JP2017533250A5 - - Google Patents
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- Publication number
- JP2017533250A5 JP2017533250A5 JP2017525079A JP2017525079A JP2017533250A5 JP 2017533250 A5 JP2017533250 A5 JP 2017533250A5 JP 2017525079 A JP2017525079 A JP 2017525079A JP 2017525079 A JP2017525079 A JP 2017525079A JP 2017533250 A5 JP2017533250 A5 JP 2017533250A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- heterocyclyl
- carbocyclyl
- optionally substituted
- independently selected
- 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
- 0 *c1cc(C(Cl=*)=CN(*)C2=O)c2[n]1 Chemical compound *c1cc(C(Cl=*)=CN(*)C2=O)c2[n]1 0.000 description 34
- UQUHZULWYMQRSS-SNAWJCMRSA-N C/C=C/CN(C=C(C(N(CC1)CCC1N(C)C)=O)c1c2[nH]cc1)C2=O Chemical compound C/C=C/CN(C=C(C(N(CC1)CCC1N(C)C)=O)c1c2[nH]cc1)C2=O UQUHZULWYMQRSS-SNAWJCMRSA-N 0.000 description 1
- LUCLJGBDSYDVPO-UHFFFAOYSA-N C/S=C/C(N(CC1)CCC1C1=CC(F)=CC#CC1)=O Chemical compound C/S=C/C(N(CC1)CCC1C1=CC(F)=CC#CC1)=O LUCLJGBDSYDVPO-UHFFFAOYSA-N 0.000 description 1
- YYJHYDDYSZUMOR-UHFFFAOYSA-N CC(C)c(cc1)ccc1N(CC1)CCC1N(C)C(C(c1c2[nH]cc1)=CN(C)C2=O)=O Chemical compound CC(C)c(cc1)ccc1N(CC1)CCC1N(C)C(C(c1c2[nH]cc1)=CN(C)C2=O)=O YYJHYDDYSZUMOR-UHFFFAOYSA-N 0.000 description 1
- HDZPZWTWOZYVDA-UHFFFAOYSA-N CC(C)c1cccc(N(CC2)CCC2N(C)C(C2=CN(C)C(C)c3c2cc[nH]3)=O)c1 Chemical compound CC(C)c1cccc(N(CC2)CCC2N(C)C(C2=CN(C)C(C)c3c2cc[nH]3)=O)c1 HDZPZWTWOZYVDA-UHFFFAOYSA-N 0.000 description 1
- LEMGAKAAUNGWHX-UHFFFAOYSA-N CC(CC1)CCN1C(C(c1c2[nH]cc1)=CN(C)C2=O)=O Chemical compound CC(CC1)CCN1C(C(c1c2[nH]cc1)=CN(C)C2=O)=O LEMGAKAAUNGWHX-UHFFFAOYSA-N 0.000 description 1
- RFLTUNKOJLSFRI-UHFFFAOYSA-N CC(CC1)CCN1C(CC1)CCN1C(C(c1c2[nH]cc1)=CN(C)C2=O)=O Chemical compound CC(CC1)CCN1C(CC1)CCN1C(C(c1c2[nH]cc1)=CN(C)C2=O)=O RFLTUNKOJLSFRI-UHFFFAOYSA-N 0.000 description 1
- HMCFXEKTKFEKCT-UHFFFAOYSA-N CC(CCC1)CN1C(CC1)CCN1C(C(c1c2[nH]cc1)=CN(C)C2=O)=O Chemical compound CC(CCC1)CN1C(CC1)CCN1C(C(c1c2[nH]cc1)=CN(C)C2=O)=O HMCFXEKTKFEKCT-UHFFFAOYSA-N 0.000 description 1
- HSXOJHXRNKVLHL-VURMDHGXSA-N CC(CN(CC1)C(C(C(/C=C\N)=C2C)=CN(C)C2=O)=O)C1N(C)C Chemical compound CC(CN(CC1)C(C(C(/C=C\N)=C2C)=CN(C)C2=O)=O)C1N(C)C HSXOJHXRNKVLHL-VURMDHGXSA-N 0.000 description 1
- VWVDYFBWPFYGNZ-UHFFFAOYSA-N CC(CN(CC1)CCC1NC)c1ccccc1 Chemical compound CC(CN(CC1)CCC1NC)c1ccccc1 VWVDYFBWPFYGNZ-UHFFFAOYSA-N 0.000 description 1
