UA72783C2 - Agonist of central canabinoid receptors for preparation of drug disaccustoming smoking, combined pharmaceutical composition and kit - Google Patents
Agonist of central canabinoid receptors for preparation of drug disaccustoming smoking, combined pharmaceutical composition and kit Download PDFInfo
- Publication number
- UA72783C2 UA72783C2 UA2002075476A UA2002075476A UA72783C2 UA 72783 C2 UA72783 C2 UA 72783C2 UA 2002075476 A UA2002075476 A UA 2002075476A UA 2002075476 A UA2002075476 A UA 2002075476A UA 72783 C2 UA72783 C2 UA 72783C2
- Authority
- UA
- Ukraine
- Prior art keywords
- solvates
- acceptable salts
- dichlorophenyl
- carboxamide
- chlorophenyl
- Prior art date
Links
- 230000000391 smoking effect Effects 0.000 title claims abstract description 7
- 239000003814 drug Substances 0.000 title claims description 9
- 229940079593 drug Drugs 0.000 title claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 8
- 239000000556 agonist Substances 0.000 title 1
- 239000013543 active substance Substances 0.000 claims description 31
- 150000003839 salts Chemical class 0.000 claims description 19
- 229960002715 nicotine Drugs 0.000 claims description 18
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 claims description 18
- 239000012453 solvate Substances 0.000 claims description 18
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims description 16
- 230000005586 smoking cessation Effects 0.000 claims description 13
- -1 M-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)4-methylpyrazole-3-carboxamide Chemical compound 0.000 claims description 11
- 239000000181 nicotinic agonist Substances 0.000 claims description 10
- 206010057852 Nicotine dependence Diseases 0.000 claims description 9
- 208000025569 Tobacco Use disease Diseases 0.000 claims description 9
- 229940123685 Monoamine oxidase inhibitor Drugs 0.000 claims description 8
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 claims description 8
- 206010048010 Withdrawal syndrome Diseases 0.000 claims description 8
- 239000002899 monoamine oxidase inhibitor Substances 0.000 claims description 8
- 238000004519 manufacturing process Methods 0.000 claims description 6
- 238000012876 topography Methods 0.000 claims 1
- 229940126062 Compound A Drugs 0.000 description 25
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 description 25
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 12
- 150000001875 compounds Chemical class 0.000 description 10
- 239000007903 gelatin capsule Substances 0.000 description 9
- 239000000203 mixture Substances 0.000 description 9
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 6
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 6
- 235000019359 magnesium stearate Nutrition 0.000 description 6
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 6
- 239000000243 solution Substances 0.000 description 6
- 239000003826 tablet Substances 0.000 description 6
- 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 5
- 229920002261 Corn starch Polymers 0.000 description 5
- 239000008120 corn starch Substances 0.000 description 5
- 229960001021 lactose monohydrate Drugs 0.000 description 5
- 239000008213 purified water Substances 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 4
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 4
- 241000208125 Nicotiana Species 0.000 description 4
- 235000002637 Nicotiana tabacum Nutrition 0.000 description 4
- 239000005557 antagonist Substances 0.000 description 4
- 239000001768 carboxy methyl cellulose Substances 0.000 description 4
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 4
- 235000019441 ethanol Nutrition 0.000 description 4
- 239000007924 injection Substances 0.000 description 4
- 238000002347 injection Methods 0.000 description 4
