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1. 发明申请

WO2008106151A2 CO-CRYSTALS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME 审中-公开
标题翻译：共晶体和包含其的药物组合物
公开(公告)号：WO2008106151A2
公开(公告)日：2008-09-04
申请号：PCT/US2008/002568
申请日：2008-02-27
申请人： VERTEX PHARMACEUTICALS INCORPORATED , CONNELLY, Patrick, R. , KADIYALA, Irina , STAVROPOLUS, Kathy , ZHANG, Yuegang , JOHNSTON, Steve , BHISETTI, Govinda, Rao , JURKAUSKAS, Valdas , ROSE, Peter
发明人： CONNELLY, Patrick, R. , KADIYALA, Irina , STAVROPOLUS, Kathy , ZHANG, Yuegang , JOHNSTON, Steve , BHISETTI, Govinda, Rao , JURKAUSKAS, Valdas , ROSE, Peter
CPC分类号： C07K5/0812 , C07D403/12
摘要： The invention relates to compositions and co-crystals each comprising VX-950 and a co-crystal former selected from the group consisting of 4-hydroxybenzoic acid, 4-amino salicylic acid, phenylalanine, threonline, tartaric acid, adipic acid, succinic acetate, proline, methyl 4-hydroxybenzoate, anthranilic acid, and d-Biotin. Also within the scope of this invention are methods of making and using the same.
摘要翻译：本发明涉及各自包含VX-950和选自4-羟基苯甲酸，4-氨基水杨酸，苯丙氨酸，苏氨酸，酒石酸的共晶体形成物的组合物和共晶体酸，己二酸，琥珀酸乙酸酯，脯氨酸，4-羟基苯甲酸甲酯，邻氨基苯甲酸和d-生物素。也在本发明的范围内的是制造和使用它们的方法。

2. 发明申请

WO2003060473A2 MUCIN IMMOBILIZED CHROMATOGRAPHY 审中-公开
标题翻译： MUCIN固定化色谱
公开(公告)号：WO2003060473A2
公开(公告)日：2003-07-24
申请号：PCT/US2003/001405
申请日：2003-01-14
申请人： VERTEX PHARMACEUTICALS INCORPORATED , KADIYALA, Irina , PANICUCCI, Riccardo
发明人： KADIYALA, Irina , PANICUCCI, Riccardo
IPC分类号： G01N
CPC分类号： G01N33/538 , C07K14/4727 , C07K17/00 , G01N2333/4725
摘要： An in vitro high-throughput screening method that models the absorption of drugs across the epithelial mucosa is provided. The invention discloses an in vitro mucin immobilized chromatography model to estimate drug permeability coefficients. The invention describes compositions for mucin immobilized chromatography media and methods to prepare this media. The invention also discloses a method to estimate in vitro drug permeability coefficients using mucin immobilized chromatography media. The invention also discloses methods to determine absorption processes in the digestive system and discloses methods of use for mucin chromatography media in column, batch, assay, diagnostic, or high-throughput screening analyses.
摘要翻译：提供了一种模拟通过上皮粘膜吸收药物的体外高通量筛选方法。本发明公开了一种用于估计药物渗透系数的体外粘蛋白固定化色谱模型。本发明描述了用于粘蛋白固定的色谱介质的组合物和制备该介质的方法。本发明还公开了使用粘蛋白固定化色谱介质估计体外药物渗透系数的方法。本发明还公开了确定消化系统中吸收过程的方法，并公开了在柱，批，测定，诊断或高通量筛选分析中使用粘蛋白色谱介质的方法。

3. 发明申请

WO2009076200A2 SOLID FORMS OF 1-ETHYL-3-(5-(5-FLUOROPYRIDIN-3-YL)-7-(PYRIMIDIN-2-YL)-1H-BENZO[D]IMIDAZOL-2-YL)UREA 审中-公开
标题翻译： 1-乙基-3-（5-（5-氟吡啶-3-基）-7-（嘧啶-2-基）-1H-苯并[d]咪唑-2-基）脲的固体形式
公开(公告)号：WO2009076200A2
公开(公告)日：2009-06-18
申请号：PCT/US2008/085673
申请日：2008-12-05
申请人： VERTEX PHARMACEUTICALS INCORPORATED , MACIKENAS, Dainius , ALARGOVA, Rossitza , KADIYALA, Irina , LE TIRAN, Arnaud , ZHANG, Yuegang
发明人： ALARGOVA, Rossitza , KADIYALA, Irina , LE TIRAN, Arnaud , ZHANG, Yuegang
IPC分类号： C07D403/14
CPC分类号： C07D401/14
摘要： Solid forms of crystalline1-ethyl-3-(5-(5-fluoropyridin-3-yl)-7-(pyrimidin-2-yl)- 1H-benzo[d]imidazol-2-yl)urea, compositions containing solid forms of crystalline 1- ethyl-3-(5-(5-fluoropyridin-3-yl)-7-(pyrimidin-2-yl)-1H-benzo[d]imidazol-2-yl)urea and methods of using the same are described.
摘要翻译：结晶1-乙基-3-（5-（5-氟吡啶-3-基）-7-（嘧啶-2-基）-1H-苯并[d]咪唑-2-基）（5-（5-氟吡啶-3-基）-7-（嘧啶-2-基）-1H-苯并[d]咪唑-2-基）固体形式的组合物）尿素及其使用方法进行了描述。

