JP2016540742A5 - - Google Patents
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- Publication number
- JP2016540742A5 JP2016540742A5 JP2016528151A JP2016528151A JP2016540742A5 JP 2016540742 A5 JP2016540742 A5 JP 2016540742A5 JP 2016528151 A JP2016528151 A JP 2016528151A JP 2016528151 A JP2016528151 A JP 2016528151A JP 2016540742 A5 JP2016540742 A5 JP 2016540742A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound according
- optionally
- substituted
- haloalkyl
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 18
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 7
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 6
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims 4
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- -1 2 -cyclopropyl Chemical group 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- WYURNTSHIVDZCO-UHFFFAOYSA-N tetrahydrofuran Substances C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 1
- 0 Cc1nnc2[n]1cc(-c1nc(*S=[Si]*)c(CS=*)[n]1*)nc2* Chemical compound Cc1nnc2[n]1cc(-c1nc(*S=[Si]*)c(CS=*)[n]1*)nc2* 0.000 description 7
- KKDDPRLFZIZNOZ-PJQLUOCWSA-N CC(/N=C(/c(nc1NC)c[n]2c1nnc2C)\NC/C=C(\N)/N1CCOCC1)=C Chemical compound CC(/N=C(/c(nc1NC)c[n]2c1nnc2C)\NC/C=C(\N)/N1CCOCC1)=C KKDDPRLFZIZNOZ-PJQLUOCWSA-N 0.000 description 1
- ORDLNMVNIUZEFN-UHFFFAOYSA-N CC(C)N(Cc(nc1NC)c[n]2c1nnc2C)c1cc(N2CCOCC2)ncc1N Chemical compound CC(C)N(Cc(nc1NC)c[n]2c1nnc2C)c1cc(N2CCOCC2)ncc1N ORDLNMVNIUZEFN-UHFFFAOYSA-N 0.000 description 1
- INDXEUWAYHQPLH-UHFFFAOYSA-N CC(C)N/C(/C1N(C)N=C(C)N1)=N/C(c([n](CCOC)c1c2)nc1cnc2N1CCOCC1)=C Chemical compound CC(C)N/C(/C1N(C)N=C(C)N1)=N/C(c([n](CCOC)c1c2)nc1cnc2N1CCOCC1)=C INDXEUWAYHQPLH-UHFFFAOYSA-N 0.000 description 1
- YDFWFCNHGMINDN-CJAAZZPWSA-N CC(C)NCc1nnc(C)[n]1/C=C(/c([n]([C@@H](C)COC)c1c2)nc1cnc2N)\N Chemical compound CC(C)NCc1nnc(C)[n]1/C=C(/c([n]([C@@H](C)COC)c1c2)nc1cnc2N)\N YDFWFCNHGMINDN-CJAAZZPWSA-N 0.000 description 1
- VFKKCRARNMPEKS-LOACHALJSA-N CC(C)Nc1nc(-c([n](C(C)CC(F)(F)F)c2c3)nc2cnc3N2[C@@H](C)COCC2)c[n]2c1nnc2C Chemical compound CC(C)Nc1nc(-c([n](C(C)CC(F)(F)F)c2c3)nc2cnc3N2[C@@H](C)COCC2)c[n]2c1nnc2C VFKKCRARNMPEKS-LOACHALJSA-N 0.000 description 1
- CFGOTAZMBODAOY-DJNXLDHESA-N CC(C)Nc1nc(-c([n](C(C)CC2CC2)c2c3)nc2cnc3N2[C@@H](C)COCC2)c[n]2c1nnc2C Chemical compound CC(C)Nc1nc(-c([n](C(C)CC2CC2)c2c3)nc2cnc3N2[C@@H](C)COCC2)c[n]2c1nnc2C CFGOTAZMBODAOY-DJNXLDHESA-N 0.000 description 1
- VZWPIGWPJXXYDY-IRXDYDNUSA-N CC(C)Nc1nc(-c([n]([C@@H](C)COC)c2c3)nc2ccc3N2[C@@H](C)COCC2)c[n]2c1nnc2C Chemical compound CC(C)Nc1nc(-c([n]([C@@H](C)COC)c2c3)nc2ccc3N2[C@@H](C)COCC2)c[n]2c1nnc2C VZWPIGWPJXXYDY-IRXDYDNUSA-N 0.000 description 1