- 230000001737 promoting effect Effects 0.000 description 4
- 208000019901 Anxiety disease Diseases 0.000 description 3
- 102000018208 Cannabinoid Receptor Human genes 0.000 description 3
- 108050007331 Cannabinoid receptor Proteins 0.000 description 3
- GJSURZIOUXUGAL-UHFFFAOYSA-N Clonidine Chemical compound ClC1=CC=CC(Cl)=C1NC1=NCCN1 GJSURZIOUXUGAL-UHFFFAOYSA-N 0.000 description 3
- PHVGLTMQBUFIQQ-UHFFFAOYSA-N Nortryptiline Chemical compound C1CC2=CC=CC=C2C(=CCCNC)C2=CC=CC=C21 PHVGLTMQBUFIQQ-UHFFFAOYSA-N 0.000 description 3
- 230000001430 anti-depressive effect Effects 0.000 description 3
- 239000000935 antidepressant agent Substances 0.000 description 3
- 229940005513 antidepressants Drugs 0.000 description 3
- 230000036506 anxiety Effects 0.000 description 3
- 239000002249 anxiolytic agent Substances 0.000 description 3
- 230000000949 anxiolytic effect Effects 0.000 description 3
- SNPPWIUOZRMYNY-UHFFFAOYSA-N bupropion Chemical compound CC(C)(C)NC(C)C(=O)C1=CC=CC(Cl)=C1 SNPPWIUOZRMYNY-UHFFFAOYSA-N 0.000 description 3
- 229960001058 bupropion Drugs 0.000 description 3
- QWCRAEMEVRGPNT-UHFFFAOYSA-N buspirone Chemical compound C1C(=O)N(CCCCN2CCN(CC2)C=2N=CC=CN=2)C(=O)CC21CCCC2 QWCRAEMEVRGPNT-UHFFFAOYSA-N 0.000 description 3
- 229960002495 buspirone Drugs 0.000 description 3
- 229960002896 clonidine Drugs 0.000 description 3
- ODQWQRRAPPTVAG-GZTJUZNOSA-N doxepin Chemical compound C1OC2=CC=CC=C2C(=C/CCN(C)C)/C2=CC=CC=C21 ODQWQRRAPPTVAG-GZTJUZNOSA-N 0.000 description 3
- 229960005426 doxepin Drugs 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 238000007918 intramuscular administration Methods 0.000 description 3
- 238000001990 intravenous administration Methods 0.000 description 3
- 229960001158 nortriptyline Drugs 0.000 description 3
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- 229920002472 Starch Polymers 0.000 description 2
- 230000003111 delayed effect Effects 0.000 description 2
- 239000002270 dispersing agent Substances 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 239000000796 flavoring agent Substances 0.000 description 2
- 235000003599 food sweetener Nutrition 0.000 description 2
- 239000008187 granular material Substances 0.000 description 2
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 description 2
- 239000007943 implant Substances 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 2
- 239000004005 microsphere Substances 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 239000008107 starch Substances 0.000 description 2
- 235000019698 starch Nutrition 0.000 description 2
- 238000007920 subcutaneous administration Methods 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 239000003765 sweetening agent Substances 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 230000000699 topical effect Effects 0.000 description 2
- 239000000080 wetting agent Substances 0.000 description 2
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 1
- UIKROCXWUNQSPJ-VIFPVBQESA-N (-)-cotinine Chemical compound C1CC(=O)N(C)[C@@H]1C1=CC=CN=C1 UIKROCXWUNQSPJ-VIFPVBQESA-N 0.000 description 1
- YZOUYRAONFXZSI-SBHWVFSVSA-N (1S,3R,5R,6R,8R,10R,11R,13R,15R,16R,18R,20R,21R,23R,25R,26R,28R,30R,31S,33R,35R,36R,37S,38R,39S,40R,41S,42R,43S,44R,45S,46R,47S,48R,49S)-5,10,15,20,25,30,35-heptakis(hydroxymethyl)-37,39,40,41,42,43,44,45,46,47,48,49-dodecamethoxy-2,4,7,9,12,14,17,19,22,24,27,29,32,34-tetradecaoxaoctacyclo[31.2.2.23,6.28,11.213,16.218,21.223,26.228,31]nonatetracontane-36,38-diol Chemical compound O([C@@H]([C@H]([C@@H]1OC)OC)O[C@H]2[C@@H](O)[C@@H]([C@@H](O[C@@H]3[C@@H](CO)O[C@@H]([C@H]([C@@H]3O)OC)O[C@@H]3[C@@H](CO)O[C@@H]([C@H]([C@@H]3OC)OC)O[C@@H]3[C@@H](CO)O[C@@H]([C@H]([C@@H]3OC)OC)O[C@@H]3[C@@H](CO)O[C@@H]([C@H]([C@@H]3OC)OC)O3)O[C@@H]2CO)OC)[C@H](CO)[C@H]1O[C@@H]1[C@@H](OC)[C@H](OC)[C@H]3[C@@H](CO)O1 YZOUYRAONFXZSI-SBHWVFSVSA-N 0.000 description 1
