JP2011520977A5 - - Google Patents
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- Publication number
- JP2011520977A5 JP2011520977A5 JP2011510691A JP2011510691A JP2011520977A5 JP 2011520977 A5 JP2011520977 A5 JP 2011520977A5 JP 2011510691 A JP2011510691 A JP 2011510691A JP 2011510691 A JP2011510691 A JP 2011510691A JP 2011520977 A5 JP2011520977 A5 JP 2011520977A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- pharmaceutically acceptable
- solvate
- compound
- 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
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- 150000001875 compounds Chemical class 0.000 claims description 41
- 239000000203 mixture Substances 0.000 claims description 36
- 150000003839 salts Chemical class 0.000 claims description 19
- 239000011780 sodium chloride Substances 0.000 claims description 19
- 239000012453 solvate Substances 0.000 claims description 18
- 206010061218 Inflammation Diseases 0.000 claims description 15
- 208000002193 Pain Diseases 0.000 claims description 15
- 206010037660 Pyrexia Diseases 0.000 claims description 15
- 230000004054 inflammatory process Effects 0.000 claims description 15
- 230000000302 ischemic Effects 0.000 claims description 15
- 206010022114 Injury Diseases 0.000 claims description 14
- 206010052639 Nerve injury Diseases 0.000 claims description 14
- 238000009472 formulation Methods 0.000 claims description 11
- 230000002265 prevention Effects 0.000 claims description 9
- 201000010099 disease Diseases 0.000 claims description 7
- 229940022659 Acetaminophen Drugs 0.000 claims description 5
- RZVAJINKPMORJF-UHFFFAOYSA-N p-acetaminophenol Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims description 5
- 229960005489 paracetamol Drugs 0.000 claims description 5
- 238000002360 preparation method Methods 0.000 claims description 5
- OROGSEYTTFOCAN-DNJOTXNNSA-N Codeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC OROGSEYTTFOCAN-DNJOTXNNSA-N 0.000 claims description 4
- XLMALTXPSGQGBX-GCJKJVERSA-N Dextropropoxyphene Chemical compound C([C@](OC(=O)CC)([C@H](C)CN(C)C)C=1C=CC=CC=1)C1=CC=CC=C1 XLMALTXPSGQGBX-GCJKJVERSA-N 0.000 claims description 4
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 claims description 4
- 239000000969 carrier Substances 0.000 claims description 4
- 229960004193 dextropropoxyphene Drugs 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims description 4
- 229940021182 non-steroidal anti-inflammatory drugs Drugs 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 3
- SVUOLADPCWQTTE-UHFFFAOYSA-N 1H-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 claims description 2
- SKTFQHRVFFOHTQ-UHFFFAOYSA-N 8-bromo-1,3-dimethyl-7H-purine-2,6-dione Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC(Br)=N2 SKTFQHRVFFOHTQ-UHFFFAOYSA-N 0.000 claims description 2
- HNYOPLTXPVRDBG-UHFFFAOYSA-N Barbituric acid Chemical compound O=C1CC(=O)NC(=O)N1 HNYOPLTXPVRDBG-UHFFFAOYSA-N 0.000 claims description 2
- OFZCIYFFPZCNJE-UHFFFAOYSA-N Carisoprodol Chemical compound NC(=O)OCC(C)(CCC)COC(=O)NC(C)C OFZCIYFFPZCNJE-UHFFFAOYSA-N 0.000 claims description 2
- 229960004587 Carisoprodol Drugs 0.000 claims description 2
- AAOVKJBEBIDNHE-UHFFFAOYSA-N Diazepam Chemical compound N=1CC(=O)N(C)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 AAOVKJBEBIDNHE-UHFFFAOYSA-N 0.000 claims description 2
