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 (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011160206A1 (en) | 2010-06-23 | 2011-12-29 | Morin Ryan D | 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 |
| JP5989805B2 (ja) | 2012-02-10 | 2016-09-07 | 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． | メチル基変更酵素の調節物質、組成物及びその使用 |
| CA2887243C (en) | 2012-10-15 | 2024-04-09 | Epizyme, Inc. | Methods of treating cancer |
| MA38341B1 (fr) * | 2013-02-11 | 2018-11-30 | Constellation Pharmaceuticals Inc | Modulateurs d'enzymes de modification par méthylation, compositions et utilisations associées |
| US9745305B2 (en) | 2013-03-15 | 2017-08-29 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| WO2014177982A1 (en) | 2013-04-30 | 2014-11-06 | Glaxosmithkline Intellectual Property (No.2) Limited | Enhancer of zeste homolog 2 inhibitors |
| AU2014288839B2 (en) | 2013-07-10 | 2017-02-02 | 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 |
| US9969716B2 (en) * | 2013-08-15 | 2018-05-15 | 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 |
| BR112017008840A2 (pt) * | 2014-10-28 | 2017-12-19 | Glaxosmithkline Ip No 2 Ltd | intensificador de inibidores do homólogo 2 de zeste |
| 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 |
| AR102767A1 (es) | 2014-12-05 | 2017-03-22 | Lilly Co Eli | Inhibidores de ezh2 |
| WO2016130396A1 (en) * | 2015-02-13 | 2016-08-18 | 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 |
| US20180214519A1 (en) | 2015-07-24 | 2018-08-02 | Constellation Pharmaceuticals, Inc. | Combination therapies for modulation of histone methyl modifying enzymes |
| WO2017023671A1 (en) | 2015-08-03 | 2017-02-09 | Constellation Pharmaceuticals, Inc. | Ezh2 inhibitors and modulation of regulatory t-cell function |
| WO2017025493A1 (en) * | 2015-08-12 | 2017-02-16 | Bayer Pharma Aktiengesellschaft | Quinoline ezh2 inhibitors |
| KR20180042356A (ko) | 2015-08-24 | 2018-04-25 | 에피자임, 인코포레이티드 | 암 치료 방법 |
| TW201718598A (zh) | 2015-08-27 | 2017-06-01 | 美國禮來大藥廠 | Ｅｚｈ２抑制劑 |
| US10577350B2 (en) * | 2015-08-28 | 2020-03-03 | 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 |
| MX394355B (es) | 2015-10-06 | 2025-03-24 | Epizyme Inc | Método de tratamiento de meduloblastoma con un inhibidor de ezh2. |
| EP3371601A1 (en) | 2015-11-05 | 2018-09-12 | Epizyme Inc | Flow cytometry for monitoring histone h3 methylation status |
| WO2017132518A1 (en) | 2016-01-29 | 2017-08-03 | Epizyme, Inc. | Combination therapy for treating cancer |
| ES3057783T3 (en) | 2016-03-15 | 2026-03-04 | Oryzon Genomics Sa | Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases |
| DK3464271T3 (da) | 2016-05-31 | 2020-06-15 | Kalvista Pharmaceuticals Ltd | Pyrazolderivater som plasma-kallikreininhibitorer |
| 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 |
| EP3471830A4 (en) | 2016-06-17 | 2020-02-26 | Epizyme Inc | EZH2 INHIBITORS TO TREAT CANCER |
| CN109843870A (zh) * | 2016-10-19 | 2019-06-04 | 星座制药公司 | Ezh2抑制剂的合成 |
| EP3548032A2 (en) | 2016-12-02 | 2019-10-09 | 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 |
| US11642346B2 (en) | 2017-03-31 | 2023-05-09 | Epizyme, Inc. | Combination therapy for treating cancer |
| US20230201212A1 (en) | 2017-06-13 | 2023-06-29 | 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 |
| BR112020008325A2 (pt) | 2017-11-14 | 2020-10-20 | Pfizer Inc. | terapias de combinação com o inibidor de ezh2 |
| PT3716952T (pt) | 2017-11-29 | 2022-04-14 | Kalvista Pharmaceuticals Ltd | Formas de administração que incluem um inibidor de calicreína plasmática |
