JP2019522673A5 - - Google Patents
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- Publication number
- JP2019522673A5 JP2019522673A5 JP2019502161A JP2019502161A JP2019522673A5 JP 2019522673 A5 JP2019522673 A5 JP 2019522673A5 JP 2019502161 A JP2019502161 A JP 2019502161A JP 2019502161 A JP2019502161 A JP 2019502161A JP 2019522673 A5 JP2019522673 A5 JP 2019522673A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- trifluoroethyl
- difluoro
- halo
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 34
- 125000001475 halogen functional group Chemical group 0.000 claims 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 9
- 125000005223 heteroarylcarbonyl group Chemical group 0.000 claims 9
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 9
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 238000000034 method Methods 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 4
- 208000008069 Geographic Atrophy Diseases 0.000 claims 4
- 206010038933 Retinopathy of prematurity Diseases 0.000 claims 4
- 208000000208 Wet Macular Degeneration Diseases 0.000 claims 4
- 206010064930 age-related macular degeneration Diseases 0.000 claims 4
- 208000011325 dry age related macular degeneration Diseases 0.000 claims 4
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 3
- -1 C 1-6 -alkyl Chemical group 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000004104 aryloxy group Chemical group 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 208000019553 vascular disease Diseases 0.000 claims 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 1
- NFTBRZHYQJZXKB-UHFFFAOYSA-N FC(C(=O)NCC(F)(F)F)(C(CC(C)C)=O)F Chemical compound FC(C(=O)NCC(F)(F)F)(C(CC(C)C)=O)F NFTBRZHYQJZXKB-UHFFFAOYSA-N 0.000 claims 1
- 206010063381 Polypoidal choroidal vasculopathy Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 150000002366 halogen compounds Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000001590 oxidative effect Effects 0.000 claims 1
- 125000004205 trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16180013 | 2016-07-18 | ||
| EP16180013.1 | 2016-07-18 | ||
| PCT/EP2017/067519 WO2018015240A1 (en) | 2016-07-18 | 2017-07-12 | New difluoroketamide derivatives as htra1 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019522673A JP2019522673A (ja) | 2019-08-15 |
| JP2019522673A5 true JP2019522673A5 (https=) | 2020-08-20 |
Family
ID=56418466
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019502161A Pending JP2019522673A (ja) | 2016-07-18 | 2017-07-12 | Ｈｔｒａ１阻害剤としての新規なジフルオロケトアミド誘導体 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US10865182B2 (https=) |
| EP (1) | EP3484859B1 (https=) |
| JP (1) | JP2019522673A (https=) |
| CN (1) | CN109415330A (https=) |
| WO (1) | WO2018015240A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL3472149T3 (pl) | 2016-06-21 | 2024-02-12 | Orion Ophthalmology LLC | Heterocykliczne pochodne prolinamidu |
| US10526315B2 (en) | 2016-06-21 | 2020-01-07 | Orion Ophthalmology LLC | Carbocyclic prolinamide derivatives |
| WO2025006856A1 (en) * | 2023-06-28 | 2025-01-02 | The Board Of Trustees Of The Leland Stanford Junior University | Htra1 inhibitors and uses thereof |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FI865196A7 (fi) * | 1985-04-19 | 1986-12-18 | Upjohn Co | Halostatiinisubstituoituja reniini-inhibiittoreita. |
| AU711035B2 (en) * | 1994-07-15 | 1999-10-07 | Merrell Pharmaceuticals Inc. | Difluorostatone antiviral agents |
| ES2234144T3 (es) | 1997-08-11 | 2005-06-16 | Boehringer Ingelheim (Canada) Ltd. | Analogos de peptidos inhibidores de la hepatitis c. |
| US6355618B1 (en) * | 1999-04-09 | 2002-03-12 | Cytovia, Inc. | Caspase inhibitors and the use thereof |
| US7244815B2 (en) | 2001-05-23 | 2007-07-17 | The Curators Of The University Of Missouri | Attachment and elaboration strategies for inverse peptide synthesis |
| TWI359147B (en) | 2003-09-05 | 2012-03-01 | Vertex Pharma | Inhibitors of serine proteases, particularly hcv n |
| US20060121039A1 (en) * | 2004-12-07 | 2006-06-08 | Alcon, Inc. | Use of agents that prevent the generation of amyloid-like proteins and/or drusen, and/or use of agents that promote sequestration and/or degradation of, and/or prevent the neurotoxic effects of such proteins in the treatment of macular degeneration |
| CN101248046A (zh) * | 2005-07-11 | 2008-08-20 | 德福根有限公司 | 作为激酶抑制剂的酰胺衍生物 |
| TW200846358A (en) | 2007-02-16 | 2008-12-01 | Genentech Inc | HtrA1-PDZ and HtrA3-PDZ modulators |
| PT2661433T (pt) | 2011-01-04 | 2017-10-24 | Novartis Ag | Compostos de indole ou seus análogos úteis para o tratamento da degeneração macular relacionada com a idade (amd) |
| US8592426B2 (en) * | 2011-01-24 | 2013-11-26 | Hoffmann—La Roche Inc. | Aryl-benzocycloalkyl amide derivatives |
| ES2644700T3 (es) | 2012-06-28 | 2017-11-30 | Novartis Ag | Derivados de pirrolidina y su uso como moduladores de la ruta del complemento |
| CN107207421B (zh) | 2015-02-25 | 2021-04-20 | 豪夫迈·罗氏有限公司 | 新的三氟甲基丙酰胺衍生物 |
| AR104856A1 (es) * | 2015-05-11 | 2017-08-23 | Hoffmann La Roche | Derivados de difluorocetamida |
-
2017
- 2017-07-12 EP EP17736967.5A patent/EP3484859B1/en not_active Not-in-force
- 2017-07-12 CN CN201780039927.8A patent/CN109415330A/zh active Pending
- 2017-07-12 JP JP2019502161A patent/JP2019522673A/ja active Pending
- 2017-07-12 WO PCT/EP2017/067519 patent/WO2018015240A1/en not_active Ceased
-
2019
- 2019-01-17 US US16/250,905 patent/US10865182B2/en not_active Expired - Fee Related
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