JP2021506975A5 - - Google Patents
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- JP2021506975A5 JP2021506975A5 JP2020552690A JP2020552690A JP2021506975A5 JP 2021506975 A5 JP2021506975 A5 JP 2021506975A5 JP 2020552690 A JP2020552690 A JP 2020552690A JP 2020552690 A JP2020552690 A JP 2020552690A JP 2021506975 A5 JP2021506975 A5 JP 2021506975A5
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- JP
- Japan
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- pharmaceutical composition
- thio
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- Prior art date
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- 102100037569 Dual specificity protein phosphatase 10 Human genes 0.000 claims description 38
- 101710096804 Dual specificity protein phosphatase 10 Proteins 0.000 claims description 38
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 28
- 238000000034 method Methods 0.000 claims description 27
- 150000001875 compounds Chemical class 0.000 claims description 26
- 208000035475 disorder Diseases 0.000 claims description 18
- 239000008194 pharmaceutical composition Substances 0.000 claims description 18
- -1 ( 5,6-dihydrobenzo [h] quinazoline-2-yl) thio Chemical group 0.000 claims description 14
- 239000000203 mixture Substances 0.000 claims description 12
- 230000001105 regulatory effect Effects 0.000 claims description 12
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims description 12
- 239000003112 inhibitor Substances 0.000 claims description 11
- 241000124008 Mammalia Species 0.000 claims description 10
- 201000010099 disease Diseases 0.000 claims description 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
- 230000000694 effects Effects 0.000 claims description 9
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 9
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims description 8
- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-Butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 claims description 6
- 125000003275 alpha amino acid group Chemical group 0.000 claims description 6
- 239000000758 substrate Substances 0.000 claims description 6
- 230000003197 catalytic effect Effects 0.000 claims description 5
- 125000001072 heteroaryl group Chemical group 0.000 claims description 4
- 239000000463 material Substances 0.000 claims description 4
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims description 4
- 229910019142 PO4 Inorganic materials 0.000 claims description 3
- 239000003795 chemical substances by application Substances 0.000 claims description 3
- 239000012634 fragment Substances 0.000 claims description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 3
- 239000010452 phosphate Substances 0.000 claims description 3
- 102000004196 processed proteins & peptides Human genes 0.000 claims description 3
- DYMYXDRPEVFZNY-UHFFFAOYSA-N 1-[(9-fluoro-5,6-dihydrobenzo[h]quinazolin-2-yl)sulfanyl]-3,3-dimethylbutan-2-one Chemical compound FC1=CC2=C(CCC=3C=NC(=NC2=3)SCC(C(C)(C)C)=O)C=C1 DYMYXDRPEVFZNY-UHFFFAOYSA-N 0.000 claims description 2
- 125000004201 2,4-dichlorophenyl group Chemical group [H]C1=C([H])C(*)=C(Cl)C([H])=C1Cl 0.000 claims description 2
- SCVJRXQHFJXZFZ-KVQBGUIXSA-N 2-amino-9-[(2r,4s,5r)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-3h-purine-6-thione Chemical compound C1=2NC(N)=NC(=S)C=2N=CN1[C@H]1C[C@H](O)[C@@H](CO)O1 SCVJRXQHFJXZFZ-KVQBGUIXSA-N 0.000 claims description 2
- ZVUPMFXOKKTVQT-UHFFFAOYSA-N 3,3-dimethyl-1-[[9-(methylthio)-5,6-dihydrothieno[3,4-h]quinazolin-2-yl]thio]-2-butanone Chemical compound N1=C(SCC(=O)C(C)(C)C)N=C2C3=C(SC)SC=C3CCC2=C1 ZVUPMFXOKKTVQT-UHFFFAOYSA-N 0.000 claims description 2
- IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 claims description 2
- 208000020446 Cardiac disease Diseases 0.000 claims description 2
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims description 2
- 208000029578 Muscle disease Diseases 0.000 claims description 2
- 230000003187 abdominal effect Effects 0.000 claims description 2
- 230000003281 allosteric effect Effects 0.000 claims description 2
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 230000000747 cardiac effect Effects 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000003176 fibrotic effect Effects 0.000 claims description 2
- 125000001475 halogen functional group Chemical group 0.000 claims description 2
- 208000019622 heart disease Diseases 0.000 claims description 2
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims description 2
- 238000007918 intramuscular administration Methods 0.000 claims description 2
- 238000001990 intravenous administration Methods 0.000 claims description 2
- 229920001184 polypeptide Polymers 0.000 claims description 2
- 238000007920 subcutaneous administration Methods 0.000 claims description 2
