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 (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015090224A1 (zh) | 2013-12-20 | 2015-06-25 | 中国人民解放军军事医学科学院毒物药物研究所 | 新型哌啶氨甲酰类化合物、制备方法及其用途 |
| EP3218376B1 (en) | 2014-11-10 | 2019-12-25 | Genentech, Inc. | Bromodomain inhibitors and uses thereof |
| 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 |
| JP6709792B2 (ja) | 2015-01-29 | 2020-06-17 | ジェネンテック， インコーポレイテッド | 治療用化合物およびその使用 |
| CN109475528B (zh) | 2016-04-22 | 2022-01-11 | 达纳-法伯癌症研究所股份有限公司 | 用于egfr降解的双功能分子和使用方法 |
| JP7300394B2 (ja) | 2017-01-17 | 2023-06-29 | ヘパリジェニックス ゲーエムベーハー | 肝再生の促進又は肝細胞死の低減もしくは予防のためのプロテインキナーゼ阻害 |
| 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 |
| EP3782995B1 (en) * | 2018-04-20 | 2023-11-22 | Shanghai Institute of Materia Medica, Chinese Academy of Sciences | Spiro condensed imidazoline-2,4-dione derivatives as histone acetyltransferase inhibitors for the treatment of cancer diseases |
| WO2020023657A1 (en) * | 2018-07-24 | 2020-01-30 | Epizyme, Inc. | Pyridin-2-one compounds useful as smarca2 antagonists |
| AR119209A1 (es) * | 2019-06-21 | 2021-12-01 | Hoffmann La Roche | DERIVADOS DE PIRROLO[1,2-c]IMIDAZOL COMO INHIBIDORES DE EGFR |
| 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 |
| CN119823124A (zh) | 2020-03-05 | 2025-04-15 | C4医药公司 | 用于brd9的靶向降解的化合物 |
| 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 |
| 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 |
| AU2022380725A1 (en) * | 2021-11-03 | 2024-05-23 | Vyne Therapeutics Inc. | Uses of pan bet inhibitors |
| CN119365198A (zh) | 2022-05-02 | 2025-01-24 | 艾斯巴赫生物有限公司 | ALC1抑制剂的用途和与PARPi的协同作用 |
| WO2023242597A1 (en) | 2022-06-16 | 2023-12-21 | Amphista Therapeutics Limited | Bifunctional molecules for targeted protein degradation |
| AU2023343029A1 (en) | 2022-09-13 | 2025-03-27 | Amphista Therapeutics Limited | Compounds for targeted protein degradation |
| GB202300833D0 (en) * | 2023-01-19 | 2023-03-08 | Nrg Therapeutics Ltd | Novel compounds |
| TW202523311A (zh) * | 2023-10-16 | 2025-06-16 | 美商克洛諾斯生技有限公司 | 離胺酸乙醯基轉移酶抑制劑 |
| 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 |
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2015
- 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
- 2015-11-10 CN CN201580072351.6A patent/CN107108613B/zh not_active Expired - Fee Related
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2017
- 2017-05-10 US US15/592,012 patent/US10258603B2/en active Active