DE60313478T2 - N-substituierte hydromorphone und ihre anwendung - Google Patents
N-substituierte hydromorphone und ihre anwendung Download PDFInfo
- Publication number
- DE60313478T2 DE60313478T2 DE60313478T DE60313478T DE60313478T2 DE 60313478 T2 DE60313478 T2 DE 60313478T2 DE 60313478 T DE60313478 T DE 60313478T DE 60313478 T DE60313478 T DE 60313478T DE 60313478 T2 DE60313478 T2 DE 60313478T2
- Authority
- DE
- Germany
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- pain
- cation
- medicament
- 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.)
- Expired - Lifetime
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- WVLOADHCBXTIJK-YNHQPCIGSA-N hydromorphone Chemical class O([C@H]1C(CC[C@H]23)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O WVLOADHCBXTIJK-YNHQPCIGSA-N 0.000 title claims abstract description 13
- 229960001410 hydromorphone Drugs 0.000 title claims description 10
- 150000003839 salts Chemical class 0.000 claims abstract description 53
- 208000002193 Pain Diseases 0.000 claims abstract description 43
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- 108020001612 μ-opioid receptors Proteins 0.000 claims abstract description 19
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- 230000002265 prevention Effects 0.000 claims abstract description 5
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- -1 organic acid salt Chemical class 0.000 claims description 11
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- 125000000217 alkyl group Chemical group 0.000 claims description 5
- 150000004820 halides Chemical group 0.000 claims description 5
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 claims description 5
- INQOMBQAUSQDDS-UHFFFAOYSA-N iodomethane Chemical compound IC INQOMBQAUSQDDS-UHFFFAOYSA-N 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
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- 231100000765 toxin Toxicity 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 229940078499 tricalcium phosphate Drugs 0.000 description 1
- 235000019731 tricalcium phosphate Nutrition 0.000 description 1
- 229910000391 tricalcium phosphate Inorganic materials 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 208000009852 uremia Diseases 0.000 description 1
- 208000030401 vitamin deficiency disease Diseases 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- 229940100445 wheat starch Drugs 0.000 description 1
- 210000002268 wool Anatomy 0.000 description 1
- 108020001588 κ-opioid receptors Proteins 0.000 description 1
Classifications
-
- 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
- C07D489/04—Salts; Organic complexes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/14—Antitussive agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/16—Central respiratory analeptics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Neurosurgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41325402P | 2002-09-25 | 2002-09-25 | |
| US413254P | 2002-09-25 | ||
| PCT/US2003/029876 WO2004029059A1 (en) | 2002-09-25 | 2003-09-24 | N-substituted hydromorphones and the use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60313478D1 DE60313478D1 (de) | 2007-06-06 |
| DE60313478T2 true DE60313478T2 (de) | 2008-01-03 |
Family
ID=32043224
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60313478T Expired - Lifetime DE60313478T2 (de) | 2002-09-25 | 2003-09-24 | N-substituierte hydromorphone und ihre anwendung |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US6825205B2 (https=) |
| EP (2) | EP1543010B1 (https=) |
| JP (2) | JP4806190B2 (https=) |
| KR (1) | KR20050074462A (https=) |
| CN (1) | CN100387600C (https=) |
| AT (1) | ATE360633T1 (https=) |
| AU (1) | AU2003272642B2 (https=) |
| BR (1) | BR0314488A (https=) |
| CA (1) | CA2500118C (https=) |
| CY (1) | CY1106697T1 (https=) |
| DE (1) | DE60313478T2 (https=) |
| DK (1) | DK1543010T3 (https=) |
| ES (1) | ES2286461T3 (https=) |
| MX (1) | MXPA05003104A (https=) |
| NZ (1) | NZ538726A (https=) |
| PT (1) | PT1543010E (https=) |
| WO (1) | WO2004029059A1 (https=) |
| ZA (1) | ZA200502174B (https=) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040202717A1 (en) | 2003-04-08 | 2004-10-14 | Mehta Atul M. | Abuse-resistant oral dosage forms and method of use thereof |
