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公开(公告)号：US07560459B2
公开(公告)日：2009-07-14
申请号：US11265670
申请日：2005-11-02
IPC分类号： A61K31/255 , C07C311/01
摘要： The present invention is directed to novel compounds of the formula (I) wherein X, R1, R2, R3, R4, R5 and R6 are as described in the specification, processes for the preparation of and pharmaceutical compositions comprising said derivatives. The compounds of the present invention are useful for the treatment of epilepsy.The invention is further directed to a process for the preparation of compounds of formula (XX), wherein X, R3, R4, R5 and R6 are as described in the specification.
摘要翻译： 本发明涉及式（I）的新化合物，其中X，R 1，R 2，R 3，R 4，R 5和R 6如说明书中所述，制备方法和包含所述衍生物的药物组合物。 本发明的化合物可用于治疗癫痫。 本发明还涉及制备式（XX）化合物的方法，其中X，R 3，R 4，R 5和R 6如说明书中所述。
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公开(公告)号：US07060725B2
公开(公告)日：2006-06-13
申请号：US10434387
申请日：2003-05-08
申请人： Ahmed Abdel-Magid , Cynthia Maryanoff , Steven Mehrman , Kirk Sorgi , Frank Villani , Cheryl Kordik , Allen B. Reitz , Bruce Maryanoff
发明人： Ahmed Abdel-Magid , Cynthia Maryanoff , Steven Mehrman , Kirk Sorgi , Frank Villani , Cheryl Kordik , Allen B. Reitz , Bruce Maryanoff
IPC分类号： C07D323/00 , A61K31/335
摘要： The present invention is directed to novel compounds of the formula (I) wherein X, R1, R2, R3, R4, R5 and R6 are as described in the specification, processes for the preparation of and pharmaceutical compositions comprising said derivatives. The compounds of the present invention are useful for the treatment of epilepsy. The invention is further directed to a process for the preparation of compounds of formula (XX), wherein X, R3, R4, R5 and R6 are as described in the specification.
摘要翻译： 本发明涉及新的式（I）化合物，其中X，R 1，R 2，R 3，R 2， > 4，R 5和R 6如说明书中所述，制备方法和包含所述衍生物的药物组合物。 本发明的化合物可用于治疗癫痫。 本发明还涉及一种制备式（ⅩⅩ）化合物的方法，其中X，R 3，R 4，R 5， >和R 6'如说明书中所述。
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公开(公告)号：US20060058373A1
公开(公告)日：2006-03-16
申请号：US11265670
申请日：2005-11-02
IPC分类号： A61K31/255 , C07C311/45 , A61K31/695
摘要： The present invention is directed to novel compounds of the formula (I) wherein X, R1, R2, R3, R4, R5 and R6 are as described in the specification, processes for the preparation of and pharmaceutical compositions comprising said derivatives. The compounds of the present invention are useful for the treatment of epilepsy. The invention is further directed to a process for the preparation of compounds of formula (XX), wherein X, R3, R4, R5 and R6 are as described in the specification.
摘要翻译： 本发明涉及新的式（I）化合物，
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公开(公告)号：US20060105966A1
公开(公告)日：2006-05-18
申请号：US11327984
申请日：2006-01-09
IPC分类号： A61K31/7024 , C07H15/04
CPC分类号： C07H11/00
摘要： The invention relates to novel pharmaceutically acceptable salts of anticonvulsant derivatives, processes for preparation of and pharmaceutical compositions containing said salts, useful in the treatment of epilepsy.
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公开(公告)号：US07041650B2
公开(公告)日：2006-05-09
申请号：US10336435
申请日：2003-01-03
摘要： The invention relates to novel pharmaceutically acceptable salts of anticonvulsant derivatives, processes for preparation of and pharmaceutical compositions containing said salts, useful in the treatment of epilepsy.
摘要翻译： 本发明涉及抗惊厥药衍生物的新药学上可接受的盐，制备方法和含有所述盐的药物组合物，其可用于治疗癫痫。
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公开(公告)号：US20060004208A1
公开(公告)日：2006-01-05
申请号：US11215329
申请日：2005-08-30
IPC分类号： C07D231/12
CPC分类号： C07D231/12 , C07C51/083 , C07C59/88
摘要： A process for making a compound of formula I wherein the substituents are as described in the specification comprising reacting a ketone of formula II with succinic anhydride and an alkoxide base to form a compound of formula III which is reacted with a compound of formula IV to form a compound of V and reacting with an alcohol to form the corresponding ester of formula VI and reacting the ester with N-methylhydroxylamine.
