JPWO2021029914A5 - - Google Patents
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- Publication number
- JPWO2021029914A5 JPWO2021029914A5 JP2022509137A JP2022509137A JPWO2021029914A5 JP WO2021029914 A5 JPWO2021029914 A5 JP WO2021029914A5 JP 2022509137 A JP2022509137 A JP 2022509137A JP 2022509137 A JP2022509137 A JP 2022509137A JP WO2021029914 A5 JPWO2021029914 A5 JP WO2021029914A5
- Authority
- JP
- Japan
- Prior art keywords
- hexadienoate
- composition
- opioid
- formula
- methylhexadienoate
- 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 description 11
- 150000003839 salts Chemical class 0.000 claims description 3
- 229960000805 nalbuphine Drugs 0.000 claims description 2
- NETZHAKZCGBWSS-CEDHKZHLSA-N nalbuphine Chemical group C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]1(O)CC[C@@H]3O)CN2CC1CCC1 NETZHAKZCGBWSS-CEDHKZHLSA-N 0.000 claims description 2
- USVPNLRUHJWRFA-UHFFFAOYSA-N 5-methylhexa-2,4-dienoic acid Chemical compound CC(C)=CC=CC(O)=O USVPNLRUHJWRFA-UHFFFAOYSA-N 0.000 claims 8
- 238000000034 method Methods 0.000 claims 5
- 208000012661 Dyskinesia Diseases 0.000 claims 4
- WSWCOQWTEOXDQX-UHFFFAOYSA-N 2,4-Hexadienoic acid Chemical compound CC=CC=CC(O)=O WSWCOQWTEOXDQX-UHFFFAOYSA-N 0.000 claims 3
- OIJXLIIMXHRJJH-KNLIIKEYSA-N Diprenorphine Chemical group C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]11CC[C@]3([C@H](C1)C(C)(C)O)OC)CN2CC1CC1 OIJXLIIMXHRJJH-KNLIIKEYSA-N 0.000 claims 2
- 208000023105 Huntington disease Diseases 0.000 claims 2
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims 2
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims 2
- JAQUASYNZVUNQP-USXIJHARSA-N Levorphanol Chemical group C1C2=CC=C(O)C=C2[C@]23CCN(C)[C@H]1[C@@H]2CCCC3 JAQUASYNZVUNQP-USXIJHARSA-N 0.000 claims 2
- 208000016285 Movement disease Diseases 0.000 claims 2
- 102000003840 Opioid Receptors Human genes 0.000 claims 2
- 108090000137 Opioid Receptors Proteins 0.000 claims 2
- UQCNKQCJZOAFTQ-ISWURRPUSA-N Oxymorphone Chemical group O([C@H]1C(CC[C@]23O)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O UQCNKQCJZOAFTQ-ISWURRPUSA-N 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 208000005374 Poisoning Diseases 0.000 claims 2
- 206010043118 Tardive Dyskinesia Diseases 0.000 claims 2
- 208000000323 Tourette Syndrome Diseases 0.000 claims 2
- 208000016620 Tourette disease Diseases 0.000 claims 2
- 229950002494 diprenorphine Drugs 0.000 claims 2
- CAHCBJPUTCKATP-FAWZKKEFSA-N etorphine Chemical group O([C@H]1[C@@]2(OC)C=C[C@@]34C[C@@H]2[C@](C)(O)CCC)C2=C5[C@]41CCN(C)[C@@H]3CC5=CC=C2O CAHCBJPUTCKATP-FAWZKKEFSA-N 0.000 claims 2
- 229950004155 etorphine Drugs 0.000 claims 2
- WVLOADHCBXTIJK-YNHQPCIGSA-N hydromorphone Chemical group O([C@H]1C(CC[C@H]23)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O WVLOADHCBXTIJK-YNHQPCIGSA-N 0.000 claims 2
- 229960001410 hydromorphone Drugs 0.000 claims 2
- HQBZLVPZOGIAIQ-SDDDUWNISA-N ketazocine Chemical group N1([C@H]2[C@@H]([C@](CC1)(C)C=1C(=CC=C(O)C=1)C2=O)C)CC1CC1 HQBZLVPZOGIAIQ-SDDDUWNISA-N 0.000 claims 2
- 229960004502 levodopa Drugs 0.000 claims 2
- 229960003406 levorphanol Drugs 0.000 claims 2
- NPZXCTIHHUUEEJ-CMKMFDCUSA-N metopon Chemical group O([C@@]1(C)C(=O)CC[C@@H]23)C4=C5[C@@]13CCN(C)[C@@H]2CC5=CC=C4O NPZXCTIHHUUEEJ-CMKMFDCUSA-N 0.000 claims 2
- 229950006080 metopon Drugs 0.000 claims 2
- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical group O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 claims 2
- 239000003401 opiate antagonist Substances 0.000 claims 2
- 229960005118 oxymorphone Drugs 0.000 claims 2
- 230000036407 pain Effects 0.000 claims 2
- 231100000572 poisoning Toxicity 0.000 claims 2
- 230000000607 poisoning effect Effects 0.000 claims 2
