JP2018172387A5 - - Google Patents
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- Publication number
- JP2018172387A5 JP2018172387A5 JP2018100108A JP2018100108A JP2018172387A5 JP 2018172387 A5 JP2018172387 A5 JP 2018172387A5 JP 2018100108 A JP2018100108 A JP 2018100108A JP 2018100108 A JP2018100108 A JP 2018100108A JP 2018172387 A5 JP2018172387 A5 JP 2018172387A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- trypsin
- ketone
- hydrogen
- 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
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- 150000001875 compounds Chemical class 0.000 claims 38
- 239000002753 trypsin inhibitor Substances 0.000 claims 13
- 229940122618 Trypsin inhibitor Drugs 0.000 claims 12
- 101710162629 Trypsin inhibitor Proteins 0.000 claims 12
- 150000002576 ketones Chemical class 0.000 claims 11
- 102000004142 Trypsin Human genes 0.000 claims 9
- 108090000631 Trypsin Proteins 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 239000000203 mixture Substances 0.000 claims 9
- 239000012588 trypsin Substances 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 230000002265 prevention Effects 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
- 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
- 125000002252 acyl 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
- 238000006243 chemical reaction Methods 0.000 claims 2
- 238000003776 cleavage reaction Methods 0.000 claims 2
- 238000013270 controlled release Methods 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000037406 food intake Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- 230000007017 scission Effects 0.000 claims 2
- NMDDZEVVQDPECF-LURJTMIESA-N (2s)-2,7-diaminoheptanoic acid Chemical compound NCCCCC[C@H](N)C(O)=O NMDDZEVVQDPECF-LURJTMIESA-N 0.000 claims 1
- 206010013654 Drug abuse Diseases 0.000 claims 1
- QUOGESRFPZDMMT-UHFFFAOYSA-N L-Homoarginine Natural products OC(=O)C(N)CCCCNC(N)=N QUOGESRFPZDMMT-UHFFFAOYSA-N 0.000 claims 1
- AHLPHDHHMVZTML-BYPYZUCNSA-N L-Ornithine Chemical compound NCCC[C@H](N)C(O)=O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 claims 1
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims 1
- QUOGESRFPZDMMT-YFKPBYRVSA-N L-homoarginine Chemical compound OC(=O)[C@@H](N)CCCCNC(N)=N QUOGESRFPZDMMT-YFKPBYRVSA-N 0.000 claims 1
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 1
- AHLPHDHHMVZTML-UHFFFAOYSA-N Orn-delta-NH2 Natural products NCCCC(N)C(O)=O AHLPHDHHMVZTML-UHFFFAOYSA-N 0.000 claims 1
- UTJLXEIPEHZYQJ-UHFFFAOYSA-N Ornithine Natural products OC(=O)C(C)CCCN UTJLXEIPEHZYQJ-UHFFFAOYSA-N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 229960003104 ornithine Drugs 0.000 claims 1
- 239000011541 reaction mixture Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 208000011117 substance-related disease Diseases 0.000 claims 1
- 230000009466 transformation Effects 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24061109P | 2009-09-08 | 2009-09-08 | |
| US61/240,611 | 2009-09-08 | ||
| US28814809P | 2009-12-18 | 2009-12-18 | |
| US61/288,148 | 2009-12-18 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015190867A Division JP2016041698A (ja) | 2009-09-08 | 2015-09-29 | 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018172387A JP2018172387A (ja) | 2018-11-08 |
| JP2018172387A5 true JP2018172387A5 (enExample) | 2019-05-23 |
| JP6778234B2 JP6778234B2 (ja) | 2020-10-28 |
Family
ID=43732738
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012527871A Pending JP2013503862A (ja) | 2009-09-08 | 2010-04-21 | 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 |
