CA2486144C - Compositions comprising an angiotensin receptor blocker, a calcium channel blocker and a diuretic - Google Patents
Compositions comprising an angiotensin receptor blocker, a calcium channel blocker and a diuretic Download PDFInfo
- Publication number
- CA2486144C CA2486144C CA2486144A CA2486144A CA2486144C CA 2486144 C CA2486144 C CA 2486144C CA 2486144 A CA2486144 A CA 2486144A CA 2486144 A CA2486144 A CA 2486144A CA 2486144 C CA2486144 C CA 2486144C
- Authority
- CA
- Canada
- Prior art keywords
- present
- amount
- amlodipine
- valsartan
- dose units
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Lifetime
Links
- 239000000203 mixture Substances 0.000 title claims description 38
- 239000002934 diuretic Substances 0.000 title description 16
- 230000001882 diuretic effect Effects 0.000 title description 16
- 229940127291 Calcium channel antagonist Drugs 0.000 title description 15
- 229940125364 angiotensin receptor blocker Drugs 0.000 title description 15
- 239000000480 calcium channel blocker Substances 0.000 title description 15
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 33
- 238000011282 treatment Methods 0.000 claims abstract description 28
- 201000010099 disease Diseases 0.000 claims abstract description 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 12
- 239000004072 C09CA03 - Valsartan Substances 0.000 claims description 61
- HTIQEAQVCYTUBX-UHFFFAOYSA-N amlodipine Chemical compound CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1Cl HTIQEAQVCYTUBX-UHFFFAOYSA-N 0.000 claims description 55
- JZUFKLXOESDKRF-UHFFFAOYSA-N Chlorothiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NCNS2(=O)=O JZUFKLXOESDKRF-UHFFFAOYSA-N 0.000 claims description 53
- 229960000528 amlodipine Drugs 0.000 claims description 53
- 229960004699 valsartan Drugs 0.000 claims description 50
- 229960002003 hydrochlorothiazide Drugs 0.000 claims description 49
- 206010020772 Hypertension Diseases 0.000 claims description 30
- 150000003839 salts Chemical class 0.000 claims description 25
- 206010012601 diabetes mellitus Diseases 0.000 claims description 19
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- 201000006370 kidney failure Diseases 0.000 claims description 12
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- SRSXLGNVWSONIS-UHFFFAOYSA-M benzenesulfonate Chemical group [O-]S(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-M 0.000 claims 6
- 238000000034 method Methods 0.000 abstract description 19
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- 150000002894 organic compounds Chemical class 0.000 abstract description 3
- ACWBQPMHZXGDFX-QFIPXVFZSA-N valsartan Chemical compound C1=CC(CN(C(=O)CCCC)[C@@H](C(C)C)C(O)=O)=CC=C1C1=CC=CC=C1C1=NN=NN1 ACWBQPMHZXGDFX-QFIPXVFZSA-N 0.000 description 38
- 241000700159 Rattus Species 0.000 description 20
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 20
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 18
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- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 8
- 239000008186 active pharmaceutical agent Substances 0.000 description 8
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- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 6
- 239000000377 silicon dioxide Substances 0.000 description 6
- 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 description 6
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- RZTAMFZIAATZDJ-HNNXBMFYSA-N 5-o-ethyl 3-o-methyl (4s)-4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate Chemical compound CCOC(=O)C1=C(C)NC(C)=C(C(=O)OC)[C@@H]1C1=CC=CC(Cl)=C1Cl RZTAMFZIAATZDJ-HNNXBMFYSA-N 0.000 description 4
