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 |
|---|---|---|---|---|
| EP3085700B1 (en) * | 2013-12-20 | 2018-10-31 | Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China | Novel piperidine carboxamide compound, preparation method, and usage thereof |
| MA40943A (fr) * | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| JP6639497B2 (ja) | 2014-11-10 | 2020-02-05 | ジェネンテック， インコーポレイテッド | ブロモドメインインヒビターおよびその使用 |
| MA40940A (fr) | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| CN107531692B (zh) | 2015-01-29 | 2020-12-25 | 基因泰克公司 | 治疗化合物及其用途 |
| WO2017185036A1 (en) | 2016-04-22 | 2017-10-26 | Dana Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of egfr and methods of use |
| AU2018209164B2 (en) | 2017-01-17 | 2021-11-04 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| WO2018137655A1 (zh) * | 2017-01-25 | 2018-08-02 | 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 |
| WO2019201291A1 (zh) * | 2018-04-20 | 2019-10-24 | 中国科学院上海药物研究所 | 组蛋白乙酰转移酶(hat)抑制剂及其用途 |
| WO2020023657A1 (en) * | 2018-07-24 | 2020-01-30 | Epizyme, Inc. | Pyridin-2-one compounds useful as smarca2 antagonists |
| AR119210A1 (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 |
| CA3165309A1 (en) | 2020-03-05 | 2021-09-10 | Christopher G. Nasveschuk | Compounds for targeted degradation of brd9 |
| 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 |
| WO2023081720A1 (en) * | 2021-11-03 | 2023-05-11 | Vyne Therapeutics Inc. | Uses of pan bet inhibitors |
| WO2023213833A1 (en) | 2022-05-02 | 2023-11-09 | Eisbach Bio Gmbh | Use of alc1 inhibitors and synergy with parpi |
| EP4540226A1 (en) | 2022-06-16 | 2025-04-23 | Amphista Therapeutics Ltd | Bifunctional molecules for targeted protein degradation |
| WO2024057021A1 (en) | 2022-09-13 | 2024-03-21 | 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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| CU22545A1 (es) | 1994-11-18 | 1999-03-31 | Centro Inmunologia Molecular | Obtención de un anticuerpo quimérico y humanizado contra el receptor del factor de crecimiento epidérmico para uso diagnóstico y terapéutico |
| US4943533A (en) | 1984-03-01 | 1990-07-24 | The Regents Of The University Of California | Hybrid cell lines that produce monoclonal antibodies to epidermal growth factor receptor |
| DE69025946T2 (de) | 1989-09-08 | 1996-10-17 | Univ Duke | Modifikationen der struktur des egf-rezeptor-gens in menschlichen glioma |
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| ID18494A (id) | 1996-10-02 | 1998-04-16 | Novartis Ag | Turunan pirazola leburan dan proses pembuatannya |
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2015
- 2015-11-10 JP JP2017525079A patent/JP6639497B2/ja not_active Expired - Fee Related
- 2015-11-10 WO PCT/US2015/059997 patent/WO2016077375A1/en not_active Ceased
- 2015-11-10 EP EP15801563.6A patent/EP3218376B1/en active Active
- 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