MX2008011984A - Derivados de buprenorfina y usos de los mismos. - Google Patents
Derivados de buprenorfina y usos de los mismos.Info
- Publication number
- MX2008011984A MX2008011984A MX2008011984A MX2008011984A MX2008011984A MX 2008011984 A MX2008011984 A MX 2008011984A MX 2008011984 A MX2008011984 A MX 2008011984A MX 2008011984 A MX2008011984 A MX 2008011984A MX 2008011984 A MX2008011984 A MX 2008011984A
- Authority
- MX
- Mexico
- Prior art keywords
- buprenorphine
- compounds
- compounds according
- integer
- salts
- Prior art date
Links
- RMRJXGBAOAMLHD-IHFGGWKQSA-N buprenorphine Chemical class 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 title claims abstract description 122
- 229960001736 buprenorphine Drugs 0.000 claims abstract description 118
- 208000002193 Pain Diseases 0.000 claims abstract description 13
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N phenol group Chemical group C1(=CC=CC=C1)O ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims abstract description 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract description 6
- 150000001875 compounds Chemical class 0.000 claims description 69
- 238000000034 method Methods 0.000 claims description 32
- 150000003839 salts Chemical class 0.000 claims description 30
- 208000026251 Opioid-Related disease Diseases 0.000 claims description 14
- 125000000217 alkyl group Chemical group 0.000 claims description 13
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 13
- 229910052717 sulfur Inorganic materials 0.000 claims description 12
- 238000006467 substitution reaction Methods 0.000 claims description 11
- 125000003118 aryl group Chemical group 0.000 claims description 9
- 230000001225 therapeutic effect Effects 0.000 claims description 9
- 229910052757 nitrogen Inorganic materials 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 201000005040 opiate dependence Diseases 0.000 claims description 7
- 206010013654 Drug abuse Diseases 0.000 claims description 6
- 201000000988 opioid abuse Diseases 0.000 claims description 6
- 229910052760 oxygen Inorganic materials 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 5
- WSNMPAVSZJSIMT-UHFFFAOYSA-N COc1c(C)c2COC(=O)c2c(O)c1CC(O)C1(C)CCC(=O)O1 Chemical compound COc1c(C)c2COC(=O)c2c(O)c1CC(O)C1(C)CCC(=O)O1 WSNMPAVSZJSIMT-UHFFFAOYSA-N 0.000 claims description 3
- 125000002843 carboxylic acid group Chemical group 0.000 claims description 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 2
- 239000001301 oxygen Substances 0.000 claims description 2
- 150000002148 esters Chemical class 0.000 abstract description 30
- 238000011282 treatment Methods 0.000 abstract description 21
- 230000009471 action Effects 0.000 abstract description 14
- 229940127240 opiate Drugs 0.000 abstract description 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 78
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 63
- 239000000203 mixture Substances 0.000 description 51
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 37
- 241000282472 Canis lupus familiaris Species 0.000 description 27
- 239000000243 solution Substances 0.000 description 25
- 239000007787 solid Substances 0.000 description 22
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 21
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 21
- 230000036470 plasma concentration Effects 0.000 description 20
- 210000002381 plasma Anatomy 0.000 description 19
- 238000001914 filtration Methods 0.000 description 17
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 16
