JP2012510985A5 - - Google Patents
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- Publication number
- JP2012510985A5 JP2012510985A5 JP2011539101A JP2011539101A JP2012510985A5 JP 2012510985 A5 JP2012510985 A5 JP 2012510985A5 JP 2011539101 A JP2011539101 A JP 2011539101A JP 2011539101 A JP2011539101 A JP 2011539101A JP 2012510985 A5 JP2012510985 A5 JP 2012510985A5
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- JP
- Japan
- Prior art keywords
- formula
- compound
- alkyl
- process according
- stereocenter
- 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
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- 150000001875 compounds Chemical class 0.000 claims 42
- 238000000034 method Methods 0.000 claims 19
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 230000003301 hydrolyzing effect Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000002184 metal Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- ASNHGEVAWNWCRQ-UHFFFAOYSA-N 4-(hydroxymethyl)oxolane-2,3,4-triol Chemical compound OCC1(O)COC(O)C1O ASNHGEVAWNWCRQ-UHFFFAOYSA-N 0.000 claims 1
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
- 230000000202 analgesic effect Effects 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 0 CN(CC1)[C@](Cc2ccc3O)[C@@](CC4)(C5)[C@]11c2c3O[C@@]1[C@]4(*)[C@]5C(*)(*)O Chemical compound CN(CC1)[C@](Cc2ccc3O)[C@@](CC4)(C5)[C@]11c2c3O[C@@]1[C@]4(*)[C@]5C(*)(*)O 0.000 description 5
- DTIQZUYBUAVHPM-OCERQIMKSA-N CCCC(C)(C)[C@@H](C[C@](CC1)([C@H](C(C)C2)C2(C2)Cc3ccc4O)[C@]22c3c4O[C@]22C)[C@]12[O]=C Chemical compound CCCC(C)(C)[C@@H](C[C@](CC1)([C@H](C(C)C2)C2(C2)Cc3ccc4O)[C@]22c3c4O[C@]22C)[C@]12[O]=C DTIQZUYBUAVHPM-OCERQIMKSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0822342A GB0822342D0 (en) | 2008-12-08 | 2008-12-08 | Dihydroetorphine |
| GB0822342.2 | 2008-12-08 | ||
| GB0920699A GB0920699D0 (en) | 2009-11-26 | 2009-11-26 | Dihydroetorphine |
| GB0920699.6 | 2009-11-26 | ||
| PCT/GB2009/051655 WO2010067101A1 (en) | 2008-12-08 | 2009-12-04 | Dihydroetorphines and their preparation |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015116455A Division JP6151307B2 (ja) | 2008-12-08 | 2015-06-09 | ジヒドロエトルフィンおよびその調製 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012510985A JP2012510985A (ja) | 2012-05-17 |
| JP2012510985A5 true JP2012510985A5 (enExample) | 2012-08-02 |
| JP5787764B2 JP5787764B2 (ja) | 2015-09-30 |
Family
ID=42046251
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011539101A Expired - Fee Related JP5787764B2 (ja) | 2008-12-08 | 2009-12-04 | ジヒドロエトルフィンおよびその調製 |
| JP2015116455A Expired - Fee Related JP6151307B2 (ja) | 2008-12-08 | 2015-06-09 | ジヒドロエトルフィンおよびその調製 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015116455A Expired - Fee Related JP6151307B2 (ja) | 2008-12-08 | 2015-06-09 | ジヒドロエトルフィンおよびその調製 |
Country Status (31)
| Country | Link |
|---|---|
| US (4) | US20120010231A1 (enExample) |
| EP (2) | EP3018133A1 (enExample) |
| JP (2) | JP5787764B2 (enExample) |
| KR (2) | KR101992272B1 (enExample) |
| CN (2) | CN104119349B (enExample) |
