ZA200203755B - Polymorphic form of atorvastatin calcium. - Google Patents

Polymorphic form of atorvastatin calcium. Download PDF

Info

Publication number: ZA200203755B
Authority: ZA; South Africa
Prior art keywords: atorvastatin; calcium; salt; atorvastatin calcium; solvent
Prior art date: 1999-11-17

Application number

ZA200203755A

Other languages

English (en)

Inventor

Ari Ayalon

Michal Levinger

Sofia Roytblat

Valerie Niddam

Revital Lifshitz

Judith Aronhime

Original Assignee

Teva Pharma

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

1999-11-17

Filing date

2002-05-10

Publication date

2004-05-26

2002-05-10 Application filed by Teva Pharma filed Critical Teva Pharma

2004-05-26 Publication of ZA200203755B publication Critical patent/ZA200203755B/en

Links

OJRHUICOVVSGSY-RXMQYKEDSA-N (2s)-2-chloro-3-methylbutan-1-ol Chemical compound CC(C)[C@H](Cl)CO OJRHUICOVVSGSY-RXMQYKEDSA-N 0.000 title claims description 56
229960001770 atorvastatin calcium Drugs 0.000 title claims description 30
XUKUURHRXDUEBC-KAYWLYCHSA-N Atorvastatin Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-KAYWLYCHSA-N 0.000 claims description 50
159000000007 calcium salts Chemical class 0.000 claims description 31
OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical group OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 27
239000002904 solvent Substances 0.000 claims description 25
XUKUURHRXDUEBC-UHFFFAOYSA-N Atorvastatin Natural products C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CCC(O)CC(O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-UHFFFAOYSA-N 0.000 claims description 24
229960005370 atorvastatin Drugs 0.000 claims description 24
239000012266 salt solution Substances 0.000 claims description 23
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 19
238000000034 method Methods 0.000 claims description 15
239000000843 powder Substances 0.000 claims description 11
230000008569 process Effects 0.000 claims description 11
239000007787 solid Substances 0.000 claims description 11
150000003839 salts Chemical class 0.000 claims description 10
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical group CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 8
WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims description 6
VSGNNIFQASZAOI-UHFFFAOYSA-L calcium acetate Chemical group [Ca+2].CC([O-])=O.CC([O-])=O VSGNNIFQASZAOI-UHFFFAOYSA-L 0.000 claims description 5
239000001639 calcium acetate Substances 0.000 claims description 5
235000011092 calcium acetate Nutrition 0.000 claims description 5
229960005147 calcium acetate Drugs 0.000 claims description 5
150000004677 hydrates Chemical class 0.000 claims description 5
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QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 claims description 2
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YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 2
125000005210 alkyl ammonium group Chemical group 0.000 claims 1
239000000243 solution Substances 0.000 description 19
-1 alkali metal salts Chemical class 0.000 description 12
HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 10
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VVRPOCPLIUDBSA-CNZCJKERSA-M sodium;(3r,5r)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-propan-2-ylpyrrol-1-yl]-3,5-dihydroxyheptanoate Chemical group [Na+].C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC([O-])=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 VVRPOCPLIUDBSA-CNZCJKERSA-M 0.000 description 5
VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 4
229940121710 HMGCoA reductase inhibitor Drugs 0.000 description 4
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 4
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IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 3
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102100029077 3-hydroxy-3-methylglutaryl-coenzyme A reductase Human genes 0.000 description 2
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PPBRXRYQALVLMV-UHFFFAOYSA-N Styrene Chemical compound C=CC1=CC=CC=C1 PPBRXRYQALVLMV-UHFFFAOYSA-N 0.000 description 2
MCMNRKCIXSYSNV-UHFFFAOYSA-N Zirconium dioxide Chemical compound O=[Zr]=O MCMNRKCIXSYSNV-UHFFFAOYSA-N 0.000 description 2
239000002253 acid Substances 0.000 description 2
150000001298 alcohols Chemical class 0.000 description 2
125000005599 alkyl carboxylate group Chemical group 0.000 description 2
125000000217 alkyl group Chemical group 0.000 description 2
239000011230 binding agent Substances 0.000 description 2
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229910000019 calcium carbonate Inorganic materials 0.000 description 2
OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 description 2
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239000003610 charcoal Substances 0.000 description 2
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238000009505 enteric coating Methods 0.000 description 2
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239000007788 liquid Substances 0.000 description 2
239000002245 particle Substances 0.000 description 2
