JP2011519930A5 - - Google Patents
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- Publication number
- JP2011519930A5 JP2011519930A5 JP2011508513A JP2011508513A JP2011519930A5 JP 2011519930 A5 JP2011519930 A5 JP 2011519930A5 JP 2011508513 A JP2011508513 A JP 2011508513A JP 2011508513 A JP2011508513 A JP 2011508513A JP 2011519930 A5 JP2011519930 A5 JP 2011519930A5
- Authority
- JP
- Japan
- Prior art keywords
- dosage form
- unit dosage
- opioid
- opioid antagonist
- antagonist
- 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.)
- Pending
Links
- 239000002552 dosage form Substances 0.000 claims 22
- 239000003401 opiate antagonist Substances 0.000 claims 9
- -1 alphaprozin Chemical compound 0.000 claims 6
- 230000000694 effects Effects 0.000 claims 6
- 230000001404 mediated effect Effects 0.000 claims 6
- 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 6
- XADCESSVHJOZHK-UHFFFAOYSA-N Meperidine Chemical compound C=1C=CC=CC=1C1(C(=O)OCC)CCN(C)CC1 XADCESSVHJOZHK-UHFFFAOYSA-N 0.000 claims 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 4
- XYYVYLMBEZUESM-UHFFFAOYSA-N dihydrocodeine Natural products C1C(N(CCC234)C)C2C=CC(=O)C3OC2=C4C1=CC=C2OC XYYVYLMBEZUESM-UHFFFAOYSA-N 0.000 claims 4
- OROGSEYTTFOCAN-UHFFFAOYSA-N hydrocodone Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OC OROGSEYTTFOCAN-UHFFFAOYSA-N 0.000 claims 4
- XQYZDYMELSJDRZ-UHFFFAOYSA-N papaverine Chemical compound C1=C(OC)C(OC)=CC=C1CC1=NC=CC2=CC(OC)=C(OC)C=C12 XQYZDYMELSJDRZ-UHFFFAOYSA-N 0.000 claims 4
- 229960000482 pethidine Drugs 0.000 claims 4
- 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 3
- 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 3
- 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 3
- 229960001410 hydromorphone Drugs 0.000 claims 3
- 229960005181 morphine Drugs 0.000 claims 3
- 229960002085 oxycodone Drugs 0.000 claims 3
- 229960005118 oxymorphone Drugs 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- YQYVFVRQLZMJKJ-JBBXEZCESA-N (+)-cyclazocine Chemical compound C([C@@]1(C)C2=CC(O)=CC=C2C[C@@H]2[C@@H]1C)CN2CC1CC1 YQYVFVRQLZMJKJ-JBBXEZCESA-N 0.000 claims 2
- AKNNEGZIBPJZJG-MSOLQXFVSA-N (-)-noscapine Chemical compound CN1CCC2=CC=3OCOC=3C(OC)=C2[C@@H]1[C@@H]1C2=CC=C(OC)C(OC)=C2C(=O)O1 AKNNEGZIBPJZJG-MSOLQXFVSA-N 0.000 claims 2
- TVYLLZQTGLZFBW-ZBFHGGJFSA-N (R,R)-tramadol Chemical compound COC1=CC=CC([C@]2(O)[C@H](CCCC2)CN(C)C)=C1 TVYLLZQTGLZFBW-ZBFHGGJFSA-N 0.000 claims 2
- 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 2
- 229930008281 A03AD01 - Papaverine Natural products 0.000 claims 2
- OGDVEMNWJVYAJL-LEPYJNQMSA-N Ethyl morphine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)=C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OCC OGDVEMNWJVYAJL-LEPYJNQMSA-N 0.000 claims 2
- OGDVEMNWJVYAJL-UHFFFAOYSA-N Ethylmorphine Natural products C1C(N(CCC234)C)C2C=CC(O)C3OC2=C4C1=CC=C2OCC OGDVEMNWJVYAJL-UHFFFAOYSA-N 0.000 claims 2
- GVGLGOZIDCSQPN-PVHGPHFFSA-N Heroin Chemical compound O([C@H]1[C@H](C=C[C@H]23)OC(C)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4OC(C)=O GVGLGOZIDCSQPN-PVHGPHFFSA-N 0.000 claims 2
- JAQUASYNZVUNQP-USXIJHARSA-N Levorphanol Chemical compound C1C2=CC=C(O)C=C2[C@]23CCN(C)[C@H]1[C@@H]2CCCC3 JAQUASYNZVUNQP-USXIJHARSA-N 0.000 claims 2
- IDBPHNDTYPBSNI-UHFFFAOYSA-N N-(1-(2-(4-Ethyl-5-oxo-2-tetrazolin-1-yl)ethyl)-4-(methoxymethyl)-4-piperidyl)propionanilide Chemical compound C1CN(CCN2C(N(CC)N=N2)=O)CCC1(COC)N(C(=O)CC)C1=CC=CC=C1 IDBPHNDTYPBSNI-UHFFFAOYSA-N 0.000 claims 2
- RGPDEAGGEXEMMM-UHFFFAOYSA-N Nefopam Chemical compound C12=CC=CC=C2CN(C)CCOC1C1=CC=CC=C1 RGPDEAGGEXEMMM-UHFFFAOYSA-N 0.000 claims 2
- ONBWJWYUHXVEJS-ZTYRTETDSA-N Normorphine Chemical compound C([C@@H](NCC1)[C@@H]2C=C[C@@H]3O)C4=CC=C(O)C5=C4[C@@]21[C@H]3O5 ONBWJWYUHXVEJS-ZTYRTETDSA-N 0.000 claims 2
- 208000030053 Opioid-Induced Constipation Diseases 0.000 claims 2
- 229960001391 alfentanil Drugs 0.000 claims 2
- AKNNEGZIBPJZJG-UHFFFAOYSA-N alpha-noscapine Natural products CN1CCC2=CC=3OCOC=3C(OC)=C2C1C1C2=CC=C(OC)C(OC)=C2C(=O)O1 AKNNEGZIBPJZJG-UHFFFAOYSA-N 0.000 claims 2
- 230000036592 analgesia Effects 0.000 claims 2
- 230000000202 analgesic effect Effects 0.000 claims 2
- 229960002512 anileridine Drugs 0.000 claims 2
- LKYQLAWMNBFNJT-UHFFFAOYSA-N anileridine Chemical compound C1CC(C(=O)OCC)(C=2C=CC=CC=2)CCN1CCC1=CC=C(N)C=C1 LKYQLAWMNBFNJT-UHFFFAOYSA-N 0.000 claims 2
- 229960001736 buprenorphine Drugs 0.000 claims 2
- RMRJXGBAOAMLHD-IHFGGWKQSA-N buprenorphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]11CC[C@]3([C@H](C1)[C@](C)(O)C(C)(C)C)OC)CN2CC1CC1 RMRJXGBAOAMLHD-IHFGGWKQSA-N 0.000 claims 2
- IFKLAQQSCNILHL-QHAWAJNXSA-N butorphanol Chemical compound N1([C@@H]2CC3=CC=C(C=C3[C@@]3([C@]2(CCCC3)O)CC1)O)CC1CCC1 IFKLAQQSCNILHL-QHAWAJNXSA-N 0.000 claims 2
- 229960001113 butorphanol Drugs 0.000 claims 2
- 229960004126 codeine Drugs 0.000 claims 2
- 229950002213 cyclazocine Drugs 0.000 claims 2
- 229960004193 dextropropoxyphene Drugs 0.000 claims 2
- XLMALTXPSGQGBX-GCJKJVERSA-N dextropropoxyphene Chemical compound C([C@](OC(=O)CC)([C@H](C)CN(C)C)C=1C=CC=CC=1)C1=CC=CC=C1 XLMALTXPSGQGBX-GCJKJVERSA-N 0.000 claims 2
- 229960003461 dezocine Drugs 0.000 claims 2
- VTMVHDZWSFQSQP-VBNZEHGJSA-N dezocine Chemical compound C1CCCC[C@H]2CC3=CC=C(O)C=C3[C@]1(C)[C@H]2N VTMVHDZWSFQSQP-VBNZEHGJSA-N 0.000 claims 2
- 229960002069 diamorphine Drugs 0.000 claims 2
- RBOXVHNMENFORY-DNJOTXNNSA-N dihydrocodeine Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)C[C@H](O)[C@@H]1OC1=C2C3=CC=C1OC RBOXVHNMENFORY-DNJOTXNNSA-N 0.000 claims 2
- 229960000920 dihydrocodeine Drugs 0.000 claims 2
- 229960004578 ethylmorphine Drugs 0.000 claims 2
- 229960002428 fentanyl Drugs 0.000 claims 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 2
- LLPOLZWFYMWNKH-CMKMFDCUSA-N hydrocodone Chemical compound C([C@H]1[C@H](N(CC[C@@]112)C)C3)CC(=O)[C@@H]1OC1=C2C3=CC=C1OC LLPOLZWFYMWNKH-CMKMFDCUSA-N 0.000 claims 2
- 229960000240 hydrocodone Drugs 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- XBMIVRRWGCYBTQ-AVRDEDQJSA-N levacetylmethadol Chemical compound C=1C=CC=CC=1C(C[C@H](C)N(C)C)([C@@H](OC(C)=O)CC)C1=CC=CC=C1 XBMIVRRWGCYBTQ-AVRDEDQJSA-N 0.000 claims 2
- 229960003406 levorphanol Drugs 0.000 claims 2
- FQXXSQDCDRQNQE-UHFFFAOYSA-N markiertes Thebain Natural products COC1=CC=C2C(N(CC3)C)CC4=CC=C(OC)C5=C4C23C1O5 FQXXSQDCDRQNQE-UHFFFAOYSA-N 0.000 claims 2
