AR036205A1 - Formas cristalinas de fluvastatina sodio, proceso para su preparacion, y composicion farmaceutica - Google Patents
Formas cristalinas de fluvastatina sodio, proceso para su preparacion, y composicion farmaceuticaInfo
- Publication number
- AR036205A1 AR036205A1 ARP020102927A ARP020102927A AR036205A1 AR 036205 A1 AR036205 A1 AR 036205A1 AR P020102927 A ARP020102927 A AR P020102927A AR P020102927 A ARP020102927 A AR P020102927A AR 036205 A1 AR036205 A1 AR 036205A1
- Authority
- AR
- Argentina
- Prior art keywords
- intensity
- methylethyl
- dihydroxy
- indole
- characteristic
- Prior art date
Links
- ZGGHKIMDNBDHJB-NRFPMOEYSA-M (3R,5S)-fluvastatin sodium Chemical compound [Na+].C12=CC=CC=C2N(C(C)C)C(\C=C\[C@@H](O)C[C@@H](O)CC([O-])=O)=C1C1=CC=C(F)C=C1 ZGGHKIMDNBDHJB-NRFPMOEYSA-M 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 238000002360 preparation method Methods 0.000 title abstract 2
- 229960000868 fluvastatin sodium Drugs 0.000 title 1
- KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical class [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 abstract 6
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 5
- 239000002253 acid Substances 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229960003765 fluvastatin Drugs 0.000 abstract 2
- 229910052708 sodium Inorganic materials 0.000 abstract 2
- 239000011734 sodium Substances 0.000 abstract 2
- -1 sodium fluvastatin hydrates Chemical class 0.000 abstract 2
- ZDZJOIIBECYKAJ-UHFFFAOYSA-N 3-(4-fluorophenyl)-1-propan-2-ylindole Chemical compound C12=CC=CC=C2N(C(C)C)C=C1C1=CC=C(F)C=C1 ZDZJOIIBECYKAJ-UHFFFAOYSA-N 0.000 abstract 1
- 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 abstract 1
- 239000007864 aqueous solution Substances 0.000 abstract 1
- 238000004108 freeze drying Methods 0.000 abstract 1
- 238000001556 precipitation Methods 0.000 abstract 1
- 239000000725 suspension Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F1/00—Compounds containing elements of Groups 1 or 11 of the Periodic Table
- C07F1/04—Sodium compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D209/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an alkyl or cycloalkyl radical attached to the ring nitrogen atom
-
- 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
Abstract
Formas cristalinas de hidratos de Fluvastatina sodio, referida como formas polimórficas C, D, E y F. Un polimorfo cristalino de sal monosódica de ácido (ñ)-7-(3-(4-fluorfenil)-1-(1-metiletil)-1H-indol-2-il)-3,5-dihidroxi-6-heptenoico, que exhibe un patrón de difracción de polvo de rayos X característico, con picos característicos expresados en valores d (L): 23,8 (vs), 11,8(w), 7,8 (vs), 7,6 (vw), 7,4 (vw), 6,4 (vw), 6,1 (vw), 5,90 (w), 5,00 (vw), 4,88 (w), 4,73 (m), 4,56 (w), 4,40 (vw), 4,12 (vw), 4,03 (vw), 3,96 (vw), 3,50 (vw), 3,36 (vw), 2,93 (vw), donde (vs) = intensidad muy fuerte; (m) = intensidad media; (w) = intensidad débil y (vw) = intensidad muy débil. Un polimorfo cristalino de sal monosódica de ácido (ñ)-7-(3-(4-fluorfenil)-1-(1-metiletil)-1H-indol-2-il)-3,5-dihidroxi-6-heptenoico, que exhibe un patrón de difracción de polvo de rayos X característico, con