- 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 1
- 102000009132 CB1 Cannabinoid Receptor Human genes 0.000 description 1
- 108010073366 CB1 Cannabinoid Receptor Proteins 0.000 description 1
- 102100033868 Cannabinoid receptor 1 Human genes 0.000 description 1
- 229940122820 Cannabinoid receptor antagonist Drugs 0.000 description 1
- UGFAIRIUMAVXCW-UHFFFAOYSA-N Carbon monoxide Chemical compound [O+]#[C-] UGFAIRIUMAVXCW-UHFFFAOYSA-N 0.000 description 1
- 208000017667 Chronic Disease Diseases 0.000 description 1
- UIKROCXWUNQSPJ-UHFFFAOYSA-N Cotinine Natural products C1CC(=O)N(C)C1C1=CC=CN=C1 UIKROCXWUNQSPJ-UHFFFAOYSA-N 0.000 description 1
- 229920000858 Cyclodextrin Polymers 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- 125000003158 alcohol group Chemical group 0.000 description 1
- 230000002421 anti-septic effect Effects 0.000 description 1
- 229940064004 antiseptic throat preparations Drugs 0.000 description 1
- 235000019789 appetite Nutrition 0.000 description 1
- 230000036528 appetite Effects 0.000 description 1
- 239000002830 appetite depressant Substances 0.000 description 1
- 230000004596 appetite loss Effects 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 239000003536 cannabinoid receptor antagonist Substances 0.000 description 1
- 235000014633 carbohydrates Nutrition 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
- 229910002091 carbon monoxide Inorganic materials 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 235000015111 chews Nutrition 0.000 description 1
- 235000019504 cigarettes Nutrition 0.000 description 1
- 229940110456 cocoa butter Drugs 0.000 description 1
- 235000019868 cocoa butter Nutrition 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 239000006184 cosolvent Substances 0.000 description 1
- 229950006073 cotinine Drugs 0.000 description 1
- 150000001907 coumarones Chemical class 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 235000013355 food flavoring agent Nutrition 0.000 description 1
- 235000012631 food intake Nutrition 0.000 description 1
- GDSRMADSINPKSL-HSEONFRVSA-N gamma-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO GDSRMADSINPKSL-HSEONFRVSA-N 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 229960001375 lactose Drugs 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 208000019017 loss of appetite Diseases 0.000 description 1
- 235000021266 loss of appetite Nutrition 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 1
- 229960002216 methylparaben Drugs 0.000 description 1
- 239000003094 microcapsule Substances 0.000 description 1
- 239000012053 oil suspension Substances 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 239000000902 placebo Substances 0.000 description 1
- 229940068196 placebo Drugs 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 229940068968 polysorbate 80 Drugs 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 230000008092 positive effect Effects 0.000 description 1
- 230000002028 premature 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
- 230000000506 psychotropic effect Effects 0.000 description 1
- 150000003217 pyrazoles Chemical class 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
- 239000000779 smoke Substances 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
-
- 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
- A61P25/34—Tobacco-abuse
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material 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)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0001682A FR2804604B1 (fr) | 2000-02-09 | 2000-02-09 | Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles pour faciliter l'arret de la consommation de tabac |
