JP2017536416A5 - - Google Patents
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- JP2017536416A5 JP2017536416A5 JP2017545881A JP2017545881A JP2017536416A5 JP 2017536416 A5 JP2017536416 A5 JP 2017536416A5 JP 2017545881 A JP2017545881 A JP 2017545881A JP 2017545881 A JP2017545881 A JP 2017545881A JP 2017536416 A5 JP2017536416 A5 JP 2017536416A5
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- JP
- Japan
- Prior art keywords
- alkyl
- unsubstituted
- substituted
- pharmaceutically acceptable
- compound according
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 7
- 239000012453 solvate Substances 0.000 claims 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 2
- -1 alkyl sulfone Chemical class 0.000 claims 2
- 125000005360 alkyl sulfoxide group Chemical group 0.000 claims 2
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- 125000005361 aryl sulfoxide group Chemical group 0.000 claims 2
- 125000005110 aryl thio group Chemical group 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 2
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 102000003566 TRPV1 Human genes 0.000 claims 1
- 101150016206 Trpv1 gene Proteins 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 125000005228 aryl sulfonate group Chemical group 0.000 claims 1
- 125000005362 aryl sulfone group Chemical group 0.000 claims 1
- 239000011230 binding agent Substances 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N phenol group Chemical group C1(=CC=CC=C1)O ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims 1
- 150000007965 phenolic acids Chemical class 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462084515P | 2014-11-25 | 2014-11-25 | |
| US62/084,515 | 2014-11-25 | ||
| US14/743,375 US9359316B1 (en) | 2014-11-25 | 2015-06-18 | Prodrugs of phenolic TRPV1 agonists |
| US14/743,375 | 2015-06-18 | ||
| PCT/US2015/062531 WO2016086063A1 (en) | 2014-11-25 | 2015-11-24 | Prodrugs of phenolic trpv1 agonists |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020032357A Division JP7026152B2 (ja) | 2014-11-25 | 2020-02-27 | フェノール性trpv1アゴニストのプロドラッグ |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017536416A JP2017536416A (ja) | 2017-12-07 |
| JP2017536416A5 true JP2017536416A5 (enExample) | 2019-01-10 |
| JP6670841B2 JP6670841B2 (ja) | 2020-03-25 |
Family
ID=56009519
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017545881A Active JP6670841B2 (ja) | 2014-11-25 | 2015-11-24 | フェノール酸trpv1アゴニストのプロドラッグ |
| JP2020032357A Expired - Fee Related JP7026152B2 (ja) | 2014-11-25 | 2020-02-27 | フェノール性trpv1アゴニストのプロドラッグ |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020032357A Expired - Fee Related JP7026152B2 (ja) | 2014-11-25 | 2020-02-27 | フェノール性trpv1アゴニストのプロドラッグ |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US9359316B1 (enExample) |
| EP (2) | EP3872063A1 (enExample) |
| JP (2) | JP6670841B2 (enExample) |
| KR (1) | KR102562571B1 (enExample) |
| CN (1) | CN107205961B (enExample) |
| AR (1) | AR102799A1 (enExample) |
| AU (1) | AU2015353532B2 (enExample) |
| BR (1) | BR112017010950B1 (enExample) |
| CA (1) | CA2968061C (enExample) |
| CY (1) | CY1124811T1 (enExample) |
| DK (1) | DK3223805T3 (enExample) |
| EA (1) | EA033619B1 (enExample) |
| ES (1) | ES2871095T3 (enExample) |
| HR (1) | HRP20210775T1 (enExample) |
| HU (1) | HUE054449T2 (enExample) |
| IL (1) | IL252307B (enExample) |
| LT (1) | LT3223805T (enExample) |
| MX (1) | MX382872B (enExample) |
| PH (1) | PH12017500974B1 (enExample) |
| PL (1) | PL3223805T3 (enExample) |
| PT (1) | PT3223805T (enExample) |
| RS (1) | RS61875B1 (enExample) |
| SG (1) | SG11201704290VA (enExample) |
| SI (1) | SI3223805T1 (enExample) |
| SM (1) | SMT202100308T1 (enExample) |
| TW (1) | TWI692465B (enExample) |
| WO (1) | WO2016086063A1 (enExample) |
| ZA (1) | ZA201703409B (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11634384B2 (en) | 2014-11-25 | 2023-04-25 | Concentric Analgesics, Inc. | Prodrugs of phenolic TRPV1 agonists |