| 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 |
| MX2020007974A (es) | 2018-01-31 | 2020-09-07 | Mirati Therapeutics Inc | Inhibidores de complejo represivo polycomb 2 (prc2). |
| JP7453916B2 (ja) | 2018-03-14 | 2024-03-21 | バイオジェン・エムエイ・インコーポレイテッド | Ｏ－糖タンパク質－２－アセトアミド－２－デオキシ－３－ｄ－グリコピラノシダーゼ阻害剤 |
| HRP20240793T1 (hr) | 2018-04-18 | 2024-09-13 | Constellation Pharmaceuticals, Inc. | Modulatori enzima koji modificiraju metil, njihovi pripravci i upotreba |
| EP3823671B1 (en) | 2018-07-09 | 2024-02-07 | Fondation Asile Des Aveugles | Inhibition of prc2 subunits to treat eye disorders |
| US12180205B2 (en) | 2018-09-19 | 2024-12-31 | 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 |
| ES2968733T3 (es) | 2018-12-05 | 2024-05-13 | Biogen Ma Inc | Derivados morfolinilo, piperazinilo, oxazepanilo y diazepanilo útiles como inhibidores de o-glicoproteína-2-acetamido-2-desoxi-3-d-glucopiranosidasa |
| 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 |
| JP7504898B2 (ja) | 2019-02-04 | 2024-06-24 | バイオジェン・エムエイ・インコーポレイテッド | 二環式エーテル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 |
| JP7663503B2 (ja) | 2019-03-08 | 2025-04-16 | バイオジェン・エムエイ・インコーポレイテッド | アゼチジニル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 |
| US12421228B2 (en) | 2019-04-22 | 2025-09-23 | Mirati Therapeutics, Inc. | Naphthyridine derivatives as PRC2 inhibitors |
| EP3980422A1 (en) | 2019-06-05 | 2022-04-13 | Mirati Therapeutics, Inc. | Imidazo[1,2-c]pyrimidine derivatives as prc2 inhibitors for treating cancer |
| LT4003532T (lt) | 2019-07-24 | 2024-11-11 | Constellation Pharmaceuticals, Inc. | 7-chlor-2- (4-(3-metoksiazetidin-1-il)cikloheksil)-2,4-dimetil-n-((6-metil-4-(metiltio)-2-okso-1,2-dihidropiridin-3-il)metil)benzo[d][1,3]dioksol-5-karboksamido kristalinės formos |
| MX2022000933A (es) * | 2019-07-24 | 2022-05-06 | Constellation Pharmaceuticals Inc | Inhibición de ezh2 en tratamientos combinados para el tratamiento del cáncer. |
| EP4010333A1 (en) | 2019-08-09 | 2022-06-15 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
| CN114555112A (zh) | 2019-08-22 | 2022-05-27 | 朱诺治疗学股份有限公司 | T细胞疗法和zeste增强子同源物2(ezh2)抑制剂的组合疗法及相关方法 |
| AR120324A1 (es) | 2019-10-29 | 2022-02-09 | Biogen Ma Inc | Inhibidores de o-glucoproteína-2-acetamido-2-deoxi-3-d-glucopiranosidasa espirocíclica |
| WO2022031701A1 (en) | 2020-08-03 | 2022-02-10 | Biogen Ma Inc. | Crystaline forms of an 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 |
| IL308348A (en) | 2021-05-20 | 2024-01-01 | Sironax Ltd | RIP1 modulators including cyclic ureas aztidine, their preparation and uses |
| WO2023115203A1 (en) * | 2021-12-20 | 2023-06-29 | Fairhaven Pharmaceuticals Inc. | Oxer1 antagonists 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 |
| AU710594B2 (en) | 1996-07-22 | 1999-09-23 | Asubio Pharma Co., Ltd. | Arylpiperidinol and arylpiperidine derivatives and pharmaceuticals containing the same |
| UA76512C2 (en) | 2001-09-04 | 2006-08-15 | Boehringer Ingelheim Pharma | Dihydropteridinones, a method for producing thereof and use thereof as medicament |
| 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 |
| WO2005074513A2 (en) | 2004-01-30 | 2005-08-18 | Merck & Co., Inc. | N-benzyl-3,4-dihyroxypyridine-2-carboxamide and n-benzyl-2,3-dihydroxypyridine-4-carboxamide compounds useful as hiv integrase inhibitors |
| 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 |
| EA200800321A1 (ru) * | 2005-07-14 | 2008-06-30 | Такеда Сан Диего, Инк. | Ингибиторы гистондеацетилазы |
