JP2014502972A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2014502972A5 JP2014502972A5 JP2013548605A JP2013548605A JP2014502972A5 JP 2014502972 A5 JP2014502972 A5 JP 2014502972A5 JP 2013548605 A JP2013548605 A JP 2013548605A JP 2013548605 A JP2013548605 A JP 2013548605A JP 2014502972 A5 JP2014502972 A5 JP 2014502972A5
- Authority
- JP
- Japan
- Prior art keywords
- prodrug
- trypsin
- oxycodone
- compound
- trypsin inhibitor
- 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
- 229940002612 prodrug Drugs 0.000 claims 37
- 239000000651 prodrug Substances 0.000 claims 37
- 239000002753 trypsin inhibitor Substances 0.000 claims 31
- 229940122618 Trypsin inhibitor Drugs 0.000 claims 29
- 101710162629 Trypsin inhibitor Proteins 0.000 claims 29
- BRUQQQPBMZOVGD-XFKAJCMBSA-N Oxycodone Chemical compound O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(OC)C2=C5[C@@]13CCN4C BRUQQQPBMZOVGD-XFKAJCMBSA-N 0.000 claims 26
- 229960002085 oxycodone Drugs 0.000 claims 26
- 150000001875 compounds Chemical class 0.000 claims 22
- 239000000203 mixture Substances 0.000 claims 22
- 102000004142 Trypsin Human genes 0.000 claims 18
- 108090000631 Trypsin Proteins 0.000 claims 18
- 239000012588 trypsin Substances 0.000 claims 18
- 238000000034 method Methods 0.000 claims 10
- 238000006243 chemical reaction Methods 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 5
- 150000002085 enols Chemical class 0.000 claims 5
- 230000037406 food intake Effects 0.000 claims 5
- 239000003112 inhibitor Substances 0.000 claims 5
- 239000001301 oxygen Substances 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- ZRALSGWEFCBTJO-UHFFFAOYSA-N Guanidine Chemical group NC(N)=N ZRALSGWEFCBTJO-UHFFFAOYSA-N 0.000 claims 4
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical group NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 4
- 150000002431 hydrogen Chemical group 0.000 claims 4
- 230000003278 mimic effect Effects 0.000 claims 4
- 230000002265 prevention Effects 0.000 claims 4
- -1 amino, substituted amino, hydroxyl Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 238000009472 formulation Methods 0.000 claims 3
- 150000004677 hydrates Chemical class 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 239000004475 Arginine Substances 0.000 claims 2
- 102000004190 Enzymes Human genes 0.000 claims 2
- 108090000790 Enzymes Proteins 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 239000004472 Lysine Substances 0.000 claims 2
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 2
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Chemical group CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000000266 alpha-aminoacyl group Chemical group 0.000 claims 2
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 2
- 239000004202 carbamide Chemical group 0.000 claims 2
- 235000013877 carbamide Nutrition 0.000 claims 2
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 claims 2
- 238000003776 cleavage reaction Methods 0.000 claims 2
- 238000013270 controlled release Methods 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Chemical group CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical group 0.000 claims 2
- 238000013160 medical therapy Methods 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 230000007017 scission Effects 0.000 claims 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims 2
