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21. 发明申请

US20110172176A1 CRYSTAL STRUCTURES OF SGLT2 INHIBITORS AND PROCESSES FOR PREPARING SAME 有权
标题翻译： SGLT2抑制剂的晶体结构及其制备方法
公开(公告)号：US20110172176A1
公开(公告)日：2011-07-14
申请号：US13049712
申请日：2011-03-16
申请人： Jack Z. Gougoutas , Hildegard Lobinger , Srividya Ramakrishnan , Prashant P. Deshpande , Jeffrey T. Bien , Chiajen Lai , Chenchi Wang , Peter Riebel , John Anthony Grosso , Alexandra A. Nirschl , Janak Singh , John D. DiMarco
发明人： Jack Z. Gougoutas , Hildegard Lobinger , Srividya Ramakrishnan , Prashant P. Deshpande , Jeffrey T. Bien , Chiajen Lai , Chenchi Wang , Peter Riebel , John Anthony Grosso , Alexandra A. Nirschl , Janak Singh , John D. DiMarco
IPC分类号： A61K31/7034 , C07H15/207 , C07H1/00 , A61P3/04 , A61P3/10 , A61P17/02 , A61P3/06 , A61P9/10 , A61P9/12
CPC分类号： C07H15/207 , A61K31/7034 , A61K45/06 , A61P3/10 , C07H7/04
摘要： The present invention relates to physical crystal structures of a compound of the formula I: wherein R1, R2, R2a, R3 and R4 are as defined herein, especially pharmaceutical compositions containing structures of compound I or II, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
摘要翻译：本发明涉及式I化合物的物理结晶结构：其中R1，R2，R2a，R3和R4如本文所定义，特别是含有化合物I或II结构的药物组合物，其制备方法，制备方法以及使用这种结构治疗糖尿病等疾病的方法。

22. 发明授权

US07932379B2 Methods of producing C-aryl glucoside SGLT2 inhibitors 有权
标题翻译：生产C-芳基葡萄糖苷SGLT2抑制剂的方法
公开(公告)号：US07932379B2
公开(公告)日：2011-04-26
申请号：US11764839
申请日：2007-06-19
申请人： Prashant P. Deshpande , Bruce A. Ellsworth , Janak Singh , Theodor W. Denzel , Chiajen Lai , Gerard Crispino , Michael E. Randazzo , Jack Z. Gougoutas
发明人： Prashant P. Deshpande , Bruce A. Ellsworth , Janak Singh , Theodor W. Denzel , Chiajen Lai , Gerard Crispino , Michael E. Randazzo , Jack Z. Gougoutas
IPC分类号： C07H1/00
CPC分类号： C07H23/00 , C07H5/04 , C07H5/06 , C07H7/00 , C07H15/207
摘要： Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.
摘要翻译：生产用于治疗糖尿病和相关疾病的C-芳基葡萄糖苷SGLT2抑制剂的方法。及其中间体。 C-芳基葡糖苷可以与形成氨基酸复合物的试剂络合。

23. 发明申请

US20110201795A1 Methods of Producing C-Aryl Glucoside SGLT2 Inhibitors 审中-公开
标题翻译：生产C-Aryl Glucoside SGLT2抑制剂的方法
公开(公告)号：US20110201795A1
公开(公告)日：2011-08-18
申请号：US13093430
申请日：2011-04-25
申请人： Prashant P. Deshpande , Bruce A. Ellsworth , Janak Singh , Theodor W. Denzel , Chiajen Lai , Gerard Crispino , Michael E. Randazzo , Jack Z. Gougoutas
发明人： Prashant P. Deshpande , Bruce A. Ellsworth , Janak Singh , Theodor W. Denzel , Chiajen Lai , Gerard Crispino , Michael E. Randazzo , Jack Z. Gougoutas
IPC分类号： C07H1/00 , C07H23/00 , C07H15/02
CPC分类号： C07H23/00 , C07H5/04 , C07H5/06 , C07H7/00 , C07H15/207
摘要： Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.
摘要翻译：生产用于治疗糖尿病和相关疾病的C-芳基葡萄糖苷SGLT2抑制剂的方法。及其中间体。 C-芳基葡糖苷可以与形成氨基酸复合物的试剂络合。