4. 发明申请

WO2007103468A2 COMPOSITIONS AND METHODS FOR TREATING RHEUMATOID ARTHRITIS 审中-公开
标题翻译：用于治疗炎症性脑膜炎的组合物和方法
公开(公告)号：WO2007103468A2
公开(公告)日：2007-09-13
申请号：PCT/US2007/005882
申请日：2007-03-07
申请人： VERTEX PHARMACEUTICALS INCORPORATED , MOHANLAL, Ramon , KAUFFMAN, Robert , ALAM, John , GODFREY, Christopher , KADIYALA, Irina
发明人： MOHANLAL, Ramon , KAUFFMAN, Robert , ALAM, John , GODFREY, Christopher , KADIYALA, Irina
CPC分类号： A61K31/519 , A61K31/44 , A61K31/455 , A61K39/395 , Y02A50/412 , A61K2300/00
摘要： The present invention relates to methods and compositions for treating RA in subjects in need thereof. The invention also relates to kits and pharmaceutical packs comprising compositions and dosage forms.
摘要翻译：本发明涉及在有需要的受试者中治疗RA的方法和组合物。本发明还涉及包含组合物和剂型的试剂盒和药物包装。

5. 发明授权

EP2114924B1 CO-CRYSTALS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME 无效
标题翻译：共晶体和药物组成，以
公开(公告)号：EP2114924B1
公开(公告)日：2012-01-25
申请号：EP08726147.5
申请日：2008-02-27
申请人： Vertex Pharmaceuticals Incorporated
发明人： CONNELLY, Patrick, R. , KADIYALA, Irina , STAVROPOLUS, Kathy , ZHANG, Yuegang , JOHNSTON, Steve , BHISETTI, Govinda, Rao , JURKAUSKAS, Valdas , ROSE, Peter
IPC分类号： C07D403/12 , C07K5/10 , A61K31/497 , A61K38/07
CPC分类号： C07K5/0812 , C07D403/12

6. 发明公开

EP1585960A2 MUCIN IMMOBILIZED CHROMATOGRAPHY 审中-公开
标题翻译：粘蛋白固定色谱
公开(公告)号：EP1585960A2
公开(公告)日：2005-10-19
申请号：EP03702151.6
申请日：2003-01-14
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： KADIYALA, Irina , PANICUCCI, Riccardo
IPC分类号： G01N1/00
CPC分类号： G01N33/538 , C07K14/4727 , C07K17/00 , G01N2333/4725
摘要： An in vitro high-throughput screening method that models the absorption of drugs across the epithelial mucosa is provided. The invention discloses an in vitro mucin immobilized chromatography model to estimate drug permeability coefficients. The invention describes compositions for mucin immobilized chromatography media and methods to prepare this media. The invention also discloses a method to estimate in vitro drug permeability coefficients using mucin immobilized chromatography media. The invention also discloses methods to determine absorption processes in the digestive system and discloses methods of use for mucin chromatography media in column, batch, assay, diagnostic, or high-throughput screening analyses.
摘要翻译：提供了模拟跨上皮粘膜的药物吸收的体外高通量筛选方法。本发明公开了一种评估药物渗透系数的体外粘蛋白固定化层析模型。本发明描述了用于粘蛋白固定化层析介质的组合物和制备该介质的方法。本发明还公开了使用粘蛋白固定化层析介质估计体外药物渗透系数的方法。本发明还公开了测定消化系统中吸收过程的方法，并且公开了在柱，分批，测定，诊断或高通量筛选分析中用于粘蛋白层析介质的方法。

7. 发明公开

EP2229379A2 SOLID FORMS OF 1-ETHYL-3-(5-(5-FLUOROPYRIDIN-3-YL)-7-(PYRIMIDIN-2-YL)-1H-BENZO[D]IMIDAZOL-2-YL)UREA 审中-公开
标题翻译： 1-乙基-3-（5-（5-氟吡啶-3-基）-7-（嘧啶-2-基）-1H-苯并[d]咪唑-2-基）脲的固体形式
公开(公告)号：EP2229379A2
公开(公告)日：2010-09-22
申请号：EP08860816.1
申请日：2008-12-05
申请人： Vertex Pharmaceuticals Incorporated
发明人： ALARGOVA, Rossitza , KADIYALA, Irina , LE TIRAN, Arnaud , ZHANG, Yuegang
IPC分类号： C07D401/14 , A61P31/00 , A61K31/4184
CPC分类号： C07D401/14
摘要： Solid forms of crystalline1-ethyl-3-(5-(5-fluoropyridin-3-yl)-7-(pyrimidin-2-yl)- 1H-benzo[d]imidazol-2-yl)urea, compositions containing solid forms of crystalline 1- ethyl-3-(5-(5-fluoropyridin-3-yl)-7-(pyrimidin-2-yl)-1H-benzo[d]imidazol-2-yl)urea and methods of using the same are described.

8. 发明公开

EP1585960A3 MUCIN IMMOBILIZED CHROMATOGRAPHY 审中-公开
标题翻译：粘蛋白固定色谱
公开(公告)号：EP1585960A3
公开(公告)日：2005-11-02
申请号：EP03702151.6
申请日：2003-01-14
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： KADIYALA, Irina , PANICUCCI, Riccardo
IPC分类号： G01N1/00

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