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1. 发明申请

WO2011079119A1 FORMULATION COMPRISING 1 H - QUINAZOLINE - 2, 4 - DIONE AMPA RECEPTOR ANTAGONISTS, IN THE FORM OF IMMEDIATE RELEASE TABLETS AND PREPARATION THEREOF 审中-公开
标题翻译：制备包含1 H-喹唑啉-2,4-二酮AMPA受体拮抗剂，立即释放片剂及其制备方法
公开(公告)号：WO2011079119A1
公开(公告)日：2011-06-30
申请号：PCT/US2010/061553
申请日：2010-12-21
申请人： NOVARTIS AG , ZIELINSKI, Joseph Lawrence , VRETTOS, John , JI, Qin , PATEL, Subash
发明人： ZIELINSKI, Joseph Lawrence , VRETTOS, John , JI, Qin , PATEL, Subash
IPC分类号： A61K9/14 , A61K9/16 , A61K9/20 , A61K31/517 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28
CPC分类号： A61K31/517 , A61K9/2027 , A61K9/2054
摘要： The present invention provides a tablet comprising a hydroxypropylcellulose and an active ingredient selected from compounds of Formula (I) and salts thereof: wherein R 1 represents CF 3 , CHF 2 , CH 2 F, CH 3 CHF-, CH 3 CF 2 -, ethyl or iso-propyl and R 2 represents alkyl substituted by one or more substituents, the substituents being selected from the group consisting of halogen, nitro, cyano, acyl, hydroxy, oxo (=0), alkoxy, cycloalkoxy, acyloxy, alkoxycarbonyloxy, amino, alkylamino, dialkylamino, formyl, acylamino, alkoxycarbonylamino or R 2 represents heterocyclylalkyl substituted by one or more substituents, the substituents being selected from the group consisting of halogen, nitro, cyano, hydroxy, alkoxy, alkylcarbonyloxy, alkoxycarbonyloxy, amino, alkylamino, dialkylamino, alkoxycarbonylamino, or R 2 represents phenyl substituted by one or more substituents, the substituents being selected from the group consisting of cyano, hydroxy, alkanediyl, alkenediyl, alkoxy, hydroxyalkyl, formyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonyloxy, alkoxycarbonyloxy, amino, alkylamino, dialkylamino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonylamino, or R 2 represents heterocyclyl optionally substituted by one or more substituents, the substituents being selected from the group consisting of halogen, hydroxy, amino, nitro, cyano, alkyl, hydroxalkyl, alkoxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, acyl, alkoxy, acyloxy, alkoxycarbonyloxy, amino, alkylamino, dialkylamino, acylamino, alkoxycarbonylamino and whereby the heterocycle is bound to the phenyl ring by a carbon-atom. The invention also provides a process for preparing the above tablet.
摘要翻译：本发明提供包含羟丙基纤维素和选自式（I）的化合物及其盐的活性成分的片剂：其中R 1表示CF 3，CHF 2，CH 2 F，CH 3 CHF-，CH 3 CF 2 - ，乙基或异丙基，R 2表示烷基取代的取代基选自卤素，硝基，氰基，酰基，羟基，氧代（= O），烷氧基，环烷氧基，酰氧基，烷氧基羰基氧基，氨基，烷基氨基，二烷基氨基，甲酰基，酰氨基，烷氧基羰基氨基或R 2表示被一个或多个取代基取代的杂环基烷基，所述取代基选自卤素，硝基，氰基，羟基，烷氧基，烷基羰基氧基，烷氧基羰基氧基，氨基，烷基氨基，二烷基氨基，烷氧基羰基氨基或R2表示被一个或更多的取代基，取代基选自氰基，羟基，烷二基，烯二基，烷氧基，羟基烷基，甲酰基，烷基羰基，烷氧基羰基，烷基羰基氧基，烷氧基羰基氧基，氨基，烷基氨基，二烷基氨基，氨基烷基，烷基氨基烷基，二烷基氨基烷基，烷氧基羰基氨基或R 2表示任选被一个或多个取代基取代的杂环基，该取代基选自卤素，羟基，氨基，硝基氰基，烷基，羟烷基，烷氧基烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基，酰基，烷氧基，酰氧基，烷氧基羰基氧基，氨基，烷基氨基，二烷基氨基，酰氨基，烷氧基羰基氨基，由此该杂环通过碳原子与苯环结合。本发明还提供了制备上述片剂的方法。