- 239000002083 C09CA01 - Losartan Substances 0.000 description 4
- VPGRYOFKCNULNK-ACXQXYJUSA-N Deoxycorticosterone acetate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)COC(=O)C)[C@@]1(C)CC2 VPGRYOFKCNULNK-ACXQXYJUSA-N 0.000 description 4
- 241001465754 Metazoa Species 0.000 description 4
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 4
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- 229960003580 felodipine Drugs 0.000 description 4
- 230000000977 initiatory effect Effects 0.000 description 4
- 229960004773 losartan Drugs 0.000 description 4
- KJJZZJSZUJXYEA-UHFFFAOYSA-N losartan Chemical compound CCCCC1=NC(Cl)=C(CO)N1CC1=CC=C(C=2C(=CC=CC=2)C=2[N]N=NN=2)C=C1 KJJZZJSZUJXYEA-UHFFFAOYSA-N 0.000 description 4
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- HMJIYCCIJYRONP-UHFFFAOYSA-N (+-)-Isradipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)C)C1C1=CC=CC2=NON=C12 HMJIYCCIJYRONP-UHFFFAOYSA-N 0.000 description 3
- SVJMLYUFVDMUHP-XIFFEERXSA-N (4S)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid O5-[3-(4,4-diphenyl-1-piperidinyl)propyl] ester O3-methyl ester Chemical compound C1([C@@H]2C(=C(C)NC(C)=C2C(=O)OC)C(=O)OCCCN2CCC(CC2)(C=2C=CC=CC=2)C=2C=CC=CC=2)=CC=CC([N+]([O-])=O)=C1 SVJMLYUFVDMUHP-XIFFEERXSA-N 0.000 description 3
- PVHUJELLJLJGLN-INIZCTEOSA-N (S)-nitrendipine Chemical compound CCOC(=O)C1=C(C)NC(C)=C(C(=O)OC)[C@@H]1C1=CC=CC([N+]([O-])=O)=C1 PVHUJELLJLJGLN-INIZCTEOSA-N 0.000 description 3
- SGTNSNPWRIOYBX-UHFFFAOYSA-N 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile Chemical compound C1=C(OC)C(OC)=CC=C1CCN(C)CCCC(C#N)(C(C)C)C1=CC=C(OC)C(OC)=C1 SGTNSNPWRIOYBX-UHFFFAOYSA-N 0.000 description 3
- VWWMGPCUZVOLLK-UHFFFAOYSA-N 2-[4-[(2-cyclopropyl-7-methylimidazo[4,5-b]pyridin-3-yl)methyl]phenyl]benzoic acid Chemical compound C1CC1C1=NC=2C(C)=CC=NC=2N1CC(C=C1)=CC=C1C1=CC=CC=C1C(O)=O VWWMGPCUZVOLLK-UHFFFAOYSA-N 0.000 description 3
- NMKSAYKQLCHXDK-UHFFFAOYSA-N 3,3-diphenyl-N-(1-phenylethyl)-1-propanamine Chemical compound C=1C=CC=CC=1C(C)NCCC(C=1C=CC=CC=1)C1=CC=CC=C1 NMKSAYKQLCHXDK-UHFFFAOYSA-N 0.000 description 3
- UIAGMCDKSXEBJQ-IBGZPJMESA-N 3-o-(2-methoxyethyl) 5-o-propan-2-yl (4s)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate Chemical compound COCCOC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)C)[C@H]1C1=CC=CC([N+]([O-])=O)=C1 UIAGMCDKSXEBJQ-IBGZPJMESA-N 0.000 description 3
- 229910002016 Aerosil® 200 Inorganic materials 0.000 description 3
- 239000002080 C09CA02 - Eprosartan Substances 0.000 description 3
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- UQSXHKLRYXJYBZ-UHFFFAOYSA-N Iron oxide Chemical compound [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 description 3
- CESYKOGBSMNBPD-UHFFFAOYSA-N Methyclothiazide Chemical compound ClC1=C(S(N)(=O)=O)C=C2S(=O)(=O)N(C)C(CCl)NC2=C1 CESYKOGBSMNBPD-UHFFFAOYSA-N 0.000 description 3
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- ZBBHBTPTTSWHBA-UHFFFAOYSA-N Nicardipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OCCN(C)CC=2C=CC=CC=2)C1C1=CC=CC([N+]([O-])=O)=C1 ZBBHBTPTTSWHBA-UHFFFAOYSA-N 0.000 description 3
- FAIIFDPAEUKBEP-UHFFFAOYSA-N Nilvadipine Chemical compound COC(=O)C1=C(C#N)NC(C)=C(C(=O)OC(C)C)C1C1=CC=CC([N+]([O-])=O)=C1 FAIIFDPAEUKBEP-UHFFFAOYSA-N 0.000 description 3
- 239000005480 Olmesartan Substances 0.000 description 3
- 206010031127 Orthostatic hypotension Diseases 0.000 description 3
- IFFPICMESYHZPQ-UHFFFAOYSA-N Prenylamine Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)CCNC(C)CC1=CC=CC=C1 IFFPICMESYHZPQ-UHFFFAOYSA-N 0.000 description 3