| US20070185145A1 (en) * | 2006-02-03 | 2007-08-09 | Royds Robert B | Pharmaceutical composition containing a central opioid agonist, a central opioid antagonist, and a peripheral opioid antagonist, and method for making the same |
| EP2099764B1 (en) | 2006-09-20 | 2011-07-27 | Mallinckrodt Inc. | Preparation of substituted morphinan-6-ones and salts and intermediates thereof |
| EP2101774A2 (en) * | 2006-11-22 | 2009-09-23 | Progenics Pharmaceuticals, Inc. | 7,8-saturated-4,5-epoxy-morphinanium analogs |
| BRPI0719327A2 (pt) * | 2006-11-22 | 2014-02-04 | Progenics Pharm Inc | N-óxidos de análogos de 4,5-epóxi-morfinano |
| EP2137189B1 (en) * | 2007-03-06 | 2015-05-06 | Mallinckrodt LLC | Process for the preparation of quaternary n-alkyl morphinan alkaloid salts |
| US9040726B2 (en) | 2007-03-06 | 2015-05-26 | Mallinckrodt Llc | Process for the preparation of quaternary N-alkyl morphinan alkaloid salts |
| AU2008286979B2 (en) * | 2007-08-09 | 2013-03-28 | Rensselaer Polytechnic Institute | Quaternary opioid carboxamides |
| JP2011500686A (ja) * | 2007-10-18 | 2011-01-06 | アイコ バイオテクノロジー | オピオイドと中性アンタゴニストを用いる組合せ鎮痛剤 |
| US8748448B2 (en) | 2007-10-18 | 2014-06-10 | Aiko Biotechnology | Combination analgesic employing opioid agonist and neutral antagonist |
| WO2009070733A1 (en) * | 2007-11-26 | 2009-06-04 | Pharmacofore, Inc. | Peripheral phenolic opioid antagonist |
| US8148528B2 (en) | 2008-05-27 | 2012-04-03 | Mallinckrodt Llc | Processes and compounds for the preparation of normorphinans |
| EP2331508B1 (en) | 2008-09-03 | 2014-11-12 | Mallinckrodt LLC | Substituted berbines and processes for their synthesis |
| ES2566828T3 (es) | 2010-09-21 | 2016-04-15 | Purdue Pharma L.P. | Análogos de buprenorfina como agonistas y/o antagonistas del receptor opioide |
| EP2917182B1 (en) | 2012-11-09 | 2018-01-03 | Purdue Pharma LP | Benzomorphan analogs and the use thereof |
| JP6182620B2 (ja) | 2013-01-31 | 2017-08-16 | パーデュー、ファーマ、リミテッド、パートナーシップ | ベンゾモルファン類似体およびその使用 |
| US8969358B2 (en) | 2013-03-15 | 2015-03-03 | Purdue Pharma L.P. | Buprenorphine analogs |
| WO2015097545A1 (en) | 2013-12-26 | 2015-07-02 | Purdue Pharma L.P. | Opioid receptor modulating oxabicyclo[2.2.2]octane morphinans |
| WO2015097548A1 (en) | 2013-12-26 | 2015-07-02 | Purdue Pharma L.P. | 7-beta-alkyl analogs of orvinols |
| WO2015097547A1 (en) | 2013-12-26 | 2015-07-02 | Purdue Pharma L.P. | 10-substituted morphinan hydantoins |
| EP3087057A4 (en) | 2013-12-26 | 2017-06-28 | Purdue Pharma LP | Ring-contracted morphinans and the use thereof |
| WO2015099863A1 (en) | 2013-12-27 | 2015-07-02 | Purdue Pharma L.P. | 6-substituted and 7-substituted morphinan analogs and the use thereof |
| CA2950567A1 (en) | 2014-05-27 | 2015-12-03 | Purdue Pharma L.P. | Spirocyclic morphinans and use thereof |
| MA40171A (fr) | 2014-06-13 | 2017-04-19 | Purdue Pharma Lp | Dérivés d'azamophinan et leur utilisation |
| MA41125A (fr) | 2014-12-05 | 2017-10-10 | Purdue Pharma Lp | Dérivés de 6.7-cyclomorphinane et leur utilisation |
| WO2018125716A1 (en) | 2017-01-02 | 2018-07-05 | Purdue Pharma L.P. | Morphinan derivatives and use thereof |
| CN117567477A (zh) * | 2023-11-15 | 2024-02-20 | 宜昌人福药业有限责任公司 | 一种氢吗啡酮和二氢吗啡类药物低分子聚乙二醇化物及其制备方法和应用 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3536809A (en) | 1969-02-17 | 1970-10-27 | Alza Corp | Medication method |
| US3598123A (en) | 1969-04-01 | 1971-08-10 | Alza Corp | Bandage for administering drugs |
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US3916899A (en) | 1973-04-25 | 1975-11-04 | Alza Corp | Osmotic dispensing device with maximum and minimum sizes for the passageway |
| US4008719A (en) | 1976-02-02 | 1977-02-22 | Alza Corporation | Osmotic system having laminar arrangement for programming delivery of active agent |
| US4176186A (en) * | 1978-07-28 | 1979-11-27 | Boehringer Ingelheim Gmbh | Quaternary derivatives of noroxymorphone which relieve intestinal immobility |
| IE58110B1 (en) | 1984-10-30 | 1993-07-14 | Elan Corp Plc | Controlled release powder and process for its preparation |
| EP0306575B1 (en) * | 1987-09-10 | 1992-07-29 | The University Of Chicago | Quaternary derivatives of noroxymorphone which relieve nausea and emesis |
| US5073543A (en) | 1988-07-21 | 1991-12-17 | G. D. Searle & Co. | Controlled release formulations of trophic factors in ganglioside-lipsome vehicle |
| IT1229203B (it) | 1989-03-22 | 1991-07-25 | Bioresearch Spa | Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative. |
| US5120548A (en) | 1989-11-07 | 1992-06-09 | Merck & Co., Inc. | Swelling modulated polymeric drug delivery device |
| US5733566A (en) | 1990-05-15 | 1998-03-31 | Alkermes Controlled Therapeutics Inc. Ii | Controlled release of antiparasitic agents in animals |
| US5698155A (en) | 1991-05-31 | 1997-12-16 | Gs Technologies, Inc. | Method for the manufacture of pharmaceutical cellulose capsules |
| US5968551A (en) | 1991-12-24 | 1999-10-19 | Purdue Pharma L.P. | Orally administrable opioid formulations having extended duration of effect |
| US5580578A (en) | 1992-01-27 | 1996-12-03 | Euro-Celtique, S.A. | Controlled release formulations coated with aqueous dispersions of acrylic polymers |
| US5591767A (en) | 1993-01-25 | 1997-01-07 | Pharmetrix Corporation | Liquid reservoir transdermal patch for the administration of ketorolac |
| IT1270594B (it) | 1994-07-07 | 1997-05-07 | Recordati Chem Pharm | Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida |
| DE69732868T2 (de) * | 1996-11-25 | 2006-04-13 | Toray Industries, Inc. | Mittel gegen Juckreiz |
| WO2001014382A1 (en) * | 1999-08-23 | 2001-03-01 | Toray Industries, Inc. | Analgesics containing as the active ingredient quaternary ammonium salt derivatives of morphinan |
-
2003
- 2003-09-24 PT PT03754837T patent/PT1543010E/pt unknown
- 2003-09-24 WO PCT/US2003/029876 patent/WO2004029059A1/en not_active Ceased
- 2003-09-24 AU AU2003272642A patent/AU2003272642B2/en not_active Ceased
- 2003-09-24 JP JP2004540164A patent/JP4806190B2/ja not_active Expired - Fee Related
- 2003-09-24 NZ NZ538726A patent/NZ538726A/en not_active IP Right Cessation
- 2003-09-24 AT AT03754837T patent/ATE360633T1/de active
- 2003-09-24 DK DK03754837T patent/DK1543010T3/da active
- 2003-09-24 CN CNB038229587A patent/CN100387600C/zh not_active Expired - Fee Related
- 2003-09-24 EP EP03754837A patent/EP1543010B1/en not_active Expired - Lifetime
- 2003-09-24 DE DE60313478T patent/DE60313478T2/de not_active Expired - Lifetime
- 2003-09-24 EP EP07007240A patent/EP1803724A1/en not_active Withdrawn
- 2003-09-24 CA CA2500118A patent/CA2500118C/en not_active Expired - Fee Related
- 2003-09-24 US US10/668,326 patent/US6825205B2/en not_active Expired - Lifetime
- 2003-09-24 KR KR1020057005255A patent/KR20050074462A/ko not_active Ceased
- 2003-09-24 BR BR0314488-7A patent/BR0314488A/pt not_active IP Right Cessation
- 2003-09-24 MX MXPA05003104A patent/MXPA05003104A/es active IP Right Grant
- 2003-09-24 ES ES03754837T patent/ES2286461T3/es not_active Expired - Lifetime
-
2005
- 2005-03-15 ZA ZA200502174A patent/ZA200502174B/en unknown
-
2007
- 2007-07-03 CY CY20071100881T patent/CY1106697T1/el unknown
-
2010
- 2010-10-28 JP JP2010242645A patent/JP2011042681A/ja not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| NZ538726A (en) | 2006-11-30 |
| CN1684967A (zh) | 2005-10-19 |
| BR0314488A (pt) | 2005-08-02 |
| MXPA05003104A (es) | 2005-05-27 |
| US6825205B2 (en) | 2004-11-30 |
| EP1543010B1 (en) | 2007-04-25 |
| ATE360633T1 (de) | 2007-05-15 |
| PT1543010E (pt) | 2007-07-26 |
| AU2003272642B2 (en) | 2009-07-09 |
| AU2003272642A1 (en) | 2004-04-19 |
| CA2500118A1 (en) | 2004-04-08 |
| JP2011042681A (ja) | 2011-03-03 |
| CY1106697T1 (el) | 2012-05-23 |
| CA2500118C (en) | 2011-04-12 |
| ES2286461T3 (es) | 2007-12-01 |
| EP1803724A1 (en) | 2007-07-04 |
| JP2006503850A (ja) | 2006-02-02 |
| JP4806190B2 (ja) | 2011-11-02 |
| DK1543010T3 (da) | 2007-09-17 |
| WO2004029059A1 (en) | 2004-04-08 |
| KR20050074462A (ko) | 2005-07-18 |
| CN100387600C (zh) | 2008-05-14 |
| HK1080456A1 (en) | 2006-04-28 |
| ZA200502174B (en) | 2006-05-31 |
| EP1543010A1 (en) | 2005-06-22 |
| DE60313478D1 (de) | 2007-06-06 |
| US20040067973A1 (en) | 2004-04-08 |
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