- 125000001424 substituent group Chemical group 0.000 claims description 2
- 230000000699 topical effect Effects 0.000 claims description 2
- 208000019553 vascular disease Diseases 0.000 claims description 2
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 210000000115 thoracic cavity Anatomy 0.000 claims 1
- 210000001215 vagina Anatomy 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 description 7
- ZMPMIXPUXSOYGB-UHFFFAOYSA-N CC(C1=NCCC=N1)=O Chemical compound CC(C1=NCCC=N1)=O ZMPMIXPUXSOYGB-UHFFFAOYSA-N 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 238000007913 intrathecal administration Methods 0.000 description 1
- 125000004001 thioalkyl group Chemical group 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023116635A JP7676477B2 (ja) | 2017-12-18 | 2023-07-18 | 線維症を処置するための化合物および組成物 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762607110P | 2017-12-18 | 2017-12-18 | |
| US62/607,110 | 2017-12-18 | ||
| PCT/US2018/066191 WO2019126141A1 (en) | 2017-12-18 | 2018-12-18 | Compounds and compositions for treating fibrosis |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023116635A Division JP7676477B2 (ja) | 2017-12-18 | 2023-07-18 | 線維症を処置するための化合物および組成物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021506975A JP2021506975A (ja) | 2021-02-22 |
| JP2021506975A5 true JP2021506975A5 (https=) | 2022-01-06 |
| JP7317039B2 JP7317039B2 (ja) | 2023-07-28 |
Family
ID=66993802
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020552690A Active JP7317039B2 (ja) | 2017-12-18 | 2018-12-18 | 線維症を処置するための化合物および組成物 |
| JP2023116635A Active JP7676477B2 (ja) | 2017-12-18 | 2023-07-18 | 線維症を処置するための化合物および組成物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023116635A Active JP7676477B2 (ja) | 2017-12-18 | 2023-07-18 | 線維症を処置するための化合物および組成物 |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US11504373B2 (https=) |
| EP (1) | EP3732179B1 (https=) |
| JP (2) | JP7317039B2 (https=) |
| KR (1) | KR20200100726A (https=) |
| CN (2) | CN116687934A (https=) |
| AU (3) | AU2018388549B2 (https=) |
| CA (1) | CA3085770A1 (https=) |
| MX (2) | MX2020006398A (https=) |
| WO (1) | WO2019126141A1 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2018388549B2 (en) * | 2017-12-18 | 2023-06-01 | Yale University | Compounds and compositions for treating fibrosis |
| US12570670B2 (en) * | 2019-01-30 | 2026-03-10 | Yale University | Compounds, compositions, and methods for treating fibrosis |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040086859A1 (en) | 2000-04-10 | 2004-05-06 | Klaus Ducker | Identification of a dual specificity phosphate: dusp-10 |
| DE60125783T2 (de) * | 2000-08-11 | 2007-10-18 | Evotec Ag | Verfahren zum nachweis von acetylase oder deacetylase-aktivität in einem immunoassay |
| US20030162230A1 (en) * | 2000-09-27 | 2003-08-28 | Reagan Kevin J. | Method for quantifying phosphokinase activity on proteins |
| JP2007518702A (ja) * | 2003-11-25 | 2007-07-12 | ノバルティス アクチエンゲゼルシャフト | ソマトスタチン類似体処置の効力についてのバイオマーカー |
| US8546410B2 (en) | 2008-05-05 | 2013-10-01 | Abbvie Inc. | Heteroaryl-fused macrocyclic pyrimidine derivatives |
| EP2351571A4 (en) * | 2008-10-09 | 2012-08-01 | Lsip Llc | PROTEINPHOSPHATASEHEMMER |
| CA2944198C (en) | 2013-04-26 | 2021-11-16 | Indiana University Research & Technology Corporation | Hydroxyindole carboxylic acid based inhibitors for oncogenic src homology-2 domain containing protein tyrosine phosphatase-2 (shp2) |
| AU2018388549B2 (en) * | 2017-12-18 | 2023-06-01 | Yale University | Compounds and compositions for treating fibrosis |
-
2018
- 2018-12-18 AU AU2018388549A patent/AU2018388549B2/en active Active
- 2018-12-18 CN CN202310653335.2A patent/CN116687934A/zh active Pending
- 2018-12-18 EP EP18890384.3A patent/EP3732179B1/en active Active
- 2018-12-18 CN CN201880088382.4A patent/CN111670188B/zh active Active
- 2018-12-18 CA CA3085770A patent/CA3085770A1/en active Pending
- 2018-12-18 US US16/954,514 patent/US11504373B2/en active Active
- 2018-12-18 KR KR1020207020574A patent/KR20200100726A/ko not_active Ceased
- 2018-12-18 JP JP2020552690A patent/JP7317039B2/ja active Active
- 2018-12-18 WO PCT/US2018/066191 patent/WO2019126141A1/en not_active Ceased
- 2018-12-18 MX MX2020006398A patent/MX2020006398A/es unknown
-
2020
- 2020-07-13 MX MX2023009895A patent/MX2023009895A/es unknown
-
2022
- 2022-10-18 US US18/047,456 patent/US20230181588A1/en not_active Abandoned
-
2023
- 2023-07-11 AU AU2023204581A patent/AU2023204581B2/en active Active
- 2023-07-18 JP JP2023116635A patent/JP7676477B2/ja active Active
-
2024
- 2024-02-27 US US18/589,173 patent/US20240335445A1/en active Pending
-
2025
- 2025-09-22 AU AU2025234269A patent/AU2025234269A1/en active Pending
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