公开(公告)号：US08148534B2

公开(公告)日：2012-04-03

申请号：US12297910

申请日：2007-04-25

Applicant: Renhua Li ,  Owen Brendan Wallace ,  Yanping Xu

Inventor： Renhua Li ,  Owen Brendan Wallace ,  Yanping Xu

IPC: C07D405/00 ,  A61K31/445

CPC classification number: C07D401/14

Abstract: The present invention discloses novel compounds of Formula I: (I) possessing 11β-HSD type 1 antagonist 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 the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11β-HSD type 1 activity.

Abstract translation: 本发明公开了新颖的式I化合物：（I）具有11＆amp; -HSD 1型拮抗剂活性，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，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征，认知障碍以及与其相关的其它病症的方法。 -HSD类型1活动。

公开(公告)号：US20090239911A1

公开(公告)日：2009-09-24

申请号：US12297877

申请日：2007-04-24

Applicant: Owen Brendan Wallace ,  Yanping Xu ,  Nancy June Snyder ,  Jeremy Schulenburg York ,  Alexei Pavlovych Krasutsky

Inventor： Owen Brendan Wallace ,  Yanping Xu ,  Nancy June Snyder ,  Jeremy Schulenburg York ,  Alexei Pavlovych Krasutsky

IPC: A61K31/4439 ,  C07D207/12 ,  A61K31/40 ,  C07D231/10 ,  A61K31/415 ,  C07D401/02 ,  A61P3/10

CPC classification number: C07D207/26 ,  C07D401/10 ,  C07D403/10

Abstract: The present invention discloses novel compounds of Formula I: having 11β-HSD type 1 antagonist 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 the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.

Abstract translation: 本发明公开了具有11β-HSD 1型拮抗剂活性的式I化合物，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，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征和与11beta-HSD 1型相关的其它病症的方法 活动。

公开(公告)号：US20090156571A1

公开(公告)日：2009-06-18

申请号：US12297349

申请日：2007-04-19

Applicant: Thomas Daniel Aicher ,  Zhaogen Chen ,  Ronald Jay Hinklin ,  Gary Alan Hite ,  Alexei Pavlovych Krasutsky ,  Renhua Li ,  Jefferson Ray McCowan ,  Ashraf Saeed ,  Nancy June Snyder ,  James Lee Toth ,  Owen Brendan Wallace ,  Leonard Larry Winneroski, Jr. ,  Yanping Xu ,  Jeremy Schulenburg York

Inventor： Thomas Daniel Aicher ,  Zhaogen Chen ,  Ronald Jay Hinklin ,  Gary Alan Hite ,  Alexei Pavlovych Krasutsky ,  Renhua Li ,  Jefferson Ray McCowan ,  Ashraf Saeed ,  Nancy June Snyder ,  James Lee Toth ,  Owen Brendan Wallace ,  Leonard Larry Winneroski, Jr. ,  Yanping Xu ,  Jeremy Schulenburg York

IPC: A61K31/453 ,  C07D405/14 ,  C07D403/08 ,  C07D413/08 ,  C07D417/08 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/553

CPC classification number: C07D207/12 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D405/14 ,  C07D413/10 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D491/08 ,  C07D491/10

Abstract: The present invention discloses novel compounds of Formula I: possessing 11 β-HSD type 1 antagonist 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 the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11 β-HSD type 1 activity.

Abstract translation: 本发明公开了具有11个β-HSD 1型拮抗剂活性的新颖的式I化合物，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，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征，认知障碍和与11β相关的其它病症的方法 -HSD类型1活动。

公开(公告)号：US07045545B1

公开(公告)日：2006-05-16

申请号：US09890311

申请日：2000-01-19

Applicant: Karin Briner ,  Joseph Paul Burkhart ,  Timothy Paul Burkholder ,  Matthew Joseph Fisher ,  William Harlan Gritton ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Shawn Christopher Miller ,  Jeffrey Thomas Mullaney ,  Yao-Chang Xu ,  Yanping Xu

Inventor： Karin Briner ,  Joseph Paul Burkhart ,  Timothy Paul Burkholder ,  Matthew Joseph Fisher ,  William Harlan Gritton ,  Daniel Timothy Kohlman ,  Sidney Xi Liang ,  Shawn Christopher Miller ,  Jeffrey Thomas Mullaney ,  Yao-Chang Xu ,  Yanping Xu

IPC: A61K31/36

CPC classification number: C07D307/79 ,  C07D405/06

Abstract: The present invention provides serotonergic aminoalkylbenzofurans of Formula (I): where R, R1, R2, R3, R4, R4′, R5, R5′, and R12 are as described in the specification.

