JPWO2020006269A5 - - Google Patents
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- Publication number
- JPWO2020006269A5 JPWO2020006269A5 JP2020573467A JP2020573467A JPWO2020006269A5 JP WO2020006269 A5 JPWO2020006269 A5 JP WO2020006269A5 JP 2020573467 A JP2020573467 A JP 2020573467A JP 2020573467 A JP2020573467 A JP 2020573467A JP WO2020006269 A5 JPWO2020006269 A5 JP WO2020006269A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- solvate
- pharmaceutically acceptable
- prodrug
- 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 description 48
- 150000001875 compounds Chemical class 0.000 claims description 37
- 229910052739 hydrogen Inorganic materials 0.000 claims description 36
- 239000001257 hydrogen Substances 0.000 claims description 36
- 150000003839 salts Chemical class 0.000 claims description 35
- 239000012453 solvate Substances 0.000 claims description 35
- 229940002612 prodrug Drugs 0.000 claims description 34
- 239000000651 prodrug Substances 0.000 claims description 34
- 150000002431 hydrogen Chemical class 0.000 claims description 27
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 22
- 125000000623 heterocyclic group Chemical group 0.000 claims description 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 17
- 125000001072 heteroaryl group Chemical group 0.000 claims description 15
- 229910052757 nitrogen Inorganic materials 0.000 claims description 14
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 13
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 11
- 229910052799 carbon Inorganic materials 0.000 claims description 10
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 9
- 125000001475 halogen functional group Chemical group 0.000 claims description 8
- 125000000304 alkynyl group Chemical group 0.000 claims description 6
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 5
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims description 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 3
- 125000003342 alkenyl group Chemical group 0.000 claims description 3
- 125000003545 alkoxy group Chemical group 0.000 claims description 3
- 125000003118 aryl group Chemical group 0.000 claims description 3
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 3
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 3
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims description 3
- 125000001424 substituent group Chemical group 0.000 claims description 3
- 125000003107 substituted aryl group Chemical group 0.000 claims description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 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 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000007111 proteostasis Effects 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024076047A JP2024112835A (ja) | 2018-06-27 | 2024-05-08 | プロテアソーム活性増強化合物 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862690554P | 2018-06-27 | 2018-06-27 | |
| US62/690,554 | 2018-06-27 | ||
| PCT/US2019/039562 WO2020006269A1 (en) | 2018-06-27 | 2019-06-27 | Proteasome activity enhancing compounds |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024076047A Division JP2024112835A (ja) | 2018-06-27 | 2024-05-08 | プロテアソーム活性増強化合物 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021530465A JP2021530465A (ja) | 2021-11-11 |
| JP2021530465A5 JP2021530465A5 (https=) | 2022-07-01 |
| JPWO2020006269A5 true JPWO2020006269A5 (https=) | 2022-07-01 |
| JP7551087B2 JP7551087B2 (ja) | 2024-09-17 |
Family
ID=67297405
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020573467A Active JP7551087B2 (ja) | 2018-06-27 | 2019-06-27 | プロテアソーム活性増強化合物 |
| JP2024076047A Withdrawn JP2024112835A (ja) | 2018-06-27 | 2024-05-08 | プロテアソーム活性増強化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024076047A Withdrawn JP2024112835A (ja) | 2018-06-27 | 2024-05-08 | プロテアソーム活性増強化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US11746098B2 (https=) |
