JP2015506985A5 - - Google Patents
Download PDFInfo
- 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
Links
- -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 (65)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2841142C (en) | 2010-06-23 | 2020-12-15 | Ryan D. Morin | Biomarkers for non-hodgkin lymphomas and uses thereof |
| US9051269B2 (en) | 2011-11-18 | 2015-06-09 | 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 |
| EP2953941B1 (en) * | 2013-02-11 | 2017-04-05 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| RS59541B1 (sr) | 2012-10-15 | 2019-12-31 | Epizyme Inc | Metodi lečenja kancera |
| WO2014151142A1 (en) * | 2013-03-15 | 2014-09-25 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| HK1214815A1 (zh) | 2013-04-30 | 2016-08-05 | Glaxosmithkline Intellectual Property (No. 2) Limited | Zeste增强子同源物2的抑制剂 |
| WO2015004618A1 (en) | 2013-07-10 | 2015-01-15 | Glaxosmithkline Intellectual Property (No.2) Limited | Enhancer of zeste homolog 2 inhibitors |
| 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 |
| US20170217941A1 (en) * | 2014-06-25 | 2017-08-03 | 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 |
| GB201421085D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | 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 |
| HK1256604A1 (zh) | 2015-08-03 | 2019-09-27 | Constellation Pharmaceuticals, Inc. | Ezh2抑制剂和调节性t细胞功能的调制 |
| WO2017025493A1 (en) * | 2015-08-12 | 2017-02-16 | Bayer Pharma Aktiengesellschaft | Quinoline ezh2 inhibitors |
| EP3341080A4 (en) | 2015-08-24 | 2019-03-20 | Epizyme Inc | METHOD FOR THE TREATMENT OF 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 |
| CN108699046A (zh) | 2015-10-06 | 2018-10-23 | Epizyme股份有限公司 | 用ezh2抑制剂治疗成神经管细胞瘤的方法 |
| 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 |
| EA201892075A1 (ru) | 2016-03-15 | 2019-04-30 | Оризон Дженомикс, С.А. | Комбинации ингибиторов lsd1 для применения для лечения солидных опухолей |
| IL263235B (en) | 2016-05-31 | 2022-07-01 | Kalvista Pharmaceuticals Ltd | History of pyrazoles as plasma kallikrein inhibitors |
| 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 |
| 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 |
| US11147819B2 (en) | 2016-06-17 | 2021-10-19 | Epizyme, Inc. | EZH2 inhibitors for treating cancer |
| WO2018075598A1 (en) | 2016-10-19 | 2018-04-26 | Constellation Pharmaceuticals, Inc. | Synthesis of inhibitors of ezh2 |
| WO2018102687A2 (en) | 2016-12-02 | 2018-06-07 | Epizyme, Inc. | Combination therapy for treating cancer |
| US20190381025A1 (en) * | 2017-01-20 | 2019-12-19 | 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 |
| WO2019014191A1 (en) | 2017-07-10 | 2019-01-17 | Constellation Pharmaceuticals, Inc. | GENE EXPRESSION INDUCED BY EZH2 INHIBITOR |
| WO2019094552A1 (en) | 2017-11-09 | 2019-05-16 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| US11529344B2 (en) | 2017-11-14 | 2022-12-20 | Pfizer Inc. | EZH2 inhibitor combination therapies |