| CA2617589A1 (en) | 2005-08-03 | 2007-02-08 | Boehringer Ingelheim International Gmbh | Dihydropteridinones in the treatment of respiratory diseases |
| KR20080080525A (ko) | 2005-12-08 | 2008-09-04 | 노파르티스 아게 | 유전자 전사에 대한 ｆｇｆｒ３의 억제제의 효과 |
| JP5277171B2 (ja) | 2006-11-03 | 2013-08-28 | コリア リサーチ インスティテュート オブ ケミカル テクノロジーズ | ヒストン脱アセチル化酵素阻害活性を有するナフタレニルオキシプロペニル誘導体およびこれを含む薬学組成物 |
| AU2008206168B2 (en) | 2007-01-19 | 2012-01-19 | The Regents Of The University Of Michigan | ADRB2 cancer markers |
| MX2009008531A (es) | 2007-02-16 | 2009-08-26 | Amgen Inc | Cetonas de heterociclilo que contienen nitrogeno y su uso como inhibidores de c-met. |
| 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 |
| 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. |
| EP2224928A4 (en) | 2007-12-06 | 2012-02-15 | Glaxosmithkline Llc | NOVEL INHIBITORS OF SEH AND THEIR USE |
| PE20091653A1 (es) * | 2008-03-26 | 2009-11-14 | Takeda Pharmaceutical | Derivados sustituidos de pirazol y su uso |
| CA2725481A1 (en) | 2008-06-18 | 2009-12-23 | Pfizer Limited | Nicotinamide derivatives |
| US8389720B2 (en) | 2008-11-13 | 2013-03-05 | 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 |
| JP2013526852A (ja) | 2010-04-06 | 2013-06-27 | 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 | 疾患に対する循環バイオマーカー |
| 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 |
| 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 |
| WO2012005805A1 (en) | 2010-05-07 | 2012-01-12 | Glaxosmithkline Llc | Azaindazoles |
| CA2808417A1 (en) | 2010-08-18 | 2012-02-23 | Caris Life Sciences Luxembourg Holdings, S.A.R.L. | Circulating biomarkers for disease |
| US9175331B2 (en) | 2010-09-10 | 2015-11-03 | Epizyme, Inc. | Inhibitors of human EZH2, and methods of use thereof |
| 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 |
| 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 |
| EP2678448A4 (en) | 2011-02-22 | 2014-10-01 | Caris Life Sciences Luxembourg Holdings S A R L | CIRCULATING BIOMARKERS |
| 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 |
| JO3363B1 (ar) * | 2011-04-13 | 2019-03-13 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| EP2755962B1 (en) * | 2011-09-13 | 2017-03-01 | Glaxosmithkline LLC | Azaindazoles |
| CA2850570A1 (en) | 2011-09-30 | 2013-04-04 | Glaxosmithkline Llc | Methods of treating cancer |
| CN104039956A (zh) | 2011-11-04 | 2014-09-10 | 葛兰素史密斯克莱知识产权（第2号）有限公司 | 治疗方法 |
| WO2013067300A1 (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 |
| EP2780014A4 (en) | 2011-11-18 | 2015-07-01 | Constellation Pharmaceuticals Inc | MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF |
| US9051269B2 (en) | 2011-11-18 | 2015-06-09 | 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 |
| JP5989805B2 (ja) * | 2012-02-10 | 2016-09-07 | 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． | メチル基変更酵素の調節物質、組成物及びその使用 |
| RU2704445C2 (ru) | 2012-03-12 | 2019-10-28 | Эпизайм, Инк. | Ингибиторы ezh2 человека и способы их применения |
| US9394283B2 (en) | 2012-04-13 | 2016-07-19 | Epizyme, Inc. | Salt form of a human histone methyltransferase EZH2 inhibitor |
| SG10201608579UA (en) | 2012-04-13 | 2016-12-29 | Epizyme Inc | Combination therapy for treating cancer |
| US9562041B2 (en) | 2012-05-16 | 2017-02-07 | Glaxosmithkline Llc | Enhancer of zeste homolog 2 inhibitors |
| CA2884848C (en) * | 2012-09-28 | 2017-08-22 | Pfizer Inc. | Benzamide and heterobenzamide compounds |
| PE20150887A1 (es) | 2012-10-15 | 2015-06-04 | Epizyme Inc | Compuestos de benceno sustituidos |
| CA2887243C (en) | 2012-10-15 | 2024-04-09 | Epizyme, Inc. | Methods of treating cancer |
