NO326465B1 - Krystallinsk natriumsalt av Telmiseartan, fremgangsmate for fremstilling av slike, farmasoytiske formuleringer innholdende slike og dets anvendelse som legemiddel - Google Patents
Krystallinsk natriumsalt av Telmiseartan, fremgangsmate for fremstilling av slike, farmasoytiske formuleringer innholdende slike og dets anvendelse som legemiddel Download PDFInfo
- Publication number
- NO326465B1 NO326465B1 NO20041758A NO20041758A NO326465B1 NO 326465 B1 NO326465 B1 NO 326465B1 NO 20041758 A NO20041758 A NO 20041758A NO 20041758 A NO20041758 A NO 20041758A NO 326465 B1 NO326465 B1 NO 326465B1
- Authority
- NO
- Norway
- Prior art keywords
- sodium salt
- acid
- telmisartan
- crystalline
- solvent
- Prior art date
Links
- 159000000000 sodium salts Chemical class 0.000 title claims description 30
- 238000000034 method Methods 0.000 title claims description 18
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 4
- 239000003814 drug Substances 0.000 title description 8
- 238000002360 preparation method Methods 0.000 title description 8
- 229940079593 drug Drugs 0.000 title description 4
- RMMXLENWKUUMAY-UHFFFAOYSA-N telmisartan Chemical compound CCCC1=NC2=C(C)C=C(C=3N(C4=CC=CC=C4N=3)C)C=C2N1CC(C=C1)=CC=C1C1=CC=CC=C1C(O)=O RMMXLENWKUUMAY-UHFFFAOYSA-N 0.000 claims description 45
- 239000002904 solvent Substances 0.000 claims description 35
- RSGAIWOEJXRYRV-UHFFFAOYSA-M sodium;2-[4-[[4-methyl-6-(1-methylbenzimidazol-2-yl)-2-propylbenzimidazol-1-yl]methyl]phenyl]benzoate Chemical compound [Na+].CCCC1=NC2=C(C)C=C(C=3N(C4=CC=CC=C4N=3)C)C=C2N1CC(C=C1)=CC=C1C1=CC=CC=C1C([O-])=O RSGAIWOEJXRYRV-UHFFFAOYSA-M 0.000 claims description 29
- 239000005537 C09CA07 - Telmisartan Substances 0.000 claims description 22
- 239000002253 acid Substances 0.000 claims description 22
- 238000004519 manufacturing process Methods 0.000 claims description 21
- 229960005187 telmisartan Drugs 0.000 claims description 21
- 239000003960 organic solvent Substances 0.000 claims description 19
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 16
- 150000001875 compounds Chemical class 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 9
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims description 8
- 239000000706 filtrate Substances 0.000 claims description 8
- 239000011541 reaction mixture Substances 0.000 claims description 7
- 150000004677 hydrates Chemical class 0.000 claims description 6
- LBLYYCQCTBFVLH-UHFFFAOYSA-N 2-Methylbenzenesulfonic acid Chemical compound CC1=CC=CC=C1S(O)(=O)=O LBLYYCQCTBFVLH-UHFFFAOYSA-N 0.000 claims description 4
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 claims description 4
- 238000010586 diagram Methods 0.000 claims description 4
- 229940126601 medicinal product Drugs 0.000 claims description 4
- 229940098779 methanesulfonic acid Drugs 0.000 claims description 4
- 239000000843 powder Substances 0.000 claims description 4
- 229940125782 compound 2 Drugs 0.000 claims description 3
- 238000002844 melting Methods 0.000 claims description 3
- 230000008018 melting Effects 0.000 claims description 3
- 239000012453 solvate Substances 0.000 claims description 3
- 238000005406 washing Methods 0.000 claims description 2
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 57
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 34
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 30
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 21
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 18
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 15
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 15
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 14
- 239000000203 mixture Substances 0.000 description 14
