JP2019535658A5 - - Google Patents
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- Publication number
- JP2019535658A5 JP2019535658A5 JP2019520591A JP2019520591A JP2019535658A5 JP 2019535658 A5 JP2019535658 A5 JP 2019535658A5 JP 2019520591 A JP2019520591 A JP 2019520591A JP 2019520591 A JP2019520591 A JP 2019520591A JP 2019535658 A5 JP2019535658 A5 JP 2019535658A5
- Authority
- JP
- Japan
- Prior art keywords
- benzo
- dimethyl
- imidazol
- piperidine
- difluorophenyl
- 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
- 150000001875 compounds Chemical class 0.000 claims 20
- -1 2 - cyclopropyl Chemical group 0.000 claims 15
- 206010028980 Neoplasm Diseases 0.000 claims 9
- 201000011510 cancer Diseases 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 8
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 claims 7
- XUWHAWMETYGRKB-UHFFFAOYSA-N piperidin-2-one Chemical group O=C1CCCCN1 XUWHAWMETYGRKB-UHFFFAOYSA-N 0.000 claims 7
- 229940124597 therapeutic agent Drugs 0.000 claims 7
- 239000003112 inhibitor Substances 0.000 claims 5
- 229920000776 Poly(Adenosine diphosphate-ribose) polymerase Polymers 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims 2
- 229940123407 Androgen receptor antagonist Drugs 0.000 claims 2
- 108091007914 CDKs Proteins 0.000 claims 2
- 102000003903 Cyclin-dependent kinases Human genes 0.000 claims 2
- 108090000266 Cyclin-dependent kinases Proteins 0.000 claims 2
- 101000896517 Homo sapiens Steroid 17-alpha-hydroxylase/17,20 lyase Proteins 0.000 claims 2
- 102000004317 Lyases Human genes 0.000 claims 2
- 108090000856 Lyases Proteins 0.000 claims 2
- 102000012338 Poly(ADP-ribose) Polymerases Human genes 0.000 claims 2
- 108010061844 Poly(ADP-ribose) Polymerases Proteins 0.000 claims 2
- 108010015330 Steroid 17-alpha-Hydroxylase Proteins 0.000 claims 2
- 102000001854 Steroid 17-alpha-Hydroxylase Human genes 0.000 claims 2
- 102100021719 Steroid 17-alpha-hydroxylase/17,20 lyase Human genes 0.000 claims 2
- 239000003936 androgen receptor antagonist Substances 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 238000006880 cross-coupling reaction Methods 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 231100000433 cytotoxic Toxicity 0.000 claims 2
- 229940127089 cytotoxic agent Drugs 0.000 claims 2
- 230000001472 cytotoxic effect Effects 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 230000001225 therapeutic effect Effects 0.000 claims 2
- JKLZUTQOIVIMDL-DEOSSOPVSA-N (5S)-5-[1-(4,4-difluorocyclohexyl)-5-(2,4-dimethylpyrazol-3-yl)benzimidazol-2-yl]-1-(3,4-difluorophenyl)pyrrolidin-2-one Chemical compound FC1(CCC(CC1)N1C(=NC2=C1C=CC(=C2)C1=C(C=NN1C)C)[C@@H]1CCC(N1C1=CC(=C(C=C1)F)F)=O)F JKLZUTQOIVIMDL-DEOSSOPVSA-N 0.000 claims 1
- GXZJYHGHHDXIML-DEOSSOPVSA-N (5S)-5-[1-(4,4-difluorocyclohexyl)-5-(3,5-dimethylimidazol-4-yl)benzimidazol-2-yl]-1-(3,4-difluorophenyl)pyrrolidin-2-one Chemical compound Cc1ncn(C)c1-c1ccc2n(C3CCC(F)(F)CC3)c(nc2c1)[C@@H]1CCC(=O)N1c1ccc(F)c(F)c1 GXZJYHGHHDXIML-DEOSSOPVSA-N 0.000 claims 1
