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 |
| CN1407884B (zh) | 1999-10-29 | 2012-06-20 | 欧罗赛铁克股份有限公司 | 控释氢可酮制剂 |
| WO2002036099A1 (en) | 2000-10-30 | 2002-05-10 | 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 |
| US10512644B2 (en) | 2007-03-12 | 2019-12-24 | Inheris Pharmaceuticals, Inc. | Oligomer-opioid agonist conjugates |
| US8173666B2 (en) | 2007-03-12 | 2012-05-08 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
| EP2456469A1 (en) * | 2009-07-21 | 2012-05-30 | 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 |
| BR112012028788A2 (pt) | 2010-05-10 | 2016-07-19 | Euro Celtique Sa | fabricação de grânulos sem ativos |
| MX2012012991A (es) | 2010-05-11 | 2012-11-30 | Cima Labs Inc | Formas de dosificacion oral de liberacion prolongada resistentes al alcohol y que contienen metoprolol. |
| AU2012336030B2 (en) * | 2011-11-07 | 2017-09-14 | Nektar Therapeutics | Compositions, dosage forms, and coadministration of an opioid agonist compound and an analgesic compound |
| 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 |
| EP2895457B1 (en) | 2012-09-17 | 2020-05-20 | Nektar Therapeutics | Oligomer-containing benzamide-based compounds |
| HUE038161T2 (hu) | 2012-10-30 | 2018-09-28 | Nektar Therapeutics | Alfa-6-mPEG6-O-hidroxikodon szilárd só formája, mint opioid agonisták, és ezek alkalmazásai |
| CA2881144A1 (en) * | 2012-11-09 | 2014-05-09 | Purdue Pharma | Pharmaceutical compositions comprising hydromorphone and naloxone |
| EP3013812B1 (en) * | 2013-06-28 | 2019-10-16 | Nektar Therapeutics | Kappa opioid agonists and uses thereof |
| JP6539274B2 (ja) | 2013-08-12 | 2019-07-03 | 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 | 押出成形された即放性乱用抑止性丸剤 |
| US20150118300A1 (en) | 2013-10-31 | 2015-04-30 | Cima Labs Inc. | Immediate Release Abuse-Deterrent Granulated Dosage Forms |
| CA2929909C (en) | 2013-11-13 | 2018-08-21 | Euro-Celtique S.A. | Hydromorphone and naloxone for treatment of pain and opioid bowel dysfunction syndrome |
| 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 |
| EP3169315B1 (en) | 2014-07-17 | 2020-06-24 | Pharmaceutical Manufacturing Research Services, Inc. | Immediate release abuse deterrent liquid fill dosage form |
| US20160106737A1 (en) | 2014-10-20 | 2016-04-21 | Pharmaceutical Manufacturing Research Services, Inc. | Extended Release Abuse Deterrent Liquid Fill Dosage Form |
| 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 |
| AU2018302253B2 (en) * | 2017-07-20 | 2023-06-01 | Suzhou Runxindatai Pharmaceutics Ltd Co. | Abuse-resistant long-acting release opioid prodrugs |
| CA3095299A1 (en) | 2018-03-29 | 2019-10-03 | Nof Corporation | Method for purifying trityl group-containing monodispersed polyethylene glycol |
| US11324707B2 (en) | 2019-05-07 | 2022-05-10 | 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 |
Family Cites Families (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US6703381B1 (en) * | 1998-08-14 | 2004-03-09 | Nobex Corporation | Methods for delivery therapeutic compounds across the blood-brain barrier |
| US6395300B1 (en) * | 1999-05-27 | 2002-05-28 | Acusphere, Inc. | Porous drug matrices and methods of manufacture thereof |
| US7919119B2 (en) * | 1999-05-27 | 2011-04-05 | Acusphere, Inc. | Porous drug matrices and methods of manufacture thereof |
| EP1221975B1 (en) * | 1999-10-04 | 2006-12-06 | Nektar Therapeutics Al, 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 |
| DE10025946A1 (de) * | 2000-05-26 | 2001-11-29 | Gruenenthal Gmbh | Wirkstoffkombination |
| US20070258894A1 (en) * | 2000-11-08 | 2007-11-08 | Melker Richard J | System and Method for Real-Time Diagnosis, Treatment, and Therapeutic Drug Monitoring |
