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公开(公告)号：US08436167B2
公开(公告)日：2013-05-07
申请号：US13038245
申请日：2011-03-01
申请人： Rebecca Jane Booth , Peter Anthony Cittern , Jeffrey Norman Crabb , John Horbury , David Wyn Calvert Jones
发明人： Rebecca Jane Booth , Peter Anthony Cittern , Jeffrey Norman Crabb , John Horbury , David Wyn Calvert Jones
IPC分类号： C07D239/36 , C07D239/42
CPC分类号： C07D239/42
摘要： Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described.
摘要翻译： 双[（E）-7- [4-（4-氟苯基）-6-异丙基-2- [甲基（甲基磺酰基）氨基]嘧啶-5-基]（3R，5S）-3,5-二 二羟基庚-6-烯酸]钙盐，其制备方法及其作为HMG Co-A还原酶抑制剂的用途。
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公开(公告)号：US20120294936A1
公开(公告)日：2012-11-22
申请号：US13509206
申请日：2010-11-12
申请人： Admassu Abebe , Kyle Martin , Jatin M. Patel , Peter Timmins
发明人： Admassu Abebe , Kyle Martin , Jatin M. Patel , Peter Timmins
IPC分类号： A61K31/155 , A61K9/14 , A61K9/52 , A61K31/17 , A61P3/06 , A61K38/28 , A61K38/26 , A61P3/10 , A61P3/04 , A61K9/28 , A61K31/426
CPC分类号： A61K31/155 , A61K9/1652 , A61K9/2054 , A61K45/06 , A61K2300/00
摘要： The present invention relates to metformin extended release (XR) formulations with improved compactability to provide reduced mass tablets, granulations, and capsules.
摘要翻译： 本发明涉及二甲双胍延长释放（XR）制剂，其具有改进的可压缩性以提供减质量的片剂，颗粒剂和胶囊。
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公开(公告)号：USD671207S1
公开(公告)日：2012-11-20
申请号：US29382991
申请日：2011-01-11
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公开(公告)号：US20120282336A1
公开(公告)日：2012-11-08
申请号：US13509210
申请日：2010-11-12
申请人： Admassu Abebe , Kyle Martin , Jatin M. Patel , Divyakant Desai , Peter Timmins
发明人： Admassu Abebe , Kyle Martin , Jatin M. Patel , Divyakant Desai , Peter Timmins
IPC分类号： A61K9/24 , A61P3/06 , A61P27/12 , A61P27/02 , A61P13/12 , A61P25/00 , A61P3/04 , A61P17/02 , A61P9/10 , A61P9/12 , A61K31/155 , A61K31/7034 , A61K38/28 , A61K38/26 , A61P3/10
CPC分类号： A61K9/209 , A61K9/2054 , A61K9/282 , A61K31/155 , A61K31/403 , A61K31/70 , A61K31/7004 , A61K31/7034 , A61K31/7042 , A61K45/06 , A61K2300/00
摘要： The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.
摘要翻译： 本发明涉及包含作为第一层的二甲双胍延长释放（XR）或还原质量二甲双胍XR制剂，作为第二层的SGLT2抑制剂制剂和任选的膜包衣的双层片剂制剂。 本发明提供制备双层片剂制剂的方法和使用双层片剂制剂治疗与SGLT2活性相关的疾病或病症的方法。
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![Process for the Manufacture of the Calcium Salt of Rosuvastatin (E)-7-[4-(4-Fluorophenyl)-6-Isopropyl-2-[Methyl(Methylsulfonyl)Amino]-Pyrimidin-5-yl](3R,5S)-3,5-Dihydroxyhept-6-Enoic Acid and Crystalline Intermediates Thereof](/abs-image/US/2011/12/08/US20110301348A1/abs.jpg.150x150.jpg)
95.发明申请Process for the Manufacture of the Calcium Salt of Rosuvastatin (E)-7-[4-(4-Fluorophenyl)-6-Isopropyl-2-[Methyl(Methylsulfonyl)Amino]-Pyrimidin-5-yl](3R,5S)-3,5-Dihydroxyhept-6-Enoic Acid and Crystalline Intermediates Thereof 审中-公开罗苏伐他汀（E）-7- [4-（4-氟苯基）-6-异丙基-2- [甲基（甲基磺酰基）氨基] - 嘧啶-5-基]（3R，5S）的钙盐的制造方法 -3,5-二羟基庚-6-烯酸及其结晶中间体公开(公告)号：US20110301348A1
公开(公告)日：2011-12-08
申请号：US13186363
申请日：2011-07-19
IPC分类号： C07D407/06 , C07D239/69
CPC分类号： C07D239/42 , C07D405/06 , Y02P20/55
摘要： A process for the manufacture of the calcium salt of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid, useful as an HMGCoA reductase inhibitor, from a compound of the formula (7) wherein A is an acetal or ketal protecting group and R is alkyl, via isolated crystalline compounds of the formula (8) or of formula (10) is described. Crystalline intermediates of formulae 7, 8 and 10 are also described.
