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21. 发明授权

US06489476B1 Heteroaromatic compounds containing a phosphonate group that are inhibitors of fructose-1,6-bisphosphatase 有权
标题翻译：含有作为果糖-1,6-二磷酸酶抑制剂的膦酸酯基的杂芳族化合物
公开(公告)号：US06489476B1
公开(公告)日：2002-12-03
申请号：US09389698
申请日：1999-09-03
申请人： Qun Dang , Srinivas Rao Kasibhatla , K. Raja Reddy , Mark D. Erion , M. Rami Reddy , Atul Agarwal
发明人： Qun Dang , Srinivas Rao Kasibhatla , K. Raja Reddy , Mark D. Erion , M. Rami Reddy , Atul Agarwal
IPC分类号： C07F902
CPC分类号： C07F9/4006 , C07F9/5728 , C07F9/58 , C07F9/650952 , C07F9/6512 , C07F9/653 , C07F9/65324 , C07F9/6539 , C07F9/65395 , C07F9/6541 , C07F9/65515 , C07F9/65517 , C07F9/655345 , C07F9/65583 , C07F9/65586 , C07F9/657181 , C07F9/6578 , C07F9/65846
摘要： FBPase inhibitors of the formula I and X are useful in the treatment of diabetes and other conditions associated with elevated blood glucose or excess glycogen storage.
摘要翻译：式I和X的FBPase抑制剂可用于治疗与升高的血糖或过量糖原储存相关的糖尿病和其他病症。

22. 发明授权

US6110903A Benzimidazole inhibitors of fructose 1,6-bisphosphatase 失效
公开(公告)号：US6110903A
公开(公告)日：2000-08-29
申请号：US36329
申请日：1998-03-06
申请人： Srinivas Rao Kasibhatla , K. Raja Reddy , Mark D. Erion , Qun Dang , Gerard R. Scarlato , M. Rami Reddy
发明人： Srinivas Rao Kasibhatla , K. Raja Reddy , Mark D. Erion , Qun Dang , Gerard R. Scarlato , M. Rami Reddy
IPC分类号： A61K31/675 , A61P3/10 , A61P9/10 , C07F9/6506 , C07F9/6558 , A61K31/662 , C07F9/06 , C07F9/38 , C07F9/40
CPC分类号： C07F9/65068 , C07F9/65586
摘要： Novel benzimidazole compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described ##STR1##

23. 发明授权

US06294672B1 Indole and azaindole inhibitors of Fructose-1,6-biphosphatase 有权
标题翻译：果糖-1,6-二磷酸酶的吲哚和azaindole抑制剂
公开(公告)号：US06294672B1
公开(公告)日：2001-09-25
申请号：US09479384
申请日：2000-01-05
申请人： K. Raja Reddy , Gerard R. Scarlato , Qun Dang , Mark D. Erion , Srinivas Rao Kasibhatla , M. Rami Reddy
发明人： K. Raja Reddy , Gerard R. Scarlato , Qun Dang , Mark D. Erion , Srinivas Rao Kasibhatla , M. Rami Reddy
IPC分类号： C07F924
CPC分类号： C07F9/5728 , C07F9/65586 , C07F9/6561
摘要： The present invention is directed towards novel azaindole compounds which bind to the AMP site and are potent FBPase inhibitors. The present invention also is directed towards the clinical use of the novel FBPase inhibitors as a method of treatment or prevention of diseases responsive to lowered blood glucose levels.
摘要翻译：本发明涉及与AMP位点结合并且是有效的FBP酶抑制剂的新颖的氮杂吲哚化合物。本发明还涉及新型FBP酶抑制剂作为治疗或预防对低血糖水平降低的疾病的方法的临床应用。

24. 发明授权

US06284748B1 Purine inhibitors of fructose 1,6-bisphosphatase 失效
标题翻译：果糖1,6-二磷酸酶的嘌呤抑制剂
公开(公告)号：US06284748B1
公开(公告)日：2001-09-04
申请号：US09036327
申请日：1998-03-06
申请人： Qun Dang , Mark D. Erion , M. Rami Reddy , Edward D. Robinson , Srinivas Rao Kasibhatla , K. Raja Reddy
发明人： Qun Dang , Mark D. Erion , M. Rami Reddy , Edward D. Robinson , Srinivas Rao Kasibhatla , K. Raja Reddy
IPC分类号： C07F96561
CPC分类号： C07F9/65616 , C07F9/657181
摘要： Novel purine compounds of the following structure and their use as fructose-1,6-bisphosphatase inhibitors is described. wherein A is selected from the group consisting of —NR82, —NHSO2R3, —OR5, —SR5, halo, lower alkyl, —CON(R4)2, guanidino, amidino, —H, and perhaloalkyl; E is selected from the group consisting of —H, halo, lower alkylthio, lower perhaloalkyl, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, —CN, and —NR72; X is selected from the group consisting of -alk-NR—, alkylene, alkenylene, alkynylene, arylene, heteroarylene, -alk-NR-alk-, -alk-O-alk-, -alk-S-alk-, -alk-S—, alicyclicene, heteroalicyclicene, 1,1-dihaloalkylene, —C(O)-alk-, —NR—C(O)—NR′—, -alk-NR—C(O)—, -alk-C(O)—NR—, —Ar-alk-, and -alk-Ar—, all optionally substituted, wherein each R and R′ is independently selected from —H and lower alkyl, and wherein each “alk” and “Ar” is an independently selected alkylene or arylene, respectively; Y is selected from the group consisting of —H, alkyl, alkenyl, alkynyl, aryl, alicyclic, heteroalicyclic, aralkyl, aryloxyalkyl, alkoxyalkyl, —C(O)R3, —S(O)2R3, —C(O)—OR3, —CONHR3, —NR22, and —OR3, all except H are optionally substituted; and pharmaceutically acceptable prodrugs and salts thereof.
摘要翻译：描述了以下结构的新型嘌呤化合物及其作为果糖-1,6-二磷酸酶抑制剂的用途，其中A选自-NR82，-NHSO2R3，-OR5，-SR5，卤素，低级烷基，-CON（ R 4）2，胍基，脒基，-H和全卤代烷基; E选自-H，卤素，低级烷硫基，低级全卤代烷基，低级烷基，低级烯基，低级炔基，低级烷氧基，-CN和 - NR72; X选自-alk-NR-，亚烷基，亚烯基，亚炔基，亚芳基，亚杂芳基，-alk-NR-烷基， - 烷基-O-烷基， - 烷基-S-烷基，（O）-NR' - ，-NR-C（O） - ， - 烷基，（C 1 -C 6） - 烷基亚磺酰基，其中每个R和R'独立地选自-H和低级烷基，并且其中每个“烷基”和“烷氧基” Ar“分别是独立选择的亚烷基或亚芳基; Y选自-H，烷基，烯基，炔基，芳基，脂环，杂脂环，芳烷基，芳氧基烷基，烷氧基烷基，-C（O）R 3，-S（O）2 R 3，-C（O）-OR 3，-CONHR 3，-NR 22和-OR 3，和药学上可接受的前药及其盐。

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