JP2019516734A5 - - Google Patents
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- Publication number
- JP2019516734A5 JP2019516734A5 JP2018560846A JP2018560846A JP2019516734A5 JP 2019516734 A5 JP2019516734 A5 JP 2019516734A5 JP 2018560846 A JP2018560846 A JP 2018560846A JP 2018560846 A JP2018560846 A JP 2018560846A JP 2019516734 A5 JP2019516734 A5 JP 2019516734A5
- Authority
- JP
- Japan
- Prior art keywords
- formula
- par
- compound
- endoso
- therapeutic agent
- 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 17
- 239000003814 drug Substances 0.000 claims 8
- 229940124597 therapeutic agent Drugs 0.000 claims 8
- 150000002632 lipids Chemical class 0.000 claims 7
- 230000019491 signal transduction Effects 0.000 claims 7
- 241000238631 Hexapoda Species 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 235000001014 amino acid Nutrition 0.000 claims 4
- 229940024606 amino acid Drugs 0.000 claims 4
- 150000001413 amino acids Chemical class 0.000 claims 4
- 125000005647 linker group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 210000000170 cell membrane Anatomy 0.000 claims 3
- 230000012202 endocytosis Effects 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- 230000037431 insertion Effects 0.000 claims 3
- 238000003780 insertion Methods 0.000 claims 3
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims 2
- 239000004475 Arginine Substances 0.000 claims 2
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 claims 2
- 102000003688 G-Protein-Coupled Receptors Human genes 0.000 claims 2
- 108090000045 G-Protein-Coupled Receptors Proteins 0.000 claims 2
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims 2
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 2
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims 2
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 claims 2
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 2
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 2
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 claims 2
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims 2
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 2
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 2
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 2
- 239000004472 Lysine Substances 0.000 claims 2
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims 2
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims 2
- 239000004473 Threonine Substances 0.000 claims 2
- 235000009697 arginine Nutrition 0.000 claims 2
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 2
- 235000009582 asparagine Nutrition 0.000 claims 2
- 229960001230 asparagine Drugs 0.000 claims 2
- 235000003704 aspartic acid Nutrition 0.000 claims 2
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims 2
- 235000018417 cysteine Nutrition 0.000 claims 2
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 2
- 125000000524 functional group Chemical group 0.000 claims 2
- 235000013922 glutamic acid Nutrition 0.000 claims 2
- 239000004220 glutamic acid Substances 0.000 claims 2
- 235000004554 glutamine Nutrition 0.000 claims 2
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 claims 2
- 235000014304 histidine Nutrition 0.000 claims 2
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 claims 2
- 235000018977 lysine Nutrition 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 235000004400 serine Nutrition 0.000 claims 2
- 230000011664 signaling Effects 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 235000008521 threonine Nutrition 0.000 claims 2
- 102000005853 Clathrin Human genes 0.000 claims 1
- 108010019874 Clathrin Proteins 0.000 claims 1
- 102000043859 Dynamin Human genes 0.000 claims 1
- 108700021058 Dynamin Proteins 0.000 claims 1
- 108010070503 PAR-2 Receptor Proteins 0.000 claims 1
- 108091005804 Peptidases Proteins 0.000 claims 1
- 239000004365 Protease Substances 0.000 claims 1
- 102000018402 Protease-activated receptor 2 Human genes 0.000 claims 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000003368 amide group Chemical group 0.000 claims 1
- 150000001412 amines Chemical group 0.000 claims 1
- 102000000072 beta-Arrestins Human genes 0.000 claims 1
- 108010080367 beta-Arrestins Proteins 0.000 claims 1
- 230000005540 biological transmission Effects 0.000 claims 1
- 210000004899 c-terminal region Anatomy 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229930193282 clathrin Natural products 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- YWXYYJSYQOXTPL-SLPGGIOYSA-N isosorbide mononitrate Chemical compound [O-][N+](=O)O[C@@H]1CO[C@@H]2[C@@H](O)CO[C@@H]21 YWXYYJSYQOXTPL-SLPGGIOYSA-N 0.000 claims 1
- 239000012528 membrane Substances 0.000 claims 1
- 239000002736 nonionic surfactant Substances 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022000286A JP7441246B2 (ja) | 2016-05-20 | 2022-01-04 | 疼痛の治療 |