| PCT/FR2001/000356 WO2001058450A2 (fr) | 2000-02-09 | 2001-02-07 | Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles pour faciliter l'arret de la consommation de tabac |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UA72783C2 true UA72783C2 (en) | 2005-04-15 |
Family
ID=8846875
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UA2002075476A UA72783C2 (en) | 2000-02-09 | 2001-07-02 | Agonist of central canabinoid receptors for preparation of drug disaccustoming smoking, combined pharmaceutical composition and kit |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US6930122B2 (ru) |
| EP (1) | EP1257275B1 (ru) |
| JP (2) | JP2003522145A (ru) |
| CN (1) | CN1250220C (ru) |
| AR (1) | AR028505A1 (ru) |
| AT (1) | ATE292467T1 (ru) |
| AU (1) | AU781827B2 (ru) |
| BG (2) | BG110386A (ru) |
| BR (1) | BR0108126A (ru) |
| CA (1) | CA2397262C (ru) |
| CZ (1) | CZ296685B6 (ru) |
| DE (1) | DE60109903T2 (ru) |
| DK (1) | DK1257275T3 (ru) |
| EE (1) | EE04836B1 (ru) |
| ES (1) | ES2240416T3 (ru) |
| FR (1) | FR2804604B1 (ru) |
| HK (1) | HK1051140A1 (ru) |
| HU (1) | HU225328B1 (ru) |
| IL (1) | IL150710A0 (ru) |
| IS (1) | IS6450A (ru) |
| MX (1) | MXPA02007766A (ru) |
| NO (1) | NO324521B1 (ru) |
| NZ (1) | NZ519924A (ru) |
| PL (1) | PL201685B1 (ru) |
| PT (1) | PT1257275E (ru) |
| RS (1) | RS50404B (ru) |
| RU (1) | RU2257207C2 (ru) |
| SI (1) | SI1257275T1 (ru) |
| SK (1) | SK284952B6 (ru) |
| TW (1) | TWI243677B (ru) |
| UA (1) | UA72783C2 (ru) |
| WO (1) | WO2001058450A2 (ru) |
| ZA (1) | ZA200205317B (ru) |
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| FR2804604B1 (fr) * | 2000-02-09 | 2005-05-27 | Sanofi Synthelabo | Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles pour faciliter l'arret de la consommation de tabac |
| US6462237B1 (en) * | 2001-06-14 | 2002-10-08 | Usv Limited | Cyclodextrin stabilized pharmaceutical compositions of bupropion hydrochloride |
| AU2002323126A1 (en) | 2001-08-13 | 2003-03-03 | Honeywell International Inc. | Systems for wafer level burn-in of electronic devices |
| ATE486842T1 (de) | 2002-03-12 | 2010-11-15 | Merck Sharp & Dohme | Substituierte amide |
| US7423067B2 (en) | 2002-03-26 | 2008-09-09 | Merck & Co., Inc. | Diphenyl cyclopentyl amides as cannabinoid-1 receptor inverse agonists |
| EP1492784A4 (en) | 2002-03-28 | 2006-03-29 | Merck & Co Inc | SUBSTITUTED 2,3-DIPHENYLPYRIDINES |
| CA2481313A1 (en) | 2002-04-12 | 2003-10-23 | Merck & Co., Inc. | Bicyclic amides |
| US6825209B2 (en) | 2002-04-15 | 2004-11-30 | Research Triangle Institute | Compounds having unique CB1 receptor binding selectivity and methods for their production and use |
| EP1558252B1 (en) | 2002-08-02 | 2007-10-10 | Merck & Co., Inc. | Substituted furo [2,3-b]pyridine derivatives |
| EP1546115A4 (en) | 2002-09-27 | 2010-08-04 | Merck Sharp & Dohme | SUBSTITUTED PYRIMIDINES |
| US7129239B2 (en) | 2002-10-28 | 2006-10-31 | Pfizer Inc. | Purine compounds and uses thereof |
| US7247628B2 (en) | 2002-12-12 | 2007-07-24 | Pfizer, Inc. | Cannabinoid receptor ligands and uses thereof |
| WO2004058145A2 (en) | 2002-12-19 | 2004-07-15 | Merck & Co., Inc. | Substituted amides |
| US7329658B2 (en) | 2003-02-06 | 2008-02-12 | Pfizer Inc | Cannabinoid receptor ligands and uses thereof |
| US7176210B2 (en) | 2003-02-10 | 2007-02-13 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
| US7268133B2 (en) | 2003-04-23 | 2007-09-11 | Pfizer, Inc. Patent Department | Cannabinoid receptor ligands and uses thereof |
| US7145012B2 (en) | 2003-04-23 | 2006-12-05 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
| US20040224963A1 (en) * | 2003-05-09 | 2004-11-11 | Pfizer Inc | Pharmaceutical composition for the prevention and treatment of nicotine addiction in a mammal |
