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1. 发明申请

WO2012150183A8 CRYSTALLINE SODIUM SALT OF AN HIV INTEGRASE INHIBITOR 审中-公开
标题翻译： HIV整合抑制剂的晶体钠盐
公开(公告)号：WO2012150183A8
公开(公告)日：2013-06-06
申请号：PCT/EP2012057712
申请日：2012-04-27
申请人： SANDOZ AG , BLATTER FRITZ , REICHENBAECHER KATHARINA , ZIEGERT ROBERT , WIESER JOSEF , LUDESCHER JOHANNES
发明人： BLATTER FRITZ , REICHENBAECHER KATHARINA , ZIEGERT ROBERT , WIESER JOSEF , LUDESCHER JOHANNES
IPC分类号： C07D413/12 , A61K31/513 , A61P31/18
CPC分类号： C07D413/12
摘要： The present invention refers to a crystalline sodium salt of a compound of formula I (INN: Raltegravir) or a hydrate/solvate thereof as well as a process for obtaining the same.
摘要翻译：本发明涉及式I化合物（INN：Raltegravir）或其水合物/溶剂化物的结晶钠盐以及其获得方法。

2. 发明申请

WO2008104512A3 NOVEL POLYMORPHS OF APREPITANT AND PROCESSES FOR PREPARATION 审中-公开
标题翻译：制剂的新型聚合物和制备方法
公开(公告)号：WO2008104512A3
公开(公告)日：2008-12-04
申请号：PCT/EP2008052192
申请日：2008-02-22
申请人： SANDOZ AG , LUDESCHER JOHANNES , WIESER JOSEF , PICHLER ARTHUR , GRIESSER ULRICH , BRAUN DORIS
发明人： LUDESCHER JOHANNES , WIESER JOSEF , PICHLER ARTHUR , GRIESSER ULRICH , BRAUN DORIS
IPC分类号： C07D413/06 , A61K31/5377 , A61P9/08
CPC分类号： C07D413/06
摘要： Novel polymorph form III of Aprepitant and a method for preparation of novel form III is disclosed. New processes for the preparation of Aprepitant form II are disclosed. The processes involve transformation of form III to form II by heating in decalin and the precipitation of form II from a solvent or solvent mixture by cooling and/or addition of addition of seed crystals or an anti solvent. Solid dispersions containing Aprepitant form II in a suitable carrier are disclosed. A process for the preparation of the solid dispersion by evaporation of a solution of Aprepitant and the carrier in a suitable solvent is disclosed. Stable Aprepitant form II is disclosed. Further pharmaceutical compositions containing Aprepitant form II, III or solid dispersions containing Aprepitant form II in a suitable carrier are disclosed. A methanol solvate of Aprepitant is disclosed.
摘要翻译：公开了Aprepitant的新型多晶型III和新型III的制备方法。公开了制备Aprepitant II型的新方法。所述方法包括通过在十氢化萘中加热和通过冷却和/或加入晶种或抗溶剂从溶剂或溶剂混合物中沉淀形式II而转化成形式II。公开了在合适的载体中含有形式II的固体分散体。公开了通过在适当溶剂中蒸发阿维地丁和载体溶液来制备固体分散体的方法。公开了稳定的Aprepitant II型。公开了另外的药物组合物，其中含有Aprepitant形式II，III或在合适的载体中含有Aprepitant II型的固体分散体。公开了一种甲酸溶剂化物的Aprepitant。

