公开(公告)号：US07989457B2

公开(公告)日：2011-08-02

申请号：US11569273

申请日：2005-05-13

申请人： Mark Donald Chappell ,  Scott Eugene Conner ,  Isabel Cristina Gonzalez Valcarcel ,  Jason Eric Lamar ,  Jianke Li ,  Julie Sue Moyers ,  Rebecca Anne Owens ,  Allie Edward Tripp ,  Guoxin Zhu

发明人： Mark Donald Chappell ,  Scott Eugene Conner ,  Isabel Cristina Gonzalez Valcarcel ,  Jason Eric Lamar ,  Jianke Li ,  Julie Sue Moyers ,  Rebecca Anne Owens ,  Allie Edward Tripp ,  Guoxin Zhu

IPC分类号： C07D239/26 ,  A61K31/505

CPC分类号： C07D213/16 ,  C07D213/26 ,  C07D213/30 ,  C07D213/32 ,  C07D213/643 ,  C07D239/26 ,  C07D401/04

摘要： The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

摘要翻译： 本发明公开了具有胰高血糖素受体拮抗剂或反向激动剂活性的式（I）的新化合物或其药学上可接受的盐，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式（I）化合物的药物组合物以及使用它们治疗糖尿病和其它与胰高血糖素相关的代谢紊乱等的方法。

公开(公告)号：US20080125468A1

公开(公告)日：2008-05-29

申请号：US11569273

申请日：2005-05-13

申请人： Mark Donald Chappell ,  Scott Eugene Conner ,  Isabel Cristina Gonzalez Valcarcel ,  Jason Eric Lamar ,  Jianke Li ,  Julie Sue Moyers ,  Rebecca Anne Owens ,  Allie Edward Tripp ,  Guoxin Zhu

发明人： Mark Donald Chappell ,  Scott Eugene Conner ,  Isabel Cristina Gonzalez Valcarcel ,  Jason Eric Lamar ,  Jianke Li ,  Julie Sue Moyers ,  Rebecca Anne Owens ,  Allie Edward Tripp ,  Guoxin Zhu

IPC分类号： A61K31/44 ,  C07D211/70 ,  A61P3/10 ,  A61K31/165 ,  C07C233/00

CPC分类号： C07D213/16 ,  C07D213/26 ,  C07D213/30 ,  C07D213/32 ,  C07D213/643 ,  C07D239/26 ,  C07D401/04

摘要： The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

公开(公告)号：US08084489B2

公开(公告)日：2011-12-27

申请号：US11815987

申请日：2006-02-09

申请人： Mark Donald Chappell ,  Scott Eugene Conner ,  Allie Edward Tripp ,  Guoxin Zhu

发明人： Mark Donald Chappell ,  Scott Eugene Conner ,  Allie Edward Tripp ,  Guoxin Zhu

IPC分类号： A61K31/381 ,  C07D333/22 ,  C07D409/12 ,  A61P3/10

CPC分类号： C07D333/38 ,  C07D409/12

摘要： The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have glucagon receptor antagonist or inverse agonist activity, as well as methods of using these compounds and intermediates and methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising N compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

摘要翻译： 本发明公开了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）化合物或其药学上可接受的盐，以及使用这些化合物和中间体的方法以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式（I）的N种化合物的药物组合物以及使用它们治疗糖尿病和其它与胰高血糖素相关的代谢紊乱等的方法。

公开(公告)号：US07807702B2

公开(公告)日：2010-10-05

申请号：US12094406

申请日：2006-11-21

申请人： Mark Donald Chappell ,  Scott Eugene Conner ,  Philip-Arthur Hipskind ,  Allie Edward Tripp ,  Guoxin Zhu

发明人： Mark Donald Chappell ,  Scott Eugene Conner ,  Philip-Arthur Hipskind ,  Allie Edward Tripp ,  Guoxin Zhu

IPC分类号： A61K31/41 ,  C07D257/04

CPC分类号： C07D409/12

摘要： The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

摘要翻译： 本发明公开了具有胰高血糖素受体拮抗剂或反向激动剂活性的式（I）的新化合物或其药学上可接受的盐，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式（I）化合物的药物组合物以及使用它们治疗糖尿病和其它与胰高血糖素相关的代谢紊乱等的方法。

公开(公告)号：US20100137417A1

公开(公告)日：2010-06-03

申请号：US11815987

申请日：2006-02-09

申请人： Mark Donald Chappell ,  Scott Eugene Conner ,  Allie Edward Tripp ,  Guoxin Zhu