- HHMLWUGUZBHHIP-FBHDLOMBSA-N CC(C)Nc1nc(-c2nc(/C=N\C=C)c[n]2CCOC(C)C)c[n]2c1nnc2C Chemical compound CC(C)Nc1nc(-c2nc(/C=N\C=C)c[n]2CCOC(C)C)c[n]2c1nnc2C HHMLWUGUZBHHIP-FBHDLOMBSA-N 0.000 description 1
- ROPUJVGYXCPJMZ-WOJGMQOQSA-N CC(C)Nc1nc(-c2nc(C)c(/C=C(\NC)/N3CCOCC3)[n]2C)c[n]2c1nnc2C Chemical compound CC(C)Nc1nc(-c2nc(C)c(/C=C(\NC)/N3CCOCC3)[n]2C)c[n]2c1nnc2C ROPUJVGYXCPJMZ-WOJGMQOQSA-N 0.000 description 1
- UAPOLSKLGHVOBF-UHFFFAOYSA-N CC(C)Nc1nc(-c2nc(cc(C(C)(C)C(N3C(C)C)=O)c3c3)c3[n]2C(C)=C)c[n]2c1nnc2C Chemical compound CC(C)Nc1nc(-c2nc(cc(C(C)(C)C(N3C(C)C)=O)c3c3)c3[n]2C(C)=C)c[n]2c1nnc2C UAPOLSKLGHVOBF-UHFFFAOYSA-N 0.000 description 1
- SWJQEZHLVSBGGV-AWEZNQCLSA-N CC(C)Nc1nc(-c2nc(cc(C(C)(C)C(N3C)=O)c3c3)c3[n]2[C@@H](C)COC)c[n]2c1nnc2C Chemical compound CC(C)Nc1nc(-c2nc(cc(C(C)(C)C(N3C)=O)c3c3)c3[n]2[C@@H](C)COC)c[n]2c1nnc2C SWJQEZHLVSBGGV-AWEZNQCLSA-N 0.000 description 1
- PMICXQNPCMHOHX-INIZCTEOSA-N CC(C)Nc1nc(-c2nc(cc(C(C)(C)S(N3C(C)C)(=O)=O)c3c3)c3[n]2[C@@H](C)COC)c[n]2c1nnc2C Chemical compound CC(C)Nc1nc(-c2nc(cc(C(C)(C)S(N3C(C)C)(=O)=O)c3c3)c3[n]2[C@@H](C)COC)c[n]2c1nnc2C PMICXQNPCMHOHX-INIZCTEOSA-N 0.000 description 1
- XYNSOALDZLYHSO-LBPRGKRZSA-N CC(C)Nc1nc(-c2nc(ccc(N)c3)c3[n]2[C@@H](C)COC)c[n]2c1nnc2C Chemical compound CC(C)Nc1nc(-c2nc(ccc(N)c3)c3[n]2[C@@H](C)COC)c[n]2c1nnc2C XYNSOALDZLYHSO-LBPRGKRZSA-N 0.000 description 1
- RBMHSADQDPVHJD-UHFFFAOYSA-N CC(C)Nc1nc(-c2nc(nc(cc3)N4CCOCC4)c3[n]2CCOC)c[n]2c1nnc2C Chemical compound CC(C)Nc1nc(-c2nc(nc(cc3)N4CCOCC4)c3[n]2CCOC)c[n]2c1nnc2C RBMHSADQDPVHJD-UHFFFAOYSA-N 0.000 description 1
- JTMJPRYUJZVGIZ-UIRIHMJUSA-N CC(C)Nc1nc(-c2nc3ccc(C4OCCN(C)C4)cc3[n]2[C@@H](C)COC)c[n]2c1nnc2CCC(C)OCC[n]1c(-c(nc2NC3CCN(C)CC3)c[n]3c2nnc3C)nc2c1cc(N1CCOCC1)nc2 Chemical compound CC(C)Nc1nc(-c2nc3ccc(C4OCCN(C)C4)cc3[n]2[C@@H](C)COC)c[n]2c1nnc2CCC(C)OCC[n]1c(-c(nc2NC3CCN(C)CC3)c[n]3c2nnc3C)nc2c1cc(N1CCOCC1)nc2 JTMJPRYUJZVGIZ-UIRIHMJUSA-N 0.000 description 1
- LBPJASLOZZASKK-HNNXBMFYSA-N CC(C)Nc1nc(-c2nc3ccc(N4CCOCC4)nc3[n]2[C@@H](C)COC)c[n]2c1nnc2C Chemical compound CC(C)Nc1nc(-c2nc3ccc(N4CCOCC4)nc3[n]2[C@@H](C)COC)c[n]2c1nnc2C LBPJASLOZZASKK-HNNXBMFYSA-N 0.000 description 1
- COAPWIVUNKVSAH-UHFFFAOYSA-N CC(C)Nc1ncc[n]2c1nnc2C Chemical compound CC(C)Nc1ncc[n]2c1nnc2C COAPWIVUNKVSAH-UHFFFAOYSA-N 0.000 description 1
- KHESJNIFSXQAGJ-UHFFFAOYSA-N CC(C)OCC[n]1c(-c(nc2NC(CC3)CCN3S(C)(=O)=O)c[n]3c2nnc3C)nc2c1cc(N1CCOCC1)nc2 Chemical compound CC(C)OCC[n]1c(-c(nc2NC(CC3)CCN3S(C)(=O)=O)c[n]3c2nnc3C)nc2c1cc(N1CCOCC1)nc2 KHESJNIFSXQAGJ-UHFFFAOYSA-N 0.000 description 1
- OYIUSPFQLJBXKK-UHFFFAOYSA-N CC(C)c1ccc2nc(-c(nc3NC(C)C)c[n]4c3nnc4C)[n](C(COC)=C)c2c1 Chemical compound CC(C)c1ccc2nc(-c(nc3NC(C)C)c[n]4c3nnc4C)[n](C(COC)=C)c2c1 OYIUSPFQLJBXKK-UHFFFAOYSA-N 0.000 description 1
