CA2754984C - Morphinan derivatives with high oral bioavailability - Google Patents
Morphinan derivatives with high oral bioavailability Download PDFInfo
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- CA2754984C CA2754984C CA2754984A CA2754984A CA2754984C CA 2754984 C CA2754984 C CA 2754984C CA 2754984 A CA2754984 A CA 2754984A CA 2754984 A CA2754984 A CA 2754984A CA 2754984 C CA2754984 C CA 2754984C
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- AWUCVROLDVIAJX-GSVOUGTGSA-N sn-glycerol 3-phosphate Chemical compound OC[C@@H](O)COP(O)(O)=O AWUCVROLDVIAJX-GSVOUGTGSA-N 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16170209P | 2009-03-19 | 2009-03-19 | |
| US61/161,702 | 2009-03-19 | ||
| PCT/US2009/066801 WO2010107457A1 (en) | 2009-03-19 | 2009-12-04 | Morphinan derivatives with high oral bioavailability |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2754984A1 CA2754984A1 (en) | 2010-09-23 |
| CA2754984C true CA2754984C (en) | 2018-06-26 |
Family
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2754984A Active CA2754984C (en) | 2009-03-19 | 2009-12-04 | Morphinan derivatives with high oral bioavailability |
Country Status (6)
| Country | Link |
|---|---|
| US (4) | US20100240691A1 (enExample) |
| EP (2) | EP3170395A1 (enExample) |
| JP (4) | JP5555890B2 (enExample) |
| AU (1) | AU2009342654B2 (enExample) |
| CA (1) | CA2754984C (enExample) |
| WO (1) | WO2010107457A1 (enExample) |
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| CA2754984C (en) * | 2009-03-19 | 2018-06-26 | Alkermes, Inc. | Morphinan derivatives with high oral bioavailability |
| DK2506712T3 (da) * | 2009-12-04 | 2019-06-03 | Alkermes Pharma Ireland Ltd | Morfinanderivater til behandling af lægemiddeloverdosering |
| HRP20240109T1 (hr) | 2010-08-23 | 2024-03-29 | Alkermes Pharma Ireland Limited | Postupci za liječenje povećanja tjelesne težine induciranog antipsihoticima |
| US9211293B2 (en) | 2011-12-15 | 2015-12-15 | Alkermes Pharma Ireland Limited | Opioid agonist antagonist combinations |
| WO2013088242A1 (en) * | 2011-12-15 | 2013-06-20 | Alkermes Pharma Ireland Limited | Samidorphan (alks 33) in combination with opioid agonists |
| US10195191B2 (en) | 2011-12-15 | 2019-02-05 | Alkermes Pharma Ireland Limited | Opioid agonist antagonist combinations |
| PL3153171T3 (pl) * | 2011-12-15 | 2019-02-28 | Alkermes Pharma Ireland Limited | Samidorfan (alks 33) w połączeniu z buprenorfiną do leczenia zaburzeń depresyjnych |
| US20140179727A1 (en) | 2012-12-14 | 2014-06-26 | Trevi Therapeutics, Inc. | Methods for treating pruritus |
| US8637538B1 (en) | 2012-12-14 | 2014-01-28 | Trevi Therapeutics, Inc. | Methods for treatment of pruritis |
| US8987289B2 (en) | 2012-12-14 | 2015-03-24 | Trevi Therapeutics, Inc. | Methods for treating pruritus |
| WO2014190270A1 (en) | 2013-05-24 | 2014-11-27 | Alkermes Pharma Ireland Limited | Morphan and morphinan analogues, and methods of use |
| US9656961B2 (en) | 2013-05-24 | 2017-05-23 | Alkermes Pharma Ireland Limited | Methods for treating depressive symptoms |
| AU2019309913B2 (en) | 2018-07-23 | 2025-02-27 | Trevi Therapeutics, Inc. | Treatment of chronic cough, breathlessness and dyspnea |
| EP4087569A4 (en) | 2020-01-10 | 2024-01-24 | Trevi Therapeutics, Inc. | METHODS OF ADMINISTRATION OF NALBUPHINE |
| WO2021178405A1 (en) * | 2020-03-02 | 2021-09-10 | University Of Southern California | Opioid receptor antagonists |
| EP4243768A1 (en) | 2020-11-12 | 2023-09-20 | Alkermes Pharma Ireland Limited | Immediate release multilayer tablet |
| WO2025038406A1 (en) * | 2023-08-11 | 2025-02-20 | Virginia Commonwealth University | Design, synthesis, and biological evaluation of nitrogen-walk derivatives of nan as mu opioid receptor selective modulators |
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| US3856795A (en) * | 1972-04-25 | 1974-12-24 | American Home Prod | Process for preparation of secondary amines from tertiary amines |
| US4032529A (en) * | 1974-09-20 | 1977-06-28 | Sterling Drug Inc. | Aminomethanobenzazocine intermediates |
| US3957793A (en) * | 1974-09-20 | 1976-05-18 | Sterling Drug Inc. | Hydroxyiminobenzazocines |
| US4127577A (en) * | 1975-11-24 | 1978-11-28 | Sterling Drug Inc. | Aminomethanobenzazocine process |
| US4205171A (en) * | 1976-01-12 | 1980-05-27 | Sterling Drug Inc. | Aminomethanobenzazocines and nitromethanobenzazocines |
