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。

公开(公告)号：US20060257987A1

公开(公告)日：2006-11-16

申请号：US10566291

申请日：2004-08-17

Applicant: Isabel Cristina Gonzalez Valcarcel ,  Nathan Mantlo ,  Qing Shi ,  Minmin Wang ,  Leonard Winneroski ,  Yanping Xu ,  Jeremy York

Inventor： Isabel Cristina Gonzalez Valcarcel ,  Nathan Mantlo ,  Qing Shi ,  Minmin Wang ,  Leonard Winneroski ,  Yanping Xu ,  Jeremy York

IPC: C12N9/96

CPC classification number: C07D213/30 ,  A61K31/095 ,  A61K31/185 ,  A61K45/06 ,  C07B2200/07 ,  C07C59/68 ,  C07C59/72 ,  C07C59/86 ,  C07C59/88 ,  C07C59/90 ,  C07C61/39 ,  C07C62/34 ,  C07C251/48 ,  C07C317/22 ,  C07C323/20 ,  C07C323/52 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/69 ,  C07D239/26 ,  C07D261/20 ,  C07D263/32 ,  C07D277/24 ,  C07D307/79 ,  A61K2300/00

Abstract: The present invention is directed to a compound of formula I, or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.

Abstract translation: 本发明涉及式I化合物或其药学上可接受的盐，溶剂合物，水合物或立体异构体，其可用于治疗或预防由过氧化物酶体增殖物激活受体（PPAR）介导的病症，例如综合征X，II型 糖尿病，高血糖症，高脂血症，肥胖症，凝血病，高血压，动脉硬化以及与X综合症和心血管疾病相关的其它疾病。

公开(公告)号：US20060217433A1

公开(公告)日：2006-09-28

申请号：US10542579

申请日：2004-02-10

Applicant: Scott Conner ,  Lynn Gosset ,  Jonathan Green ,  Winton Jones ,  Nathan Mantlo ,  Donald Matthews ,  Daniel Mayhugh ,  Daryl Smith ,  Jennifer Vance ,  Xiaodong Wang ,  Alan Warshawsky ,  Leonard Winneroski ,  Yanping Xu ,  Guoxin Zhu

Inventor： Scott Conner ,  Lynn Gosset ,  Jonathan Green ,  Winton Jones ,  Nathan Mantlo ,  Donald Matthews ,  Daniel Mayhugh ,  Daryl Smith ,  Jennifer Vance ,  Xiaodong Wang ,  Alan Warshawsky ,  Leonard Winneroski ,  Yanping Xu ,  Guoxin Zhu

IPC: A61K31/404 ,  A61K31/381 ,  A61K31/343 ,  A61K31/195 ,  C07D333/64

CPC classification number: C07D207/08 ,  A61K31/00 ,  A61K45/06 ,  C07C311/13 ,  C07C311/17 ,  C07C311/19 ,  C07C311/29 ,  C07C317/14 ,  C07C323/49 ,  C07C323/52 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/08 ,  C07D209/48 ,  C07D213/64 ,  C07D213/71 ,  C07D213/74 ,  C07D215/36 ,  C07D231/12 ,  C07D231/18 ,  C07D263/32 ,  C07D271/12 ,  C07D277/36 ,  C07D307/79 ,  C07D307/82 ,  C07D319/18 ,  C07D333/34 ,  C07D333/62 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04 ,  A61K2300/00

Abstract: The present invention is directed to a compound of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates or stereoisomers thereof, which are useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.

Abstract translation: 本发明涉及式（I）化合物及其药学上可接受的盐，溶剂合物，水合物或立体异构体，其可用于治疗或预防由过氧化物酶体增殖物激活受体（PPAR）介导的病症，例如综合征X型 II型糖尿病，高血糖症，高脂血症，肥胖症，凝血病，高血压，动脉硬化以及与X综合症和心血管疾病有关的其他疾病。

公开(公告)号：US20050245584A1

公开(公告)日：2005-11-03

申请号：US11054226

申请日：2005-02-09

Applicant: Dawn Brooks ,  Alexander Godfrey ,  Sarah Jones ,  James McCarthy ,  Christopher Rito ,  Leonard Winneroski ,  Yanping Xu

Inventor： Dawn Brooks ,  Alexander Godfrey ,  Sarah Jones ,  James McCarthy ,  Christopher Rito ,  Leonard Winneroski ,  Yanping Xu

IPC: A61K31/421 ,  A61K31/422 ,  A61K31/4709 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P7/04 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D263/32 ,  C07D413/04 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D263/30 ,  C07D49/02

CPC classification number: C07D413/04 ,  C07D263/32 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14

Abstract: Compounds represented by the following structural formula (I), and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein: n is 2, 3, or 4 and W is CH2, CH(OH), C(O) or O; R1 is an unsubstituted or substituted aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aryl-alkyl, heteroaryl-alkyl, cycloalkyl-alkyl, or t-butyl; R2 is H, alkyl, haloalkyl or phenyl; Y is an unsubstituted or substituted thiophen-2,5-diyl or phenylene; R3 is alkyl or haloalkyl; R4 is a substituted or unsubstituted phenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, quinolyl, pyridyl or benzo[1,3]dioxol-5-yl group; and R5 is H, alkyl, or aminoalkyl; are useful for modulating a peroxisome proliferator activated receptor, particularly in the treatment of diabetes mellitus.