- IFYBRLGWEVSZAC-UHFFFAOYSA-N CC[n](c1c2)c(C3=CN=C(C)N=NC=C(NC)[N]3)nc1cnc2N(C)C Chemical compound CC[n](c1c2)c(C3=CN=C(C)N=NC=C(NC)[N]3)nc1cnc2N(C)C IFYBRLGWEVSZAC-UHFFFAOYSA-N 0.000 description 1
- SJRJJKPEHAURKC-UHFFFAOYSA-N CN1CCOCC1 Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 description 1
- NENUULUAEJSJJC-LBPRGKRZSA-N C[C@@H](COC)[n](c1c2)c(-c(nc3N)c[n]4c3nnc4C)nc1cnc2N1CCOCC1 Chemical compound C[C@@H](COC)[n](c1c2)c(-c(nc3N)c[n]4c3nnc4C)nc1cnc2N1CCOCC1 NENUULUAEJSJJC-LBPRGKRZSA-N 0.000 description 1
- OFFSCXWKTSLOHD-UHFFFAOYSA-N Cc1nnc2[n]1cc(CN(CCOC)c1cc(N3CCOCC3)ncc1NC)nc2NC Chemical compound Cc1nnc2[n]1cc(CN(CCOC)c1cc(N3CCOCC3)ncc1NC)nc2NC OFFSCXWKTSLOHD-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13192002 | 2013-11-07 | ||
| EP13192002.7 | 2013-11-07 | ||
| PCT/EP2014/074069 WO2015067770A1 (en) | 2013-11-07 | 2014-11-07 | Triazolopyrazine derivatives as brd4 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016540742A JP2016540742A (ja) | 2016-12-28 |
| JP2016540742A5 true JP2016540742A5 (enExample) | 2017-12-21 |
| JP6370376B2 JP6370376B2 (ja) | 2018-08-08 |
Family
ID=49518874
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016528151A Active JP6370376B2 (ja) | 2013-11-07 | 2014-11-07 | Ｂｒｄ４阻害薬としてのトリアゾロピラジン誘導体 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9428513B2 (enExample) |
| EP (1) | EP3066104B1 (enExample) |
| JP (1) | JP6370376B2 (enExample) |
| AR (1) | AR098337A1 (enExample) |
| TW (1) | TW201609731A (enExample) |
| UY (1) | UY35827A (enExample) |
| WO (1) | WO2015067770A1 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9266891B2 (en) | 2012-11-16 | 2016-02-23 | Boehringer Ingelheim International Gmbh | Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| AU2016232705C1 (en) | 2015-03-18 | 2021-06-17 | Arvinas, Inc. | Compounds and methods for the enhanced degradation of targeted proteins |
| EP3319944A4 (en) | 2015-07-10 | 2019-04-24 | Arvinas, Inc. | MDM2-BASED MODULATORS OF PROTEOLYSIS AND RELATED USE METHODS |
| CA2994969A1 (en) | 2015-08-06 | 2017-02-09 | Dana-Farber Cancer Institute, Inc. | Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses |
| EP3337476A4 (en) | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| US10517877B2 (en) | 2016-03-30 | 2019-12-31 | Wisconsin Alumni Research Foundation | Compounds and methods for modulating frataxin expression |
| US20170281784A1 (en) | 2016-04-05 | 2017-10-05 | Arvinas, Inc. | Protein-protein interaction inducing technology |
| CN121974842A (zh) | 2016-05-10 | 2026-05-05 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| CN109562113A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的螺环降解决定子体 |
| WO2017197046A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
| CN109562107A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的杂环降解决定子体 |