230000002093 peripheral effect Effects 0.000 description 2
XNGIFLGASWRNHJ-UHFFFAOYSA-L phthalate(2-) Chemical compound [O-]C(=O)C1=CC=CC=C1C([O-])=O XNGIFLGASWRNHJ-UHFFFAOYSA-L 0.000 description 2
XNGIFLGASWRNHJ-UHFFFAOYSA-N phthalic acid Chemical compound OC(=O)C1=CC=CC=C1C(O)=O XNGIFLGASWRNHJ-UHFFFAOYSA-N 0.000 description 2
230000009467 reduction Effects 0.000 description 2
239000011734 sodium Substances 0.000 description 2
239000012453 solvate Substances 0.000 description 2
239000000126 substance Substances 0.000 description 2
150000003871 sulfonates Chemical class 0.000 description 2
LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 description 1
CABVTRNMFUVUDM-VRHQGPGLSA-N (3S)-3-hydroxy-3-methylglutaryl-CoA Chemical compound O[C@@H]1[C@H](OP(O)(O)=O)[C@@H](COP(O)(=O)OP(O)(=O)OCC(C)(C)[C@@H](O)C(=O)NCCC(=O)NCCSC(=O)C[C@@](O)(CC(O)=O)C)O[C@H]1N1C2=NC=NC(N)=C2N=C1 CABVTRNMFUVUDM-VRHQGPGLSA-N 0.000 description 1
XUKUURHRXDUEBC-SVBPBHIXSA-N (3s,5s)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-propan-2-ylpyrrol-1-yl]-3,5-dihydroxyheptanoic acid Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@H](O)C[C@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-SVBPBHIXSA-N 0.000 description 1
KJTLQQUUPVSXIM-ZCFIWIBFSA-M (R)-mevalonate Chemical compound OCC[C@](O)(C)CC([O-])=O KJTLQQUUPVSXIM-ZCFIWIBFSA-M 0.000 description 1
IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 1
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QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
FERIUCNNQQJTOY-UHFFFAOYSA-M Butyrate Chemical compound CCCC([O-])=O FERIUCNNQQJTOY-UHFFFAOYSA-M 0.000 description 1
FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Natural products CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 description 1
OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical class [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
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FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
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FQCKMBLVYCEXJB-MNSAWQCASA-L atorvastatin calcium Chemical compound [Ca+2].C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC([O-])=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1.C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC([O-])=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 FQCKMBLVYCEXJB-MNSAWQCASA-L 0.000 description 1
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229910002804 graphite Inorganic materials 0.000 description 1
238000010438 heat treatment Methods 0.000 description 1
238000004128 high performance liquid chromatography Methods 0.000 description 1
230000036571 hydration Effects 0.000 description 1
238000006703 hydration reaction Methods 0.000 description 1
235000019447 hydroxyethyl cellulose Nutrition 0.000 description 1
239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 description 1
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239000001863 hydroxypropyl cellulose Substances 0.000 description 1
235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
229920003088 hydroxypropyl methyl cellulose Polymers 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
229940031704 hydroxypropyl methylcellulose phthalate Drugs 0.000 description 1
239000012535 impurity Substances 0.000 description 1
230000002401 inhibitory effect Effects 0.000 description 1
230000005764 inhibitory process Effects 0.000 description 1
229910052500 inorganic mineral Inorganic materials 0.000 description 1
230000003993 interaction Effects 0.000 description 1
210000000936 intestine Anatomy 0.000 description 1
238000007918 intramuscular administration Methods 0.000 description 1
238000001990 intravenous administration Methods 0.000 description 1
150000002596 lactones Chemical class 0.000 description 1
238000007273 lactonization reaction Methods 0.000 description 1
230000003902 lesion Effects 0.000 description 1
150000002632 lipids Chemical class 0.000 description 1
229940002661 lipitor Drugs 0.000 description 1
239000006194 liquid suspension Substances 0.000 description 1
229910052744 lithium Inorganic materials 0.000 description 1
229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 1
239000000314 lubricant Substances 0.000 description 1
239000011777 magnesium Substances 0.000 description 1
229910052749 magnesium Inorganic materials 0.000 description 1
159000000003 magnesium salts Chemical class 0.000 description 1
235000019359 magnesium stearate Nutrition 0.000 description 1
HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Substances [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 1
MZUOYVUQORIPHP-MNSAWQCASA-L magnesium;(3r,5r)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-propan-2-ylpyrrol-1-yl]-3,5-dihydroxyheptanoate Chemical group [Mg+2].C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC([O-])=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1.C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC([O-])=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 MZUOYVUQORIPHP-MNSAWQCASA-L 0.000 description 1
VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
