DE60215195T2 - Derivate morphinähnlicher opioidverbindungen - Google Patents
Derivate morphinähnlicher opioidverbindungen Download PDFInfo
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- DE60215195T2 DE60215195T2 DE60215195T DE60215195T DE60215195T2 DE 60215195 T2 DE60215195 T2 DE 60215195T2 DE 60215195 T DE60215195 T DE 60215195T DE 60215195 T DE60215195 T DE 60215195T DE 60215195 T2 DE60215195 T2 DE 60215195T2
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- 150000001875 compounds Chemical class 0.000 title claims abstract description 148
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- 239000000203 mixture Substances 0.000 claims abstract description 24
- 238000011282 treatment Methods 0.000 claims abstract description 20
- 230000002829 reductive effect Effects 0.000 claims abstract description 16
- 150000003839 salts Chemical class 0.000 claims abstract description 15
- 208000024891 symptom Diseases 0.000 claims abstract description 13
- 102000003840 Opioid Receptors Human genes 0.000 claims abstract description 11
- 108090000137 Opioid Receptors Proteins 0.000 claims abstract description 11
- 230000008569 process Effects 0.000 claims abstract description 7
- 230000004913 activation Effects 0.000 claims abstract description 6
- 239000000651 prodrug Substances 0.000 claims abstract description 4
- 229940002612 prodrug Drugs 0.000 claims abstract description 4
- 239000012453 solvate Substances 0.000 claims abstract description 3
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- 229910052757 nitrogen Inorganic materials 0.000 claims description 43
- 125000000217 alkyl group Chemical group 0.000 claims description 34
- 125000003118 aryl group Chemical group 0.000 claims description 31
- 125000000623 heterocyclic group Chemical group 0.000 claims description 31
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- 125000004432 carbon atom Chemical group C* 0.000 claims description 18
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- ALFGKMXHOUSVAD-UHFFFAOYSA-N Ketobemidone Chemical compound C=1C=CC(O)=CC=1C1(C(=O)CC)CCN(C)CC1 ALFGKMXHOUSVAD-UHFFFAOYSA-N 0.000 claims description 2
- BRUQQQPBMZOVGD-XFKAJCMBSA-N Oxycodone Chemical compound O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(OC)C2=C5[C@@]13CCN4C BRUQQQPBMZOVGD-XFKAJCMBSA-N 0.000 claims description 2
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- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 1
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- 125000001181 organosilyl group Chemical group [SiH3]* 0.000 description 1
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- 125000002971 oxazolyl group Chemical group 0.000 description 1
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- 239000000312 peanut oil Substances 0.000 description 1
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N pentanoic acid group Chemical class C(CCCC)(=O)O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 description 1
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- WLJVXDMOQOGPHL-UHFFFAOYSA-N phenylacetic acid Chemical compound OC(=O)CC1=CC=CC=C1 WLJVXDMOQOGPHL-UHFFFAOYSA-N 0.000 description 1
- 150000008105 phosphatidylcholines Chemical class 0.000 description 1
- 150000003904 phospholipids Chemical class 0.000 description 1
- 229910052698 phosphorus Inorganic materials 0.000 description 1
- 239000011574 phosphorus Substances 0.000 description 1
- 230000001766 physiological effect Effects 0.000 description 1
- 230000005371 pilomotor reflex Effects 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 description 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
- 229920000136 polysorbate Polymers 0.000 description 1
- 239000013641 positive control Substances 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
- 229960003415 propylparaben Drugs 0.000 description 1
- 208000005333 pulmonary edema Diseases 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 125000002098 pyridazinyl group Chemical group 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 150000003235 pyrrolidines Chemical class 0.000 description 1
- 125000001422 pyrrolinyl group Chemical group 0.000 description 1
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- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
- 235000019204 saccharin Nutrition 0.000 description 1
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- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
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- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
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- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
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- 239000004299 sodium benzoate Substances 0.000 description 1
- 229960003885 sodium benzoate Drugs 0.000 description 1
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- 229910001467 sodium calcium phosphate Inorganic materials 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- 239000008279 sol Substances 0.000 description 1
- 238000001179 sorption measurement Methods 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 210000000278 spinal cord Anatomy 0.000 description 1
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- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000007929 subcutaneous injection Substances 0.000 description 1
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- 150000008163 sugars Chemical class 0.000 description 1
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- 235000020357 syrup Nutrition 0.000 description 1
- 239000003760 tallow Substances 0.000 description 1
