JP2012510985A5 - - Google Patents
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- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 42
- 238000000034 method Methods 0.000 claims 18
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 5
- 239000011780 sodium chloride Substances 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 230000003301 hydrolyzing 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
- 230000000202 analgesic Effects 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 150000003840 hydrochlorides Chemical class 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
Description
Claims (33)
- 式(VI)の化合物、またはその塩もしくは誘導体
- 前記(V)の化合物が、式(IV)の化合物
式R2M(X)Pの化合物[式中、R2はC1〜8アルキルであり、Mは金属であり、Xはハライドであり、pは1または0である]を反応させることによって調製される、請求項1に記載のプロセス。 - 前記式(IV)の化合物が、式(III)の化合物
- 前記式(III)の化合物が、式(I)の化合物
- 式(VI)の化合物、またはその塩もしくは誘導体
前記式(III)の化合物を還元して、式(IV)の化合物
前記式(IV)の化合物と式R2M(X)Pの化合物[式中、R2はC1〜8アルキルであり、Mは金属であり、Xはハライドであり、pは1または0である]を反応させて、式(V)の化合物
前記式(V)の化合物を加水分解して、式(VI)の化合物を得るステップと
を含むプロセス。 - 前記式(VI)の化合物を結晶化するステップをさらに含む、請求項1から5のいずれか一項に記載のプロセス。
- R1がC 3〜5 アルキルである、請求項1から6のいずれか一項に記載のプロセス。
- R1がプロピルである、請求項1から6のいずれか一項に記載のプロセス。
- R1がn-プロピルである、請求項1から6のいずれか一項に記載のプロセス。
- R2がC 1〜2 アルキルである、請求項1から7のいずれか一項に記載のプロセス。
- R2がメチルである、請求項1から7のいずれか一項に記載のプロセス。
- 式(V)および(VI)における前記立体中心(*)が(S)である、請求項1から8のいずれか一項に記載のプロセス。
- 式(V)の化合物が少なくとも90%のジアステレオマー過剰率で生じる、請求項12に記載のプロセス。
- 前記式(V)の化合物が、
- 前記式(VI)の化合物が、
- 式(V)および(VI)における前記立体中心(*)が(R)である、請求項1から8のいずれか一項に記載のプロセス。
- 式(VI)
- 式(VI)
- 式(V)
- 式(Va)
- 遊離塩基形態で存在する、請求項17から20のいずれか一項に記載の化合物
- 薬学的に許容される塩としての、請求項17から20のいずれか一項に記載の化合物
- 塩酸塩としての、請求項22に記載の化合物
- 式(IV)
- 式(III)
- R1がプロピルである、請求項17または請求項18に記載の化合物。
- 式(III)の化合物を作製するプロセスであって、式(I)の化合物
を含むプロセス。 - 請求項13から19のいずれか一項に記載の化合物を含む医薬組成物。
- 経皮投与に適した剤形で存在する、請求項28に記載の医薬組成物。
- 医薬品で使用するための、請求項13から19のいずれか一項に記載の化合物。
- 鎮痛剤として使用するための、請求項13から19のいずれか一項に記載の化合物。
- 疼痛を治療するための医薬品の製造における、請求項13から19のいずれか一項に記載の化合物の使用。
- 疼痛軽減を必要とする対象を治療する方法であって、前記対象に治療有効量の請求項13から19のいずれか一項に記載の化合物を投与するステップを含む方法。
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0822342.2 | 2008-12-08 | ||
| GB0822342A GB0822342D0 (en) | 2008-12-08 | 2008-12-08 | Dihydroetorphine |
| 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 (ja) | 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 (32)
| Country | Link |
|---|---|
| US (4) | US20120010231A1 (ja) |
| EP (2) | EP2370443B1 (ja) |
| JP (2) | JP5787764B2 (ja) |
| KR (2) | KR101992272B1 (ja) |
| CN (2) | CN102307877B (ja) |
| AR (1) | AR074545A1 (ja) |
| AU (1) | AU2009326196B2 (ja) |
| CA (1) | CA2745537C (ja) |
| CL (1) | CL2011001363A1 (ja) |
| CY (1) | CY1116875T1 (ja) |
| DK (1) | DK2370443T3 (ja) |
| EA (1) | EA022210B1 (ja) |
| ES (1) | ES2548881T3 (ja) |
| HK (1) | HK1161720A1 (ja) |
| HR (1) | HRP20151138T1 (ja) |
| HU (1) | HUE025913T2 (ja) |
| IL (1) | IL213207B (ja) |
| ME (1) | ME02262B (ja) |
| MX (2) | MX2011006095A (ja) |
| MY (1) | MY159913A (ja) |
| NZ (1) | NZ593102A (ja) |
| PA (1) | PA8852801A1 (ja) |
| PL (1) | PL2370443T3 (ja) |
| PT (1) | PT2370443E (ja) |
| RS (1) | RS54309B1 (ja) |
| SG (1) | SG171456A1 (ja) |
| SI (1) | SI2370443T1 (ja) |
| SM (1) | SMT201500273B (ja) |
| TW (2) | TWI541246B (ja) |
| UY (1) | UY32295A (ja) |
| WO (1) | WO2010067101A1 (ja) |
| ZA (1) | ZA201104161B (ja) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI541246B (zh) * | 2008-12-08 | 2016-07-11 | 歐陸斯迪公司 | 二氫羥戊甲嗎啡 |
| JP6181770B2 (ja) | 2012-12-31 | 2017-08-16 | ローズ テクノロジーズ | ７β−置換６α，１４α−エテノモルフィナンおよび７β−置換６α，１４α−エタノモルフィナンを調製するための方法 |
| 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 |
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-
2009
- 2009-11-30 TW TW098140743A patent/TWI541246B/zh not_active IP Right Cessation
- 2009-11-30 TW TW104114556A patent/TWI630208B/zh not_active IP Right Cessation
- 2009-12-04 NZ NZ593102A patent/NZ593102A/xx not_active IP Right Cessation
- 2009-12-04 UY UY0001032295A patent/UY32295A/es not_active Application Discontinuation
- 2009-12-04 RS RS20150684A patent/RS54309B1/en unknown
- 2009-12-04 AR ARP090104700A patent/AR074545A1/es unknown
- 2009-12-04 PL PL09760972T patent/PL2370443T3/pl unknown
- 2009-12-04 KR KR1020117015829A patent/KR101992272B1/ko active IP Right Grant
- 2009-12-04 WO PCT/GB2009/051655 patent/WO2010067101A1/en active Application Filing
- 2009-12-04 AU AU2009326196A patent/AU2009326196B2/en active Active
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