| JP7078722B2 (ja) | 2017-11-29 | 2022-05-31 | カルビスタ・ファーマシューティカルズ・リミテッド | 血漿カリクレイン阻害剤を含む剤形 |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| 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 |
| US11485738B2 (en) | 2018-01-31 | 2022-11-01 | Mirati Therapeutics, Inc. | Substituted imidazo[1,2-c]pyrimidines as PRC2 inhibitors |
| MX2020009530A (es) | 2018-03-14 | 2021-01-15 | Biogen Ma Inc | Inhibidores de la o-glicoproteína-2-acetamido-2-desoxi-3-dglicopir anosidasa. |
| MY208662A (en) * | 2018-04-18 | 2025-05-22 | Constellation Pharmaceuticals Inc | Modulators of methyl modifying enzymes, compositions and uses thereof |
| CN112399857A (zh) | 2018-07-09 | 2021-02-23 | 盲人庇护基金会 | Prc2亚单位的抑制治疗眼失调 |
| AU2019344922B2 (en) | 2018-09-19 | 2025-02-06 | Biogen Ma Inc. | O-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors |
| AR116898A1 (es) * | 2018-10-30 | 2021-06-23 | H Lundbeck As | DERIVADOS DE ARILSULFONILPIRROLCARBOXAMIDA COMO ACTIVADORES DE CANALES DE POTASIO Kv3 |
| AR117252A1 (es) | 2018-12-05 | 2021-07-21 | Biogen Ma Inc | Inhibidores de o-glucoproteína-2-acetamido-2-desoxi-3-d-glucopiranosidasa de morfolinilo, piperazinilo, oxazepanilo y diazepanilo |
| 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 |
| US12522595B2 (en) | 2019-02-04 | 2026-01-13 | Biogen Ma Inc. | Bicyclic ether O-glycoprotein-2-acetamido-2-deoxy-3-D-glucopyranosidase inhibitors |
| EP3935055A1 (en) | 2019-03-08 | 2022-01-12 | Biogen MA Inc. | Azetidinyl 0-glyc0pr0tein-2-acetamid0-2-deoxy-3-d-gluc0pyran0sidase inhibitors |
| WO2020219448A1 (en) | 2019-04-22 | 2020-10-29 | Mirati Therapeutics, Inc. | Naphthyridine derivatives as prc2 inhibitors |
| US12252493B2 (en) | 2019-06-05 | 2025-03-18 | Mirati Therapeutics, Inc. | Imidazo[1,2-c]pyrimidine derivatives as PRC2 inhibitors for treating cancer |
| WO2021016409A1 (en) * | 2019-07-24 | 2021-01-28 | Constellation Pharmaceuticals, Inc. | Ezh2 inhibition in combination therapies for the treatment of cancers |
| WO2021016414A1 (en) | 2019-07-24 | 2021-01-28 | Constellation Pharmaceuticals, Inc. | Crystalline forms of 7-chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-2,4-dimethyl-n-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzo[d][1,3]dioxole-5-carboxamide |
| CN114206852A (zh) | 2019-08-09 | 2022-03-18 | 卡尔维斯塔制药有限公司 | 血浆激肽释放酶抑制剂 |
| KR20220066892A (ko) | 2019-08-22 | 2022-05-24 | 주노 쎄러퓨티크스 인코퍼레이티드 | Ｔ 세포 요법 및 제스트 동족체 2의 인핸서 (ｅｚｈ2) 억제제의 병용 요법 및 관련 방법 |
| JP2023501949A (ja) | 2019-10-29 | 2023-01-20 | バイオジェン・エムエイ・インコーポレイテッド | スピロ環ｏ－糖タンパク質－２－アセトアミド－２－デオキシ－３－ｄ－グルコピラノシダーゼ阻害剤 |
| IL300365A (en) | 2020-08-03 | 2023-04-01 | Biogen Ma Inc | Crystal forms of O-glycoprotein-2-acetamido-2-deoxy-3-D-glucopyranosidase inhibitor |
| 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 |
| HUP9904335A3 (en) | 1996-07-22 | 2001-07-30 | Daiichi Asubio Pharma Co Ltd | Arylpiperidinol and arylpiperidine derivatives and drugs containing the same |
| EA007062B1 (ru) | 2001-09-04 | 2006-06-30 | Бёрингер Ингельхайм Фарма Гмбх Унд Ко. Кг | Новые дигидроптеридиноны, способы их получения и их применение в качестве лекарственных средств |