- SXNCILYLEKIXPV-IZZNHLLZSA-N (4s)-4-[[(2r)-2-(benzylsulfonylamino)-4-phenylbutanoyl]amino]-5-[(4-carbamimidoylphenyl)methylamino]-5-oxopentanoic acid Chemical compound C1=CC(C(=N)N)=CC=C1CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](NS(=O)(=O)CC=1C=CC=CC=1)CCC1=CC=CC=C1 SXNCILYLEKIXPV-IZZNHLLZSA-N 0.000 claims 1
- WPANETAWYGDRLL-UHFFFAOYSA-N 4-aminobenzenecarboximidamide Chemical compound NC(=N)C1=CC=C(N)C=C1 WPANETAWYGDRLL-UHFFFAOYSA-N 0.000 claims 1
- LPRSIBLBCFRSKX-QFIPXVFZSA-N 6-[4-[(2s)-5-(diaminomethylideneamino)-2-(naphthalen-2-ylsulfonylamino)pentanoyl]piperazin-1-yl]-6-oxohexanoic acid Chemical compound O=C([C@@H](NS(=O)(=O)C=1C=C2C=CC=CC2=CC=1)CCCNC(=N)N)N1CCN(C(=O)CCCCC(O)=O)CC1 LPRSIBLBCFRSKX-QFIPXVFZSA-N 0.000 claims 1
- 206010013654 Drug abuse Diseases 0.000 claims 1
- ZXBYWYQEQQBMBT-UHFFFAOYSA-N amido phenyl pyruvic acid Chemical compound NC(=N)C1=CC=C(CC(=O)C(O)=O)C=C1 ZXBYWYQEQQBMBT-UHFFFAOYSA-N 0.000 claims 1
- 125000000637 arginyl group Chemical group N[C@@H](CCCNC(N)=N)C(=O)* 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 238000010228 ex vivo assay Methods 0.000 claims 1
- 238000005462 in vivo assay Methods 0.000 claims 1
- 239000011541 reaction mixture Substances 0.000 claims 1
- 208000011117 substance-related disease Diseases 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- YVTDJCBGKCQSPF-DFIMAEIUSA-N CC(C)(CNC([C@H](CCCNC(N)=N)NC(CNC(CC(O)=O)=O)=O)=O)CN(C)C(OC([C@@H]([C@]12CCN(C)[C@@H]3C4)Oc5c1c4ccc5OC)=CC[C@]23O)=O Chemical compound CC(C)(CNC([C@H](CCCNC(N)=N)NC(CNC(CC(O)=O)=O)=O)=O)CN(C)C(OC([C@@H]([C@]12CCN(C)[C@@H]3C4)Oc5c1c4ccc5OC)=CC[C@]23O)=O YVTDJCBGKCQSPF-DFIMAEIUSA-N 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161431781P | 2011-01-11 | 2011-01-11 | |
| US61/431,781 | 2011-01-11 | ||
| PCT/US2012/020649 WO2012096887A2 (en) | 2011-01-11 | 2012-01-09 | Compositions comprising enzyme-cleavable oxycodone prodrug |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014502972A JP2014502972A (ja) | 2014-02-06 |
| JP2014502972A5 true JP2014502972A5 (enExample) | 2015-06-18 |
| JP6016810B2 JP6016810B2 (ja) | 2016-10-26 |
Family
ID=46455749
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013548605A Active JP6016810B2 (ja) | 2011-01-11 | 2012-01-09 | 酵素切断可能なオキシコドンプロドラッグを含んでなる組成物 |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US8569228B2 (enExample) |
| EP (1) | EP2663187B1 (enExample) |
| JP (1) | JP6016810B2 (enExample) |
| CN (1) | CN103384472B (enExample) |
| AU (1) | AU2012205733B2 (enExample) |
| BR (1) | BR112013017296B1 (enExample) |
| CA (1) | CA2814763C (enExample) |
| DK (1) | DK2663187T3 (enExample) |
| ES (1) | ES2584634T3 (enExample) |
| IL (1) | IL225904B (enExample) |
| RU (1) | RU2609412C2 (enExample) |
| TW (1) | TWI526209B (enExample) |
| WO (1) | WO2012096887A2 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2653568T3 (es) | 2004-06-12 | 2018-02-07 | Collegium Pharmaceutical, Inc. | Formulaciones de fármacos para la prevención del abuso |
| UA102916C2 (uk) | 2009-07-02 | 2013-08-27 | Кемфарм, Інк. | Композиція на основі кон'югату гідрокодону з бензойною кислотою, похідними бензойної кислоти або гетероарилкарбоновою кислотою, проліки, спосіб лікування від зловживань |
| 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 |
