JP2019503356A5 - - Google Patents
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- Publication number
- JP2019503356A5 JP2019503356A5 JP2018532435A JP2018532435A JP2019503356A5 JP 2019503356 A5 JP2019503356 A5 JP 2019503356A5 JP 2018532435 A JP2018532435 A JP 2018532435A JP 2018532435 A JP2018532435 A JP 2018532435A JP 2019503356 A5 JP2019503356 A5 JP 2019503356A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- optionally
- formula
- alkyl
- pharmaceutically acceptable
- 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 25
- 125000005647 linker group Chemical group 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 16
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 13
- 125000000524 functional group Chemical group 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 102000003688 G-Protein-Coupled Receptors Human genes 0.000 claims 8
- 108090000045 G-Protein-Coupled Receptors Proteins 0.000 claims 8
- 235000001014 amino acid Nutrition 0.000 claims 8
- 229940024606 amino acid Drugs 0.000 claims 8
- 150000001413 amino acids Chemical class 0.000 claims 8
- 150000002632 lipids Chemical class 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 6
- 239000004475 Arginine Substances 0.000 claims 6
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 claims 6
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims 6
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 6
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims 6
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 claims 6
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 6
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 6
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 claims 6
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims 6
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 6
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 6
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 6
- 239000004472 Lysine Substances 0.000 claims 6
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims 6
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims 6
- 239000004473 Threonine Substances 0.000 claims 6
- 235000009697 arginine Nutrition 0.000 claims 6
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 6
- 235000009582 asparagine Nutrition 0.000 claims 6
- 229960001230 asparagine Drugs 0.000 claims 6
- 235000003704 aspartic acid Nutrition 0.000 claims 6
- 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 6
- 235000018417 cysteine Nutrition 0.000 claims 6
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 6
- 235000013922 glutamic acid Nutrition 0.000 claims 6
- 239000004220 glutamic acid Substances 0.000 claims 6
- 235000004554 glutamine Nutrition 0.000 claims 6
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 claims 6
- 235000014304 histidine Nutrition 0.000 claims 6
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 claims 6
- 235000018977 lysine Nutrition 0.000 claims 6
- 235000004400 serine Nutrition 0.000 claims 6
- 235000008521 threonine Nutrition 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 230000011664 signaling Effects 0.000 claims 5
- 210000000170 cell membrane Anatomy 0.000 claims 4
- 229910052801 chlorine Inorganic materials 0.000 claims 4
- 125000001309 chloro group Chemical group Cl* 0.000 claims 4
- 230000037431 insertion Effects 0.000 claims 4
- 238000003780 insertion Methods 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 150000001370 alpha-amino acid derivatives Chemical class 0.000 claims 3
- 235000008206 alpha-amino acids Nutrition 0.000 claims 3
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 108090000765 processed proteins & peptides Proteins 0.000 claims 3
- 102000005962 receptors Human genes 0.000 claims 3
- 108020003175 receptors Proteins 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- -1 f3) optionally Chemical group 0.000 claims 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 2
- 125000003368 amide group Chemical group 0.000 claims 2
- 150000001412 amines Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 102000014468 Calcitonin Gene-Related Peptide Receptors Human genes 0.000 claims 1
- 108010078311 Calcitonin Gene-Related Peptide Receptors Proteins 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 208000012931 Urologic disease Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 210000004899 c-terminal region Anatomy 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 239000002462 tachykinin receptor antagonist Substances 0.000 claims 1
- 230000008685 targeting Effects 0.000 claims 1
- 208000014001 urinary system disease Diseases 0.000 claims 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022078995A JP7458681B2 (ja) | 2015-12-22 | 2022-05-12 | エンドソーマルｇタンパク質共役受容体のトリパータイト・モジュレーター |
| JP2024041282A JP2024073581A (ja) | 2015-12-22 | 2024-03-15 | エンドソーマルｇタンパク質共役受容体のトリパータイト・モジュレーター |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2015905333A AU2015905333A0 (en) | 2015-12-22 | Modulators of Endosomal G Protein-Coupled Receptors | |