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| JP4850346B2 (ja) * | 2001-03-15 | 2012-01-11 | 救急薬品工業株式会社 | 粘膜貼付剤 |
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| US6835802B2 (en) | 2001-06-04 | 2004-12-28 | Nobex Corporation | Methods of synthesizing substantially monodispersed mixtures of polymers having polyethylene glycol moieties |
| CN1514729B (zh) * | 2001-06-05 | 2012-09-05 | 控制释放系统公司 | 缓释的止痛化合物 |
| US7338939B2 (en) * | 2003-09-30 | 2008-03-04 | New River Pharmaceuticals Inc. | Abuse-resistant hydrocodone compounds |
| PT2939696E (pt) * | 2001-10-18 | 2016-06-17 | Nektar Therapeutics | Conjugados poliméricos de antagonistas de opióides |
| ATE358275T1 (de) * | 2001-11-16 | 2007-04-15 | Randox Lab Ltd | Verfahren und kit zum nachweis, oder zum quantifizieren von, metaboliten von fentanyl und metaboliten von fentanyl analoga |
| FR2832311B1 (fr) * | 2001-11-21 | 2004-04-16 | Besins Int Belgique | Poudre filmogene, compositions la comprenant, leurs procedes de preparation et leurs utilisations |
| 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 |
| ATE454169T1 (de) * | 2003-03-13 | 2010-01-15 | Controlled Chemicals Inc | Oxycodon- konjugate mit niedrigerem missbrauch- potential und ausgedehnter tätigkeitsdauer |
| 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 |
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| JP2007532645A (ja) * | 2004-04-13 | 2007-11-15 | アルザ コーポレイション | フェンタニルに基づく薬剤の経皮送達システム用の器具および方法 |
| 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 |
| KR20080080087A (ko) * | 2005-09-30 | 2008-09-02 | 티티아이 엘뷰 가부시키가이샤 | 신규 약학 담체를 이용한 경피 약물 전달시스템, 장치 및방법 |
| MX2008013594A (es) * | 2006-04-21 | 2009-01-16 | Nektar Therapeutics Al Corp | Reduccion estereoselectiva de una morfinona. |
| US8217005B2 (en) * | 2006-05-26 | 2012-07-10 | Signature Therapeutics, Inc. | Controlled release of phenolic opioids |
| US20080066739A1 (en) * | 2006-09-20 | 2008-03-20 | Lemahieu Edward | Methods and systems of delivering medication via inhalation |
| WO2008036980A1 (en) * | 2006-09-22 | 2008-03-27 | Alltranz Inc. | Transdermally deliverable buprenorphine prodrugs and abuse-resistant compositions thereof |
| CA2667259A1 (en) * | 2006-11-07 | 2008-05-15 | Nektar Therapeutics Al, Corporation | Dosage forms and co-administration of an opioid agonist and an opioid antagonist |
| EP2129683A4 (en) * | 2007-02-26 | 2011-01-05 | Ironwood Pharmaceuticals Inc | METHODS AND COMPOSITIONS FOR TREATMENT OF HEART FAILURE AND OTHER DISORDERS |
| US8173666B2 (en) * | 2007-03-12 | 2012-05-08 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
| SI2134371T1 (sl) * | 2007-03-12 | 2015-04-30 | Nektar Therapeutics | Konjugati agonista oligomer-opioid |
| JP5693967B2 (ja) * | 2008-01-25 | 2015-04-01 | ウェルズ ファーゴ バンク ナショナル アソシエイション | オリゴマー−ジアリールピペラジンコンジュゲート |
| US20090246265A1 (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 |
| US20110165248A1 (en) * | 2008-09-18 | 2011-07-07 | Meridith Lee Machonis | Pharmaceutical dosage forms comprising poly(e-caprolactone) |
| US20130023553A1 (en) * | 2010-01-12 | 2013-01-24 | Nektar Therapeutics | Pegylated opioids with low potential for abuse and side effects |
-
2009
- 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 AU AU2009292631A patent/AU2009292631A1/en not_active Abandoned
- 2009-09-16 EP EP17198484.2A patent/EP3342427A1/en not_active Withdrawn
- 2009-09-16 CA CA2734333A patent/CA2734333A1/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 EP EP09789323A patent/EP2340044A1/en not_active Withdrawn
- 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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