ES2174490T3 - Sales de adicion de acido de alcaloide de morfina y su utilizacion. - Google Patents
Sales de adicion de acido de alcaloide de morfina y su utilizacion.Info
- Publication number
- ES2174490T3 ES2174490T3 ES98945312T ES98945312T ES2174490T3 ES 2174490 T3 ES2174490 T3 ES 2174490T3 ES 98945312 T ES98945312 T ES 98945312T ES 98945312 T ES98945312 T ES 98945312T ES 2174490 T3 ES2174490 T3 ES 2174490T3
- Authority
- ES
- Spain
- Prior art keywords
- group
- acids
- substituted
- atom
- optionally substituted
- 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
Links
- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical compound O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 title abstract 3
- -1 methanol Chemical class 0.000 abstract 5
- 239000002253 acid Substances 0.000 abstract 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 abstract 3
- 150000007513 acids Chemical class 0.000 abstract 2
- 150000001559 benzoic acids Chemical group 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 229930013053 morphinan alkaloid Natural products 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 150000007524 organic acids Chemical class 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 150000001298 alcohols Chemical class 0.000 abstract 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 150000001413 amino acids Chemical group 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 235000010233 benzoic acid Nutrition 0.000 abstract 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001735 carboxylic acids Chemical group 0.000 abstract 1
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 abstract 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 150000001991 dicarboxylic acids Chemical class 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
- ODUCDPQEXGNKDN-UHFFFAOYSA-N nitroxyl Chemical group O=N ODUCDPQEXGNKDN-UHFFFAOYSA-N 0.000 abstract 1
- 230000035699 permeability Effects 0.000 abstract 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 abstract 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 150000003460 sulfonic acids Chemical class 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 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
- A61P23/00—Anaesthetics
- A61P23/02—Local anaesthetics
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Addiction (AREA)
- Anesthesiology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
Abstract
Sales de adición de ácido de alcaloide de morfina y ácido orgánico, presentando el alcaloide de morfina la fórmula I siguiente: (I) en donde R 1 está seleccionado entre el grupo compuesto por H, radicales alquilo C1aC6-, preferentemente los metilo, etilo, propilo, isopropilo, C(O)CH3, R 2 está seleccionado entre el grupo compuesto por los radicales monovalentes H, OH, OC(O)CH3, estando en este caso la cuarta valencia del átomo de C (6) ocupada por H, o por los radicales divalentes =O, =CH2, R 3 está seleccionado entre el grupo compuesto por -CH3, ciclopropilo, ciclobutilo y alilo, así como pudiendo estar saturado el enlace entre C7/C8 o haber un grupo nitroxilo en N17, caracterizadas por estar seleccionado el ácido orgánico entre los: monoésteres de ácidos dicarboxílicos C3 a C18 con alcoholes monovalentes C1 a C4, particularmente metanol, ácidos sulfónicos C2 a C6 ó C8 a C16, ácidos del grupo de los ácidos benzoicos sustituidos con grupos halógeno, py mhidroxilo, alquilo, hidroxialquilo, alcoxialquilo y/o alcoxi, así como de los ácidos benzoicos alquilados aminosustituidos unidos facultativamente al átomo de N, heterociclos de 5 ó 6 anillos sustituidos o no sustituidos con al menos un átomo de N o de S y con una función de grupo carboxilo como sustituyente, especialmente un grupo carboxilo, carboximetilo, carboxietilo o los grupos carboxipropilo o carboxibutilo ramicados facultativamente, ácidos oxocarboxílicos de 5 a lo átomos de C saturados o insaturados y facultativamente sustituidos, ácidos carboxílicos saturados C2 a C4 sustituidos con grupos fenoxi, aminoácidos alifáticos, aromáticos o heterocíclicos C2-C12, en donde hay un grupo amino sustituido con un grupo alcanoilo C2C6 facultativamente sustituido, o con un grupo benzoilo facultativamente sustituido, y por poseer la sal de adición de ácido una permeabilidad a través de la piel con un flujo de al menos 2,34 g/cm 2 h.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19742296 | 1997-09-25 | ||
| DE19834005A DE19834005A1 (de) | 1997-09-25 | 1998-07-29 | Säureadditionssalze von Morphin-Alkaloiden und deren Verwendung |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2174490T3 true ES2174490T3 (es) | 2002-11-01 |
Family
ID=26040297
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES98945312T Expired - Lifetime ES2174490T3 (es) | 1997-09-25 | 1998-09-05 | Sales de adicion de acido de alcaloide de morfina y su utilizacion. |
Country Status (20)
| Country | Link |
|---|---|
| EP (1) | EP1017696B1 (es) |
| JP (1) | JP2001517669A (es) |
| AT (1) | ATE214702T1 (es) |
| AU (1) | AU741434B2 (es) |
| CA (1) | CA2304722C (es) |
| CZ (1) | CZ300532B6 (es) |
| DK (1) | DK1017696T3 (es) |
| ES (1) | ES2174490T3 (es) |
| HU (1) | HUP0003686A3 (es) |
| ID (1) | ID26296A (es) |
| IL (1) | IL134787A (es) |
| MX (1) | MXPA00002658A (es) |
| NO (1) | NO20001465L (es) |
| NZ (1) | NZ503459A (es) |
| PL (1) | PL193321B1 (es) |
| PT (1) | PT1017696E (es) |
| SK (1) | SK4322000A3 (es) |
| TR (1) | TR200000653T2 (es) |
| TW (1) | TW576836B (es) |
| WO (1) | WO1999015528A1 (es) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9924797D0 (en) | 1999-10-20 | 1999-12-22 | West Pharm Serv Drug Res Ltd | Compound |
| GB0218811D0 (en) * | 2002-08-14 | 2002-09-18 | Cenes Ltd | Salts of morphine-6-glucuronide |
| DE102006054732B4 (de) | 2006-11-21 | 2010-12-30 | Lts Lohmann Therapie-Systeme Ag | Transdermales therapeutisches System mit Ionenpaar-Mikroreservoiren |
| JP5544544B2 (ja) * | 2008-08-05 | 2014-07-09 | 株式会社 メドレックス | 塩基性薬効成分の脂肪酸塩、安息香酸塩を含有する外用剤とその製造方法 |
| CA2842370C (en) * | 2011-08-02 | 2020-03-24 | Mallinckrodt Llc | Stepwise process for the production of alkaloid salts |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE524639C (de) * | 1929-05-25 | 1931-05-09 | Chem Fab Vorm Sandoz | Verfahren zur Darstellung von leichtloeslichen Salzen des Benzylmorphons |
| DE728804C (de) * | 1935-04-02 | 1942-12-03 | Jean Lucien Regnier | Verfahren zur Herstellung von Salzen des Morphins mit Aralkylcarbonsaeuren |
| DE1172267B (de) * | 1961-09-19 | 1964-06-18 | Dausse S A Lab | Verfahren zur Herstellung des bis-guajakol-sulfonsauren Salzes des Morphin-ª‰-morpholyl-aethylaethers |
| FR6598M (es) * | 1967-07-28 | 1969-01-06 | ||
| US4626539A (en) * | 1984-08-10 | 1986-12-02 | E. I. Dupont De Nemours And Company | Trandermal delivery of opioids |
| US4908389A (en) * | 1986-08-27 | 1990-03-13 | Warner-Lambert Company | Penetration enhancement system |
| US4879297A (en) * | 1987-06-01 | 1989-11-07 | Warner-Lambert Company | Fatty acids and their small chain esters as penetration enhancers in aqueous systems |
| US5374645A (en) * | 1990-01-22 | 1994-12-20 | Ciba-Geigy Corporation | Transdermal administation of ionic pharmaceutically active agents via aqueous isopropanol |
| TW225536B (es) * | 1990-08-23 | 1994-06-21 | Ciba Geigy Ag | |
| FR2708611B1 (fr) * | 1993-07-29 | 1995-10-27 | Meram Lab | Sel de codéine de l'acide 2-(3-benzoylphényl)propionique, procédé d'obtention et compositions pharmaceutiques le contenant. |
| DE19607395C2 (de) * | 1996-02-28 | 2002-11-21 | Lohmann Therapie Syst Lts | Salze aus einem kationischen narkotischen Analgetikum mit einem anionischen nichtnarkotischen Analgetikum, Verfahren zu deren Herstellung und die diese Salze enthaltenden pharmazeutischen Präparate |
-
1998
- 1998-09-05 JP JP2000512833A patent/JP2001517669A/ja active Pending
- 1998-09-05 AU AU92666/98A patent/AU741434B2/en not_active Ceased
- 1998-09-05 PL PL339516A patent/PL193321B1/pl not_active IP Right Cessation
- 1998-09-05 TR TR2000/00653T patent/TR200000653T2/xx unknown
- 1998-09-05 EP EP98945312A patent/EP1017696B1/de not_active Expired - Lifetime
- 1998-09-05 SK SK432-2000A patent/SK4322000A3/sk unknown
- 1998-09-05 AT AT98945312T patent/ATE214702T1/de active
- 1998-09-05 NZ NZ503459A patent/NZ503459A/en not_active IP Right Cessation
- 1998-09-05 PT PT98945312T patent/PT1017696E/pt unknown
- 1998-09-05 HU HU0003686A patent/HUP0003686A3/hu unknown
- 1998-09-05 MX MXPA00002658A patent/MXPA00002658A/es active IP Right Grant
- 1998-09-05 WO PCT/EP1998/005652 patent/WO1999015528A1/de not_active Ceased
- 1998-09-05 IL IL134787A patent/IL134787A/en not_active IP Right Cessation
- 1998-09-05 ID IDW20000549A patent/ID26296A/id unknown
- 1998-09-05 ES ES98945312T patent/ES2174490T3/es not_active Expired - Lifetime
- 1998-09-05 DK DK98945312T patent/DK1017696T3/da active
- 1998-09-05 CA CA002304722A patent/CA2304722C/en not_active Expired - Fee Related
- 1998-09-05 CZ CZ20001048A patent/CZ300532B6/cs not_active IP Right Cessation
- 1998-09-23 TW TW087115805A patent/TW576836B/zh not_active IP Right Cessation
-
2000
- 2000-03-21 NO NO20001465A patent/NO20001465L/no unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL134787A0 (en) | 2001-04-30 |
| EP1017696A1 (de) | 2000-07-12 |
| PL193321B1 (pl) | 2007-01-31 |
| TW576836B (en) | 2004-02-21 |
| ID26296A (id) | 2000-12-14 |
| CA2304722C (en) | 2005-11-22 |
| CZ300532B6 (cs) | 2009-06-10 |
| DK1017696T3 (da) | 2002-07-08 |
| CZ20001048A3 (cs) | 2000-08-16 |
| AU9266698A (en) | 1999-04-12 |
| NO20001465D0 (no) | 2000-03-21 |
| JP2001517669A (ja) | 2001-10-09 |
| AU741434B2 (en) | 2001-11-29 |
| HUP0003686A3 (en) | 2003-04-28 |
| NZ503459A (en) | 2001-12-21 |
| PL339516A1 (en) | 2000-12-18 |
| CA2304722A1 (en) | 1999-04-01 |
| IL134787A (en) | 2007-05-15 |
| WO1999015528A1 (de) | 1999-04-01 |
| MXPA00002658A (es) | 2004-03-10 |
| TR200000653T2 (tr) | 2000-07-21 |
| NO20001465L (no) | 2000-03-21 |
| EP1017696B1 (de) | 2002-03-20 |
| HUP0003686A2 (hu) | 2001-09-28 |
| ATE214702T1 (de) | 2002-04-15 |
| PT1017696E (pt) | 2002-09-30 |
| SK4322000A3 (en) | 2000-10-09 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG2A | Definitive protection |
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