JP2012509846A5 - - Google Patents
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- Publication number
- JP2012509846A5 JP2012509846A5 JP2011532298A JP2011532298A JP2012509846A5 JP 2012509846 A5 JP2012509846 A5 JP 2012509846A5 JP 2011532298 A JP2011532298 A JP 2011532298A JP 2011532298 A JP2011532298 A JP 2011532298A JP 2012509846 A5 JP2012509846 A5 JP 2012509846A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- pharmaceutical composition
- group
- amino acid
- alkyl
- 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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- 239000008194 pharmaceutical composition Substances 0.000 claims 18
- 125000002252 acyl group Chemical group 0.000 claims 14
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N phenol group Chemical group C1(=CC=CC=C1)O ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims 14
- 108010016626 Dipeptides Proteins 0.000 claims 12
- 125000000217 alkyl group Chemical group 0.000 claims 11
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 9
- 150000001413 amino acids Chemical class 0.000 claims 8
- 229940002612 prodrug Drugs 0.000 claims 8
- 239000000651 prodrug Substances 0.000 claims 8
- 102000004190 Enzymes Human genes 0.000 claims 7
- 108090000790 Enzymes Proteins 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 125000000547 substituted alkyl group Chemical group 0.000 claims 6
- 125000003107 substituted aryl group Chemical group 0.000 claims 6
- 125000000266 alpha-aminoacyl group Chemical group 0.000 claims 5
- 150000001875 compounds Chemical class 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 150000008575 L-amino acids Chemical class 0.000 claims 4
- 229940122618 Trypsin inhibitor Drugs 0.000 claims 4
- 101710162629 Trypsin inhibitor Proteins 0.000 claims 4
- 125000000539 amino acid group Chemical group 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 150000001721 carbon Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 238000013270 controlled release Methods 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 239000002532 enzyme inhibitor Substances 0.000 claims 4
- 229940125532 enzyme inhibitor Drugs 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 4
- 239000002753 trypsin inhibitor Substances 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 230000003278 mimic effect Effects 0.000 claims 2
- 230000001629 suppression Effects 0.000 claims 2
- 125000004080 3-carboxypropanoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C(O[H])=O 0.000 claims 1
- 239000004475 Arginine Substances 0.000 claims 1
- 206010013654 Drug abuse Diseases 0.000 claims 1
- JOYRKODLDBILNP-UHFFFAOYSA-N Ethyl urethane Chemical compound CCOC(N)=O JOYRKODLDBILNP-UHFFFAOYSA-N 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 1
- VEYYWZRYIYDQJM-ZETCQYMHSA-N N(2)-acetyl-L-lysine Chemical compound CC(=O)N[C@H](C([O-])=O)CCCC[NH3+] VEYYWZRYIYDQJM-ZETCQYMHSA-N 0.000 claims 1
- SNEIUMQYRCDYCH-LURJTMIESA-N N(alpha)-acetyl-L-arginine Chemical compound CC(=O)N[C@H](C(O)=O)CCCNC(N)=N SNEIUMQYRCDYCH-LURJTMIESA-N 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 1
- 125000000637 arginyl group Chemical group N[C@@H](CCCNC(N)=N)C(=O)* 0.000 claims 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 1
- 125000001721 carboxyacetyl group Chemical group 0.000 claims 1
- 238000003776 cleavage reaction Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000002255 enzymatic effect Effects 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 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 1