239000011976 maleic acid Substances 0.000 description 1
239000000594 mannitol Substances 0.000 description 1
235000010355 mannitol Nutrition 0.000 description 1
238000005259 measurement Methods 0.000 description 1
230000010534 mechanism of action Effects 0.000 description 1
230000004060 metabolic process Effects 0.000 description 1
238000005272 metallurgy Methods 0.000 description 1
229920003145 methacrylic acid copolymer Polymers 0.000 description 1
229920000609 methyl cellulose Polymers 0.000 description 1
235000010981 methylcellulose Nutrition 0.000 description 1
239000001923 methylcellulose Substances 0.000 description 1
229940016286 microcrystalline cellulose Drugs 0.000 description 1
235000019813 microcrystalline cellulose Nutrition 0.000 description 1
239000008108 microcrystalline cellulose Substances 0.000 description 1
239000011707 mineral Substances 0.000 description 1
238000012986 modification Methods 0.000 description 1
230000004048 modification Effects 0.000 description 1
235000019691 monocalcium phosphate Nutrition 0.000 description 1
210000003205 muscle Anatomy 0.000 description 1
229910052757 nitrogen Inorganic materials 0.000 description 1
238000010899 nucleation Methods 0.000 description 1
QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
235000010987 pectin Nutrition 0.000 description 1
239000001814 pectin Substances 0.000 description 1
229920001277 pectin Polymers 0.000 description 1
230000000144 pharmacologic effect Effects 0.000 description 1
239000004014 plasticizer Substances 0.000 description 1
229920000058 polyacrylate Polymers 0.000 description 1
229920002451 polyvinyl alcohol Polymers 0.000 description 1
235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 1
229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
159000000001 potassium salts Chemical class 0.000 description 1
229920003124 powdered cellulose Polymers 0.000 description 1
235000019814 powdered cellulose Nutrition 0.000 description 1
238000002360 preparation method Methods 0.000 description 1
239000003755 preservative agent Substances 0.000 description 1
238000012545 processing Methods 0.000 description 1
238000000746 purification Methods 0.000 description 1
230000005855 radiation Effects 0.000 description 1
238000009790 rate-determining step (RDS) Methods 0.000 description 1
239000011541 reaction mixture Substances 0.000 description 1
238000001953 recrystallisation Methods 0.000 description 1
238000011160 research Methods 0.000 description 1
229910052710 silicon Inorganic materials 0.000 description 1
239000010703 silicon Substances 0.000 description 1
239000000377 silicon dioxide Substances 0.000 description 1
RYMZZMVNJRMUDD-HGQWONQESA-N simvastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 RYMZZMVNJRMUDD-HGQWONQESA-N 0.000 description 1
229960002855 simvastatin Drugs 0.000 description 1
229910052708 sodium Inorganic materials 0.000 description 1
235000010413 sodium alginate Nutrition 0.000 description 1
239000000661 sodium alginate Substances 0.000 description 1
229940005550 sodium alginate Drugs 0.000 description 1
229920003109 sodium starch glycolate Polymers 0.000 description 1
239000008109 sodium starch glycolate Substances 0.000 description 1
229940079832 sodium starch glycolate Drugs 0.000 description 1
229940045902 sodium stearyl fumarate Drugs 0.000 description 1
HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
239000007909 solid dosage form Substances 0.000 description 1
239000000600 sorbitol Substances 0.000 description 1
238000001228 spectrum Methods 0.000 description 1
239000008107 starch Substances 0.000 description 1
235000019698 starch Nutrition 0.000 description 1
229940032147 starch Drugs 0.000 description 1
150000003432 sterols Chemical class 0.000 description 1
235000003702 sterols Nutrition 0.000 description 1
210000002784 stomach Anatomy 0.000 description 1
238000007920 subcutaneous administration Methods 0.000 description 1
KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
235000000346 sugar Nutrition 0.000 description 1
150000005846 sugar alcohols Chemical class 0.000 description 1
150000008163 sugars Chemical class 0.000 description 1
239000000829 suppository Substances 0.000 description 1
230000004083 survival effect Effects 0.000 description 1
239000003765 sweetening agent Substances 0.000 description 1
238000003786 synthesis reaction Methods 0.000 description 1
229940095064 tartrate Drugs 0.000 description 1
VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
230000017105 transposition Effects 0.000 description 1
150000003626 triacylglycerols Chemical class 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
235000019731 tricalcium phosphate Nutrition 0.000 description 1
VLCLHFYFMCKBRP-UHFFFAOYSA-N tricalcium;diborate Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]B([O-])[O-].[O-]B([O-])[O-] VLCLHFYFMCKBRP-UHFFFAOYSA-N 0.000 description 1
238000003828 vacuum filtration Methods 0.000 description 1
239000001993 wax Substances 0.000 description 1
238000005550 wet granulation Methods 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- 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
- A61P3/06—Antihyperlipidemics