| US10668060B2 (en) | 2009-12-10 | 2020-06-02 | Collegium Pharmaceutical, Inc. | Tamper-resistant pharmaceutical compositions of opioids and other drugs |
| 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 |
| US20110262355A1 (en) | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
| AU2012205733B2 (en) * | 2011-01-11 | 2015-10-08 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
| WO2012122420A2 (en) | 2011-03-09 | 2012-09-13 | Pharmacofore, Inc. | Opioid prodrugs with heterocyclic linkers |
| EP2683394B1 (en) | 2011-03-09 | 2021-01-06 | Signature Therapeutics, Inc. | Active agent prodrugs with heterocyclic linkers |
| WO2015081891A1 (en) | 2013-12-06 | 2015-06-11 | Baikang (Suzhou) Co., Ltd | Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs |
| MX2017006520A (es) | 2014-11-25 | 2017-08-09 | Kempharm Inc * | Acido benzoico, derivados de acido benzoico y conjugados de oxicodona de acido heteroaril carboxilico. |
| US11634384B2 (en) | 2014-11-25 | 2023-04-25 | Concentric Analgesics, Inc. | Prodrugs of phenolic TRPV1 agonists |
| WO2017059459A1 (en) * | 2015-10-01 | 2017-04-06 | Elysium Therapeutics, Inc. | Polysubunit opioid prodrugs resistant to overdose and abuse |
| US10335406B2 (en) | 2015-10-01 | 2019-07-02 | Elysium Therapeutics, Inc. | Opioid compositions resistant to overdose and abuse |
| EP3210630A1 (en) * | 2016-02-29 | 2017-08-30 | G.L. Pharma GmbH | Abuse-deterrent pharmaceutical compositions |
| CA3025268A1 (en) | 2016-05-25 | 2017-11-30 | Concentric Analgesics, Inc. | Prodrugs of phenolic trpv1 agonists in combination with local anesthetics and vasoconstrictors for improved local anesthesia |
| US9737530B1 (en) | 2016-06-23 | 2017-08-22 | Collegium Pharmaceutical, Inc. | Process of making stable abuse-deterrent oral formulations |
| US11879019B2 (en) | 2016-12-19 | 2024-01-23 | The Regents Of The University Of California | Dual-enzyme responsive peptides |
| EP3554548A4 (en) | 2016-12-19 | 2020-08-19 | The Regents of The University of California | NON-CRUSHABLE PILL FORMULATIONS |
| CA3056239C (en) | 2017-03-17 | 2023-09-12 | Elysium Therapeutics, Inc. | Polysubunit opioid prodrugs resistant to overdose and abuse |
| CN111683976B (zh) | 2018-02-05 | 2022-11-18 | 生物辐射实验室股份有限公司 | 具有阴离子交换-疏水混合模式配体的色谱树脂 |
| US10717712B2 (en) | 2018-07-27 | 2020-07-21 | Concentric Analgesics, Inc. | Pegylated prodrugs of phenolic TRPV1 agonists |
| KR20230174213A (ko) | 2021-03-09 | 2023-12-27 | 엔사이스 바이오사이언시즈 인크. | 나파모스타트의 변형된 방출 조성물 및 그의 사용 방법 |
| CN117715632A (zh) | 2021-03-09 | 2024-03-15 | 恩赛斯生物科学股份有限公司 | 包含酶可裂解的前药和萘莫司他的组合物及其使用方法 |
| 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 (58)
| 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 |
| US5217987A (en) | 1989-10-30 | 1993-06-08 | Berger Stephen P | Dopamine uptake inhibitors in reducing substance abuse and/or craving |
| 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 |
| EP0893437A4 (en) | 1996-04-10 | 2000-12-27 | Ono Pharmaceutical Co | GUANIDINO TRYPTASE INHIBITOR |
| ES2194536T3 (es) | 1998-11-13 | 2003-11-16 | Lilly Co Eli | Combinacion de duloxetina con farmacos antiinflamatorios no esteroideos. |
| AU781255B2 (en) | 1998-12-15 | 2005-05-12 | Applied Biosystems, Llc | Multiple enzyme assays |
| US6849263B2 (en) | 1998-12-21 | 2005-02-01 | Generex Pharmaceutical Incorporated | Pharmaceutical compositions for buccal delivery of pain relief medications |