Abstract translation: 本发明提供式（I）的5-羟色胺氨基烷基苯并呋喃：其中R，R 1，R 2，R 3，R 4， R 4，R 4，R 5，R 5和R 12如上所述 在规范中。

公开(公告)号：US06881733B1

公开(公告)日：2005-04-19

申请号：US10031414

申请日：2000-07-21

Applicant: Karin Briner ,  Joseph Paul Burkhart ,  Timothy Paul Burkholder ,  Brian Eugene Cunningham ,  Matthew Joseph Fisher ,  William Harlan Gritton ,  Cynthia Darshini Jesudason ,  Shawn Christopher Miller ,  Jeffrey Thomas Mullaney ,  Matthew Robert Reinhard ,  Roger Ryan Rothhaar ,  Freddie Craig Stevens ,  Leonard Larry Winneroski ,  Yanping Xu ,  Yao-Chang Xu

Inventor： Karin Briner ,  Joseph Paul Burkhart ,  Timothy Paul Burkholder ,  Brian Eugene Cunningham ,  Matthew Joseph Fisher ,  William Harlan Gritton ,  Cynthia Darshini Jesudason ,  Shawn Christopher Miller ,  Jeffrey Thomas Mullaney ,  Matthew Robert Reinhard ,  Roger Ryan Rothhaar ,  Freddie Craig Stevens ,  Leonard Larry Winneroski ,  Yanping Xu ,  Yao-Chang Xu

IPC: A61K31/4025 ,  A61K31/4525 ,  A61K31/55 ,  A61P25/24 ,  C07D405/04 ,  C07D413/04

CPC classification number: C07D405/04

Abstract: The present invention provides serotonergic benzofurans of Formula (I): where A, R, R1, R2, R3, and R4 are as described in the specification.

Abstract translation: 本发明提供式（I）的5-羟色胺能的苯并呋喃：其中A，R，R 1，R 2，R 3和R 3， SUP> 4 如说明书中所述。

公开(公告)号：US08153807B2

公开(公告)日：2012-04-10

申请号：US12297873

申请日：2007-04-23

Applicant: Julie Kay Bush ,  Marvin Martin Hansen ,  Renhua Li ,  Thomas Edward Mabry ,  Nancy June Snyder ,  Owen Brendan Wallace ,  Yanping Xu

Inventor： Julie Kay Bush ,  Marvin Martin Hansen ,  Renhua Li ,  Thomas Edward Mabry ,  Nancy June Snyder ,  Owen Brendan Wallace ,  Yanping Xu

IPC: C07D405/00 ,  A61K31/535 ,  A61K31/445

CPC classification number: C07D207/50 ,  C07D207/26 ,  C07D401/04 ,  C07D401/14

Abstract: The present invention discloses novel compounds of Formula I: (I) having 11-HSD type 1 antagonist 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 the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11-HSD type 1 activity.

Abstract translation: 本发明公开了具有11-HSD 1型拮抗剂活性的式I的新化合物：（I），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，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征和与11-HSD 1型相关的其它病症的方法 活动。

公开(公告)号：US07820659B2

公开(公告)日：2010-10-26

申请号：US12297361

申请日：2007-04-19

Applicant: Ashraf Saeed ,  Owen Brendan Wallace ,  Yanping Xu ,  Thomas Edward Mabry ,  Rebecca Lynn Rezac Guenther ,  Nancy June Snyder

Inventor： Ashraf Saeed ,  Owen Brendan Wallace ,  Yanping Xu ,  Thomas Edward Mabry ,  Rebecca Lynn Rezac Guenther ,  Nancy June Snyder

IPC: A61K31/41 ,  A61K31/42 ,  A61K31/44 ,  A61K31/445 ,  A61K31/497 ,  A61K31/505 ,  A61K31/535 ,  C07D211/32 ,  C07D403/02 ,  C07D413/14

CPC classification number: C07D405/14 ,  C07D207/12 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D413/10 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D491/08 ,  C07D491/10

Abstract: The present invention discloses novel compounds of Formula I: (I) having 11β-HSD type 1 antagonist 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 the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.

Abstract translation: 本发明公开了具有11bb -HSD 1型拮抗剂活性的式I的新化合物：（I），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，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征以及与其相关的其它病症的方法。 1活动。

公开(公告)号：US20090088430A1

公开(公告)日：2009-04-02

申请号：US12297951

申请日：2007-04-27

Applicant: Owen Brendan Wallace ,  Yanping Xu ,  Jeremy Schulenburg York

Inventor： Owen Brendan Wallace ,  Yanping Xu ,  Jeremy Schulenburg York

IPC: A61K31/454 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  A61P3/10 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4545

CPC classification number: C07D401/04

Abstract: The present invention discloses novel compounds of Formula I: having 11β-HSD type 1 antagonist 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 the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.