- HCFDWZZGGLSKEP-UHFFFAOYSA-N Doxylamine Chemical compound C=1C=CC=NC=1C(C)(OCCN(C)C)C1=CC=CC=C1 HCFDWZZGGLSKEP-UHFFFAOYSA-N 0.000 claims description 2
- 229960005178 Doxylamine Drugs 0.000 claims description 2
- 229960005293 Etodolac Drugs 0.000 claims description 2
- XFBVBWWRPKNWHW-UHFFFAOYSA-N Etodolac Chemical compound C1COC(CC)(CC(O)=O)C2=N[C]3C(CC)=CC=CC3=C21 XFBVBWWRPKNWHW-UHFFFAOYSA-N 0.000 claims description 2
- SYTBZMRGLBWNTM-UHFFFAOYSA-N Flurbiprofen Chemical compound FC1=CC(C(C(O)=O)C)=CC=C1C1=CC=CC=C1 SYTBZMRGLBWNTM-UHFFFAOYSA-N 0.000 claims description 2
- LLPOLZWFYMWNKH-CMKMFDCUSA-N Hydrocodone Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)CC(=O)[C@@H]1OC1=C2C3=CC=C1OC LLPOLZWFYMWNKH-CMKMFDCUSA-N 0.000 claims description 2
- WVLOADHCBXTIJK-YNHQPCIGSA-N Hydromorphone Chemical compound 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 description 2
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 claims description 2
- ZRVUJXDFFKFLMG-UHFFFAOYSA-N Ilacox Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=NC=C(C)S1 ZRVUJXDFFKFLMG-UHFFFAOYSA-N 0.000 claims description 2
- DKYWVDODHFEZIM-UHFFFAOYSA-N Ketoprofen Chemical compound OC(=O)C(C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-UHFFFAOYSA-N 0.000 claims description 2
- OZWKMVRBQXNZKK-UHFFFAOYSA-N Ketorolac Chemical compound OC(=O)C1CCN2C1=CC=C2C(=O)C1=CC=CC=C1 OZWKMVRBQXNZKK-UHFFFAOYSA-N 0.000 claims description 2
- JAQUASYNZVUNQP-USXIJHARSA-N Levorphanol Chemical compound C1C2=CC=C(O)C=C2[C@]23CCN(C)[C@H]1[C@@H]2CCCC3 JAQUASYNZVUNQP-USXIJHARSA-N 0.000 claims description 2
- 229960003406 Levorphanol Drugs 0.000 claims description 2
- DIWRORZWFLOCLC-UHFFFAOYSA-N Lorazepam Chemical compound C12=CC(Cl)=CC=C2NC(=O)C(O)N=C1C1=CC=CC=C1Cl DIWRORZWFLOCLC-UHFFFAOYSA-N 0.000 claims description 2
- DDLIGBOFAVUZHB-UHFFFAOYSA-N Midazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NC=C2CN=C1C1=CC=CC=C1F DDLIGBOFAVUZHB-UHFFFAOYSA-N 0.000 claims description 2
- 229960003793 Midazolam Drugs 0.000 claims description 2
- BQJCRHHNABKAKU-KBQPJGBKSA-N Morphine Chemical compound 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 description 2
- CMWTZPSULFXXJA-VIFPVBQESA-N Naproxen Chemical compound C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-N 0.000 claims description 2
- QYSPLQLAKJAUJT-UHFFFAOYSA-N Piroxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=CC=CC=N1 QYSPLQLAKJAUJT-UHFFFAOYSA-N 0.000 claims description 2
- 229940069956 Propoxyphene Drugs 0.000 claims description 2
- TVYLLZQTGLZFBW-ZBFHGGJFSA-N Tramadol Chemical compound COC1=CC=CC([C@]2(O)[C@H](CCCC2)CN(C)C)=C1 TVYLLZQTGLZFBW-ZBFHGGJFSA-N 0.000 claims description 2
- 229960004380 Tramadol Drugs 0.000 claims description 2
- 229960001138 acetylsalicylic acid Drugs 0.000 claims description 2
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims description 2
- 229960001948 caffeine Drugs 0.000 claims description 2
- 229960004126 codeine Drugs 0.000 claims description 2
- 229960003529 diazepam Drugs 0.000 claims description 2
- 229960001259 diclofenac Drugs 0.000 claims description 2
- DCOPUUMXTXDBNB-UHFFFAOYSA-N diclofenac Chemical compound OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl DCOPUUMXTXDBNB-UHFFFAOYSA-N 0.000 claims description 2
- 229960002390 flurbiprofen Drugs 0.000 claims description 2