3. 发明申请

WO2008092816A3 NOVEL POLYMORPHIC FORMS OF N-PIPERIDINO-5-(4-CHLOROPHENYL)-1(2, 4-DICHLORPHENYL)-4-METHYL-3-PYRAZOLECARBOXAMIDE 审中-公开
标题翻译： N-哌啶-5-基（4-氯苯基）-1（2,4-二氯苯基）-4-甲基-3-吡咯酰胺的新型多晶型
公开(公告)号：WO2008092816A3
公开(公告)日：2008-09-18
申请号：PCT/EP2008050924
申请日：2008-01-28
申请人： SANDOZ AG , LUDESCHER JOHANNES , GRIESSER ULRICH , WIESER JOSEF , FUCKE KATHARINA , LANGES CHRISTOPH
发明人： LUDESCHER JOHANNES , GRIESSER ULRICH , WIESER JOSEF , FUCKE KATHARINA , LANGES CHRISTOPH
IPC分类号： C07D231/14 , A61K31/415 , A61P3/00
CPC分类号： C07D231/14
摘要： The present invention relates to a novel polymorphic form of N-piperidino-5-(4-chlorophenyl)-l-(2, 4-dichlophenyl)-4-methyl-3-pyrazolecarboxamide and to novel methods for its preparation. More particularly the invention relates to the preparation of a novel anhydrous form of N-piperidino-5-(4-chlorophenyl)-l-(2,4-dichlophenyl)-4-methyl-3-pyrazolecarboxamide, hereinafter called form III, and to pharmaceutical compositions thereof.
摘要翻译：本发明涉及N-哌啶子基-5-（4-氯苯基）-1-（2,4-二氯苯基）-4-甲基-3-吡唑酰胺的新型多晶型物及其制备方法。更具体地说，本发明涉及制备新的无水形式的N-哌啶子基-5-（4-氯苯基）-1-（2,4-二氯苯基）-4-甲基-3-吡唑甲酰胺，以下称为形式III，以及至其药物组合物。

4. 发明申请

WO2005080358A3 ROSIGLITAZONE PHOSPHATE AND POLYMORPHIC FORMS 审中-公开
标题翻译： ROSIGLITAZONE磷酸盐和多晶型
公开(公告)号：WO2005080358A3
公开(公告)日：2006-12-28
申请号：PCT/EP2005001378
申请日：2005-02-11
申请人： SANDOZ AG , GREIL JULIA , LUDESCHER JOHANNES , WOLF SIEGFRIED
发明人： GREIL JULIA , LUDESCHER JOHANNES , WOLF SIEGFRIED
IPC分类号： C07D417/12 , A61K31/4439 , A61P3/10
CPC分类号： C07D417/12
摘要： The present invention relates to 5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-2,4-thiazolidinedione phosphate, a novel salt of rosiglitazone and to novel polymorphic forms thereof. The invention is also directed to processes for preparation of rosiglitazone phosphate and its polymorphs. The compounds of the invention are useful for treatment and/or prophylaxis of diabetes mellitus, conditions associated with diabetes mellitus and certain complications thereof.
摘要翻译：本发明涉及5 - [[4- [2-（甲基-2-吡啶基氨基）乙氧基]苯基]甲基] -2,4-噻唑烷二酮磷酸酯，罗格列酮的新型盐及其新颖的多晶型物。本发明还涉及制备罗格列酮磷酸酯及其多晶型物的方法。本发明的化合物可用于治疗和/或预防糖尿病，与糖尿病有关的病症及其某些并发症。

5. 发明申请

WO2007087555A3 NOVEL POLYMORPH "FORM E " OF OLANZAPINE (2-METHYL-4- (4-METHYL-1-PIPERAZINYL) -10H-THIENO [2, 3-B] [1, 5] BENZODIAZEPINE) AND PREPARATION OF THE ANHYDROUS NON-SOLVATED CRYSTALLINE POLYMORPHIC "FORM I" OF OLANZAPINE FROM THE POLYMORPHIC OLANZAPINE "FO 审中-公开
标题翻译：（2-甲基-4-（4-甲基-1-哌啶子基）-10H-噻吩并[2,3-B] [1,5]苯并嗪）的新型聚合物“形式E”）和无溶剂的非溶剂化的制备多形态OLANZAPINE“O”的结晶多晶“I”
公开(公告)号：WO2007087555A3
公开(公告)日：2007-10-25
申请号：PCT/US2007060958
申请日：2007-01-24
申请人： SANDOZ AG , RAY ANUP KUMAR , PATEL HIREN KUMAR V , LUDESCHER JOHANNES , PATEL MAHENDRA R
发明人： RAY ANUP KUMAR , PATEL HIREN KUMAR V , LUDESCHER JOHANNES , PATEL MAHENDRA R
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The invention provides an Olanzapine pseudopolymoph Form E. The invention provides methods of preparing polymorphic Olanzapine Form E employing rapid crystallization and seeding. The invention provides methods of preparing anhydrous Olanzapine Form I from the Olanzapine Form E by step-wise drying.
摘要翻译：本发明提供了一种奥氮平假多产型E。本发明提供了使用快速结晶和接种制备多晶型奥氮平片E的方法。本发明提供了通过逐步干燥从奥氮平形式E制备无水奥氮平I型的方法。