Abstract translation: 本发明公开了具有11β-HSD 1型拮抗剂活性的式I化合物，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，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征和与11beta-HSD 1型相关的其它病症的方法 活动。

公开(公告)号：US20090088428A1

公开(公告)日：2009-04-02

申请号：US12297361

申请日：2007-04-19

Applicant: Ashraf Saeed ,  Owen Brendan Wallace ,  Yanping Xu ,  Thomas Edward Mabry ,  Rebecca Lynn Rezac Guenther ,  Nancy June Snyder

Inventor： Ashraf Saeed ,  Owen Brendan Wallace ,  Yanping Xu ,  Thomas Edward Mabry ,  Rebecca Lynn Rezac Guenther ,  Nancy June Snyder

IPC: A61K31/4184 ,  C07D403/02 ,  C07D405/14 ,  C07D413/14 ,  C07D401/14 ,  C07D403/14 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  A61K31/506 ,  A61K31/437 ,  A61P3/10

CPC classification number: C07D405/14 ,  C07D207/12 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D413/10 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D491/08 ,  C07D491/10

Abstract: The present invention discloses novel compounds of Formula I: (I) having 11β-HSD type 1 antagonist 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 the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.

Abstract translation: 本发明公开了具有11β-HSD 1型拮抗剂活性的式I的新化合物：（I），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，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征和与11beta-HSD 1型相关的其它病症的方法 活动。

公开(公告)号：US20090062358A1

公开(公告)日：2009-03-05

申请号：US11828446

申请日：2007-07-26

Applicant: Ivan Collado Cano ,  Samuel James Dominianni ,  Garret Jay Etgen, JR. ,  Cristina Garcia-Paredes ,  Richard Duane Johnston ,  Michael Edward Letourneau ,  Nathan Bryan Mantlo ,  Michael John Martinelli ,  Daniel Ray Mayhugh ,  Ashraf Saeed ,  Richard Craig Thompson ,  Xiaodong Wang ,  David Scott Coffey ,  Christopher Randall Schmid ,  Jeffrey Thomas Vicenzi ,  Yanping Xu

Inventor： Ivan Collado Cano ,  Samuel James Dominianni ,  Garret Jay Etgen, JR. ,  Cristina Garcia-Paredes ,  Richard Duane Johnston ,  Michael Edward Letourneau ,  Nathan Bryan Mantlo ,  Michael John Martinelli ,  Daniel Ray Mayhugh ,  Ashraf Saeed ,  Richard Craig Thompson ,  Xiaodong Wang ,  David Scott Coffey ,  Christopher Randall Schmid ,  Jeffrey Thomas Vicenzi ,  Yanping Xu

IPC: A61K31/4196 ,  C07D249/12 ,  C07D405/02

CPC classification number: C07C281/06 ,  C07C257/22 ,  C07C281/04 ,  C07D249/12 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06 ,  C07D417/12

Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C1-C5 alkyl, C1-C5 alkoxy, C3-C6 cycloalkyl, arylC0-C4alkyl and phenyl, or R3 and R4 are combined to form a C3-C4 cycloalkyl.

Abstract translation: 本发明涉及由以下结构式表示的化合物及其药学上可接受的盐，溶剂合物和水合物，R 1是选自C 1 -C 8烷基，芳基-C 0-2 - 烷基，杂芳基-C 0 - C 3 -C 6环烷基芳基-C 0-2 - 烷基或苯基。 W是O或S.R 2是H或选自C 1 -C 6烷基，C 3 -C 6环烷基和杂芳基的取代或未取代的基团。 X是C2-C5亚烷基连接体，连接体的一个碳原子可被O，NH或S取代.Y是C，O，S，NH或单键。 此外，E是（CH 2）n COOH，其中n是0,1,2或3或C（R3）（R4）A，其中A是酸性官能团如羧基，甲酰胺取代或未取代的磺酰胺，或取代或未取代的 未取代的四唑。 R3是H，饱和或不饱和的C1-C5烷基，C1-C5烷氧基。 另外，R 4为H，卤素，取代或未取代的选自C 1 -C 5烷基，C 1 -C 5烷氧基，C 3 -C 6环烷基，芳基C 0 -C 4烷基和苯基，或R 3和R 4的基团，形成C 3 -C 4环烷基。