JP2005517696A5 - - Google Patents
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- Publication number
- JP2005517696A5 JP2005517696A5 JP2003565980A JP2003565980A JP2005517696A5 JP 2005517696 A5 JP2005517696 A5 JP 2005517696A5 JP 2003565980 A JP2003565980 A JP 2003565980A JP 2003565980 A JP2003565980 A JP 2003565980A JP 2005517696 A5 JP2005517696 A5 JP 2005517696A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- inhibitor
- salt
- tetrahydrate
- 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.)
- Granted
Links
- 150000003839 salts Chemical class 0.000 claims description 11
- 239000011780 sodium chloride Substances 0.000 claims description 11
- 239000011575 calcium Substances 0.000 claims description 6
- 238000002844 melting Methods 0.000 claims description 5
- 239000004072 C09CA03 - Valsartan Substances 0.000 claims description 3
- 229960004699 valsartan Drugs 0.000 claims description 3
- SJSNUMAYCRRIOM-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=N[N]1 SJSNUMAYCRRIOM-QFIPXVFZSA-N 0.000 claims description 2
- -1 valsartan calcium salt Chemical class 0.000 claims description 2
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 claims 4
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 claims 4
- 239000003112 inhibitor Substances 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- 150000004685 tetrahydrates Chemical class 0.000 claims 3
- 108090000028 MMP12 Proteins 0.000 claims 2
- 102000003729 Neprilysin Human genes 0.000 claims 2
- 102100017557 CYP11B2 Human genes 0.000 claims 1
- 108010009911 Cytochrome P-450 CYP11B2 Proteins 0.000 claims 1
- 108090000854 Oxidoreductases Proteins 0.000 claims 1
- 102000004316 Oxidoreductases Human genes 0.000 claims 1
- 238000004279 X-ray Guinier Methods 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive Effects 0.000 claims 1
- 239000002170 aldosterone antagonist Substances 0.000 claims 1
- 230000001396 anti-anti-diuretic Effects 0.000 claims 1
- 239000000480 calcium channel blocker Substances 0.000 claims 1
- 159000000007 calcium salts Chemical class 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 239000002934 diuretic Substances 0.000 claims 1
- 230000001882 diuretic Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000002308 endothelin receptor antagonist Substances 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 239000002461 renin inhibitor Substances 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 description 2
- 229910052791 calcium Inorganic materials 0.000 description 1
- MMFBVFWEERQGJK-UHFFFAOYSA-N calcium;tetrahydrate Chemical compound O.O.O.O.[Ca] MMFBVFWEERQGJK-UHFFFAOYSA-N 0.000 description 1
- PCHJSUWPFVWCPO-UHFFFAOYSA-N gold Chemical compound [Au] PCHJSUWPFVWCPO-UHFFFAOYSA-N 0.000 description 1
- 239000010931 gold Substances 0.000 description 1
- 229910052737 gold Inorganic materials 0.000 description 1
- 239000012299 nitrogen atmosphere Substances 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
Description
バルサルタンカルシウム塩の四水和物の別の多形形態は、固体状形態Ａ２,Ｃａである。形態Ａ ２,Ｃａの融点は１９５±１.５℃であり、融解エンタルピーは９８±８ｋＪ／Ｍｏｌである。示された融点は、密閉試料容器でしか測定され得ない水和物融点である。金容器および塩水和物２〜４ｍｇ間の試料重量を使用する。適用加熱速度はＴｒ＝１０Ｋ／分である。詳細については、形態Ａ１,Ｃａについて記載した説明を参照。カルシウムバルサルタン塩の四水和物Ａ２,Ｃａは、水不含有Ｎ２雰囲気中、１０Ｋ／分の加熱速度で熱重量測定装置ＴＧＳ−２（パーキン‐エルマー・コーポレーション、ノアウォーク、コネティカット、米国）を用いることにより温度の関数として以下の水分喪失を明らかにしており、重量喪失を表２に示す。
