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1. 发明申请

WO2013149981A1 PHARMACEUTICAL COMPOSITION WITH IMPROVED BIOAVAILABILITY, SAFETY AND TOLERABILITY 审中-公开
标题翻译：具有改善生物利用性，安全性和耐受性的药物组合物
公开(公告)号：WO2013149981A1
公开(公告)日：2013-10-10
申请号：PCT/EP2013/056856
申请日：2013-04-02
申请人： F. HOFFMANN-LA ROCHE AG , ANAND, Shalini , CHATTERJI, Ashish , MATCHETT SR, Michael Allen , SANDHU, Harpreet K. , SHAH, Navnit Hargovindas
发明人： ANAND, Shalini , CHATTERJI, Ashish , MATCHETT SR, Michael Allen , SANDHU, Harpreet K. , SHAH, Navnit Hargovindas
IPC分类号： A61K47/32
CPC分类号： A61K47/34 , A61K9/10 , A61K9/146 , A61K31/4709 , A61K47/32 , A61K47/40
摘要： The invention relates to solid dispersions of poorly soluble compounds formed by coprecipitation, resulting in improved bioavailability, safety and tolerability. The invention also relates to Purified Eudragit L100-55 used to prepare such solid dispersions.
摘要翻译：本发明涉及通过共沉淀形成的难溶性化合物的固体分散体，从而提高生物利用度，安全性和耐受性。本发明还涉及用于制备这种固体分散体的纯化Eudragit L100-55。

2. 发明申请

WO2008138755A3 PHARMACEUTICAL COMPOSITIONS FOR POORLY SOLUBLE DRUGS 审中-公开
公开(公告)号：WO2008138755A3
公开(公告)日：2008-11-20
申请号：PCT/EP2008/055292
申请日：2008-04-30
申请人： F. HOFFMANN-LA ROCHE AG , CHATTERJI, Ashish , DONG, Zedong , SANDHU, Harpreet K. , SHAH, Navnit Hargovindas
发明人： CHATTERJI, Ashish , DONG, Zedong , SANDHU, Harpreet K. , SHAH, Navnit Hargovindas
IPC分类号： A61K9/14
摘要： The invention relates to solid dispersions of poorly soluble compounds formed by co-precipitation and hot melt extrusion, resulting in improved stability and bioavailability. The invention also relates to hot melt extrusion processes used to prepare such solid dispersions.

3. 发明申请

WO2006094640A2 ROFLUMILAST AND INTEGRIN INHIBITOR COMBINATION AND METHOD OF TREATMENT 审中-公开
标题翻译： ROFLUMILAST和INTEGRIN缓蚀剂组合及处理方法
公开(公告)号：WO2006094640A2
公开(公告)日：2006-09-14
申请号：PCT/EP2006001639
申请日：2006-02-23
申请人： HOFFMANN LA ROCHE , SANDHU HARPREET K , VALACER DAVID J
发明人： SANDHU HARPREET K , VALACER DAVID J
CPC分类号： A61K9/2077 , A61K9/2018 , A61K9/2054 , A61K9/2081 , A61K9/209 , A61K9/2866 , A61K31/44 , A61K31/52 , A61K38/04 , A61K2300/00
摘要： The present invention provides novel solid pharmaceutical dosage forms for oral administration comprising a therapeutically active amount of roflumilast, or a pharmaceutically acceptable salt thereof, a therapeutically effective amount of N- ( chloro-6-methylbenzoyl)-4-[(2,6-dichlorobenzoyl)amino]-L-phenylalanine 2- (diethylamino)ethyl ester, or a pharmaceutically acceptable thereof, and one or more pharmaceutically acceptable excipients. These novel solid pharmaceutical dosage forms are useful in the treatment or control of asthma. The present invention also provides a method for treating asthma employing the solid pharmaceutical dosage forms and a method for preparing the pharmaceutical dosage forms.
摘要翻译：本发明提供了用于口服给药的新型固体药物剂型，其包含治疗有效量的罗氟司特或其药学上可接受的盐，治疗有效量的N-（氯-6-甲基苯甲酰基）-4 - [（2,6-二甲基苯甲酰基）（二氯苯甲酰基）氨基] -L-苯丙氨酸2-（二乙氨基）乙酯或其药学上可接受的盐和一种或多种药学上可接受的赋形剂。这些新型固体药物剂型可用于治疗或控制哮喘。本发明还提供了使用固体药物剂型治疗哮喘的方法和制备药物剂型的方法。

