов fgfr3 на транскрипцию генов |
| WO2008054154A1 (en) | 2006-11-03 | 2008-05-08 | Korea Research Institute Of Chemical Technology | Naphthalenyloxypropenyl derivatives having inhibitory activity against histone deacetylase and pharmaceutical composition comprising the same |
| EP2115162B1 (en) | 2007-01-19 | 2012-09-26 | The Regents of the University of Michigan | Adrb2 cancer markers |
| EP2114898A2 (en) | 2007-02-16 | 2009-11-11 | Amgen Inc. | Nitrogen-containing heterocyclyl ketones and their use as c-met inhibitors |
| US8030344B2 (en) | 2007-03-13 | 2011-10-04 | Methylgene Inc. | Inhibitors of histone deacetylase |
| WO2009006577A2 (en) * | 2007-07-03 | 2009-01-08 | The Regents Of The University Of Michigan | Compositions and methods for inhibiting ezh2 |
| US20100298270A1 (en) | 2007-07-23 | 2010-11-25 | Syndax Pharmaceuticals, Inc. | Novel Compounds and Methods of Using Them |
| FR2922209B1 (fr) | 2007-10-12 | 2010-06-11 | Sanofi Aventis | 5,6-DIARYLES PYRIDINES SUBSTITUES EN POSITION 2 et 3, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE. |
| JP2011506333A (ja) | 2007-12-06 | 2011-03-03 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | 新規ｓＥＨ阻害剤およびその使用 |
| WO2009119880A1 (en) | 2008-03-26 | 2009-10-01 | Takeda Pharmaceutical Company Limited | Substituted pyrazole derivatives and use thereof |
| CA2725481A1 (en) | 2008-06-18 | 2009-12-23 | Pfizer Limited | Nicotinamide derivatives |
| EP2365749A4 (en) | 2008-11-13 | 2012-05-30 | Merck Sharp & Dohme | Quinolone NEURO PEPTIDE-S-Receptor Antagonists |
| WO2011055270A1 (en) * | 2009-11-04 | 2011-05-12 | Wyeth Llc | Indole based receptor crth2 antagonists |
| US8468343B2 (en) | 2010-01-13 | 2013-06-18 | Futurewei Technologies, Inc. | System and method for securing wireless transmissions |
| US9469876B2 (en) | 2010-04-06 | 2016-10-18 | Caris Life Sciences Switzerland Holdings Gmbh | Circulating biomarkers for metastatic prostate cancer |
| US8575203B2 (en) | 2010-04-21 | 2013-11-05 | Boehringer Ingelheim International Gmbh | Chemical compounds |
| HRP20170736T1 (hr) | 2010-05-07 | 2017-07-28 | Glaxosmithkline Llc | Indoli |
| ES2528269T3 (es) | 2010-05-07 | 2015-02-06 | Glaxosmithkline Llc | Azaindazoles |
| ES2534804T3 (es) | 2010-05-07 | 2015-04-28 | Glaxosmithkline Llc | Indazoles |
| JP2013540995A (ja) | 2010-08-18 | 2013-11-07 | カリス ライフ サイエンシズ ルクセンブルク ホールディングス エス．アー．エール．エル． | 疾患に対する循環バイオマーカー |
| JP6389036B2 (ja) | 2010-09-10 | 2018-09-12 | エピザイム インコーポレイテッド | ヒトｅｚｈ２の阻害剤、およびその使用方法 |
| US9175331B2 (en) | 2010-09-10 | 2015-11-03 | Epizyme, Inc. | Inhibitors of human EZH2, and methods of use thereof |
| WO2012051492A2 (en) | 2010-10-14 | 2012-04-19 | University Of Georgia Research Foundation, Inc. | Compounds and methods for inhibiting hiv latency |
| WO2012068589A2 (en) | 2010-11-19 | 2012-05-24 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
| EP2646020B1 (en) | 2010-12-01 | 2016-09-21 | Glaxosmithkline LLC | Indoles |
| CA2827894A1 (en) | 2011-02-22 | 2012-08-30 | Caris Life Sciences Luxembourg Holdings, S.A.R.L. | Circulating biomarkers |
| EP3323820B1 (en) | 2011-02-28 | 2023-05-10 | 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 |
| US9073924B2 (en) | 2011-09-13 | 2015-07-07 | Glaxosmithkline Llc | Azaindazoles |
| CN103987842A (zh) | 2011-09-30 | 2014-08-13 | 葛兰素史密斯克莱有限责任公司 | 治疗癌症的方法 |
| WO2013067302A1 (en) | 2011-11-04 | 2013-05-10 | Glaxosmithkline Intellectual Property (No. 2) Limited | Method of treatment |
| EP2773754B1 (en) | 2011-11-04 | 2016-08-03 | Glaxosmithkline Intellectual Property (No. 2) Limited | Compounds for use in the treatment of T-cell mediated diseases |