- PLWILTBCWYTPPW-QHCPKHFHSA-N (5S)-5-[1-(4,4-difluorocyclohexyl)-5-(3,5-dimethyltriazol-4-yl)benzimidazol-2-yl]-1-(3,4-difluorophenyl)pyrrolidin-2-one Chemical compound CN1N=NC(C)=C1C1=CC=C2N(C3CCC(F)(F)CC3)C(=NC2=C1)[C@@H]1CCC(=O)N1C1=CC(F)=C(F)C=C1 PLWILTBCWYTPPW-QHCPKHFHSA-N 0.000 claims 1
- VEJNCEXCHDKFMP-VWLOTQADSA-N (6S)-6-[1-(4,4-difluorocyclohexyl)-5-(2,4-dimethylpyrazol-3-yl)benzimidazol-2-yl]-1-(3-fluoro-4-methoxyphenyl)piperidin-2-one Chemical compound FC1(CCC(CC1)N1C(=NC2=C1C=CC(=C2)C1=C(C=NN1C)C)[C@@H]1CCCC(N1C1=CC(=C(C=C1)OC)F)=O)F VEJNCEXCHDKFMP-VWLOTQADSA-N 0.000 claims 1
- DGELDDLMFWVEIU-VWLOTQADSA-N (6S)-6-[1-(4,4-difluorocyclohexyl)-5-(3,5-dimethylimidazol-4-yl)benzimidazol-2-yl]-1-(3-fluoro-4-methoxyphenyl)piperidin-2-one Chemical compound FC1(CCC(CC1)N1C(=NC2=C1C=CC(=C2)C1=C(N=CN1C)C)[C@@H]1CCCC(N1C1=CC(=C(C=C1)OC)F)=O)F DGELDDLMFWVEIU-VWLOTQADSA-N 0.000 claims 1
- SMPWGRNRGLIMKS-DEOSSOPVSA-N (6S)-6-[1-(4,4-difluorocyclohexyl)-5-(3,5-dimethyltriazol-4-yl)benzimidazol-2-yl]-1-(3,4-difluorophenyl)piperidin-2-one Chemical compound CN1N=NC(C)=C1C1=CC=C2N(C3CCC(F)(F)CC3)C(=NC2=C1)[C@@H]1CCCC(=O)N1C1=CC(F)=C(F)C=C1 SMPWGRNRGLIMKS-DEOSSOPVSA-N 0.000 claims 1
- SAFFKKSHCVBSOP-DEOSSOPVSA-N (6S)-6-[1-(4,4-difluorocyclohexyl)-5-(3,5-dimethyltriazol-4-yl)benzimidazol-2-yl]-1-(3-fluoro-4-methoxyphenyl)piperidin-2-one Chemical compound FC1(CCC(CC1)N1C(=NC2=C1C=CC(=C2)C1=C(N=NN1C)C)[C@@H]1CCCC(N1C1=CC(=C(C=C1)OC)F)=O)F SAFFKKSHCVBSOP-DEOSSOPVSA-N 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- RLYGNTVDLHUMND-ZVOVDXHFSA-N C1(F)=CC=C(N2C(=O)CCC[C@H]2C=2N(C3=CC=C(C4=C(N=CN4C)C)C=C3N=2)[C@H]2CC[C@@H](CC2)O)C=C1F Chemical compound C1(F)=CC=C(N2C(=O)CCC[C@H]2C=2N(C3=CC=C(C4=C(N=CN4C)C)C=C3N=2)[C@H]2CC[C@@H](CC2)O)C=C1F RLYGNTVDLHUMND-ZVOVDXHFSA-N 0.000 claims 1
- HXUVQMNBLOUESF-YBXDKENTSA-N C1(OC)=CC=C(N2C(=O)CCC[C@H]2C=2N(C3=CC=C(C4=C(N=NN4C)C)C=C3N=2)[C@H]2CC[C@@H](CC2)OC)C=C1F Chemical compound C1(OC)=CC=C(N2C(=O)CCC[C@H]2C=2N(C3=CC=C(C4=C(N=NN4C)C)C=C3N=2)[C@H]2CC[C@@H](CC2)OC)C=C1F HXUVQMNBLOUESF-YBXDKENTSA-N 0.000 claims 1
- 229940124297 CDK 4/6 inhibitor Drugs 0.000 claims 1
- GMASEHDKHWQKFW-MYIHVTGJSA-N CN1C=NC(=C1C1=CC2=C(N(C(=N2)[C@@H]2CCCC(N2C2=CC(=C(C=C2)OC)F)=O)[C@@H]2CC[C@H](CC2)OC)C=C1)C Chemical compound CN1C=NC(=C1C1=CC2=C(N(C(=N2)[C@@H]2CCCC(N2C2=CC(=C(C=C2)OC)F)=O)[C@@H]2CC[C@H](CC2)OC)C=C1)C GMASEHDKHWQKFW-MYIHVTGJSA-N 0.000 claims 1
- LDTKXIYTYIBHEU-MYIHVTGJSA-N CN1N=CC(=C1C1=CC2=C(N(C(=N2)[C@@H]2CCCC(N2C2=CC(=C(C=C2)OC)F)=O)[C@@H]2CC[C@H](CC2)OC)C=C1)C Chemical compound CN1N=CC(=C1C1=CC2=C(N(C(=N2)[C@@H]2CCCC(N2C2=CC(=C(C=C2)OC)F)=O)[C@@H]2CC[C@H](CC2)OC)C=C1)C LDTKXIYTYIBHEU-MYIHVTGJSA-N 0.000 claims 1
- IDGSMDZPNMBSKN-KHOMTPLRSA-N ClC=1C=C(C=CC=1F)N1C(CCC[C@H]1C1=NC2=C(N1[C@@H]1CC[C@H](CC1)O)C=CC(=C2)C1=C(N=NN1C)C)=O Chemical compound ClC=1C=C(C=CC=1F)N1C(CCC[C@H]1C1=NC2=C(N1[C@@H]1CC[C@H](CC1)O)C=CC(=C2)C1=C(N=NN1C)C)=O IDGSMDZPNMBSKN-KHOMTPLRSA-N 0.000 claims 1
- 102000013701 Cyclin-Dependent Kinase 4 Human genes 0.000 claims 1