- 208000017520 skin disease Diseases 0.000 claims 2
- KWTWDQCKEHXFFR-SMDDNHRTSA-N tapentadol Chemical group CN(C)C[C@H](C)[C@@H](CC)C1=CC=CC(O)=C1 KWTWDQCKEHXFFR-SMDDNHRTSA-N 0.000 claims 2
- 229960005126 tapentadol Drugs 0.000 claims 2
- YQYVFVRQLZMJKJ-JBBXEZCESA-N (+)-cyclazocine Chemical compound C([C@@]1(C)C2=CC(O)=CC=C2C[C@@H]2[C@@H]1C)CN2CC1CC1 YQYVFVRQLZMJKJ-JBBXEZCESA-N 0.000 claims 1
- WSWCOQWTEOXDQX-MQQKCMAXSA-M (E,E)-sorbate Chemical compound C\C=C\C=C\C([O-])=O WSWCOQWTEOXDQX-MQQKCMAXSA-M 0.000 claims 1
- -1 3-(Cyclobutylmethyl)-4a,7-dihydroxy-2,3,4,4a,5,6,7,7a-octahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-9- yl(2E,4E)-hexa-2,4-dienoate Chemical compound 0.000 claims 1
- 206010002091 Anaesthesia Diseases 0.000 claims 1
- UIQMVEYFGZJHCZ-SSTWWWIQSA-N Nalorphine Chemical group C([C@@H](N(CC1)CC=C)[C@@H]2C=C[C@@H]3O)C4=CC=C(O)C5=C4[C@@]21[C@H]3O5 UIQMVEYFGZJHCZ-SSTWWWIQSA-N 0.000 claims 1
- 208000012488 Opiate Overdose Diseases 0.000 claims 1
- 230000037005 anaesthesia Effects 0.000 claims 1
- IFKLAQQSCNILHL-QHAWAJNXSA-N butorphanol Chemical group N1([C@@H]2CC3=CC=C(C=C3[C@@]3([C@]2(CCCC3)O)CC1)O)CC1CCC1 IFKLAQQSCNILHL-QHAWAJNXSA-N 0.000 claims 1
- 229960001113 butorphanol Drugs 0.000 claims 1
- 229950002213 cyclazocine Drugs 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 229960005181 morphine Drugs 0.000 claims 1
- 229960000938 nalorphine Drugs 0.000 claims 1
- 229960004127 naloxone Drugs 0.000 claims 1
- UZHSEJADLWPNLE-GRGSLBFTSA-N naloxone Chemical group O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(O)C2=C5[C@@]13CCN4CC=C UZHSEJADLWPNLE-GRGSLBFTSA-N 0.000 claims 1
- DQCKKXVULJGBQN-XFWGSAIBSA-N naltrexone Chemical group N1([C@@H]2CC3=CC=C(C=4O[C@@H]5[C@](C3=4)([C@]2(CCC5=O)O)CC1)O)CC1CC1 DQCKKXVULJGBQN-XFWGSAIBSA-N 0.000 claims 1
- 229960003086 naltrexone Drugs 0.000 claims 1
- 229940127240 opiate Drugs 0.000 claims 1
- 238000002638 palliative care Methods 0.000 claims 1
- KHUXNRRPPZOJPT-UHFFFAOYSA-N phenoxy radical Chemical group O=C1C=C[CH]C=C1 KHUXNRRPPZOJPT-UHFFFAOYSA-N 0.000 claims 1
- 230000002980 postoperative effect Effects 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 238000012453 sprague-dawley rat model Methods 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962885311P | 2019-08-11 | 2019-08-11 | |
| US62/885,311 | 2019-08-11 | ||
| US16/540,058 US11186585B2 (en) | 2018-08-17 | 2019-08-14 | Compositions and methods of enhancing opioid receptor engagement by opioid hexadienoates and optionally substituted hexadienoates |
| US16/540,058 | 2019-08-14 | ||
| PCT/US2020/021599 WO2021029914A1 (en) | 2019-08-11 | 2020-03-07 | Compositions and methods of enhancing opioid receptor engagement by opioid hexadienoates and optionally substituted hexadienoates |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022544564A JP2022544564A (ja) | 2022-10-19 |
| JPWO2021029914A5 true JPWO2021029914A5 (https=) | 2023-03-15 |
| JP2022544564A5 JP2022544564A5 (https=) | 2023-03-15 |
| JP7535569B2 JP7535569B2 (ja) | 2024-08-16 |
Family
ID=74571142
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022509137A Active JP7535569B2 (ja) | 2019-08-11 | 2020-03-07 | オピオイドヘキサジエノエート及び選択的に置換されたヘキサジエノエートによってオピオイド受容体の結合を改善する組成物並びに方法 |
Country Status (6)
| Country | Link |
|---|---|
| EP (1) | EP4010078A4 (https=) |
| JP (1) | JP7535569B2 (https=) |
| CN (1) | CN114828961B (https=) |
| CA (1) | CA3149152A1 (https=) |
| MX (1) | MX2022001520A (https=) |
| WO (1) | WO2021029914A1 (https=) |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4668685A (en) | 1984-07-05 | 1987-05-26 | E.I. Du Pont De Nemours And Company | Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans, which are analgesics or narcotic antagonists |
| EP0615756B1 (en) * | 1993-03-15 | 2001-06-27 | National Science Council | Nalbuphine esters and long-acting pharmaceutical compositions containing them |
| CN1050130C (zh) | 1997-07-04 | 2000-03-08 | 卢正堂 | 纳洛酮酸脂和纳屈酮酸脂及系列物和制备方法 |
| ES2188481T3 (es) | 2000-04-27 | 2003-07-01 | Oliver Yoa-Pu Hu | Derivados de polinalbufina. |
| TWI226239B (en) | 2000-05-15 | 2005-01-11 | You-Pu Hu | Novel oral pharmaceutical composition containing nalbuphine ester prodrug |
| CA2771263A1 (en) | 2000-07-27 | 2002-02-07 | Rutgers, The State University | Therapeutic polyesters and polyamides |
| US6569449B1 (en) * | 2000-11-13 | 2003-05-27 | University Of Kentucky Research Foundation | Transdermal delivery of opioid antagonist prodrugs |
| US20040033253A1 (en) | 2002-02-19 | 2004-02-19 | Ihor Shevchuk | Acyl opioid antagonists |
| US7759358B2 (en) | 2003-07-23 | 2010-07-20 | Crooks Peter A | Oral bioavailable prodrugs |
| US20050137141A1 (en) | 2003-10-24 | 2005-06-23 | John Hilfinger | Prodrug composition |
| EP1928881A2 (en) | 2005-08-19 | 2008-06-11 | Pharmacofore, Inc. | Prodrugs of active agents |
| US20090186832A1 (en) | 2008-01-18 | 2009-07-23 | Shire Llc | Amino acid peptide pro-drugs of phenolic analgesics and uses thereof |
| EP2413937A1 (en) | 2009-04-02 | 2012-02-08 | Shire LLC | Novel dicarboxylic acid linked amino acid and peptide prodrugs of opioids and uses thereof |
| AU2010272233A1 (en) | 2009-07-17 | 2012-02-09 | Shire Llc | Novel carbamate amino acid and peptide prodrugs of opioids and uses thereof |
| EP2628489B1 (en) * | 2009-07-21 | 2017-03-01 | Nektar Therapeutics | PEG oligomer-fentanyl conjugates |
| US20110190267A1 (en) * | 2010-01-05 | 2011-08-04 | Shire Pharmaceuticals, Inc. | Prodrugs of opioids and uses thereof |
| US8461171B2 (en) * | 2010-02-09 | 2013-06-11 | QRxPharma Ltd. | Hybrid opioid compounds and compositions |
| EP2552924B1 (en) * | 2010-04-02 | 2015-09-16 | Zynerba Pharmaceuticals, Inc. | Transdermally deliverable opioid prodrugs, abuse-resistant compositions and methods of using opioid prodrugs |
| AR084620A1 (es) * | 2010-12-28 | 2013-05-29 | Euro Celtique Sa | Una combinacion de un agonista opiaceo y un antagonista opiaceo en el tratamiento de la enfermedad de parkinson |
| US10017519B2 (en) * | 2015-04-27 | 2018-07-10 | 3St Research Llc | Alpha-hydroxy carboxylic acid and derivatives and other GRAS based prodrugs of oxycodone and uses thereof |
| US9987269B2 (en) * | 2015-04-27 | 2018-06-05 | 3St Research Llc | Alpha-hydroxy carboxylic acid and derivatives and other GRAS-based prodrugs of oxymorphone and uses thereof |
| US10449190B2 (en) * | 2015-04-27 | 2019-10-22 | John K. Thottathil | Alpha-hydroxy carboxylic acid and derivatives and other GRAS-based prodrugs of opioids and uses thereof |
| US9974858B2 (en) * | 2015-08-29 | 2018-05-22 | Medrx Co., Ltd | Percutaneous absorption composition |
| US12590065B2 (en) * | 2017-04-14 | 2026-03-31 | Zevra Therapeutics, Inc. | Levorphanol prodrugs and processes for making and using them |
| US11186585B2 (en) * | 2018-08-17 | 2021-11-30 | Kappa-Pharma LLC | Compositions and methods of enhancing opioid receptor engagement by opioid hexadienoates and optionally substituted hexadienoates |
-
2020
- 2020-03-07 CA CA3149152A patent/CA3149152A1/en active Pending
- 2020-03-07 EP EP20852037.9A patent/EP4010078A4/en active Pending
- 2020-03-07 CN CN202080071185.9A patent/CN114828961B/zh active Active
- 2020-03-07 MX MX2022001520A patent/MX2022001520A/es unknown
- 2020-03-07 JP JP2022509137A patent/JP7535569B2/ja active Active
- 2020-03-07 WO PCT/US2020/021599 patent/WO2021029914A1/en not_active Ceased
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