| US20040224962A1 (en) * | 2003-05-09 | 2004-11-11 | Pfizer Inc | Pharmaceutical composition for the treatment of obesity or to facilitate or promote weight loss |
| JP2007501279A (ja) * | 2003-05-20 | 2007-01-25 | ユニバーシティ・オブ・テネシー・リサーチ・ファウンデイション | カンナビノイド誘導体、その製造方法、および使用 |
| US7232823B2 (en) | 2003-06-09 | 2007-06-19 | Pfizer, Inc. | Cannabinoid receptor ligands and uses thereof |
| JP2007510647A (ja) * | 2003-10-30 | 2007-04-26 | メルク エンド カムパニー インコーポレーテッド | カンナビノイド受容体調節剤としてのアラルキルアミン類 |
| NZ580387A (en) | 2004-07-12 | 2011-06-30 | Cadila Healthcare Ltd | Tricyclic pyrazole derivatives as cannabinoid receptor modulators |
| US20060025448A1 (en) | 2004-07-22 | 2006-02-02 | Cadila Healthcare Limited | Hair growth stimulators |
| ES2435790T3 (es) | 2004-12-03 | 2013-12-23 | Intervet International B.V. | Piperazinas sustituidas como antagonistas de CB1 |
| CA2637565A1 (en) * | 2006-01-18 | 2007-07-26 | Schering Corporation | Cannibinoid receptor modulators |
| CN101062919B (zh) * | 2006-04-26 | 2012-08-15 | 中国人民解放军军事医学科学院毒物药物研究所 | 4-甲基-1h-二芳基吡唑衍生物及其作为药物的用途 |
| WO2007121687A1 (fr) * | 2006-04-26 | 2007-11-01 | Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. China | Dérivés du 4-méthyl-1h-diaryl pyrazole et leur utilisation comme médicaments |
| US20070287734A1 (en) * | 2006-06-09 | 2007-12-13 | Auspex Pharmaceuticals, Inc. | Preparation and utility of substituted pyrazole compounds with cannabinoid receptor activity |
| RU2477634C2 (ru) * | 2006-06-16 | 2013-03-20 | Теракос, Инк. | Лечение психологических состояний с применением антагонистов m1-мускариновых рецепторов |
| EA026213B1 (ru) * | 2006-10-20 | 2017-03-31 | Солвей Фармасьютикалс Б.В. | Термостабильная твердая фармацевтическая композиция, содержащая наномицеллы, и способ ее получения |
| WO2008130616A2 (en) * | 2007-04-19 | 2008-10-30 | Schering Corporation | Diaryl morpholines as cb1 modulators |
| JP2010531874A (ja) * | 2007-06-28 | 2010-09-30 | インターベット インターナショナル ベー． フェー． | Ｃｂ１アンタゴニストとしての置換ピペラジン |
| BRPI0814806A2 (pt) * | 2007-06-28 | 2015-02-03 | Intervet Int Bv | Pirazinas substituídas como antagonistas de cb1 |
| EP2095814A1 (de) * | 2008-02-26 | 2009-09-02 | Wolfgang J. Kox | Medikamentengestützter Nikotinentzug |
| WO2010018856A1 (ja) * | 2008-08-13 | 2010-02-18 | 持田製薬株式会社 | カンナビノイド受容体関連疾患の予防／改善または治療剤 |
| RU2533224C2 (ru) * | 2010-07-21 | 2014-11-20 | Мапикс Эс.Эй.Ар.Эл. | Способ лечения зависимости от психоактивных веществ, алкоголизма и табакокурения и лекарственное средство для лечения зависимости от психоактивных веществ, алкоголизма и табакокурения |
| WO2013068371A1 (en) | 2011-11-08 | 2013-05-16 | Intervet International B.V. | Soft chewable dosage form compositions of cannabinoid receptor type 1 (cb-1) antagonists |
| WO2014181357A1 (en) * | 2013-05-09 | 2014-11-13 | Council Of Scientific & Industrial Research | Novel pyrazole derivatives with silicon incorporation |
| US10897925B2 (en) | 2018-07-27 | 2021-01-26 | Joseph Pandolfino | Articles and formulations for smoking products and vaporizers |
| US20200035118A1 (en) | 2018-07-27 | 2020-01-30 | Joseph Pandolfino | Methods and products to facilitate smokers switching to a tobacco heating product or e-cigarettes |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US5780051A (en) * | 1992-04-02 | 1998-07-14 | Dynagen, Inc. | Methods and articles of manufacture for nicotine cessation and monitoring nicotine use |
| FR2692575B1 (fr) * | 1992-06-23 | 1995-06-30 | Sanofi Elf | Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| FR2713225B1 (fr) * | 1993-12-02 | 1996-03-01 | Sanofi Sa | N-pipéridino-3-pyrazolecarboxamide substitué. |
| US5596106A (en) * | 1994-07-15 | 1997-01-21 | Eli Lilly And Company | Cannabinoid receptor antagonists |