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 12
- WQDUMFSSJAZKTM-UHFFFAOYSA-N Sodium methoxide Chemical compound [Na+].[O-]C WQDUMFSSJAZKTM-UHFFFAOYSA-N 0.000 description 10
- 235000011121 sodium hydroxide Nutrition 0.000 description 10
- 239000011877 solvent mixture Substances 0.000 description 10
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 9
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 9
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 8
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 8
- 239000013543 active substance Substances 0.000 description 8
- 239000013078 crystal Substances 0.000 description 8
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 7
- 229960004592 isopropanol Drugs 0.000 description 7
- 239000000243 solution Substances 0.000 description 7
- TTWVBVXEOQKSLK-UHFFFAOYSA-N 2-[4-[[4-methyl-6-(1-methylbenzimidazol-2-yl)-2-propylbenzimidazol-1-yl]methyl]phenyl]benzoic acid;hydrochloride Chemical compound Cl.CCCC1=NC2=C(C)C=C(C=3N(C4=CC=CC=C4N=3)C)C=C2N1CC(C=C1)=CC=C1C1=CC=CC=C1C(O)=O TTWVBVXEOQKSLK-UHFFFAOYSA-N 0.000 description 6
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 6
- NTIZESTWPVYFNL-UHFFFAOYSA-N Methyl isobutyl ketone Chemical compound CC(C)CC(C)=O NTIZESTWPVYFNL-UHFFFAOYSA-N 0.000 description 6
- UIHCLUNTQKBZGK-UHFFFAOYSA-N Methyl isobutyl ketone Natural products CCC(C)C(C)=O UIHCLUNTQKBZGK-UHFFFAOYSA-N 0.000 description 6
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 description 6
- 238000006243 chemical reaction Methods 0.000 description 6
- 239000007787 solid Substances 0.000 description 6
- 238000011282 treatment Methods 0.000 description 6
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 5
- DKGAVHZHDRPRBM-UHFFFAOYSA-N Tert-Butanol Chemical compound CC(C)(C)O DKGAVHZHDRPRBM-UHFFFAOYSA-N 0.000 description 5
- 150000001298 alcohols Chemical class 0.000 description 5
- BTANRVKWQNVYAZ-UHFFFAOYSA-N butan-2-ol Chemical compound CCC(C)O BTANRVKWQNVYAZ-UHFFFAOYSA-N 0.000 description 5
- 239000011734 sodium Substances 0.000 description 5
- 229910052708 sodium Inorganic materials 0.000 description 5
- 239000000725 suspension Substances 0.000 description 5
- 206010019280 Heart failures Diseases 0.000 description 4
- KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 description 4
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 4
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 4
- 239000000010 aprotic solvent Substances 0.000 description 4
- 230000015572 biosynthetic process Effects 0.000 description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- ZXEKIIBDNHEJCQ-UHFFFAOYSA-N isobutanol Chemical compound CC(C)CO ZXEKIIBDNHEJCQ-UHFFFAOYSA-N 0.000 description 4
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 description 4
- 238000010992 reflux Methods 0.000 description 4
- 239000012312 sodium hydride Substances 0.000 description 4
- 229910000104 sodium hydride Inorganic materials 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- 238000003786 synthesis reaction Methods 0.000 description 4
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 4
- MSXVEPNJUHWQHW-UHFFFAOYSA-N 2-methylbutan-2-ol Chemical compound CCC(C)(C)O MSXVEPNJUHWQHW-UHFFFAOYSA-N 0.000 description 3
- ZAFNJMIOTHYJRJ-UHFFFAOYSA-N Diisopropyl ether Chemical compound CC(C)OC(C)C ZAFNJMIOTHYJRJ-UHFFFAOYSA-N 0.000 description 3
- 206010020772 Hypertension Diseases 0.000 description 3
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 description 3
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 3
- 229960000583 acetic acid Drugs 0.000 description 3
- 239000007864 aqueous solution Substances 0.000 description 3