4. 发明申请

WO2013087546A1 PHARMACEUTICAL COMPOSITION WITH IMPROVED BIOAVAILABILITY FOR HIGH MELTING HYDROPHOBIC COMPOUND 审中-公开
标题翻译：具有改善高熔点化合物生物利用度的药物组合物
公开(公告)号：WO2013087546A1
公开(公告)日：2013-06-20
申请号：PCT/EP2012/074884
申请日：2012-12-10
申请人： F. HOFFMANN-LA ROCHE AG , ALBANO, Antonio, A. , DESAI, Dipen , DINUNZIO, James , GO, Zenaida , IYER, Raman, Mahadevan , SANDHU, Harpreet, K. , SHAH, Navnit, Hargovindas
发明人： ALBANO, Antonio, A. , DESAI, Dipen , DINUNZIO, James , GO, Zenaida , IYER, Raman, Mahadevan , SANDHU, Harpreet, K. , SHAH, Navnit, Hargovindas
IPC分类号： A61K31/437 , A61K31/4745 , A61K31/506 , A61K9/14 , A61K9/20 , A61K47/32 , A61K47/38 , A61P35/00
CPC分类号： A61K47/32 , A61K9/143 , A61K9/146 , A61K9/2027 , A61K9/2054 , A61K9/2077 , A61K9/4858 , A61K31/437 , A61K31/4745 , A61K31/506 , A61K47/38
摘要： The present invention relates to a pharmaceutical composition comprising a solid dispersion of a drug, represented by the compounds of the formulae (I) or (II) as disclosed herein. In the composition, the drug is in substantially amorphous form.
摘要翻译：本发明涉及包含由本文公开的式（I）或（II）化合物表示的药物的固体分散体的药物组合物。在组合物中，药物是基本无定形的。

5. 发明申请

WO2012110469A1 A PROCESS FOR CONTROLLED CRYSTALLIZATION OF AN ACTIVE PHARMACEUTICAL INGREDIENT FROM SUPERCOOLED LIQUID STATE BY HOT MELT EXTRUSION 审中-公开
标题翻译：通过热熔融挤出从超级液体状态控制活性药物成分的结晶过程
公开(公告)号：WO2012110469A1
公开(公告)日：2012-08-23
申请号：PCT/EP2012/052439
申请日：2012-02-14
申请人： F. HOFFMANN-LA ROCHE AG , CHATTERJI, Ashish , DESAI, Dipen , MILLER, Dave Alan , SANDHU, Harpreet K. , SHAH, Navnit Hargovindas
发明人： CHATTERJI, Ashish , DESAI, Dipen , MILLER, Dave Alan , SANDHU, Harpreet K. , SHAH, Navnit Hargovindas
IPC分类号： A61K9/14
CPC分类号： A61K9/146 , A61K31/167 , A61K31/192 , A61K31/265 , A61K31/405 , B29C47/0009 , B29C47/827
摘要： A process for controlling the crystallization of certain hydrophobic active pharmaceutical ingredients (APIs) from a supercooled liquid state by hot-melt extrusion processing is described. Also provided is a pharmaceutical composition comprising a solid crystalline dispersion of a cholesterol ester transfer protein inhibitor in a hydrophilic excipient matrix. By the claimed process, the API is fed to an extrusion system in a crystalline state contemporaneously with carrier excipients where it is first converted to a non-crystalline state by the application of heat and then subsequently recrystallized in-situ by the removal of heat and application of shear. Recrystallization of the API is controlled by carrier formulation design and the hot-melt extrusion process parameters; i.e. barrel temperature profile, feed rate, etc. The resultant product is a crystalline solid dispersion of the API in the excipient matrix where the mean particle diameter of the API after processing is reduced as compared to the API in the process feed. The resultant product exhibits a more rapid rate of dissolution as compared to the crystalline API formulated by conventional means; e.g. micronization or co- micronization. The carrier system is comprised of at least one thermoplastic, hydrophilic polymer and may also contain various functional excipients, such as: antioxidants, surfactants, wetting agents, disintegrants, stabilizing agents, acidifying agents, or similar functional excipients.
摘要翻译：描述了通过热熔挤出处理从过冷液体状态控制某些疏水性活性药物成分（API）的结晶的方法。还提供了包含亲水性赋形剂基质中胆固醇酯转移蛋白抑制剂的固体结晶分散体的药物组合物。通过要求保护的方法，将API以与载体赋形剂同时的结晶状态进料至挤出系统，其中首先通过施加热量将其转化为非结晶状态，然后通过除去热而原位重结晶，剪切应用。 API的重结晶由载体配方设计和热熔挤出工艺参数控制; 即桶温度分布，进料速率等。所得产物是API在赋形剂基质中的结晶固体分散体，其中加工后的API的平均粒径与工艺进料中的API相比降低。与通过常规方法配制的结晶API相比，所得产物表现出更快的溶解速率; 例如微粉化或共微粉化。载体系统由至少一种热塑性亲水性聚合物组成，并且还可以含有各种功能赋形剂，例如：抗氧化剂，表面活性剂，润湿剂，崩解剂，稳定剂，酸化剂或类似的功能赋形剂。

