PT2251330E - 4-hidroxibenzomorfanos - Google Patents
4-hidroxibenzomorfanos Download PDFInfo
- Publication number
- PT2251330E PT2251330E PT10008474T PT10008474T PT2251330E PT 2251330 E PT2251330 E PT 2251330E PT 10008474 T PT10008474 T PT 10008474T PT 10008474 T PT10008474 T PT 10008474T PT 2251330 E PT2251330 E PT 2251330E
- Authority
- PT
- Portugal
- Prior art keywords
- hydrogen
- compound according
- mmol
- hydroxy
- disease
- Prior art date
Links
- 239000003814 drug Substances 0.000 claims abstract description 5
- 150000001875 compounds Chemical class 0.000 claims description 46
- -1 C2 -C6 alkyl Chemical group 0.000 claims description 32
- 239000001257 hydrogen Substances 0.000 claims description 18
- 229910052739 hydrogen Inorganic materials 0.000 claims description 18
- 125000000217 alkyl group Chemical group 0.000 claims description 14
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 13
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- 108090000137 Opioid Receptors Proteins 0.000 claims description 12
- 125000003118 aryl group Chemical group 0.000 claims description 10
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
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- IZUPBVBPLAPZRR-UHFFFAOYSA-N pentachloro-phenol Natural products OC1=C(Cl)C(Cl)=C(Cl)C(Cl)=C1Cl IZUPBVBPLAPZRR-UHFFFAOYSA-N 0.000 description 1
- 230000000505 pernicious effect Effects 0.000 description 1
- FTDXCHCAMNRNNY-UHFFFAOYSA-N phenol Chemical compound OC1=CC=CC=C1.OC1=CC=CC=C1 FTDXCHCAMNRNNY-UHFFFAOYSA-N 0.000 description 1
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- 230000003389 potentiating effect Effects 0.000 description 1
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- 230000000069 prophylactic effect Effects 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
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- 239000000377 silicon dioxide Substances 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 239000002002 slurry Substances 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000012312 sodium hydride Substances 0.000 description 1
- 229910000104 sodium hydride Inorganic materials 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 229910052682 stishovite Inorganic materials 0.000 description 1
- 150000003457 sulfones Chemical class 0.000 description 1
- 150000003462 sulfoxides Chemical class 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
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- FTVLMFQEYACZNP-UHFFFAOYSA-N trimethylsilyl trifluoromethanesulfonate Chemical compound C[Si](C)(C)OS(=O)(=O)C(F)(F)F FTVLMFQEYACZNP-UHFFFAOYSA-N 0.000 description 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
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- GTLDTDOJJJZVBW-UHFFFAOYSA-N zinc cyanide Chemical compound [Zn+2].N#[C-].N#[C-] GTLDTDOJJJZVBW-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
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- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
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- C07D215/14—Radicals substituted by oxygen atoms
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- C07—ORGANIC CHEMISTRY
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- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/20—Oxygen atoms
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
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-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
- C07D489/02—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
- C07D489/06—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with a hetero atom directly attached in position 14