| JP2015190867A Pending JP2016041698A (ja) | 2009-09-08 | 2015-09-29 | 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 |
| JP2018100108A Active JP6778234B2 (ja) | 2009-09-08 | 2018-05-25 | 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 |
Family Applications Before (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012527871A Pending JP2013503862A (ja) | 2009-09-08 | 2010-04-21 | 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 |
| JP2015190867A Pending JP2016041698A (ja) | 2009-09-08 | 2015-09-29 | 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 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US9493477B2 (enExample) |
| EP (1) | EP2475429B1 (enExample) |
| JP (3) | JP2013503862A (enExample) |
| CN (1) | CN102695545B (enExample) |
| AU (1) | AU2010293028B2 (enExample) |
| BR (1) | BR112012005124B1 (enExample) |
| CA (1) | CA2773340C (enExample) |
| IL (1) | IL218498A (enExample) |
| MX (1) | MX348262B (enExample) |
| PH (1) | PH12012500485A1 (enExample) |
| RU (1) | RU2600736C2 (enExample) |
| SG (1) | SG179026A1 (enExample) |
| WO (1) | WO2011031350A1 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9493477B2 (en) * | 2009-09-08 | 2016-11-15 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof |
| US20110262355A1 (en) | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
| EP2560489A4 (en) * | 2010-04-21 | 2014-01-22 | Signature Therapeutics Inc | COMPOSITIONS WITH ENZYMSPALTBAR OPIOID PRODRUGS AND HEMMER FOR THIS |
| US20130059914A1 (en) | 2010-04-21 | 2013-03-07 | Signature Therapeutics, Inc. | Compositions Comprising Enzyme-Cleavable Amphetamine Prodrugs and Inhibitors Thereof |
| CA2798884C (en) | 2010-05-10 | 2016-09-13 | Euro-Celtique S.A. | Manufacturing of active-free granules and tablets comprising the same |
| MX347105B (es) | 2010-05-10 | 2017-04-12 | Euro Celtique Sa | Composiciones farmaceuticas que comprenden hidromorfona y naloxona. |
| CA2798885C (en) | 2010-05-10 | 2014-11-18 | Euro-Celtique S.A. | Combination of active loaded granules with additional actives |
| BR112013017296B1 (pt) | 2011-01-11 | 2021-02-17 | Signature Therapeutics, Inc. | composto e composição compreendendo oxicodona, método para reduzir o abuso potencial da referida composição, unidade de dose e método para a sua preparação, e método para identificar um composto e um inibidor de tripsina |
| US8685916B2 (en) | 2011-03-09 | 2014-04-01 | Signature Therapeutics, Inc. | Opioid prodrugs with heterocyclic linkers |
| JP6148182B2 (ja) | 2011-03-09 | 2017-06-14 | シグネーチャー セラピューティクス, インク.Signature Therapeutics, Inc. | 複素環式リンカーを有する活性薬剤プロドラッグ |
| EP2760844B1 (fr) * | 2011-09-29 | 2018-11-21 | Ecole Normale Superieure De Lyon | Substrat de peptidase fluorogene |
| KR101589846B1 (ko) | 2011-10-26 | 2016-01-28 | 켐팜 인코포레이티드 | 히드로모르폰의 벤조산, 벤조산 유도체 및 헤테로아릴 카르복실산 컨쥬게이트, 전구약물, 이의 제조 방법 및 용도 |
| EP3068397A1 (en) | 2013-11-13 | 2016-09-21 | Euro-Celtique S.A. | Hydromorphone and naloxone for treatment of pain and opioid bowel dysfunction syndrome |
| EP3077008B1 (en) | 2013-12-06 | 2023-10-04 | Jie Han | Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs |
| BR112017011764A2 (pt) | 2014-12-02 | 2018-07-10 | Kempharm, Inc. | ácido benzóico, derivados de ácido benzóico e conjugados de ácido heteroaril carboxílico de oximorfona, pro-fármacos, métodos e preparação e uso dos mesmos |
| PT3713939T (pt) * | 2017-11-24 | 2021-09-16 | Byondis Bv | Processo melhorado para a síntese de fármaco ligante vcseco- duba |