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Life Sciences & Earth Sciences (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Epidemiology (AREA)
Obesity (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Hematology (AREA)
Diabetes (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Pyrrole Compounds (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Steroid Compounds (AREA)

ZA200203755A 1999-11-17 2002-05-10 Polymorphic form of atorvastatin calcium. ZA200203755B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US16615399P	1999-11-17	1999-11-17

Publications (1)

Publication Number	Publication Date
ZA200203755B true ZA200203755B (en)	2004-05-26

Family

ID=22602039

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
ZA200203755A ZA200203755B (en)	1999-11-17	2002-05-10	Polymorphic form of atorvastatin calcium.

Country Status (20)

Country	Link
EP (3)	EP2206497A1 (de)
JP (2)	JP2003514798A (de)
KR (1)	KR20020063190A (de)
CN (1)	CN1423634A (de)
AT (2)	ATE478665T1 (de)
AU (1)	AU783002B2 (de)
CA (1)	CA2392096C (de)
CZ (1)	CZ20021642A3 (de)
DE (2)	DE60044884D1 (de)
ES (2)	ES2349364T3 (de)
HR (1)	HRP20020429B8 (de)
HU (1)	HUP0203257A3 (de)
IL (2)	IL149681A0 (de)
PL (1)	PL355805A1 (de)
PT (2)	PT1235799E (de)
SI (2)	SI1535613T1 (de)
SK (1)	SK286789B6 (de)
WO (1)	WO2001036384A1 (de)
YU (1)	YU35802A (de)
ZA (1)	ZA200203755B (de)

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EP1807055A1 (de)	2004-10-28	2007-07-18	Warner-Lambert Company LLC	Verfahren zur herstellung von amorphem atorvastatin
WO2006048894A1 (en) *	2004-11-05	2006-05-11	Morepen Laboratories Limited	Novel crystalline forms of atorvastatin calcium and processes for preparing them.
WO2006054308A2 (en)	2004-11-22	2006-05-26	Dexcel Pharma Technologies Ltd.	Stable atorvastatin formulations
CA2499047A1 (en)	2005-03-01	2006-09-01	Apotex Pharmachem Inc.	Process for producing atorvastatin hemicalcium
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EP1928823B1 (de)	2005-08-15	2014-10-08	Arrow International Limited	Verfahren zur Herstellung eines kristallinen ATORVASTATIN Natrium Salzes
CA2547216A1 (en)	2005-09-21	2007-03-21	Renuka D. Reddy	Process for annealing amorphous atorvastatin
EP1923057A1 (de)	2005-11-21	2008-05-21	Teva Pharmaceutical Industries Ltd	Pharmazeutische Atorvastatin-Formulierung
EP1808162A1 (de)	2005-11-21	2007-07-18	Teva Pharmaceutical Industries Ltd.	Pharmazeutische Formulierung von Atorvastatin
DK1957452T3 (da)	2005-11-21	2010-07-26	Warner Lambert Co	Nye former af [R-(R,R)]-2-(4-fluorphenyl)-B,B-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-heptansyre- magnesium
MX2007014329A (es) *	2005-12-13	2008-03-19	Teva Pharma	Forma cristalina de hemi-calcio de atorvastatina y procesos para la preparacion de ella.
EP1810667A1 (de)	2006-01-20	2007-07-25	KRKA, tovarna zdravil, d.d., Novo mesto	Pharmazeutische Zusammensetzung enthaltend amorphes Atorvastatin
AU2007219107B2 (en) *	2006-02-22	2012-12-06	Mylan Laboratories Ltd.	New crystalline form of Atorvastatin hemi-calcium
JP2010520273A (ja) *	2007-03-02	2010-06-10	ドン・ア・ファーム・カンパニー・リミテッド	ピロリルヘプタン酸誘導体の新規な結晶形態
EP2170841A1 (de)	2007-06-29	2010-04-07	Merck Generics (UK) Limited	Verfahren zur einführung einer hydroxyethoxy-seitenkette in bosentan
EP2185527A2 (de) *	2007-07-11	2010-05-19	Actavis Group PTC EHF	Neues polymorph von atorvastatin-calcium und seine verwendung zur herstellung von amorphem atorvastatin-calcium
US8530488B2 (en)	2007-10-24	2013-09-10	Generics [Uk] Limited	Crystalline forms of bosentan
NZ587793A (en)	2008-02-08	2012-06-29	Generics Uk Ltd	Process for preparing bosentan
CA2741928A1 (en)	2008-11-03	2010-06-03	Generics [Uk] Limited	Hplc method for the analysis of bosentan and related substances and use of these substances as reference standards and markers
EP2327682A1 (de) *	2009-10-29	2011-06-01	KRKA, D.D., Novo Mesto	Verwendung von amphiphilen Verbindungen zur gesteuerten Kristallisation von Statinen und Statin Zwischenprodukte.
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KR20120011249A (ko) *	2010-07-28	2012-02-07	주식회사 경보제약	아토바스타틴 헤미칼슘염의 신규한 결정형, 이의 수화물, 및 그의 제조방법
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DE69324504T2 (de) *	1993-01-19	1999-08-26	Warner-Lambert Co.	Stabilisierte, oral anzuwendende zusammensetzung enthaltend die verbindung ci-981 und verfahren
IL128864A (en) *	1995-07-17	2007-10-31	Warner Lambert Co	Atorostatin II form crystals and its hydrates, methods of preparation and pharmaceutical preparations containing it
HRP960313B1 (en) *	1995-07-17	2002-08-31	Warner Lambert Co	Form iii crystalline (r- (r, r)-2- (4-fluorophenyl) -beta-delta-hydroxy-5-(1-methylethyl) -3-phenyl-4- ((phenylamino) carbonyl -1h-pyrrole-1-heptanoic acid calcium salt (2:1)

2000
- 2000-11-16 DE DE60044884T patent/DE60044884D1/de not_active Expired - Lifetime
- 2000-11-16 JP JP2001538875A patent/JP2003514798A/ja not_active Withdrawn
- 2000-11-16 CZ CZ20021642A patent/CZ20021642A3/cs unknown
- 2000-11-16 HU HU0203257A patent/HUP0203257A3/hu unknown
- 2000-11-16 EP EP10157435A patent/EP2206497A1/de not_active Withdrawn
- 2000-11-16 PL PL00355805A patent/PL355805A1/xx not_active Application Discontinuation
- 2000-11-16 AT AT04027375T patent/ATE478665T1/de not_active IP Right Cessation
- 2000-11-16 SI SI200031061T patent/SI1535613T1/sl unknown
- 2000-11-16 CA CA002392096A patent/CA2392096C/en not_active Expired - Fee Related
- 2000-11-16 EP EP04027375A patent/EP1535613B1/de not_active Expired - Lifetime
- 2000-11-16 PT PT00978744T patent/PT1235799E/pt unknown
- 2000-11-16 KR KR1020027006304A patent/KR20020063190A/ko not_active Ceased
- 2000-11-16 CN CN00818409A patent/CN1423634A/zh active Pending
- 2000-11-16 SI SI200030648T patent/SI1235799T1/xx unknown
- 2000-11-16 EP EP00978744A patent/EP1235799B1/de not_active Expired - Lifetime
- 2000-11-16 YU YU35802A patent/YU35802A/sh unknown
- 2000-11-16 IL IL14968100A patent/IL149681A0/xx active IP Right Grant
- 2000-11-16 AU AU16173/01A patent/AU783002B2/en not_active Ceased
- 2000-11-16 ES ES04027375T patent/ES2349364T3/es not_active Expired - Lifetime
- 2000-11-16 SK SK674-2002A patent/SK286789B6/sk not_active IP Right Cessation
- 2000-11-16 HR HR20020429A patent/HRP20020429B8/xx not_active IP Right Cessation
- 2000-11-16 ES ES00978744T patent/ES2234699T3/es not_active Expired - Lifetime
- 2000-11-16 AT AT00978744T patent/ATE288893T1/de not_active IP Right Cessation
- 2000-11-16 WO PCT/US2000/031555 patent/WO2001036384A1/en not_active Ceased
- 2000-11-16 PT PT04027375T patent/PT1535613E/pt unknown
- 2000-11-16 DE DE60018100T patent/DE60018100T2/de not_active Expired - Lifetime
2002
- 2002-05-10 ZA ZA200203755A patent/ZA200203755B/en unknown
- 2002-05-15 IL IL149681A patent/IL149681A/en unknown
2009
- 2009-02-12 JP JP2009030514A patent/JP2009102439A/ja active Pending

