JPWO2020025517A5 - - Google Patents
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- Publication number
- JPWO2020025517A5 JPWO2020025517A5 JP2021505638A JP2021505638A JPWO2020025517A5 JP WO2020025517 A5 JPWO2020025517 A5 JP WO2020025517A5 JP 2021505638 A JP2021505638 A JP 2021505638A JP 2021505638 A JP2021505638 A JP 2021505638A JP WO2020025517 A5 JPWO2020025517 A5 JP WO2020025517A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- compound
- independently
- nrc
- acceptable salt
- 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
- 150000001875 compounds Chemical class 0.000 claims 20
- 150000003839 salts Chemical class 0.000 claims 19
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 12
- 229910052717 sulfur Inorganic materials 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 7
- 239000012453 solvate Substances 0.000 claims 7
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 239000001301 oxygen Substances 0.000 claims 6
- 239000011593 sulfur Substances 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 150000004677 hydrates Chemical class 0.000 claims 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Chemical group C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 3
- 201000005569 Gout Diseases 0.000 claims 2
- 101000669402 Homo sapiens Toll-like receptor 7 Proteins 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical group C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 2
- 102100039390 Toll-like receptor 7 Human genes 0.000 claims 2
- 125000001931 aliphatic group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 125000004306 triazinyl group Chemical group 0.000 claims 2
- -1 -OEt Chemical group 0.000 claims 1
- 208000007815 Acquired Hyperostosis Syndrome Diseases 0.000 claims 1
- 208000026326 Adult-onset Still disease Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000005024 Castleman disease Diseases 0.000 claims 1
- 208000015943 Coeliac disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 102100026018 Interleukin-1 receptor antagonist protein Human genes 0.000 claims 1
- 101710144554 Interleukin-1 receptor antagonist protein Proteins 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 208000005777 Lupus Nephritis Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical group C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 201000004854 SAPHO syndrome Diseases 0.000 claims 1
- 201000010848 Schnitzler Syndrome Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical group C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 208000022993 cryopyrin-associated periodic syndrome Diseases 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 230000007812 deficiency Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical group C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims 1
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 208000025487 periodic fever syndrome Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024080418A JP2024105611A (ja) | 2018-07-31 | 2024-05-16 | Ｔｌｒ７／８アンタゴニストおよびそれらの使用 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862712439P | 2018-07-31 | 2018-07-31 | |
| US62/712,439 | 2018-07-31 | ||
| PCT/EP2019/070312 WO2020025517A1 (en) | 2018-07-31 | 2019-07-29 | Tlr7/8 antagonists and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024080418A Division JP2024105611A (ja) | 2018-07-31 | 2024-05-16 | Ｔｌｒ７／８アンタゴニストおよびそれらの使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021533125A JP2021533125A (ja) | 2021-12-02 |
| JPWO2020025517A5 true JPWO2020025517A5 (ko) | 2022-08-08 |
| JP7491900B2 JP7491900B2 (ja) | 2024-05-28 |
Family
ID=67660056
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021505638A Active JP7491900B2 (ja) | 2018-07-31 | 2019-07-29 | Ｔｌｒ７／８アンタゴニストおよびそれらの使用 |
| JP2024080418A Pending JP2024105611A (ja) | 2018-07-31 | 2024-05-16 | Ｔｌｒ７／８アンタゴニストおよびそれらの使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024080418A Pending JP2024105611A (ja) | 2018-07-31 | 2024-05-16 | Ｔｌｒ７／８アンタゴニストおよびそれらの使用 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20210300940A1 (ko) |
| EP (1) | EP3830080A1 (ko) |
| JP (2) | JP7491900B2 (ko) |
| KR (1) | KR20210040085A (ko) |
| CN (1) | CN112513024A (ko) |
| AU (2) | AU2019313441B2 (ko) |
| BR (2) | BR122023023308A2 (ko) |
| CA (1) | CA3108099A1 (ko) |
| IL (1) | IL280479A (ko) |
| MX (1) | MX2021000093A (ko) |
| SG (1) | SG11202100818RA (ko) |
| TW (2) | TWI827641B (ko) |
| WO (1) | WO2020025517A1 (ko) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201804170RA (en) * | 2015-12-17 | 2018-06-28 | Merck Patent Gmbh | Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders |
| EP3497094B1 (en) | 2016-08-08 | 2023-02-15 | Merck Patent GmbH | Tlr7/8 antagonists and uses thereof |
| EP3728229A1 (en) * | 2017-12-19 | 2020-10-28 | Merck Patent GmbH | Tlr7/8 antagonists and uses thereof |
| JP2022081710A (ja) * | 2019-03-29 | 2022-06-01 | ユーティアイ リミテッド パートナーシップ | 関節リウマチを治療するためのｔ型カルシウムチャネル阻害剤の使用 |
| CA3135344A1 (en) * | 2019-03-29 | 2020-10-08 | Nippon Chemiphar Co., Ltd. | Use of t-type calcium channel blocker for treating pruritus |
| CN114401954A (zh) * | 2019-09-16 | 2022-04-26 | 豪夫迈·罗氏有限公司 | 用于治疗自身免疫性疾病的哌啶基胺化合物 |
| CA3163105A1 (en) | 2019-11-28 | 2021-06-03 | Bayer Aktiengesellschaft | Substituted aminoquinolones as dgkalpha inhibitors for immune activation |
| US20240024308A1 (en) * | 2020-05-14 | 2024-01-25 | Merck Healthcare Kgaa | Tlr7/8 antagonists for the treatment of coronavirus infections |
| CN116745291A (zh) | 2020-12-17 | 2023-09-12 | 阿斯利康(瑞典)有限公司 | N-(2-(4-氰基噻唑烷-3-基)-2-氧代乙基)-喹啉-4-甲酰胺 |
| MX2023012110A (es) | 2021-04-16 | 2023-10-24 | Gilead Sciences Inc | Compuestos de tienopirrol. |
| CN117957234A (zh) | 2021-09-10 | 2024-04-30 | 吉利德科学公司 | 噻吩并吡咯化合物 |
| WO2024153063A1 (zh) * | 2023-01-18 | 2024-07-25 | 苏州科睿思制药有限公司 | Enpatoran的晶型及其制备方法和用途 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI529171B (zh) * | 2013-07-29 | 2016-04-11 | 赫孚孟拉羅股份公司 | １，７－萘啶衍生物 |
| US9663486B2 (en) * | 2013-10-14 | 2017-05-30 | Eisai R&D Management Co., Ltd. | Selectively substituted quinoline compounds |
| CN104557913B (zh) * | 2013-10-28 | 2017-02-08 | 上海汇伦生命科技有限公司 | 吡啶并嘧啶类化合物，其制备方法和用途 |
| MX2016006052A (es) | 2013-11-12 | 2016-07-18 | Hoffmann La Roche | Pirido[4,3-b]pirazin-2-carboxamidas como agentes neurogenicos para el tratamiento de trastornos neurodegenerativos. |
| EP3317265A4 (en) | 2015-07-01 | 2019-04-17 | Northwestern University | SUBSTITUTED CHINAZOLIN COMPOUNDS AND USES THEREOF FOR MODULATING GLUCOCEREBROSIDASE ACTIVITY |
| WO2017031427A1 (en) | 2015-08-19 | 2017-02-23 | 3-V Biosciences, Inc. | COMPOUNDS AND METHODS FOR INHIBITING mTOR |
| SG11201804170RA (en) * | 2015-12-17 | 2018-06-28 | Merck Patent Gmbh | Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders |
| CN106632089B (zh) * | 2016-11-04 | 2019-06-18 | 中山大学 | 一类喹唑啉类化合物及其制备方法与应用 |
| JP7239554B2 (ja) | 2017-07-18 | 2023-03-14 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｔｌｒ７／８アンタゴニストおよびそれらの使用 |
| EP3728229A1 (en) | 2017-12-19 | 2020-10-28 | Merck Patent GmbH | Tlr7/8 antagonists and uses thereof |
-
2019
- 2019-07-29 CA CA3108099A patent/CA3108099A1/en active Pending
- 2019-07-29 MX MX2021000093A patent/MX2021000093A/es unknown
- 2019-07-29 BR BR122023023308-5A patent/BR122023023308A2/pt unknown
- 2019-07-29 US US17/250,489 patent/US20210300940A1/en active Pending
- 2019-07-29 SG SG11202100818RA patent/SG11202100818RA/en unknown
- 2019-07-29 EP EP19755290.4A patent/EP3830080A1/en active Pending
- 2019-07-29 WO PCT/EP2019/070312 patent/WO2020025517A1/en unknown
- 2019-07-29 CN CN201980051004.3A patent/CN112513024A/zh active Pending
- 2019-07-29 JP JP2021505638A patent/JP7491900B2/ja active Active
- 2019-07-29 KR KR1020217005440A patent/KR20210040085A/ko not_active Application Discontinuation
- 2019-07-29 BR BR112021001618-0A patent/BR112021001618A2/pt unknown
- 2019-07-29 AU AU2019313441A patent/AU2019313441B2/en active Active
- 2019-07-30 TW TW108126963A patent/TWI827641B/zh active
- 2019-07-30 TW TW112144948A patent/TW202423913A/zh unknown
-
2021
- 2021-01-28 IL IL280479A patent/IL280479A/en unknown
-
2024
- 2024-05-16 JP JP2024080418A patent/JP2024105611A/ja active Pending
- 2024-05-30 AU AU2024203629A patent/AU2024203629A1/en active Pending
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