- 238000009835 boiling Methods 0.000 description 3
- 238000010438 heat treatment Methods 0.000 description 3
- 238000011321 prophylaxis Methods 0.000 description 3
- QDRKDTQENPPHOJ-UHFFFAOYSA-N sodium ethoxide Chemical compound [Na+].CC[O-] QDRKDTQENPPHOJ-UHFFFAOYSA-N 0.000 description 3
- 239000007858 starting material Substances 0.000 description 3
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 2
- 206010002383 Angina Pectoris Diseases 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 description 2
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 2
- ZHNUHDYFZUAESO-UHFFFAOYSA-N Formamide Chemical compound NC=O ZHNUHDYFZUAESO-UHFFFAOYSA-N 0.000 description 2
- 208000018522 Gastrointestinal disease Diseases 0.000 description 2
- 208000010412 Glaucoma Diseases 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Chemical compound 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 2
- SECXISVLQFMRJM-UHFFFAOYSA-N N-Methylpyrrolidone Chemical compound CN1CCCC1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 description 2
- 239000002333 angiotensin II receptor antagonist Substances 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- 230000017531 blood circulation Effects 0.000 description 2
- WERYXYBDKMZEQL-UHFFFAOYSA-N butane-1,4-diol Chemical compound OCCCCO WERYXYBDKMZEQL-UHFFFAOYSA-N 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 239000013583 drug formulation Substances 0.000 description 2
- 230000007613 environmental effect Effects 0.000 description 2
- 239000012362 glacial acetic acid Substances 0.000 description 2
- 230000000302 ischemic effect Effects 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 239000012907 medicinal substance Substances 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 208000010125 myocardial infarction Diseases 0.000 description 2
- 208000031225 myocardial ischemia Diseases 0.000 description 2
- 239000012454 non-polar solvent Substances 0.000 description 2
- 210000005259 peripheral blood Anatomy 0.000 description 2
- 239000011886 peripheral blood Substances 0.000 description 2
- 230000004526 pharmaceutical effect Effects 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 2
- 235000017557 sodium bicarbonate Nutrition 0.000 description 2
- 229910000029 sodium carbonate Inorganic materials 0.000 description 2
- 208000026533 urinary bladder disease Diseases 0.000 description 2
- ARXJGSRGQADJSQ-UHFFFAOYSA-N 1-methoxypropan-2-ol Chemical compound COCC(C)O ARXJGSRGQADJSQ-UHFFFAOYSA-N 0.000 description 1
- 229940123413 Angiotensin II antagonist Drugs 0.000 description 1
- 229940123073 Angiotensin antagonist Drugs 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- 229920000623 Cellulose acetate phthalate Polymers 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- 229910016523 CuKa Inorganic materials 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- FXHOOIRPVKKKFG-UHFFFAOYSA-N N,N-Dimethylacetamide Chemical compound CN(C)C(C)=O FXHOOIRPVKKKFG-UHFFFAOYSA-N 0.000 description 1
- 241000004441 Sorites Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000008186 active pharmaceutical agent Substances 0.000 description 1
- 239000000783 alginic acid Substances 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 229920000615 alginic acid Polymers 0.000 description 1
- 229960001126 alginic acid Drugs 0.000 description 1
- 150000004781 alginic acids Chemical class 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 238000005452 bending Methods 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- 235000010216 calcium carbonate Nutrition 0.000 description 1
- 239000001506 calcium phosphate Substances 0.000 description 1