- 229960001797 methadone Drugs 0.000 claims 2
- 229960000805 nalbuphine Drugs 0.000 claims 2
- NETZHAKZCGBWSS-CEDHKZHLSA-N nalbuphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]1(O)CC[C@@H]3O)CN2CC1CCC1 NETZHAKZCGBWSS-CEDHKZHLSA-N 0.000 claims 2
- PLPRGLOFPNJOTN-UHFFFAOYSA-N narcotine Natural products COc1ccc2C(OC(=O)c2c1OC)C3Cc4c(CN3C)cc5OCOc5c4OC PLPRGLOFPNJOTN-UHFFFAOYSA-N 0.000 claims 2
- 229960000751 nefopam Drugs 0.000 claims 2
- 229950006134 normorphine Drugs 0.000 claims 2
- 229960004708 noscapine Drugs 0.000 claims 2
- 229960001789 papaverine Drugs 0.000 claims 2
- VOKSWYLNZZRQPF-GDIGMMSISA-N pentazocine Chemical compound C1C2=CC=C(O)C=C2[C@@]2(C)[C@@H](C)[C@@H]1N(CC=C(C)C)CC2 VOKSWYLNZZRQPF-GDIGMMSISA-N 0.000 claims 2
- 229960005301 pentazocine Drugs 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- GGCSSNBKKAUURC-UHFFFAOYSA-N sufentanil Chemical compound C1CN(CCC=2SC=CC=2)CCC1(COC)N(C(=O)CC)C1=CC=CC=C1 GGCSSNBKKAUURC-UHFFFAOYSA-N 0.000 claims 2
- 229960004739 sufentanil Drugs 0.000 claims 2
- FQXXSQDCDRQNQE-VMDGZTHMSA-N thebaine Chemical compound C([C@@H](N(CC1)C)C2=CC=C3OC)C4=CC=C(OC)C5=C4[C@@]21[C@H]3O5 FQXXSQDCDRQNQE-VMDGZTHMSA-N 0.000 claims 2
- 229930003945 thebaine Natural products 0.000 claims 2
- 229960004380 tramadol Drugs 0.000 claims 2
- TVYLLZQTGLZFBW-GOEBONIOSA-N tramadol Natural products COC1=CC=CC([C@@]2(O)[C@@H](CCCC2)CN(C)C)=C1 TVYLLZQTGLZFBW-GOEBONIOSA-N 0.000 claims 2
- LLPOLZWFYMWNKH-UHFFFAOYSA-N trans-dihydrocodeinone Natural products C1C(N(CCC234)C)C2CCC(=O)C3OC2=C4C1=CC=C2OC LLPOLZWFYMWNKH-UHFFFAOYSA-N 0.000 claims 2
- 206010010774 Constipation Diseases 0.000 claims 1
- 241000282412 Homo Species 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940005483 opioid analgesics Drugs 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12686808P | 2008-05-07 | 2008-05-07 | |
| US61/126,868 | 2008-05-07 | ||
| PCT/US2009/002856 WO2009137086A1 (en) | 2008-05-07 | 2009-05-07 | Oral administration of peripherally-acting opioid antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011519930A JP2011519930A (ja) | 2011-07-14 |
| JP2011519930A5 true JP2011519930A5 (enExample) | 2012-06-21 |
Family
ID=40888194
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011508513A Pending JP2011519930A (ja) | 2008-05-07 | 2009-05-07 | 末梢性オピオイドアンタゴニストの経口投与 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20110160239A1 (enExample) |
| EP (1) | EP2300009A1 (enExample) |
| JP (1) | JP2011519930A (enExample) |
| KR (1) | KR20110004425A (enExample) |
| CN (1) | CN102014907A (enExample) |
| AU (1) | AU2009244805B2 (enExample) |
| BR (1) | BRPI0912219A2 (enExample) |
| CA (1) | CA2723685C (enExample) |
| EA (1) | EA201001643A1 (enExample) |
| IL (1) | IL208794A0 (enExample) |
| MX (1) | MX2010011727A (enExample) |
| MY (1) | MY156913A (enExample) |
| NZ (1) | NZ589733A (enExample) |
| WO (1) | WO2009137086A1 (enExample) |
| ZA (1) | ZA201007531B (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20150037T4 (hr) | 2003-04-08 | 2022-09-02 | Progenics Pharmaceuticals, Inc. | Farmaceutske formulacije koje sadrže metilnaltrekson |
| TWI489984B (zh) | 2006-08-04 | 2015-07-01 | Wyeth Corp | 用於非經腸道傳輸化合物之配方及其用途 |
| EA029096B1 (ru) * | 2010-03-11 | 2018-02-28 | Вайет Ллк | Твердая лекарственная форма для перорального введения, содержащая метилналтрексон |
| PE20140636A1 (es) | 2010-09-30 | 2014-06-18 | Astrazeneca Ab | Conjugado de naloxol-peg cristalino |
| AU2012359013A1 (en) * | 2011-12-19 | 2014-06-26 | Salix Pharmaceuticals, Ltd. | Methods for treatment and prevention of opioid induced constipation using oral compositions of methylnaltrexone |
| AU2014306759B2 (en) | 2013-08-12 | 2018-04-26 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded immediate release abuse deterrent pill |
| CN104546791A (zh) * | 2013-10-16 | 2015-04-29 | 辽宁亿灵科创生物医药科技有限公司 | 一种阿片受体拮抗剂的固体制剂及其制备方法 |
| US10172797B2 (en) | 2013-12-17 | 2019-01-08 | 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 |
| HUE036084T2 (hu) | 2014-04-28 | 2018-06-28 | Orphomed Inc | Buprenorfin dimer és alkalmazása gasztrointesztinális rendellenességek kezelésénél |
| 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 |
| CN107406456B (zh) * | 2015-12-01 | 2019-08-30 | 江苏恒瑞医药股份有限公司 | 阿片样受体拮抗剂类衍生物、其制备方法及其在医药上的应用 |
| 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 |
| CN109134479A (zh) * | 2017-06-27 | 2019-01-04 | 石家庄蒎格医药科技有限公司 | 结晶聚乙二醇纳洛酮草酸盐及制备方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6451806B2 (en) * | 1999-09-29 | 2002-09-17 | Adolor Corporation | Methods and compositions involving opioids and antagonists thereof |
| PT1225897E (pt) * | 1999-11-01 | 2005-01-31 | John Rhodes | Composicao para o tratamento da obstipacao e do sindroma do intestino irritavel |
| EP2236161A1 (en) * | 2001-10-18 | 2010-10-06 | Nektar Therapeutics | Polymer conjugates of opioid antagonists |
| US20060182692A1 (en) * | 2003-12-16 | 2006-08-17 | Fishburn C S | Chemically modified small molecules |
| HRP20140361T1 (hr) * | 2003-12-16 | 2014-05-23 | Nektar Therapeutics | Monodisperzne smjese pegiliranog naloksola |
| MX2008013594A (es) * | 2006-04-21 | 2009-01-16 | Nektar Therapeutics Al Corp | Reduccion estereoselectiva de una morfinona. |
| 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 |
-
2009
- 2009-05-07 KR KR1020107024868A patent/KR20110004425A/ko not_active Ceased
- 2009-05-07 CN CN2009801164862A patent/CN102014907A/zh active Pending
- 2009-05-07 MX MX2010011727A patent/MX2010011727A/es not_active Application Discontinuation
- 2009-05-07 NZ NZ589733A patent/NZ589733A/xx unknown
- 2009-05-07 WO PCT/US2009/002856 patent/WO2009137086A1/en not_active Ceased
- 2009-05-07 EP EP09743073A patent/EP2300009A1/en not_active Withdrawn
- 2009-05-07 BR BRPI0912219A patent/BRPI0912219A2/pt not_active Application Discontinuation
- 2009-05-07 US US12/991,229 patent/US20110160239A1/en not_active Abandoned
- 2009-05-07 JP JP2011508513A patent/JP2011519930A/ja active Pending
- 2009-05-07 AU AU2009244805A patent/AU2009244805B2/en active Active
- 2009-05-07 CA CA2723685A patent/CA2723685C/en active Active
- 2009-05-07 MY MYPI2010005212A patent/MY156913A/en unknown
- 2009-05-07 EA EA201001643A patent/EA201001643A1/ru unknown
-
2010
- 2010-10-18 IL IL208794A patent/IL208794A0/en unknown
- 2010-10-21 ZA ZA2010/07531A patent/ZA201007531B/en unknown
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