- CVIJJOARNCQGON-XYQNZYJMSA-N buprenorphine hemiadipate Chemical compound C([C@]12[C@H]3OC=4C(OC(=O)CCCCC(O)=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 CVIJJOARNCQGON-XYQNZYJMSA-N 0.000 description 16
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 15
- 230000007062 hydrolysis Effects 0.000 description 15
- 238000006460 hydrolysis reaction Methods 0.000 description 15
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 15
- 230000009747 swallowing Effects 0.000 description 14
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 13
- 210000004369 blood Anatomy 0.000 description 13
- 239000008280 blood Substances 0.000 description 13
- 239000000463 material Substances 0.000 description 13
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 12
- 239000002253 acid Substances 0.000 description 12
- -1 buprenorphine ester Chemical class 0.000 description 12
- 230000006870 function Effects 0.000 description 12
- 239000002904 solvent Substances 0.000 description 12
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 11
- 239000003814 drug Substances 0.000 description 11
- 239000002244 precipitate Substances 0.000 description 11
- WNLRTRBMVRJNCN-UHFFFAOYSA-N adipic acid Chemical compound OC(=O)CCCCC(O)=O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 description 10
- 229940079593 drug Drugs 0.000 description 10
- 238000002844 melting Methods 0.000 description 10
- 230000008018 melting Effects 0.000 description 10
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 9
- 230000015572 biosynthetic process Effects 0.000 description 9
- 102000051367 mu Opioid Receptors Human genes 0.000 description 9
- 238000003786 synthesis reaction Methods 0.000 description 9
- 108020001612 μ-opioid receptors Proteins 0.000 description 9
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 8
- 238000004458 analytical method Methods 0.000 description 8
- 239000002585 base Substances 0.000 description 8
- 238000009472 formulation Methods 0.000 description 8
- 239000000843 powder Substances 0.000 description 8
- 239000000047 product Substances 0.000 description 8
- 239000003826 tablet Substances 0.000 description 8
- DLYUQMMRRRQYAE-UHFFFAOYSA-N tetraphosphorus decaoxide Chemical compound O1P(O2)(=O)OP3(=O)OP1(=O)OP2(=O)O3 DLYUQMMRRRQYAE-UHFFFAOYSA-N 0.000 description 8
- 150000008064 anhydrides Chemical class 0.000 description 7
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 6
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 6
- 239000003795 chemical substances by application Substances 0.000 description 6
- 238000004587 chromatography analysis Methods 0.000 description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 6
- 230000002354 daily effect Effects 0.000 description 6
- 239000006185 dispersion Substances 0.000 description 6
- 230000000694 effects Effects 0.000 description 6
- LBAQSKZHMLAFHH-UHFFFAOYSA-N ethoxyethane;hydron;chloride Chemical compound Cl.CCOCC LBAQSKZHMLAFHH-UHFFFAOYSA-N 0.000 description 6
- 239000003921 oil Substances 0.000 description 6
- 239000002245 particle Substances 0.000 description 6
- 238000001953 recrystallisation Methods 0.000 description 6
- 238000003756 stirring Methods 0.000 description 6
- 201000009032 substance abuse Diseases 0.000 description 6
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 5
- GVGLGOZIDCSQPN-PVHGPHFFSA-N Heroin Chemical compound O([C@H]1[C@H](C=C[C@H]23)OC(C)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4OC(C)=O GVGLGOZIDCSQPN-PVHGPHFFSA-N 0.000 description 5
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 5
