JP2013518129A5 - - Google Patents
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- JP2013518129A5 JP2013518129A5 JP2012551323A JP2012551323A JP2013518129A5 JP 2013518129 A5 JP2013518129 A5 JP 2013518129A5 JP 2012551323 A JP2012551323 A JP 2012551323A JP 2012551323 A JP2012551323 A JP 2012551323A JP 2013518129 A5 JP2013518129 A5 JP 2013518129A5
- Authority
- JP
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- Prior art keywords
- alkyl
- proteasome
- fluoroalkyl
- haloalkyl
- compound according
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims 37
- 150000001875 compounds Chemical class 0.000 claims 30
- 102000004245 Proteasome Endopeptidase Complex Human genes 0.000 claims 18
- 108090000708 Proteasome Endopeptidase Complex Proteins 0.000 claims 18
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 15
- 125000001188 haloalkyl group Chemical group 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 14
- 239000012453 solvate Substances 0.000 claims 14
- 229940002612 prodrug Drugs 0.000 claims 13
- 239000000651 prodrug Substances 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 238000000034 method Methods 0.000 claims 11
- 150000002431 hydrogen Chemical class 0.000 claims 10
- 101100371648 Caenorhabditis elegans usp-14 gene Proteins 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000005843 halogen group Chemical group 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- -1 4-methylpiperidin-1-yl Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 125000003710 aryl alkyl group Chemical group 0.000 claims 6
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 6
- 125000004438 haloalkoxy group Chemical group 0.000 claims 6
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 125000000547 substituted alkyl group Chemical group 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 5
- JUWDSDKJBMFLHE-UHFFFAOYSA-N 1-[1-(4-fluorophenyl)-2,5-dimethylpyrrol-3-yl]-2-pyrrolidin-1-ylethanone Chemical compound CC=1N(C=2C=CC(F)=CC=2)C(C)=CC=1C(=O)CN1CCCC1 JUWDSDKJBMFLHE-UHFFFAOYSA-N 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 2
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 241001529936 Murinae Species 0.000 claims 2
- 102000007056 Recombinant Fusion Proteins Human genes 0.000 claims 2
- 108010008281 Recombinant Fusion Proteins Proteins 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- ICCBZGUDUOMNOF-UHFFFAOYSA-N azidoamine Chemical compound NN=[N+]=[N-] ICCBZGUDUOMNOF-UHFFFAOYSA-N 0.000 claims 2
- 230000009504 deubiquitination Effects 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 239000000758 substrate Substances 0.000 claims 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical group C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- 239000005977 Ethylene Chemical group 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000005090 alkenylcarbonyl group Chemical group 0.000 claims 1
- 125000005193 alkenylcarbonyloxy group Chemical group 0.000 claims 1
- 125000003302 alkenyloxy group Chemical group 0.000 claims 1
- 125000005092 alkenyloxycarbonyl group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 1
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000005087 alkynylcarbonyl group Chemical group 0.000 claims 1
- 125000005198 alkynylcarbonyloxy group Chemical group 0.000 claims 1
- 125000005133 alkynyloxy group Chemical group 0.000 claims 1
- 125000005225 alkynyloxycarbonyl group Chemical group 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 125000001091 aminosulfinyl group Chemical group [H]N([H])S(*)=O 0.000 claims 1
- 150000001540 azides Chemical class 0.000 claims 1
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims 1
- 150000005347 biaryls Chemical group 0.000 claims 1
- 125000004452 carbocyclyl group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical group C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 1
- 125000004993 haloalkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004692 haloalkylcarbonyl group Chemical group 0.000 claims 1
- 125000005203 haloalkylcarbonyloxy group Chemical group 0.000 claims 1
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 125000005322 morpholin-1-yl group Chemical group 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000001181 organosilyl group Chemical group [SiH3]* 0.000 claims 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- LFGREXWGYUGZLY-UHFFFAOYSA-N phosphoryl Chemical group [P]=O LFGREXWGYUGZLY-UHFFFAOYSA-N 0.000 claims 1
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 230000017854 proteolysis Effects 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 238000012216 screening Methods 0.000 claims 1
- 125000004469 siloxy group Chemical group [SiH3]O* 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 1
- 229920002554 vinyl polymer Polymers 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US33695910P | 2010-01-28 | 2010-01-28 | |
| US61/336,959 | 2010-01-28 | ||
| US37340410P | 2010-08-13 | 2010-08-13 | |
| US61/373,404 | 2010-08-13 | ||
| PCT/US2011/022929 WO2011094545A2 (en) | 2010-01-28 | 2011-01-28 | Compositions and methods for enhancing proteasome activity |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016060063A Division JP6371786B2 (ja) | 2010-01-28 | 2016-03-24 | プロテアソーム活性を向上させるための組成物および方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013518129A JP2013518129A (ja) | 2013-05-20 |
| JP2013518129A5 true JP2013518129A5 (enExample) | 2013-12-26 |
Family
ID=44320152
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012551323A Pending JP2013518129A (ja) | 2010-01-28 | 2011-01-28 | プロテアソーム活性を向上させるための組成物および方法 |
| JP2016060063A Expired - Fee Related JP6371786B2 (ja) | 2010-01-28 | 2016-03-24 | プロテアソーム活性を向上させるための組成物および方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016060063A Expired - Fee Related JP6371786B2 (ja) | 2010-01-28 | 2016-03-24 | プロテアソーム活性を向上させるための組成物および方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US20130045992A1 (enExample) |
| EP (1) | EP2528911B1 (enExample) |
| JP (2) | JP2013518129A (enExample) |
| KR (1) | KR20120117905A (enExample) |
| CN (1) | CN102844313B (enExample) |
| AU (1) | AU2011210765A1 (enExample) |
| BR (1) | BR112012018631A8 (enExample) |
| CA (1) | CA2787785C (enExample) |
| MX (1) | MX336731B (enExample) |
| RU (1) | RU2012136451A (enExample) |
| SG (1) | SG182662A1 (enExample) |
| WO (1) | WO2011094545A2 (enExample) |
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112012018631A8 (pt) | 2010-01-28 | 2017-12-19 | President And Fellows Of Harvard Colege | composições e métodos para intensificação da atividade do proteassoma |
| CA2808432C (en) | 2010-07-23 | 2019-06-04 | President And Fellows Of Harvard College | Tricyclic proteasome activity enhancing compounds with thieno[2,3-d]pyrimidine core |
| ES2724531T3 (es) * | 2011-05-12 | 2019-09-11 | Proteostasis Therapeutics Inc | Reguladores de proteostasis |
| EP2756310B1 (en) * | 2011-09-16 | 2017-05-03 | Vivolux Ab | Proteasome deubiquitinating inhibitor screening |
| JP2015504919A (ja) * | 2012-01-25 | 2015-02-16 | プロテオステイシス セラピューティクス，インコーポレイテッド | プロテアソーム活性を調節する化合物 |
| JP2016504365A (ja) | 2012-12-28 | 2016-02-12 | アメリカ合衆国 | Ｕｓｐ１／ｕａｆ１デユビキチナーゼ複合体阻害剤及びその使用 |
| WO2014116228A1 (en) * | 2013-01-25 | 2014-07-31 | President And Fellows Of Harvard College | Usp14 inhibitors for treating or preventing viral infections |
| US10563225B2 (en) * | 2013-07-26 | 2020-02-18 | President And Fellows Of Harvard College | Genome engineering |
| WO2015073528A1 (en) | 2013-11-12 | 2015-05-21 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
| JP6466461B2 (ja) | 2014-02-03 | 2019-02-06 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | Ｒｏｒガンマのジヒドロピロロピリジン阻害剤 |
| CN104844704B (zh) * | 2014-02-17 | 2018-02-23 | 华东师范大学 | Ub‑Nanoluc、Ub‑Ub‑GS‑Nanoluc报告基因系统及其构建和应用 |
| EP3207043B3 (en) | 2014-10-14 | 2019-10-02 | Vitae Pharmaceuticals, LLC | Dihydropyrrolopyridine inhibitors of ror-gamma |
| US9845308B2 (en) | 2014-11-05 | 2017-12-19 | Vitae Pharmaceuticals, Inc. | Isoindoline inhibitors of ROR-gamma |