- 229960001410 hydromorphone Drugs 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229940005483 opioid analgesics Drugs 0.000 claims 1
- 229960005235 piperonyl butoxide Drugs 0.000 claims 1
- 125000004591 piperonyl group Chemical group C(C1=CC=2OCOC2C=C1)* 0.000 claims 1
- 230000007017 scission Effects 0.000 claims 1
- 208000011117 substance-related disease Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10640008P | 2008-10-17 | 2008-10-17 | |
| US61/106,400 | 2008-10-17 | ||
| PCT/US2009/061068 WO2010045599A1 (en) | 2008-10-17 | 2009-10-16 | Pharmaceutical compositions with attenuated release of phenolic opioids |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015037724A Division JP2015129167A (ja) | 2008-10-17 | 2015-02-27 | フェノール性オピオイドの放出が減弱された医薬組成物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012509846A JP2012509846A (ja) | 2012-04-26 |
| JP2012509846A5 true JP2012509846A5 (OSRAM) | 2012-12-06 |
| JP5706825B2 JP5706825B2 (ja) | 2015-04-22 |
Family
ID=41466912
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011532298A Active JP5706825B2 (ja) | 2008-10-17 | 2009-10-16 | フェノール性オピオイドの放出が減弱された医薬組成物 |
| JP2015037724A Pending JP2015129167A (ja) | 2008-10-17 | 2015-02-27 | フェノール性オピオイドの放出が減弱された医薬組成物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015037724A Pending JP2015129167A (ja) | 2008-10-17 | 2015-02-27 | フェノール性オピオイドの放出が減弱された医薬組成物 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US8802681B2 (OSRAM) |
| EP (1) | EP2349241B1 (OSRAM) |
| JP (2) | JP5706825B2 (OSRAM) |
| KR (1) | KR20110081852A (OSRAM) |
| CN (1) | CN102186467B (OSRAM) |
| AU (1) | AU2009305563C1 (OSRAM) |
| BR (1) | BRPI0919711A2 (OSRAM) |
| CA (1) | CA2739936C (OSRAM) |
| IL (1) | IL212081A (OSRAM) |
| MX (1) | MX2011004095A (OSRAM) |
| RU (1) | RU2562583C2 (OSRAM) |
| WO (1) | WO2010045599A1 (OSRAM) |
| ZA (1) | ZA201102361B (OSRAM) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8802681B2 (en) | 2008-10-17 | 2014-08-12 | Signature Therapeutics, Inc. | Pharmaceutical compositions with attenuated release of phenolic opioids |
| WO2011008636A1 (en) * | 2009-07-15 | 2011-01-20 | Mallinckrodt Inc. | 3-oxy-hydromorphone derivatives |
| JP2013503862A (ja) * | 2009-09-08 | 2013-02-04 | シグネーチャー セラピューティクス，インク． | 酵素切断可能なケトン修飾オピオイドプロドラッグとその任意選択のインヒビターとを含んでなる組成物 |
| US20110262359A1 (en) * | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions comprising enzyme-cleavable prodrugs of active agents and inhibitors thereof |
| US20130059914A1 (en) | 2010-04-21 | 2013-03-07 | Signature Therapeutics, Inc. | Compositions Comprising Enzyme-Cleavable Amphetamine Prodrugs and Inhibitors Thereof |
| WO2011133151A1 (en) * | 2010-04-21 | 2011-10-27 | Pharmacofore, Inc. | Compositions comprising enzyme-cleavable phenol-modified opioid prodrugs and inhibitors thereof |
| US9238020B2 (en) | 2010-04-21 | 2016-01-19 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable phenol-modified tapentadol prodrug |
| BR112012026768A2 (pt) * | 2010-04-21 | 2015-09-29 | Signature Therapeutics Inc | composições compreendendo pró-farmacos de opioides cliváveis de modo enzimático e seus inibidores. |
| US20110262355A1 (en) | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
| WO2012096886A1 (en) * | 2011-01-11 | 2012-07-19 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
| WO2012096887A2 (en) * | 2011-01-11 | 2012-07-19 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