- 229960000240 hydrocodone Drugs 0.000 claims description 2
- 229960001410 hydromorphone Drugs 0.000 claims description 2
- 229960001680 ibuprofen Drugs 0.000 claims description 2
- 229960000991 ketoprofen Drugs 0.000 claims description 2
- 229960004752 ketorolac Drugs 0.000 claims description 2
- 229960004391 lorazepam Drugs 0.000 claims description 2
- 229960001929 meloxicam Drugs 0.000 claims description 2
- OJLOPKGSLYJEMD-URPKTTJQSA-N methyl 7-[(1R,2R,3R)-3-hydroxy-2-[(1E)-4-hydroxy-4-methyloct-1-en-1-yl]-5-oxocyclopentyl]heptanoate Chemical compound CCCCC(C)(O)C\C=C\[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC OJLOPKGSLYJEMD-URPKTTJQSA-N 0.000 claims description 2
- -1 methylhexital Chemical compound 0.000 claims description 2
- 229960005249 misoprostol Drugs 0.000 claims description 2
- 229960005181 morphine Drugs 0.000 claims description 2
- 229930014694 morphine Natural products 0.000 claims description 2
- 229960002009 naproxen Drugs 0.000 claims description 2
- 230000003364 opioid Effects 0.000 claims description 2
- 229960003357 pamabrom Drugs 0.000 claims description 2
- 239000002504 physiological saline solution Substances 0.000 claims description 2
- 229960002702 piroxicam Drugs 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 210000004556 Brain Anatomy 0.000 description 1
- UZVHFVZFNXBMQJ-UHFFFAOYSA-N Butalbital Chemical compound CC(C)CC1(CC=C)C(=O)NC(=O)NC1=O UZVHFVZFNXBMQJ-UHFFFAOYSA-N 0.000 description 1
- 210000004165 Myocardium Anatomy 0.000 description 1
- 229960002546 butalbital Drugs 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- QXNVGIXVLWOKEQ-UHFFFAOYSA-N disodium Chemical class [Na][Na] QXNVGIXVLWOKEQ-UHFFFAOYSA-N 0.000 description 1
- 238000007614 solvation Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US5477408P | 2008-05-20 | 2008-05-20 | |
| US61/054,774 | 2008-05-20 | ||
| PCT/US2009/044743 WO2009143295A1 (en) | 2008-05-20 | 2009-05-20 | Water-soluble acetaminophen analogs |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014049672A Division JP2014111658A (ja) | 2008-05-20 | 2014-03-13 | 水溶性アセトアミノフェン類似体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011520977A JP2011520977A (ja) | 2011-07-21 |
| JP2011520977A5 true JP2011520977A5 (US07981874-20110719-C00313.png) | 2012-07-05 |
| JP5757864B2 JP5757864B2 (ja) | 2015-08-05 |
Family
ID=41340538
Family Applications (6)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011510691A Expired - Fee Related JP5757864B2 (ja) | 2008-05-20 | 2009-05-20 | 水溶性アセトアミノフェン類似体 |
| JP2014049672A Withdrawn JP2014111658A (ja) | 2008-05-20 | 2014-03-13 | 水溶性アセトアミノフェン類似体 |
| JP2016016971A Expired - Fee Related JP6063072B2 (ja) | 2008-05-20 | 2016-02-01 | 水溶性アセトアミノフェン類似体 |
| JP2016242968A Withdrawn JP2017057217A (ja) | 2008-05-20 | 2016-12-15 | 水溶性アセトアミノフェン類似体 |
| JP2018098716A Withdrawn JP2018135392A (ja) | 2008-05-20 | 2018-05-23 | 水溶性アセトアミノフェン類似体 |
| JP2020074690A Withdrawn JP2020114876A (ja) | 2008-05-20 | 2020-04-20 | 水溶性アセトアミノフェン類似体 |
Family Applications After (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014049672A Withdrawn JP2014111658A (ja) | 2008-05-20 | 2014-03-13 | 水溶性アセトアミノフェン類似体 |
| JP2016016971A Expired - Fee Related JP6063072B2 (ja) | 2008-05-20 | 2016-02-01 | 水溶性アセトアミノフェン類似体 |
| JP2016242968A Withdrawn JP2017057217A (ja) | 2008-05-20 | 2016-12-15 | 水溶性アセトアミノフェン類似体 |