| AR (1) | AR074545A1 (enExample) |
| AU (1) | AU2009326196B2 (enExample) |
| CA (1) | CA2745537C (enExample) |
| CL (1) | CL2011001363A1 (enExample) |
| CY (1) | CY1116875T1 (enExample) |
| DK (1) | DK2370443T3 (enExample) |
| EA (1) | EA022210B1 (enExample) |
| ES (1) | ES2548881T3 (enExample) |
| HR (1) | HRP20151138T1 (enExample) |
| HU (1) | HUE025913T2 (enExample) |
| IL (1) | IL213207B (enExample) |
| ME (1) | ME02262B (enExample) |
| MX (2) | MX2011006095A (enExample) |
| MY (1) | MY159913A (enExample) |
| NZ (1) | NZ593102A (enExample) |
| PA (1) | PA8852801A1 (enExample) |
| PL (1) | PL2370443T3 (enExample) |
| PT (1) | PT2370443E (enExample) |
| RS (1) | RS54309B1 (enExample) |
| SG (1) | SG171456A1 (enExample) |
| SI (1) | SI2370443T1 (enExample) |
| SM (1) | SMT201500273B (enExample) |
| TW (2) | TWI630208B (enExample) |
| UY (1) | UY32295A (enExample) |
| WO (1) | WO2010067101A1 (enExample) |
| ZA (1) | ZA201104161B (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI630208B (zh) | 2008-12-08 | 2018-07-21 | 歐陸斯迪公司 | 二氫羥戊甲嗎啡 |
| CA2896919C (en) | 2012-12-31 | 2019-01-29 | Rhodes Technologies | Process for preparing 7.beta.-substituted 6.alpha.,14.alpha.-ethenomorphinans and 7.beta.-substituted 6.alpha.,14.alpha.-ethanomorphinans |
| GB201309654D0 (en) | 2013-05-30 | 2013-07-17 | Euro Celtique Sa | Method |
| EP3023427A1 (en) * | 2014-11-19 | 2016-05-25 | Siegfried AG | Improved method of manufacturing buprenorphine and analogues thereof from oripavine |
| EP3067357A1 (en) * | 2015-03-11 | 2016-09-14 | Siegfried AG | Method of manufacturing stereoisomers of buprenorphine and analogues thereof |
| GB201513441D0 (en) * | 2015-07-30 | 2015-09-16 | Euro Celtique Sa | Transdermal delivery system |
| GB201513442D0 (en) * | 2015-07-30 | 2015-09-16 | Euro Celtique Sa | Transdermal patch |
| CN114105875B (zh) * | 2021-12-06 | 2023-11-03 | 四川大学 | 一种吗啡衍生物二氢埃托啡的合成方法 |
| EP4613751A1 (en) | 2024-03-07 | 2025-09-10 | Siegfried AG | Method of making chemical compounds useful for the synthesis of buprenorphine |
Family Cites Families (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB937214A (en) | 1961-06-02 | 1963-09-18 | J F Macfarlan & Company Ltd | Oripavine derivatives |
| GB925723A (en) | 1960-09-05 | 1963-05-08 | J F Macfarlan & Company Ltd | Novel thebaine derivatives |
| JPS59184182A (ja) | 1983-04-02 | 1984-10-19 | Res Inst For Prod Dev | ３−ベンゾイルチオ−４、５α−エポキシ−７α−〔１（Ｒ）−ヒドロキシ−１−メチルベンチル〕−６−メトキシ−１７−メチル−６、１４−エンド−エタノモルヒナン |
| JPS62153214A (ja) | 1985-12-26 | 1987-07-08 | Nitto Electric Ind Co Ltd | 医薬製剤 |
| JPS62281815A (ja) | 1986-05-27 | 1987-12-07 | Teisan Seiyaku Kk | 貼付剤及びその製造法 |
| JPS63201119A (ja) | 1987-02-17 | 1988-08-19 | Kao Corp | 貼付剤組成物 |
| US4891377A (en) | 1988-12-02 | 1990-01-02 | Board Of Regents Acting For And On Behalf Of University Of Michigan | Transdermal delivery of the narcotic analgesics etorphine and analogs |
| PT95069B (pt) | 1989-08-24 | 1997-10-31 | Searle & Co | Processo para a preparacao de (+)-isomeros de derivados de endoetano/endoetanoepoximofinano, uteis como agentes anti-tussicos |