| EP (1) | EP3814336A1 (https=) |
| JP (2) | JP7551087B2 (https=) |
| CN (1) | CN112585130A (https=) |
| WO (1) | WO2020006269A1 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112585130A (zh) * | 2018-06-27 | 2021-03-30 | 蛋白质平衡治疗股份有限公司 | 蛋白酶体活性增强化合物 |
| CN114699394B (zh) * | 2022-05-24 | 2022-09-13 | 中山大学附属第一医院 | 用于肝癌放疗增敏的药物组合物及其应用 |
Family Cites Families (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1142508A (en) * | 1966-04-27 | 1969-02-12 | Whitefin Holding Sa | Pyrrole derivatives |
| GB1154744A (en) * | 1966-05-17 | 1969-06-11 | Whitefin Holding Sa | Disubstituted Aminoethanols |
| CZ20002669A3 (cs) | 1998-01-23 | 2001-11-14 | National Jewish Medical And Research Center | Pouľití proteinů tepelného ąoku nebo molekuly nukleové kyseliny, která jej kóduje, přípravek tyto látky obsahující, způsob výběru léčby přecitlivělosti nebo nedostatečnosti průchodu dýchacích cest |
| US7842470B2 (en) | 2001-10-09 | 2010-11-30 | Oregon Health & Science University | Method for pharmacoperones correction of GnRHR mutant protein misfolding |
| US20060148767A1 (en) | 2001-12-06 | 2006-07-06 | George Cioca | Use of acyl salicylates as heat shock inducers |
| EP1682504B1 (en) | 2003-11-12 | 2012-12-26 | Amicus Therapeutics Inc. | Hydroxy piperidine derivatives to treat gaucher disease |
| EP2932982B1 (en) | 2005-05-17 | 2018-10-03 | Amicus Therapeutics, Inc. | A method for the treatment of pompe disease using 1-deoxynojirimycin and derivatives |
| CN101541172A (zh) | 2005-06-08 | 2009-09-23 | 阿米库斯治疗学公司 | 溶酶体酶编码基因突变相关的cns紊乱的治疗 |
| US20070207992A1 (en) | 2006-02-21 | 2007-09-06 | Board Of Trustees Of Michigan State University | Geldanamycin derivatives and method of use thereof |
| WO2007131034A1 (en) | 2006-05-03 | 2007-11-15 | The Regents Of The University Of Michigan | Pyrimidone derivatives which are modulators of heat shock protein (hsp) 70 |
| ES2573498T3 (es) | 2006-05-16 | 2016-06-08 | Amicus Therapeutics, Inc. | Opciones de tratamiento para la enfermedad de Fabry |
| PT1860101E (pt) | 2006-05-24 | 2011-07-12 | Amicus Therapeutics Inc | Sal de tartrato da isofagomina e métodos de uso |
| JP5303458B2 (ja) | 2006-06-23 | 2013-10-02 | アミークス セラピューティックス インコーポレイテッド | β−グルコセレブロシダーゼの活性増強による神経学的疾患の治療方法 |
| US8143269B2 (en) * | 2008-10-03 | 2012-03-27 | Calcimedica, Inc. | Inhibitors of store operated calcium release |
| MX336731B (es) * | 2010-01-28 | 2016-01-28 | Harvard College | Composiciones y metodos para potenciar la actividad de proteasoma. |
| WO2011127333A2 (en) * | 2010-04-09 | 2011-10-13 | University Of Louisville Research Foundation, Inc. | Compounds for treating disease, for administering, and for pharmaceutical compositions |
| WO2012078902A2 (en) | 2010-12-08 | 2012-06-14 | Proteostasis Therapeutics, Inc. | Proteostasis regulators |
| WO2012078909A1 (en) | 2010-12-08 | 2012-06-14 | Proteostasis Therapeutics, Inc. | Thiazolpyrimidine proteostasis regulators |
| WO2012154880A1 (en) | 2011-05-09 | 2012-11-15 | Proteostasis Therapeutics, Inc. | Proteostasis regulators for treating cystic fibrosis and other protein misfolding diseases |
| DK2707101T3 (da) * | 2011-05-12 | 2019-05-13 | Proteostasis Therapeutics Inc | Proteostaseregulatorer |
| WO2013112699A2 (en) | 2012-01-25 | 2013-08-01 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
| CA2861464C (en) | 2012-01-25 | 2018-03-06 | Proteostasis Therapeutics, Inc. | Proteasome activity modulating tricyclic compounds |
| US9849135B2 (en) * | 2013-01-25 | 2017-12-26 | President And Fellows Of Harvard College | USP14 inhibitors for treating or preventing viral infections |
| AU2014302458A1 (en) | 2013-06-26 | 2015-12-24 | Proteostasis Therapeutics, Inc. | Methods of modulating CFTR activity |