picos característicos expresados en valores d (L): 24,6 (vs), 12,5 (w), 8,3 (vs), 7,4 (vw), 6,2 (m), 4,97 (w), 4,85 (vw), 4,52 (vw), 4,40 (vw), 4,14 (vw), 3,96 (vw), 3,41 (vw), 3,10 (vw), donde (vs) = intensidad muy fuerte; (m) = intensidad media; (w) = intensidad débil y (vw) = intensidad muy débil. Un polimorfo cristalino de sal monosódica de ácido (ñ)-7-(3-(4-fluorofenil)-1-(1-metiletil)-1H-indol-2-il)-3,5-dihidroxi-6-heptenoico, que puede tener una pequena desviación con los picos característicos expresados en valores d (L) en el patrón de difracción de polvo de rayos X en el rango de 24,6-26,2 (vs), 12,5-13,2 (w), 8,3-8,9 (vs) y 6,2-6,7 (m), dependiendo de la humedad relativa que varía desde 35 a 50%, donde (vs) = intensidad muy fuerte; (m) = intensidad media; (w) = intensidad débil. Un polimorfo cristalino de sal monosódica de ácido (ñ)-7-(3-(4-fluorfenil)-1-(1-metiletil)-1H-indol-2-il)-3,5-dihidroxi-6-heptenoico, que exhibe un patrón de difracción de polvo de rayos X característico, con picos característicos expresados en valores d (L): 27,6 (m), 13,9 (vw), 9,2 (m), 8,5 (vw), 8,1 (vw), 7,4 (vw), 6,9 (s), 6,1 (vw), 4,98 (m), 4,77 (m), 4,63 (m), 4,15 (w), 4,03 (w), 3,97 (vw), 3,52 (vw), 3,33 (vw), 3,08 (vw), 2,99 (vw), donde (s) = intensidad fuerte; (m) = intensidad media; (w) = intensidad débil y (vw) = intensidad muy débil. Un polimorfo cristalino de sal monosódica de ácido (ñ)-7-(3-(4-fluorofenil)-1-(1-metiletil)-1H-indol-2-il)-3,5-dihidroxi-6-heptenoico, que exhibe un patrón de difracción de polvo de rayos X característico, con picos característicos expresados en valores d (L): 29,6 (w), 14,8 (vw), 9,9 (w), 8,6 (vw), 8,3 (vw), 7,4 (s), 6,6 (vw), 6,2 (vw), 5,93 (w), 5,03 (m), 4,94 (m), 4,35 (vw), 4,23 (w), 3,98 (vw), 3,54 (vw), 2,98 (vw), donde (s) = intensidad fuerte; (m) = intensidad media; (w) = intensidad débil y (vw) = intensidad muy débil. Un proceso para la preparación de Fluvastatina sodio Forma A altamente cristalina, que comprende tratar una solución acuosa de sal monosódica de ácido (ñ)-7-(3-(4-fluorfenil)-1-(1-metiletil)-1H-indol-2-il)-3,5-dihidroxi-6-heptenoico, para efectuar por lo menos la precipitación mínima del compuesto, seguido de secado por congelamiento de la suspensión o del compuesto precipitado. Composiciones farmacéuticas que comprenden estas formas cristalinas.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP01810756 | 2001-08-03 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR036205A1 true AR036205A1 (es) | 2004-08-18 |
Family
ID=8184071
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP020102927A AR036205A1 (es) | 2001-08-03 | 2002-08-01 | Formas cristalinas de fluvastatina sodio, proceso para su preparacion, y composicion farmaceutica |
Country Status (16)
Country | Link |
---|---|
US (1) | US6696479B2 (es) |
EP (1) | EP1429757B8 (es) |
JP (2) | JP4681808B2 (es) |
KR (1) | KR100975782B1 (es) |
CN (2) | CN1536999B (es) |
AR (1) | AR036205A1 (es) |
AT (1) | ATE391502T1 (es) |
AU (1) | AU2002333271B2 (es) |
CA (1) | CA2454072A1 (es) |
DE (1) | DE60226044T2 (es) |
ES (1) | ES2304140T3 (es) |
HU (1) | HUP0401141A3 (es) |
IL (2) | IL159861A0 (es) |
PL (1) | PL366905A1 (es) |
