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1. 发明申请

WO2013030803A1 CHOLINE SALT OF AN ANTI - INFLAMMATORY SUBSTITUTED CYCLOBUTENEDIONE COMPOUND 审中-公开
标题翻译：抗炎剂的溶液 - 炎症取代的环糊精化合物
公开(公告)号：WO2013030803A1
公开(公告)日：2013-03-07
申请号：PCT/IB2012/054502
申请日：2012-08-31
申请人： NOVARTIS AG , AMBARKHANE, Ameet Vijay , MAULER, Arnaud , TIMPE, Carsten , BAETTIG, Urs
发明人： AMBARKHANE, Ameet Vijay , MAULER, Arnaud , TIMPE, Carsten , BAETTIG, Urs
IPC分类号： C07C215/40 , C07C311/48 , A61K31/18 , A61P29/00
CPC分类号： C07C317/36 , A61K31/18 , C07C215/40 , C07C311/48 , C07C2601/04
摘要： 6-chloro-3-[2-(1-ethyl-propylamino)-3,4-dioxo-cyclobut-1-enylamino]-2-hydroxy-N- methoxy-N-methyl-benzenesulfonamide choline, solid pharmaceutical compositions and oral dosage forms that contain said compound, and a method of using such compositions and oral dosage forms to treat people who have inflammatory, obstructive or allergic conditions and diseases.
摘要翻译： 6-氯-3- [2-（1-乙基 - 丙基氨基）-3,4-二氧代环丁-1-烯基氨基] -2-羟基-N-甲氧基-N-甲基 - 苯磺酰胺胆碱，固体药物组合物和口服含有所述化合物的剂型，以及使用这些组合物和口服剂型的方法来治疗患有炎性，阻塞性或过敏性疾病的人。

2. 发明申请

WO2008077591A3 PHARMACEUTICAL FORMULATION COMPRISING NEUROKININ ANTAGONIST 审中-公开
公开(公告)号：WO2008077591A3
公开(公告)日：2008-07-03
申请号：PCT/EP2007/011293
申请日：2007-12-20
申请人： NOVARTIS AG , DIEDERICH, Anke , TIMPE, Carsten , RIES, Angelika , OTTINGER, Isabel , MUELLER, Irene , HERBIG, Michael , SCHUETZ, Helmut , LAKSHMAN, Jay Parthiban , KALB, Oskar
发明人： DIEDERICH, Anke , TIMPE, Carsten , RIES, Angelika , OTTINGER, Isabel , MUELLER, Irene , HERBIG, Michael , SCHUETZ, Helmut , LAKSHMAN, Jay Parthiban , KALB, Oskar
IPC分类号： A61K9/14 , A61K9/16 , A61K31/55 , A61K31/4468
摘要： Solid dispersion comprising (4R)-4-[N'-methyl-N'-(3,5-bistrifluoromethyl-benzoyl)-amino]-4-(3,4-dichlorobenzyl)-but-2-enoic acid N-[(R)-epsilon-caprolactam-3-yl]-amide or a pharmaceutically acceptable salt or solvate thereof and a carrier. Pharmaceutical compositions comprising such solid dispersion are useful to treat patients who have functional motility disorders of the viscera, especially irritable bowel syndrome or functional dyspepsia, or urinary bladder disorders, especially urinary incontinence.

3. 发明申请

WO2008077591A2 SOLID DISPERSION OF A NEUROKININ ANTAGONIST 审中-公开
标题翻译：神经营养因子拮抗剂的固体分散体
公开(公告)号：WO2008077591A2
公开(公告)日：2008-07-03
申请号：PCT/EP2007011293
申请日：2007-12-20
申请人： NOVARTIS AG , DIEDERICH ANKE , TIMPE CARSTEN , RIES ANGELIKA , OTTINGER ISABEL , MUELLER IRENE , HERBIG MICHAEL , SCHUETZ HELMUT , LAKSHMAN JAY PARTHIBAN , KALB OSKAR
发明人： DIEDERICH ANKE , TIMPE CARSTEN , RIES ANGELIKA , OTTINGER ISABEL , MUELLER IRENE , HERBIG MICHAEL , SCHUETZ HELMUT , LAKSHMAN JAY PARTHIBAN , KALB OSKAR
IPC分类号： A61K9/14 , A61K9/16 , A61K31/165 , A61K31/55
CPC分类号： A61K31/4468 , A61K9/10 , A61K9/1611 , A61K9/1617 , A61K9/1623 , A61K9/1635 , A61K9/1641 , A61K9/1652 , A61K9/2009 , A61K9/2018 , A61K9/205 , A61K9/2059 , A61K9/4866 , A61K31/55
摘要： Solid dispersion comprising (4R)-4-[N'-methyl-N'-(3,5-bistrifluoromethyl-benzoyl)-amino]-4- (3,4-dichlorobenzyl)-but-2-enoic acid N-[(R)-epsilon-caprolactam-3-yl]-amide or a pharmaceutically acceptable salt or solvate thereof and a carrier. Pharmaceutical compositions comprising such solid dispersion are useful to treat patients who have functional motility disorders of the viscera, especially irritable bowel syndrome or functional dyspepsia, or urinary bladder disorders, especially urinary incontinence.
摘要翻译：包含（4R）-4- [N'-甲基-N' - （3,5-双三氟甲基 - 苯甲酰基） - 氨基] -4-（3,4-二氯苄基） - 丁-2-烯酸N- [ （R） - 己内酰胺-3-基] - 酰胺或其药学上可接受的盐或溶剂化物和载体。包含这种固体分散体的药物组合物可用于治疗具有内脏功能性运动障碍，特别是肠易激综合征或功能性消化不良或尿膀胱障碍，特别是尿失禁的患者。

4. 发明申请

WO2005042515A1 NOVEL CRYSTALLINE FORMS OF {2-[1-(3,5-BIS-TRIFLUOROMETHYLBENZYL)-5-PYRIDIN-4-YL-1H-[1,2,3]TRIAZOL-4-YL]-PYRIDIN-3-YL}-(2-CHLOROPHENYL)-METHANONE 审中-公开
标题翻译： {2- [1-（3,5-双 - 三氟甲基苄基）-5-吡啶-4-基] - [1,2,3]三唑-4-基] - 吡啶-3-YL的新型结晶形式 - （2-氯苯基） - 甲酮
公开(公告)号：WO2005042515A1
公开(公告)日：2005-05-12
申请号：PCT/US2004/030914
申请日：2004-10-12
申请人： ELI LILLY AND COMPANY , TIMPE, Carsten , BORGHESE, Alfio , COFFEY, David, Scott , FOOTMAN, Pamela, Kaye , PEDERSEN, Steven, Wayne , REUTZEL-EDENS, Susan, Marie , TAMEZE, Shella, Lenyonga , WEBER, Carsten
发明人： TIMPE, Carsten , BORGHESE, Alfio , COFFEY, David, Scott , FOOTMAN, Pamela, Kaye , PEDERSEN, Steven, Wayne , REUTZEL-EDENS, Susan, Marie , TAMEZE, Shella, Lenyonga , WEBER, Carsten
IPC分类号： C07D401/04
CPC分类号： C07D401/14 , C07D213/50
摘要： The present invention provides novel crystalline forms of {2-[1-(3,5-bistrifluoromethylbenzyl)-5-pyridin-4-yl-1H-[1,2,3]triazol-4-yl]- pyridin-3-yl}-(2-chlorophenyl)-methanone, compositions thereof, intermediates thereof, methods of using the same, processes for making the same, and processes for making intermediates thereof. X-16289
摘要翻译：本发明提供{2- [1-（3,5-双三氟甲基苄基）-5-吡啶-4-基-1H- [1,2,3]三唑-4-基] - 吡啶-3-基] （2-氯苯基） - 甲酮，其组合物，其中间体，其使用方法，制备方法及其制备中间体的方法。 X-16289

5. 发明申请

WO1998026762A1 HOMOGENEOUS PREFORMULATIONS CONTAINING WIGH CONCENTRATIONS OF STEROIDS, FOR PRODUCING LOW-DOSE SOLID AND SEMI-SOLID PHARMACEUTICAL PREPARATIONS 审中-公开
标题翻译：同质化，类固醇含高浓度预制剂用于制造低剂量固体和半固体药物制剂
公开(公告)号：WO1998026762A1
公开(公告)日：1998-06-25
申请号：PCT/DE1997002915
申请日：1997-12-15
申请人： JENAPHARM GMBH & CO. KG , GRAWE, Detlef , HÖSEL, Peter , MÖLLMANN, Peter , TIMPE, Carsten , DITTGEN, Michael , MATTHEY, Klaus
发明人： JENAPHARM GMBH & CO. KG
IPC分类号： A61K09/14
CPC分类号： A61K31/569 , A61K9/1623 , A61K9/1676 , A61K31/567 , A61K31/575
摘要： The invention relates to homogeneous preformulations containing high concentrations of steroids, which are suitable for producing low-dose solid and semi-solid pharmaceutical preparations with a steroid concentration of between 0.001 and 1 weight percent. Said preformulations are obtained by evaporating the dispersing agent containing the steroidal active ingredient from a suspension containing the usual pharmaceutical additives. To this end, a spray mist is produced in which the average drop diameter is greater than the average diameter of the additive particles, and the maximum grain size of the dried particles of the steroidal preformulation is increased by less than 30 % in relation to the grain size of the additive. Said preformulations are characterised by their homogenity and resistance to demixing, whereby the steroidal active ingredient is finely dispersed and integrally bonded to the additive. Surprinsingly it was discovered that these types of steroidal preformulations, in comparison with conventional methods, can be processed without difficulty into low-dose pharmaceutical preparations with very good homogeneity and active ingredient stability. The method for producing homogeneous steroid preformulations for low-dose solid and semi-solid pharmaceutical preparations with a steroid concentration of between 0.001 and 1 weight percent stands out among other things by the fact that the active ingredient and additive particles from the atomized suspension are not dried one next to the other. The choice of processing conditions during atomization makes it possible for practically all the active ingredient to be bonded integrally to the additive.
摘要翻译：在高浓度的预制剂均匀的，含有类固醇的适于与按重量计为0.001的浓度含量到百分之1类固醇产生的低剂量固体和半固体的药物制剂。它们是通过从一个交错的甾体包含活性物质的分散剂与药学上常用的赋形剂悬浮液的蒸发而获得，它产生的喷雾，其平均的液滴直径比赋形剂颗粒和含类固醇的预制剂的干燥颗粒的最大粒径的平均直径增加小于大与的赋形剂增加粒度比较30％。从，甾体活性成分存在于与辅助材料连接精细分散形式的含类固醇的预制剂的特征在于它们的均匀性和稳定性对分离。已经令人惊讶地发现，这样的甾体预制剂可以很容易地加工成低剂量药物制剂具有非常好的，稳定的活性成分的均匀性与常规方法相比。用于产生均匀的预制剂甾体与按重量计为0.001的浓度含量到百分之1类固醇的低剂量固体和半固体的药物制剂的方法，是可分辨尤其其特征在于，将药物和赋形剂颗粒不会从悬浮液喷洒彼此相邻干燥。通过将活性成分的喷雾过程中选择的工艺条件可以完全和物质被虚拟地结合到赋形剂。

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