| AU2015905333 | 2015-12-22 | ||
| US201662291161P | 2016-02-04 | 2016-02-04 | |
| US62/291,161 | 2016-02-04 | ||
| PCT/US2016/068075 WO2017112792A1 (en) | 2015-12-22 | 2016-12-21 | Tripartite modulators of endosomal g protein-coupled receptors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022078995A Division JP7458681B2 (ja) | 2015-12-22 | 2022-05-12 | エンドソーマルｇタンパク質共役受容体のトリパータイト・モジュレーター |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019503356A JP2019503356A (ja) | 2019-02-07 |
| JP2019503356A5 true JP2019503356A5 (enExample) | 2020-02-06 |
| JP7074673B2 JP7074673B2 (ja) | 2022-05-24 |
Family
ID=59091175
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018532435A Active JP7074673B2 (ja) | 2015-12-22 | 2016-12-21 | エンドソーマルｇタンパク質共役受容体のトリパータイト・モジュレーター |
| JP2022078995A Active JP7458681B2 (ja) | 2015-12-22 | 2022-05-12 | エンドソーマルｇタンパク質共役受容体のトリパータイト・モジュレーター |
| JP2024041282A Pending JP2024073581A (ja) | 2015-12-22 | 2024-03-15 | エンドソーマルｇタンパク質共役受容体のトリパータイト・モジュレーター |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022078995A Active JP7458681B2 (ja) | 2015-12-22 | 2022-05-12 | エンドソーマルｇタンパク質共役受容体のトリパータイト・モジュレーター |
| JP2024041282A Pending JP2024073581A (ja) | 2015-12-22 | 2024-03-15 | エンドソーマルｇタンパク質共役受容体のトリパータイト・モジュレーター |
Country Status (8)
| Country | Link |
|---|---|
| US (3) | US11324832B2 (enExample) |
| EP (1) | EP3393519A1 (enExample) |
| JP (3) | JP7074673B2 (enExample) |
| CN (2) | CN115531553A (enExample) |
| AU (3) | AU2016377658B2 (enExample) |
| CA (1) | CA3009325A1 (enExample) |
| EA (1) | EA201891472A1 (enExample) |
| WO (1) | WO2017112792A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112017018620A2 (pt) | 2015-03-04 | 2018-04-17 | Vanda Pharmaceuticals Inc. | método de administração de tradipitanto, e, tradipitanto. |
| 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 |
| EA201892672A1 (ru) * | 2016-05-20 | 2019-04-30 | Такеда Фармасьютикал Компани Лимитед | Лечение боли |
| CN119074729A (zh) * | 2017-11-17 | 2024-12-06 | 万达制药公司 | 使用川地匹坦治疗胃肠疾病的方法 |
| IT202200018768A1 (it) * | 2022-09-14 | 2024-03-14 | Alberto Chiarugi | Trattamento della nausea e vomito da chemioterapia |
| IT202200018780A1 (it) * | 2022-09-14 | 2024-03-14 | Alberto Chiarugi | Modulatori degli effetti della chemioterapia |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL350428A1 (en) | 1999-02-24 | 2002-12-16 | Hoffmann La Roche | 3-phenylpyridine derivatives and their use as nk-1 receptor antagonists |
| PT1035115E (pt) * | 1999-02-24 | 2005-01-31 | Hoffmann La Roche | Derivados de 4-fenilpiridina e a sua utilizacao como antagonistas do receptor nk-1 |
| US7696168B2 (en) | 2000-04-21 | 2010-04-13 | Tufts Medical Center, Inc. | G protein coupled receptor agonists and antagonists and methods of activating and inhibiting G protein coupled receptors using the same |
| TWI287003B (en) | 2000-07-24 | 2007-09-21 | Hoffmann La Roche | 4-phenyl-pyridine derivatives |
| TWI259180B (en) | 2000-08-08 | 2006-08-01 | Hoffmann La Roche | 4-Phenyl-pyridine derivatives |
| WO2005097199A1 (en) * | 2004-04-08 | 2005-10-20 | Jadolabs Gmbh | Tripartite conjugates containing a structure interacting with cell membrane rafts and their use |
| JP2008505092A (ja) | 2004-06-30 | 2008-02-21 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 立体選択的脱水によるα，β−不飽和エステル類および酸類 |
| TW200606152A (en) * | 2004-07-02 | 2006-02-16 | Tanabe Seiyaku Co | Piperidine compound and process for preparing the same |
| US9133116B2 (en) * | 2010-09-28 | 2015-09-15 | Panacea Biotec Ltd. | Bicyclic compounds |
| WO2014168721A2 (en) * | 2013-04-12 | 2014-10-16 | Tufts Medical Center | Methods and systems for designing and/or characterizing soluble lipidated ligand agents |
| JP6427491B2 (ja) * | 2013-07-03 | 2018-11-21 | 武田薬品工業株式会社 | 複素環化合物 |
| 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 |
-
2016
- 2016-12-21 CN CN202210637197.4A patent/CN115531553A/zh active Pending
- 2016-12-21 JP JP2018532435A patent/JP7074673B2/ja active Active
- 2016-12-21 WO PCT/US2016/068075 patent/WO2017112792A1/en not_active Ceased
- 2016-12-21 EA EA201891472A patent/EA201891472A1/ru unknown
- 2016-12-21 EP EP16831867.3A patent/EP3393519A1/en active Pending
- 2016-12-21 US US16/064,061 patent/US11324832B2/en active Active
- 2016-12-21 CA CA3009325A patent/CA3009325A1/en active Pending
- 2016-12-21 CN CN201680074910.1A patent/CN108712913B/zh active Active
- 2016-12-21 AU AU2016377658A patent/AU2016377658B2/en active Active
-
2022
- 2022-05-06 US US17/738,739 patent/US20230119819A1/en not_active Abandoned
- 2022-05-12 JP JP2022078995A patent/JP7458681B2/ja active Active
- 2022-12-28 AU AU2022291659A patent/AU2022291659A1/en not_active Abandoned
-
2024
- 2024-03-15 JP JP2024041282A patent/JP2024073581A/ja active Pending
- 2024-09-03 US US18/823,317 patent/US20250235544A1/en active Pending
-
2025
- 2025-02-18 AU AU2025201136A patent/AU2025201136A1/en active Pending
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