公开(公告)号：US08710236B2

公开(公告)日：2014-04-29

申请号：US13083321

申请日：2011-04-08

申请人： Jorge E. Gomez-Galeno ,  K. Raja Reddy ,  Paul D. van Poelje ,  Robert Huerta Lemus ,  Thanh Huu Nguyen ,  Matthew P. Grote ,  Qun Dang ,  Scott J. Hecker ,  Venkat Reddy Mali ,  Mingwei Chen ,  Zhili Sun ,  Serge Henri Boyer ,  Haiqing Li ,  William Craigo

发明人： Jorge E. Gomez-Galeno ,  K. Raja Reddy ,  Paul D. van Poelje ,  Robert Huerta Lemus ,  Thanh Huu Nguyen ,  Matthew P. Grote ,  Qun Dang ,  Scott J. Hecker ,  Venkat Reddy Mali ,  Mingwei Chen ,  Zhili Sun ,  Serge Henri Boyer ,  Haiqing Li ,  William Craigo

IPC分类号： C07D263/57 ,  C07D307/81 ,  C07C309/15

CPC分类号： C07C309/15 ,  C07C307/02 ,  C07C309/11 ,  C07C317/44 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2603/74 ,  C07D209/20 ,  C07D213/53 ,  C07D213/75 ,  C07D235/30 ,  C07D261/08 ,  C07D263/56 ,  C07D277/66 ,  C07D307/68 ,  C07D307/81 ,  C07D317/66 ,  C07D333/38 ,  C07D405/04 ,  C07D409/12 ,  C07D413/04 ,  C07D471/04 ,  C07D498/04

摘要： The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

摘要翻译： 本发明提供具有胰高血糖素受体拮抗剂或反向激动剂活性的新颖的式（I）化合物及其药学上可接受的盐和共晶体。 本发明进一步提供了包含其的药物组合物以及治疗，预防，延迟发病时间或降低其中指示一种或多种胰高血糖素受体拮抗剂的疾病或病症的发展或进展的风险的方法， 包括I型和II型糖尿病，胰岛素抵抗和高血糖。 本发明还提供制备式I化合物的方法，包括其盐和共结晶，以及包含其的药物组合物。

公开(公告)号：US20120214769A1

公开(公告)日：2012-08-23

申请号：US13083321

申请日：2011-04-08

申请人： Jorge E. Gomez-Galeno ,  K. Raja Reddy ,  Paul D. van Poelje ,  Robert Huerta Lemus ,  Thanh Huu Nguyen ,  Matthew P. Grote ,  Qun Dang ,  Scott J. Hecker ,  Venkat Reddy Mali ,  Mingwei Chen ,  Zhili Sun ,  Serge Henri Boyer ,  Haiqing Li ,  William Craigo

发明人： Jorge E. Gomez-Galeno ,  K. Raja Reddy ,  Paul D. van Poelje ,  Robert Huerta Lemus ,  Thanh Huu Nguyen ,  Matthew P. Grote ,  Qun Dang ,  Scott J. Hecker ,  Venkat Reddy Mali ,  Mingwei Chen ,  Zhili Sun ,  Serge Henri Boyer ,  Haiqing Li ,  William Craigo

IPC分类号： A61K31/675 ,  A61K31/185 ,  C07D307/81 ,  A61K31/343 ,  C07D295/185 ,  A61K31/4965 ,  C07D213/75 ,  A61K31/4418 ,  C07D405/04 ,  A61K31/443 ,  C07D235/30 ,  A61K31/4184 ,  C07F9/655 ,  A61K31/665 ,  C07D471/04 ,  A61K31/437 ,  C07F9/40 ,  A61K31/662 ,  C07D295/135 ,  A61K31/5375 ,  C07D261/08 ,  A61K31/42 ,  C07F9/653 ,  A61P3/10 ,  A61P3/08 ,  A61P1/16 ,  A61P3/06 ,  A61P9/10 ,  A61P3/04 ,  A61P3/00 ,  C07C309/15

CPC分类号： C07C309/15 ,  C07C307/02 ,  C07C309/11 ,  C07C317/44 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2603/74 ,  C07D209/20 ,  C07D213/53 ,  C07D213/75 ,  C07D235/30 ,  C07D261/08 ,  C07D263/56 ,  C07D277/66 ,  C07D307/68 ,  C07D307/81 ,  C07D317/66 ,  C07D333/38 ,  C07D405/04 ,  C07D409/12 ,  C07D413/04 ,  C07D471/04 ,  C07D498/04

摘要： The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

摘要翻译： 本发明提供具有胰高血糖素受体拮抗剂或反向激动剂活性的新颖的式（I）化合物及其药学上可接受的盐和共晶体。 本发明进一步提供了包含其的药物组合物以及治疗，预防，延迟发病时间或降低其中指示一种或多种胰高血糖素受体拮抗剂的疾病或病症的发展或进展的风险的方法， 包括I型和II型糖尿病，胰岛素抵抗和高血糖。 本发明还提供制备式I化合物的方法，包括其盐和共结晶，以及包含其的药物组合物。

公开(公告)号：US07498320B2

公开(公告)日：2009-03-03

申请号：US11528283

申请日：2006-09-28

申请人： K. Raja Reddy ,  William Craigo ,  Zhili Sun ,  Serge Boyer ,  Bheemarao G. Ugarkar

发明人： K. Raja Reddy ,  William Craigo ,  Zhili Sun ,  Serge Boyer ,  Bheemarao G. Ugarkar

IPC分类号： A61K31/665 ,  C07F9/02

CPC分类号： C07F9/65742 ,  C07H19/04

摘要： Compounds of Formula I, their preparation and synthetic intermediates, and their use in the synthesis of prodrugs: wherein: V and L are trans relative to one another; V is selected from group consisting of carbocyclic aryl, substituted carbocyclic aryl, heteroaryl, and substituted heteroaryl; and L is a leaving group selected from the group consisting of halogen, alkyl sulfonate, aryloxy optionally substituted with 1-2 substituents, N-containing heteroaryl, and N-hydroxy-nitrogen containing heteroaryl; and salts thereof.

摘要翻译： 式I化合物，其制备方法和合成中间体及其在前体药物合成中的应用：其中：V和L相对于彼此是反式的; V选自碳环芳基，取代的碳环芳基，杂芳基和取代的杂芳基; 并且L是选自卤素，烷基磺酸酯，任选被1-2个取代基取代的芳氧基，含N杂芳基和N-羟基 - 含氮杂芳基的离去基团; 及其盐。

公开(公告)号：US07148349B2

公开(公告)日：2006-12-12

申请号：US10698924

申请日：2003-10-31

申请人： K. Raja Reddy ,  William Craigo ,  Zhili Sun ,  Serge Boyer ,  Bheemarao G. Ugarkar

发明人： K. Raja Reddy ,  William Craigo ,  Zhili Sun ,  Serge Boyer ,  Bheemarao G. Ugarkar

IPC分类号： C07D239/02 ,  C07D487/06 ,  C07C9/02

CPC分类号： C07F9/65742 ,  C07H19/04

摘要： Compounds of Formula I, their preparation and synthetic intermediates, and their use in the synthesis of prodrugs: wherein: V and L are trans relative to one another; V is selected from group consisting of carbocyclic aryl, substituted carbocyclic aryl, heteroaryl, and substituted heteroaryl; and L is a leaving group selected from the group consisting of halogen, alkyl sulfonate, aryloxy optionally substituted with 1–2 substituents, N-containing heteroaryl, and N-hydroxy-nitrogen containing heteroaryl; and salts thereof.

公开(公告)号：US20070021388A1

公开(公告)日：2007-01-25

申请号：US11528283

申请日：2006-09-28

申请人： K. Reddy ,  William Craigo ,  Zhili Sun ,  Serge Boyer ,  Bheemarao Ugarkar

发明人： K. Reddy ,  William Craigo ,  Zhili Sun ,  Serge Boyer ,  Bheemarao Ugarkar

IPC分类号： A61K31/675 ,  C07F9/6512 ,  C07F9/6509

CPC分类号： C07F9/65742 ,  C07H19/04

摘要： Compounds of Formula I, their preparation and synthetic intermediates, and their use in the synthesis of prodrugs: wherein: V and L are trans relative to one another; V is selected from group consisting of carbocyclic aryl, substituted carbocyclic aryl, heteroaryl, and substituted heteroaryl; and L is a leaving group selected from the group consisting of halogen, alkyl sulfonate, aryloxy optionally substituted with 1-2 substituents, N-containing heteroaryl, and N-hydroxy-nitrogen containing heteroaryl; and salts thereof.

摘要翻译： 式I化合物，其制备方法和合成中间体及其在前体药物合成中的应用：其中：V和L相对于彼此是反式的; V选自碳环芳基，取代的碳环芳基，杂芳基和取代的杂芳基; 并且L是选自卤素，烷基磺酸酯，任选被1-2个取代基取代的芳氧基，含N杂芳基和N-羟基 - 含氮杂芳基的离去基团; 及其盐。