| EP1161226B1 (en) | 1999-02-18 | 2004-05-26 | 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 |
| EP2295043A1 (en) * | 1999-10-29 | 2011-03-16 | Euro-Celtique S.A. | Controlled release hydrocodone formulations |
| US20030180352A1 (en) | 1999-11-23 | 2003-09-25 | Patel Mahesh V. | Solid carriers for improved delivery of active ingredients in pharmaceutical compositions |
| US6673574B2 (en) | 2000-11-30 | 2004-01-06 | Unigene Laboratories Inc. | Oral delivery of peptides using enzyme-cleavable membrane translocators |
| ES2364452T3 (es) | 2001-06-11 | 2011-09-02 | Medarex, Inc. | Método para diseñar compuestos profármacos activados por cd10. |
| 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 |
| AU2003219863C1 (en) | 2002-02-22 | 2009-03-05 | Shire Llc | Novel sustained release pharmaceutical compounds to prevent abuse of controlled substances |
| US20100092562A1 (en) | 2002-11-26 | 2010-04-15 | Hollenbeck R Gary | Sustained-release drug delivery compositions and methods |
| MXPA05009757A (es) | 2003-03-13 | 2005-12-05 | Controlled Chemicals Inc | Conjugados de oxicodona con menor potencial de abuso y duracion de accion extendida. |
| EP1782834A3 (en) * | 2003-03-13 | 2007-08-01 | Controlled Chemicals, Inc. | Oxycodone conjugates with lower abuse potential and extended duration of action |
| JP4898445B2 (ja) | 2003-05-29 | 2012-03-14 | シャイア エルエルシー | 乱用抵抗性アンフェタミン化合物類 |
| EA008864B1 (ru) | 2003-09-30 | 2007-08-31 | Нью Ривер Фармасьютикалз Инк. | Фармацевтические композиции для предотвращения передозировки или неправильного употребления лекарственных средств |
| WO2005042773A1 (en) | 2003-10-24 | 2005-05-12 | Gilead Sciences, Inc. | Methods and compositions for identifying therapeutic compounds |
| EP1928881A2 (en) * | 2005-08-19 | 2008-06-11 | Pharmacofore, Inc. | Prodrugs of active agents |
| JP5276982B2 (ja) | 2005-08-26 | 2013-08-28 | ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティ | オキシトシンの投与による頭痛の処置のための方法 |
| 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 |
| US7563821B2 (en) | 2005-12-05 | 2009-07-21 | Xenoport, Inc. | Levodopa prodrug mesylate, compositions thereof, and uses thereof |
| AU2007238858A1 (en) | 2006-04-10 | 2007-10-25 | Shire Llc | Mono and di-substituted oxycodone compounds and compositions |
| US20100144645A1 (en) | 2006-04-14 | 2010-06-10 | Shire Llc | Compositions and methods for enhancing analgesic potency of covalently bound-compounds, attenuating its adverse side effects, and preventing their abuse |
| 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 | |
| WO2008033980A2 (en) | 2006-09-14 | 2008-03-20 | Starfire Systems, Inc. | Synthetic process for cyclic organosilanes |
| WO2008101202A1 (en) | 2007-02-16 | 2008-08-21 | Pharmacofore, Inc. | N-17-alkylated prodrugs of opioids |
| WO2008101187A2 (en) * | 2007-02-16 | 2008-08-21 | Pharmacofore, Inc. | Pro-drugs of peripheral phenolic opioid antagonists |
| MX2010005680A (es) | 2007-11-23 | 2010-12-21 | Protect Pharmaceutical Corp | Composiciones de tapentadol. |
| US9023860B2 (en) | 2007-11-26 | 2015-05-05 | Signature Therapeutics, Inc. | Pro-drugs for controlled release of biologically active compounds |
| WO2009080030A1 (en) | 2007-12-21 | 2009-07-02 | Lifecycle Pharma A/S | Treatment of autoimmune hepatitis with a once daily oral dosage form comprising tacrolimus |
