公开(公告)号：US07220880B2

公开(公告)日：2007-05-22

申请号：US10517581

申请日：2003-06-11

Applicant: Rafael Ferritto Crespo ,  Jose Alfredo Martin ,  Maria Dolores Martin-Ortega Finger ,  Isabel Rojo Garcia ,  Quanrong Shen ,  Alan M Warshawsky ,  Yanping Xu

Inventor： Rafael Ferritto Crespo ,  Jose Alfredo Martin ,  Maria Dolores Martin-Ortega Finger ,  Isabel Rojo Garcia ,  Quanrong Shen ,  Alan M Warshawsky ,  Yanping Xu

IPC: C07C229/28 ,  A61K31/195

CPC classification number: C07C235/06 ,  C07C69/734 ,  C07C233/18 ,  C07C235/08 ,  C07C235/14 ,  C07C235/20 ,  C07C235/22 ,  C07C235/24 ,  C07C235/26 ,  C07C235/34 ,  C07C323/41 ,  C07C2601/04 ,  C07C2601/14 ,  C07D211/32 ,  C07D213/40 ,  C07D217/06 ,  C07D277/46 ,  C07D277/82 ,  C07D285/12 ,  C07D285/135 ,  C07D295/18 ,  C07D295/185 ,  C07D317/58 ,  C07D317/60 ,  C07D333/20

Abstract: The present invention is directed to compounds, compositions, and use of compounds the structural Formula (I)

Abstract translation: 本发明涉及化合物，组合物和化合物的用途，结构式（I）

公开(公告)号：US07176224B2

公开(公告)日：2007-02-13

申请号：US10343187

申请日：2001-08-23

Applicant: Robert J Ardecky ,  Dawn Alisa Brooks ,  Alexander Glenn Godfrey ,  Sarah Beth Jones ,  Nathan Bryan Mantlo ,  James Ray McCarthy ,  Pierre Yves Michellys ,  Christopher John Rito ,  John S Tyhonas ,  Leonard Larry Winneroski ,  Yanping Xu

Inventor： Robert J Ardecky ,  Dawn Alisa Brooks ,  Alexander Glenn Godfrey ,  Sarah Beth Jones ,  Nathan Bryan Mantlo ,  James Ray McCarthy ,  Pierre Yves Michellys ,  Christopher John Rito ,  John S Tyhonas ,  Leonard Larry Winneroski ,  Yanping Xu

IPC: C07D263/32 ,  A61K31/421

CPC classification number: C07D263/32 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14

Abstract: Novel compounds that are modulators of PPAR receptors, and pharmaceutically acceptable salts, solvates and hydrates thereof, processes for making the compounds, pharmaceutical compositions containing the compounds, or pharmaceutically acceptable salts, solvates and hydrates thereof

Abstract translation: 作为PPAR受体的调节剂的新型化合物及其药学上可接受的盐，溶剂合物和水合物，制备该化合物的方法，含该化合物的药物组合物或其药学上可接受的盐，溶剂化物和水合物

公开(公告)号：US06310058B1

公开(公告)日：2001-10-30

申请号：US09578973

申请日：2000-05-25

Applicant: Marvin J. Miller ,  Yanping Xu

Inventor： Marvin J. Miller ,  Yanping Xu

IPC: A61K3155

CPC classification number: C07D403/12 ,  C07D413/12

Abstract: Compounds represented by the formula [1] R1 is H or a substituent; R2 and R3 are C1-C3 alkyl; R4 is siderophore group e.g. CH3—(CH2)n—C(O)—N(OH)—(CH2)m— with n=10-22, m=2-6; X is O, S, or NH; X1 is O or NH; Y is H or alkyl; Z is H or substituted amino, e.g., t-BocNH or CbzNH, and r is 2-4; are useful in the method provided for treating tuberculosis. [1] is prepared by coupling [7], wherein HX1 is HO— or H2N—,  with [4] obtained as the free acid after saponification of the methyl ester.

Abstract translation: 由式[1] R 1表示的化合物是H或取代基; R2和R3是C1-C3烷基; R4是铁载体基团 CH 3 - （CH 2）n -C（O）-N（OH） - （CH 2）m - ，其中n = 10-22，m = 2-6; X是O，S或NH; X1是O或NH; Y是H或烷基; Z是H或取代的氨基，例如t-BocNH或CbzNH，r是2-4; 可用于治疗结核病的方法。 [1]通过偶联[7]制备，其中HX1是HO-或H2N-，其中[4]在甲酯皂化后作为游离酸获得。

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。