| US8685916B2 (en) | 2011-03-09 | 2014-04-01 | Signature Therapeutics, Inc. | Opioid prodrugs with heterocyclic linkers |
| BR112013022946A2 (pt) | 2011-03-09 | 2017-07-18 | Signature Therapeutics Inc | pró-fármacos de agentes ativos com ligantes heterocíclocos |
| US10314839B2 (en) | 2014-10-20 | 2019-06-11 | Elysium Therapeutics, Inc. | Diversion-resistant opioid formulations |
| US11634384B2 (en) | 2014-11-25 | 2023-04-25 | Concentric Analgesics, Inc. | Prodrugs of phenolic TRPV1 agonists |
| US10335406B2 (en) * | 2015-10-01 | 2019-07-02 | Elysium Therapeutics, Inc. | Opioid compositions resistant to overdose and abuse |
| AU2016332071B2 (en) * | 2015-10-01 | 2019-04-18 | Elysium Therapeutics, Inc. | Polysubunit opioid prodrugs resistant to overdose and abuse |
| JP2019516773A (ja) | 2016-05-25 | 2019-06-20 | コンセントリック アナルジジックス，インク． | 改善された局所麻酔のための局所麻酔薬及び血管収縮薬と組み合わせたフェノールｔｒｐｖ１アゴニストのプロドラッグ |
| AU2018234911B2 (en) * | 2017-03-17 | 2024-04-18 | Elysium Therapeutics, Inc. | Polysubunit opioid prodrugs resistant to overdose and abuse |
| TW202019887A (zh) | 2018-07-27 | 2020-06-01 | 美商同心止痛劑股份有限公司 | 酚系trpv1促效劑之聚乙二醇化前藥 |
| EP3934635A4 (en) | 2019-03-06 | 2022-12-07 | Ensysce Biosciences, Inc. | COMPOSITIONS OF ENZYME-CLEAVABLE AMPHETAMINE PRODRUGS AND INHIBITORS THEREOF |
| WO2022192197A1 (en) * | 2021-03-09 | 2022-09-15 | Ensysce Biosciences Inc. | Compositions comprising enzyme-cleavable prodrugs and controlled release nafamostat and methods of use thereof |
| MX2024003466A (es) | 2021-09-29 | 2024-06-04 | Ensysce Biosciences Inc | Profarmacos de metadona escindibles por enzimas y metodos de uso de los mismos. |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU527371B2 (en) | 1980-09-16 | 1983-03-03 | Torii & Co., Ltd. | Amidine |
| US5109118A (en) * | 1989-07-06 | 1992-04-28 | Yutaka Mizushima | Modified biologically active proteins |
| CA2032420A1 (en) | 1989-12-22 | 1991-06-23 | Akira Okuyama | Guanidinobenzene derivatives |
| US6692766B1 (en) | 1994-06-15 | 2004-02-17 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Controlled release oral drug delivery system |
| BR9607492A (pt) * | 1995-01-16 | 1999-06-29 | Commw Scient Ind Res Org | Conjugados de ácidos graxos de composto terapêutico |
| WO1997037969A1 (en) | 1996-04-10 | 1997-10-16 | Ono Pharmaceutical Co., Ltd. | Tryptase inhibitor and novel guanidino derivatives |
| CA2353872C (en) | 1998-12-15 | 2011-05-03 | Tropix, Inc. | Multiple enzyme assays |
| US6849263B2 (en) * | 1998-12-21 | 2005-02-01 | Generex Pharmaceutical Incorporated | Pharmaceutical compositions for buccal delivery of pain relief medications |
| AU3000800A (en) | 1999-02-18 | 2000-09-04 | Supergen, Inc. | Phosphocholine linked prodrug derivatives |
| US7060708B2 (en) | 1999-03-10 | 2006-06-13 | New River Pharmaceuticals Inc. | Active agent delivery systems and methods for protecting and administering active agents |
| US20030180352A1 (en) * | 1999-11-23 | 2003-09-25 | Patel Mahesh V. | Solid carriers for improved delivery of active ingredients in pharmaceutical compositions |
| DE60239679D1 (de) | 2001-06-11 | 2011-05-19 | Medarex Inc | Methode für die ausarbeitung von cd10-aktivierten prodrug-verbindungen |
| US7375082B2 (en) | 2002-02-22 | 2008-05-20 | Shire Llc | Abuse-resistant hydrocodone compounds |
| US7169752B2 (en) | 2003-09-30 | 2007-01-30 | New River Pharmaceuticals Inc. | Compounds and compositions for prevention of overdose of oxycodone |
| US20100092562A1 (en) | 2002-11-26 | 2010-04-15 | Hollenbeck R Gary | Sustained-release drug delivery compositions and methods |