RU (1) | RU2334738C2 (es) |
WO (1) | WO2003013512A2 (es) |
Families Citing this family (24)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7087631B2 (en) * | 2002-07-18 | 2006-08-08 | Inotek Pharmaceuticals Corporation | Aryltetrazole compounds, and compositions thereof |
EP1525189A1 (en) * | 2002-07-26 | 2005-04-27 | Ciba Specialty Chemicals Holding Inc. | Crystalline polymorphic and amorphous forms of benazepril hydrochloride |
WO2004096765A2 (en) * | 2003-05-01 | 2004-11-11 | Morepen Laboratories Ltd. | A novel crystalline polymorph of fluvastatin sodium and a process for preparing it |
US7368581B2 (en) | 2003-06-18 | 2008-05-06 | Teva Pharmaceutical Industries Ltd. | Process for the preparation of fluvastatin sodium crystal from XIV |
US7368468B2 (en) | 2003-06-18 | 2008-05-06 | Teva Pharmaceutical Industries Ltd. | Fluvastatin sodium crystal forms XIV, LXXIII, LXXIX, LXXX and LXXXVII, processes for preparing them, compositions containing them and methods of using them |
CA2610633A1 (en) | 2003-06-18 | 2004-12-29 | Teva Pharmaceutical Industries Ltd | Fluvastatin sodium crystal form lxxix, processes for preparing, compositions and methods of using |
US7892354B2 (en) * | 2003-10-06 | 2011-02-22 | Solvias Ag | Process for the parallel detection of crystalline forms of molecular solids |
US7432380B2 (en) | 2003-10-16 | 2008-10-07 | Ciba Specialty Chemicals Corp. | Crystalline form of Fluvastatin sodium |
US20070179166A1 (en) * | 2003-12-24 | 2007-08-02 | Valerie Niddam-Hildesheim | Process for preparation of statins with high syn to anti ratio |
US7851624B2 (en) * | 2003-12-24 | 2010-12-14 | Teva Pharamaceutical Industries Ltd. | Triol form of rosuvastatin and synthesis of rosuvastatin |
WO2005080332A1 (en) * | 2004-01-14 | 2005-09-01 | Cadila Healthcare Limited | Novel form of fluvastatin sodium |
US20070173536A1 (en) * | 2004-02-06 | 2007-07-26 | Ciba Specialty Chemicals Holding Inc. | Crystalline forms of zolmitriptan |
US7241800B2 (en) | 2004-03-17 | 2007-07-10 | Mai De Ltd. | Anhydrous amorphous form of fluvastatin sodium |
WO2006021967A1 (en) * | 2004-08-26 | 2006-03-02 | Biocon Limited | Process for the preparation of fluvastatin sodium form a. |
WO2006030304A2 (en) * | 2004-09-17 | 2006-03-23 | Ranbaxy Laboratories Limited | Novel forms of fluvastatin sodium, processes for preparation and pharmaceutical compositions thereof |
US7795451B2 (en) * | 2005-02-11 | 2010-09-14 | Jubilant Organosys Limited | Polymorphic forms of fluvastatin sodium and process for preparing the same |
WO2006109147A1 (en) * | 2005-04-12 | 2006-10-19 | Glenmark Pharmaceuticals Limited | Substantially pure amorphous fluvastatin, processes for its preparation and pharmaceutical compositions containing same |
WO2007039784A2 (en) * | 2005-10-06 | 2007-04-12 | Wockhardt Limited | A novel crystalline polymorph of fluvastatin sodium and process for preparing it |
WO2007054951A1 (en) * | 2005-11-14 | 2007-05-18 | Hetero Drugs Limited | Process for amorphous esomeprazole |
KR20080005230A (ko) * | 2006-02-27 | 2008-01-10 | 테바 파마슈티컬 인더스트리즈 리미티드 | 플루바스타틴 나트륨 신규 형태 및 이의 제조 방법 |