- JAKDWKVKEBOKAO-UHFFFAOYSA-N CC(N(CC1)CCC1C1=NCCC=C1)=O Chemical compound CC(N(CC1)CCC1C1=NCCC=C1)=O JAKDWKVKEBOKAO-UHFFFAOYSA-N 0.000 description 1
- ADKJRMANIGACDE-UHFFFAOYSA-N CC(N(CC1)CCC1[n]1c(cccc2)c2nc1)=O Chemical compound CC(N(CC1)CCC1[n]1c(cccc2)c2nc1)=O ADKJRMANIGACDE-UHFFFAOYSA-N 0.000 description 1
- GWFPELGLVGDRGE-UHFFFAOYSA-N CCCC(N(CC1)CC=C1c1nccnc1)=O Chemical compound CCCC(N(CC1)CC=C1c1nccnc1)=O GWFPELGLVGDRGE-UHFFFAOYSA-N 0.000 description 1
- UGJCAXHVKZMJJA-UHFFFAOYSA-N CCN(CC)C(CC1)CCN1C(C(c1c2[nH]cc1)=CN(C)C2=O)=O Chemical compound CCN(CC)C(CC1)CCN1C(C(c1c2[nH]cc1)=CN(C)C2=O)=O UGJCAXHVKZMJJA-UHFFFAOYSA-N 0.000 description 1
- FBVGIYYPPOCZOL-UHFFFAOYSA-N CCS(C)C(N(C)CC1CCN(CC2COCCC2)CC1)=O Chemical compound CCS(C)C(N(C)CC1CCN(CC2COCCC2)CC1)=O FBVGIYYPPOCZOL-UHFFFAOYSA-N 0.000 description 1
- ZEXPBEBJNWJYOD-UHFFFAOYSA-N CCc(cc1)ccc1N(CC1)CCC1N(C)C(C(c1c2[nH]cc1)=CN(C)C2=O)=O Chemical compound CCc(cc1)ccc1N(CC1)CCC1N(C)C(C(c1c2[nH]cc1)=CN(C)C2=O)=O ZEXPBEBJNWJYOD-UHFFFAOYSA-N 0.000 description 1
- BXDBCNHTWWMPOP-UHFFFAOYSA-N CCc1cccc(N(CC2)CCC2N(C)C(C(C2C=CNC22)=CN(C)C2=O)=O)c1 Chemical compound CCc1cccc(N(CC2)CCC2N(C)C(C(C2C=CNC22)=CN(C)C2=O)=O)c1 BXDBCNHTWWMPOP-UHFFFAOYSA-N 0.000 description 1
- JZSMQBUKLWKLAH-UHFFFAOYSA-N CN(C(CC1)CCN1c1nc(C#N)ncc1)C(C(c1c2[nH]cc1)=CN(CC=C)C2O)=O Chemical compound CN(C(CC1)CCN1c1nc(C#N)ncc1)C(C(c1c2[nH]cc1)=CN(CC=C)C2O)=O JZSMQBUKLWKLAH-UHFFFAOYSA-N 0.000 description 1
- MKBQGEGVONDJOL-UHFFFAOYSA-N CN(C(CC1)CCN1c1nc(C(F)(F)F)ccn1)C(C(C1C=CNC11)=CN(CC=C)C1O)=O Chemical compound CN(C(CC1)CCN1c1nc(C(F)(F)F)ccn1)C(C(C1C=CNC11)=CN(CC=C)C1O)=O MKBQGEGVONDJOL-UHFFFAOYSA-N 0.000 description 1
- HPNQBNLYZZQXKT-UHFFFAOYSA-N CN(C(CC1)CCN1c1ncncc1)C(C(c1c2[nH]cc1)=CN(CC=C)C2=O)=O Chemical compound CN(C(CC1)CCN1c1ncncc1)C(C(c1c2[nH]cc1)=CN(CC=C)C2=O)=O HPNQBNLYZZQXKT-UHFFFAOYSA-N 0.000 description 1
- BKNNKEDBPTYNGM-UHFFFAOYSA-N CN(C)C(C(CC1)CCN1C(C(c1c2[nH]cc1)=CN(C)C2=O)=O)=O Chemical compound CN(C)C(C(CC1)CCN1C(C(c1c2[nH]cc1)=CN(C)C2=O)=O)=O BKNNKEDBPTYNGM-UHFFFAOYSA-N 0.000 description 1
- CFXSNMNOGBSDGU-UHFFFAOYSA-N CN(C)C(CC1)CCN1C(C(c1c2[nH]cc1)=CN(CCC1CC1)C2=O)=O Chemical compound CN(C)C(CC1)CCN1C(C(c1c2[nH]cc1)=CN(CCC1CC1)C2=O)=O CFXSNMNOGBSDGU-UHFFFAOYSA-N 0.000 description 1
- RHTIIFADKOEUSR-UHFFFAOYSA-N CN(C)C(N(CC1)CCC1c1ncncc1)=O Chemical compound CN(C)C(N(CC1)CCC1c1ncncc1)=O RHTIIFADKOEUSR-UHFFFAOYSA-N 0.000 description 1