| US5271940A (en) | 1989-09-14 | 1993-12-21 | Cygnus Therapeutic Systems | Transdermal delivery device having delayed onset |
| WO1994006426A1 (en) | 1992-09-21 | 1994-03-31 | Qin Bo Yi | Methods for identifying and using low/non-addictive opioid analgesics |
| US5633259A (en) | 1992-09-21 | 1997-05-27 | United Biomedical, Inc. | Method for identification of low/non-addictive opioid analgesics and the use of said analgesics for treatment of opioid addiction |
| JP2819236B2 (ja) | 1994-05-06 | 1998-10-30 | 日東電工株式会社 | 経皮吸収製剤 |
| AU703593B2 (en) | 1995-06-07 | 1999-03-25 | Ortho-Mcneil Pharmaceutical, Inc. | Transdermal patch and method for administering 17-deacetyl norgestimate alone or in combination with an estrogen |
| AUPN603895A0 (en) | 1995-10-19 | 1995-11-09 | University Of Queensland, The | Production of analgesic synergy by co-administration of sub-analgesic doses of two strong opioids |
| US6103258A (en) | 1996-04-12 | 2000-08-15 | Simon; David Lew | Salts and bases of the 17-(Cyclopropylmethyl)-4,5 alpha-epoxy-6-Methylenemorphinan-3,14 diol molecule for optimizing dopamine homeostasis during administration of opioid analgesics |
| KR100204659B1 (ko) * | 1996-05-28 | 1999-06-15 | 강재헌 | 신규한 부프레노핀계 진통제용 화합물 |
| JPH10231248A (ja) | 1997-02-19 | 1998-09-02 | T T S Gijutsu Kenkyusho:Kk | ジヒドロエトルフィン含有経皮吸収型製剤 |
| ME00850B (me) | 1998-08-27 | 2008-08-07 | Pfizer Health Ab | Nove perle sa kontrolisanim oslobađanjem, postupak za njihovu proizvodnju i višestruka jedinična formulacija koja ih sadrži |
| US6194382B1 (en) * | 1999-03-03 | 2001-02-27 | Albert Einstein College Of Medicine Of Yeshiva University | Method and composition for treating irritable bowel syndrome using low doses of opioid receptor antagonists |
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| AU2003219680A1 (en) | 2002-01-23 | 2003-09-02 | The Regents Of The University Of California | Methods and compositions for reducing the development of drug tolerance and/or physical dependence |
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| CN100525767C (zh) | 2002-06-10 | 2009-08-12 | 欧洲凯尔特公司 | 防止所含活性剂被误用的经皮给药器的处置系统 |
| ATE423560T1 (de) | 2002-08-20 | 2009-03-15 | Euro Celtique Sa | Transdermale dosierungsform enthaltend einen wirkstoff und einen antagonisten in freier base und in salz form |
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| TWI296531B (en) | 2002-10-18 | 2008-05-11 | Hisamitsu Pharmaceutical Co | Transdermal adhesive preparations for topical administration of fentanyl |
| TW200500067A (en) | 2003-01-21 | 2005-01-01 | Control Delivery Sys Inc | Salts of codrugs and uses related thereto |
| US20040208917A1 (en) | 2003-04-16 | 2004-10-21 | Wilfried Fischer | Transdermal systems for the release of clonidine |
| EP1641441B1 (en) | 2003-04-30 | 2014-03-12 | Purdue Pharma L.P. | Tamper-resistant transdermal dosage form comprising an active agent component and an adverse agent component at the distal site of the active agent layer |