US20110015247A1 (en) * | 2008-04-04 | 2011-01-20 | Shodhana Laboratories Limited | Novel crystalline form of carvedilol dihydrogen phosphate and related processes |
CN101684121B (zh) * | 2008-09-22 | 2013-04-03 | 重庆医药工业研究院有限责任公司 | 培美曲塞二酸的新晶型及其制备方法 |
JP6115288B2 (ja) * | 2012-04-27 | 2017-04-19 | 株式会社島津製作所 | 質量分析におけるピーク検出方法及びそのシステム |
TW201806928A (zh) * | 2016-07-01 | 2018-03-01 | 第一三共股份有限公司 | 胺基羧酸之酸加成鹽的結晶及其製造方法 |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
HU204253B (en) * | 1982-11-22 | 1991-12-30 | Sandoz Ag | Process for producing mevalonolactone analogues and derivatives and pharmaceutical compositions containing them |
JPS60500015A (ja) * | 1982-11-22 | 1985-01-10 | サンド・アクチエンゲゼルシヤフト | メバロラクトン同族体とその誘導体、これらの製造法およびこれらを含有する製薬学的組成物 |
US4739073A (en) * | 1983-11-04 | 1988-04-19 | Sandoz Pharmaceuticals Corp. | Intermediates in the synthesis of indole analogs of mevalonolactone and derivatives thereof |
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) |
ES2194202T3 (es) * | 1996-06-24 | 2003-11-16 | Novartis Ag | Compuestos polimorfos. |
US6858643B2 (en) * | 2000-10-31 | 2005-02-22 | Ciba Specialty Chemicals Corporation | Crystalline forms of Fluvastatin sodium |
-
2002
- 2002-07-25 AU AU2002333271A patent/AU2002333271B2/en not_active Ceased
- 2002-07-25 JP JP2003518521A patent/JP4681808B2/ja not_active Expired - Fee Related
- 2002-07-25 EP EP02794517A patent/EP1429757B8/en not_active Expired - Lifetime
- 2002-07-25 IL IL15986102A patent/IL159861A0/xx active IP Right Grant
- 2002-07-25 CN CN028151321A patent/CN1536999B/zh not_active Expired - Fee Related
- 2002-07-25 HU HU0401141A patent/HUP0401141A3/hu unknown
- 2002-07-25 DE DE60226044T patent/DE60226044T2/de not_active Expired - Lifetime
- 2002-07-25 PL PL02366905A patent/PL366905A1/xx not_active Application Discontinuation
- 2002-07-25 CA CA002454072A patent/CA2454072A1/en not_active Abandoned
- 2002-07-25 RU RU2004106528/04A patent/RU2334738C2/ru not_active IP Right Cessation
- 2002-07-25 AT AT02794517T patent/ATE391502T1/de not_active IP Right Cessation
- 2002-07-25 CN CN2011103995817A patent/CN102516150A/zh active Pending
- 2002-07-25 ES ES02794517T patent/ES2304140T3/es not_active Expired - Lifetime
- 2002-07-25 KR KR1020047001615A patent/KR100975782B1/ko not_active IP Right Cessation
- 2002-07-25 WO PCT/EP2002/008276 patent/WO2003013512A2/en active IP Right Grant
- 2002-07-30 US US10/208,687 patent/US6696479B2/en not_active Expired - Lifetime
- 2002-08-01 AR ARP020102927A patent/AR036205A1/es unknown
-
2004
- 2004-01-14 IL IL159861A patent/IL159861A/en not_active IP Right Cessation
-
2010
- 2010-07-23 JP JP2010165635A patent/JP2010265308A/ja active Pending
Also Published As
Publication number | Publication date |
---|---|
JP4681808B2 (ja) | 2011-05-11 |
WO2003013512A3 (en) | 2003-11-20 |
IL159861A0 (en) | 2004-06-20 |
DE60226044D1 (de) | 2008-05-21 |
KR20040022226A (ko) | 2004-03-11 |
US6696479B2 (en) | 2004-02-24 |
JP2010265308A (ja) | 2010-11-25 |
JP2005501838A (ja) | 2005-01-20 |
RU2004106528A (ru) | 2005-07-27 |
EP1429757B8 (en) | 2008-07-16 |
PL366905A1 (en) | 2005-02-07 |
IL159861A (en) | 2009-02-11 |
HUP0401141A2 (hu) | 2004-09-28 |
WO2003013512A2 (en) | 2003-02-20 |
EP1429757A2 (en) | 2004-06-23 |