| 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. |
| US7101883B2 (en) | 2002-03-18 | 2006-09-05 | Bristol-Myers Squibb Company | Uracil derivatives as inhibitors of TNF-α 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 |
| CN101014571A (zh) | 2004-01-30 | 2007-08-08 | 默克公司 | 用作hiv整合酶抑制剂的n－苄基－3,4－二羟基吡啶－2－羧酰胺类和n－苄基－2,3－二羟基吡啶－4－羧酰胺类化合物 |
| ZA200609259B (en) | 2004-04-30 | 2008-07-30 | Takeda Pharmaceutical | Heterocyclic amide compound and use thereof as an mmp-13 inhibitor |
| EP1765994B1 (en) | 2004-06-01 | 2009-11-18 | 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 |
| CA2617589A1 (en) | 2005-08-03 | 2007-02-08 | Boehringer Ingelheim International Gmbh | Dihydropteridinones in the treatment of respiratory diseases |
| CA2630597A1 (en) | 2005-12-08 | 2007-06-14 | Novartis Ag | Effects of inhibitors of fgfr3 on gene transcription |
| EP2913322A3 (en) | 2006-11-03 | 2015-11-11 | 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 |
| JP2010519204A (ja) | 2007-02-16 | 2010-06-03 | アムジエン・インコーポレーテツド | 窒素含有複素環ケトン類およびそれらのｃ−Ｍｅｔ阻害薬としての使用 |
| US8030344B2 (en) | 2007-03-13 | 2011-10-04 | Methylgene Inc. | Inhibitors of histone deacetylase |
| US20090012031A1 (en) | 2007-07-03 | 2009-01-08 | The Regents Of The University Of Michigan | EZH2 Cancer Markers |
| WO2009015203A1 (en) | 2007-07-23 | 2009-01-29 | 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. |
| US20100261743A1 (en) | 2007-12-06 | 2010-10-14 | Glaxosmithkline Llc | Novel seh inhibitors and their use |
| AR071069A1 (es) * | 2008-03-26 | 2010-05-26 | Takeda Pharmaceutical | Derivados sustituidos de pirazol y su uso para la prevencion o el tratamiento de cancer |
| JP2011524894A (ja) | 2008-06-18 | 2011-09-08 | ファイザー・リミテッド | ニコチンアミド誘導体 |
| WO2010056564A1 (en) | 2008-11-13 | 2010-05-20 | Merck Sharp & Dohme Corp. | Quinolone neuropeptide 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 |
| CA2795776A1 (en) | 2010-04-06 | 2011-10-13 | Caris Life Sciences Luxembourg Holdings, S.A.R.L. | Circulating biomarkers for disease |
| US8575203B2 (en) | 2010-04-21 | 2013-11-05 | Boehringer Ingelheim International Gmbh | Chemical compounds |
| EA023788B1 (ru) | 2010-05-07 | 2016-07-29 | ГЛЭКСОСМИТКЛАЙН ЭлЭлСи | Производные индола и фармацевтические композиции на их основе |
| JP5889875B2 (ja) | 2010-05-07 | 2016-03-22 | 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ＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ | アザインダゾール |
| JP5864546B2 (ja) | 2010-05-07 | 2016-02-17 | 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ＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ | インダゾール |
| EP2606353A4 (en) | 2010-08-18 | 2014-10-15 | Caris Life Sciences Luxembourg Holdings | CIRCULATING BIOMARKERS FOR DISEASES |
| AU2011298987B2 (en) * | 2010-09-10 | 2017-09-28 | Epizyme, Inc. | Inhibitors of human EZH2, and methods of use thereof |
| 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 |
| US20130310379A1 (en) | 2010-11-19 | 2013-11-21 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
| EP2646020B1 (en) | 2010-12-01 | 2016-09-21 | Glaxosmithkline LLC | Indoles |