| US4464378A (en) * | 1981-04-28 | 1984-08-07 | University Of Kentucky Research Foundation | Method of administering narcotic antagonists and analgesics and novel dosage forms containing same |
| US4649200A (en) * | 1986-05-08 | 1987-03-10 | Regents Of The University Of Minnesota | Substituted pyrroles with opioid receptor activity |
| US5028612A (en) * | 1990-03-22 | 1991-07-02 | Hillel Glover | Method for treating emotional numbness |
| US5258386A (en) * | 1991-06-05 | 1993-11-02 | The United States Of America As Represented By The Secretary Of The Army | (+)-3-substituted-N alkylmorphinans, synthesis and use as anticonvulsant and neuroprotective agents |
| US5607941A (en) * | 1992-06-26 | 1997-03-04 | Boehringer Ingelheim Kg | Useful for treating neurodegenerative diseases |
| US5512593A (en) * | 1993-03-02 | 1996-04-30 | John S. Nagle | Composition and method of treating depression using natoxone or naltrexone in combination with a serotonin reuptake inhibitor |
| NZ326331A (en) * | 1996-01-10 | 2000-01-28 | Smithkline Beecham Spa | Heterocycle-condensed morphinoid derivatives and medicaments |
| GB9912411D0 (en) * | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| DE60133584T2 (de) * | 2000-10-31 | 2009-06-04 | Rensselaer Polytechnic Institute | 4-arylpiperidine als opioidrezeptorbindende agenzien |
| JP5420170B2 (ja) * | 2004-05-14 | 2014-02-19 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | カルボキサミド系オピオイド化合物 |
| US20060063792A1 (en) * | 2004-09-17 | 2006-03-23 | Adolor Corporation | Substituted morphinans and methods of their use |
| RU2480455C2 (ru) * | 2004-11-05 | 2013-04-27 | Ренссилэйер Политекник Инститьют | 4-гидроксибензоморфаны |
| US20070099947A1 (en) * | 2005-11-03 | 2007-05-03 | Alkermes, Inc. | Methods and compositions for the treatment of brain reward system disorders by combination therapy |
| EP1983991A2 (en) * | 2006-02-01 | 2008-10-29 | Alkermes, Inc. | Methods of treating alcoholism and alcohol related disorders using combination drug therapy and swellable polymers |
| JP5581211B2 (ja) * | 2007-08-09 | 2014-08-27 | レンセラール ポリテクニック インスティチュート | 第四級オピオイドカルボキサミド |
| CA2754984C (en) * | 2009-03-19 | 2018-06-26 | Alkermes, Inc. | Morphinan derivatives with high oral bioavailability |
| WO2010141666A2 (en) * | 2009-06-04 | 2010-12-09 | The General Hospital Corporation | Modulating endogenous beta-endorphin levels |
| US9211293B2 (en) * | 2011-12-15 | 2015-12-15 | Alkermes Pharma Ireland Limited | Opioid agonist antagonist combinations |
| JP5929635B2 (ja) * | 2012-08-30 | 2016-06-08 | 株式会社デンソー | 多段式横型鍛造装置 |
-
2009
- 2009-12-04 CA CA2754984A patent/CA2754984C/en active Active
- 2009-12-04 EP EP16193161.3A patent/EP3170395A1/en not_active Withdrawn
- 2009-12-04 JP JP2012500776A patent/JP5555890B2/ja not_active Expired - Fee Related
- 2009-12-04 WO PCT/US2009/066801 patent/WO2010107457A1/en not_active Ceased
- 2009-12-04 EP EP09842019A patent/EP2408303A4/en not_active Withdrawn
- 2009-12-04 AU AU2009342654A patent/AU2009342654B2/en not_active Ceased
-
2010
- 2010-03-19 US US12/727,784 patent/US20100240691A1/en not_active Abandoned
-
2014
- 2014-03-10 JP JP2014046328A patent/JP2014101388A/ja active Pending
- 2014-05-09 JP JP2014097613A patent/JP2014139257A/ja not_active Withdrawn
- 2014-10-06 US US14/506,941 patent/US20150094325A1/en not_active Abandoned
-
2016
- 2016-08-03 JP JP2016153074A patent/JP6362644B2/ja not_active Expired - Fee Related
- 2016-11-17 US US15/354,244 patent/US20170112827A1/en not_active Abandoned
-
2020
- 2020-01-10 US US16/739,262 patent/US20200383970A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| JP2012520877A (ja) | 2012-09-10 |
| EP3170395A1 (en) | 2017-05-24 |
| US20150094325A1 (en) | 2015-04-02 |
| US20170112827A1 (en) | 2017-04-27 |
| US20200383970A1 (en) | 2020-12-10 |
| JP2014139257A (ja) | 2014-07-31 |
| US20100240691A1 (en) | 2010-09-23 |
| EP2408303A4 (en) | 2012-07-25 |
| WO2010107457A1 (en) | 2010-09-23 |
| JP5555890B2 (ja) | 2014-07-23 |
| EP2408303A1 (en) | 2012-01-25 |
| AU2009342654A1 (en) | 2011-10-06 |
| JP2014101388A (ja) | 2014-06-05 |
| AU2009342654B2 (en) | 2013-09-05 |
| CA2754984A1 (en) | 2010-09-23 |
| JP2016185995A (ja) | 2016-10-27 |
| JP6362644B2 (ja) | 2018-07-25 |
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| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |