AU784541B2 - Novel methods and compositions involving opioids and antagonists thereof - Google Patents
Novel methods and compositions involving opioids and antagonists thereof Download PDFInfo
- Publication number
- AU784541B2 AU784541B2 AU39706/01A AU3970601A AU784541B2 AU 784541 B2 AU784541 B2 AU 784541B2 AU 39706/01 A AU39706/01 A AU 39706/01A AU 3970601 A AU3970601 A AU 3970601A AU 784541 B2 AU784541 B2 AU 784541B2
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- alkyl
- hydrogen
- substituted alkyl
- cycloalkyl
- nhch
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- 238000000034 method Methods 0.000 title claims description 189
- 239000000203 mixture Substances 0.000 title claims description 86
- 239000005557 antagonist Substances 0.000 title claims description 7
- 229940005483 opioid analgesics Drugs 0.000 title description 20
- 125000000217 alkyl group Chemical group 0.000 claims description 450
- 229910052739 hydrogen Inorganic materials 0.000 claims description 387
- 239000001257 hydrogen Substances 0.000 claims description 370
- 150000001875 compounds Chemical class 0.000 claims description 282
- 125000003342 alkenyl group Chemical group 0.000 claims description 206
- 150000002431 hydrogen Chemical class 0.000 claims description 198
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 163
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 144
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 143
- 125000003118 aryl group Chemical group 0.000 claims description 97
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 86
- 125000003107 substituted aryl group Chemical group 0.000 claims description 84
- 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 claims description 82
- 230000002093 peripheral effect Effects 0.000 claims description 80
- 125000002947 alkylene group Chemical group 0.000 claims description 73
- 125000000623 heterocyclic group Chemical group 0.000 claims description 73
- 229910052757 nitrogen Inorganic materials 0.000 claims description 73
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 72
- 239000002623 mu opiate receptor antagonist Substances 0.000 claims description 71
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- 150000003839 salts Chemical class 0.000 claims description 40
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 23
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- TVYLLZQTGLZFBW-GOEBONIOSA-N tramadol Natural products COC1=CC=CC([C@@]2(O)[C@@H](CCCC2)CN(C)C)=C1 TVYLLZQTGLZFBW-GOEBONIOSA-N 0.000 claims description 17
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims description 14
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- SVSARCCKBMZNMR-UHFFFAOYSA-N [1-[2-[methyl-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethyl]amino]ethyl]pyridin-4-ylidene]methyl-oxoazanium;dichloride Chemical compound [Cl-].[Cl-].C1=CC(=C[NH+]=O)C=CN1CCN(C)CCN1C=CC(=C[NH+]=O)C=C1 SVSARCCKBMZNMR-UHFFFAOYSA-N 0.000 claims description 12
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- 230000008673 vomiting Effects 0.000 claims description 11
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims description 10
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- IDBPHNDTYPBSNI-UHFFFAOYSA-N N-(1-(2-(4-Ethyl-5-oxo-2-tetrazolin-1-yl)ethyl)-4-(methoxymethyl)-4-piperidyl)propionanilide Chemical compound C1CN(CCN2C(N(CC)N=N2)=O)CCC1(COC)N(C(=O)CC)C1=CC=CC=C1 IDBPHNDTYPBSNI-UHFFFAOYSA-N 0.000 claims description 9
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- RMRJXGBAOAMLHD-IHFGGWKQSA-N buprenorphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]11CC[C@]3([C@H](C1)[C@](C)(O)C(C)(C)C)OC)CN2CC1CC1 RMRJXGBAOAMLHD-IHFGGWKQSA-N 0.000 claims description 9
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- IFKLAQQSCNILHL-QHAWAJNXSA-N butorphanol Chemical compound N1([C@@H]2CC3=CC=C(C=C3[C@@]3([C@]2(CCCC3)O)CC1)O)CC1CCC1 IFKLAQQSCNILHL-QHAWAJNXSA-N 0.000 claims description 9
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- WVLOADHCBXTIJK-YNHQPCIGSA-N hydromorphone Chemical compound O([C@H]1C(CC[C@H]23)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O WVLOADHCBXTIJK-YNHQPCIGSA-N 0.000 claims description 9
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- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 6
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Classifications
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- 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
- A61K31/4748—Quinolines; Isoquinolines forming part of bridged ring systems
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
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- 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
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- 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
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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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US45080699A | 1999-11-29 | 1999-11-29 | |
| US09/450806 | 1999-11-29 | ||
| PCT/US2000/042315 WO2001037785A2 (en) | 1999-11-29 | 2000-11-29 | Novel methods and compositions involving opioids and antagonists thereof |
Publications (2)
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| AU3970601A AU3970601A (en) | 2001-06-04 |
| AU784541B2 true AU784541B2 (en) | 2006-04-27 |
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| AU39706/01A Ceased AU784541B2 (en) | 1999-11-29 | 2000-11-29 | Novel methods and compositions involving opioids and antagonists thereof |
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| EP (1) | EP1244447B1 (https=) |
| JP (1) | JP2003528819A (https=) |
| AU (1) | AU784541B2 (https=) |
| CA (1) | CA2392362A1 (https=) |
| CY (1) | CY1106359T1 (https=) |
| DE (1) | DE60032940T2 (https=) |
| DK (1) | DK1244447T3 (https=) |
| ES (1) | ES2278647T3 (https=) |
| IL (2) | IL149600A0 (https=) |
| MX (1) | MXPA02005335A (https=) |
| NZ (1) | NZ518562A (https=) |
| PT (1) | PT1244447E (https=) |
| WO (1) | WO2001037785A2 (https=) |
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| US6274591B1 (en) | 1997-11-03 | 2001-08-14 | Joseph F. Foss | Use of methylnaltrexone and related compounds |
| EP1041987B1 (en) | 1997-12-22 | 2006-04-19 | Euro-Celtique S.A. | Pharmaceutical oral dosage form comprising a combination of an opioid agonist and naltrexone |
| EP2092936B1 (en) | 2000-02-08 | 2013-03-20 | Euro-Celtique S.A. | Tamper-resistant oral opioid agonist formulations |
| EP1387673B1 (en) | 2001-05-11 | 2010-12-29 | Endo Pharmaceuticals Inc. | Abuse-resistant controlled-release opioid dosage form |
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- 2000-11-29 DK DK00992256T patent/DK1244447T3/da active
- 2000-11-29 DE DE60032940T patent/DE60032940T2/de not_active Expired - Lifetime
- 2000-11-29 IL IL14960000A patent/IL149600A0/xx unknown
- 2000-11-29 ES ES00992256T patent/ES2278647T3/es not_active Expired - Lifetime
- 2000-11-29 JP JP2001539402A patent/JP2003528819A/ja active Pending
- 2000-11-29 WO PCT/US2000/042315 patent/WO2001037785A2/en not_active Ceased
- 2000-11-29 EP EP00992256A patent/EP1244447B1/en not_active Expired - Lifetime
- 2000-11-29 CA CA002392362A patent/CA2392362A1/en not_active Abandoned
- 2000-11-29 AU AU39706/01A patent/AU784541B2/en not_active Ceased
- 2000-11-29 MX MXPA02005335A patent/MXPA02005335A/es active IP Right Grant
- 2000-11-29 PT PT00992256T patent/PT1244447E/pt unknown
-
2002
- 2002-05-12 IL IL149600A patent/IL149600A/en not_active IP Right Cessation
-
2007
- 2007-03-07 CY CY20071100318T patent/CY1106359T1/el unknown
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4457933A (en) * | 1980-01-24 | 1984-07-03 | Bristol-Myers Company | Prevention of analgesic abuse |
| US4582835A (en) * | 1983-12-06 | 1986-04-15 | Reckitt & Colman Products Limited | Analgesic compositions |
| US4769372A (en) * | 1986-06-18 | 1988-09-06 | The Rockefeller University | Method of treating patients suffering from chronic pain or chronic cough |
Also Published As
| Publication number | Publication date |
|---|---|
| IL149600A0 (en) | 2002-11-10 |
| EP1244447A4 (en) | 2003-06-04 |
| EP1244447B1 (en) | 2007-01-10 |
| CA2392362A1 (en) | 2001-05-31 |
| WO2001037785A3 (en) | 2002-01-10 |
| CY1106359T1 (el) | 2011-10-12 |
| ES2278647T3 (es) | 2007-08-16 |
| JP2003528819A (ja) | 2003-09-30 |
| MXPA02005335A (es) | 2003-01-28 |
| NZ518562A (en) | 2005-04-29 |
| WO2001037785A9 (en) | 2002-08-29 |
| IL149600A (en) | 2010-06-16 |
| DE60032940D1 (de) | 2007-02-22 |
| EP1244447A2 (en) | 2002-10-02 |
| PT1244447E (pt) | 2007-02-28 |
| DE60032940T2 (de) | 2007-11-08 |
| AU3970601A (en) | 2001-06-04 |
| WO2001037785A2 (en) | 2001-05-31 |
| DK1244447T3 (da) | 2007-04-23 |
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