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| TWI630208B (zh) | 2008-12-08 | 2018-07-21 | 歐陸斯迪公司 | 二氫羥戊甲嗎啡 |
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-
2009
- 2009-11-30 TW TW104114556A patent/TWI630208B/zh not_active IP Right Cessation
- 2009-11-30 TW TW098140743A patent/TWI541246B/zh not_active IP Right Cessation
- 2009-12-04 SG SG2011039310A patent/SG171456A1/en unknown
- 2009-12-04 ES ES09760972.1T patent/ES2548881T3/es active Active
- 2009-12-04 ME MEP-2015-684A patent/ME02262B/me unknown
- 2009-12-04 CN CN201410312065.XA patent/CN104119349B/zh not_active Expired - Fee Related
- 2009-12-04 EP EP15177476.7A patent/EP3018133A1/en not_active Withdrawn
- 2009-12-04 AU AU2009326196A patent/AU2009326196B2/en not_active Ceased
- 2009-12-04 SI SI200931281T patent/SI2370443T1/sl unknown
- 2009-12-04 CN CN200980156324.1A patent/CN102307877B/zh not_active Expired - Fee Related
- 2009-12-04 KR KR1020117015829A patent/KR101992272B1/ko not_active Expired - Fee Related
- 2009-12-04 MX MX2011006095A patent/MX2011006095A/es active IP Right Grant
- 2009-12-04 EA EA201170781A patent/EA022210B1/ru not_active IP Right Cessation
- 2009-12-04 KR KR1020177018820A patent/KR20170082665A/ko not_active Ceased
- 2009-12-04 PL PL09760972T patent/PL2370443T3/pl unknown
- 2009-12-04 HR HRP20151138TT patent/HRP20151138T1/hr unknown
- 2009-12-04 AR ARP090104700A patent/AR074545A1/es unknown
- 2009-12-04 CA CA2745537A patent/CA2745537C/en active Active
- 2009-12-04 HU HUE09760972A patent/HUE025913T2/en unknown
- 2009-12-04 MX MX2014015079A patent/MX359363B/es unknown
- 2009-12-04 WO PCT/GB2009/051655 patent/WO2010067101A1/en not_active Ceased
- 2009-12-04 NZ NZ593102A patent/NZ593102A/xx not_active IP Right Cessation
- 2009-12-04 MY MYPI2011002541A patent/MY159913A/en unknown
- 2009-12-04 US US13/133,472 patent/US20120010231A1/en not_active Abandoned
- 2009-12-04 PT PT97609721T patent/PT2370443E/pt unknown
- 2009-12-04 RS RS20150684A patent/RS54309B1/sr unknown
- 2009-12-04 DK DK09760972.1T patent/DK2370443T3/en active
- 2009-12-04 EP EP09760972.1A patent/EP2370443B1/en active Active
- 2009-12-04 JP JP2011539101A patent/JP5787764B2/ja not_active Expired - Fee Related
- 2009-12-04 UY UY0001032295A patent/UY32295A/es not_active Application Discontinuation
- 2009-12-07 PA PA20098852801A patent/PA8852801A1/es unknown
-
2011
- 2011-05-29 IL IL213207A patent/IL213207B/en active IP Right Grant
- 2011-06-03 ZA ZA2011/04161A patent/ZA201104161B/en unknown
- 2011-06-07 CL CL2011001363A patent/CL2011001363A1/es unknown
-
2014
- 2014-08-29 US US14/473,751 patent/US9206190B2/en not_active Expired - Fee Related
-
2015
- 2015-06-09 JP JP2015116455A patent/JP6151307B2/ja not_active Expired - Fee Related
- 2015-10-28 US US14/925,406 patent/US9481681B2/en not_active Expired - Fee Related
- 2015-10-30 SM SM201500273T patent/SMT201500273B/it unknown
- 2015-11-02 CY CY20151100975T patent/CY1116875T1/el unknown
-
2016
- 2016-10-28 US US15/336,970 patent/US10745406B2/en not_active Expired - Fee Related
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