| WO2013067300A1 (en) * | 2011-11-04 | 2013-05-10 | Glaxosmithkline Intellectual Property (No. 2) Limited | Method of treatment |
| US9206128B2 (en) | 2011-11-18 | 2015-12-08 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| EP2780013A4 (en) | 2011-11-18 | 2015-07-01 | Constellation Pharmaceuticals Inc | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF |
| WO2013078320A1 (en) | 2011-11-21 | 2013-05-30 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
| US20130230511A1 (en) | 2012-02-03 | 2013-09-05 | Board Of Regents, The University Of Texas System | Biomarkers for response to tyrosine kinase pathway inhibitors in cancer |
| EP2812001B1 (en) | 2012-02-10 | 2017-06-14 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| CA2867282C (en) | 2012-03-12 | 2024-04-02 | Epizyme, Inc. | Inhibitors of human ezh2, and methods of use thereof |
| PL3184523T3 (pl) | 2012-04-13 | 2019-12-31 | Epizyme Inc | Bromowodorek N-((4,6-dimetylo-2-okso-1,2-dihydropirydyn-3-ylo)metylo)-5- (etylo(tetrahydro-2H-piran-4-ylo)amino)-4-metylo-4'-(morfolinometylo)-[1,1'- bifenylo]-3-karboksyamidu do zastosowania w leczeniu zaburzenia proliferacji komórkowej układu hematologicznego |
| RU2699546C2 (ru) | 2012-04-13 | 2019-09-06 | Эпизайм, Инк. | Комбинированная терапия для лечения рака |
| WO2013173441A2 (en) | 2012-05-16 | 2013-11-21 | Glaxosmithkline Llc | Enhancer of zeste homolog 2 inhibitors |
| EP2900653A1 (en) * | 2012-09-28 | 2015-08-05 | Pfizer Inc. | Benzamide and heterobenzamide compounds |
| BR112015008447A2 (pt) | 2012-10-15 | 2017-07-04 | Epizyme Inc | métodos para tratar câncer |
| SG10201705989YA (en) | 2012-10-15 | 2017-08-30 | Epizyme Inc | Substituted benzene compounds |
| CN103794728A (zh) | 2012-10-30 | 2014-05-14 | 中国科学院长春光学精密机械与物理研究所 | 高导电性有机透明导电薄膜的制备方法 |
| WO2014071109A1 (en) | 2012-11-01 | 2014-05-08 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using pi3 kinase isoform modulators |
| WO2014077784A1 (en) | 2012-11-19 | 2014-05-22 | Agency For Science, Technology And Research | Method of treating cancer |
| WO2014085666A1 (en) | 2012-11-27 | 2014-06-05 | Board Of Regents, The University Of Texas System | Methods of characterizing and treating molecular subset of muscle-invasive bladder cancer |
| US9895390B2 (en) | 2012-12-10 | 2018-02-20 | Children's Medical Center Corporation | Methods and assays for combination treatment of cancer |
| US20150313906A1 (en) | 2012-12-19 | 2015-11-05 | Glaxosmithkline Llc | Combination |
| UA111305C2 (uk) | 2012-12-21 | 2016-04-11 | Пфайзер Інк. | Конденсовані лактами арилу та гетероарилу |
| RS56207B1 (sr) | 2013-02-11 | 2017-11-30 | Constellation Pharmaceuticals Inc | Modulatori enzima koji modifikuju metil, njihove kompozicije i upotreba |
| EP2970305B1 (en) | 2013-03-15 | 2017-02-22 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| CA2910873A1 (en) * | 2013-04-30 | 2014-11-06 | Glaxosmithkline Intellectual Property (No.2) Limited | Enhancer of zeste homolog 2 inhibitors |
| US9624205B2 (en) * | 2013-07-19 | 2017-04-18 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| EP3033334A1 (en) * | 2013-08-15 | 2016-06-22 | Constellation Pharmaceuticals, Inc. | Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof |
| US9374093B2 (en) | 2014-01-10 | 2016-06-21 | Freescale Semiconductor, Inc. | Capacitively coupled input buffer |
| WO2015200650A1 (en) * | 2014-06-25 | 2015-12-30 | Epizyme, Inc. | Substituted benzene and 6,5-fused bicyclic heteroaryl compounds |
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