Also Published As

Publication number	Publication date
HUP0203257A2 (hu)	2003-01-28
PT1535613E (pt)	2010-10-04
EP1235799A1 (de)	2002-09-04
PT1235799E (pt)	2005-05-31
CN1423634A (zh)	2003-06-11
IL149681A0 (en)	2002-11-10
JP2009102439A (ja)	2009-05-14
ATE478665T1 (de)	2010-09-15
DE60044884D1 (de)	2010-10-07
IL149681A (en)	2007-06-17
AU783002B2 (en)	2005-09-15
SK6742002A3 (en)	2003-05-02
DE60018100T2 (de)	2005-09-15
SK286789B6 (sk)	2009-05-07
YU35802A (sh)	2005-07-19
SI1535613T1 (sl)	2010-12-31
EP1535613A3 (de)	2005-08-31
EP1235799A4 (de)	2003-05-28
HRP20020429B1 (en)	2006-05-31
WO2001036384A1 (en)	2001-05-25
CA2392096A1 (en)	2001-05-25
HRP20020429A2 (en)	2004-04-30
EP1535613B1 (de)	2010-08-25
KR20020063190A (ko)	2002-08-01
SI1235799T1 (en)	2005-06-30
EP1535613A2 (de)	2005-06-01
CA2392096C (en)	2008-07-15
EP2206497A1 (de)	2010-07-14
ES2349364T3 (es)	2010-12-30
EP1235799B1 (de)	2005-02-09
HRP20020429B8 (hr)	2007-03-31
AU1617301A (en)	2001-05-30
ES2234699T3 (es)	2005-07-01
DE60018100D1 (en)	2005-03-17
CZ20021642A3 (cs)	2003-05-14
ATE288893T1 (de)	2005-02-15
PL355805A1 (en)	2004-05-17
JP2003514798A (ja)	2003-04-22
HUP0203257A3 (en)	2003-05-28

Publication	Publication Date	Title
CA2392096C (en)	2008-07-15	Polymorphic form of atorvastatin calcium
CA2426632C (en)	2008-08-05	Atorvastatin hemi-calcium form vii
US7144916B2 (en)	2006-12-05	Crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms
US7732623B2 (en)	2010-06-08	Polymorphic form of atorvastatin calcium
CA2505968C (en)	2008-08-05	Novel crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms
CA2475864A1 (en)	2003-08-28	Novel crystal forms of atorvastatin hemi-calcium and processes for their preparation, as well as novel processes for preparing atorvastatin hemi-calcium forms i, viii and ix
AU2002241506B2 (en)	2008-01-24	Atorvastatin hemi-calcium form VII
ZA200406579B (en)	2005-11-30	Novel crystal forms of atorvastatin hemi-calcium and processes for their preparation, as well as novel processes for preparing atorvastatin hemi-calcium forms I, VIII and IX.
AU2002241506A1 (en)	2002-08-08	Atorvastatin hemi-calcium form VII
ZA200303976B (en)	2004-11-22	Novel crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms.