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 (OSRAM) | 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 (OSRAM) |
| EP (2) | EP2340044A1 (OSRAM) |
| JP (1) | JP5827123B2 (OSRAM) |
| KR (1) | KR101660996B1 (OSRAM) |
| CN (1) | CN102159249A (OSRAM) |
| AU (1) | AU2009292631A1 (OSRAM) |
| CA (1) | CA2734333A1 (OSRAM) |
| IL (1) | IL211762A (OSRAM) |
| MX (1) | MX347741B (OSRAM) |
| WO (1) | WO2010033195A1 (OSRAM) |
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 |
| JP5837491B2 (ja) * | 2009-07-21 | 2015-12-24 | 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−オピオイドアゴニスト抱合体 |
| WO2011088140A1 (en) * | 2010-01-12 | 2011-07-21 | Nektar Therapeutics | Pegylated opioids with low potential for abuse and side effects |
| EP2568968B1 (en) | 2010-05-10 | 2017-07-12 | Euro-Celtique S.A. | Manufacturing of active-free granules and tablets comprising the same |
| US8927025B2 (en) | 2010-05-11 | 2015-01-06 | Cima Labs Inc. | Alcohol-resistant metoprolol-containing extended-release oral dosage forms |
| 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 |
| MX348933B (es) | 2011-11-07 | 2017-07-03 | Nektar Therapeutics | Composiciones, formas de dosificacion y coadministracion de un compuesto agonista opioide y un compuesto analgesico. |
| EP2895457B1 (en) | 2012-09-17 | 2020-05-20 | Nektar Therapeutics | Oligomer-containing benzamide-based compounds |
| CA2886276A1 (en) | 2012-10-30 | 2014-05-08 | 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 |
| 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 |
| WO2015065547A1 (en) | 2013-10-31 | 2015-05-07 | Cima Labs Inc. | Immediate release abuse-deterrent granulated dosage forms |
| US9814710B2 (en) | 2013-11-13 | 2017-11-14 | 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 |
| US10172797B2 (en) | 2013-12-17 | 2019-01-08 | 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 |
| 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 |
| EP3654977A4 (en) * | 2017-07-20 | 2021-06-09 | Suzhou Runxindatai Pharmaceutics Ltd Co. | SUSTAINABLE RELEASE, ABUSE RESISTANT OPIOID PRODRUGS |
| CA3095299A1 (en) | 2018-03-29 | 2019-10-03 | Nof Corporation | Method for purifying trityl group-containing monodispersed polyethylene glycol |
| 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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| 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 |
| 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 |
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| AU782298B2 (en) * | 1999-10-04 | 2005-07-14 | Nektar Therapeutics | 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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| EP2402037B8 (en) * | 2006-05-26 | 2019-12-04 | Signature Therapeutics, Inc. | Controlled release of phenolic opioids |
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| 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 |
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| EP2249872B1 (en) * | 2008-01-25 | 2017-03-22 | Nektar Therapeutics | Oligomer-diarylpiperazine conjugates |
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-
2009
- 2009-09-16 US US13/063,919 patent/US20110237614A1/en not_active Abandoned
- 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 WO PCT/US2009/005174 patent/WO2010033195A1/en not_active Ceased
- 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 KR KR1020117004392A patent/KR101660996B1/ko not_active Expired - Fee Related
- 2009-09-16 CA CA2734333A patent/CA2734333A1/en not_active Abandoned
- 2009-09-16 EP EP17198484.2A patent/EP3342427A1/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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