JP2016147893A5 - - Google Patents
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- JP2016147893A5 JP2016147893A5 JP2016060063A JP2016060063A JP2016147893A5 JP 2016147893 A5 JP2016147893 A5 JP 2016147893A5 JP 2016060063 A JP2016060063 A JP 2016060063A JP 2016060063 A JP2016060063 A JP 2016060063A JP 2016147893 A5 JP2016147893 A5 JP 2016147893A5
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- 125000000217 alkyl group Chemical group 0.000 claims 23
- 239000008194 pharmaceutical composition Substances 0.000 claims 18
- 125000001188 haloalkyl group Chemical group 0.000 claims 17
- 125000003545 alkoxy group Chemical group 0.000 claims 15
- 125000005843 halogen group Chemical group 0.000 claims 15
- 125000004438 haloalkoxy group Chemical group 0.000 claims 11
- 125000001424 substituent group Chemical group 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 7
- -1 N-pyrrolidinyl Chemical group 0.000 claims 6
- 206010002022 amyloidosis Diseases 0.000 claims 6
- 150000001540 azides Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 239000012453 solvate Substances 0.000 claims 5
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 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 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000010859 Creutzfeldt-Jakob disease Diseases 0.000 claims 2
- 206010012289 Dementia Diseases 0.000 claims 2
- 208000002339 Frontotemporal Lobar Degeneration Diseases 0.000 claims 2
- 208000021642 Muscular disease Diseases 0.000 claims 2
- 201000009623 Myopathy Diseases 0.000 claims 2
- 150000001408 amides Chemical group 0.000 claims 2
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 2
- 230000007850 degeneration Effects 0.000 claims 2
- 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 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 208000023769 AA amyloidosis Diseases 0.000 claims 1
- 208000023761 AL amyloidosis Diseases 0.000 claims 1
- 208000022385 ALys amyloidosis Diseases 0.000 claims 1
- 208000011403 Alexander disease Diseases 0.000 claims 1
- 102100034452 Alternative prion protein Human genes 0.000 claims 1
- 206010001881 Alveolar proteinosis Diseases 0.000 claims 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 1
- 208000009575 Angelman syndrome Diseases 0.000 claims 1
- 206010059245 Angiopathy Diseases 0.000 claims 1
- 102000005666 Apolipoprotein A-I Human genes 0.000 claims 1
- 108010059886 Apolipoprotein A-I Proteins 0.000 claims 1
- 208000010482 CADASIL Diseases 0.000 claims 1
- 208000002177 Cataract Diseases 0.000 claims 1
- 208000033221 Cerebral autosomal dominant arteriopathy with subcortical infarcts and leukoencephalopathy Diseases 0.000 claims 1
- 208000033935 Cerebral autosomal dominant arteriopathy-subcortical infarcts-leukoencephalopathy Diseases 0.000 claims 1
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 1
- 206010010996 Corneal degeneration Diseases 0.000 claims 1
- 208000020406 Creutzfeldt Jacob disease Diseases 0.000 claims 1
- 208000003407 Creutzfeldt-Jakob Syndrome Diseases 0.000 claims 1
- 206010011659 Cutaneous amyloidosis Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 206010064553 Dialysis amyloidosis Diseases 0.000 claims 1
- 208000034846 Familial Amyloid Neuropathies Diseases 0.000 claims 1
- 206010016202 Familial Amyloidosis Diseases 0.000 claims 1
- 102000008946 Fibrinogen Human genes 0.000 claims 1
- 108010049003 Fibrinogen Proteins 0.000 claims 1
- 201000004176 Gelatinous drop-like corneal dystrophy Diseases 0.000 claims 1
- 208000009119 Giant Axonal Neuropathy Diseases 0.000 claims 1
- 206010019889 Hereditary neuropathic amyloidosis Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 208000005531 Immunoglobulin Light-chain Amyloidosis Diseases 0.000 claims 1
- 102000010445 Lactoferrin Human genes 0.000 claims 1
- 108010063045 Lactoferrin Proteins 0.000 claims 1
- 208000002569 Machado-Joseph Disease Diseases 0.000 claims 1
- 201000002481 Myositis Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000007871 Odontogenic Tumors Diseases 0.000 claims 1