EP1429757B1 (en) | 2008-04-09 |
DE60226044T2 (de) | 2009-05-14 |
RU2334738C2 (ru) | 2008-09-27 |
ATE391502T1 (de) | 2008-04-15 |
KR100975782B1 (ko) | 2010-08-17 |
AU2002333271B2 (en) | 2007-08-09 |
CA2454072A1 (en) | 2003-02-20 |
CN1536999A (zh) | 2004-10-13 |
HUP0401141A3 (en) | 2011-07-28 |
ES2304140T3 (es) | 2008-09-16 |
CN102516150A (zh) | 2012-06-27 |
US20030032666A1 (en) | 2003-02-13 |
CN1536999B (zh) | 2012-08-08 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR036205A1 (es) | Formas cristalinas de fluvastatina sodio, proceso para su preparacion, y composicion farmaceutica | |
JP2005501838A5 (es) | ||
MY143367A (en) | Substituted indole derivatives for pharmaceutical compositions for treating respiratory diseases | |
CO5640116A2 (es) | Produccion mejorada de sal de calcio de rosuvastatina | |
CY1119256T1 (el) | Βελτιωμενες συνθεσεις και μεθοδοι για λυοφιλοποιηση και προϊοντα λυοφιλοποιησης που παρεχονται απο αυτες | |
MY144483A (en) | 1,2,3,4-tetrasubstituted indole for the treatment of respiratory diseases | |
MX2009004426A (es) | Derivados biciclicos fusionados de 2,4-diaminopirimidina como inhibidores alk y c-met. | |
BR0108893B1 (pt) | composiÇço farmacÊutica contendo derivados de azetidina, composto derivado de azetidina, e, processo para a preparaÇço de compostos. | |
WO2004020431A3 (en) | Novel benzoimidazole derivatives useful as antiproliferative agents | |
IL190346A0 (en) | Pharmaceutical preparation having excellent photostability | |
EA200100972A1 (ru) | Новые соединения и композиции как ингибиторы протеаз | |
ATE294185T1 (de) | Neue pyrazin-derivate oder salze davon, pharmazeutische zusammensetzungen, die die derivate oder deren salze enthalten und intermediäre zur herstellung der derivate | |
ATE165830T1 (de) | Dihydro pyrazolopyrrole | |
EA200100412A1 (ru) | Замещенные 3-цианохинолины в качестве ингибиторов протеинтирозинкиназ | |
WO2004098494A3 (en) | Compounds, compositions, and methods | |
SI1155015T1 (sl) | Postopek za proizvodnjo terc.-butil (E)-(6-(2-(4-(4-fluorofenil)-6- izopropil-2-(metil(metilsulfonil)amino)pirimidin-5-il)vinil)(4R,6S)-2, 2-dimetil-(1,3)dioksan-4-il)acetata | |
BG108650A (en) | Azabicyclic-substituted fused-heteroaryl compounds for the treatment of disease | |
EA200702589A1 (ru) | 2,6-хинолинильные производные, способы их получения и их применение | |
WO2007014848A3 (en) | Stabilization of body-care and household products against degradation by uv radiation using merocyanine derivatives | |
NO20050664L (no) | 2,4 substituerte indoler og anvendelse derav som 5-HT6 modulatorer | |
HUP0203619A2 (hu) | Moxifloxacint és konyhasót tartalmazó készítmény és eljárás az előállítására | |
EA200300103A1 (ru) | НОВАЯ β КРИСТАЛЛИЧЕСКАЯ ФОРМА ТРЕТ-БУТИЛАМИНОВОЙ СОЛИ ПЕРИНДОПРИЛА, СПОСОБ ЕЕ ПОЛУЧЕНИЯ И СОДЕРЖАЩИЕ ЕЕ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ | |
ATE449776T1 (de) | Pyrroloä2,3-cüpyridinderivate | |
WO2006077024A3 (en) | 5-aminoindole derivatives | |
CA2412208A1 (en) | Use of 3-substituted oxindole derivatives as kcnq potassium channel modulators |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FB | Suspension of granting procedure |