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。

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：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：US06930120B2

公开(公告)日：2005-08-16

申请号：US10343476

申请日：2001-08-23

申请人： Dawn Alisa Brooks ,  Alexander Glenn Godfrey ,  Sarah Beth Jones ,  James Ray McCarthy ,  Christopher John Rito ,  Leonard Larry Winneroski ,  Yanping Xu

发明人： Dawn Alisa Brooks ,  Alexander Glenn Godfrey ,  Sarah Beth Jones ,  James Ray McCarthy ,  Christopher John Rito ,  Leonard Larry Winneroski ,  Yanping Xu

IPC分类号： 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

CPC分类号： C07D413/04 ,  C07D263/32 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14

摘要： 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.

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：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：US07345070B2

公开(公告)日：2008-03-18

申请号：US11054226

申请日：2005-02-09

申请人： Dawn Alisa Brooks ,  Alexander Glenn Godfrey ,  Sarah Beth Jones ,  James Ray McCarthy ,  Christopher John Rito ,  Leonard Larry Winneroski ,  Yanping Xu

发明人： Dawn Alisa Brooks ,  Alexander Glenn Godfrey ,  Sarah Beth Jones ,  James Ray McCarthy ,  Christopher John Rito ,  Leonard Larry Winneroski ,  Yanping Xu

IPC分类号： A31K31/421 ,  C07D263/32

CPC分类号： C07D413/04 ,  C07D263/32 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14

摘要： 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.

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：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：US07176224B2

公开(公告)日：2007-02-13

申请号：US10343187

申请日：2001-08-23

申请人： 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

发明人： 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分类号： C07D263/32 ,  A61K31/421

CPC分类号： C07D263/32 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14

摘要： 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

摘要翻译： 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：US07309702B2

公开(公告)日：2007-12-18

申请号：US11225541

申请日：2005-09-13

申请人： Alexander Glenn Godfrey ,  Daniel Timothy Kohlman ,  John Cunningham O'Toole ,  Yao-Chang Xu ,  Tony Yantao Zhang ,  Jeffrey Forrester McKelvy

发明人： Alexander Glenn Godfrey ,  Daniel Timothy Kohlman ,  John Cunningham O'Toole ,  Yao-Chang Xu ,  Tony Yantao Zhang ,  Jeffrey Forrester McKelvy

IPC分类号： A61K31/497 ,  C07D241/04 ,  C07D401/04

CPC分类号： C07D295/088 ,  A61K31/495 ,  A61K31/496 ,  C07C45/004 ,  C07C45/29 ,  C07C45/40 ,  C07C45/515 ,  C07C45/59 ,  C07C45/68 ,  C07C49/563 ,  C07C49/577 ,  C07C49/583 ,  C07C49/86 ,  C07D213/74 ,  C07D295/104 ,  C07D295/108

摘要： A series of aryl piperazine compounds are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.

摘要翻译： 一系列芳基哌嗪化合物是用于治疗与5-羟色胺1 A受体相关或受其影响的病症的有效药物; 该化合物在该受体上是特别有效的拮抗剂，特别可用于缓解尼古丁和烟草戒断症状。

公开(公告)号：US07087626B2

公开(公告)日：2006-08-08

申请号：US10477111

申请日：2002-05-13

申请人： Douglas Wade Beight ,  Todd Vincent DeCollo ,  Alexander Glenn Godfrey ,  Theodore Goodson, Jr. ,  Hong-Yu Li ,  William Thomas McMillen ,  Shawn Christopher Miller ,  Jason Scott Sawyer ,  Edward C. R. Smith ,  Jonathan Michael Yingling

发明人： Douglas Wade Beight ,  Todd Vincent DeCollo ,  Alexander Glenn Godfrey ,  Theodore Goodson, Jr. ,  Hong-Yu Li ,  William Thomas McMillen ,  Shawn Christopher Miller ,  Jason Scott Sawyer ,  Edward C. R. Smith ,  Jonathan Michael Yingling

IPC分类号： A61K31/47 ,  C07D205/16 ,  C07D307/00 ,  C07D405/00

CPC分类号： C07D471/04 ,  C07D487/04

摘要： Novel pyrrazole derivative compounds and their use as pharmaceutical agents, in particular their use as TGF-beta signal transduction inhibitors. The disclosed invention relates to compounds of the structure (I) wherein (I) is a four, five, or six membered saturated ring and X is C, O or S

摘要翻译： 新型吡唑衍生物化合物及其作为药剂的用途，特别是其作为TGF-β信号转导抑制剂的用途。 所公开的发明涉及结构（I）的化合物，其中（I）是四，五或六元饱和环，X是C，O或S

公开(公告)号：US07405299B2

公开(公告)日：2008-07-29

申请号：US10535381

申请日：2003-11-24

申请人： Douglas Wade Beight ,  Timothy Paul Burkholder ,  Todd Vincent Decollo ,  Alexander Glenn Godfrey ,  Charles Raymond Heap ,  Chi-Hsin Richard King ,  Hong-Yu Li ,  William Thomas McMillen ,  Jason Scott Sawyer ,  Yan Wang ,  Clive Gideon Diefenbacher ,  Thomas Albert Engler ,  Sushant Malhotra ,  Sreenivasa Reedy Mundla

发明人： Douglas Wade Beight ,  Timothy Paul Burkholder ,  Todd Vincent Decollo ,  Alexander Glenn Godfrey ,  Charles Raymond Heap ,  Chi-Hsin Richard King ,  Hong-Yu Li ,  William Thomas McMillen ,  Jason Scott Sawyer ,  Yan Wang ,  Clive Gideon Diefenbacher ,  Thomas Albert Engler ,  Sushant Malhotra ,  Sreenivasa Reedy Mundla

IPC分类号： C07D241/36 ,  C07D217/00 ,  C07D401/00

CPC分类号： C07D487/04

摘要： The current invention relates to compounds of the formula: (Ia) and the pharmaceutically acceptable salts thereof and their use as TGF-beta signal transduction inhibitors for treating cancer and other diseases in a patient in need thereof by administration of said compounds.

摘要翻译： 本发明涉及式（Ia）化合物及其药学上可接受的盐及其作为TGF-β信号转导抑制剂的用途，其用于通过施用所述化合物治疗有需要的患者中的癌症和其它疾病。

公开(公告)号：US07001908B2

公开(公告)日：2006-02-21

申请号：US10419063

申请日：2003-04-16

申请人： Alexander Glenn Godfrey ,  Daniel Timothy Kohlman ,  John Cunningham O'Toole ,  Yao-Chang Xu ,  Tony Yantao Zhang

发明人： Alexander Glenn Godfrey ,  Daniel Timothy Kohlman ,  John Cunningham O'Toole ,  Yao-Chang Xu ,  Tony Yantao Zhang

IPC分类号： A61K31/497 ,  C07D401/00

CPC分类号： C07D295/088 ,  A61K31/495 ,  A61K31/496 ,  C07C45/004 ,  C07C45/29 ,  C07C45/40 ,  C07C45/515 ,  C07C45/59 ,  C07C45/68 ,  C07C49/563 ,  C07C49/577 ,  C07C49/583 ,  C07C49/86 ,  C07D213/74 ,  C07D295/104 ,  C07D295/108

摘要： A series of aryl piperazine compounds are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.