- 108010025464 Cyclin-Dependent Kinase 4 Proteins 0.000 claims 1
- YYLLIJHXUHJATK-UHFFFAOYSA-N Cyclohexyl acetate Chemical compound CC(=O)OC1CCCCC1 YYLLIJHXUHJATK-UHFFFAOYSA-N 0.000 claims 1
- MWIWFLRUTYDDEI-ZVOVDXHFSA-N FC=1C=C(C=CC=1F)N1C(CCC[C@H]1C1=NC2=C(N1[C@@H]1CC[C@H](CC1)O)C=CC(=C2)C1=C(C=NN1C)C)=O Chemical compound FC=1C=C(C=CC=1F)N1C(CCC[C@H]1C1=NC2=C(N1[C@@H]1CC[C@H](CC1)O)C=CC(=C2)C1=C(C=NN1C)C)=O MWIWFLRUTYDDEI-ZVOVDXHFSA-N 0.000 claims 1
- 101710135898 Myc proto-oncogene protein Proteins 0.000 claims 1
- 102100038895 Myc proto-oncogene protein Human genes 0.000 claims 1
- 102000007399 Nuclear hormone receptor Human genes 0.000 claims 1
- 108020005497 Nuclear hormone receptor Proteins 0.000 claims 1
- 101710150448 Transcriptional regulator Myc Proteins 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 230000003197 catalytic effect Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 230000004777 loss-of-function mutation Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- GJVFBWCTGUSGDD-UHFFFAOYSA-L pentamethonium bromide Chemical compound [Br-].[Br-].C[N+](C)(C)CCCCC[N+](C)(C)C GJVFBWCTGUSGDD-UHFFFAOYSA-L 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 125000003003 spiro group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1617627.3A GB201617627D0 (en) | 2016-10-18 | 2016-10-18 | Pharmaceutical compounds |
| GB1617627.3 | 2016-10-18 | ||
| PCT/GB2017/053153 WO2018073587A1 (en) | 2016-10-18 | 2017-10-18 | Pharmaceutical compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019535658A JP2019535658A (ja) | 2019-12-12 |
| JP2019535658A5 true JP2019535658A5 (cg-RX-API-DMAC7.html) | 2020-11-26 |
| JP7082616B2 JP7082616B2 (ja) | 2022-06-08 |
Family
ID=57680679
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019520591A Active JP7082616B2 (ja) | 2016-10-18 | 2017-10-18 | 医薬化合物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US10647704B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3529240B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP7082616B2 (cg-RX-API-DMAC7.html) |
| CN (1) | CN110036002B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2017346454B2 (cg-RX-API-DMAC7.html) |
| DK (1) | DK3529240T3 (cg-RX-API-DMAC7.html) |
| ES (1) | ES2824814T3 (cg-RX-API-DMAC7.html) |
| GB (1) | GB201617627D0 (cg-RX-API-DMAC7.html) |
| HU (1) | HUE052107T2 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2018073587A1 (cg-RX-API-DMAC7.html) |
| ZA (1) | ZA201902335B (cg-RX-API-DMAC7.html) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201617630D0 (en) * | 2016-10-18 | 2016-11-30 | Cellcentric Ltd | Pharmaceutical compounds |
| CA3075880A1 (en) | 2017-09-15 | 2019-03-21 | Forma Therapeutics, Inc. | Tetrahydro-imidazo quinoline compositions as cbp/p300 inhibitors |
| MX2023013508A (es) | 2018-06-29 | 2023-12-13 | Forma Therapeutics Inc | Inhibicion de la proteina de union a creb (cbp). |
| EP3937940A4 (en) | 2019-03-15 | 2022-12-21 | Forma Therapeutics, Inc. | Inhibiting cyclic amp-responsive element-binding protein (creb) |