| US10807995B2 (en) | 2018-07-13 | 2020-10-20 | Alkermes Pharma Ireland Limited | Thienothiophene compounds for long-acting injectable compositions and related methods |
| US10799496B2 (en) | 2018-07-13 | 2020-10-13 | Alkermes Pharma Ireland Limited | Naphthylenyl compounds for long-acting injectable compositions and related methods |
| US10717712B2 (en) * | 2018-07-27 | 2020-07-21 | Concentric Analgesics, Inc. | Pegylated prodrugs of phenolic TRPV1 agonists |
| US10975099B2 (en) | 2018-11-05 | 2021-04-13 | Alkermes Pharma Ireland Limited | Thiophene compounds for long-acting injectable compositions and related methods |
| CN113624665A (zh) * | 2021-07-30 | 2021-11-09 | 中国药科大学 | 一种抗肿瘤候选化合物在治疗结直肠癌药物中的应用及测定方法 |
| CA3230025A1 (en) | 2021-09-29 | 2023-04-06 | Lynn Kirkpatrick | Enzyme-cleavable methadone prodrugs and methods of use thereof |
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| KR20000005312A (ko) | 1996-04-10 | 2000-01-25 | 오노 야꾸힝 고교 가부시키가이샤 | 트립타아제 억제제 및 신규 구아니디노 유도체 |
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| 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 |
| US9493477B2 (en) * | 2009-09-08 | 2016-11-15 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof |
| EP2560489A4 (en) * | 2010-04-21 | 2014-01-22 | Signature Therapeutics Inc | COMPOSITIONS WITH ENZYMSPALTBAR OPIOID PRODRUGS AND HEMMER FOR THIS |
| US20110262360A1 (en) | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions Comprising Enzyme-Cleavable Phenol-Modified Opioid Prodrugs and Inhibitors Thereof |
| EP2560491A1 (en) | 2010-04-21 | 2013-02-27 | Signature Therapeutics, Inc. | Peripheral opioid agonists and peripheral opioid antagonists |
| US20110262355A1 (en) * | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
| BR112013017296B1 (pt) * | 2011-01-11 | 2021-02-17 | Signature Therapeutics, Inc. | composto e composição compreendendo oxicodona, método para reduzir o abuso potencial da referida composição, unidade de dose e método para a sua preparação, e método para identificar um composto e um inibidor de tripsina |
| US8497237B2 (en) * | 2011-01-11 | 2013-07-30 | 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 |
| JP6148182B2 (ja) * | 2011-03-09 | 2017-06-14 | シグネーチャー セラピューティクス, インク.Signature Therapeutics, Inc. | 複素環式リンカーを有する活性薬剤プロドラッグ |
-
2010
- 2010-04-21 US US13/393,470 patent/US9493477B2/en active Active
- 2010-04-21 BR BR112012005124-5A patent/BR112012005124B1/pt active IP Right Grant
- 2010-04-21 PH PH1/2012/500485A patent/PH12012500485A1/en unknown
- 2010-04-21 JP JP2012527871A patent/JP2013503862A/ja active Pending
- 2010-04-21 EP EP10815769.4A patent/EP2475429B1/en active Active
- 2010-04-21 RU RU2012108874/04A patent/RU2600736C2/ru active
- 2010-04-21 SG SG2012016036A patent/SG179026A1/en unknown
- 2010-04-21 AU AU2010293028A patent/AU2010293028B2/en active Active
- 2010-04-21 MX MX2012002847A patent/MX348262B/es active IP Right Grant
- 2010-04-21 CA CA2773340A patent/CA2773340C/en active Active
- 2010-04-21 CN CN201080048158.6A patent/CN102695545B/zh active Active
- 2010-04-21 WO PCT/US2010/031956 patent/WO2011031350A1/en not_active Ceased
-
2012
- 2012-03-06 IL IL218498A patent/IL218498A/en active IP Right Grant
-
2015
- 2015-09-29 JP JP2015190867A patent/JP2016041698A/ja active Pending
-
2016
- 2016-10-05 US US15/285,818 patent/US10028945B2/en active Active
-
2018
- 2018-05-25 JP JP2018100108A patent/JP6778234B2/ja active Active
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