Claims (4)
- 固体状形態Ａ２,Ｃａを有し、融点が１９５±１.５℃であることを特徴とする、バルサルタンのカルシウム塩の四水和物の結晶。
- ギニエカメラにより撮られたＸ線粉末パターンが、格子面間隔：ｄ［Å］：１６.２±０.３、９.９±０.２、９.４±０.２、８.０５±０.１、７.０４±０.１、６.４９±０.０５、５.８２±０.０５、４.９４±０.０５、４.１３±０.０５、３.９３±０.０５を有することを特徴とする、請求項１記載のバルサルタンのカルシウム塩の四水和物の結晶。
- 請求項１記載の塩の四水和物の結晶および医薬上許容される賦形剤または添加剤を含む医薬組成物。
- さらに、
（ｉ）ＨＭＧ−Ｃｏ−Ａレダクターゼ阻害剤またはその医薬上許容される塩、
（ｉｉ）アンギオテンシン変換酵素（ＡＣＥ）阻害剤またはその医薬上許容される塩、
（ｉｉｉ）カルシウムチャンネル遮断薬またはその医薬上許容される塩、
（ｉｖ）アルドステロンシンターゼ阻害剤またはその医薬上許容される塩、
（ｖ）アルドステロンアンタゴニストまたはその医薬上許容される塩、
（ｖｉ）二重アンギオテンシン変換酵素／中性エンドペプチダーゼ（ＡＣＥ／ＮＥＰ）阻害剤またはその医薬上許容される塩、
（ｖｉｉ）エンドセリンアンタゴニストまたはその医薬上許容される塩、
（ｖｉｉｉ）レニン阻害剤またはその医薬上許容される塩、および
（ｉｘ）利尿剤またはその医薬上許容される塩
から成る群から選択される少なくとも１種の化合物を含む、請求項３記載の医薬調製物。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35419902P | 2002-02-04 | 2002-02-04 | |
| US60/354,199 | 2002-02-04 | ||
| PCT/EP2003/001047 WO2003066606A1 (en) | 2002-02-04 | 2003-02-03 | Salts of valsartan |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009139245A Division JP5303370B2 (ja) | 2002-02-04 | 2009-06-10 | バルサルタンの塩類 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005517696A JP2005517696A (ja) | 2005-06-16 |
| JP2005517696A5 true JP2005517696A5 (ja) | 2009-07-30 |
| JP4895475B2 JP4895475B2 (ja) | 2012-03-14 |
Family
ID=27734333
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003565980A Expired - Fee Related JP4895475B2 (ja) | 2002-02-04 | 2003-02-03 | バルサルタンの塩類 |
| JP2009139245A Expired - Fee Related JP5303370B2 (ja) | 2002-02-04 | 2009-06-10 | バルサルタンの塩類 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009139245A Expired - Fee Related JP5303370B2 (ja) | 2002-02-04 | 2009-06-10 | バルサルタンの塩類 |
Country Status (18)
| Country | Link |
|---|---|
| US (3) | US6869970B2 (ja) |
| EP (1) | EP1474402A1 (ja) |
| JP (2) | JP4895475B2 (ja) |
| KR (3) | KR20110101257A (ja) |
| CN (2) | CN100548993C (ja) |
| AU (1) | AU2003214054B2 (ja) |
| BR (1) | BR0307442A (ja) |
| CA (2) | CA2474424C (ja) |
| CO (1) | CO5611107A2 (ja) |
| EC (1) | ECSP045221A (ja) |
| HK (1) | HK1139681A1 (ja) |
| MX (1) | MXPA04007525A (ja) |
| NO (1) | NO328155B1 (ja) |
| NZ (1) | NZ534560A (ja) |
| PL (1) | PL370481A1 (ja) |
| RU (1) | RU2004126862A (ja) |
| WO (1) | WO2003066606A1 (ja) |
| ZA (1) | ZA200405698B (ja) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7468390B2 (en) | 2002-01-17 | 2008-12-23 | Novartis Ag | Methods of treatment and pharmaceutical composition |
| US6869970B2 (en) | 2002-02-04 | 2005-03-22 | Novartis Ag | Crystalline salt forms of valsartan |
| SI1515717T1 (sl) * | 2002-06-13 | 2009-02-28 | Novartis Ag | Kalcijeve soli statinov, izvedenih iz indola |
| DE602004013405T2 (de) * | 2003-03-17 | 2009-05-07 | Teva Pharmaceutical Industries Ltd. | Polymorphe formen von valsartan |
| JP4783733B2 (ja) * | 2003-05-16 | 2011-09-28 | ノバルティス アーゲー | バルサルタンを含む医薬組成物 |
| WO2005046677A2 (en) * | 2003-11-14 | 2005-05-26 | Novartis Ag | At1-receptor antagonists for treating nephrotic syndrome |
| ITMI20032267A1 (it) * | 2003-11-21 | 2005-05-22 | Dinamite Dipharma S P A In Forma A Bbreviata Diph | Procdimento per la preparzione di valsartan e suoi intermedi |
| WO2005049587A1 (en) * | 2003-11-21 | 2005-06-02 | Ranbaxy Laboratories Limited | Process for preparation of biphenyl tetrazole |
| TWI328006B (en) * | 2003-12-26 | 2010-08-01 | Nissan Chemical Ind Ltd | Crystal form of quinoline compound and process for its production |