2. 发明申请

WO2009064681A2 PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：药物组合物
公开(公告)号：WO2009064681A2
公开(公告)日：2009-05-22
申请号：PCT/US2008/082932
申请日：2008-11-10
申请人： NOVARTIS AG , HARASYMIW, Gregory , TALAMONTI, Wayne , WAGNER, Robert, Frank , ZIELINSKI, Joseph, Lawrence
发明人： HARASYMIW, Gregory , TALAMONTI, Wayne , WAGNER, Robert, Frank , ZIELINSKI, Joseph, Lawrence
IPC分类号： A61K9/00 , A61K31/41
CPC分类号： A61K31/41 , A61K9/0053 , A61K9/0095
摘要： Provided are compositions comprising aqueous solutions of valsartan suitable for oral administration, preferably in pediatric and geriatric populations. Methods for making such compositions and methods for their stabilization are provided.
摘要翻译：提供了包含适合于口服给药的缬沙坦水溶液的组合物，优选在儿科和老年人群中。提供制备这些组合物的方法及其稳定化方法。

3. 发明申请

WO2008060734A2 NANOPARTICLE COMPOSITIONS 审中-公开
标题翻译：纳米复合材料
公开(公告)号：WO2008060734A2
公开(公告)日：2008-05-22
申请号：PCT/US2007/075968
申请日：2007-08-15
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , KUMAR, Saran , SHIEH, Wen-Chung , TOMER, Seema , ZIELINSKI, Joseph Lawrence
发明人： KUMAR, Saran , SHIEH, Wen-Chung , TOMER, Seema , ZIELINSKI, Joseph Lawrence
IPC分类号： A61K9/51
CPC分类号： A61K9/5115 , A61K9/5153 , A61K31/663
摘要： A method of Nanoparticle-based therapy for a mammalian subject is disclosed. The method uses Nanoparticles and/or Nanoparticles with outer surfaces that contain an affinity moiety effective to bind specifically to a biological surface at which the therapy is aimed, and a hydrophilic polymer coating. The hydrophilic polymer coating is made up of polymer chains either covalently linked or surface adsorbed to the polymer components. After a desired Nanoparticle biodistribution is achieved, the affinity agent binds to the target surface and helps internalize the Nanoparticles
摘要翻译：公开了一种哺乳动物受试者基于纳米粒子的治疗方法。该方法使用具有外部表面的纳米颗粒和/或纳米颗粒，所述外表面含有有效结合治疗目标的生物表面的亲和部分和亲水性聚合物涂层。亲水聚合物涂层由聚合物组分共价连接或表面吸附的聚合物链组成。在实现所需的纳米粒子生物分布之后，亲和剂结合靶表面并有助于内化纳米颗粒

4. 发明申请

WO2009064681A3 LIQUID COMPOSITIONS COMPRISING VALSARTAN 审中-公开
标题翻译：包含VALSARTAN的液体组合物
公开(公告)号：WO2009064681A3
公开(公告)日：2009-10-08
申请号：PCT/US2008082932
申请日：2008-11-10
申请人： NOVARTIS AG , HARASYMIW GREGORY , TALAMONTI WAYNE , WAGNER ROBERT FRANK , ZIELINSKI JOSEPH LAWRENCE
发明人： HARASYMIW GREGORY , TALAMONTI WAYNE , WAGNER ROBERT FRANK , ZIELINSKI JOSEPH LAWRENCE
IPC分类号： A61K9/00 , A61K31/41
CPC分类号： A61K31/41 , A61K9/0053 , A61K9/0095
摘要： Provided are compositions comprising aqueous solutions of valsartan suitable for oral administration, preferably in pediatric and geriatric populations. Methods for making such compositions and methods for their stabilization are provided.
摘要翻译：提供了包含适合于口服给药的缬沙坦水溶液的组合物，优选在儿科和老年人群中。提供制备这些组合物的方法及其稳定化方法。

