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
Links
- 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 (https=) | 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 (https=) |
| EP (1) | EP2475429B1 (https=) |
| JP (3) | JP2013503862A (https=) |
| CN (1) | CN102695545B (https=) |
| AU (1) | AU2010293028B2 (https=) |
| BR (1) | BR112012005124B1 (https=) |
| CA (1) | CA2773340C (https=) |
| IL (1) | IL218498A (https=) |
| MX (1) | MX348262B (https=) |
| PH (1) | PH12012500485A1 (https=) |
| RU (1) | RU2600736C2 (https=) |
| SG (1) | SG179026A1 (https=) |
| WO (1) | WO2011031350A1 (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112012005124B1 (pt) * | 2009-09-08 | 2021-11-09 | Signature Therapeutics, Inc. | Pro-fármaco de opioide modificado por cetona, seu método de preparação, sua composição farmacêutica, sua unidade de dose, métodos e usos |
| US20110262355A1 (en) | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
| US20130059914A1 (en) | 2010-04-21 | 2013-03-07 | Signature Therapeutics, Inc. | Compositions Comprising Enzyme-Cleavable Amphetamine Prodrugs and Inhibitors Thereof |
| CA2795222A1 (en) * | 2010-04-21 | 2011-10-27 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable opioid 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 |
| CN103002881B (zh) | 2010-05-10 | 2015-09-02 | 欧洲凯尔特公司 | 载有活性剂的颗粒与额外活性剂的组合 |
| AU2011252039B2 (en) | 2010-05-10 | 2014-06-12 | Euro-Celtique S.A. | Pharmaceutical compositions comprising hydromorphone and naloxone |
| ES2584634T3 (es) * | 2011-01-11 | 2016-09-28 | Signature Therapeutics, Inc. | Composiciones que comprenden un profármaco de oxicodona escindible enzimáticamente |
| AU2012225337B2 (en) | 2011-03-09 | 2016-04-28 | Signature Therapeutics, Inc. | Active agent prodrugs with heterocyclic linkers |
| WO2012122420A2 (en) | 2011-03-09 | 2012-09-13 | Pharmacofore, Inc. | Opioid prodrugs with heterocyclic linkers |
| WO2013045854A1 (fr) * | 2011-09-29 | 2013-04-04 | Ecole Normale Superieure De Lyon | Substrat de peptidase fluorogene |
| JP5769889B2 (ja) | 2011-10-26 | 2015-08-26 | ケムファーム・インコーポレーテッド | ヒドロモルホンの安息香酸、安息香酸誘導体及びヘテロアリールカルボン酸結合体、そのプロドラッグ、製造法及び使用 |
| WO2015071380A1 (en) | 2013-11-13 | 2015-05-21 | Euro-Celtique S.A. | Hydromorphone and naloxone for treatment of pain and opioid bowel dysfunction syndrome |
| CN112043835B (zh) | 2013-12-06 | 2022-10-21 | 韩捷 | 用于含氮和羟基的药物的生物可逆引入基团 |
| MA40937A (fr) | 2014-12-02 | 2017-10-11 | Kempharm Inc | Acide benzoïque, dérivés d'acide benzoïque et conjugués d'acide hétéroarylcarboxylique d'oxymorphone, promédicaments, leurs procédés de fabrication et d'utilisation |
| WO2019101850A1 (en) * | 2017-11-24 | 2019-05-31 | Synthon Biopharmaceuticals B.V. | Improved process for the synthesis of linker-drug vc-seco-duba |
| US10807995B2 (en) | 2018-07-13 | 2020-10-20 | Alkermes Pharma Ireland Limited | Thienothiophene compounds for long-acting injectable compositions and related methods |
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| 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 |
| US12599578B2 (en) | 2021-03-09 | 2026-04-14 | Ensysce Biosciences Inc. | Compositions comprising enzyme-cleavable prodrugs and controlled release nafamostat and methods of use thereof |
| 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 |
| MX2024003466A (es) | 2021-09-29 | 2024-06-04 | Ensysce Biosciences Inc | Profarmacos de metadona escindibles por enzimas y metodos de uso de los mismos. |
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| US20110262355A1 (en) * | 2010-04-21 | 2011-10-27 | Jenkins Thomas E | Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof |
| ES2584634T3 (es) * | 2011-01-11 | 2016-09-28 | Signature Therapeutics, Inc. | Composiciones que comprenden un profármaco de oxicodona escindible enzimáticamente |
| WO2012096886A1 (en) * | 2011-01-11 | 2012-07-19 | Signature Therapeutics, Inc. | Compositions comprising enzyme-cleavable oxycodone prodrug |
| AU2012225337B2 (en) * | 2011-03-09 | 2016-04-28 | Signature Therapeutics, Inc. | Active agent prodrugs with heterocyclic linkers |
| WO2012122420A2 (en) * | 2011-03-09 | 2012-09-13 | Pharmacofore, Inc. | Opioid prodrugs with heterocyclic linkers |
-
2010
- 2010-04-21 BR BR112012005124-5A patent/BR112012005124B1/pt active IP Right Grant
- 2010-04-21 CA CA2773340A patent/CA2773340C/en active Active
- 2010-04-21 EP EP10815769.4A patent/EP2475429B1/en active Active
- 2010-04-21 MX MX2012002847A patent/MX348262B/es active IP Right Grant
- 2010-04-21 WO PCT/US2010/031956 patent/WO2011031350A1/en not_active Ceased
- 2010-04-21 PH PH1/2012/500485A patent/PH12012500485A1/en unknown
- 2010-04-21 US US13/393,470 patent/US9493477B2/en active Active
- 2010-04-21 JP JP2012527871A patent/JP2013503862A/ja active Pending
- 2010-04-21 CN CN201080048158.6A patent/CN102695545B/zh active Active
- 2010-04-21 SG SG2012016036A patent/SG179026A1/en unknown
- 2010-04-21 RU RU2012108874/04A patent/RU2600736C2/ru active
- 2010-04-21 AU AU2010293028A patent/AU2010293028B2/en active Active
-
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