| BRPI0410792B8 (pt) | 2003-05-29 | 2021-05-25 | New River Pharmaceuticals Inc | compostos de anfetamina resistentes à dependencia |
| WO2007022535A2 (en) | 2005-08-19 | 2007-02-22 | Pharmacofore, Inc. | Prodrugs of active agents |
| WO2007025286A2 (en) * | 2005-08-26 | 2007-03-01 | The Board Of Trustees Of The Leland Stanford Junior University | Therapy procedure for drug delivery for trigeminal pain |
| CN101309917B (zh) | 2005-10-06 | 2013-09-11 | 奥斯拜客斯制药有限公司 | 具有增强治疗性质的胃h+，k+-atp酶氘代抑制剂 |
| RU2429223C2 (ru) | 2005-12-05 | 2011-09-20 | Ксенопорт, Инк. | Мезилатное пролекарство леводопы, его композиции и применение |
| JP2009533459A (ja) | 2006-04-14 | 2009-09-17 | シャイア エルエルシー | 共有結合する化合物の鎮痛作用の増強と、有害な副作用の減衰と、前記化合物の乱用の予防とのための組成物及び方法 |
| SG172633A1 (en) * | 2006-05-26 | 2011-07-28 | Pharmacofore Inc | Controlled release of phenolic opioids |
| TWI401237B (zh) | 2006-07-24 | 2013-07-11 | ３-〔（１ｒ，２ｒ）-３-（二甲基氨基）-１-乙基-２-甲基丙基〕酚之製備 | |
| WO2008101202A1 (en) * | 2007-02-16 | 2008-08-21 | Pharmacofore, Inc. | N-17-alkylated prodrugs of opioids |
| US20110105381A2 (en) | 2007-02-16 | 2011-05-05 | Pharmacofore, Inc. | Prodrugs of Peripheral Phenolic Opioid Antagonists |
| PL2596784T3 (pl) | 2007-11-23 | 2017-06-30 | Grünenthal GmbH | Kompozycje tapentadolu |
| US9023860B2 (en) | 2007-11-26 | 2015-05-05 | Signature Therapeutics, Inc. | Pro-drugs for controlled release of biologically active compounds |
| US20090186832A1 (en) | 2008-01-18 | 2009-07-23 | Shire Llc | Amino acid peptide pro-drugs of phenolic analgesics and uses thereof |
| AU2009214500B2 (en) | 2008-02-14 | 2014-10-23 | Alkermes, Inc. | Selective opioid compounds |
| US8802681B2 (en) | 2008-10-17 | 2014-08-12 | Signature Therapeutics, Inc. | Pharmaceutical compositions with attenuated release of phenolic opioids |
| US20100227921A1 (en) | 2009-03-03 | 2010-09-09 | Shire Llc | Amino acid and peptide carbamate prodrugs of tapentadol and uses thereof |
| AU2010231126A1 (en) | 2009-04-02 | 2011-10-13 | Shire Llc | Novel dicarboxylic acid linked amino acid and peptide prodrugs of opioids and uses thereof |
| JP2013527124A (ja) | 2009-07-17 | 2013-06-27 | シャイア エルエルシー | オピオイドの新規カルバマートアミノ酸およびペプチドプロドラッグならびにその使用 |
| EP2560491A1 (en) | 2010-04-21 | 2013-02-27 | Signature Therapeutics, Inc. | Peripheral opioid agonists and peripheral opioid antagonists |
-
2009
- 2009-10-16 US US13/121,335 patent/US8802681B2/en active Active
- 2009-10-16 BR BRPI0919711A patent/BRPI0919711A2/pt active IP Right Grant
- 2009-10-16 AU AU2009305563A patent/AU2009305563C1/en active Active
- 2009-10-16 KR KR1020117011102A patent/KR20110081852A/ko not_active Withdrawn
- 2009-10-16 CN CN200980141547.0A patent/CN102186467B/zh active Active
- 2009-10-16 CA CA2739936A patent/CA2739936C/en active Active
- 2009-10-16 RU RU2011119643/15A patent/RU2562583C2/ru active
- 2009-10-16 WO PCT/US2009/061068 patent/WO2010045599A1/en not_active Ceased
- 2009-10-16 JP JP2011532298A patent/JP5706825B2/ja active Active
- 2009-10-16 EP EP09740597.1A patent/EP2349241B1/en active Active
- 2009-10-16 MX MX2011004095A patent/MX2011004095A/es not_active Application Discontinuation
-
2011
- 2011-03-30 ZA ZA2011/02361A patent/ZA201102361B/en unknown
- 2011-04-03 IL IL212081A patent/IL212081A/en active IP Right Grant
-
2014
- 2014-06-30 US US14/320,351 patent/US9534014B2/en active Active
-
2015
- 2015-02-27 JP JP2015037724A patent/JP2015129167A/ja active Pending
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