| JP2018098716A Withdrawn JP2018135392A (ja) | 2008-05-20 | 2018-05-23 | 水溶性アセトアミノフェン類似体 |
| JP2020074690A Withdrawn JP2020114876A (ja) | 2008-05-20 | 2020-04-20 | 水溶性アセトアミノフェン類似体 |
Country Status (12)
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009143295A1 (en) | 2008-05-20 | 2009-11-26 | Neurogesx, Inc. | Water-soluble acetaminophen analogs |
| RU2010151951A (ru) | 2008-05-20 | 2012-06-27 | Ньюроджесэкс, Инк. (Us) | Общие пролекарства гепатопротектора и ацетаминофена |
| EP2291084A4 (en) | 2008-05-20 | 2012-04-25 | Neurogesx Inc | CARBONATE PRODRUGS AND METHOD FOR THEIR USE |
| EP2177215A1 (en) | 2008-10-17 | 2010-04-21 | Laboratorios Del. Dr. Esteve, S.A. | Co-crystals of tramadol and NSAIDs |
| US9359376B2 (en) * | 2011-04-08 | 2016-06-07 | Sphaera Pharma Pte. Ltd | Substituted methylformyl reagents and method of using same to modify physicochemical and/or pharmacokinetic properties of compounds |
| WO2013044064A1 (en) | 2011-09-22 | 2013-03-28 | Neurogesx, Inc. | Acetaminophen conjugates, compositions and methods of use thereof |
| CA3042642A1 (en) | 2013-08-12 | 2015-02-19 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded immediate release abuse deterrent pill |
| US10172797B2 (en) | 2013-12-17 | 2019-01-08 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| US9492444B2 (en) | 2013-12-17 | 2016-11-15 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| US9707184B2 (en) | 2014-07-17 | 2017-07-18 | Pharmaceutical Manufacturing Research Services, Inc. | Immediate release abuse deterrent liquid fill dosage form |
| US11311512B2 (en) | 2014-08-12 | 2022-04-26 | Monash University | Lymph directing prodrugs |
| CA2964628A1 (en) | 2014-10-20 | 2016-04-28 | Pharmaceutical Manufacturing Research Services, Inc. | Extended release abuse deterrent liquid fill dosage form |
| PL3209302T3 (pl) | 2014-10-21 | 2019-10-31 | Abbvie Inc | Proleki karbidopy i L-dopy oraz ich zastosowanie do leczenia choroby Parkinsona |
| EP3265097A4 (en) * | 2015-03-03 | 2018-11-07 | Kindred Biosciences Inc. | Compositions and methods for treatment and prevention of pyrexia in horses |
| CN108137482B (zh) | 2015-09-08 | 2024-03-15 | 莫纳什大学 | 定向淋巴的前药 |
| EP3445346A1 (en) * | 2016-04-20 | 2019-02-27 | AbbVie Inc. | Carbidopa and l-dopa prodrugs and methods of use |
| US11883497B2 (en) | 2017-08-29 | 2024-01-30 | Puretech Lyt, Inc. | Lymphatic system-directing lipid prodrugs |
| CA3077739A1 (en) | 2017-08-29 | 2019-03-07 | Puretech Lyt, Inc. | Lymphatic system-directing lipid prodrugs |
| US11304954B2 (en) | 2017-12-19 | 2022-04-19 | Puretech Lyt, Inc. | Lipid prodrugs of mycophenolic acid and uses thereof |
| US11608345B1 (en) | 2017-12-19 | 2023-03-21 | Puretech Lyt, Inc. | Lipid prodrugs of rapamycin and its analogs and uses thereof |
| WO2019126378A1 (en) | 2017-12-19 | 2019-06-27 | Ariya Therapeutics, Inc. | Lipid prodrugs of mycophenolic acid and uses thereof |
| US11389409B2 (en) * | 2019-08-30 | 2022-07-19 | Remedy Diagnostics LLC | Transdermal device comprising acetaminophen prodrug |
| WO2021159021A1 (en) | 2020-02-05 | 2021-08-12 | Puretech Lyt, Inc. | Lipid prodrugs of neurosteroids |
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| FR2444043A1 (fr) * | 1978-12-15 | 1980-07-11 | Bottu | Nouveau derive du paracetamol, son procede de preparation et son utilisation en therapeutique |
