JP2012502904A5 - - Google Patents
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- Publication number
- JP2012502904A5 JP2012502904A5 JP2011526872A JP2011526872A JP2012502904A5 JP 2012502904 A5 JP2012502904 A5 JP 2012502904A5 JP 2011526872 A JP2011526872 A JP 2011526872A JP 2011526872 A JP2011526872 A JP 2011526872A JP 2012502904 A5 JP2012502904 A5 JP 2012502904A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- poly
- opioid
- less
- compound according
- 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 description 84
- 229940002612 prodrug Drugs 0.000 claims description 21
- 239000000651 prodrug Substances 0.000 claims description 21
- 230000008499 blood brain barrier function Effects 0.000 claims description 14
- 210000001218 blood-brain barrier Anatomy 0.000 claims description 14
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 12
- 238000009825 accumulation Methods 0.000 claims description 10
- 229920001223 polyethylene glycol Polymers 0.000 claims description 10
- 239000000841 delta opiate receptor agonist Substances 0.000 claims description 9
- 239000002632 kappa opiate receptor agonist Substances 0.000 claims description 9
- 239000002756 mu opiate receptor agonist Substances 0.000 claims description 9
- 238000000034 method Methods 0.000 claims description 7
- 230000001268 conjugating effect Effects 0.000 claims description 6
- 239000003814 drug Substances 0.000 claims description 6
- 241000124008 Mammalia Species 0.000 claims description 5
- 210000003169 central nervous system Anatomy 0.000 claims description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 5
- 229940127450 Opioid Agonists Drugs 0.000 claims description 4
- 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
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- 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 4
- 239000003402 opiate agonist Substances 0.000 claims description 4
- 238000002560 therapeutic procedure Methods 0.000 claims description 4
- USSIQXCVUWKGNF-UHFFFAOYSA-N 6-(dimethylamino)-4,4-diphenylheptan-3-one Chemical compound C=1C=CC=CC=1C(CC(C)N(C)C)(C(=O)CC)C1=CC=CC=C1 USSIQXCVUWKGNF-UHFFFAOYSA-N 0.000 claims description 2
- 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 description 2
- UQCNKQCJZOAFTQ-ISWURRPUSA-N Oxymorphone Chemical compound O([C@H]1C(CC[C@]23O)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O UQCNKQCJZOAFTQ-ISWURRPUSA-N 0.000 claims description 2
- 239000002202 Polyethylene glycol Substances 0.000 claims description 2
- 229960004126 codeine Drugs 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- PJMPHNIQZUBGLI-UHFFFAOYSA-N fentanyl Chemical compound C=1C=CC=CC=1N(C(=O)CC)C(CC1)CCN1CCC1=CC=CC=C1 PJMPHNIQZUBGLI-UHFFFAOYSA-N 0.000 claims description 2
- 229960002428 fentanyl Drugs 0.000 claims description 2
- OROGSEYTTFOCAN-UHFFFAOYSA-N hydrocodone Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OC OROGSEYTTFOCAN-UHFFFAOYSA-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
- 229960001410 hydromorphone Drugs 0.000 claims description 2
- 229960001797 methadone Drugs 0.000 claims description 2
- 229960005181 morphine Drugs 0.000 claims description 2
- 229960002085 oxycodone Drugs 0.000 claims description 2
- 229960005118 oxymorphone Drugs 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19224708P | 2008-09-16 | 2008-09-16 | |
| US61/192,247 | 2008-09-16 | ||
| US12/558,395 | 2009-09-11 | ||
| US12/558,395 US8173666B2 (en) | 2007-03-12 | 2009-09-11 | Oligomer-opioid agonist conjugates |
| PCT/US2009/005174 WO2010033195A1 (en) | 2008-09-16 | 2009-09-16 | Pegylated opioids with low potential for abuse |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012502904A JP2012502904A (ja) | 2012-02-02 |
| JP2012502904A5 true JP2012502904A5 (enExample) | 2012-11-08 |
| JP5827123B2 JP5827123B2 (ja) | 2015-12-02 |
Family
ID=41611345
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011526872A Expired - Fee Related JP5827123B2 (ja) | 2008-09-16 | 2009-09-16 | 乱用の可能性が低いｐｅｇ化オピオイド |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US20110237614A1 (enExample) |
| EP (2) | EP3342427A1 (enExample) |
| JP (1) | JP5827123B2 (enExample) |
| KR (1) | KR101660996B1 (enExample) |
| CN (1) | CN102159249A (enExample) |
| AU (1) | AU2009292631A1 (enExample) |
| CA (1) | CA2734333A1 (enExample) |
| IL (1) | IL211762A (enExample) |
| MX (1) | MX347741B (enExample) |
| WO (1) | WO2010033195A1 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10179130B2 (en) | 1999-10-29 | 2019-01-15 | Purdue Pharma L.P. | Controlled release hydrocodone formulations |
| EP2295043A1 (en) | 1999-10-29 | 2011-03-16 | Euro-Celtique S.A. | Controlled release hydrocodone formulations |
| EP2932964A1 (en) | 2000-10-30 | 2015-10-21 | Euro-Celtique S.A. | Controlled release hydrocodone formulations |
| US20080069891A1 (en) | 2006-09-15 | 2008-03-20 | Cima Labs, Inc. | Abuse resistant drug formulation |
| US8445018B2 (en) | 2006-09-15 | 2013-05-21 | Cima Labs Inc. | Abuse resistant drug formulation |
| US8173666B2 (en) | 2007-03-12 | 2012-05-08 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
| US10512644B2 (en) | 2007-03-12 | 2019-12-24 | Inheris Pharmaceuticals, Inc. | Oligomer-opioid agonist conjugates |
| CA2768392C (en) * | 2009-07-21 | 2018-04-17 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
| US20130023553A1 (en) * | 2010-01-12 | 2013-01-24 | Nektar Therapeutics | Pegylated opioids with low potential for abuse and side effects |
| CA2798884C (en) | 2010-05-10 | 2016-09-13 | Euro-Celtique S.A. | Manufacturing of active-free granules and tablets comprising the same |
| JP2013526523A (ja) | 2010-05-11 | 2013-06-24 | シマ ラブス インク． | メトプロロールを含むアルコール耐性持続放出性経口剤形 |
| US10525054B2 (en) | 2011-11-07 | 2020-01-07 | Inheris Biopharma, Inc. | Compositions, dosage forms, and co-administration of an opioid agonist compound and an analgesic compound |
| AU2012336030B2 (en) | 2011-11-07 | 2017-09-14 | Nektar Therapeutics | Compositions, dosage forms, and coadministration of an opioid agonist compound and an analgesic compound |
| EP2895457B1 (en) | 2012-09-17 | 2020-05-20 | Nektar Therapeutics | Oligomer-containing benzamide-based compounds |
| MX367773B (es) | 2012-10-30 | 2019-09-05 | Nektar Therapeutics | Forma salina sólida de la alfa-6-mpeg6-o-hidroxicodona como agonistas opioides y sus usos. |
| CA2881144A1 (en) * | 2012-11-09 | 2014-05-09 | Purdue Pharma | Pharmaceutical compositions comprising hydromorphone and naloxone |
| US9815824B2 (en) * | 2013-06-28 | 2017-11-14 | Nektar Therapeutics | Kappa opioid agonists and uses thereof |
| CA3042642A1 (en) | 2013-08-12 | 2015-02-19 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded immediate release abuse deterrent pill |
| US20150118300A1 (en) | 2013-10-31 | 2015-04-30 | Cima Labs Inc. | Immediate Release Abuse-Deterrent Granulated Dosage Forms |
| EP3068397A1 (en) | 2013-11-13 | 2016-09-21 | Euro-Celtique S.A. | Hydromorphone and naloxone for treatment of pain and opioid bowel dysfunction syndrome |