| CN109562281B (zh) * | 2016-05-25 | 2021-12-17 | 同心镇痛药物公司 | 酚类trpv1激动剂的前药与局部麻醉药和血管收缩剂联合用于改善局部麻醉 |
| KR102657458B1 (ko) | 2016-11-02 | 2024-04-12 | 센트렉시온 테라퓨틱스 코포레이션 | 안정한 수성의 캡사이신 주사 가능한 제형 및 이의 의학적 용도 |
| CN108069898B (zh) * | 2016-11-16 | 2021-11-23 | 南华大学 | 含烟酸辣椒碱酯衍生物、制备方法及其用途 |
| WO2018217937A1 (en) * | 2017-05-24 | 2018-11-29 | Concentric Analgesics, Inc. | Prodrugs of phenolic trpv1 agonists in combination with local anesthetics and vasoconstrictors for improved local anesthesia |
| MX2020000488A (es) | 2017-07-20 | 2020-10-28 | Centrexion Therapeutics Corp | Metodos y composiciones para el tratamiento del dolor usando capsaicina. |
| US10717712B2 (en) | 2018-07-27 | 2020-07-21 | Concentric Analgesics, Inc. | Pegylated prodrugs of phenolic TRPV1 agonists |
| WO2020023793A1 (en) * | 2018-07-27 | 2020-01-30 | Concentric Analgesics, Inc. | Pegylated prodrugs of phenolic trpv1 agonists |
| US11254659B1 (en) | 2019-01-18 | 2022-02-22 | Centrexion Therapeutics Corporation | Capsaicinoid prodrug compounds and their use in treating medical conditions |
| US11447444B1 (en) | 2019-01-18 | 2022-09-20 | Centrexion Therapeutics Corporation | Capsaicinoid prodrug compounds and their use in treating medical conditions |
| WO2021034863A1 (en) * | 2019-08-19 | 2021-02-25 | Chorda Pharma, Inc. | Chemical derivatives and methods for synthesizing and compounding chemical derivatives related to capsaicin palmitate and capsaicin prodrugs |
| EP4023631A4 (en) * | 2019-09-30 | 2022-12-07 | Nanjing Delova Biotech Co. Ltd. | TRPV1 AGONIST, METHOD FOR PREPARATION AND USE |
| WO2022132649A1 (en) * | 2020-12-14 | 2022-06-23 | Concentric Analgesics, Inc. | Pharmaceutical formulations of a phenolic trpv1 agonist prodrug |
| WO2022132650A1 (en) * | 2020-12-14 | 2022-06-23 | Concentric Analgesics, Inc. | Prodrug of a phenolic trpv1 agonist for the treatment of pain |
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-
2015
- 2015-06-18 US US14/743,375 patent/US9359316B1/en active Active
- 2015-11-24 WO PCT/US2015/062531 patent/WO2016086063A1/en not_active Ceased
- 2015-11-24 HR HRP20210775TT patent/HRP20210775T1/hr unknown
- 2015-11-24 PL PL15863380T patent/PL3223805T3/pl unknown
- 2015-11-24 KR KR1020177017437A patent/KR102562571B1/ko active Active
- 2015-11-24 EP EP21156331.7A patent/EP3872063A1/en not_active Withdrawn
- 2015-11-24 DK DK15863380.0T patent/DK3223805T3/da active
- 2015-11-24 SM SM20210308T patent/SMT202100308T1/it unknown
- 2015-11-24 EP EP15863380.0A patent/EP3223805B1/en active Active
- 2015-11-24 BR BR112017010950-6A patent/BR112017010950B1/pt active IP Right Grant
- 2015-11-24 CA CA2968061A patent/CA2968061C/en active Active
- 2015-11-24 EA EA201790896A patent/EA033619B1/ru unknown
- 2015-11-24 AU AU2015353532A patent/AU2015353532B2/en active Active
- 2015-11-24 HU HUE15863380A patent/HUE054449T2/hu unknown
- 2015-11-24 CN CN201580074440.4A patent/CN107205961B/zh active Active
- 2015-11-24 MX MX2017006818A patent/MX382872B/es unknown
- 2015-11-24 ES ES15863380T patent/ES2871095T3/es active Active
- 2015-11-24 PT PT158633800T patent/PT3223805T/pt unknown
- 2015-11-24 JP JP2017545881A patent/JP6670841B2/ja active Active
- 2015-11-24 SG SG11201704290VA patent/SG11201704290VA/en unknown
- 2015-11-24 SI SI201531607T patent/SI3223805T1/sl unknown
- 2015-11-24 RS RS20210635A patent/RS61875B1/sr unknown
- 2015-11-24 LT LTEP15863380.0T patent/LT3223805T/lt unknown
- 2015-11-25 TW TW104139294A patent/TWI692465B/zh active
- 2015-11-25 AR ARP150103868A patent/AR102799A1/es active IP Right Grant
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2017
- 2017-05-16 IL IL252307A patent/IL252307B/en active IP Right Grant
- 2017-05-17 ZA ZA2017/03409A patent/ZA201703409B/en unknown
- 2017-05-25 PH PH12017500974A patent/PH12017500974B1/en unknown
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2020
- 2020-02-27 JP JP2020032357A patent/JP7026152B2/ja not_active Expired - Fee Related
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2021
- 2021-05-24 CY CY20211100446T patent/CY1124811T1/el unknown