- 238000010521 absorption reaction Methods 0.000 description 5
- 239000001361 adipic acid Substances 0.000 description 5
- 235000011037 adipic acid Nutrition 0.000 description 5
- UAIXRPCCYXNJMQ-RZIPZOSSSA-N buprenorphine hydrochlorie Chemical compound [Cl-].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)C[NH+]2CC1CC1 UAIXRPCCYXNJMQ-RZIPZOSSSA-N 0.000 description 5
- 239000000706 filtrate Substances 0.000 description 5
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- 239000002243 precursor Substances 0.000 description 5
- 239000000651 prodrug Substances 0.000 description 5
- 229940002612 prodrug Drugs 0.000 description 5
- 229910000104 sodium hydride Inorganic materials 0.000 description 5
- 239000007909 solid dosage form Substances 0.000 description 5
- 239000003981 vehicle Substances 0.000 description 5
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 description 4
- USSIQXCVUWKGNF-UHFFFAOYSA-N 6-(dimethylamino)-4,4-diphenylheptan-3-one Chemical compound C=1C=CC=CC=1C(CC(C)N(C)C)(C(=O)CC)C1=CC=CC=C1 USSIQXCVUWKGNF-UHFFFAOYSA-N 0.000 description 4
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 4
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 4
- KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 description 4
- 125000002837 carbocyclic group Chemical group 0.000 description 4
- IJOOHPMOJXWVHK-UHFFFAOYSA-N chlorotrimethylsilane Chemical compound C[Si](C)(C)Cl IJOOHPMOJXWVHK-UHFFFAOYSA-N 0.000 description 4
- 230000000295 complement effect Effects 0.000 description 4
- 229960002069 diamorphine Drugs 0.000 description 4
- 239000007789 gas Substances 0.000 description 4
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- 238000001727 in vivo Methods 0.000 description 4
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- 159000000000 sodium salts Chemical class 0.000 description 4
- 241000894007 species Species 0.000 description 4
- 239000000725 suspension Substances 0.000 description 4
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 4
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 3
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 3
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 3
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- QOSSAOTZNIDXMA-UHFFFAOYSA-N Dicylcohexylcarbodiimide Chemical compound C1CCCCC1N=C=NC1CCCCC1 QOSSAOTZNIDXMA-UHFFFAOYSA-N 0.000 description 3
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 3
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- LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 description 2
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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
- 238000002098 selective ion monitoring Methods 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
- CIJQGPVMMRXSQW-UHFFFAOYSA-M sodium;2-aminoacetic acid;hydroxide Chemical compound O.[Na+].NCC([O-])=O CIJQGPVMMRXSQW-UHFFFAOYSA-M 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 239000002195 soluble material Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 238000001228 spectrum Methods 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 229910001220 stainless steel Inorganic materials 0.000 description 1
- 239000010935 stainless steel Substances 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 239000011550 stock solution Substances 0.000 description 1
- 208000011117 substance-related disease Diseases 0.000 description 1
