公开(公告)号：EP1373240A2

公开(公告)日：2004-01-02

申请号：EP02728502.2

申请日：2002-03-14

申请人： ELI LILLY AND COMPANY ,  LIGAND PHARMACEUTICALS INCORPORATED

发明人： GARDINIER, Kevin, Matthew ,  GERNERT, Douglas, Linn ,  GRESE, Timothy, Alan ,  NEEL, David, Andrew ,  MAPES, Christopher, M. ,  MICHELLYS, Pierre-Yves ,  BOEHM, Marcus, F.

IPC分类号： C07D307/80

CPC分类号： C07D261/20 ,  C07D209/12 ,  C07D215/14 ,  C07D217/16 ,  C07D231/56 ,  C07D307/80 ,  C07D307/85 ,  C07D333/56 ,  C07D333/60 ,  C07D333/70 ,  C07D471/04 ,  C07D495/04

摘要： The present invention is directed to compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof: (I). The invention is also directed to pharmaceutical compositions, methods of use and methods of making compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof.

公开(公告)号：EP1368296A1

公开(公告)日：2003-12-10

申请号：EP02725147.9

申请日：2002-03-12

申请人： ELI LILLY AND COMPANY ,  LIGAND PHARMACEUTICALS INCORPORATED

发明人： BELL, Michael, Gregory ,  GRESE, Timothy, Alan ,  GERNERT, Doug, Linn ,  YUMIBE, Nathan, P. ,  BOEHM, Marcus, F. ,  MICHELLYS, Pierre-Yves ,  ARDECKY, Robert, J. ,  MAPES, Christopher, M. ,  CHEN, Jyun-Hung ,  TYHONAS, John, S.

IPC分类号： C07C59/64 ,  A61K31/192 ,  A61P3/00 ,  A61P17/00

CPC分类号： C07C59/64

摘要： The present invention relates to a method of modulating retinoid X receptor activity in a mammal, novel compounds and pharmaceutical compositions for modulating retinoid X receptor activity in a mammal, and methods of making compounds that modulate retinoid X receptor activity in a mammal. The compounds are represented by Structural Formula 1: The compounds of Structural Formual 1 are efficacious insulin sensitizers and do not have the undesirable side effects of increasing triglycerides or suppressing the thyroid hormone axis.

公开(公告)号：EP1373240B1

公开(公告)日：2005-06-15

申请号：EP02728502.2

申请日：2002-03-14

申请人： ELI LILLY AND COMPANY ,  LIGAND PHARMACEUTICALS INCORPORATED

发明人： GARDINIER, Kevin, Matthew ,  GERNERT, Douglas, Linn ,  GRESE, Timothy, Alan ,  NEEL, David, Andrew ,  MAPES, Christopher, M. ,  MICHELLYS, Pierre-Yves ,  BOEHM, Marcus, F.

IPC分类号： C07D307/80

CPC分类号： C07D261/20 ,  C07D209/12 ,  C07D215/14 ,  C07D217/16 ,  C07D231/56 ,  C07D307/80 ,  C07D307/85 ,  C07D333/56 ,  C07D333/60 ,  C07D333/70 ,  C07D471/04 ,  C07D495/04

摘要： The present invention is directed to compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof: (I). The invention is also directed to pharmaceutical compositions, methods of use and methods of making compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof.

公开(公告)号：EP1414450A1

公开(公告)日：2004-05-06

申请号：EP02750182.4

申请日：2002-07-18

申请人： ELI LILLY AND COMPANY ,  LIGAND PHARMACEUTICALS INCORPORATED

发明人： GRESE, Timothy, Alan ,  GARDINIER, Kevin, M. ,  BOEHM, Marcus, F.

IPC分类号： A61K31/44 ,  A61K31/513 ,  A61P3/10 ,  C07D213/65 ,  C07D239/34

CPC分类号： C07D213/65

摘要： The present invention relates to a method of modulating retinoid X receptor activity in a mammal, novel compounds and pharmaceutical compositions for modulating retinoid X receptor activity in a mammal, and methods of making compounds that modulate retinoid X receptor activity in a mammal. The compounds are represented by Structural Formula I: The compounds of Structural Formula I are efficacious insulin sensitizers and do not have the undesirable side effects of increasing triglycerides or suppressing the thyroid hormone axis.