发明人： Mark Donald Chappell ,  Scott Eugene Conner ,  Allie Edward Tripp ,  Guoxin Zhu

IPC分类号： A61K31/381 ,  C07D333/22 ,  C07D409/12 ,  A61P3/10

CPC分类号： C07D333/38 ,  C07D409/12

摘要： The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have glucagon receptor antagonist or inverse agonist activity, as well as methods of using these compounds and intermediates and methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising N compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

摘要翻译： 本发明公开了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）化合物或其药学上可接受的盐，以及使用这些化合物和中间体的方法以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式（I）的N种化合物的药物组合物以及使用它们治疗糖尿病和其它与胰高血糖素相关的代谢紊乱等的方法。

公开(公告)号：US20080300289A1

公开(公告)日：2008-12-04

申请号：US12094406

申请日：2006-11-21

申请人： Mark Donald Chappell ,  Scott Eugene Conner ,  Philip-Arthur Hipskind ,  Allie Edward Tripp ,  Guoxin Zhu

发明人： Mark Donald Chappell ,  Scott Eugene Conner ,  Philip-Arthur Hipskind ,  Allie Edward Tripp ,  Guoxin Zhu

IPC分类号： A61K31/41 ,  C07D257/04 ,  A61P3/10

CPC分类号： C07D409/12

摘要： The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

公开(公告)号：US20080146631A1

公开(公告)日：2008-06-19

申请号：US11972668

申请日：2008-01-11

申请人： Dawn Alisa Brooks ,  Scott Eugene Conner ,  Samuel James Dominianni ,  Alexander Glenn Godfrey ,  Lynn Stacy Gossett ,  Christopher John Rito ,  Allie Edward Tripp ,  Alan M. Warshawsky ,  Leonard Larry Winneroski ,  Guoxin Zhu

发明人： Dawn Alisa Brooks ,  Scott Eugene Conner ,  Samuel James Dominianni ,  Alexander Glenn Godfrey ,  Lynn Stacy Gossett ,  Christopher John Rito ,  Allie Edward Tripp ,  Alan M. Warshawsky ,  Leonard Larry Winneroski ,  Guoxin Zhu

IPC分类号： A61K31/421 ,  A61P3/06 ,  A61P3/10 ,  C07D263/32

CPC分类号： C07D413/12 ,  C07D263/32 ,  C07D413/04 ,  C07F5/025

摘要： Compounds represented by the following structural formula (I), and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein R1 is an unsubstituted or substituted aryl, heteroaryl, cycloalkyl, aryl-alkyl, heteroaryl-alkyl or cycloalkyl-alkyl, R2 is H, alkyl or haloalkyl, the polymethylene chain (II), is saturated or may contain a carbon-carbon double bond, while n is 2, 3, 4, W is O or S, Y is an unsubstituted or substituted phenylene, naphthylene or 1, 2, 3, 4 tetrahydronaphthylene, R3 is H, alkyl or haloalkyl, R4 is H, alkyl, haloalkyl or a substituted or unsubstituted benzyl, are useful for modulating a preoxisome proliferator activated receptor, particularly in the treatment of diabetes mellitus.

摘要翻译： 由以下结构式（I）表示的化合物及其药学上可接受的盐，溶剂合物和水合物，其中R1是未取代或取代的芳基，杂芳基，环烷基，芳基 - 烷基，杂芳基 - 烷基或环烷基 - 烷基，R2是H， 烷基或卤代烷基，多亚甲基链（II）饱和或可含有碳 - 碳双键，而n为2,3,4，W为O或S，Y为未取代或取代的亚苯基，亚萘基或亚乙基， 2,3,4四氢萘，R3为H，烷基或卤代烷基，R4为H，烷基，卤代烷基或取代或未取代的苄基，可用于调节预氧化物酶体增殖物激活受体，特别是治疗糖尿病。

公开(公告)号：US07351728B2

公开(公告)日：2008-04-01

申请号：US11181640

申请日：2005-07-14

申请人： Dawn Alisa Brooks ,  Scott Eugene Conner ,  Samuel James Dominianni ,  Alexander Glenn Godfrey ,  Lynn Stacy Gossett ,  Christopher John Rito ,  Allie Edward Tripp ,  Alan M. Warshawsky ,  Leonard Larry Winneroski, Jr. ,  Guoxin Zhu