摘要翻译： （E）-7- [4-（4-氟苯基）-6-异丙基-2- [甲基（甲基磺酰基）氨基]嘧啶-5-基]（3R，5S）的钙盐的制备方法 由式（7）的化合物（其中A是缩醛或缩酮保护基，R是烷基）用作HMGCoA还原酶抑制剂的3,5-二羟基庚-6-烯酸经由分离的式（8）的结晶化合物 ）或式（10）。 还描述了式7,8和10的结晶中间体。
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公开(公告)号：US07888083B2
公开(公告)日：2011-02-15
申请号：US12768459
申请日：2010-04-27
CPC分类号： C07D319/06 , C07C67/03 , C07C69/675 , C12P7/62 , C12P17/06 , C07C69/716
摘要： A process is provided for the preparation of a compound of formula (1) wherein R and R′ represent optionally substituted hydrocarbyl groups and X represents a hydrocarbyl linking group. The process comprises either the stereoselective reduction of the keto group in a dihydroxy keto precursor followed by selective esterification of a primary hydroxy, or selective esterification of a primary hydroxy of a dihydroxy keto precursor followed by stereoselective reduction of the keto group.
摘要翻译： 提供了制备式（1）化合物的方法，其中R和R'代表任选取代的烃基，X代表烃基连接基团。 该方法包括立体选择性还原二羟基酮基前体中的酮基，然后选择性酯化初级羟基，或选择性酯化二羟基酮基前体的伯羟基，然后立体选择性还原酮基。
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97.发明申请METHOD FOR TREATING CANCERS HAVING HIGH GLUCOSE REQUIREMENTS EMPLOYING AN SGLT2 INHIBITOR AND COMPOSITIONS THEREOF 失效用于治疗采用SGLT2抑制剂及其组合物的高葡萄糖需求的癌症的方法公开(公告)号：US20110015141A1
公开(公告)日：2011-01-20
申请号：US12933013
申请日：2009-03-16
申请人： Mario Maldonado , Paul Strumph
发明人： Mario Maldonado , Paul Strumph
IPC分类号： A61K31/7034 , A61P35/02
CPC分类号： A61K31/70
摘要： Methods are provided for treating cancers that have high glucose requirements and that express SGLT2 at levels higher than normal cells, such as metastatic cancers, for example, metastatic lung cancers, employing an SGLT2 inhibitor alone or in combination with a cytotoxic agent and to a composition containing a combination of an SGLT2 inhibitor and a cytotoxic agent.
摘要翻译： 提供了用于治疗具有高葡萄糖要求并以高于正常细胞的水平表达SGLT2的癌症的方法，例如转移性癌症，例如转移性肺癌，单独使用SGLT2抑制剂或与细胞毒性剂组合，以及组合物 含有SGLT2抑制剂和细胞毒性剂的组合。
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公开(公告)号：US20100278835A1
公开(公告)日：2010-11-04
申请号：US12720094
申请日：2010-03-09
申请人： Helen Blade , Heather Marie Jackson , Gary Peter Tomkinson , Elisa Ann Carron , James Andrew Lumley , Christopher John Pilkington , Alexander James Floyd Thomas , Justin Warne
发明人： Helen Blade , Heather Marie Jackson , Gary Peter Tomkinson , Elisa Ann Carron , James Andrew Lumley , Christopher John Pilkington , Alexander James Floyd Thomas , Justin Warne
IPC分类号： A61K31/519 , C07D403/06 , A61K31/517 , C07D471/04 , A61P31/14 , A61P11/00 , A61K39/42
CPC分类号： C07D403/06 , C07D471/04
摘要： The invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and R12 are as defined in the specification, and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are useful in the treatment of respiratory syncytial virus (RSV).
摘要翻译： 本发明提供式（I）化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 11和R 12如本说明书中所定义，及其旋光异构体，外消旋体和互变异构体， 其药学上可接受的盐; 以及其制备方法，含有它们的药物组合物及其在治疗中的用途。 该化合物可用于治疗呼吸道合胞病毒（RSV）。
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公开(公告)号：US20100260765A1
公开(公告)日：2010-10-14
申请号：US12669724
申请日：2008-07-23
CPC分类号： C07K16/2863 , A61K38/16 , A61K2039/505 , C07K2317/21 , C07K2317/56 , C07K2317/73 , C07K2317/75 , C07K2317/76 , C07K2317/92
摘要： The invention relates to targeted binding agents against KDR and uses of such agents. More specifically, the invention relates to fully human monoclonal antibodies directed to KDR. The described targeted binding agents are useful in the treatment of diseases associated with the activity and/or overproduction of KDR and as diagnostics.
摘要翻译： 本发明涉及针对KDR的靶向结合剂及其用途。 更具体地，本发明涉及针对KDR的完全人单克隆抗体。 所描述的靶向结合剂可用于治疗与KDR的活性和/或过量产生相关的疾病和作为诊断。
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公开(公告)号：US07732171B2
公开(公告)日：2010-06-08
申请号：US12178424
申请日：2008-07-23
CPC分类号： C07D319/06 , C07C67/03 , C07C69/675 , C12P7/62 , C12P17/06 , C07C69/716
摘要： A process is provided for the preparation of a compound of formula (1) wherein R and R′ represent optionally substituted hydrocarbyl groups and X represents a hydrocarbyl linking group. The process comprises either the stereoselective reduction of the keto group in a dihydroxy keto precursor followed by selective esterification of a primary hydroxy, or selective esterification of a primary hydroxy of a dihydroxy keto precursor followed by stereoselective reduction of the keto group.
摘要翻译： 提供了制备式（1）化合物的方法，其中R和R'代表任选取代的烃基，X代表烃基连接基团。 该方法包括立体选择性还原二羟基酮基前体中的酮基，然后选择性酯化初级羟基，或选择性酯化二羟基酮基前体的伯羟基，然后立体选择性还原酮基。
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