| JP2024022451A JP2024073450A (ja) | 2016-05-20 | 2024-02-16 | 疼痛の治療 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2016901912 | 2016-05-20 | ||
| AU2016901912A AU2016901912A0 (en) | 2016-05-20 | Treatment of Pain | |
| PCT/AU2017/050469 WO2017197463A1 (en) | 2016-05-20 | 2017-05-19 | Treatment of pain |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022000286A Division JP7441246B2 (ja) | 2016-05-20 | 2022-01-04 | 疼痛の治療 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019516734A JP2019516734A (ja) | 2019-06-20 |
| JP2019516734A5 true JP2019516734A5 (https=) | 2020-06-25 |
Family
ID=60324618
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018560846A Pending JP2019516734A (ja) | 2016-05-20 | 2017-05-19 | 疼痛の治療 |
| JP2022000286A Active JP7441246B2 (ja) | 2016-05-20 | 2022-01-04 | 疼痛の治療 |
| JP2024022451A Pending JP2024073450A (ja) | 2016-05-20 | 2024-02-16 | 疼痛の治療 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022000286A Active JP7441246B2 (ja) | 2016-05-20 | 2022-01-04 | 疼痛の治療 |
| JP2024022451A Pending JP2024073450A (ja) | 2016-05-20 | 2024-02-16 | 疼痛の治療 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20190298743A1 (https=) |
| EP (1) | EP3458062A4 (https=) |
| JP (3) | JP2019516734A (https=) |
| CN (1) | CN109152777A (https=) |
| AU (3) | AU2017268039A1 (https=) |
| CA (1) | CA3024719A1 (https=) |
| EA (1) | EA201892672A1 (https=) |
| MX (2) | MX395658B (https=) |
| WO (1) | WO2017197463A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA202091524A1 (ru) * | 2017-12-20 | 2020-09-16 | Такеда Фармасьютикал Компани Лимитед | Ингибиторы рецептора, активируемого протеазой 2 |
| US20240066027A1 (en) | 2020-12-03 | 2024-02-29 | Domain Therapeutics | Novel par-2 inhibitors |
| KR20250057699A (ko) | 2022-06-03 | 2025-04-29 | 도메인 테라퓨틱스 | 신규한 par-2 억제제 |
| WO2025172573A1 (en) | 2024-02-16 | 2025-08-21 | Domain Therapeutics | Combinations of par2 inhibitors and immune checkpoint inhibitors for the treatment of cancer |
| WO2025191185A1 (en) | 2024-03-15 | 2025-09-18 | Domain Therapeutics | Azine-based compounds as par-2 inhibitors and therapeutic uses thereof |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL106998A0 (en) * | 1992-09-17 | 1993-12-28 | Univ Florida | Brain-enhanced delivery of neuroactive peptides by sequential metabolism |
| US7541156B1 (en) * | 2000-03-01 | 2009-06-02 | Pasricha Pankaj J | Method of identifying antinociceptive compounds using protease activated receptor-2 |
| CN1938013A (zh) * | 2003-11-21 | 2007-03-28 | 纽卡斯尔大学研究协会有限公司 | 抑制发动蛋白依赖性的细胞内摄作用的方法和药剂 |
| US20070225363A1 (en) * | 2003-11-21 | 2007-09-27 | The University Of Newcastle Research Associates Ltd. | Methods and Agents for Inhibiting Dynamin-Dependent Endocytosis |
| JP4896870B2 (ja) * | 2004-04-08 | 2012-03-14 | ヤード・テヒノロギース・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング | 細胞膜ラフトと相互作用する構造を含む三者複合体およびその使用 |
| EP2119455A1 (en) * | 2004-04-08 | 2009-11-18 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Tripartite raftophilic structures and their use |
| WO2009034464A2 (en) * | 2007-09-12 | 2009-03-19 | Newcastle Innovation Limited | Indole related compounds with physiological activity |
| AR070911A1 (es) * | 2008-03-19 | 2010-05-12 | Regeneron Pharma | Uso de antagonistas del receptor par2 activado con proteasa |
| WO2013010218A1 (en) * | 2011-07-15 | 2013-01-24 | Freie Universität Berlin | Inhibition of clathrin |
| HK1223096A1 (zh) * | 2013-09-25 | 2017-07-21 | Vertex Pharmaceuticals Incorporated | 用作par-2信號通路抑制劑的咪唑並噠嗪 |
| CN115531553A (zh) * | 2015-12-22 | 2022-12-30 | 武田药品工业株式会社 | 内体g蛋白-偶联的受体的三部分调节剂 |
| AT518095B1 (de) * | 2015-12-30 | 2018-01-15 | Univ Wien Tech | Verfahren zur Herstellung von ionischen Flüssigkeiten auf Basis des Bistriflimid-Anions |
| EA202091524A1 (ru) * | 2017-12-20 | 2020-09-16 | Такеда Фармасьютикал Компани Лимитед | Ингибиторы рецептора, активируемого протеазой 2 |
-
2017
- 2017-05-19 WO PCT/AU2017/050469 patent/WO2017197463A1/en not_active Ceased
- 2017-05-19 EA EA201892672A patent/EA201892672A1/ru unknown
- 2017-05-19 EP EP17798408.5A patent/EP3458062A4/en active Pending
- 2017-05-19 MX MX2018014135A patent/MX395658B/es unknown
- 2017-05-19 JP JP2018560846A patent/JP2019516734A/ja active Pending
- 2017-05-19 US US16/303,023 patent/US20190298743A1/en active Pending
- 2017-05-19 CN CN201780031175.0A patent/CN109152777A/zh active Pending
- 2017-05-19 CA CA3024719A patent/CA3024719A1/en active Pending
- 2017-05-19 AU AU2017268039A patent/AU2017268039A1/en not_active Abandoned
-
2018
- 2018-11-16 MX MX2022011564A patent/MX2022011564A/es unknown
-
2022
- 2022-01-04 JP JP2022000286A patent/JP7441246B2/ja active Active
-
2023
- 2023-03-20 AU AU2023201732A patent/AU2023201732A1/en not_active Abandoned
-
2024
- 2024-02-16 JP JP2024022451A patent/JP2024073450A/ja active Pending
-
2025
- 2025-04-28 AU AU2025202933A patent/AU2025202933A1/en active Pending
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