| CN112574189B (zh) * | 2019-09-27 | 2024-05-31 | 海创药业股份有限公司 | 一种ep300/cbp抑制剂 |
| CN112574191B (zh) * | 2019-09-29 | 2024-01-23 | 南京圣和药业股份有限公司 | 异噁唑杂环类化合物及其应用 |
| US11795168B2 (en) | 2020-09-23 | 2023-10-24 | Forma Therapeutics, Inc. | Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP) |
| US11801243B2 (en) | 2020-09-23 | 2023-10-31 | Forma Therapeutics, Inc. | Bromodomain inhibitors for androgen receptor-driven cancers |
| TW202227429A (zh) * | 2020-11-06 | 2022-07-16 | 大陸商貝達藥業股份有限公司 | Ｐ３００抑制劑、包含其的藥物組合物、其應用及製備其的方法 |
| US20240109879A1 (en) * | 2020-12-31 | 2024-04-04 | Medshine Discovery Inc. | Benzimidazole compound and application thereof |
| CN114989158A (zh) * | 2021-03-02 | 2022-09-02 | 复旦大学 | 组蛋白乙酰转移酶p300溴结构域抑制剂及其药用组合物及其应用 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200501960A (en) * | 2002-10-02 | 2005-01-16 | Bristol Myers Squibb Co | Synergistic kits and compositions for treating cancer |
| AU2006311433B2 (en) * | 2005-11-08 | 2012-06-28 | Choongwae Pharma Corporation | Alpha-helix mimetics and method relating to the treatment of cancer stem cells |
| US8501957B2 (en) | 2008-12-10 | 2013-08-06 | China Medical University | Benzimidazole compounds and their use as anticancer agents |
| WO2011085039A2 (en) * | 2010-01-05 | 2011-07-14 | The Johns Hopkins University | Use of histone acetyltransferase inhibitors as novel anti-cancer therapies |
| EP2397471A1 (en) | 2010-06-16 | 2011-12-21 | China Medical University | Benzimidazole compounds and their use |
| TWI527811B (zh) | 2013-05-09 | 2016-04-01 | 吉李德科學股份有限公司 | 作爲溴結構域抑制劑的苯並咪唑衍生物 |
| WO2015004534A2 (en) * | 2013-06-21 | 2015-01-15 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| JP6771464B2 (ja) * | 2014-11-27 | 2020-10-21 | ジェネンテック， インコーポレイテッド | Ｃｂｐおよび／またはｅｐ３００インヒビターとしての、４，５，６，７−テトラヒドロ−１ｈ−ピラゾロ［４，３−ｃ］ピリジン−３−アミン化合物 |
| CA2966452A1 (en) | 2014-12-17 | 2016-06-23 | Samuel David Brown | Substituted bicyclic compounds as bromodomain inhibitors |
| GB201506658D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| CN108137539B (zh) | 2015-08-12 | 2022-01-11 | 尼奥迈德研究所 | 取代的苯并咪唑、它们的制备和它们作为药物的用途 |
| GB201617630D0 (en) * | 2016-10-18 | 2016-11-30 | Cellcentric Ltd | Pharmaceutical compounds |
-
2016
- 2016-10-18 GB GBGB1617627.3A patent/GB201617627D0/en not_active Ceased
-
2017
- 2017-10-18 WO PCT/GB2017/053153 patent/WO2018073587A1/en not_active Ceased
- 2017-10-18 HU HUE17790814A patent/HUE052107T2/hu unknown
- 2017-10-18 EP EP17790814.2A patent/EP3529240B1/en active Active
- 2017-10-18 US US16/341,650 patent/US10647704B2/en active Active
- 2017-10-18 CN CN201780072397.7A patent/CN110036002B/zh active Active
- 2017-10-18 JP JP2019520591A patent/JP7082616B2/ja active Active
- 2017-10-18 AU AU2017346454A patent/AU2017346454B2/en active Active
- 2017-10-18 DK DK17790814.2T patent/DK3529240T3/da active
- 2017-10-18 ES ES17790814T patent/ES2824814T3/es active Active
-
2019
- 2019-04-12 ZA ZA2019/02335A patent/ZA201902335B/en unknown
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