6. 发明申请

WO2012019990A2 PHARMACEUTICAL COMPOSITIONS OF METABOTROPIC GLUTAMATE 5 RECEPTOR (MGLU5) ANTAGONISTS 审中-公开
标题翻译：代谢谷氨酸盐5受体（MGLU5）拮抗剂的药物组合物
公开(公告)号：WO2012019990A2
公开(公告)日：2012-02-16
申请号：PCT/EP2011/063604
申请日：2011-08-08
申请人： F. HOFFMANN-LA ROCHE AG , CHATTERJI, Ashish , HUANG, Jingjun , KOENNINGS, Stephanie , LINDENSTRUTH, Kai , SANDHU, Harpreet K. , SHAH, Navnit Hargovindas
发明人： CHATTERJI, Ashish , HUANG, Jingjun , KOENNINGS, Stephanie , LINDENSTRUTH, Kai , SANDHU, Harpreet K. , SHAH, Navnit Hargovindas
IPC分类号： A61K9/16 , A61K9/20 , A61K9/50 , A61K31/00
CPC分类号： A61K31/4439 , A61K9/2027 , A61K9/2054 , A61K9/5078
摘要： Pharmaceutical compositions of metabotropic glutamate 5 receptor (mGlu5) antagonists or a pharmacologically acceptable salt thereof are disclosed. The compositions contain the therapeutic active compound with non-ionic polymer and ionic polymer, binder and fillers in either matrix pellet, matrix tablet or coated pellets. The compositions provide a p H-independent in vitro release profile with NMT 70 % in one hour, NMT 85 % in 4 hour, and NLT 80 % in 8 hours. The compositions are useful for the treatment of CNS disorders, such as Treatment- Resistant Depression (TRD) and Fragile X Syndrome.
摘要翻译：披露代谢型谷氨酸5受体（mGlu5）拮抗剂或其药理学上可接受的盐的药物组合物。组合物在基质颗粒，基质片剂或包衣颗粒中含有治疗活性化合物与非离子聚合物和离子聚合物，粘合剂和填料。该组合物在一小时内提供具有NMT 70％，4小时内NMT 85％和8小时中NLT 80％的p H独立体外释放曲线。该组合物可用于治疗CNS疾病，例如耐药性抑郁症（TRD）和脆性X综合征。

7. 发明申请

WO2010084041A3 PHARMACEUTICAL COMPOSITIONS COMPRISING A HCV POLYMERASE INHIBITOR PRODRUG 审中-公开
标题翻译：包含HCV聚合酶抑制剂原料的药物组合物
公开(公告)号：WO2010084041A3
公开(公告)日：2011-08-18
申请号：PCT/EP2010050182
申请日：2010-01-11
申请人： HOFFMANN LA ROCHE , CHATTERJI ASHISH , DESAI DIPEN , SANDHU HARPREET K , SHAH NAVNIT HARGOVINDAS
发明人： CHATTERJI ASHISH , DESAI DIPEN , SANDHU HARPREET K , SHAH NAVNIT HARGOVINDAS
IPC分类号： A61K9/20 , A61K31/513
CPC分类号： A61K9/2054 , A61K31/513
摘要： The present invention provides novel formulations of isobutyric acid (2R,3R,4R,5R)-5-(4-amino-2-oxo-2H-pyrimidin-1-yl)-4-fluoro-2-isobutyryloxymethyl-4-methyl-tetrahydro-furan-3-yl ester) and hydroxypropylcellulose that provide high bulk density, low particle size better suited for improved compression and flow, good compression, and fast dissolution profiles.
摘要翻译：本发明提供了异丁酸（2R，3R，4R，5R）-5-（4-氨基-2-氧代-2H-嘧啶-1-基）-4-氟-2-异丁酰氧基甲基-4-甲基四氢呋喃-3-基酯）和羟丙基纤维素，其提供高堆积密度，较低的颗粒尺寸，更适合改进的压缩和流动，良好的压缩和快速的溶解曲线。