| IL319363A (en) | 2017-01-31 | 2025-05-01 | Arvinas Operations Inc | Cervalon ligands and bifunctional compounds containing them |
| EP4119552A1 (en) | 2017-02-08 | 2023-01-18 | Dana-Farber Cancer Institute, Inc. | Regulating chimeric antigen receptors |
| US11759533B2 (en) | 2017-03-29 | 2023-09-19 | Wisconsin Alumni Research Foundation | Methods and compositions for modulating gene expression |
| EP4717317A3 (en) | 2017-06-20 | 2026-06-03 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| WO2019145410A1 (en) * | 2018-01-25 | 2019-08-01 | Boehringer Ingelheim International Gmbh | Combination treatment of acute myeloid leukemia |
| JP2021512153A (ja) | 2018-01-26 | 2021-05-13 | イエール ユニバーシティ | タンパク質分解のイミド系モジュレーターおよび使用方法 |
| CA3095912A1 (en) | 2018-04-13 | 2019-10-17 | Arvinas Operations, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| EP3897631A4 (en) | 2018-12-20 | 2022-11-23 | C4 Therapeutics, Inc. | TARGETED PROTEIN BREAKDOWN |
| WO2021127443A1 (en) | 2019-12-19 | 2021-06-24 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| WO2021175432A1 (en) | 2020-03-04 | 2021-09-10 | Boehringer Ingelheim International Gmbh | Method for administration of an anti cancer agent |
| US12527741B2 (en) | 2021-06-17 | 2026-01-20 | Wisconsin Alumni Research Foundation | Modular dendron micelles for treatment of pulmonary diseases related to fibrosis and viral infection including COVID-19 |
| WO2025049555A1 (en) | 2023-08-31 | 2025-03-06 | Oerth Bio Llc | Compositions and methods for targeted inhibition and degradation of proteins in an insect cell |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2310072A1 (en) | 1997-11-11 | 1999-05-20 | Hiroyuki Ohno | Fused pyrazine compounds |
| EP1598353A1 (en) * | 2004-05-17 | 2005-11-23 | Boehringer Ingelheim International GmbH | Pyrrolobenzimidazolones and their use as antiproliferative agents |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| CA2779355C (en) | 2009-11-05 | 2018-01-16 | Glaxosmithkline Llc | Benzodiazepine bromodomain inhibitor |
| WO2012174487A2 (en) | 2011-06-17 | 2012-12-20 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| US9266891B2 (en) | 2012-11-16 | 2016-02-23 | Boehringer Ingelheim International Gmbh | Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors |
-
2014
- 2014-11-04 US US14/532,405 patent/US9428513B2/en active Active
- 2014-11-06 AR ARP140104188A patent/AR098337A1/es unknown
- 2014-11-06 TW TW103138596A patent/TW201609731A/zh unknown
- 2014-11-07 EP EP14793870.8A patent/EP3066104B1/en active Active
- 2014-11-07 JP JP2016528151A patent/JP6370376B2/ja active Active
- 2014-11-07 UY UY0001035827A patent/UY35827A/es unknown
- 2014-11-07 WO PCT/EP2014/074069 patent/WO2015067770A1/en not_active Ceased
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