5. 发明申请

WO2008060734A3 NANOPARTICLE COMPOSITIONS 审中-公开
标题翻译：纳米颗粒组合物
公开(公告)号：WO2008060734A3
公开(公告)日：2008-07-10
申请号：PCT/US2007075968
申请日：2007-08-15
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , KUMAR SARAN , SHIEH WEN-CHUNG , TOMER SEEMA , ZIELINSKI JOSEPH LAWRENCE
发明人： KUMAR SARAN , SHIEH WEN-CHUNG , TOMER SEEMA , ZIELINSKI JOSEPH LAWRENCE
IPC分类号： A61K9/51 , A61K31/663
CPC分类号： A61K9/5115 , A61K9/5153 , A61K31/663
摘要： A method of Nanoparticle-based therapy for a mammalian subject is disclosed. The method uses Nanoparticles and/or Nanoparticles with outer surfaces that contain an affinity moiety effective to bind specifically to a biological surface at which the therapy is aimed, and a hydrophilic polymer coating. The hydrophilic polymer coating is made up of polymer chains either covalently linked or surface adsorbed to the polymer components. After a desired Nanoparticle biodistribution is achieved, the affinity agent binds to the target surface and helps internalize the Nanoparticles
摘要翻译：公开了一种用于哺乳动物受试者的基于纳米颗粒的疗法。该方法使用具有外表面的纳米颗粒和/或纳米颗粒以及亲水性聚合物涂层，所述外表面含有有效地特异性结合所述疗法所针对的生物学表面的亲和部分。亲水聚合物涂层由共价连接或表面吸附到聚合物组分的聚合物链构成。在获得期望的纳米颗粒生物分布后，亲和试剂结合到靶表面并帮助内化纳米颗粒

6. 发明申请

WO2004080451A1 PHARMACEUTICAL COMPOSITION COMPRISING 5-METHYL-2-2’-(CHLORO-6’-FLUOROANILINO) PHE NYLACETIC ACID 审中-公开
标题翻译：包含5-甲基-2,2' - （氯代-6'-氟亚氨基）苯基氨基酸的药物组合物
公开(公告)号：WO2004080451A1
公开(公告)日：2004-09-23
申请号：PCT/EP2004/002528
申请日：2004-03-11
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FORENZO, Patrick , KHALED, Maha, Y. , WANG, Barbara , ZIELINSKI, Joseph, Lawrence
发明人： FORENZO, Patrick , KHALED, Maha, Y. , WANG, Barbara , ZIELINSKI, Joseph, Lawrence
IPC分类号： A61K31/195
CPC分类号： A61K9/0095 , A61K31/195
摘要： Provided are compositions comprising aqueous suspensions of 5-methyl-2-(2’-chloro-6’-fluoroanilino)phenylacetic acid suitable for oral administration. Methods for making such compositions and methods for their stabilization are provided.
摘要翻译：提供了包含适合于口服给药的5-甲基-2-（2'-氯-6'-氟苯胺基）苯乙酸的水悬浮液的组合物。提供制备这些组合物的方法及其稳定化方法。

7. 发明申请

WO2009039226A1 LYOPHILIZED PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译： LYOPHILIZED药物组合物
公开(公告)号：WO2009039226A1
公开(公告)日：2009-03-26
申请号：PCT/US2008/076752
申请日：2008-09-18
申请人： NOVARTIS AG , BURANACHOKPAISAN, Thitiwan , JIANG, Wenlei , TONG, Wei-Qin , ZIELINSKI, Joseph, Lawrence , ZHU, Jiahao , ZOBEL, Hans-Peter
发明人： BURANACHOKPAISAN, Thitiwan , JIANG, Wenlei , TONG, Wei-Qin , ZIELINSKI, Joseph, Lawrence , ZHU, Jiahao , ZOBEL, Hans-Peter
IPC分类号： A61K9/19 , A61K47/02 , A61K47/12 , A61K47/18 , A61K47/26 , A61K47/36 , A61K47/40 , A61K31/4045
CPC分类号： A61K31/4045 , A61K9/0019 , A61K9/0095 , A61K9/19
摘要： Pharmaceutical compositions that include a poorly water-soluble therapeutic compound, an aqueous solvent, an chelator/antioxidant, a buffer or buffer component, and a bulking agent. The pharmaceutical compositions can be orally ingested or administered parenterally. The pharmaceutical compositions can further be lyophilized to form a pharmaceutically acceptable cake that can be administered orally, e.g., as a solid oral dosage form; or reconstituted and administered parenterally, e.g. as a single i.v. bolus or iv infusion, or administered orally, e.g. as a drink solution.
摘要翻译：包含难溶于水的治疗化合物，水性溶剂，螯合剂/抗氧化剂，缓冲剂或缓冲剂组分以及填充剂的药物组合物。药物组合物可以口服摄取或肠胃外给药。药物组合物可以进一步冻干以形成可以口服给药的药学上可接受的蛋糕，例如作为固体口服剂型; 或重组和肠胃外给药，例如作为一个i.v. 推注或静脉输注，或口服给药，例如作为饮料溶液。

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