| FR2758723B1 (fr) * | 1997-01-28 | 1999-04-23 | Sanofi Sa | Utilisation des antagonistes des recepteurs aux cannabinoides centraux pour la preparation de medicaments |
| FR2765107B1 (fr) * | 1997-06-26 | 2000-03-24 | Sanofi Sa | Utilisation d'un antagoniste specifique des recepteurs 5ht2 pour la preparation de medicaments utiles dans le traitement du syndrome d'apnee du sommeil |
| FR2789079B3 (fr) | 1999-02-01 | 2001-03-02 | Sanofi Synthelabo | Derive d'acide pyrazolecarboxylique, sa preparation, les compositions pharmaceutiques en contenant |
| FR2804604B1 (fr) * | 2000-02-09 | 2005-05-27 | Sanofi Synthelabo | Utilisation d'un antagoniste des recepteurs aux cannabinoides centraux pour la preparation de medicaments utiles pour faciliter l'arret de la consommation de tabac |
-
2000
- 2000-02-09 FR FR0001682A patent/FR2804604B1/fr not_active Expired - Fee Related
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2001
- 2001-02-07 BR BR0108126-8A patent/BR0108126A/pt not_active Application Discontinuation
- 2001-02-07 EE EEP200200439A patent/EE04836B1/xx not_active IP Right Cessation
- 2001-02-07 AT AT01907722T patent/ATE292467T1/de not_active IP Right Cessation
- 2001-02-07 ES ES01907722T patent/ES2240416T3/es not_active Expired - Lifetime
- 2001-02-07 US US10/203,077 patent/US6930122B2/en not_active Expired - Fee Related
- 2001-02-07 MX MXPA02007766A patent/MXPA02007766A/es active IP Right Grant
- 2001-02-07 RS YUP-590/02A patent/RS50404B/sr unknown
- 2001-02-07 NZ NZ519924A patent/NZ519924A/en unknown
- 2001-02-07 EP EP01907722A patent/EP1257275B1/fr not_active Expired - Lifetime
- 2001-02-07 CA CA002397262A patent/CA2397262C/en not_active Expired - Fee Related
- 2001-02-07 AU AU35620/01A patent/AU781827B2/en not_active Ceased
- 2001-02-07 HU HU0300237A patent/HU225328B1/hu not_active IP Right Cessation
- 2001-02-07 PL PL358221A patent/PL201685B1/pl not_active IP Right Cessation
- 2001-02-07 JP JP2001557560A patent/JP2003522145A/ja not_active Ceased
- 2001-02-07 DE DE60109903T patent/DE60109903T2/de not_active Expired - Fee Related
- 2001-02-07 IL IL15071001A patent/IL150710A0/xx not_active IP Right Cessation
- 2001-02-07 RU RU2002118309/15A patent/RU2257207C2/ru not_active IP Right Cessation
- 2001-02-07 SI SI200130365T patent/SI1257275T1/xx unknown
- 2001-02-07 PT PT01907722T patent/PT1257275E/pt unknown
- 2001-02-07 BG BG110386A patent/BG110386A/en unknown
- 2001-02-07 CZ CZ20022698A patent/CZ296685B6/cs not_active IP Right Cessation
- 2001-02-07 DK DK01907722T patent/DK1257275T3/da active
- 2001-02-07 CN CNB018047130A patent/CN1250220C/zh not_active Expired - Fee Related
- 2001-02-07 WO PCT/FR2001/000356 patent/WO2001058450A2/fr active IP Right Grant
- 2001-02-07 SK SK1129-2002A patent/SK284952B6/sk not_active IP Right Cessation
- 2001-02-09 AR ARP010100587A patent/AR028505A1/es unknown
- 2001-02-19 TW TW090102783A patent/TWI243677B/zh active
- 2001-07-02 UA UA2002075476A patent/UA72783C2/uk unknown
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2002
- 2002-06-28 IS IS6450A patent/IS6450A/is unknown
- 2002-07-03 ZA ZA200205317A patent/ZA200205317B/en unknown
- 2002-07-23 BG BG106946A patent/BG65856B1/bg unknown
- 2002-08-08 NO NO20023765A patent/NO324521B1/no not_active IP Right Cessation
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2003
- 2003-05-12 HK HK03103301A patent/HK1051140A1/xx not_active IP Right Cessation
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2005
- 2005-04-25 US US11/113,864 patent/US20050187253A1/en not_active Abandoned
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- 2009-09-18 JP JP2009217269A patent/JP2010018622A/ja not_active Withdrawn
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