- 229910000389 calcium phosphate Inorganic materials 0.000 description 1
- 235000011010 calcium phosphates Nutrition 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 229940081734 cellulose acetate phthalate Drugs 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000004087 circulation Effects 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 238000000113 differential scanning calorimetry Methods 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 238000004821 distillation Methods 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- -1 ethyl diglycol Chemical compound 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 description 1
- 239000003701 inert diluent Substances 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 229940101564 micardis Drugs 0.000 description 1
- MCSAJNNLRCFZED-UHFFFAOYSA-N nitroethane Chemical compound CC[N+]([O-])=O MCSAJNNLRCFZED-UHFFFAOYSA-N 0.000 description 1
- LYGJENNIWJXYER-UHFFFAOYSA-N nitromethane Chemical compound C[N+]([O-])=O LYGJENNIWJXYER-UHFFFAOYSA-N 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229920002689 polyvinyl acetate Polymers 0.000 description 1
- 239000011118 polyvinyl acetate Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 230000000750 progressive effect Effects 0.000 description 1
- 230000005855 radiation Effects 0.000 description 1
- 238000007127 saponification reaction Methods 0.000 description 1
- 238000004611 spectroscopical analysis Methods 0.000 description 1
- 238000001694 spray drying Methods 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- JSCFLEBEWCTASN-UHFFFAOYSA-N tert-butyl 2-[4-[[4-methyl-6-(1-methylbenzimidazol-2-yl)-2-propylbenzimidazol-1-yl]methyl]phenyl]benzoate Chemical compound CCCC1=NC2=C(C)C=C(C=3N(C4=CC=CC=C4N=3)C)C=C2N1CC(C=C1)=CC=C1C1=CC=CC=C1C(=O)OC(C)(C)C JSCFLEBEWCTASN-UHFFFAOYSA-N 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/20—Two benzimidazolyl-2 radicals linked together directly or via a hydrocarbon or substituted hydrocarbon radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Ophthalmology & Optometry (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10153737A DE10153737A1 (de) | 2001-10-31 | 2001-10-31 | Kristallines Natriumsalz des Telmisartans, Verfahren zu dessen Herstellung und dessen Verwendung zur Herstellung eines Arzneimittels |
| PCT/EP2002/011394 WO2003037876A1 (de) | 2001-10-31 | 2002-10-11 | Kristallines natriumsalz des telmisartans und dessen verwendung als angiotensin antagonist |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NO20041758L NO20041758L (no) | 2004-04-29 |
| NO326465B1 true NO326465B1 (no) | 2008-12-08 |
Family
ID=7704331
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO20041758A NO326465B1 (no) | 2001-10-31 | 2004-04-29 | Krystallinsk natriumsalt av Telmiseartan, fremgangsmate for fremstilling av slike, farmasoytiske formuleringer innholdende slike og dets anvendelse som legemiddel |
Country Status (35)
| Country | Link |
|---|---|
| EP (1) | EP1442023B1 (hu) |
| JP (1) | JP5124076B2 (hu) |
| KR (1) | KR100929502B1 (hu) |
| CN (1) | CN100509789C (hu) |
| AR (1) | AR037148A1 (hu) |
| AT (1) | ATE370125T1 (hu) |
| AU (1) | AU2002338886B2 (hu) |
| BR (1) | BR0213568A (hu) |
| CA (1) | CA2463146C (hu) |
| CO (1) | CO5580785A2 (hu) |
| CY (1) | CY1107504T1 (hu) |
| DE (2) | DE10153737A1 (hu) |
| DK (1) | DK1442023T3 (hu) |
| EA (1) | EA007596B1 (hu) |
| EC (1) | ECSP045089A (hu) |
| ES (1) | ES2291505T3 (hu) |
| HK (1) | HK1073841A1 (hu) |
| HR (1) | HRPK20040372B3 (hu) |
| HU (1) | HUP0402391A3 (hu) |
| IL (2) | IL161165A0 (hu) |
| ME (1) | MEP43608A (hu) |
| MX (1) | MXPA04004013A (hu) |
| MY (1) | MY129741A (hu) |
| NO (1) | NO326465B1 (hu) |
| NZ (1) | NZ532716A (hu) |