发明人： Dawn Alisa Brooks ,  Scott Eugene Conner ,  Samuel James Dominianni ,  Alexander Glenn Godfrey ,  Lynn Stacy Gossett ,  Christopher John Rito ,  Allie Edward Tripp ,  Alan M. Warshawsky ,  Leonard Larry Winneroski, Jr. ,  Guoxin Zhu

IPC分类号： A61K31/421 ,  C07D263/32

CPC分类号： C07D413/12 ,  C07D263/32 ,  C07D413/04 ,  C07F5/025

摘要： Compounds represented by the following structural formula (I), and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein R1 is an unsubstituted or substituted aryl, heteroaryl, cycloalkyl, aryl-alkyl, heteroaryl-alkyl or cycloalkyl-alkyl, R2 is H, alkyl or haloalkyl, the polymethylene chain (II), is saturated or may contain a carbon-carbon double bond, while n is 2, 3, 4, W is O or S, Y is an unsubstituted phenylene, naphthylene or 1, 2, 3, 4 tetrahydronaphthylene, R3 is II, alkyl or haloalkyl, R4 is II, alkyl, haloalkyl or a substituted or unsubstituted benzyl, are useful for modulating a peroxisome proliferator activated receptor, particularly in the treatment of diabetes mellitus.

摘要翻译： 由以下结构式（I）表示的化合物及其药学上可接受的盐，溶剂合物和水合物，其中R1是未取代或取代的芳基，杂芳基，环烷基，芳基 - 烷基，杂芳基 - 烷基或环烷基 - 烷基，R2是H， 烷基或卤代烷基，多亚甲基链（II）是饱和的或可以含有碳 - 碳双键，而n为2,3,4，W为O或S，Y为未取代的亚苯基，亚萘基或1,2-亚乙基， 3,4四氢萘，R3为II，烷基或卤代烷基，R4为II，烷基，卤代烷基或取代或未取代的苄基，可用于调节过氧化物酶体增殖物激活受体，特别是治疗糖尿病。

公开(公告)号：US06982278B2

公开(公告)日：2006-01-03

申请号：US10343474

申请日：2001-08-23

申请人： Dawn Alisa Brooks ,  Scott Eugene Conner ,  Samuel James Dominianni ,  Alexander Glenn Godfrey ,  Lynn Stacy Gossett ,  Christopher John Rit ,  Allie Edward Tripp ,  Alan M. Warshawsky ,  Leonard Larry Winneroski, Jr. ,  Guoxin Zhu

发明人： Dawn Alisa Brooks ,  Scott Eugene Conner ,  Samuel James Dominianni ,  Alexander Glenn Godfrey ,  Lynn Stacy Gossett ,  Christopher John Rit ,  Allie Edward Tripp ,  Alan M. Warshawsky ,  Leonard Larry Winneroski, Jr. ,  Guoxin Zhu

IPC分类号： A61K31/421 ,  C07D263/30

CPC分类号： C07D413/12 ,  C07D263/32 ,  C07D413/04 ,  C07F5/025

摘要： Compounds represented by the following structural formula (I), and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein R1 is an unsubstituted or substituted aryl, heteroaryl, cycloalkyl, aryl-alkyl, heteroaryl-alkyl or cycloalkyl-alkyl, R2 is H, alkyl or haloalkyl, the polymethylene chain (II), is saturated or may contain a carbon-carbon double bond, while n is 2, 3, 4, W is O or S, Y is an unsubsituted or substituted phenylene, naphthylene or 1, 2, 3, 4 tetrahydronaphthylene, R3 is H, alkyl or haloalkyl. R4 is H, alkyl, haloalkyl or a substituted or unsubstituted benzyl, are useful for modulating a peroxisome proliferator activated receptor, particularly in the treatment of diabetes mellitus.

摘要翻译： 由以下结构式（I）表示的化合物及其药学上可接受的盐，溶剂合物和水合物，其中R1是未取代或取代的芳基，杂芳基，环烷基，芳基 - 烷基，杂芳基 - 烷基或环烷基 - 烷基，R2是H， 烷基或卤代烷基，多亚甲基链（II）是饱和的或可以含有碳 - 碳双键，而n为2,3,4，W为O或S，Y为未取代或取代的亚苯基，亚萘基或亚乙基， 2,3,4四氢萘，R3是H，烷基或卤代烷基。 R4是H，烷基，卤代烷基或取代或未取代的苄基，可用于调节过氧化物酶体增殖物激活受体，特别是用于治疗糖尿病。