- BWDUSWMVCCCWOD-UHFFFAOYSA-N CN(C1CCCCC1)C(CC1)CCN1C=O Chemical compound CN(C1CCCCC1)C(CC1)CCN1C=O BWDUSWMVCCCWOD-UHFFFAOYSA-N 0.000 description 1
- IYIIMQCNUYRHBO-UHFFFAOYSA-N CN(C1O)C=C(C2OC2N(CC2)CCC2N2CCOCC2)c2c1[nH]cc2 Chemical compound CN(C1O)C=C(C2OC2N(CC2)CCC2N2CCOCC2)c2c1[nH]cc2 IYIIMQCNUYRHBO-UHFFFAOYSA-N 0.000 description 1
- RNYPMKBFHRSMPM-UHFFFAOYSA-N CN(C=C(C(N(CC1)CCC1C#N)=O)c1c2[nH]cc1)C2=O Chemical compound CN(C=C(C(N(CC1)CCC1C#N)=O)c1c2[nH]cc1)C2=O RNYPMKBFHRSMPM-UHFFFAOYSA-N 0.000 description 1
- BXQUMVORFIOMJP-UHFFFAOYSA-N CN(C=C(C(N(CC1)CCC1C(F)(F)F)=O)c1c2[nH]cc1)C2=O Chemical compound CN(C=C(C(N(CC1)CCC1C(F)(F)F)=O)c1c2[nH]cc1)C2=O BXQUMVORFIOMJP-UHFFFAOYSA-N 0.000 description 1
- KFFRKYMJDNFLSJ-UHFFFAOYSA-N CN(C=C(C(N(CC1)CCC1OC)=O)c1c2[nH]cc1)C2=O Chemical compound CN(C=C(C(N(CC1)CCC1OC)=O)c1c2[nH]cc1)C2=O KFFRKYMJDNFLSJ-UHFFFAOYSA-N 0.000 description 1
- MOVIQYNEXLEQEM-UHFFFAOYSA-N CN(C=C(C(N1CCC(CC2N=CC=CC2)CC1)=O)c1c2[nH]cc1)C2=O Chemical compound CN(C=C(C(N1CCC(CC2N=CC=CC2)CC1)=O)c1c2[nH]cc1)C2=O MOVIQYNEXLEQEM-UHFFFAOYSA-N 0.000 description 1
- SVPKPAOXAZWQPH-UHFFFAOYSA-N CN(C=C(C(N1CCC(CCc2ccncc2)CC1)O)c1c2[nH]cc1)C2=O Chemical compound CN(C=C(C(N1CCC(CCc2ccncc2)CC1)O)c1c2[nH]cc1)C2=O SVPKPAOXAZWQPH-UHFFFAOYSA-N 0.000 description 1
- NQUSIPINLCHYRE-UHFFFAOYSA-N CN(C=C(C(N1CCC(CO)CC1)=O)c1c2[nH]cc1)C2=O Chemical compound CN(C=C(C(N1CCC(CO)CC1)=O)c1c2[nH]cc1)C2=O NQUSIPINLCHYRE-UHFFFAOYSA-N 0.000 description 1
- FUDSXSIRXAOABP-UHFFFAOYSA-N CN(C=C(C(N1CCCCC1)=O)c1c2[nH]cc1)C2=O Chemical compound CN(C=C(C(N1CCCCC1)=O)c1c2[nH]cc1)C2=O FUDSXSIRXAOABP-UHFFFAOYSA-N 0.000 description 1
- VZDGRRGLSFQPCC-UHFFFAOYSA-N CN(C=C(C1OC1N(CC1)CCC1c1ccccc1)c1c2[nH]cc1)C2=O Chemical compound CN(C=C(C1OC1N(CC1)CCC1c1ccccc1)c1c2[nH]cc1)C2=O VZDGRRGLSFQPCC-UHFFFAOYSA-N 0.000 description 1
- DOJJCJLLNUPQSU-UHFFFAOYSA-N CN(CC(CC1)CCN1c1ncncc1)C(C(c1c2[nH]cc1)=CN(C)C2=O)=O Chemical compound CN(CC(CC1)CCN1c1ncncc1)C(C(c1c2[nH]cc1)=CN(C)C2=O)=O DOJJCJLLNUPQSU-UHFFFAOYSA-N 0.000 description 1
- OSOZVNXWKSZTGJ-UHFFFAOYSA-N CN(CC1)CCN1C(CC1)CCN1C(C(c1c2[nH]cc1)=CN(C)C2=O)=O Chemical compound CN(CC1)CCN1C(CC1)CCN1C(C(c1c2[nH]cc1)=CN(C)C2=O)=O OSOZVNXWKSZTGJ-UHFFFAOYSA-N 0.000 description 1
- TYWQMEBQIZLNKW-UHFFFAOYSA-N Cc(cc1)ccc1N(CC1)CCC1N(C)C(C(c1c2[nH]cc1)=CN(C)C2=O)=O Chemical compound Cc(cc1)ccc1N(CC1)CCC1N(C)C(C(c1c2[nH]cc1)=CN(C)C2=O)=O TYWQMEBQIZLNKW-UHFFFAOYSA-N 0.000 description 1