| PE (1) | PE20030629A1 (hu) |
| PL (1) | PL211462B1 (hu) |
| PT (1) | PT1442023E (hu) |
| RS (1) | RS50879B (hu) |
| SA (1) | SA02230419B1 (hu) |
| SI (1) | SI1442023T1 (hu) |
| TW (2) | TWI341200B (hu) |
| UA (1) | UA82833C2 (hu) |
| UY (1) | UY27520A1 (hu) |
| WO (1) | WO2003037876A1 (hu) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10319450A1 (de) * | 2003-04-30 | 2004-11-18 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pharmazeutische Formulierung des Telmisartan Natriumsalzes |
| US9029363B2 (en) | 2003-04-30 | 2015-05-12 | Boehringer Ingelheim International Gmbh | Telmisartan sodium salt pharmaceutical formulation |
| WO2005077941A2 (en) | 2004-02-11 | 2005-08-25 | Teva Pharmaceutical Industries Ltd. | Candesartan cilexetil polymorphs |
| CN1953973A (zh) * | 2004-05-05 | 2007-04-25 | 特瓦制药工业有限公司 | 高纯度坎地沙坦酯的制备 |
| WO2006044754A2 (en) | 2004-10-18 | 2006-04-27 | Dr. Reddy's Laboratories Ltd. | Process for preparing telmisartan |
| WO2006050509A2 (en) * | 2004-11-03 | 2006-05-11 | Teva Pharmaceutical Industries Ltd. | Amorphous and polymorphic forms of telmisartan sodium |
| EP1908469A1 (en) | 2006-10-06 | 2008-04-09 | Boehringer Ingelheim Vetmedica Gmbh | Angiotensin II receptor antagonist for the treatment of systemic diseases in cats |
| EP2151450A1 (de) * | 2008-07-29 | 2010-02-10 | Sandoz AG | Verfahren zur Aufarbeitung von mikrobiologisch hergestellten zyklischen Oligopeptiden |
| MX346039B (es) | 2009-05-20 | 2017-03-03 | Boehringer Ingelheim Vetmedica Gmbh | Solucion farmaceutica bebible de telmisartan. |
| EP2448576A2 (en) | 2009-07-02 | 2012-05-09 | Mahmut Bilgic | Solubility enhancing pharmaceutical composition |
| EP2448575A2 (en) | 2009-07-02 | 2012-05-09 | Bilgic Mahmut | Pharmaceutical composition increasing solubility and stability |
| EP2632438A1 (en) | 2010-10-27 | 2013-09-04 | KRKA, tovarna zdravil, d.d., Novo mesto | Multilayer pharmaceutical composition comprising telmisartan and amlodipine |
| CN103619556B (zh) * | 2011-06-24 | 2016-12-07 | 本田技研工业株式会社 | 注塑成形方法及其装置 |
| ES2864009T3 (es) | 2011-11-25 | 2021-10-13 | Adverio Pharma Gmbh | 5-Fluoro-1H-pirazolopiridinas sustituidas en forma cristalina |
| KR102331856B1 (ko) | 2014-10-21 | 2021-11-29 | 다케다 야쿠힌 고교 가부시키가이샤 | 결정 형태의 5-클로로-n4-[2-(디메틸포스포릴)페닐]-n2-｛2-메톡시-4-[4-(4-메틸피페라진-1-일)피페리딘-1-일]피리미딘-2,4-디아민 |
| KR101872726B1 (ko) * | 2016-07-28 | 2018-06-29 | 주식회사 씨트리 | 텔미사르탄 메탄술폰산염 및 이를 포함하는 약제학적 조성물 |
| CA3067918A1 (en) | 2017-07-07 | 2019-01-10 | Boehringer Ingelheim Vetmedica Gmbh | Angiotensin ii receptor antagonish for the prevention or treatment of hypertension in cats |
| CN113330013B (zh) * | 2019-01-10 | 2022-12-27 | 石药集团中奇制药技术（石家庄）有限公司 | 杂环化合物盐及其应用 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI9210098B (sl) * | 1991-02-06 | 2000-06-30 | Dr. Karl Thomae | Benzimidazoli, zdravila, ki te spojine vsebujejo, in postopek za njihovo pripravo |
| US5594003A (en) * | 1991-02-06 | 1997-01-14 | Dr. Karl Thomae Gmbh | Tetrahydroimidazo[1,2-a]pyridin-2-yl-(benzimidazol-1-yl)-methyl-biphenyls useful as angiotensin-II antagonists |
| JP4369994B2 (ja) * | 1996-02-29 | 2009-11-25 | ノバルティス アクチエンゲゼルシャフト | アポトーシスの刺激のためのａｔ▲下１▼レセプターアンタゴニスト |
| DE19901921C2 (de) * | 1999-01-19 | 2001-01-04 | Boehringer Ingelheim Pharma | Polymorphe von Telmisartan, Verfahren zu deren Herstellung und deren Verwendung zur Herstellung eines Arzneimittels |
-
2001
- 2001-10-31 DE DE10153737A patent/DE10153737A1/de not_active Ceased
-
2002
- 2002-10-11 BR BR0213568-0A patent/BR0213568A/pt active Pending
- 2002-10-11 RS YUP-363/04A patent/RS50879B/sr unknown
- 2002-10-11 WO PCT/EP2002/011394 patent/WO2003037876A1/de active IP Right Grant