| WO2012115885A1 (en) | 2011-02-22 | 2012-08-30 | Caris Life Sciences Luxembourg Holdings, S.A.R.L. | Circulating biomarkers |
| EP2681216B1 (en) * | 2011-02-28 | 2017-09-27 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| JO3438B1 (ar) * | 2011-04-13 | 2019-10-20 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| TW201733984A (zh) * | 2011-04-13 | 2017-10-01 | 雅酶股份有限公司 | 經取代之苯化合物 |
| WO2013039988A1 (en) | 2011-09-13 | 2013-03-21 | Glax0Smithkline Llc | Azaindazoles |
| CA2850570A1 (en) | 2011-09-30 | 2013-04-04 | Glaxosmithkline Llc | Methods of treating cancer |
| WO2013067296A1 (en) * | 2011-11-04 | 2013-05-10 | 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 |
| WO2013067300A1 (en) | 2011-11-04 | 2013-05-10 | Glaxosmithkline Intellectual Property (No. 2) Limited | Method of treatment |
| US9051269B2 (en) | 2011-11-18 | 2015-06-09 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| US9206128B2 (en) | 2011-11-18 | 2015-12-08 | 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 |
| EP2953941B1 (en) | 2013-02-11 | 2017-04-05 | 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 |
| DK2825161T3 (en) | 2012-03-12 | 2019-04-08 | Epizyme Inc | HUMAN EZH2 INHIBITORS AND PROCEDURES FOR USING IT |
| SG10201912111TA (en) | 2012-04-13 | 2020-02-27 | Epizyme Inc | Combination therapy for treating cancer |
| RS59392B1 (sr) | 2012-04-13 | 2019-11-29 | Epizyme Inc | N-((4,6-dimetil-2-okso-l,2-dihidropiridin-3-il)metil)-5-(etil(tetrahidro-2h-piran-4-il)amino)-4-metil-4’ (morfolinometil)-[l,1’-bifenil]-3-karboksamid hidrobromid za upotrebu u lečenju proliferativnih poremećaja ćelija hematološkog sistema |
| US9562041B2 (en) | 2012-05-16 | 2017-02-07 | Glaxosmithkline Llc | Enhancer of zeste homolog 2 inhibitors |
| JP6254169B2 (ja) | 2012-09-28 | 2017-12-27 | ファイザー・インク | ベンズアミドおよびヘテロベンズアミド化合物 |
| HK1213552A1 (zh) | 2012-10-15 | 2016-07-08 | Epizyme, Inc. | 经取代的苯化合物 |
| RS59541B1 (sr) | 2012-10-15 | 2019-12-31 | Epizyme Inc | Metodi lečenja kancera |
| 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 |
| MX386085B (es) | 2012-11-01 | 2025-03-18 | Infinity Pharmaceuticals Inc | Tratamiento de canceres utilizando moduladores de las isoformas de pi3 cinasa |
| EP2908843B1 (en) | 2012-11-19 | 2019-09-04 | Agency For Science, Technology And Research | 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 |
| WO2014151142A1 (en) * | 2013-03-15 | 2014-09-25 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| HK1214815A1 (zh) * | 2013-04-30 | 2016-08-05 | Glaxosmithkline Intellectual Property (No. 2) Limited | Zeste增强子同源物2的抑制剂 |
| 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 |
| US20170217941A1 (en) * | 2014-06-25 | 2017-08-03 | Epizyme, Inc. | Substituted benzene and 6,5-fused bicyclic heteroaryl compounds |
-
2013
- 2013-02-11 EP EP13746186.9A patent/EP2812001B1/en active Active
- 2013-02-11 NZ NZ628762A patent/NZ628762A/en unknown
- 2013-02-11 CA CA2862289A patent/CA2862289C/en active Active
- 2013-02-11 AU AU2013216721A patent/AU2013216721B2/en active Active