- 229960004793 sucrose Drugs 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000002511 suppository base Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 238000007910 systemic administration Methods 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000001973 tert-pentyl group Chemical group [H]C([H])([H])C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 231100001274 therapeutic index Toxicity 0.000 description 1
- RTKIYNMVFMVABJ-UHFFFAOYSA-L thimerosal Chemical compound [Na+].CC[Hg]SC1=CC=CC=C1C([O-])=O RTKIYNMVFMVABJ-UHFFFAOYSA-L 0.000 description 1
- 229940033663 thimerosal Drugs 0.000 description 1
- 150000003577 thiophenes Chemical class 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 229940074410 trehalose Drugs 0.000 description 1
- 238000001291 vacuum drying Methods 0.000 description 1
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- 238000009777 vacuum freeze-drying Methods 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
-
- 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
-
- 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
-
- 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
- A61P25/36—Opioid-abuse
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0606124.6A GB0606124D0 (en) | 2006-03-28 | 2006-03-28 | Buprenorphine derivatives and uses thereof |
| PCT/GB2007/001120 WO2007110636A1 (en) | 2006-03-28 | 2007-03-27 | Buprenorphine derivatives and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2008011984A true MX2008011984A (es) | 2008-10-03 |
Family
ID=36384277
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2008011984A MX2008011984A (es) | 2006-03-28 | 2007-03-27 | Derivados de buprenorfina y usos de los mismos. |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US7964610B2 (enExample) |
| EP (1) | EP2001891B1 (enExample) |
| JP (1) | JP5167446B2 (enExample) |
| KR (1) | KR101430626B1 (enExample) |
| CN (2) | CN104151320A (enExample) |
| AU (1) | AU2007231133B2 (enExample) |
| BR (1) | BRPI0709157A8 (enExample) |
| CA (1) | CA2647417C (enExample) |
| DK (1) | DK2001891T3 (enExample) |
| ES (1) | ES2432169T3 (enExample) |
| GB (1) | GB0606124D0 (enExample) |
| IL (1) | IL193917A (enExample) |
| MX (1) | MX2008011984A (enExample) |
| MY (1) | MY151025A (enExample) |
| NZ (1) | NZ570997A (enExample) |
| PL (1) | PL2001891T3 (enExample) |
| PT (1) | PT2001891E (enExample) |
| RU (1) | RU2435773C2 (enExample) |
| TW (1) | TWI501969B (enExample) |
| WO (1) | WO2007110636A1 (enExample) |
| ZA (1) | ZA200807614B (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2549115T3 (es) | 2006-09-22 | 2015-10-23 | Zynerba Pharmaceuticals, Inc. | Profármacos de buprenorfina administrables por vía transdérmica y composiciones resistentes al consumo excesivo de los mismos |
| US20110053971A1 (en) * | 2008-04-24 | 2011-03-03 | Janssen Pharmaceutica Nv | Nalmefene di-ester prodrugs |
| FR2975912B1 (fr) | 2011-05-30 | 2013-06-14 | Flamel Tech Sa | Composition a liberation controlee de buprenorphine |
| CA3002082A1 (en) * | 2015-10-26 | 2017-05-04 | Orphomed, Inc. | Ethylene glycol ether of buprenorphine |
| EP3426234A1 (en) | 2016-03-09 | 2019-01-16 | Indivior UK Limited | Abuse-resistant pharmaceutical formulations |
| PL3512518T3 (pl) | 2016-09-13 | 2023-03-27 | Alar Pharmaceuticals Inc. | Preparaty buprenorfiny o przedłużonym uwalnianiu |
| WO2019064026A1 (en) | 2017-09-29 | 2019-04-04 | Orexo Ab | NEW PHARMACEUTICAL COMPOSITIONS |
| TWI838372B (zh) | 2018-05-11 | 2024-04-11 | 昱展新藥生技股份有限公司 | 丁基原啡因衍生物之長效注射劑型及結晶型 |
| GB201904767D0 (en) | 2019-04-04 | 2019-05-22 | Orexo Ab | New pharmaceutical compositions |
