JP2017522383A5 - - Google Patents
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- Publication number
- JP2017522383A5 JP2017522383A5 JP2017523185A JP2017523185A JP2017522383A5 JP 2017522383 A5 JP2017522383 A5 JP 2017522383A5 JP 2017523185 A JP2017523185 A JP 2017523185A JP 2017523185 A JP2017523185 A JP 2017523185A JP 2017522383 A5 JP2017522383 A5 JP 2017522383A5
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- JP
- Japan
- Prior art keywords
- compound
- pharmaceutical composition
- alkyl
- disease
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims 19
- 239000008194 pharmaceutical composition Substances 0.000 claims 17
- 125000000217 alkyl group Chemical group 0.000 claims 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 102000004245 Proteasome Endopeptidase Complex Human genes 0.000 claims 5
- 108090000708 Proteasome Endopeptidase Complex Proteins 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- DGYIJVNZSDYBOE-UHFFFAOYSA-N [CH2]C1=CC=NC=C1 Chemical group [CH2]C1=CC=NC=C1 DGYIJVNZSDYBOE-UHFFFAOYSA-N 0.000 claims 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 238000007913 intrathecal administration Methods 0.000 claims 2
- 239000002184 metal Substances 0.000 claims 2
- -1 methyl - oxy - methyl Chemical group 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 238000007920 subcutaneous administration Methods 0.000 claims 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 1
- 208000010444 Acidosis Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000031886 HIV Infections Diseases 0.000 claims 1
- 208000037357 HIV infectious disease Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 206010028289 Muscle atrophy Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000030852 Parasitic disease Diseases 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 230000007950 acidosis Effects 0.000 claims 1
- 208000026545 acidosis disease Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 230000030741 antigen processing and presentation Effects 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 230000008468 bone growth Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000004452 carbocyclyl group Chemical group 0.000 claims 1
- 230000003197 catalytic effect Effects 0.000 claims 1
- 230000003247 decreasing effect Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 208000037824 growth disorder Diseases 0.000 claims 1
- 230000003779 hair growth Effects 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 238000001802 infusion Methods 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 238000001361 intraarterial administration Methods 0.000 claims 1
- 238000007918 intramuscular administration Methods 0.000 claims 1
- 238000007912 intraperitoneal administration Methods 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 201000000585 muscular atrophy Diseases 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 231100000189 neurotoxic Toxicity 0.000 claims 1
- 230000002887 neurotoxic effect Effects 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
- 230000006648 viral gene expression Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462024024P | 2014-07-14 | 2014-07-14 | |
| US62/024,024 | 2014-07-14 | ||
| PCT/US2015/040459 WO2016011088A2 (en) | 2014-07-14 | 2015-07-14 | Epoxyketone compounds for enzyme inhibition |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017522383A JP2017522383A (ja) | 2017-08-10 |
| JP2017522383A5 true JP2017522383A5 (enExample) | 2018-06-21 |
| JP6608442B2 JP6608442B2 (ja) | 2019-11-20 |
Family
ID=55079165
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017523185A Active JP6608442B2 (ja) | 2014-07-14 | 2015-07-14 | 酵素阻害に用いられるエポキシケトン化合物 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US10640533B2 (enExample) |
| EP (1) | EP3166933B1 (enExample) |
| JP (1) | JP6608442B2 (enExample) |
| KR (2) | KR102462240B1 (enExample) |
| CN (1) | CN105960399B (enExample) |
| DK (1) | DK3166933T3 (enExample) |
| ES (1) | ES2704056T3 (enExample) |
| PT (1) | PT3166933T (enExample) |
| TR (1) | TR201816372T4 (enExample) |
| WO (1) | WO2016011088A2 (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6608442B2 (ja) | 2014-07-14 | 2019-11-20 | セントラックス インターナショナル,インコーポレイテッド | 酵素阻害に用いられるエポキシケトン化合物 |
| WO2021072212A1 (en) * | 2019-10-11 | 2021-04-15 | Mayo Foundation For Medical Education And Research | Proteasome inhibitors |
| TWI869142B (zh) * | 2022-12-27 | 2025-01-01 | 大陸商上海美悦生物科技發展有限公司 | 三肽環氧酮化合物、藥物組合物及其製備方法和用途 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0509879A (pt) | 2004-04-15 | 2007-10-16 | Proteolix Inc | compostos para inibição enzimática |
| US20050256324A1 (en) | 2004-05-10 | 2005-11-17 | Proteolix, Inc. | Synthesis of amino acid keto-epoxides |
| PT2261236E (pt) * | 2004-12-07 | 2015-10-30 | Onyx Therapeutics Inc | Composição para a inibição de proteassoma |
| NZ595196A (en) | 2005-11-09 | 2013-03-28 | Proteolix Inc | Peptide-based compounds for enzyme inhibition |
| WO2008140782A2 (en) | 2007-05-10 | 2008-11-20 | Proteolix, Inc. | Compounds for enzyme inhibition |
| EA035100B1 (ru) * | 2008-10-21 | 2020-04-28 | Оникс Терапьютикс, Инк. | Комбинированная терапия с применением пептид эпоксикетонов |
| RU2012147246A (ru) * | 2010-04-07 | 2014-05-20 | Оникс Терапьютикс, Инк. | Кристаллический пептидный эпоксикетонный ингебитор иммунопротеасомы |
| EP4144354B1 (en) * | 2011-08-30 | 2025-11-26 | Trustees Of Tufts College | Fap-activated proteasome inhibitors for treating solid tumors |
| US9388126B2 (en) | 2012-07-19 | 2016-07-12 | Drexel University | Sigma receptor ligands and methods of modulating cellular protein homeostasis using same |
| WO2014018807A1 (en) | 2012-07-26 | 2014-01-30 | Centrax International, Inc. | Peptide epoxyketone compounds |
| AU2013302269A1 (en) * | 2012-08-14 | 2015-03-12 | Trillium Therapeutics Inc. | Fluorinated epoxyketone-based compounds and uses thereof as proteasome inhibitors |
| CA2881986A1 (en) | 2012-08-21 | 2014-02-27 | Fluorinov Pharma Inc. | Fluorinated epoxyketone-based tetrapeptide compounds and uses thereof as proteasome inhibitors |
| JP6608442B2 (ja) | 2014-07-14 | 2019-11-20 | セントラックス インターナショナル,インコーポレイテッド | 酵素阻害に用いられるエポキシケトン化合物 |
-
2015
- 2015-07-14 JP JP2017523185A patent/JP6608442B2/ja active Active
- 2015-07-14 TR TR2018/16372T patent/TR201816372T4/tr unknown
- 2015-07-14 KR KR1020217022768A patent/KR102462240B1/ko active Active
- 2015-07-14 ES ES15821964T patent/ES2704056T3/es active Active
- 2015-07-14 KR KR1020177004070A patent/KR102360356B1/ko active Active
- 2015-07-14 DK DK15821964.2T patent/DK3166933T3/en active
- 2015-07-14 EP EP15821964.2A patent/EP3166933B1/en active Active
- 2015-07-14 US US15/325,998 patent/US10640533B2/en active Active
- 2015-07-14 WO PCT/US2015/040459 patent/WO2016011088A2/en not_active Ceased
- 2015-07-14 PT PT15821964T patent/PT3166933T/pt unknown
- 2015-07-14 CN CN201580002532.1A patent/CN105960399B/zh active Active
-
2019
- 2019-10-28 US US16/665,010 patent/US10787482B2/en active Active