| WO2009092073A2 (en) | 2008-01-18 | 2009-07-23 | Shire Llc | Amino acid and peptide prodrugs of opioid analgesics with reduced gi side-effects |
| JP2011512360A (ja) | 2008-02-14 | 2011-04-21 | アルカーメス，インコーポレイテッド | 選択的オピオイド化合物 |
| CA2723434C (en) | 2008-05-05 | 2018-01-23 | Oramed Ltd. | Methods and compositions for oral administration of exenatide |
| CA2739936C (en) * | 2008-10-17 | 2017-12-12 | Pharmacofore, Inc. | Pharmaceutical compositions with attenuated release of phenolic opioids |
| WO2010100477A2 (en) | 2009-03-03 | 2010-09-10 | Shire Llc | Amino acid and peptide carbamate prodrugs of tapentadol and uses thereof |
| CA2756397A1 (en) * | 2009-04-02 | 2010-10-07 | Shire Llc | Novel dicarboxylic acid linked amino acid and peptide prodrugs of opioids and uses thereof |
| EP2453900A1 (en) | 2009-07-17 | 2012-05-23 | Shire LLC | Novel carbamate amino acid and peptide prodrugs of opioids and uses thereof |
| 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 |
| CA2795222A1 (en) * | 2010-04-21 | 2011-10-27 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
| EP2560490A1 (en) * | 2010-04-21 | 2013-02-27 | Signature Therapeutics, Inc. | 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 |
| US20110262359A1 (en) | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions comprising enzyme-cleavable prodrugs of active agents and inhibitors thereof |
| US20110262355A1 (en) | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
| US20110262360A1 (en) | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions Comprising Enzyme-Cleavable Phenol-Modified Opioid Prodrugs and Inhibitors Thereof |
| WO2011133346A1 (en) * | 2010-04-21 | 2011-10-27 | Pharmacofore, Inc. | Peripheral opioid agonists and peripheral opioid antagonists |
| US9238020B2 (en) | 2010-04-21 | 2016-01-19 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable phenol-modified tapentadol prodrug |
| AU2012205733B2 (en) * | 2011-01-11 | 2015-10-08 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
| WO2012096886A1 (en) | 2011-01-11 | 2012-07-19 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
| EP2683394B1 (en) | 2011-03-09 | 2021-01-06 | Signature Therapeutics, Inc. | Active agent prodrugs with heterocyclic linkers |
| WO2012122420A2 (en) | 2011-03-09 | 2012-09-13 | Pharmacofore, Inc. | Opioid prodrugs with heterocyclic linkers |
-
2012
- 2012-01-09 AU AU2012205733A patent/AU2012205733B2/en active Active
- 2012-01-09 CA CA2814763A patent/CA2814763C/en active Active
- 2012-01-09 ES ES12734573.4T patent/ES2584634T3/es active Active
- 2012-01-09 WO PCT/US2012/020649 patent/WO2012096887A2/en not_active Ceased
- 2012-01-09 BR BR112013017296-7A patent/BR112013017296B1/pt active IP Right Grant
- 2012-01-09 JP JP2013548605A patent/JP6016810B2/ja active Active
- 2012-01-09 RU RU2013137452A patent/RU2609412C2/ru active
- 2012-01-09 CN CN201280003814.XA patent/CN103384472B/zh active Active
- 2012-01-09 EP EP12734573.4A patent/EP2663187B1/en active Active
- 2012-01-09 DK DK12734573.4T patent/DK2663187T3/en active
- 2012-01-09 US US13/346,062 patent/US8569228B2/en active Active
- 2012-01-10 TW TW101100923A patent/TWI526209B/zh active
-
2013
- 2013-04-23 IL IL225904A patent/IL225904B/en active IP Right Grant
- 2013-09-24 US US14/035,871 patent/US8962547B2/en active Active
-
2015
- 2015-01-09 US US14/593,855 patent/US9499581B2/en active Active