Abstract translation: 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：n为2,3或4，W为CH 2，CH（OH），C （O）或O; R 1是未取代或取代的芳基，杂芳基，环烷基，杂环烷基，芳基 - 烷基，杂芳基 - 烷基，环烷基 - 烷基或叔丁基; R2是H，烷基，卤代烷基或苯基; Y是未取代或取代的噻吩-2,5-二基或亚苯基; R3是烷基或卤代烷基; R4是取代或未取代的苯基，萘基，1,2,3,4-四氢萘基，喹啉基，吡啶基或苯并[1,3]二氧杂环戊烯-5-基; 并且R 5是H，烷基或氨基烷基; 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。

公开(公告)号：US20130004477A1

公开(公告)日：2013-01-03

申请号：US13504286

申请日：2010-10-22

Applicant: Zhe Lu ,  Yanping Xu

Inventor： Zhe Lu ,  Yanping Xu

IPC: A61K31/26 ,  A61K38/44 ,  A61P29/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P1/18 ,  A61K33/18 ,  A61P11/08

CPC classification number: G01N33/84 ,  A23L33/10 ,  A61K8/23 ,  A61K31/26 ,  A61K31/275 ,  A61K38/44 ,  A61Q5/10 ,  A61Q19/08 ,  C12Y111/01007 ,  G01N2800/382 ,  A61K2300/00

Abstract: This invention provides compositions and methods for treating inflammation related diseases. Particularly, the present invention provides methods and compositions of administering thiocyanate to treat inflammation related diseases, such as cystic fibrosis, lung disease, lung cancer, asthma, bronchitis, pancreatic disease, digestive track disease, diabetes, neurological disorder, cardio-vascular disease, atherosclerosis, arthritis, nephritis, or stroke, and neurological disorders such as Alzheimer's disease, Parkinson's disease, multiple sclerosis, or autism. The invention provides the use of thiocyanate to diagnose inflammation related diseases.

Abstract translation: 本发明提供了治疗炎症相关疾病的组合物和方法。 特别地，本发明提供了硫氰酸盐治疗炎症相关疾病如囊性纤维化，肺部疾病，肺癌，哮喘，支气管炎，胰腺疾病，消化道疾病，糖尿病，神经障碍，心血管疾病， 动脉粥样硬化，关节炎，肾炎或中风，以及诸如阿尔茨海默病，帕金森病，多发性硬化或自闭症的神经障碍。 本发明提供了硫氰酸盐诊断炎症相关疾病的用途。

公开(公告)号：US07998999B2

公开(公告)日：2011-08-16

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: A61K31/4015 ,  C07D207/26

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11＆amp; b -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，代谢综合征以及与其相关的其它病症的方法。 1活动。

公开(公告)号：US07994176B2

公开(公告)日：2011-08-09

申请号：US12297964

申请日：2007-04-24

Applicant: Renhua Li ,  Thomas Edward Mabry ,  Owen Brendan Wallace ,  Leonard Larry Winneroski, Jr. ,  Yanping Xu

Inventor： Renhua Li ,  Thomas Edward Mabry ,  Owen Brendan Wallace ,  Leonard Larry Winneroski, Jr. ,  Yanping Xu

IPC: A61K31/496 ,  A61K31/454 ,  C07D403/02 ,  C07D401/14 ,  C07D401/04 ,  C07D207/26

CPC classification number: C07D207/26 ,  C07D207/27 ,  C07D401/02 ,  C07D401/10 ,  C07D401/14

Abstract: The present invention discloses novel compounds of Formula I: having 11 Beta-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 Beta-HSD type 1 activity. X-17377

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，代谢综合征以及与11β-HSD型相关的其它病症的方法 1活动。 X-17377

公开(公告)号：US07981918B2

公开(公告)日：2011-07-19

申请号：US12297375

申请日：2007-04-05

Applicant: Thomas Daniel Aicher ,  Peter Biagio Anzeveno ,  Renhua Li ,  Alexei Pavlovych Krasutsky ,  Thomas Edward Mabry ,  Ashraf Saeed ,  Nancy June Snyder ,  Hongqi Tian ,  Owen Brendan Wallace ,  Leonard Larry Winneroski ,  Yanping Xu

Inventor： Thomas Daniel Aicher ,  Peter Biagio Anzeveno ,  Renhua Li ,  Alexei Pavlovych Krasutsky ,  Thomas Edward Mabry ,  Ashraf Saeed ,  Nancy June Snyder ,  Hongqi Tian ,  Owen Brendan Wallace ,  Leonard Larry Winneroski ,  Yanping Xu

IPC: A61K31/416 ,  C07D231/56

CPC classification number: C07D403/04

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11＆amp; b -HSD 1拮抗剂活性的式（I）的新化合物，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，代谢综合征以及与其相关的其它病症的方法。 HSD 1型活动。