- TYELAZUJANXRHV-UHFFFAOYSA-N Cc1cc(NC(C(CN(C)C2=O)c3c2[nH]cc3)=O)ccc1 Chemical compound Cc1cc(NC(C(CN(C)C2=O)c3c2[nH]cc3)=O)ccc1 TYELAZUJANXRHV-UHFFFAOYSA-N 0.000 description 1
- INBAALZXDRSEDW-UHFFFAOYSA-N Cc1ccccc1CN1CCC(CN(C)C=O)CC1 Chemical compound Cc1ccccc1CN1CCC(CN(C)C=O)CC1 INBAALZXDRSEDW-UHFFFAOYSA-N 0.000 description 1
- FHXKOHRPZOJNSQ-UHFFFAOYSA-N O=CN(CC1)CCC1c(cc1)ccc1Cl Chemical compound O=CN(CC1)CCC1c(cc1)ccc1Cl FHXKOHRPZOJNSQ-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462077711P | 2014-11-10 | 2014-11-10 | |
| US62/077,711 | 2014-11-10 | ||
| PCT/US2015/059997 WO2016077375A1 (en) | 2014-11-10 | 2015-11-10 | Bromodomain inhibitors and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017533250A JP2017533250A (ja) | 2017-11-09 |
| JP2017533250A5 true JP2017533250A5 (enExample) | 2018-12-20 |
| JP6639497B2 JP6639497B2 (ja) | 2020-02-05 |
Family
ID=54705827
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017525079A Expired - Fee Related JP6639497B2 (ja) | 2014-11-10 | 2015-11-10 | ブロモドメインインヒビターおよびその使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US10258603B2 (enExample) |
| EP (1) | EP3218376B1 (enExample) |
| JP (1) | JP6639497B2 (enExample) |
| CN (1) | CN107108613B (enExample) |
| WO (1) | WO2016077375A1 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9840489B2 (en) | 2013-12-20 | 2017-12-12 | Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. China | Piperidine carboxamide compound, preparation method, and usage thereof |
| CN107108613B (zh) | 2014-11-10 | 2020-02-25 | 基因泰克公司 | 布罗莫结构域抑制剂及其用途 |
| MA40940A (fr) | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| MA40943A (fr) * | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| EP3250571B1 (en) | 2015-01-29 | 2022-11-30 | Genentech, Inc. | Therapeutic compounds and uses thereof |
| AU2017254713C1 (en) | 2016-04-22 | 2021-04-29 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of EGFR and methods of use |
| ES2928773T3 (es) | 2017-01-17 | 2022-11-22 | Heparegenix Gmbh | Inhibidores de proteína cinasas para fomentar la regeneración hepática o reducir o prevenir la muerte de hepatocitos |
| CN110198941B (zh) * | 2017-01-25 | 2021-09-28 | 江苏豪森药业集团有限公司 | 吡咯并吡啶类n-氧化衍生物及其制备方法和应用 |
| JP7197075B2 (ja) * | 2018-04-20 | 2022-12-27 | 中国科学院上海薬物研究所 | ヒストンアセチルトランスフェラーゼ（ｈａｔ）阻害剤及びその用途 |
