公开(公告)号：EP1817300B1

公开(公告)日：2010-03-17

申请号：EP05823343.8

申请日：2005-11-15

申请人： ELI LILLY AND COMPANY

发明人： AICHER, Thomas, Daniel ,  BENESH, Dana, Rae ,  BLANCO-PILLADO, Maria-Jesus ,  CORTEZ, Guillermo, S. ,  GROENDYKE, Todd, Michael ,  KHILEVICH, Albert ,  KNOBELSDORF, James, Allen ,  MARMSATER, Fredrik, Pehr ,  SCHKERYANTZ, Jeffrey, Michael ,  TANG, Tony, Pisal

IPC分类号： C07D401/04 ,  C07D257/04 ,  C07D213/79 ,  C07D213/70 ,  A61K31/4427 ,  A61P25/00 ,  A61P37/08

CPC分类号： C07C229/60 ,  C07C317/44 ,  C07D213/61 ,  C07D213/64 ,  C07D213/65 ,  C07D213/70 ,  C07D213/79 ,  C07D213/80 ,  C07D213/84 ,  C07D213/85 ,  C07D257/04 ,  C07D401/04 ,  C07D401/12

摘要： The present invention provides compounds of formula (I); pharmaceutical compositions thereof, and methods of using the same, processes or preparing the same, and intermediates thereof.

公开(公告)号：EP1817300A1

公开(公告)日：2007-08-15

申请号：EP05823343.8

申请日：2005-11-15

申请人： ELI LILLY AND COMPANY

发明人： AICHER, Thomas, Daniel ,  BENESH, Dana, Rae ,  BLANCO-PILLADO, Maria-Jesus ,  CORTEZ, Guillermo, S. ,  GROENDYKE, Todd, Michael ,  KHILEVICH, Albert ,  KNOBELSDORF, James, Allen ,  MARMSATER, Fredrik, Pehr ,  SCHKERYANTZ, Jeffrey, Michael ,  TANG, Tony, Pisal

IPC分类号： C07D401/04 ,  C07D257/04 ,  C07D213/79 ,  C07D213/70 ,  A61K31/4427 ,  A61P25/00 ,  A61P37/08

CPC分类号： C07C229/60 ,  C07C317/44 ,  C07D213/61 ,  C07D213/64 ,  C07D213/65 ,  C07D213/70 ,  C07D213/79 ,  C07D213/80 ,  C07D213/84 ,  C07D213/85 ,  C07D257/04 ,  C07D401/04 ,  C07D401/12

摘要： The present invention provides compounds of formula (I); pharmaceutical compositions thereof, and methods of using the same, processes or preparing the same, and intermediates thereof.

摘要翻译： 本发明提供了式（I）的化合物; 其药物组合物及其使用方法，其制备方法或制备方法及其中间体。

公开(公告)号：EP1585733A1

公开(公告)日：2005-10-19

申请号：EP03815195.7

申请日：2003-12-31

申请人： ELI LILLY AND COMPANY

发明人： CONNER, Scott, Eugene ,  MA, Tianwei ,  MANTLO, Nathan, Bryan ,  MAYHUGH, Daniel, Ray ,  SCHKERYANTZ, Jeffrey, Michael ,  WARSHAWSKY, Alan, M. ,  ZHU, Guoxin

IPC分类号： C07D231/12 ,  C07D253/04 ,  A61K31/415 ,  A61P9/00 ,  A61P3/00 ,  C07D261/08 ,  C07D233/20 ,  C07D233/22

CPC分类号： C07D231/12 ,  C07D233/20 ,  C07D233/22 ,  C07D233/64 ,  C07D249/06 ,  C07D253/04 ,  C07D261/08

摘要： The present invention is directed to compounds represented by the following structural formula, Formula I: wherein: (a) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (b) U is an aliphatic linker; (c) Y is selected from the group consisting of O, C, S, NH and a single bond; (d) E is C(R3)(R4)A or A and wherein (i) A is selected from the group consisting of carboxyl, tetrazole, C1-C6 alkylnitrile, carboxamide, sulfonamide and acylsulfonamide; (e) Z1 and Z2 are each independently selected from the group consisting of N, O, and C with the proviso that at least one of Z1 and Z2 is N; (f) Z3 is selected from the group consisting of N, O, and C. (g) R8 is selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C4 alkylenyl and halo; (h) R9 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkylenyl, halo, aryl- C0-C4 alkyl, heteroaryl, C1-C6 allyl, and OR29.

公开(公告)号：EP1581521A1

公开(公告)日：2005-10-05

申请号：EP03808624.5

申请日：2003-12-31

申请人： ELI LILLY AND COMPANY

发明人： CONNER, Scott, Eugene ,  KNOBELSDORF, James, Allen ,  MANTLO, Nathan, Bryan ,  MAYHUGH, Daniel, Ray ,  WANG, Xiaodong ,  ZHU, Guoxin ,  SCHKERYANTZ, Jeffrey, Michael

IPC分类号： C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/4155 ,  A61K31/423 ,  A61K31/427 ,  A61K31/428 ,  A61K31/437 ,  A61K31/55 ,  A61P3/10 ,  A61P29/00

CPC分类号： C07D263/57 ,  C07D209/10 ,  C07D235/18 ,  C07D277/60 ,  C07D277/66 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

摘要： The present invention is directed to a method of treatment by modulating a peroxisome proliferator activated receptor by employing a compound of Structural Formula (I). The variables in I are defined herein. Also included are compounds, methods of making compounds, and pharmaceutical compositions. The compounds of the present invention are believed to be effective in treating and preventing Syndrome X, Type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, atherosclerosis, and other disorders related to Syndrome X and cardiovascular diseases.

公开(公告)号：EP1480640A1

公开(公告)日：2004-12-01

申请号：EP03713316.2

申请日：2003-02-13

申请人： ELI LILLY AND COMPANY

发明人： CONNER, Scott, Eugene ,  KNOBELSDORF, James, Allen ,  MANTLO, Nathan, Bryan ,  SCHKERYANTZ, Jeffrey, Michael ,  SHEN, Quanrong ,  WARSHAWSKY, Alan, M. ,  ZHU, Guoxin

IPC分类号： A61K31/421 ,  A61K31/426 ,  A61K31/429 ,  A61K31/506 ,  C07D277/30 ,  C07D277/26 ,  C07D277/28 ,  C07D277/24 ,  C07D263/32 ,  C07D513/04 ,  C07D413/12 ,  C07D413/10 ,  C07D417/04 ,  C07D417/10 ,  C07D413/04

CPC分类号： C07D263/32 ,  C07D277/24 ,  C07D277/26 ,  C07D277/28 ,  C07D277/30 ,  C07D403/10 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14

摘要： The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I: (Formula I); wherein: (a) R5 is selected from the group consisting of (C1-C6) alkyl, (C1-C6) alkenyl, aryl (C0-C4) alkyl, aryloxy (C0-C4) alkyl, arylthio (C0-C4) alkyl, and further wherein when R5 is alkyl, R5 can optionally combine with W to form a 6 membered cycloheteroalkyl ring that is fused with the oxazole or thiazole ring to which the R5 group is attached; (b) R9 is selected from the group consisting of C1-C5 alkyl, C1-C5 alkenyl, and arylC0-C3alkyl; (c) T1 is selected from the group consisting of C and N; (d) W is selected from the group consisting of CH2, C(O)N(R21), N(R21), N(R21)CH2, O, OCH2, S, and SO2; and(e) X is selected from the group consisting of C, CH2C, and CCH2.

摘要翻译： 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，式I：（式I）; 其中：（a）R 5选自（C 1 -C 6）烷基，（C 1 -C 6）烯基，芳基（C 0 -C 4）烷基，芳氧基（C 0 -C 4）烷基，芳硫基（C 0 -C 4）烷基 并且其中当R 5为烷基时，R 5可以任选地与W结合以形成与R5基团所连接的恶唑或噻唑环稠合的6元环杂烷基环; （b）R 9选自C 1 -C 5烷基，C 1 -C 5链烯基和芳基C 0 -C 3烷基; （c）T1选自C和N; （d）W选自CH 2，C（O）N（R 21），N（R 21），N（R 21）CH 2，O，OCH 2，S和SO 2; 和（e）X选自C，CH 2 C和CCH 2。

公开(公告)号：EP2318375A1

公开(公告)日：2011-05-11

申请号：EP09790351.2

申请日：2009-07-14

申请人： ELI LILLY AND COMPANY

发明人： KHILEVICH, Albert ,  LIU, Bin ,  MAYHUGH, Daniel, Ray ,  SCHKERYANTZ, Jeffrey, Michael ,  ZHANG, Deyi

IPC分类号： C07D233/92 ,  A61K31/4164 ,  A61P25/00

CPC分类号： C07D233/92

摘要： The present invention provides certain imidazole carboxamide derivatives, pharmaceutical compositions thereof, methods of using the same for preparing a medicament useful in the treatment of conditions associated with the mGluR
2 receptor, such as depression and anxiety, and processes of the following Formula (I) for preparing the same.