- 2002-10-11 JP JP2003540158A patent/JP5124076B2/ja not_active Expired - Lifetime
- 2002-10-11 PL PL367477A patent/PL211462B1/pl unknown
- 2002-10-11 DE DE50210719T patent/DE50210719D1/de not_active Expired - Lifetime
- 2002-10-11 HU HU0402391A patent/HUP0402391A3/hu not_active Application Discontinuation
- 2002-10-11 ES ES02777305T patent/ES2291505T3/es not_active Expired - Lifetime
- 2002-10-11 EP EP02777305A patent/EP1442023B1/de not_active Expired - Lifetime
- 2002-10-11 MX MXPA04004013A patent/MXPA04004013A/es active IP Right Grant
- 2002-10-11 EA EA200400479A patent/EA007596B1/ru not_active IP Right Cessation
- 2002-10-11 PT PT02777305T patent/PT1442023E/pt unknown
- 2002-10-11 SI SI200230594T patent/SI1442023T1/sl unknown
- 2002-10-11 KR KR1020047006317A patent/KR100929502B1/ko not_active IP Right Cessation
- 2002-10-11 NZ NZ532716A patent/NZ532716A/en not_active IP Right Cessation
- 2002-10-11 ME MEP-436/08A patent/MEP43608A/xx unknown
- 2002-10-11 IL IL16116502A patent/IL161165A0/xx unknown
- 2002-10-11 DK DK02777305T patent/DK1442023T3/da active
- 2002-10-11 CN CNB028216202A patent/CN100509789C/zh not_active Expired - Fee Related
- 2002-10-11 CA CA2463146A patent/CA2463146C/en not_active Expired - Fee Related
- 2002-10-11 AU AU2002338886A patent/AU2002338886B2/en not_active Ceased
- 2002-10-11 AT AT02777305T patent/ATE370125T1/de active
- 2002-10-28 UY UY27520A patent/UY27520A1/es not_active Application Discontinuation
- 2002-10-28 PE PE2002001061A patent/PE20030629A1/es not_active Application Discontinuation
- 2002-10-29 MY MYPI20024051A patent/MY129741A/en unknown
- 2002-10-29 TW TW099114822A patent/TWI341200B/zh not_active IP Right Cessation
- 2002-10-29 TW TW091132070A patent/TWI333419B/zh not_active IP Right Cessation
- 2002-10-30 AR ARP020104113A patent/AR037148A1/es active Pending
- 2002-11-05 SA SA02230419A patent/SA02230419B1/ar unknown
- 2002-11-10 UA UA20040503959A patent/UA82833C2/uk unknown
-
2004
- 2004-03-30 IL IL161165A patent/IL161165A/en not_active IP Right Cessation
- 2004-04-26 HR HR20040372A patent/HRPK20040372B3/xx not_active IP Right Cessation
- 2004-04-27 EC EC2004005089A patent/ECSP045089A/es unknown
- 2004-04-29 NO NO20041758A patent/NO326465B1/no not_active IP Right Cessation
- 2004-05-07 CO CO04042445A patent/CO5580785A2/es not_active Application Discontinuation
-
2005
- 2005-07-26 HK HK05106371.1A patent/HK1073841A1/xx not_active IP Right Cessation
-
2007
- 2007-10-15 CY CY20071101332T patent/CY1107504T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| NO326465B1 (no) | Krystallinsk natriumsalt av Telmiseartan, fremgangsmate for fremstilling av slike, farmasoytiske formuleringer innholdende slike og dets anvendelse som legemiddel | |
| US20060276526A1 (en) | Crystalline Form of Telmisartan Sodium | |
| ZA200507223B (en) | Pharmaceutical formulation of the sodium salt of telmisartan | |
| US9029363B2 (en) | Telmisartan sodium salt pharmaceutical formulation | |
| US20080234323A1 (en) | Amorphous and Three Crystalline Forms of Rimonabant Hydrochloride | |
| EP2552910B1 (en) | New polymorph | |
| EP2139866B1 (en) | Crystalline 1-(cyclohexyloxycarbonyloxy) ethyl 1-((2'-cyanobiphenyl-4-yl)methyl)-2-ethoxy-1h-benzo[d]imidazole-7-carboxylate and a process for its preparation | |
| CN110483401A (zh) | 艾沙利酮药用盐及其制备方法和医药应用 | |
| EP1944297A1 (en) | Solid and crystalline rimonabant and processes for preparation, and pharmaceutical composition thereof | |
| CN108530391B (zh) | 一种酰胺类芳基哌嗪衍生物及其制备方法与应用 | |
| ZA200401780B (en) | Crystalline sodium salt of telmisartan and the use of the same as an angiotensin antagonist |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM1K | Lapsed by not paying the annual fees |