- C07D489/08—Oxygen atom
Landscapes
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- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Hydrogenated Pyridines (AREA)
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| CA2426942C (en) * | 2000-10-31 | 2014-06-03 | Mark P. Wentland | 8-carboxamido-2,6-methano-3-benzazocines |
| PT2251330E (pt) * | 2004-11-05 | 2012-07-20 | Rensselaer Polytech Inst | 4-hidroxibenzomorfanos |
| EP2266959B1 (en) | 2005-07-21 | 2013-05-01 | Rensselaer Polytechnic Institute | 8-carboxamido-substituted-2, 6-methano-3-benzazocines and 3-carboxamido-substituted morphanes as opioid receptor binding agents |
| AU2008207580B2 (en) | 2007-05-04 | 2011-04-14 | SpecGx LLC | Improved process for the preparation of 6-alpha-hydroxy-N-alkylated opiates |
| EP2167505B1 (en) | 2007-07-17 | 2012-11-28 | Mallinckrodt LLC | Preparation of n-alkylated opiates by reductive amination |
| EP2190819B1 (en) | 2007-08-09 | 2016-05-25 | Rensselaer Polytechnic Institute | Quaternary opioid carboxamides |
| WO2010039222A2 (en) | 2008-09-30 | 2010-04-08 | Mallinckrodt Inc. | Processes for the selective amination of ketomorphinans |
| US8946419B2 (en) | 2009-02-23 | 2015-02-03 | Mallinckrodt Llc | (+)-6-hydroxy-morphinan or (+)-6-amino-morphinan derivatives |
| EP3170395A1 (en) * | 2009-03-19 | 2017-05-24 | Alkermes Pharma Ireland Limited | Morphinan derivatives with high oral bioavailability |
| WO2010118274A1 (en) * | 2009-04-09 | 2010-10-14 | Mallinckrodt Inc. | Preparation of 6-keto, 3-alkoxy morphinans |
| JP5680069B2 (ja) | 2009-06-11 | 2015-03-04 | マリンクロッド エルエルシー | 触媒的水素移動による６−ケトノルモルフィナンの還元アミノ化 |
| EP2440562B1 (en) | 2009-06-11 | 2016-08-10 | Mallinckrodt LLC | Preparation of 6-alpha-amino n-substituted morphinans by catalytic hydrogen transfer |
| NZ600379A (en) * | 2009-12-04 | 2014-05-30 | Alkermes Pharma Ireland Ltd | Morphinan derivatives for the treatment of drug overdose |
| US8436175B2 (en) * | 2010-03-22 | 2013-05-07 | Rensselaer Polytechnic Institute | Carboxamide bioisosteres of opiates |
| EP2563793B1 (en) * | 2010-04-29 | 2014-10-22 | Mallinckrodt LLC | Preparation of saturated ketone morphinan compounds having low metal content |
| WO2012005795A1 (en) | 2010-07-08 | 2012-01-12 | Alkermes, Inc. | Process for the synthesis of substituted morphinans |
| SI3446565T1 (sl) | 2010-08-23 | 2024-03-29 | Alkermes Pharma Ireland Limited | Metode zdravljenja povečanja teže, povzročene z antipsihotiki |
| WO2012138888A1 (en) | 2011-04-05 | 2012-10-11 | Alkermes, Inc. | Process for the synthesis of quaternary amine compounds |
| RU2013157298A (ru) | 2011-06-09 | 2015-07-20 | МАЛЛИНКРОДТ Эл-Эл-Си | Восстановительное аминирование 6-кетоморфинанов посредством каталитического переноса водорода |
| RS56181B1 (sr) | 2011-06-29 | 2017-11-30 | Alkermes Inc | Periferno delujuća opioidna jedinjenja |
| JP2014526467A (ja) | 2011-09-08 | 2014-10-06 | マリンクロッド エルエルシー | 中間体の単離なしでのアルカロイドの調製 |
| HUE041883T2 (hu) | 2011-12-15 | 2019-06-28 | Alkermes Pharma Ireland Ltd | Samidorphan (ALKS 33) és buprenorfin kombináció, depressziós zavarok kezelésére |
| US9211293B2 (en) | 2011-12-15 | 2015-12-15 | Alkermes Pharma Ireland Limited | Opioid agonist antagonist combinations |
| US9656961B2 (en) | 2013-05-24 | 2017-05-23 | Alkermes Pharma Ireland Limited | Methods for treating depressive symptoms |
| JP2016519161A (ja) | 2013-05-24 | 2016-06-30 | アルカームス ファーマ アイルランド リミテッド | モルファン及びモルフィナン類似物及び使用の方法 |
| CA3054122A1 (en) * | 2017-03-02 | 2018-09-07 | Sanwa Kagaku Kenkyusho Co., Ltd. | Therapeutic agent for alcohol use disorders |
| CN107089948B (zh) * | 2017-04-28 | 2020-07-17 | 云南大学 | 吗吩衍生物及其制备方法和应用 |
| CN111978252A (zh) * | 2019-05-21 | 2020-11-24 | 复旦大学 | 手性苯并吗吩烷类衍生物及其制备方法和在药学上的应用 |
| CN113248435B (zh) * | 2020-02-13 | 2024-06-04 | 上海翰森生物医药科技有限公司 | 3-甲酰胺基-4-羟基纳曲酮氘代衍生物、其制备方法及其在医药上的应用 |
| CN111205151B (zh) * | 2020-02-29 | 2021-03-05 | 深圳市祥根生物科技有限公司 | 一种布洛芬杂质i的环保制备方法 |
| EP4243768A1 (en) | 2020-11-12 | 2023-09-20 | Alkermes Pharma Ireland Limited | Immediate release multilayer tablet |
| CN114621238A (zh) * | 2020-12-10 | 2022-06-14 | 鲁南制药集团股份有限公司 | 一种制备纳呋拉啡的方法 |
| KR102663533B1 (ko) * | 2021-11-09 | 2024-05-08 | 백미선 | 레이저 치료기기용 온냉각장치 |
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| US3957793A (en) | 1974-09-20 | 1976-05-18 | Sterling Drug Inc. | Hydroxyiminobenzazocines |
| US4032529A (en) | 1974-09-20 | 1977-06-28 | Sterling Drug Inc. | Aminomethanobenzazocine intermediates |
| SU635868A3 (ru) * | 1974-11-12 | 1978-11-30 | Бристол Мейерз Компани (Фирма) | Способ получени морфиновых производных или их солей |
| US4205171A (en) | 1976-01-12 | 1980-05-27 | Sterling Drug Inc. | Aminomethanobenzazocines and nitromethanobenzazocines |
| US4373139A (en) | 1979-04-30 | 1983-02-08 | Motorola, Inc. | Detectors |
| US4649200A (en) | 1986-05-08 | 1987-03-10 | Regents Of The University Of Minnesota | Substituted pyrroles with opioid receptor activity |
| EP0632041A1 (en) | 1993-07-01 | 1995-01-04 | Katholieke Universiteit Nijmegen | New morphine derivatives having improved analgesic and narcotic properties |
| AU706370B2 (en) | 1996-01-10 | 1999-06-17 | Smithkline Beecham Spa | Heterocycle-condensed morphinoid derivatives (II) |
| CA2426942C (en) | 2000-10-31 | 2014-06-03 | Mark P. Wentland | 8-carboxamido-2,6-methano-3-benzazocines |
| AU2003281060A1 (en) | 2002-07-16 | 2004-02-02 | Rensselaer Polytechnic Institute | Process for conversion of phenols to carboxamides via the succinimide esters |
| PT2251330E (pt) * | 2004-11-05 | 2012-07-20 | Rensselaer Polytech Inst | 4-hidroxibenzomorfanos |
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2005
- 2005-11-03 PT PT10008474T patent/PT2251330E/pt unknown
- 2005-11-03 RU RU2010147915/04A patent/RU2480455C2/ru active
- 2005-11-03 KR KR1020077012582A patent/KR101115841B1/ko not_active Expired - Lifetime
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- 2005-11-03 AU AU2005304950A patent/AU2005304950B2/en not_active Expired
- 2005-11-03 EP EP10008474A patent/EP2251330B1/en not_active Expired - Lifetime
- 2005-11-03 SI SI200531549T patent/SI2251330T1/sl unknown
- 2005-11-03 BR BRPI0517091A patent/BRPI0517091B8/pt active IP Right Grant
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- 2005-11-03 AT AT10008474T patent/ATE557006T1/de active
- 2005-11-03 PL PL10008474T patent/PL2251330T3/pl unknown
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- 2005-11-03 ES ES10008474T patent/ES2387737T3/es not_active Expired - Lifetime
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- 2005-11-03 RU RU2007120759/04A patent/RU2415131C2/ru active
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2007
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2012
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2013
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2014
- 2014-01-31 US US14/169,305 patent/US8802655B2/en not_active Expired - Lifetime
- 2014-07-02 US US14/321,885 patent/US20150011768A1/en not_active Abandoned
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2015
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2023
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