6. 发明申请

WO03011871A3 INTERMEDIATES IN CEPHALOSPORIN PRODUCTION 审中-公开
标题翻译： CEPHALOSPORIN生产中的中间体
公开(公告)号：WO03011871A3
公开(公告)日：2003-12-04
申请号：PCT/EP0208554
申请日：2002-07-31
申请人： SANDOZ AG , GREIL JULIA , LUDESCHER JOHANNES , WOLF SIEGFRIED
发明人： GREIL JULIA , LUDESCHER JOHANNES , WOLF SIEGFRIED
IPC分类号： C07D501/00
CPC分类号： C07D501/00
摘要： A salt of PACA with an amidine and its use in the production of cefprozil. [6R-[6alpha,7beta(R*)]]-7-[[amino(4-hydroxyphenyl)acetyl]amino]-8-oxo-3-(1-propenyl)-3-thia-1-azabicyclo[4.2.0]oct-2-ene-2carboxylic acid; (Formula I).
摘要翻译： PACA与脒的盐及其在头孢丙烯生产中的用途。 [6R- [6alpha，7beta（R *）]] - 7 - [[氨基（4-羟基苯基）乙酰基]氨基] -8-氧代-3-（1-丙烯基）-3-硫杂-1-氮杂双环[4.2 .0]辛-2-烯-2-羧酸; （式I）。

7. 发明申请

WO2005095390A3 NOVEL CO-PRECIPITATE OF AMORPHOUS ROSIGLITAZONE 审中-公开
标题翻译：新型无定形罗格列酮共沉淀物
公开(公告)号：WO2005095390A3
公开(公告)日：2005-11-10
申请号：PCT/EP2005003332
申请日：2005-03-30
申请人： SANDOZ AG , GREIL JULIA , WOLF SIEGFRIED , LUDESCHER JOHANNES
发明人： GREIL JULIA , WOLF SIEGFRIED , LUDESCHER JOHANNES
IPC分类号： A61K9/16 , C07D417/12 , A61P5/00
CPC分类号： A61K9/1635 , A61K9/1623 , A61K9/1694 , C07D417/12
摘要： A novel coprecipitate of amorphous rosiglitazone maleate with a pharmaceutically acceptable carrier, e.g. polyvinylpyrolidone, mannitol, lactose, methylcellulose, cyclodextrin or silicon dioxide, a process for the preparation of said novel coprecipitate and the use of said novel coprecipitate of amorphous rosiglitazone with a pharmaceutically acceptable carrier in the treatment and / or prophylaxis of diabetes mellitus, conditions associated with diabetes mellitus and certain complications thereof, are disclosed. A novel solid solution of rosiglitazone maleate with a pharmaceutically acceptable carrier, preferably with polyethyelene glycol PEG from 4000 to 40.000 of average mol. wt., a process for the preparation thereof and use are disclosed. A novel coprecipitate of amorphous rosiglitazone maleate with a pharmaceutically acceptable carrier and a novel solid solution of rosiglitazone maleate with a pharmaceutically acceptable inert carrier are stable and may be particularly suitable for bulk preparation, handling and formulation advantages.
摘要翻译：无定形罗格列酮马来酸盐与药学上可接受的载体例如马来酸盐的新型共沉淀物。聚乙烯吡咯烷酮，甘露糖醇，乳糖，甲基纤维素，环糊精或二氧化硅，制备所述新型共沉淀物的方法以及所述无定形罗格列酮与药学上可接受的载体的新型共沉淀物在治疗和/或预防糖尿病，伴有糖尿病及其某些并发症。马来酸罗格列酮与药学上可接受的载体，优选与平均摩尔数为4000至40.000的聚乙二醇PEG的新型固溶体。公开了其制备方法和用途。无定形罗格列酮马来酸盐与药学上可接受的载体以及马来酸罗格列酮与药学上可接受的惰性载体的新型固体溶液的新型共沉淀物是稳定的，并且可能特别适用于批量制备，处理和配制优点。

8. 发明申请

WO2004092183A3 PROCESSES FOR THE PREPARATIONS OF CEFEPIME 审中-公开
标题翻译： CEFEPIME的制备方法
公开(公告)号：WO2004092183A3
公开(公告)日：2004-12-09
申请号：PCT/EP2004003988
申请日：2004-04-15
申请人： SANDOZ AG , LUDESCHER JOHANNES , STURM HUBERT , WOLF SIEGFRIED
发明人： LUDESCHER JOHANNES , STURM HUBERT , WOLF SIEGFRIED
IPC分类号： C07D501/00 , C07D501/06 , C07D501/44
CPC分类号： C07D513/04
摘要： This invention provides processes for preparing cefepime, including crystalline intermediates of Formula (V).
摘要翻译：本发明提供了制备头孢吡肟的方法，包括式（Ⅴ）的结晶中间体。

9. 发明申请

WO2007017244A3 A PROCESS FOR THE PURIFICATION OF SUBSTITUTED 2-(2-PYRIDYLMETHYL)SULFINYL-lH-BENZIMIDAZOLE COMPOUNDS BY PRECIPITATION IN THE PRESENCE OF A QUATERNARY AMMONIUM SALT 审中-公开
标题翻译：在季铵盐存在下，通过降解来纯化取代的2-（2-吡啶基甲基）磺酰基-1H-苯并咪唑化合物的方法
公开(公告)号：WO2007017244A3
公开(公告)日：2007-04-26
申请号：PCT/EP2006007832
申请日：2006-08-08
申请人： SANDOZ AG , LUDESCHER JOHANNES , KHAN RASHID ABDUL REHMAN , DAS TONMOY CHITTA
发明人： LUDESCHER JOHANNES , KHAN RASHID ABDUL REHMAN , DAS TONMOY CHITTA
IPC分类号： C07D401/12 , A61K31/4439 , A61P1/04
CPC分类号： C07D401/12
摘要： A process for the preparation of substituted 2-(2-pyridylmethyl) sulfinyl-1H- benzimidazoles compounds from a suitable solvent or a mixture of solvents in the presence of a quaternary ammonium compound.
摘要翻译：一种在季铵化合物存在下由合适的溶剂或溶剂混合物制备取代的2-（2-吡啶基甲基）亚磺酰基-1H-苯并咪唑化合物的方法。

10. 发明申请

WO2005023791A3 PROCESS FOR THE PRODUCTION OF MYCOPHENOLATE MOFETIL 审中-公开
标题翻译：生产霉酚酸酯的方法MOFETIL
公开(公告)号：WO2005023791A3
公开(公告)日：2005-11-17
申请号：PCT/EP2004010134
申请日：2004-09-10
申请人： SANDOZ AG , GREIL JULIA , LUDESCHER JOHANNES , WOLF SIEGFRIED
发明人： GREIL JULIA , LUDESCHER JOHANNES , WOLF SIEGFRIED
IPC分类号： C07D307/88
CPC分类号： C07D307/88
摘要： The present invention relates to a new and economically attractive process for the production of mycophenolate mofetil in a high degree of pharmaceutically acceptable purity, which comprises the reaction of a reactive derivative of mycophenolic acid with 4-(2-hydroxyethyl)morpholine under acidic reaction conditions and the subsequent extraction of the pure mycophenolate mofetil through salt formation and release of the free base. A further aspect of the invention relates to the purification of mycophenolate mofetil by removing its by products, in particular its dimeric by-products, by means of treatment with a primary or secondary amine.
摘要翻译：本发明涉及一种以高度药学上可接受的纯度生产霉酚酸吗啉乙酯的新的且经济上有吸引力的方法，其包括霉酚酸的反应性衍生物与4-（2-羟乙基）吗啉在酸性反应条件下反应并随后通过盐形成和游离碱的释放来提取纯麦考酚酸吗乙酯。本发明的另一方面涉及通过用伯胺或仲胺处理除去其副产物，特别是其二聚副产物来纯化麦考酚酸吗啉乙酯。

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