摘要翻译： 本发明提供某些咪唑甲酰胺衍生物，其药物组合物，其用于制备可用于治疗与mGluR 2受体相关的病症（例如抑郁和焦虑）的药物的方法，以及下式（I）的方法： 为了准备它。

公开(公告)号：EP1817296A1

公开(公告)日：2007-08-15

申请号：EP05824423.7

申请日：2005-11-15

申请人： ELI LILLY AND COMPANY

发明人： AICHER, Thomas, Daniel ,  CORTEZ, Guillermo, S. ,  GROENDYKE, Todd, Michael ,  KHILEVICH, Albert ,  KNOBELSDORF, James, Allen ,  MARMSATER, Fredrik, Pehr ,  SCHKERYANTZ, Jeffrey, Michael ,  TANG, Tony, Pisal

IPC分类号： C07D257/04 ,  A61K31/4427 ,  A61P25/00 ,  A61P37/08 ,  C07C235/18

CPC分类号： C07C229/60 ,  C07C317/44 ,  C07D213/61 ,  C07D213/64 ,  C07D213/65 ,  C07D213/70 ,  C07D213/79 ,  C07D213/80 ,  C07D213/84 ,  C07D213/85 ,  C07D257/04 ,  C07D401/04 ,  C07D401/12

摘要： The present invention provides a compound of formula (I): pharmaceutical compositions thereof, and methods of using the same, processes for preparing the same, and intermediates thereof.

公开(公告)号：EP1581491A1

公开(公告)日：2005-10-05

申请号：EP03800390.1

申请日：2003-12-31

申请人： ELI LILLY AND COMPANY ,  LIGAND PHARMACEUTICALS INCORPORATED

发明人： CONNER, Scott, Eugene ,  KNOBELSDORF, James, Allen ,  MANTLO, Nathan, Bryan ,  MAYHUGH, Daniel, Ray ,  WANG, Xiaodong ,  ZHU, Guoxin ,  SCHKERYANTZ, Jeffrey, Michael ,  MICHELLYS, Pierre-Yves

IPC分类号： C07D209/08 ,  C07D209/42 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  A61K31/404 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/4409 ,  A61K31/5377 ,  A61P3/10 ,  A61P29/00

CPC分类号： C07D263/57 ,  C07D209/10 ,  C07D235/18 ,  C07D277/60 ,  C07D277/66 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

摘要： The present invention is directed to a method of treatment by modulating a peroxisome proliferator activated receptor by employing a compound of Structural Formula (I). The variables in (I) are defined herein. Also included are compounds, methods of making compounds, and pharmaceutical compositions. The compounds of the present invention are believed to be effective in treating and preventing Syndrome X, Type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, atherosclerosis, and other disorders related to Syndrome X and cardiovascular diseases.

公开(公告)号：EP1817301B1

公开(公告)日：2012-02-01

申请号：EP05824420.3

申请日：2005-11-15

申请人： ELI LILLY AND COMPANY

发明人： AICHER, Thomas, Daniel ,  CORTEZ, Guillermo, S. ,  GROENDYKE, Todd, Michael ,  KHILEVICH, Albert ,  KNOBELSDORF, James, Allen ,  MAGNUS, Nicholas, Andrew ,  MARMSATER, Fredrik, Pehr ,  SCHKERYANTZ, Jeffrey, Michael ,  TANG, Tony, Pisal

IPC分类号： C07D401/04 ,  C07D257/04 ,  C07D213/79 ,  C07D213/70 ,  A61K31/4427 ,  A61P25/00 ,  A61P37/08

CPC分类号： C07C229/60 ,  C07C317/44 ,  C07D213/61 ,  C07D213/64 ,  C07D213/65 ,  C07D213/70 ,  C07D213/79 ,  C07D213/80 ,  C07D213/84 ,  C07D213/85 ,  C07D257/04 ,  C07D401/04 ,  C07D401/12

公开(公告)号：EP1817296B1

公开(公告)日：2009-11-04

申请号：EP05824423.7

申请日：2005-11-15

申请人： ELI LILLY AND COMPANY

发明人： AICHER, Thomas, Daniel ,  CORTEZ, Guillermo, S. ,  GROENDYKE, Todd, Michael ,  KHILEVICH, Albert ,  KNOBELSDORF, James, Allen ,  MARMSATER, Fredrik, Pehr ,  SCHKERYANTZ, Jeffrey, Michael ,  TANG, Tony, Pisal

IPC分类号： C07D257/04 ,  A61K31/4427 ,  A61P25/00 ,  A61P37/08 ,  C07C235/18

CPC分类号： C07C229/60 ,  C07C317/44 ,  C07D213/61 ,  C07D213/64 ,  C07D213/65 ,  C07D213/70 ,  C07D213/79 ,  C07D213/80 ,  C07D213/84 ,  C07D213/85 ,  C07D257/04 ,  C07D401/04 ,  C07D401/12

摘要： The present invention provides a compound of formula (I): pharmaceutical compositions thereof, and methods of using the same, processes for preparing the same, and intermediates thereof.