- 2013-02-11 WO PCT/US2013/025639 patent/WO2013120104A2/en not_active Ceased
- 2013-02-11 JP JP2014556793A patent/JP5989805B2/ja active Active
- 2013-02-11 US US14/377,214 patent/US9085583B2/en active Active
-
2014
- 2014-02-11 LT LTEP14708987.4T patent/LT2953941T/lt unknown
- 2014-02-11 BR BR112015018508-8A patent/BR112015018508B1/pt active IP Right Grant
- 2014-02-11 MY MYPI2015001865A patent/MY172156A/en unknown
- 2014-02-11 UA UAA201508755A patent/UA117362C2/uk unknown
- 2014-02-11 JP JP2015557190A patent/JP5989923B2/ja active Active
- 2014-02-11 ES ES14708987.4T patent/ES2632241T3/es active Active
- 2014-02-11 MX MX2015010377A patent/MX363392B/es unknown
- 2014-02-11 HR HRP20171030TT patent/HRP20171030T1/hr unknown
- 2014-02-11 SM SM20170340T patent/SMT201700340T1/it unknown
- 2014-02-11 DK DK14708987.4T patent/DK2953941T3/en active
- 2014-02-11 US US14/766,632 patent/US20150376190A1/en not_active Abandoned
- 2014-02-11 EA EA201591474A patent/EA029089B9/ru unknown
- 2014-02-11 AR ARP140100433A patent/AR094755A1/es active IP Right Grant
- 2014-02-11 PT PT147089874T patent/PT2953941T/pt unknown
-
2015
- 2015-03-18 US US14/661,797 patent/US9371331B2/en active Active
- 2015-08-28 US US14/839,273 patent/US9469646B2/en not_active Ceased
-
2016
- 2016-05-16 US US15/155,749 patent/US9980952B2/en active Active
- 2016-09-06 US US15/257,275 patent/US10016405B2/en active Active
-
2017
- 2017-07-05 CY CY20171100718T patent/CY1119060T1/el unknown
-
2018
- 2018-01-24 US US15/878,663 patent/USRE47428E1/en active Active
- 2018-05-31 US US15/994,005 patent/US20190125737A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2015506985A5 (enExample) | ||
| RU2017125025A (ru) | Конденсированные кольцевые гетероарильные соединения и их применение в качестве ингибиторов trk | |
| EA201001126A1 (ru) | Пирролопиримидины и пирролопиридины | |
| JP2015535277A5 (enExample) | ||
| JP2014508811A5 (enExample) | ||
| JP2018519323A5 (enExample) | ||
| MY145465A (en) | Diaminopyrimidines as p2x3 and p2x2/3 antagonists. | |
| TW200716648A (en) | Heterocycles as nicotinic acid receptor agonists for the treatment of dyslipidemia | |
| JP2016516043A5 (enExample) | ||
| EA200970856A1 (ru) | Ингибиторы пути хеджхога | |
| JP2017511321A5 (enExample) | ||
| JP2017519781A5 (enExample) | ||
| JP2017501237A5 (enExample) | ||
| EA201071232A1 (ru) | Триазины как ингибиторы киназы pi3 и mtor | |
| EA201290260A1 (ru) | Бензимидазол-имидазольные производные | |
| PE20090506A1 (es) | DERIVADOS DE IMIDAZO-[1,2-b]-PIRIDAZIN COMO INHIBIDORES DE ALK5 Y/O ALK4 | |
| JP2011515397A5 (enExample) | ||
| JP2014520898A5 (enExample) | ||
| JP2013542261A5 (enExample) | ||
| EA201001687A1 (ru) | Производные имидазопиридина в качестве ингибиторов активиноподобной рецепторной киназы ( alk-4 или alk-5 ) | |
| RU2012134306A (ru) | Азотосодержащие производные гетероарилов | |
| RU2015143843A (ru) | Ингибиторы гистондеацетилазы | |
| JP2010532387A5 (enExample) | ||
| JP2013523814A5 (enExample) | ||
| PE20141167A1 (es) | Piridopirazinas sustituidas como inhibidores novedosos de ptk |