| 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 |
| AU2013337717B2 (en) | 2012-11-01 | 2018-10-25 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using PI3 kinase isoform modulators |
| US9889180B2 (en) | 2012-11-19 | 2018-02-13 | Agency For Science, Technology And Research | Method of treating cancer |
| US20150292030A1 (en) | 2012-11-27 | 2015-10-15 | Board Of Regents, The University Of Texas System | Methods of characterizing and treating molecular subset of muscle-invasive bladder cancer |
| WO2014092905A1 (en) | 2012-12-10 | 2014-06-19 | 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 |
| MA38341B1 (fr) | 2013-02-11 | 2018-11-30 | Constellation Pharmaceuticals Inc | Modulateurs d'enzymes de modification par méthylation, compositions et utilisations associées |
| US9745305B2 (en) | 2013-03-15 | 2017-08-29 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| WO2014177982A1 (en) * | 2013-04-30 | 2014-11-06 | Glaxosmithkline Intellectual Property (No.2) Limited | Enhancer of zeste homolog 2 inhibitors |
| EP3022195A2 (en) * | 2013-07-19 | 2016-05-25 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| US9969716B2 (en) | 2013-08-15 | 2018-05-15 | 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 JP JP2014556793A patent/JP5989805B2/ja active Active
- 2013-02-11 EP EP13746186.9A patent/EP2812001B1/en active Active
- 2013-02-11 WO PCT/US2013/025639 patent/WO2013120104A2/en not_active Ceased
- 2013-02-11 US US14/377,214 patent/US9085583B2/en active Active
- 2013-02-11 AU AU2013216721A patent/AU2013216721B2/en active Active
- 2013-02-11 CA CA2862289A patent/CA2862289C/en active Active
- 2013-02-11 NZ NZ628762A patent/NZ628762A/en unknown
-
2014
- 2014-02-11 HR HRP20171030TT patent/HRP20171030T1/hr unknown
- 2014-02-11 UA UAA201508755A patent/UA117362C2/uk unknown
- 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 ES ES14708987.4T patent/ES2632241T3/es active Active
- 2014-02-11 DK DK14708987.4T patent/DK2953941T3/en active
- 2014-02-11 PT PT147089874T patent/PT2953941T/pt unknown
- 2014-02-11 AR ARP140100433A patent/AR094755A1/es active IP Right Grant
- 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 LT LTEP14708987.4T patent/LT2953941T/lt unknown
- 2014-02-11 JP JP2015557190A patent/JP5989923B2/ja active Active
- 2014-02-11 MX MX2015010377A patent/MX363392B/es unknown
- 2014-02-11 SM SM20170340T patent/SMT201700340T1/it 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) | ||
| JP2016501185A5 (enExample) | ||
| JP2018519323A5 (enExample) | ||
| TW200716648A (en) | Heterocycles as nicotinic acid receptor agonists for the treatment of dyslipidemia | |
| JP2016516043A5 (enExample) | ||
| EA201170520A1 (ru) | Ингибитор p38 mapk-киназы | |
| EA200970856A1 (ru) | Ингибиторы пути хеджхога | |
| JP2017519781A5 (enExample) | ||
| JP2017511321A5 (enExample) | ||
| EA201071232A1 (ru) | Триазины как ингибиторы киназы pi3 и mtor | |
| EA201000615A1 (ru) | Производные имидазо[1,2-а]пиридина, применимые в качестве ингибиторов апк (активиноподобной киназы) | |
| EA201290260A1 (ru) | Бензимидазол-имидазольные производные | |
| JP2011132222A5 (enExample) | ||
| JP2014520898A5 (enExample) | ||
| EA201001687A1 (ru) | Производные имидазопиридина в качестве ингибиторов активиноподобной рецепторной киназы ( alk-4 или alk-5 ) | |
| JP2013542261A5 (enExample) | ||
| RU2012134306A (ru) | Азотосодержащие производные гетероарилов | |
| RU2015143843A (ru) | Ингибиторы гистондеацетилазы | |
| JP2015515961A5 (enExample) | ||
| JP2010532387A5 (enExample) | ||
| JP2013523814A5 (enExample) |