公开(公告)号：EP1487792A1

公开(公告)日：2004-12-22

申请号：EP03723665.0

申请日：2003-03-11

申请人： ELI LILLY AND COMPANY

发明人： GRESE, Timothy, Alan ,  JADHAV, Prabhakar, Kondaji ,  NEEL, David, Andrew ,  STEINBERG, Mitchell, Irvin ,  LANDER, Peter, Ambrose

IPC分类号： C07D209/34 ,  A61K31/404 ,  A61P7/10 ,  A61P9/12

CPC分类号： C07D401/04 ,  C07D209/34 ,  C07D401/06 ,  C07D403/04 ,  C07D413/06 ,  C07D417/06

摘要： he present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation, particularly congestive heart failure, comprising administering to a patient in need thereof an effective amount of a compound of the formula: I or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula I, including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula I.

公开(公告)号：EP1597254A1

公开(公告)日：2005-11-23

申请号：EP04703558.9

申请日：2004-01-20

申请人： ELI LILLY AND COMPANY

发明人： BELL, Michael, Gregory ,  GAVARDINAS, Konstantinos ,  GERNERT, Douglas, Linn ,  GRESE, Timothy, Alan ,  JADHAV, Prabhakar, Kondaji ,  LANDER, Peter, Ambrose ,  STEINBERG, Mitchell, Irvin

IPC分类号： C07D409/06 ,  C07D209/10 ,  C07D407/06 ,  C07D209/08 ,  A61K31/404

CPC分类号： C07D401/06 ,  C07D209/08 ,  C07D209/10 ,  C07D333/56 ,  C07D333/68 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D491/04 ,  C07F5/003 ,  C07F5/069 ,  C07F7/0836

摘要： The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient, and methods for treating physiological disorders, particularly congestive heart disease, comprising administering to a patient in thereof an effective amount of a compound of Formula I.

公开(公告)号：EP1519915A2

公开(公告)日：2005-04-06

申请号：EP03810038.4

申请日：2003-06-13

申请人： ELI LILLY AND COMPANY

发明人： COGHLAN, Michael, Joseph ,  GREEN, Jonathan, Edward ,  GRESE, Timothy, Alan ,  JADHAV, Prabhakar, Kondaji ,  MATTHEWS, Donald, Paul ,  STEINBERG, Mitchell, Irvin ,  FALES, Kevin, Robert ,  BELL, Michael, Gregory

IPC分类号： C07C311/08 ,  C07D221/16 ,  C07D235/14 ,  C07D313/12 ,  C07D401/06 ,  C07D403/06 ,  A61K31/18 ,  A61K31/553 ,  A61P7/10 ,  A61P9/12

CPC分类号： C07D213/16 ,  C07C22/04 ,  C07C22/08 ,  C07C25/24 ,  C07C33/38 ,  C07C39/17 ,  C07C39/23 ,  C07C39/42 ,  C07C43/215 ,  C07C43/225 ,  C07C43/23 ,  C07C47/548 ,  C07C47/57 ,  C07C49/835 ,  C07C69/00 ,  C07C69/618 ,  C07C69/65 ,  C07C205/06 ,  C07C205/34 ,  C07C205/35 ,  C07C211/28 ,  C07C211/32 ,  C07C211/45 ,  C07C215/76 ,  C07C217/84 ,  C07C233/07 ,  C07C233/65 ,  C07C233/84 ,  C07C235/16 ,  C07C251/40 ,  C07C251/48 ,  C07C255/50 ,  C07C261/04 ,  C07C271/14 ,  C07C275/28 ,  C07C307/10 ,  C07C311/03 ,  C07C311/08 ,  C07C311/09 ,  C07C311/16 ,  C07C311/20 ,  C07C311/21 ,  C07C311/29 ,  C07C317/14 ,  C07C317/32 ,  C07C321/28 ,  C07C323/49 ,  C07C2601/02 ,  C07C2603/32 ,  C07C2603/40 ,  C07C2603/78 ,  C07C2603/86 ,  C07D209/08 ,  C07D209/34 ,  C07D211/96 ,  C07D213/06 ,  C07D213/73 ,  C07D213/76 ,  C07D213/81 ,  C07D221/16 ,  C07D223/20 ,  C07D231/12 ,  C07D231/18 ,  C07D233/26 ,  C07D233/68 ,  C07D233/84 ,  C07D235/26 ,  C07D241/12 ,  C07D241/20 ,  C07D261/08 ,  C07D261/10 ,  C07D263/52 ,  C07D263/56 ,  C07D263/58 ,  C07D277/60 ,  C07D295/088 ,  C07D295/26 ,  C07D313/12 ,  C07D333/78 ,  C07D333/80 ,  C07D337/12 ,  C07D401/06 ,  C07D405/06 ,  C07D409/04 ,  C07D471/04 ,  C07D471/06 ,  C07D487/04 ,  C07D491/044

摘要： The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation comprising administering to a patient in need thereof an effective amount of a compound of the formula (I): or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula (I), including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula (I).