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- LXMSZDCAJNLERA-ZHYRCANASA-N spironolactone Chemical compound C([C@@H]1[C@]2(C)CC[C@@H]3[C@@]4(C)CCC(=O)C=C4C[C@H]([C@@H]13)SC(=O)C)C[C@@]21CCC(=O)O1 LXMSZDCAJNLERA-ZHYRCANASA-N 0.000 description 3
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| US38154702P | 2002-05-17 | 2002-05-17 | |
| US60/381,547 | 2002-05-17 | ||
| PCT/EP2003/005180 WO2003097045A1 (en) | 2002-05-17 | 2003-05-16 | Combination of organic compounds |
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| CA2486144A1 CA2486144A1 (en) | 2003-11-27 |
| CA2486144C true CA2486144C (en) | 2012-02-07 |
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| EA013053B1 (ru) * | 2004-11-05 | 2010-02-26 | Бёрингер Ингельхайм Интернациональ Гмбх | Двуслойная таблетка, содержащая телмисартан и амлодипин |
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| RU2490014C2 (ru) | 2007-10-05 | 2013-08-20 | Альцгеймер'С Инститьют Оф Америка, Инк. | Способ уменьшения отложения амилоида, амилоидной нейротоксичности и микроглиоза с помощью (-)-энантиомера нилвадипина |
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- 2003-05-15 AR ARP030101691A patent/AR040014A1/es unknown
- 2003-05-15 PE PE2003000470A patent/PE20040439A1/es not_active Application Discontinuation
- 2003-05-15 TW TW092113236A patent/TWI358291B/zh not_active IP Right Cessation
- 2003-05-16 NZ NZ536557A patent/NZ536557A/en not_active IP Right Cessation
- 2003-05-16 WO PCT/EP2003/005180 patent/WO2003097045A1/en not_active Ceased
- 2003-05-16 AT AT03732397T patent/ATE429223T1/de active
- 2003-05-16 PT PT03732397T patent/PT1507529E/pt unknown
- 2003-05-16 CN CN2009102075232A patent/CN101890166A/zh active Pending
- 2003-05-16 JP JP2004505044A patent/JP5132872B2/ja not_active Expired - Lifetime
- 2003-05-16 CA CA2486144A patent/CA2486144C/en not_active Expired - Lifetime
- 2003-05-16 DK DK03732397T patent/DK1507529T3/da active
- 2003-05-16 KR KR10-2004-7018461A patent/KR20050000546A/ko not_active Ceased
- 2003-05-16 MY MYPI20031827A patent/MY138838A/en unknown
- 2003-05-16 BR BR0310092-8A patent/BR0310092A/pt not_active Application Discontinuation
- 2003-05-16 PL PL03372369A patent/PL372369A1/xx not_active Application Discontinuation
- 2003-05-16 RU RU2004137105/15A patent/RU2324482C2/ru not_active IP Right Cessation
- 2003-05-16 KR KR1020117021915A patent/KR101454070B1/ko not_active Expired - Lifetime
- 2003-05-16 EP EP03732397A patent/EP1507529B8/en not_active Revoked
- 2003-05-16 ES ES03732397T patent/ES2325207T3/es not_active Expired - Lifetime
- 2003-05-16 CN CNA038112442A patent/CN1652777A/zh active Pending
- 2003-05-16 AU AU2003240261A patent/AU2003240261B2/en not_active Expired
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- 2003-05-16 MX MXPA04011385A patent/MXPA04011385A/es active IP Right Grant
- 2003-05-16 SI SI200331623T patent/SI1507529T1/sl unknown
- 2003-05-16 US US10/514,682 patent/US20050222137A1/en not_active Abandoned
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2004
- 2004-10-28 IL IL164925A patent/IL164925A/en unknown
- 2004-10-28 ZA ZA200408737A patent/ZA200408737B/en unknown
- 2004-11-12 EC EC2004005429A patent/ECSP045429A/es unknown
- 2004-12-13 NO NO20045429A patent/NO333011B1/no not_active IP Right Cessation
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2008
- 2008-12-18 US US12/338,066 patent/US8101599B2/en not_active Expired - Fee Related
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- 2010-07-02 JP JP2010152053A patent/JP2010209123A/ja active Pending
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