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 (cg-RX-API-DMAC7.html) | 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 (cg-RX-API-DMAC7.html) |
| EP (2) | EP2340044A1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP5827123B2 (cg-RX-API-DMAC7.html) |
| KR (1) | KR101660996B1 (cg-RX-API-DMAC7.html) |
| CN (1) | CN102159249A (cg-RX-API-DMAC7.html) |
| AU (1) | AU2009292631A1 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2734333A1 (cg-RX-API-DMAC7.html) |
| IL (1) | IL211762A (cg-RX-API-DMAC7.html) |
| MX (1) | MX347741B (cg-RX-API-DMAC7.html) |
| WO (1) | WO2010033195A1 (cg-RX-API-DMAC7.html) |
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 |
| EP1623703B1 (en) | 1999-10-29 | 2011-10-05 | Euro-Celtique S.A. | Controlled release hydrocodone formulations |
| HU230875B1 (hu) | 2000-10-30 | 2018-11-29 | Euro-Celtique S.A. | Szabályozott hatóanyag-leadású hidrokodon készítmények |
| 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 |
| EP2628489B1 (en) * | 2009-07-21 | 2017-03-01 | Nektar Therapeutics | PEG oligomer-fentanyl conjugates |
| US20130023553A1 (en) * | 2010-01-12 | 2013-01-24 | Nektar Therapeutics | Pegylated opioids with low potential for abuse and side effects |
| US9993433B2 (en) | 2010-05-10 | 2018-06-12 | Euro-Celtique S.A. | Manufacturing of active-free granules and tablets comprising the same |
| WO2011143120A1 (en) | 2010-05-11 | 2011-11-17 | Cima Labs Inc. | Alcoholres i stant metoprolol - containing extended - release oral dosage forms |
| KR102016305B1 (ko) | 2011-11-07 | 2019-08-30 | 넥타르 테라퓨틱스 | 오피오이드 작용제 화합물 및 진통제 화합물의 조성물, 투여형 및 공동 투여 |
| 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 |
| WO2014043707A1 (en) * | 2012-09-17 | 2014-03-20 | Nektar Therapeutics | Oligomer-containing benzamide-based compounds |
| EP3327022A1 (en) | 2012-10-30 | 2018-05-30 | Nektar Therapeutics | Solid salt form of alpha-6-mpeg6-o-hydroxycodone as opioid agonists and uses thereof |
| CA2881144A1 (en) * | 2012-11-09 | 2014-05-09 | Purdue Pharma | Pharmaceutical compositions comprising hydromorphone and naloxone |
| JP6577943B2 (ja) * | 2013-06-28 | 2019-09-18 | ネクター セラピューティクス | κオピオイド作動薬及びその使用 |
| CA2919892C (en) | 2013-08-12 | 2019-06-18 | 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 |
| EA030310B1 (ru) | 2013-11-13 | 2018-07-31 | Эро-Селтик С.А. | Гидроморфон и налоксон для лечения боли и индуцированного опиоидами синдрома дисфункции кишечника |
| US9492444B2 (en) | 2013-12-17 | 2016-11-15 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| WO2015095391A1 (en) | 2013-12-17 | 2015-06-25 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| DK3169315T3 (da) | 2014-07-17 | 2020-08-10 | Pharmaceutical Manufacturing Res Services In | Væskefyldt doseringsform til forhindring af misbrug med øjeblikkelig frigivelse |
| JP2017531026A (ja) | 2014-10-20 | 2017-10-19 | ファーマシューティカル マニュファクチュアリング リサーチ サービシズ，インコーポレーテッド | 徐放性乱用抑止性液体充填剤形 |
| US11066366B2 (en) | 2015-09-03 | 2021-07-20 | 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 |
| US11254685B2 (en) * | 2017-07-20 | 2022-02-22 | Suzhou Runxindatai Pharmaceutics Ltd Co. | Abuse-resistant long-acting release opioid prodrugs |
| JP7177392B2 (ja) | 2018-03-29 | 2022-11-24 | 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 |
| US20220062200A1 (en) | 2019-05-07 | 2022-03-03 | Clexio Biosciences Ltd. | Abuse-deterrent dosage forms containing esketamine |
| WO2020225773A1 (en) | 2019-05-07 | 2020-11-12 | 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 |
Family Cites Families (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2628962A (en) * | 1949-10-20 | 1953-02-17 | Mallinckrodt Chemical Works | Method for preparing dihydrocodeinone, dihydromorphinone, and codeinone |
| US2654756A (en) | 1949-10-20 | 1953-10-06 | Mallinckrodt Chemical Works | Process of preparing codeinone, dihydrocodeinone, and dihydromorphinone |
| 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 |
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| 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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| 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 |
| DE10025946A1 (de) * | 2000-05-26 | 2001-11-29 | Gruenenthal Gmbh | Wirkstoffkombination |
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| US20020106331A1 (en) * | 2000-12-08 | 2002-08-08 | Joan Rosell | Use of electrolytes (ions in solution) to suppress charging of inhalation aerosols |
| JP4850346B2 (ja) * | 2001-03-15 | 2012-01-11 | 救急薬品工業株式会社 | 粘膜貼付剤 |
| US6835802B2 (en) | 2001-06-04 | 2004-12-28 | Nobex Corporation | Methods of synthesizing substantially monodispersed mixtures of polymers having polyethylene glycol moieties |
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| DE60219124T2 (de) * | 2001-11-16 | 2008-01-31 | Randox Laboratories Ltd., Crumlin | Verfahren und Kit zum Nachweis, oder zum Quantifizieren von, Metaboliten von Fentanyl und Metaboliten von Fentanyl Analoga |
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| TW200500067A (en) * | 2003-01-21 | 2005-01-01 | Control Delivery Sys Inc | Salts of codrugs and uses related thereto |
| EP1782834A3 (en) * | 2003-03-13 | 2007-08-01 | Controlled Chemicals, Inc. | Oxycodone conjugates with lower abuse potential and extended duration of action |
| MXPA05009757A (es) * | 2003-03-13 | 2005-12-05 | Controlled Chemicals Inc | Conjugados de oxicodona con menor potencial de abuso y duracion de accion extendida. |
| US20060009478A1 (en) * | 2003-10-15 | 2006-01-12 | Nadav Friedmann | Methods for the treatment of back pain |
| US20060182692A1 (en) * | 2003-12-16 | 2006-08-17 | Fishburn C S | Chemically modified small molecules |
| CN1925875A (zh) * | 2003-12-16 | 2007-03-07 | 尼克塔治疗亚拉巴马公司 | 化学改性的小分子 |
| MXPA06011972A (es) * | 2004-04-13 | 2007-04-16 | Johnson & Johnson | Aparato y metodo para el suministro transdermico de agentes a base de fentanilo. |
| AU2005283326B2 (en) * | 2004-09-13 | 2011-07-21 | Ono Pharmaceutical Co., Ltd. | Nitrogenous heterocyclic derivative and medicine containing the same as an active ingredient |
| 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 |
| US20070083186A1 (en) * | 2005-09-30 | 2007-04-12 | Darrick Carter | Transdermal drug delivery systems, devices, and methods employing novel pharmaceutical vehicles |
| CA2646313C (en) * | 2006-04-21 | 2014-05-20 | Nektar Therapeutics Al, Corporation | Stereoselective reduction of a morphinone |
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| US20080066739A1 (en) * | 2006-09-20 | 2008-03-20 | Lemahieu Edward | Methods and systems of delivering medication via inhalation |
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| CN101534827A (zh) * | 2006-11-07 | 2009-09-16 | 尼克塔治疗亚拉巴马公司 | 阿片样物质激动剂和阿片样物质拮抗剂的剂型和联合给药 |
| EP2129683A4 (en) * | 2007-02-26 | 2011-01-05 | Ironwood Pharmaceuticals Inc | METHODS AND COMPOSITIONS FOR TREATMENT OF HEART FAILURE AND OTHER DISORDERS |
| EP2134371B1 (en) * | 2007-03-12 | 2015-01-14 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
| US8173666B2 (en) * | 2007-03-12 | 2012-05-08 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
| WO2009094209A1 (en) * | 2008-01-25 | 2009-07-30 | Nektar Therapeutics Al, Corporation | Oligomer-diarylpiperazine conjugates |
| WO2009120889A2 (en) * | 2008-03-26 | 2009-10-01 | Alltranz Inc. | Abuse deterrent transdermal formulations of opiate agonists and agonist-antagonists |
| WO2009151590A2 (en) * | 2008-06-09 | 2009-12-17 | Nektar Therapeutics | Methods of treating cyp2d6 alternative metabolizers |
| US20100016365A1 (en) * | 2008-07-17 | 2010-01-21 | Auspex Pharmaceuticals, Inc. | Substituted 4-amino-piperidines |
| JP5539991B2 (ja) * | 2008-09-18 | 2014-07-02 | パーデュー、ファーマ、リミテッド、パートナーシップ | ポリ（ε−カプロラクトン）を含む医薬剤形 |
| US20130023553A1 (en) * | 2010-01-12 | 2013-01-24 | Nektar Therapeutics | Pegylated opioids with low potential for abuse and side effects |
-
2009
- 2009-09-16 WO PCT/US2009/005174 patent/WO2010033195A1/en not_active Ceased
- 2009-09-16 EP EP09789323A patent/EP2340044A1/en not_active Withdrawn
- 2009-09-16 JP JP2011526872A patent/JP5827123B2/ja not_active Expired - Fee Related
- 2009-09-16 EP EP17198484.2A patent/EP3342427A1/en not_active Withdrawn
- 2009-09-16 CN CN2009801360891A patent/CN102159249A/zh active Pending
- 2009-09-16 US US13/063,919 patent/US20110237614A1/en not_active Abandoned
- 2009-09-16 MX MX2011002748A patent/MX347741B/es active IP Right Grant
- 2009-09-16 CA CA2734333A patent/CA2734333A1/en not_active Abandoned
- 2009-09-16 AU AU2009292631A patent/AU2009292631A1/en not_active Abandoned
- 2009-09-16 KR KR1020117004392A patent/KR101660996B1/ko not_active Expired - Fee Related
-
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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