| WO2023102489A1 (en) * | 2021-12-03 | 2023-06-08 | Board Of Regents Of The University Of Nebraska | Compounds, nanoparticles, and pharmaceutical compositions for the treatment of drug addiction |
| CN116283893B (zh) * | 2023-03-22 | 2024-04-26 | 阜阳欣奕华制药科技有限公司 | 硫代羟基乙酸酐的制备方法 |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4668685A (en) * | 1984-07-05 | 1987-05-26 | E.I. Du Pont De Nemours And Company | Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans, which are analgesics or narcotic antagonists |
| GB8728294D0 (en) * | 1987-12-03 | 1988-01-06 | Reckitt & Colmann Prod Ltd | Treatment compositions |
| US5985880A (en) * | 1996-06-05 | 1999-11-16 | Delta Pharmaceuticals | Compositions and methods for reducing respiratory depression and attendant side effects of mu opioid compounds |
| 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 |
| US5750534A (en) * | 1994-03-16 | 1998-05-12 | National Science Council | Nalbuphine esters having long acting analgesic action and method of use |
| US6004969A (en) * | 1996-04-15 | 1999-12-21 | National Science Council | Transdermal delivery of buprenorphine preparations |
| KR100204659B1 (ko) * | 1996-05-28 | 1999-06-15 | 강재헌 | 신규한 부프레노핀계 진통제용 화합물 |
| US6225321B1 (en) * | 1997-06-05 | 2001-05-01 | Oliver Yoa-Pu Hu | Long analgesic acting nalbuphine polyester derivative and method of use |
| CN1150895C (zh) | 1998-11-13 | 2004-05-26 | 杰格研究股份公司 | 用于吸入给药的干粉 |
| US6716449B2 (en) * | 2000-02-08 | 2004-04-06 | Euro-Celtique S.A. | Controlled-release compositions containing opioid agonist and antagonist |
| SI2283842T1 (sl) * | 2000-02-08 | 2015-07-31 | Euro-Celtique S.A. | Oralne formulacije opioidnih agonistov, varne pred zlorabo |
| WO2003026743A2 (en) * | 2001-09-26 | 2003-04-03 | Penwest Pharmaceuticals Company | Opioid formulations having reduced potential for abuse |
| US20040033253A1 (en) * | 2002-02-19 | 2004-02-19 | Ihor Shevchuk | Acyl opioid antagonists |
| US7666876B2 (en) * | 2002-03-19 | 2010-02-23 | Vernalis (R&D) Limited | Buprenorphine formulations for intranasal delivery |
| US7776314B2 (en) * | 2002-06-17 | 2010-08-17 | Grunenthal Gmbh | Abuse-proofed dosage system |
| EP1554290B1 (en) * | 2002-10-25 | 2009-09-30 | Euro-Celtique S.A. | Analogs and prodrugs of buprenorphine |
| DE10250084A1 (de) * | 2002-10-25 | 2004-05-06 | Grünenthal GmbH | Gegen Missbrauch gesicherte Darreichungsform |
| DE10250087A1 (de) | 2002-10-25 | 2004-05-06 | Grünenthal GmbH | Gegen Missbrauch gesicherte Darreichungsform |
| US20050186139A1 (en) * | 2002-10-25 | 2005-08-25 | Gruenenthal Gmbh | Abuse-proofed dosage form |
| US20050191244A1 (en) * | 2002-10-25 | 2005-09-01 | Gruenenthal Gmbh | Abuse-resistant pharmaceutical dosage form |
| RU2215741C1 (ru) * | 2002-11-05 | 2003-11-10 | Открытое Акционерное Общество "Международная Научно-Технологическая Корпорация" | Сложные эфиры n-замещенных 14-гидроксиморфинанов и способ их получения |
| CN1263760C (zh) * | 2002-11-12 | 2006-07-12 | 财团法人奇美医院 | 新颖的丁丙诺啡酯衍生物及其制备方法，以及长效作用镇痛药学组合物 |
| ATE382050T1 (de) * | 2002-11-25 | 2008-01-15 | Chi Mei Foundation Medical Ct | Buprenorphinesterderivate, verfahren zu ihrer herstellung, und langwirksame analgetische arzneimittel |
| JP2004175706A (ja) * | 2002-11-26 | 2004-06-24 | Chi Mei Foundation Medical Center | 新規なブプレノルフィンのエステル誘導体及びそれらの調製方法、及び長時間効力持続性鎮痛薬剤組成物 |
| TW200500067A (en) * | 2003-01-21 | 2005-01-01 | Control Delivery Sys Inc | Salts of codrugs and uses related thereto |