| WO2015095391A1 (en) | 2013-12-17 | 2015-06-25 | 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 |
| EP3169315B1 (en) | 2014-07-17 | 2020-06-24 | Pharmaceutical Manufacturing Research Services, Inc. | Immediate release abuse deterrent liquid fill dosage form |
| WO2016064873A1 (en) | 2014-10-20 | 2016-04-28 | Pharmaceutical Manufacturing Research Services, Inc. | Extended release abuse deterrent liquid fill dosage form |
| WO2017041095A1 (en) | 2015-09-03 | 2017-03-09 | Allegheny-Singer Research Institute | Hydrophilic fentanyl derivatives |
| CN107019803B (zh) * | 2016-01-29 | 2020-09-15 | 北京键凯科技股份有限公司 | 具有低成瘾作用的聚乙二醇化阿片样物质 |
| CN107033154B (zh) * | 2016-02-02 | 2020-02-04 | 上海瀚迈生物医药科技有限公司 | 阿片受体拮抗剂缀合物及其应用 |
| CN108210933B (zh) * | 2016-12-22 | 2021-05-04 | 北京键凯科技股份有限公司 | 一种地佐辛与聚乙二醇的结合物 |
| JP7369687B2 (ja) * | 2017-07-20 | 2023-10-26 | スーチョウ ランシンダタイ ファーマシューティクス エルティーディー シーオー． | 乱用防止長期作用型徐放性オピオイドプロドラッグ |
| WO2019189188A1 (ja) | 2018-03-29 | 2019-10-03 | 日油株式会社 | トリチル基含有単分散ポリエチレングリコールの精製方法 |
| WO2020225773A1 (en) | 2019-05-07 | 2020-11-12 | Clexio Biosciences Ltd. | Abuse-deterrent dosage forms containing esketamine |
| US20220062200A1 (en) | 2019-05-07 | 2022-03-03 | Clexio Biosciences Ltd. | Abuse-deterrent dosage forms containing esketamine |
| CN115181109B (zh) * | 2021-04-02 | 2024-06-04 | 南京正大天晴制药有限公司 | 吗啡喃衍生物的晶体及其制备方法 |
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| US2654756A (en) * | 1949-10-20 | 1953-10-06 | Mallinckrodt Chemical Works | Process of preparing codeinone, dihydrocodeinone, and dihydromorphinone |
| US2628962A (en) * | 1949-10-20 | 1953-02-17 | Mallinckrodt Chemical Works | Method for preparing dihydrocodeinone, dihydromorphinone, and codeinone |
| US2715626A (en) * | 1950-07-05 | 1955-08-16 | Merck & Co Inc | Process of preparing dihydrocodeinone |
| US2649454A (en) | 1951-08-20 | 1953-08-18 | Univ California | Method for preparing dihydromorphinone, dihydrocodeinone, and dihydropseudocodeinone |
| US2806033A (en) | 1955-08-03 | 1957-09-10 | Lewenstein | Morphine derivative |
| US3254088A (en) * | 1961-03-14 | 1966-05-31 | Lewenstein | Morphine derivative |
| JPS60149589A (ja) * | 1984-01-14 | 1985-08-07 | Daiichi Rajio Isotope Kenkyusho:Kk | クラウン化コデイノン類 |
| US5843900A (en) * | 1991-04-01 | 1998-12-01 | Cortech, Inc. | Bradykinin antagonists |
| DE4132159A1 (de) * | 1991-09-27 | 1993-04-01 | Boehringer Ingelheim Kg | 14-hydroxy-n-(2-methoxyethyl)-7,8-dihydromorphin und -norisomorphin, verfahren zu deren herstellung und deren verwendung als arzneimittel |
| US5428159A (en) * | 1994-04-08 | 1995-06-27 | Ciba-Geigy Corporation | Method of manufacture of (-)-galanthamine in high yield and purity substantially free of epigalanthamine |
| US5672662A (en) | 1995-07-07 | 1997-09-30 | Shearwater Polymers, Inc. | Poly(ethylene glycol) and related polymers monosubstituted with propionic or butanoic acids and functional derivatives thereof for biotechnical applications |
| US6004577A (en) * | 1997-08-12 | 1999-12-21 | Murdock; Thomas O. | Enhanced electrotransport of therapeutic agents having polybasic anionic counter ions |
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| WO2001024831A2 (en) * | 1999-10-04 | 2001-04-12 | Shearwater Corporation | Polymer stabilized neuropeptides |
| US20050233459A1 (en) * | 2003-11-26 | 2005-10-20 | Melker Richard J | Marker detection method and apparatus to monitor drug compliance |
| US7049326B2 (en) * | 2000-05-12 | 2006-05-23 | The University Of Toledo | Method and compositions for temporarily incapacitating subjects |
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| US7338939B2 (en) * | 2003-09-30 | 2008-03-04 | New River Pharmaceuticals Inc. | Abuse-resistant hydrocodone compounds |
| DK2939696T3 (en) * | 2001-10-18 | 2016-05-23 | Nektar Therapeutics | Polymer Conjugates of Opioid Antagonists |
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| FR2832311B1 (fr) * | 2001-11-21 | 2004-04-16 | Besins Int Belgique | Poudre filmogene, compositions la comprenant, leurs procedes de preparation et leurs utilisations |
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| PE20060598A1 (es) * | 2004-09-13 | 2006-08-21 | Ono Pharmaceutical Co | Derivado heterociclo conteniendo nitrogeno como antagonista de quimiocina ccr5 |
| WO2006126529A1 (ja) * | 2005-05-25 | 2006-11-30 | Shionogi & Co., Ltd. | ６，７－不飽和－７－カルバモイル置換モルヒナン誘導体 |
| EP1931417A2 (en) * | 2005-09-30 | 2008-06-18 | Transcutaneous Technologies Inc. | Transdermal drug delivery systems, devices, and methods employing novel pharmaceutical vehicles |
| EP2010539B1 (en) * | 2006-04-21 | 2017-06-14 | Nektar Therapeutics | Stereoselective reduction of a morphinone |
| KR20090031519A (ko) * | 2006-05-26 | 2009-03-26 | 파마코포어, 인크. | 페놀계 오피오이드의 제어 방출 |
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| JP2010509227A (ja) * | 2006-11-07 | 2010-03-25 | ネクター セラピューティックス エイエル，コーポレイション | オピオイド作動薬およびオピオイド拮抗薬の用量形態および同時投与 |
| EP2650303A1 (en) * | 2007-02-26 | 2013-10-16 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of heart failure and other disorders |
| US8173666B2 (en) * | 2007-03-12 | 2012-05-08 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
| EP2134371B1 (en) * | 2007-03-12 | 2015-01-14 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
| WO2009094209A1 (en) * | 2008-01-25 | 2009-07-30 | Nektar Therapeutics Al, Corporation | Oligomer-diarylpiperazine conjugates |
| JP2011515495A (ja) * | 2008-03-26 | 2011-05-19 | オールトランツ インコーポレイティド | オピエートアゴニスト及びアゴニスト−アンタゴニストの乱用抑制経皮製剤 |
| US11033631B2 (en) * | 2008-06-09 | 2021-06-15 | Nektar Therapeutics | Methods of treating CYP2D6 alternative metabolizers |
| US20100016365A1 (en) * | 2008-07-17 | 2010-01-21 | Auspex Pharmaceuticals, Inc. | Substituted 4-amino-piperidines |
| CN102159193B (zh) * | 2008-09-18 | 2015-09-16 | 普渡制药公司 | 包含聚(ε-己内酯)的药物剂型 |
| US20130023553A1 (en) * | 2010-01-12 | 2013-01-24 | Nektar Therapeutics | Pegylated opioids with low potential for abuse and side effects |
-
2009
- 2009-09-16 AU AU2009292631A patent/AU2009292631A1/en not_active Abandoned
- 2009-09-16 WO PCT/US2009/005174 patent/WO2010033195A1/en not_active Ceased
- 2009-09-16 KR KR1020117004392A patent/KR101660996B1/ko not_active Expired - Fee Related
- 2009-09-16 JP JP2011526872A patent/JP5827123B2/ja not_active Expired - Fee Related
- 2009-09-16 US US13/063,919 patent/US20110237614A1/en not_active Abandoned
- 2009-09-16 EP EP17198484.2A patent/EP3342427A1/en not_active Withdrawn
- 2009-09-16 MX MX2011002748A patent/MX347741B/es active IP Right Grant
- 2009-09-16 EP EP09789323A patent/EP2340044A1/en not_active Withdrawn
- 2009-09-16 CA CA2734333A patent/CA2734333A1/en not_active Abandoned
- 2009-09-16 CN CN2009801360891A patent/CN102159249A/zh active Pending
-
2011
- 2011-03-16 IL IL211762A patent/IL211762A/en active IP Right Grant
-
2016
- 2016-02-18 US US15/047,497 patent/US20160243111A1/en not_active Abandoned
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