24. 发明授权

US06774112B2 Amino acid complexes of C-aryl glucosides for treatment of diabetes and method 有权
标题翻译：用于治疗糖尿病的C-芳基葡糖苷的氨基酸配合物及方法
公开(公告)号：US06774112B2
公开(公告)日：2004-08-10
申请号：US10117914
申请日：2002-04-08
申请人： Jack Z. Gougoutas
发明人： Jack Z. Gougoutas
IPC分类号： A61K3170
CPC分类号： A61K45/06 , A61K31/351 , C07H15/203 , Y10S514/866 , A61K2300/00
摘要： Crystalline complexes are obtained from a 1:1 or 2:1 mixtures of either the (D) or (L) enantiomer of natural amino acids and compounds of formula wherein R1, R2 and R2a are independently hydrogen, OH, OR5, alkyl, —OCHF2, —OCF3, —SR5a or halogen; R3 and R4 are independently hydrogen, OH, OR5b, alkyl, cycloalkyl, CF3, —OCHF2, —OCF3, halogen, —CONR6R6a, —CO2R5c, —CO2H, —COR6b, —CH(OH)R6c, —CH(OR5d)R6d, —CN, —NHCOR5e, —NHSO2R5f, —NHSO2Aryl, —SR5g, —SOR5h, —SO2R5i, or a five, six or seven membered heterocycle which may contain 1 to 4 heteroatoms in the ring which are N, O, S, SO, and/or SO2, or R3 and R4 together with the carbons to which they are attached form an annelated five, six or seven membered carbocycle or heterocycle which may contain 1 to 4 heteroatoms in the ring which are N, O, S, SO, and/or SO2; R5, R5a, R5b, R5c, R5d, R5e, R5f, R5g, R5h and R5i are independently alkyl; R6, R6a, R6b, R6c and R6d are independently hydrogen, alkyl, aryl, alkylaryl or cycloalkyl, or R6 and R6a together with the nitrogen to which they are attached form an annelated five, six or seven membered heterocycle which may contain 1 to 4 heteroatoms in the ring which are N, O, S, SO, and/or SO2. A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above complex alone or in combination with another antidiabetic agent or other therapeutic agent.
摘要翻译：结晶配合物由天然氨基酸的（D）或（L）对映异构体与式1，R 2和R 2a的化合物的1:1或2:1混合物分别获得氢， OH，OR 5，烷基，-OCHF 2，-OCF 3，-SR 5a或卤素; R 3和R 4独立地是氢，OH，OR 5b，烷基，环烷基，CF 3 - OCHF 2，-OCF 3，卤素，-CONR 6 R 6a，-CO 2 R 5c，-CO 2 H，-COR 6b，-CH（OH）R 6c，-CH（OR 5） R 6，-CN，-NHCOR 5e，-NHSO 2 R 5，-NHSO 2芳基，-SR 5g，-SOR 5h，-SO 2 R 5，或五，六或七元杂环其可以在环中含有1至4个N，O，S，SO和/或SO 2的杂原子，或者R 3和R 4与它们所连接的碳一起形成五至六个或七元碳环或杂环，其在环中可以含有1至4个杂原子，其为N，O，S，SO和/或SO 2; R 5，R 5a，R 5b，R 5c， R 5，R 5e，R 5f，R 5g，R 5h和R 5独立地是烷基; R 6，R 6a，R 6b，R <6c>和R <6d>是独立的氢，烷基，芳基，烷基芳基或环烷基，或R 6和R 6a与它们所连接的氮一起形成环状的五，六或七元杂环，其可以在环中含有1至4个杂原子其也是N，O，S，SO和/或SO2的方法。还提供了单独使用上述复合物的SGLT2抑制量或与另一种抗糖尿病药或其它治疗剂组合治疗糖尿病和相关疾病的方法。

25. 发明申请

US20080287529A1 CRYSTAL STRUCTURES OF SGLT2 INHIBITORS AND PROCESSES FOR PREPARING SAME 审中-公开
标题翻译： SGLT2抑制剂的晶体结构及其制备方法
公开(公告)号：US20080287529A1
公开(公告)日：2008-11-20
申请号：US12120722
申请日：2008-05-15
申请人： Prashant P. Deshpande , Lifen Lori Shen , Jack Z. Gougoutas
发明人： Prashant P. Deshpande , Lifen Lori Shen , Jack Z. Gougoutas
IPC分类号： A61K31/351 , C07D315/00 , A61P3/00
CPC分类号： C07H7/04 , A61K31/351 , A61K45/06 , A61K2300/00
摘要： The present invention relates to physical crystal structures of compound of the formula (I): which is an H-1 form, H-2 form or S-PG form, pharmaceutical compositions containing structures of compound I and methods of treating diseases using compound I.
摘要翻译：本发明涉及式（I）化合物的物理结晶结构：其为H-1形式，H-2形式或S-PG形式，含有化合物I结构的药物组合物和使用化合物I治疗疾病的方法。

26. 发明授权

US07375213B2 Methods of producing C-aryl glucoside SGLT2 inhibitors 有权
标题翻译：生产C-芳基葡萄糖苷SGLT2抑制剂的方法
公开(公告)号：US07375213B2
公开(公告)日：2008-05-20
申请号：US10745075
申请日：2003-12-23
申请人： Prashant P. Deshpande , Bruce A. Ellsworth , Janak Singh , Theodor W. Denzel , Chiajen Lai , Gerard Crispino , Michael E. Randazzo , Jack Z. Gougoutas
发明人： Prashant P. Deshpande , Bruce A. Ellsworth , Janak Singh , Theodor W. Denzel , Chiajen Lai , Gerard Crispino , Michael E. Randazzo , Jack Z. Gougoutas
IPC分类号： C07H15/203 , C07H15/20 , C07H1/00
CPC分类号： C07H23/00 , C07H5/04 , C07H5/06 , C07H7/00 , C07H15/207
摘要： Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.
摘要翻译：生产用于治疗糖尿病和相关疾病的C-芳基葡萄糖苷SGLT2抑制剂的方法。及其中间体。 C-芳基葡糖苷可以与形成氨基酸复合物的试剂络合。

27. 发明授权

US07241899B2 Methods for the preparation, isolation and purification of epothilone B, and X-ray crystal structures of epothilone B 有权
标题翻译：埃坡霉素B的制备，分离和纯化方法以及埃坡霉素B的X射线晶体结构
公开(公告)号：US07241899B2
公开(公告)日：2007-07-10
申请号：US10805724
申请日：2004-03-22
申请人： Daniel A. Benigni , Jack Z. Gougoutas , John D. DiMarco
发明人： Daniel A. Benigni , Jack Z. Gougoutas , John D. DiMarco
IPC分类号： A61K31/724 , C12P17/14 , C07D417/02
CPC分类号： C07D493/04 , C12N1/20 , C12N1/38 , C12P17/181 , C12R1/01
摘要： The present invention relates to improved methods for the production, isolation and purification of epothilone B. These methods include, for example, a fermentation process for the production of epothilone B, isolation via adsorption onto a resin, and subsequent purification.
摘要翻译：本发明涉及埃坡霉素B的生产，分离和纯化的改进方法。这些方法包括例如用于生产埃坡霉素B的发酵方法，通过吸附到树脂上进行分离和随后的纯化。

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