| DE502004002443D1 (de) * | 2004-04-15 | 2007-02-08 | Helm Ag | Verfahren zur Herstellung von freifliessenden, pulverförmigen Valsartan-Adsorbaten |
| AR050043A1 (es) * | 2004-08-03 | 2006-09-20 | Novartis Ag | Metodos para mejorar la biodisponibilidad y composicion farmaceutica para trastornos cardiovasculares |
| WO2006021443A2 (en) * | 2004-08-26 | 2006-03-02 | Novartis Ag | Composition comprising an at1 receptor blocker and a macrolide t-cell immunomodulator |
| EP1806137A4 (en) * | 2004-10-29 | 2011-03-30 | Kowa Co | THERAPEUTIC AGENT FOR THE TREATMENT OF GLOMERULAR DISEASE |
| US20100028439A1 (en) * | 2005-05-23 | 2010-02-04 | Elan Pharma International Limited | Nanoparticulate stabilized anti-hypertensive compositions |
| AR057882A1 (es) * | 2005-11-09 | 2007-12-26 | Novartis Ag | Compuestos de accion doble de bloqueadores del receptor de angiotensina e inhibidores de endopeptidasa neutra |
| WO2008035364A2 (en) * | 2006-06-23 | 2008-03-27 | Usv Limited | Process for the preparation of micronized valsartan |
| AR061627A1 (es) | 2006-06-27 | 2008-09-10 | Novartis Ag | Formas de dosificacion solidas de valsartan, amlodipina, e hidroclorotiazida, y metodo para elaborarlas |
| WO2008018843A1 (en) * | 2006-08-08 | 2008-02-14 | Ulkar Kimya Sanayi Ve Ticaret As | Process for producing useful salts form of biphenyl-tetrazole compounds |
| PE20080907A1 (es) * | 2006-08-31 | 2008-08-22 | Novartis Ag | Sistema de suministro de farmaco oral gastro-retentivo de liberacion extendida para valsartan |
| WO2008088727A2 (en) | 2007-01-12 | 2008-07-24 | Concert Pharmaceuticals, Inc. | Endothelin receptor antagonists |
| US8080549B2 (en) * | 2007-01-12 | 2011-12-20 | Concert Pharmaceuticals, Inc. | Endothelin receptor antagonists |
| CN101396366B (zh) * | 2007-09-25 | 2010-10-13 | 浙江华海药业股份有限公司 | 含缬沙坦的固体口服制剂及其制备方法 |
| ES2336755B1 (es) * | 2008-10-07 | 2011-01-21 | Activery Biotech, S.L. | Procedimiento para la preparacion de combinaciones de valsartan y simvastatina. |
| JP2011063518A (ja) * | 2009-09-15 | 2011-03-31 | Tohoku Univ | Ａｒｂ及び／又はグリタゾン系血糖降下物質を含有するｏａｔｐ−ｒ遺伝子発現増強組成物 |
| MX2013001251A (es) | 2010-08-03 | 2013-03-18 | Novartis Ag | Valsartan altamente cristalino. |
| CN103012301B (zh) * | 2013-01-05 | 2015-06-17 | 江苏施美康药业股份有限公司 | 缬沙坦甲酯碱金属盐及其制备方法 |
| DE102014004512A1 (de) * | 2014-03-28 | 2015-10-01 | Georg-August-Universität Göttingen Stiftung Öffentlichen Rechts Bereich Universitätsmedizin | Anorganisch-organische Hybridverbindung |
| WO2017012600A1 (en) | 2015-07-20 | 2017-01-26 | Zentiva, K.S. | A pharmaceutical composition containing valsartan and sacubitril and methods for preparation and stabilization thereof |
| WO2018002673A1 (en) | 2016-07-01 | 2018-01-04 | N4 Pharma Uk Limited | Novel formulations of angiotensin ii receptor antagonists |
| EP3498698A1 (en) | 2017-12-15 | 2019-06-19 | Mankind Pharma Ltd | Solid forms of valsartan disodium and process of preparation thereof |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE59107440D1 (de) * | 1990-02-19 | 1996-04-04 | Ciba Geigy Ag | Acylverbindungen |
| MX9707683A (es) * | 1995-04-07 | 1997-12-31 | Novartis Ag | Composiciones de combinacion que contienen benazepril o benazeprilat y valsartan. |