- ILMRJRBKQSSXGY-UHFFFAOYSA-N tert-butyl(dimethyl)silicon Chemical group C[Si](C)C(C)(C)C ILMRJRBKQSSXGY-UHFFFAOYSA-N 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- 125000001984 thiazolidinyl group Chemical group 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 239000004408 titanium dioxide Substances 0.000 description 1
- AOBORMOPSGHCAX-DGHZZKTQSA-N tocofersolan Chemical compound OCCOC(=O)CCC(=O)OC1=C(C)C(C)=C2O[C@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C AOBORMOPSGHCAX-DGHZZKTQSA-N 0.000 description 1
- 229960000984 tocofersolan Drugs 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 125000004385 trihaloalkyl group Chemical group 0.000 description 1
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- PTLOPIHJOPWUNN-UHFFFAOYSA-N triphenyl(phenylimino)-$l^{5}-phosphane Chemical compound C1=CC=CC=C1N=P(C=1C=CC=CC=1)(C=1C=CC=CC=1)C1=CC=CC=C1 PTLOPIHJOPWUNN-UHFFFAOYSA-N 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 239000002691 unilamellar liposome Substances 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 239000000052 vinegar Substances 0.000 description 1
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- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
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- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 239000002076 α-tocopherol Substances 0.000 description 1
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- 108020001588 κ-opioid receptors Proteins 0.000 description 1
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
- 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
-
- 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:
- C07D489/09—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: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems
- C07D489/10—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: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14
- C07D489/12—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: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Compositions Of Macromolecular Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AUPR693801 | 2001-08-10 | ||
| AUPR6938A AUPR693801A0 (en) | 2001-08-10 | 2001-08-10 | Therapeutic compounds |
| AUPR964001 | 2001-12-19 | ||
| AUPR9640A AUPR964001A0 (en) | 2001-12-19 | 2001-12-19 | Therapeutic compounds |
| PCT/AU2002/001088 WO2003014122A1 (en) | 2001-08-10 | 2002-08-09 | Derivatives of morphine-like opioid compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60215195D1 DE60215195D1 (de) | 2006-11-16 |
| DE60215195T2 true DE60215195T2 (de) | 2007-08-23 |
Family
ID=25646773
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60215195T Expired - Fee Related DE60215195T2 (de) | 2001-08-10 | 2002-08-09 | Derivate morphinähnlicher opioidverbindungen |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US7199129B2 (enExample) |
| EP (1) | EP1423392B1 (enExample) |
| JP (1) | JP2005500373A (enExample) |
| AT (1) | ATE341552T1 (enExample) |
| AU (1) | AU2002322169B2 (enExample) |
| DE (1) | DE60215195T2 (enExample) |
| WO (1) | WO2003014122A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040204862A1 (en) * | 2003-04-11 | 2004-10-14 | Wainer Irving W. | Computer-based model for identification and characterization for non-competitive inhibitors of nicotinic acetylcholine receptors and related ligand-gated ion channel receptors |
| TWI541246B (zh) | 2008-12-08 | 2016-07-11 | 歐陸斯迪公司 | 二氫羥戊甲嗎啡 |
| WO2013043521A1 (en) | 2011-09-22 | 2013-03-28 | Merck Sharp & Dohme Corp. | Pyrazolopyridyl compounds as aldosterone synthase inhibitors |
| EP2757883B1 (en) | 2011-09-22 | 2021-01-13 | Merck Sharp & Dohme Corp. | Triazolopyridyl compounds as aldosterone synthase inhibitors |
| US20140235667A1 (en) | 2011-09-22 | 2014-08-21 | Merck Sharp & Dohme Corp. | Imidazopyridyl compounds as aldosterone synthase inhibitors |
| CA2879454A1 (en) | 2012-07-19 | 2014-01-23 | Drexel University | Novel sigma receptor ligands and methods of modulating cellular protein homeostasis using same |
| GB201309654D0 (en) | 2013-05-30 | 2013-07-17 | Euro Celtique Sa | Method |
| CN105683630B (zh) * | 2013-10-18 | 2017-11-21 | 株式会社理研 | 内燃机用活塞环 |
| US11117870B2 (en) | 2017-11-01 | 2021-09-14 | Drexel University | Compounds, compositions, and methods for treating diseases |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3341538A (en) * | 1965-06-18 | 1967-09-12 | Geigy Chem Corp | Certain 2, 6-methano-3-benzazocines |
| DE69929173T2 (de) * | 1998-01-29 | 2006-08-24 | Monash University, Clayton | Therapeutische verbindungen |
| ATE309240T1 (de) | 2000-08-31 | 2005-11-15 | Hoffmann La Roche | Chinazolin-derivate als alpha-1 adrenerge antagonisten |
-
2002
- 2002-08-09 WO PCT/AU2002/001088 patent/WO2003014122A1/en not_active Ceased
- 2002-08-09 DE DE60215195T patent/DE60215195T2/de not_active Expired - Fee Related
- 2002-08-09 JP JP2003519071A patent/JP2005500373A/ja not_active Abandoned
- 2002-08-09 US US10/486,536 patent/US7199129B2/en not_active Expired - Fee Related
- 2002-08-09 EP EP02753923A patent/EP1423392B1/en not_active Expired - Lifetime
- 2002-08-09 AT AT02753923T patent/ATE341552T1/de not_active IP Right Cessation
- 2002-08-09 AU AU2002322169A patent/AU2002322169B2/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| ATE341552T1 (de) | 2006-10-15 |
| US20040242616A1 (en) | 2004-12-02 |
| EP1423392A4 (en) | 2004-11-17 |
| JP2005500373A (ja) | 2005-01-06 |
| WO2003014122A1 (en) | 2003-02-20 |
| EP1423392A1 (en) | 2004-06-02 |
| US7199129B2 (en) | 2007-04-03 |
| DE60215195D1 (de) | 2006-11-16 |
| AU2002322169B2 (en) | 2008-10-30 |
| EP1423392B1 (en) | 2006-10-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8364 | No opposition during term of opposition | ||
| 8339 | Ceased/non-payment of the annual fee |