| DK406686D0 (da) * | 1986-08-26 | 1986-08-26 | Hans Bundgaard | Carboxylsyrederivater |
| US5001115A (en) * | 1989-05-17 | 1991-03-19 | University Of Florida | Prodrugs of biologically active hydroxyaromatic compounds |
| JPH06501448A (ja) * | 1989-12-26 | 1994-02-17 | ノバ ファーマシューティカル コーポレイション | 無水物プロドラッグ組成物 |
| US5627165A (en) * | 1990-06-13 | 1997-05-06 | Drug Innovation & Design, Inc. | Phosphorous prodrugs and therapeutic delivery systems using same |
| US5272171A (en) * | 1992-02-13 | 1993-12-21 | Bristol-Myers Squibb Company | Phosphonooxy and carbonate derivatives of taxol |
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| IT1282736B1 (it) * | 1996-05-21 | 1998-03-31 | Angelini Ricerche Spa | Uso di derivati del p-amminofenolo per preparare composizioni farmaceutiche utili nel trattamento di malattie neurodegenerative |
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| WO2009143295A1 (en) | 2008-05-20 | 2009-11-26 | Neurogesx, Inc. | Water-soluble acetaminophen analogs |
| EP2291084A4 (en) * | 2008-05-20 | 2012-04-25 | Neurogesx Inc | CARBONATE PRODRUGS AND METHOD FOR THEIR USE |
| RU2010151951A (ru) | 2008-05-20 | 2012-06-27 | Ньюроджесэкс, Инк. (Us) | Общие пролекарства гепатопротектора и ацетаминофена |
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| WO2013044064A1 (en) | 2011-09-22 | 2013-03-28 | Neurogesx, Inc. | Acetaminophen conjugates, compositions and methods of use thereof |
-
2009
- 2009-05-20 WO PCT/US2009/044743 patent/WO2009143295A1/en active Application Filing
- 2009-05-20 JP JP2011510691A patent/JP5757864B2/ja not_active Expired - Fee Related
- 2009-05-20 BR BRPI0912326A patent/BRPI0912326A2/pt not_active IP Right Cessation
- 2009-05-20 CN CN2009801282182A patent/CN102149672A/zh active Pending
- 2009-05-20 KR KR1020107027998A patent/KR101698028B1/ko active IP Right Grant
- 2009-05-20 MX MX2010012648A patent/MX2010012648A/es active IP Right Grant
- 2009-05-20 RU RU2010151952/04A patent/RU2010151952A/ru not_active Application Discontinuation
- 2009-05-20 EP EP09751523.3A patent/EP2291348A4/en not_active Withdrawn
- 2009-05-20 US US12/993,088 patent/US20110212926A1/en not_active Abandoned
- 2009-05-20 CA CA2724877A patent/CA2724877C/en not_active Expired - Fee Related
- 2009-05-20 AU AU2009249067A patent/AU2009249067A1/en not_active Abandoned
- 2009-05-20 CN CN201510381430.7A patent/CN105254662A/zh active Pending
-
2010
- 2010-11-17 IL IL209382A patent/IL209382A0/en unknown
-
2014
- 2014-03-13 JP JP2014049672A patent/JP2014111658A/ja not_active Withdrawn
-
2016
- 2016-02-01 JP JP2016016971A patent/JP6063072B2/ja not_active Expired - Fee Related
- 2016-03-22 US US15/077,802 patent/US9981998B2/en not_active Expired - Fee Related
- 2016-12-15 JP JP2016242968A patent/JP2017057217A/ja not_active Withdrawn
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2018
- 2018-04-25 US US15/962,934 patent/US10442826B2/en not_active Expired - Fee Related
- 2018-05-23 JP JP2018098716A patent/JP2018135392A/ja not_active Withdrawn
-
2019
- 2019-09-09 US US16/565,173 patent/US11021498B2/en active Active
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2020
- 2020-04-20 JP JP2020074690A patent/JP2020114876A/ja not_active Withdrawn
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