公开(公告)号：EP1519915B1

公开(公告)日：2009-05-27

申请号：EP03810038.4

申请日：2003-06-13

申请人： ELI LILLY AND COMPANY

发明人： COGHLAN, Michael, Joseph ,  GREEN, Jonathan, Edward ,  GRESE, Timothy, Alan ,  JADHAV, Prabhakar, Kondaji ,  MATTHEWS, Donald, Paul ,  STEINBERG, Mitchell, Irvin ,  FALES, Kevin, Robert ,  BELL, Michael, Gregory

IPC分类号： C07C311/08 ,  C07D221/16 ,  C07D235/14 ,  C07D313/12 ,  C07D401/06 ,  C07D403/06 ,  A61K31/18 ,  A61K31/553 ,  A61P7/10 ,  A61P9/12

CPC分类号： C07D213/16 ,  C07C22/04 ,  C07C22/08 ,  C07C25/24 ,  C07C33/38 ,  C07C39/17 ,  C07C39/23 ,  C07C39/42 ,  C07C43/215 ,  C07C43/225 ,  C07C43/23 ,  C07C47/548 ,  C07C47/57 ,  C07C49/835 ,  C07C69/00 ,  C07C69/618 ,  C07C69/65 ,  C07C205/06 ,  C07C205/34 ,  C07C205/35 ,  C07C211/28 ,  C07C211/32 ,  C07C211/45 ,  C07C215/76 ,  C07C217/84 ,  C07C233/07 ,  C07C233/65 ,  C07C233/84 ,  C07C235/16 ,  C07C251/40 ,  C07C251/48 ,  C07C255/50 ,  C07C261/04 ,  C07C271/14 ,  C07C275/28 ,  C07C307/10 ,  C07C311/03 ,  C07C311/08 ,  C07C311/09 ,  C07C311/16 ,  C07C311/20 ,  C07C311/21 ,  C07C311/29 ,  C07C317/14 ,  C07C317/32 ,  C07C321/28 ,  C07C323/49 ,  C07C2601/02 ,  C07C2603/32 ,  C07C2603/40 ,  C07C2603/78 ,  C07C2603/86 ,  C07D209/08 ,  C07D209/34 ,  C07D211/96 ,  C07D213/06 ,  C07D213/73 ,  C07D213/76 ,  C07D213/81 ,  C07D221/16 ,  C07D223/20 ,  C07D231/12 ,  C07D231/18 ,  C07D233/26 ,  C07D233/68 ,  C07D233/84 ,  C07D235/26 ,  C07D241/12 ,  C07D241/20 ,  C07D261/08 ,  C07D261/10 ,  C07D263/52 ,  C07D263/56 ,  C07D263/58 ,  C07D277/60 ,  C07D295/088 ,  C07D295/26 ,  C07D313/12 ,  C07D333/78 ,  C07D333/80 ,  C07D337/12 ,  C07D401/06 ,  C07D405/06 ,  C07D409/04 ,  C07D471/04 ,  C07D471/06 ,  C07D487/04 ,  C07D491/044

摘要： The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation comprising administering to a patient in need thereof an effective amount of a compound of the formula (I): or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula (I), including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula (I).

摘要翻译： 本发明涉及治疗对类固醇激素核受体调节敏感的病理学障碍的方法，其包括向有需要的患者施用有效量的下式化合物或其药学上可接受的盐。 此外，本发明提供了新颖的式I的药物化合物，包括其药学上可接受的盐，以及包含作为活性成分的式I化合物的药物组合物。

公开(公告)号：EP0796095A1

公开(公告)日：1997-09-24

申请号：EP95943965.0

申请日：1995-12-22

申请人： ELI LILLY AND COMPANY

发明人： GRESE, Timothy, Alan

IPC分类号： C07D333 ,  A61K31 ,  A61P5

CPC分类号： A61K31/4535 ,  A61K31/4025 ,  A61K31/55

摘要： A method of inhibiting effects of growth hormone comprising administering to a human in need thereof an effective amount of a compound having formula (I), wherein R?1 and R3¿ are independently hydrogen, -CH¿3?, (a), or (b), wherein Ar is optionally substituted phenyl; R?2¿ is selected from the group consisting of pyrrolidine, hexamethyleneimino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.