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1. 发明申请

WO2014199316A1 MODIFIED RELEASE FORMULATION 审中-公开
标题翻译：修改释放公式
公开(公告)号：WO2014199316A1
公开(公告)日：2014-12-18
申请号：PCT/IB2014/062136
申请日：2014-06-11
申请人： GALLI, Bruno , THOMA, Hubert , GRANDEURY, Arnaud , SPICKERMANN, Dirk , PUTZBACH, Karsten , MOLL, Klaus-Peter , UFER, Mike , GLANTZMANN, Jean-Marie , MUELLER-ZSIGMONDY, Martin , NOVARTIS AG
发明人： GALLI, Bruno , THOMA, Hubert , GRANDEURY, Arnaud , SPICKERMANN, Dirk , PUTZBACH, Karsten , MOLL, Klaus-Peter , UFER, Mike , GLANTZMANN, Jean-Marie , MUELLER-ZSIGMONDY, Martin
IPC分类号： A61K9/20 , A61K31/4439
CPC分类号： A61K31/404 , A61J3/02 , A61J3/10 , A61K9/1652 , A61K9/1682 , A61K9/2004 , A61K9/2072 , A61K9/28 , A61K9/50 , A61K9/5089 , A61K31/4045 , A61K47/38
摘要： Drug products in the form of modified release formulations comprising the drug substance (-)-(3aR,4S,7aR)-4-Hydroxy-4m-tolylethynyl-octahydro-indole-1-carboxylic acid methyl ester (AFQ056), as well as processes for making such drug products are 5 provided. The drug products are useful in treating patients with Parkinson's disease and exhibiting L-dopa induced dyskinesia.
摘要翻译：包含药物（ - ） - （3aR，4S，7aR）-4-羟基-4m-甲苯乙炔基 - 八氢 - 吲哚-1-甲酸甲酯（AFQ056）的改性释放制剂形式的药物产品，以及提供制备这些药物的方法是5。该药物可用于治疗帕金森病患者，并表现出左旋多巴引起的运动障碍。

2. 发明申请

WO2014161606A9 IDENTIFYING PATIENT RESPONSE TO S1P RECEPTOR MODULATOR ADMINISTRATION 审中-公开
公开(公告)号：WO2014161606A9
公开(公告)日：2014-10-09
申请号：PCT/EP2013/058226
申请日：2013-04-19
申请人： NOVARTIS AG , BORELL, Hubert , GARDIN, Anne , JIN, Yi , LEGANGNEUX, Eric , UFER, Mike
发明人： BORELL, Hubert , GARDIN, Anne , JIN, Yi , LEGANGNEUX, Eric , UFER, Mike
IPC分类号： G01N33/50 , C12Q1/68 , G01N33/569
摘要： The invention provides a method of assessing the appropriate therapeutic dose of 1-{4- [1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3- carboxylic acid to administer to a patient in need thereof, comprising the steps of: (i) testing whether or not the patient has the poor metabolizer genotype; and (ii) if the patient does not have the poor metaboliser genotype, administering -{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl- benzyl}-azetidine-3-carboxylic acid, or a pharmaceutically acceptable salt thereof, to the patient at the standard therapeutic dose; and (iii) if the patient does have the poor metaboliser genotype, either (a) administering 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)- ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid, or a pharmaceutically acceptable salt thereof, to the patient at a therapeutic dose below that of the standard therapeutic dose; or (b) not administering 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl- benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid, or a pharmaceutically acceptable salt thereof, to the patient.

3. 发明申请

WO2014161606A1 IDENTIFYING PATIENT RESPONSE TO S1P RECEPTOR MODULATOR ADMINISTRATION 审中-公开
标题翻译：鉴定患者对S1P受体调节剂的作用
公开(公告)号：WO2014161606A1
公开(公告)日：2014-10-09
申请号：PCT/EP2013/058226
申请日：2013-04-19
申请人： NOVARTIS AG , BORELL, Hubert , GARDIN, Anne , JIN, Yi , LEGANGNEUX, Eric , UFER, Mike
发明人： BORELL, Hubert , GARDIN, Anne , JIN, Yi , LEGANGNEUX, Eric , UFER, Mike
IPC分类号： G01N33/50 , C12Q1/68 , G01N33/569
CPC分类号： C07D205/04 , C12Q1/6883 , C12Q2600/106 , C12Q2600/156 , G01N33/5094 , G01N33/56972 , G01N2800/52
摘要： The invention provides a method of assessing the appropriate therapeutic dose of 1-{4- [1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3- carboxylic acid to administer to a patient in need thereof, comprising the steps of: (i) testing whether or not the patient has the poor metabolizer genotype; and (ii) if the patient does not have the poor metaboliser genotype, administering -{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl- benzyl}-azetidine-3-carboxylic acid, or a pharmaceutically acceptable salt thereof, to the patient at the standard therapeutic dose; and (iii) if the patient does have the poor metaboliser genotype, either (a) administering 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)- ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid, or a pharmaceutically acceptable salt thereof, to the patient at a therapeutic dose below that of the standard therapeutic dose; or (b) not administering 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl- benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid, or a pharmaceutically acceptable salt thereof, to the patient.
摘要翻译：本发明提供了评估1- {4- [1-（4-环己基-3-三氟甲基 - 苄氧基亚氨基） - 乙基] -2-乙基 - 苄基} - 氮杂环丁烷-3-羧酸的合适治疗剂量的方法，包括以下步骤：（i）测试患者是否具有不良代谢基因型; 给予 - {4- [1-（4-环己基-3-三氟甲基 - 苄氧基亚氨基） - 乙基] -2-乙基 - 苄基} - 氮杂环丁烷-3-羧酸，并且（ii）如果患者不具有差的代谢基因型，酸或其药学上可接受的盐以标准治疗剂量给予患者; （iii）如果患者确实具有差的代谢基因型，则（a）给予1- {4- [1-（4-环己基-3-三氟甲基 - 苄氧亚氨基） - 乙基] -2-乙基 - 苄基} - 氮杂环丁烷 -3-羧酸或其药学上可接受的盐以低于标准治疗剂量的治疗剂量给予患者; 或（b）不给予1- {4- [1-（4-环己基-3-三氟甲基 - 苄氧基亚氨基） - 乙基] -2-乙基 - 苄基} - 氮杂环丁烷-3-羧酸或其药学上可接受的盐，给病人

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