8. 发明申请

WO2010084041A2 PHARMACEUTICAL COMPOSITIONS WITH SUPERIOR PRODUCT PERFORMANCE AND PATIENT COMPLIANCE 审中-公开
标题翻译：具有高级产品性能和患者依从性的药物组合物
公开(公告)号：WO2010084041A2
公开(公告)日：2010-07-29
申请号：PCT/EP2010/050182
申请日：2010-01-11
申请人： F. HOFFMANN-LA ROCHE AG , CHATTERJI, Ashish , DESAI, Dipen , SANDHU, Harpreet K. , SHAH, Navnit Hargovindas
发明人： CHATTERJI, Ashish , DESAI, Dipen , SANDHU, Harpreet K. , SHAH, Navnit Hargovindas
IPC分类号： A61K9/20 , A61K31/513
CPC分类号： A61K9/2054 , A61K31/513
摘要： The present invention provides novel formulations of isobutyric acid (2R,3R,4R,5R)- 5-(4-amino-2-oxo-2H-pyrimidin-1-yl)-4-fluoro-2-isobutyryloxymethyl-4-methyl-tetrahydro-furan-3-yl ester) and hydroxypropylcellulose that provide high bulk density, low particle size better suited for improved compression and flow, good compression, and fast dissolution profiles.
摘要翻译：本发明提供了异丁酸（2R，3R，4R，5R）-5-（4-氨基-2-氧代-2H-嘧啶-1-基）-4-氟-2-异丁酰氧基甲基-4-甲基四氢呋喃-3-基酯）和羟丙基纤维素，其提供高堆积密度，较低的颗粒尺寸，更适合改进的压缩和流动，良好的压缩和快速的溶解曲线。

9. 发明申请

WO2008138755A2 PHARMACEUTICAL COMPOSITIONS FOR POORLY SOLUBLE DRUGS 审中-公开
标题翻译：不溶性药物的药物组合物
公开(公告)号：WO2008138755A2
公开(公告)日：2008-11-20
申请号：PCT/EP2008055292
申请日：2008-04-30
申请人： HOFFMANN LA ROCHE , CHATTERJI ASHISH , DONG ZEDONG , SANDHU HARPREET K , SHAH NAVNIT HARGOVINDAS
发明人： CHATTERJI ASHISH , DONG ZEDONG , SANDHU HARPREET K , SHAH NAVNIT HARGOVINDAS
IPC分类号： A61K9/14
CPC分类号： A61K9/146 , A61K9/1694 , A61K31/426 , A61K47/32 , A61K47/38
摘要： The invention relates to solid dispersions of poorly soluble compounds formed by co-precipitation and hot melt extrusion, resulting in improved stability and bioavailability. The invention also relates to hot melt extrusion processes used to prepare such solid dispersions.
摘要翻译：本发明涉及通过共沉淀和热熔融挤出形成的难溶性化合物的固体分散体，从而提高稳定性和生物利用度。本发明还涉及用于制备这种固体分散体的热熔融挤出方法。

10. 发明申请

WO2012019990A3 PHARMACEUTICAL COMPOSITIONS OF METABOTROPIC GLUTAMATE 5 RECEPTOR (MGLU5) ANTAGONISTS 审中-公开
标题翻译：代谢型谷氨酸5受体（MGLU5）拮抗剂的药物组合物
公开(公告)号：WO2012019990A3
公开(公告)日：2012-08-02
申请号：PCT/EP2011063604
申请日：2011-08-08
申请人： HOFFMANN LA ROCHE , CHATTERJI ASHISH , HUANG JINGJUN , KOENNINGS STEPHANIE , LINDENSTRUTH KAI , SANDHU HARPREET K , SHAH NAVNIT HARGOVINDAS
发明人： CHATTERJI ASHISH , HUANG JINGJUN , KOENNINGS STEPHANIE , LINDENSTRUTH KAI , SANDHU HARPREET K , SHAH NAVNIT HARGOVINDAS
IPC分类号： A61K9/16 , A61K9/20 , A61K9/50 , A61K31/00
CPC分类号： A61K31/4439 , A61K9/2027 , A61K9/2054 , A61K9/5078
摘要： Pharmaceutical compositions of metabotropic glutamate 5 receptor (mGlu5) antagonists or a pharmacologically acceptable salt thereof are disclosed. The compositions contain the therapeutic active compound with non-ionic polymer and ionic polymer, binder and fillers in either matrix pellet, matrix tablet or coated pellets. The compositions provide a p H-independent in vitro release profile with NMT 70 % in one hour, NMT 85 % in 4 hour, and NLT 80 % in 8 hours. The compositions are useful for the treatment of CNS disorders, such as Treatment- Resistant Depression (TRD) and Fragile X Syndrome.
摘要翻译：公开了代谢型谷氨酸5受体（mGlu5）拮抗剂或其药理学上可接受的盐的药物组合物。该组合物含有治疗活性化合物与非离子聚合物和离子聚合物，基质丸剂，基质片剂或包衣丸剂中的粘合剂和填充剂。该组合物提供不依赖于p H的体外释放曲线，其中1小时内NMT为70％，4小时内NMT为85％，8小时内为80％NLT。该组合物可用于治疗CNS障碍，例如治疗抵抗性抑郁症（TRD）和脆性X综合征。

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