- 206010033799 Paralysis Diseases 0.000 claims 1
- 108091000054 Prion Proteins 0.000 claims 1
- 102000008847 Serpin Human genes 0.000 claims 1
- 108050000761 Serpin Proteins 0.000 claims 1
- 208000009415 Spinocerebellar Ataxias Diseases 0.000 claims 1
- 208000036834 Spinocerebellar ataxia type 3 Diseases 0.000 claims 1
- 208000018756 Variant Creutzfeldt-Jakob disease Diseases 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 230000001746 atrial effect Effects 0.000 claims 1
- 210000004227 basal ganglia Anatomy 0.000 claims 1
- 208000016738 bone Paget disease Diseases 0.000 claims 1
- 208000005881 bovine spongiform encephalopathy Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 208000016886 cerebral arteriopathy with subcortical infarcts and leukoencephalopathy Diseases 0.000 claims 1
- 230000002490 cerebral effect Effects 0.000 claims 1
- 201000006061 fatal familial insomnia Diseases 0.000 claims 1
- 229940012952 fibrinogen Drugs 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 210000003000 inclusion body Anatomy 0.000 claims 1
- 206010023497 kuru Diseases 0.000 claims 1
- CSSYQJWUGATIHM-IKGCZBKSSA-N l-phenylalanyl-l-lysyl-l-cysteinyl-l-arginyl-l-arginyl-l-tryptophyl-l-glutaminyl-l-tryptophyl-l-arginyl-l-methionyl-l-lysyl-l-lysyl-l-leucylglycyl-l-alanyl-l-prolyl-l-seryl-l-isoleucyl-l-threonyl-l-cysteinyl-l-valyl-l-arginyl-l-arginyl-l-alanyl-l-phenylal Chemical compound C([C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CS)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)C1=CC=CC=C1 CSSYQJWUGATIHM-IKGCZBKSSA-N 0.000 claims 1
- 229940078795 lactoferrin Drugs 0.000 claims 1
- 235000021242 lactoferrin Nutrition 0.000 claims 1
- 208000015413 lichen amyloidosis Diseases 0.000 claims 1
- 125000005322 morpholin-1-yl group Chemical group 0.000 claims 1
- 208000027825 odontogenic neoplasm Diseases 0.000 claims 1
- 230000000750 progressive effect Effects 0.000 claims 1
- 208000030153 prolactin-producing pituitary gland adenoma Diseases 0.000 claims 1
- 235000018102 proteins Nutrition 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 210000003994 retinal ganglion cell Anatomy 0.000 claims 1
- 239000003001 serine protease inhibitor Substances 0.000 claims 1
- 208000007056 sickle cell anemia Diseases 0.000 claims 1
- 201000003624 spinocerebellar ataxia type 1 Diseases 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 201000007905 transthyretin amyloidosis Diseases 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 208000006542 von Hippel-Lindau disease Diseases 0.000 claims 1
- 208000027121 wild type ATTR amyloidosis Diseases 0.000 claims 1
Applications Claiming Priority (4)
| 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 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012551323A Division 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016147893A JP2016147893A (ja) | 2016-08-18 |
| JP2016147893A5 true JP2016147893A5 (enExample) | 2016-12-15 |
| JP6371786B2 JP6371786B2 (ja) | 2018-08-08 |
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 Before (1)
| 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 |
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)
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| US20130045992A1 (en) | 2010-01-28 | 2013-02-21 | President And Fellows Of Harvard College | Compositions and Methods for Enhancing Proteasome Activity |
| 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 |
| SI2707101T1 (sl) | 2011-05-12 | 2019-06-28 | Proteostasis Therapeutics, Inc. | Regulatorji proteostaze |
| WO2013039438A1 (en) | 2011-09-16 | 2013-03-21 | Vivolux Ab | Proteasome deubiquinating inhibitor screening |
| WO2013112706A1 (en) | 2012-01-25 | 2013-08-01 | Proteostasis Therapeutics, Inc. | Proteasome activity modulating compounds |
| EP2938610A2 (en) | 2012-12-28 | 2015-11-04 | The U.S.A. as represented by the Secretary, Department of Health and Human Services | Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof |
| WO2014116228A1 (en) * | 2013-01-25 | 2014-07-31 | President And Fellows Of Harvard College | Usp14 inhibitors for treating or preventing viral infections |
| US11306328B2 (en) * | 2013-07-26 | 2022-04-19 | President And Fellows Of Harvard College | Genome engineering |
| WO2015073528A1 (en) | 2013-11-12 | 2015-05-21 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
| CA2938311C (en) | 2014-02-03 | 2023-03-07 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ror-gamma |
| 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 |
| WO2016061160A1 (en) | 2014-10-14 | 2016-04-21 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ror-gamma |
| US9663515B2 (en) | 2014-11-05 | 2017-05-30 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
| US9845308B2 (en) | 2014-11-05 | 2017-12-19 | Vitae Pharmaceuticals, Inc. | Isoindoline 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 |
| ES2856931T3 (es) | 2015-08-05 | 2021-09-28 | Vitae Pharmaceuticals Llc | Moduladores de ROR-gamma |
| BR112018010018A2 (pt) | 2015-11-20 | 2018-11-21 | Vitae Pharmaceuticals Inc | moduladores de ror-gama |
| GB201521109D0 (en) * | 2015-11-30 | 2016-01-13 | Mission Therapeutics Ltd | Novel compounds |
| US20190016680A1 (en) | 2016-01-14 | 2019-01-17 | Beth Israel Deaconess Medical Center, Inc. | Mast-cell modulators and uses thereof |
| 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 |
| WO2017197051A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Amine-linked c3-glutarimide degronimers for target protein degradation |
| WO2017197046A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
| EP4491236A3 (en) | 2016-05-10 | 2025-04-02 | 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 |
| CN118440096A (zh) | 2017-06-20 | 2024-08-06 | C4医药公司 | 用于蛋白降解的n/o-连接的降解决定子和降解决定子体 |
| WO2019018975A1 (en) | 2017-07-24 | 2019-01-31 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF ROR GAMMA |
| MA49685A (fr) | 2017-07-24 | 2021-04-14 | Vitae Pharmaceuticals Llc | INHIBITEURS DE 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 |
| WO2019191112A1 (en) | 2018-03-26 | 2019-10-03 | C4 Therapeutics, Inc. | Cereblon binders for the degradation of ikaros |
| CN119751456A (zh) | 2018-04-16 | 2025-04-04 | C4医药公司 | 螺环化合物 |
| EP3814336A1 (en) * | 2018-06-27 | 2021-05-05 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
| JP7561632B2 (ja) * | 2018-06-27 | 2024-10-04 | 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 |
| CN120698983A (zh) | 2018-12-20 | 2025-09-26 | C4医药公司 | 靶向蛋白降解 |
| AU2021207643A1 (en) * | 2020-01-14 | 2022-08-18 | The Trustees Of Columbia University In The City Of New York | Compositions and methods for targeted protein stabilization by redirecting endogenous deubiquitinases |
| 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 US US13/575,812 patent/US20130045992A1/en not_active Abandoned
- 2011-01-28 MX MX2012008626A patent/MX336731B/es unknown
- 2011-01-28 SG SG2012054235A patent/SG182662A1/en unknown
- 2011-01-28 AU AU2011210765A patent/AU2011210765A1/en not_active Abandoned
- 2011-01-28 CA CA2787785A patent/CA2787785C/en not_active Expired - Fee Related
- 2011-01-28 BR BR112012018631A patent/BR112012018631A8/pt not_active Application Discontinuation
- 2011-01-28 KR KR1020127022300A patent/KR20120117905A/ko not_active Ceased
- 2011-01-28 CN CN201180016116.9A patent/CN102844313B/zh not_active Expired - Fee Related
- 2011-01-28 WO PCT/US2011/022929 patent/WO2011094545A2/en not_active Ceased
- 2011-01-28 RU RU2012136451/04A patent/RU2012136451A/ru not_active Application Discontinuation
- 2011-01-28 JP JP2012551323A patent/JP2013518129A/ja active Pending
- 2011-01-28 EP EP11737731.7A patent/EP2528911B1/en not_active Not-in-force
-
2015
- 2015-11-05 US US14/933,671 patent/US10351568B2/en not_active Expired - Fee Related
-
2016
- 2016-03-24 JP JP2016060063A patent/JP6371786B2/ja not_active Expired - Fee Related
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