| WO2015073528A1 (en) | 2013-11-12 | 2015-05-21 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
| US9745292B2 (en) | 2014-03-13 | 2017-08-29 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing CFTR activity |
| WO2015138909A1 (en) | 2014-03-13 | 2015-09-17 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing cftr activity |
| EP3157917B1 (en) | 2014-06-19 | 2020-03-18 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods of increasing cftr activity |
| 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 |
| US10738011B2 (en) | 2014-12-23 | 2020-08-11 | Proteostasis Therapeutics, Inc. | Derivatives of 5-(hetero)arylpyrazol-3-carboxylic amide or 1-(hetero)aryltriazol-4-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| US10392378B2 (en) | 2014-12-23 | 2019-08-27 | Proteostasis Therapeutics, Inc. | Derivatives of 5-phenyl- or 5-heteroarylathiazol-2-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| US10344023B2 (en) | 2014-12-23 | 2019-07-09 | Proteostasis Therapeutics, Inc. | Derivatives of 3-heteroarylisoxazol-5-carboxylic amide useful for the treatment of inter alia cystic fibrosis |
| MA41253A (fr) | 2014-12-23 | 2017-10-31 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
| US20180147187A1 (en) | 2015-01-12 | 2018-05-31 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing cftr activity |
| US10548878B2 (en) | 2015-07-24 | 2020-02-04 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods of increasing CFTR activity |
| US20190022071A1 (en) | 2015-08-31 | 2019-01-24 | Proteostasis Therapeutics, Inc. | Methods of treating pulmonary diseases and disorders |
| BR112018007021B1 (pt) | 2015-10-06 | 2024-01-09 | Proteostasis Therapeutics, Inc | Composto, composição compreendendo os ditos compostos e uso dos mesmos para tratar fibrose cística |
| US20180369209A1 (en) | 2015-12-22 | 2018-12-27 | Proteostasis Therapeutics, Inc. | Methods of treating pulmonary diseases and disorders |
| MA43775A (fr) | 2016-04-07 | 2021-05-05 | Proteostasis Therapeutics Inc | Analogues du ivacaftor conentant des atomes de silicium |
| US20190154661A1 (en) | 2016-05-09 | 2019-05-23 | Proteostasis Therapeutics, Inc. | Methods of identifying cftr modulators |
| MA45397A (fr) | 2016-06-21 | 2019-04-24 | Proteostasis Therapeutics Inc | Composés, compositions et procédés pour augmenter l'activité du cftr |
| CA3041675A1 (en) | 2016-10-26 | 2018-05-03 | Proteostasis Therapeutics, Inc. | N-phenyl-2-(3-phenyl-6-oxo-1,6-dihydropyridazin-1-yl)acetamide derivatives for treating cystic fibrosis |
| WO2018081378A1 (en) | 2016-10-26 | 2018-05-03 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for modulating cftr |
| AU2017348186A1 (en) | 2016-10-26 | 2019-05-16 | Proteostasis Therapeutics, Inc | Pyridazine derivatives, compositions and methods for modulating CFTR |
| MA49061A (fr) | 2017-04-28 | 2021-04-21 | Proteostasis Therapeutics Inc | Dérivés 4-sulfonylaminocarbonylquinoline pour augmenter l'activité cftr |
| AU2018346602B2 (en) | 2017-10-06 | 2024-10-17 | Proteostasis Therapeutics, Inc. | Compounds, compositions and methods for increasing CFTR activity |
| CN112585130A (zh) * | 2018-06-27 | 2021-03-30 | 蛋白质平衡治疗股份有限公司 | 蛋白酶体活性增强化合物 |
-
2019
- 2019-06-27 CN CN201980055145.2A patent/CN112585130A/zh active Pending
- 2019-06-27 EP EP19740258.9A patent/EP3814336A1/en not_active Withdrawn
- 2019-06-27 WO PCT/US2019/039562 patent/WO2020006269A1/en not_active Ceased
- 2019-06-27 JP JP2020573467A patent/JP7551087B2/ja active Active
-
2020
- 2020-12-23 US US17/133,362 patent/US11746098B2/en active Active
-
2023
- 2023-07-12 US US18/351,264 patent/US20240116894A1/en not_active Abandoned
-
2024
- 2024-05-08 JP JP2024076047A patent/JP2024112835A/ja not_active Withdrawn
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