| MA53377A (fr) * | 2018-07-24 | 2021-06-02 | Epizyme Inc | Composés de pyridin-2-one utiles en tant qu'antagonistes de smarca2 |
| IL288522B2 (en) * | 2019-06-21 | 2025-02-01 | Hoffmann La Roche | EGFR inhibitor for cancer treatment |
| US11171132B2 (en) * | 2019-10-03 | 2021-11-09 | Globalfoundries U.S. Inc. | Bi-directional breakdown silicon controlled rectifiers |
| CN112625036A (zh) * | 2019-10-08 | 2021-04-09 | 上海海和药物研究开发股份有限公司 | 一类具有brd4抑制活性的化合物、其制备方法及用途 |
| TW202146412A (zh) | 2020-03-05 | 2021-12-16 | 美商Ｃ４醫藥公司 | 用於標靶降解brd9之化合物 |
| WO2022051565A1 (en) * | 2020-09-04 | 2022-03-10 | Ikena Oncology, Inc. | Substituted 4-piperidinyl-quinazolines, 4-piperidinyl-pyrimidine-2-amines, and related compounds and their use in treating medical conditions |
| CN117377668A (zh) * | 2020-10-15 | 2024-01-09 | 迈欧伏特治疗公司 | Pgdh抑制剂的吸入制剂及其使用方法 |
| TW202237095A (zh) | 2020-12-03 | 2022-10-01 | 德商艾斯巴赫生物有限公司 | Ａｌｃ１抑制劑及與ｐａｒｐｉ之協同性 |
| JP2024542045A (ja) * | 2021-11-03 | 2024-11-13 | バイン セラピューティクス インコーポレイテッド | 汎ｂｅｔ阻害剤の使用 |
| CA3250274A1 (en) | 2022-05-02 | 2023-11-09 | Eisbach Bio Gmbh | USE OF ALC1 INHIBITORS AND SYNERGY WITH PARPI |
| CN119384408A (zh) | 2022-06-16 | 2025-01-28 | 安菲斯塔治疗有限责任公司 | 用于靶向蛋白降解的双功能分子 |
| EP4587126A1 (en) | 2022-09-13 | 2025-07-23 | Amphista Therapeutics Ltd | Compounds for targeted protein degradation |
| GB202300833D0 (en) * | 2023-01-19 | 2023-03-08 | Nrg Therapeutics Ltd | Novel compounds |
| WO2025085564A1 (en) * | 2023-10-16 | 2025-04-24 | Kronos Bio, Inc. | Lysine acetyltransferase inhibitors |
| GB202319256D0 (en) | 2023-12-15 | 2024-01-31 | Amphista Therapeutics Ltd | Novel compounds for targeted protein degradation |
| WO2025191109A1 (en) | 2024-03-13 | 2025-09-18 | Amphista Therapeutics Limited | Combinations comprising brd9 bifunctional compounds and their use in the treatment of cancer |
| WO2026052822A1 (en) | 2024-09-06 | 2026-03-12 | Amphista Therapeutics Limited | Tetrahydroisoquinoline compounds for targeted protein degradation |
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2015
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- 2015-11-10 EP EP15801563.6A patent/EP3218376B1/en active Active
- 2015-11-10 WO PCT/US2015/059997 patent/WO2016077375A1/en not_active Ceased
- 2015-11-10 JP JP2017525079A patent/JP6639497B2/ja not_active Expired - Fee Related
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2017
- 2017-05-10 US US15/592,012 patent/US10258603B2/en active Active