| ES2099031B1 (es) | 1995-05-31 | 1997-12-01 | Esteve Labor Dr | Nuevos polimorfos de diclorhidrato de lesopitron y sus formas hidratadas, procedimientos de preparacion y composiciones que los contienen. |
| US5877193A (en) * | 1996-07-19 | 1999-03-02 | Hoffmann-La Roche Inc. | Use of N-(4-aryl-thiazol-2-yl)-sulfonamides |
| AP9901660A0 (en) * | 1997-02-28 | 1999-09-30 | Burstein Lab Inc | Laboratory in a disk. |
| US6641886B1 (en) * | 1999-03-23 | 2003-11-04 | Flexplay Technologies, Inc. | Directory read inhibitor for optical storage media |
| JP2001155346A (ja) * | 1999-11-26 | 2001-06-08 | Toshiba Corp | 情報記録媒体、情報記録装置、情報記録方法、情報再生装置、情報再生方法 |
| HUP0300701A2 (hu) | 2000-04-24 | 2003-07-28 | Teva Pharmaceutical Industries Ltd. | Zolpidem hemitartarát, eljárás az előállítására és ezt tartalmazó gyógyszerkészítmények |
| US20020132839A1 (en) * | 2000-06-22 | 2002-09-19 | Ganter Sabina Maria | Tablet formulations comprising valsartan |
| PE20020613A1 (es) | 2000-07-19 | 2002-08-07 | Novartis Ag | Sales de (s)-n-(1-carboxi-2-metil-prop-1-il)-n-pentanoil-n-[2'-(1h-tetrazol-5-il)-bifenil-4-ilmetil]-amina como antagonista del receptor at1 |
| US6869970B2 (en) | 2002-02-04 | 2005-03-22 | Novartis Ag | Crystalline salt forms of valsartan |
-
2003
- 2003-01-29 US US10/353,389 patent/US6869970B2/en not_active Expired - Lifetime
- 2003-02-03 MX MXPA04007525A patent/MXPA04007525A/es active IP Right Grant
- 2003-02-03 AU AU2003214054A patent/AU2003214054B2/en not_active Ceased
- 2003-02-03 JP JP2003565980A patent/JP4895475B2/ja not_active Expired - Fee Related
- 2003-02-03 KR KR1020117020401A patent/KR20110101257A/ko active Application Filing
- 2003-02-03 KR KR10-2004-7012006A patent/KR20040081178A/ko not_active Application Discontinuation
- 2003-02-03 NZ NZ534560A patent/NZ534560A/en not_active IP Right Cessation
- 2003-02-03 CN CNB038032600A patent/CN100548993C/zh not_active Expired - Lifetime
- 2003-02-03 PL PL03370481A patent/PL370481A1/xx not_active Application Discontinuation
- 2003-02-03 RU RU2004126862/04A patent/RU2004126862A/ru unknown
- 2003-02-03 EP EP03709700A patent/EP1474402A1/en not_active Withdrawn
- 2003-02-03 WO PCT/EP2003/001047 patent/WO2003066606A1/en active Application Filing
- 2003-02-03 CN CN200910167071XA patent/CN101633646B/zh not_active Expired - Lifetime
- 2003-02-03 BR BR0307442-0A patent/BR0307442A/pt active Search and Examination
- 2003-02-03 KR KR1020127011954A patent/KR20120054667A/ko not_active Application Discontinuation
- 2003-02-03 CA CA2474424A patent/CA2474424C/en not_active Expired - Fee Related
- 2003-02-03 CA CA2776902A patent/CA2776902A1/en not_active Abandoned
-
2004
- 2004-07-16 ZA ZA200405698A patent/ZA200405698B/en unknown
- 2004-08-04 EC EC2004005221A patent/ECSP045221A/es unknown
- 2004-09-01 NO NO20043660A patent/NO328155B1/no not_active IP Right Cessation
- 2004-09-02 CO CO04086386A patent/CO5611107A2/es not_active Application Discontinuation
- 2004-12-15 US US11/013,111 patent/US8058301B2/en active Active
-
2009
- 2009-06-10 JP JP2009139245A patent/JP5303370B2/ja not_active Expired - Fee Related
-
2010
- 2010-06-14 HK HK10105932.8A patent/HK1139681A1/xx not_active IP Right Cessation
-
2011
- 2011-09-28 US US13/247,281 patent/US8329919B2/en not_active Expired - Lifetime
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