| WO2004071491A1 (en) * | 2003-02-04 | 2004-08-26 | Chrysalis Technologies Incorporated | Aerosol formulations and aerosol delivery of buspirone, buprenorphine, triazolam, cyclobenzaprine and zolpidem |
| US7195882B2 (en) * | 2003-06-03 | 2007-03-27 | Roche Diagnostics Operations, Inc. | Monoclonal antibodies specific for buprenorphine and metabolites thereof |
| WO2005009377A2 (en) * | 2003-07-23 | 2005-02-03 | University Of Kentucky Research Foundation | Novel oral bioavailable prodrugs |
| US7589233B2 (en) * | 2003-07-29 | 2009-09-15 | Signature R&D Holdings, Llc | L-Threonine derivatives of high therapeutic index |
| US7220842B2 (en) * | 2004-04-05 | 2007-05-22 | Dade Behring Inc. | Immunoassays for buprenorphine and norbuprenorphine |
-
2006
- 2006-03-28 GB GBGB0606124.6A patent/GB0606124D0/en not_active Ceased
-
2007
- 2007-03-27 KR KR1020087023692A patent/KR101430626B1/ko not_active Expired - Fee Related
- 2007-03-27 MY MYPI20083500 patent/MY151025A/en unknown
- 2007-03-27 NZ NZ570997A patent/NZ570997A/en not_active IP Right Cessation
- 2007-03-27 PT PT77321776T patent/PT2001891E/pt unknown
- 2007-03-27 US US12/294,462 patent/US7964610B2/en not_active Expired - Fee Related
- 2007-03-27 CA CA2647417A patent/CA2647417C/en not_active Expired - Fee Related
- 2007-03-27 CN CN201410318622.9A patent/CN104151320A/zh active Pending
- 2007-03-27 TW TW096110534A patent/TWI501969B/zh not_active IP Right Cessation
- 2007-03-27 ES ES07732177T patent/ES2432169T3/es active Active
- 2007-03-27 EP EP07732177.6A patent/EP2001891B1/en active Active
- 2007-03-27 BR BRPI0709157A patent/BRPI0709157A8/pt not_active IP Right Cessation
- 2007-03-27 CN CNA2007800108118A patent/CN101410402A/zh active Pending
- 2007-03-27 DK DK07732177.6T patent/DK2001891T3/da active
- 2007-03-27 JP JP2009502210A patent/JP5167446B2/ja not_active Expired - Fee Related
- 2007-03-27 AU AU2007231133A patent/AU2007231133B2/en not_active Ceased
- 2007-03-27 WO PCT/GB2007/001120 patent/WO2007110636A1/en not_active Ceased
- 2007-03-27 PL PL07732177T patent/PL2001891T3/pl unknown
- 2007-03-27 MX MX2008011984A patent/MX2008011984A/es active IP Right Grant
- 2007-03-27 RU RU2008142527/04A patent/RU2435773C2/ru not_active IP Right Cessation
-
2008
- 2008-09-04 ZA ZA200807614A patent/ZA200807614B/xx unknown
- 2008-09-04 IL IL193917A patent/IL193917A/en not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| GB0606124D0 (en) | 2006-05-03 |
| KR101430626B1 (ko) | 2014-08-18 |
| BRPI0709157A8 (pt) | 2018-04-24 |
| TWI501969B (zh) | 2015-10-01 |
| ES2432169T3 (es) | 2013-12-02 |
| AU2007231133B2 (en) | 2011-09-01 |
| EP2001891B1 (en) | 2013-07-24 |
| PL2001891T3 (pl) | 2014-03-31 |
| CN101410402A (zh) | 2009-04-15 |
| CN104151320A (zh) | 2014-11-19 |
| JP2009531406A (ja) | 2009-09-03 |
| JP5167446B2 (ja) | 2013-03-21 |
| US7964610B2 (en) | 2011-06-21 |
| US20100234412A1 (en) | 2010-09-16 |
| RU2435773C2 (ru) | 2011-12-10 |
| IL193917A (en) | 2014-12-31 |
| TW200806672A (en) | 2008-02-01 |
| ZA200807614B (en) | 2009-10-28 |
| BRPI0709157A2 (pt) | 2011-06-28 |
| AU2007231133A2 (en) | 2008-10-16 |
| CA2647417C (en) | 2014-09-23 |
| NZ570997A (en) | 2011-08-26 |
| DK2001891T3 (da) | 2013-11-04 |
| AU2007231133A8 (en) | 2011-08-25 |
| PT2001891E (pt) | 2013-10-30 |
| MY151025A (en) | 2014-03-31 |
| RU2008142527A (ru) | 2010-05-10 |
| WO2007110636A1 (en) | 2007-10-04 |
| AU2007231133A1 (en) | 2007-10-04 |
| EP2001891A1 (en) | 2008-12-17 |
| KR20080105124A (ko) | 2008-12-03 |
| CA2647417A1 (en) | 2007-10-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration | ||
| GB | Transfer or rights |