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公开(公告)号：US07098188B2
公开(公告)日：2006-08-29
申请号：US10188924
申请日：2002-07-03
CPC分类号： C07H11/00
摘要： The invention relates to novel pharmaceutically acceptable salts of anticonvulsant derivatives, processes for preparation of and pharmaceutical compositions containing said salts, useful in the treatment of epilepsy.
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公开(公告)号：US20060014929A9
公开(公告)日：2006-01-19
申请号：US10156882
申请日：2002-05-29
IPC分类号： C07K7/08
CPC分类号： C07K5/0808 , A61K38/00 , C07K1/126 , C07K5/0815 , C07K14/785
摘要： The invention realtes to improved liquid phase processes for the preparation of the 21 residue protein component, (Lys-Leu4)4-Lys, of the pulmonary surfactant KL-4. These process are amenable to large scale synthesis and one process employs a method of saponifying an ester which reduces the inherent racemization of the α-carbon.
摘要翻译： 本发明涉及用于制备肺表面活性剂KL-4的21残基蛋白组分（Lys-Leu 4 N 4）4 -Sys的改进的液相方法。 这些方法适合于大规模合成，一种方法采用皂化方法来降低α-碳的固有外消旋化。
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9.发明申请公开(公告)号：US20080228428A1
公开(公告)日：2008-09-18
申请号：US11780342
申请日：2007-07-19
IPC分类号： G06F15/00
CPC分类号： G01N21/65 , G01N21/95 , G06F19/00 , G06F19/703 , G06F19/707 , G16H40/20
摘要： A method and system for the non-destructive analysis of medical devices uses a confocal Raman microscope and other non-destructive analytical tools to assess the spatial distribution of components of an object such as the distribution of an active pharmaceutical ingredient (API) within a polymer matrix. In a preferred embodiment, confocal Raman spectroscopy was used to differentiate each component found in the sirolimus-eluting coronary stent. The unique spectral features identified for each component were then used to develop three separate calibration curves to describe the solid phase distribution found on drug-polymer coated stents. The calibration curves were obtained by analyzing confocal Raman spectral depth profiles from a set of 16 unique formulations of drug-polymer coatings sprayed onto stents and planar substrates.
摘要翻译： 用于医疗装置的非破坏性分析的方法和系统使用共焦拉曼显微镜和其他非破坏性分析工具来评估物体的组分的空间分布，例如聚合物中活性药物成分（API）的分布 矩阵。 在优选实施方案中，使用共焦拉曼光谱法来区分在西罗莫司洗脱冠状动脉支架中发现的每种成分。 然后使用为每个组分鉴定的独特光谱特征来开发三个单独的校准曲线来描述在药物聚合物涂覆的支架上发现的固相分布。 校准曲线通过从喷雾在支架和平面基底上的16组独特的药物 - 聚合物涂层制剂的分析共聚焦拉曼光谱深度分布图获得。
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10.发明授权Arylsubstituted piperazines useful in the treatment of benign prostatic hyperplasia 有权用于治疗良性前列腺增生的芳基取代哌嗪公开(公告)号：US06593474B1
公开(公告)日：2003-07-15
申请号：US09591814
申请日：2000-06-12
申请人： Linda Jolliffe , William Murray , Virginia Pulito , Linda Mulcahy , Xiaobing Li , Allen Reitz , Cynthia Maryanoff , Frank Villani
发明人： Linda Jolliffe , William Murray , Virginia Pulito , Linda Mulcahy , Xiaobing Li , Allen Reitz , Cynthia Maryanoff , Frank Villani
IPC分类号： C07D29514
CPC分类号： C07D207/27 , C07D207/28 , C07D209/48 , C07D211/76 , C07D223/10 , C07D295/13
摘要： This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.
摘要翻译： 本发明涉及一系列芳基取代的哌嗪，含有它们的式I药物组合物和用于其制备的中间体。 本发明的化合物选择性地抑制与α-1a肾上腺素能受体的结合，α受体是与良性前列腺增生有关的受体。 因此，这些化合物在治疗这种疾病和其他疾病中潜在有用。
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