JP2015531366A5 - - Google Patents
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- Publication number
- JP2015531366A5 JP2015531366A5 JP2015533726A JP2015533726A JP2015531366A5 JP 2015531366 A5 JP2015531366 A5 JP 2015531366A5 JP 2015533726 A JP2015533726 A JP 2015533726A JP 2015533726 A JP2015533726 A JP 2015533726A JP 2015531366 A5 JP2015531366 A5 JP 2015531366A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- methyl
- alkoxy
- group
- halo
- 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
- 125000001072 heteroaryl group Chemical group 0.000 claims 28
- 125000000623 heterocyclic group Chemical group 0.000 claims 24
- 125000005843 halogen group Chemical group 0.000 claims 19
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 125000003118 aryl group Chemical group 0.000 claims 15
- 229910052799 carbon Inorganic materials 0.000 claims 15
- -1 —OH Chemical group 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 12
- 229910052760 oxygen Inorganic materials 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 4
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 3
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 3
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 3
- 125000006731 (C1-C8) thioalkoxy group Chemical group 0.000 claims 2
- 230000002159 abnormal effect Effects 0.000 claims 2
- KXDAEFPNCMNJSK-UHFFFAOYSA-N benzene carboxamide Natural products NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 2
- 230000010261 cell growth Effects 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims 2
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- LMABPVOSHFLTJO-UHFFFAOYSA-N 5-[2-(dimethylamino)pyrimidin-5-yl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-3-(2-methylpyrazol-3-yl)benzamide Chemical compound CN(C1=NC=C(C=N1)C=1C=C(C(=C(C(=O)NCC=2C(NC(=CC2C)C)=O)C1)C)C1=CC=NN1C)C LMABPVOSHFLTJO-UHFFFAOYSA-N 0.000 claims 1
- VUNABXRMGVXNIV-UHFFFAOYSA-N N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-(2,4-dimethylpyrazol-3-yl)-2-methyl-5-(2-morpholin-4-ylpyrimidin-5-yl)benzamide Chemical compound CC1=C(C(NC(=C1)C)=O)CNC(C1=C(C(=CC(=C1)C=1C=NC(=NC1)N1CCOCC1)C1=C(C=NN1C)C)C)=O VUNABXRMGVXNIV-UHFFFAOYSA-N 0.000 claims 1
- KLBUHKIAUSWYNS-UHFFFAOYSA-N N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-(2,4-dimethylpyrazol-3-yl)-2-methyl-5-[2-(methylamino)pyrimidin-5-yl]benzamide Chemical compound CC1=C(C(NC(=C1)C)=O)CNC(C1=C(C(=CC(=C1)C=1C=NC(=NC1)NC)C1=C(C=NN1C)C)C)=O KLBUHKIAUSWYNS-UHFFFAOYSA-N 0.000 claims 1
- RGZWOLWVDDAMHM-UHFFFAOYSA-N N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-(2,4-dimethylpyrazol-3-yl)-5-[2-(3-fluoroazetidin-1-yl)pyrimidin-5-yl]-2-methylbenzamide Chemical compound CC1=C(C(NC(=C1)C)=O)CNC(C1=C(C(=CC(=C1)C=1C=NC(=NC1)N1CC(C1)F)C1=C(C=NN1C)C)C)=O RGZWOLWVDDAMHM-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 1
- 229940127084 other anti-cancer agent Drugs 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261707447P | 2012-09-28 | 2012-09-28 | |
| US61/707,447 | 2012-09-28 | ||
| PCT/IB2013/058580 WO2014049488A1 (en) | 2012-09-28 | 2013-09-16 | Benzamide and heterobenzamide compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015531366A JP2015531366A (ja) | 2015-11-02 |
| JP2015531366A5 true JP2015531366A5 (enExample) | 2016-09-23 |
| JP6254169B2 JP6254169B2 (ja) | 2017-12-27 |
Family
ID=49681084
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015533726A Expired - Fee Related JP6254169B2 (ja) | 2012-09-28 | 2013-09-16 | ベンズアミドおよびヘテロベンズアミド化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US20150239842A1 (enExample) |
| EP (1) | EP2900653A1 (enExample) |
| JP (1) | JP6254169B2 (enExample) |
| CA (1) | CA2884848C (enExample) |
| WO (1) | WO2014049488A1 (enExample) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| UA111305C2 (uk) | 2012-12-21 | 2016-04-11 | Пфайзер Інк. | Конденсовані лактами арилу та гетероарилу |
| US9745305B2 (en) | 2013-03-15 | 2017-08-29 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| US9969716B2 (en) | 2013-08-15 | 2018-05-15 | Constellation Pharmaceuticals, Inc. | Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof |
| GB201316600D0 (en) * | 2013-09-18 | 2013-10-30 | Redx Pharma Ltd | Agricultural chemicals |
| 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 |
| CN105037360B (zh) * | 2014-04-28 | 2016-08-17 | 四川大学 | 吡啶酮衍生物及其制备方法和用途 |
| WO2015179697A1 (en) * | 2014-05-21 | 2015-11-26 | Taxis Pharmaceuticals, Inc. | Compounds for the treatment of bacterial infections |
| TN2016000529A1 (en) | 2014-06-17 | 2018-04-04 | Pfizer | Substituted dihydroisoquinolinone compounds |
| WO2015193768A1 (en) * | 2014-06-17 | 2015-12-23 | Pfizer Inc. | Aryl fused lactams as ezh2 modulators |
| AR102767A1 (es) | 2014-12-05 | 2017-03-22 | Lilly Co Eli | Inhibidores de ezh2 |
| EP3230281B1 (en) | 2014-12-09 | 2021-05-26 | Bayer Aktiengesellschaft | 1,3-thiazol-2-yl substituted benzamides |
| US10183937B2 (en) * | 2014-12-09 | 2019-01-22 | Bayer Aktiengesellschaft | 1,3-thiazol-2-yl substituted benzamides |
| EP3236962A2 (en) | 2014-12-23 | 2017-11-01 | University of Copenhagen | Treatment of cancer by inhibiting ezh2 activity |
| 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 |
| CN106496130B (zh) * | 2016-09-09 | 2019-09-20 | 苏州大学 | 一种甲基酮衍生物及其制备方法与应用 |
| CN109843870A (zh) | 2016-10-19 | 2019-06-04 | 星座制药公司 | Ezh2抑制剂的合成 |
| US10266542B2 (en) | 2017-03-15 | 2019-04-23 | Mirati Therapeutics, Inc. | EZH2 inhibitors |
| BR112020008325A2 (pt) | 2017-11-14 | 2020-10-20 | Pfizer Inc. | terapias de combinação com o inibidor de ezh2 |
| MX2020007974A (es) | 2018-01-31 | 2020-09-07 | Mirati Therapeutics Inc | Inhibidores de complejo represivo polycomb 2 (prc2). |
| EP3823671B1 (en) | 2018-07-09 | 2024-02-07 | Fondation Asile Des Aveugles | Inhibition of prc2 subunits to treat eye disorders |
| EP3831822A4 (en) * | 2018-07-27 | 2022-03-23 | Suzhou Sinovent Pharmaceuticals Co., Ltd. | POLY-SUBSTITUTED BENZENE COMPOUND, PROCESS OF MANUFACTURE AND USE THEREOF |
| WO2020192652A1 (zh) * | 2019-03-25 | 2020-10-01 | 上海华汇拓医药科技有限公司 | 酰胺类化合物制备方法及其在医药领域的应用 |
| 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 |
| MX2023001384A (es) * | 2020-08-06 | 2023-04-26 | Chdi Foundation Inc | Compuestos de heterobiarilo y agentes de imagenologia para imagenologia de proteina huntingtina. |
| JP7785375B2 (ja) | 2020-10-13 | 2025-12-15 | エボポイント、バイオサイエンシズ、カンパニー、リミテッド | 多置換ベンゼン環化合物マレイン酸塩の結晶形、その調製方法及びその用途 |
| CN115093400B (zh) * | 2021-09-18 | 2023-09-05 | 北京华森英诺生物科技有限公司 | AhR抑制剂及其用途和制备方法 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| GB9518953D0 (en) | 1995-09-15 | 1995-11-15 | Pfizer Ltd | Pharmaceutical formulations |
| WO2000035296A1 (en) | 1996-11-27 | 2000-06-22 | Wm. Wrigley Jr. Company | Improved release of medicament active agents from a chewing gum coating |
| GB9711643D0 (en) | 1997-06-05 | 1997-07-30 | Janssen Pharmaceutica Nv | Glass thermoplastic systems |
| ATE355273T1 (de) | 2003-05-12 | 2006-03-15 | Pfizer Prod Inc | Benzamidinhibitoren des p2x7-rezeptors |
| UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| WO2012005805A1 (en) * | 2010-05-07 | 2012-01-12 | Glaxosmithkline Llc | Azaindazoles |
| 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 |
| EA023788B1 (ru) * | 2010-05-07 | 2016-07-29 | ГЛЭКСОСМИТКЛАЙН ЭлЭлСи | Производные индола и фармацевтические композиции на их основе |
| 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 |
| RU2704445C2 (ru) * | 2012-03-12 | 2019-10-28 | Эпизайм, Инк. | Ингибиторы ezh2 человека и способы их применения |
| US9562041B2 (en) * | 2012-05-16 | 2017-02-07 | Glaxosmithkline Llc | Enhancer of zeste homolog 2 inhibitors |
-
2013
- 2013-09-16 CA CA2884848A patent/CA2884848C/en not_active Expired - Fee Related
- 2013-09-16 WO PCT/IB2013/058580 patent/WO2014049488A1/en not_active Ceased
- 2013-09-16 US US14/430,799 patent/US20150239842A1/en not_active Abandoned
- 2013-09-16 JP JP2015533726A patent/JP6254169B2/ja not_active Expired - Fee Related
- 2013-09-16 EP EP13798742.6A patent/EP2900653A1/en not_active Withdrawn
-
2017
- 2017-02-06 US US15/425,732 patent/US20170152239A1/en not_active Abandoned
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