| US9663515B2 (en) | 2014-11-05 | 2017-05-30 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| CN104478780B (zh) * | 2014-11-17 | 2017-04-19 | 华东师范大学 | 酰基吡咯类小分子有机化合物及其衍生物、用途及其制备方法 |
| DK3331876T3 (da) | 2015-08-05 | 2021-01-11 | Vitae Pharmaceuticals Llc | Modulators of ror-gamma |
| EP3377482B1 (en) | 2015-11-20 | 2021-05-12 | Vitae Pharmaceuticals, LLC | Modulators of ror-gamma |
| GB201521109D0 (en) * | 2015-11-30 | 2016-01-13 | Mission Therapeutics Ltd | Novel compounds |
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| TWI757266B (zh) | 2016-01-29 | 2022-03-11 | 美商維它藥物有限責任公司 | ＲＯＲ－γ調節劑 |
| CN109641874A (zh) | 2016-05-10 | 2019-04-16 | C4医药公司 | 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体 |
| WO2017197051A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Amine-linked c3-glutarimide degronimers for target protein degradation |
| EP3454856B1 (en) * | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| US9481674B1 (en) | 2016-06-10 | 2016-11-01 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| CN106281935A (zh) * | 2016-08-08 | 2017-01-04 | 山东理工大学 | 一种促进中性蛋白酶活性的方法及其在啤酒澄清中的应用 |
| CN106065389A (zh) * | 2016-08-08 | 2016-11-02 | 山东理工大学 | 一种促进木瓜蛋白酶活性的方法及其在啤酒澄清中的应用 |
| CN107903208B (zh) * | 2016-12-26 | 2021-09-03 | 杭州市西溪医院 | 一类联芳吡啶类去泛素化酶抑制剂、其制备方法及应用 |
| EP3641762A4 (en) | 2017-06-20 | 2021-03-10 | C4 Therapeutics, Inc. | N / O-LINKED DEGRONES AND DEGRONIMERS FOR PROTEIN DEGRADATION |
| BR112020001246A2 (pt) | 2017-07-24 | 2020-07-21 | Vitae Pharmaceuticals, Llc | inibidores de rory |
| WO2019018975A1 (en) | 2017-07-24 | 2019-01-31 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF ROR GAMMA |
| CN111372585A (zh) | 2017-11-16 | 2020-07-03 | C4医药公司 | 用于靶蛋白降解的降解剂和降解决定子 |
| EP3773576A4 (en) | 2018-03-26 | 2021-12-29 | C4 Therapeutics, Inc. | Cereblon binders for the degradation of ikaros |
| EP3781156A4 (en) | 2018-04-16 | 2022-05-18 | C4 Therapeutics, Inc. | SPIROCYCLIC COMPOUNDS |
| SG11202013026WA (en) * | 2018-06-27 | 2021-01-28 | Proteostasis Therapeutics Inc | Proteasome activity enhancing compounds |
| JP7551087B2 (ja) * | 2018-06-27 | 2024-09-17 | キネタ， インコーポレイテッド | プロテアソーム活性増強化合物 |
| EP3897631A4 (en) | 2018-12-20 | 2022-11-23 | C4 Therapeutics, Inc. | TARGETED PROTEIN BREAKDOWN |
| CN115190804A (zh) * | 2020-01-14 | 2022-10-14 | 纽约市哥伦比亚大学理事会 | 通过重定向内源性去泛素化酶稳定靶向蛋白质的组合物和方法 |
| JP2022012379A (ja) * | 2020-07-01 | 2022-01-17 | 国立大学法人富山大学 | ユビキチン－プロテアソーム系の活性化剤、およびその利用 |
| WO2022250363A1 (ko) * | 2021-05-24 | 2022-12-01 | 재단법인대구경북과학기술원 | 아이유원 계열의 유비퀴틴 특이적 프로테아제 14 억제제를 유효성분으로 포함하는, 프로탁의 항암 효과 증진용 약학적 조성물 |
| WO2025219559A1 (en) * | 2024-04-18 | 2025-10-23 | Booster Therapeutics Gmbh | Pyrrolidine compounds as proteasome stimulators |
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2011
- 2011-01-28 BR BR112012018631A patent/BR112012018631A8/pt not_active Application Discontinuation
- 2011-01-28 CA CA2787785A patent/CA2787785C/en not_active Expired - Fee Related
- 2011-01-28 RU RU2012136451/04A patent/RU2012136451A/ru not_active Application Discontinuation
- 2011-01-28 SG SG2012054235A patent/SG182662A1/en unknown
- 2011-01-28 JP JP2012551323A patent/JP2013518129A/ja active Pending
- 2011-01-28 CN CN201180016116.9A patent/CN102844313B/zh not_active Expired - Fee Related
- 2011-01-28 EP EP11737731.7A patent/EP2528911B1/en not_active Not-in-force
- 2011-01-28 WO PCT/US2011/022929 patent/WO2011094545A2/en not_active Ceased
- 2011-01-28 MX MX2012008626A patent/MX336731B/es unknown
- 2011-01-28 AU AU2011210765A patent/AU2011210765A1/en not_active Abandoned
- 2011-01-28 KR KR1020127022300A patent/KR20120117905A/ko not_active Ceased
- 2011-01-28 US US13/575,812 patent/US20130045992A1/en not_active Abandoned
-
2015
- 2015-11-05 US US14/933,671 patent/US10351568B2/en not_active Expired - Fee Related
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2016
- 2016-03-24 JP JP2016060063A patent/JP6371786B2/ja not_active Expired - Fee Related
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