公开(公告)号：EP1819693B1

公开(公告)日：2009-08-26

申请号：EP05851697.2

申请日：2005-11-15

申请人： ELI LILLY AND COMPANY

发明人： FRANCISKOVICH, Jeffry, Bernard ,  HERRON, David, Kent ,  KLIMKOWSKI, Valentine, Joseph ,  MARQUART, Angela, Lynn ,  MASTERS, John, Joseph ,  MENDEL, David ,  RATZ, Andrew, Michael ,  SMITH, Gerald, Floyd ,  WILEY, Michael, Robert ,  YEE, Ying, Kwong

IPC分类号： C07D401/00 ,  C07D409/00 ,  C07D401/12 ,  C07D409/12 ,  C07D213/75 ,  C07D409/14 ,  C07C271/16 ,  C07C235/64 ,  A61K31/4465 ,  A61K31/4436 ,  A61P7/02

CPC分类号： C07D213/75 ,  C07C235/64 ,  C07C237/06 ,  C07C271/16 ,  C07C275/10 ,  C07C275/16 ,  C07C275/26 ,  C07C275/28 ,  C07C275/30 ,  C07D211/22 ,  C07D211/46 ,  C07D295/088 ,  C07D295/192 ,  C07D295/205 ,  C07D295/215 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

摘要： This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.

公开(公告)号：EP1511740B1

公开(公告)日：2009-07-08

申请号：EP03728782.8

申请日：2003-05-22

申请人： ELI LILLY AND COMPANY

发明人： DAHNKE, Karl, Robert ,  GAJEWSKI, Robert, Peter ,  JONES, Charles, David ,  LINEBARGER, Jared, Harris ,  LU, Jianliang ,  MA, Tianwei ,  NAGPAL, Sunil ,  SIMARD, Todd, Parker ,  YEE, Ying, Kwong ,  BUNEL, Emilio, Enrique ,  STITES, Ryan, Edward

IPC分类号： C07D333/38 ,  C07D333/16 ,  C07D333/18 ,  C07D333/22 ,  C07D409/12 ,  C07D409/06 ,  C07D333/34 ,  C07D413/04 ,  C07D409/04 ,  A61K31/381 ,  A61K31/401 ,  A61K31/41 ,  A61K31/4245 ,  A61P19/10

CPC分类号： C07F9/655345 ,  C07D333/18 ,  C07D333/20 ,  C07D333/22 ,  C07D333/24 ,  C07D333/34 ,  C07D333/38 ,  C07D333/40 ,  C07D409/06 ,  C07D409/12 ,  C07D413/04

摘要： The present invention relates to novel, non-secosteroidal, phenyl-thiophene compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1α,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.

公开(公告)号：EP1836177A2

公开(公告)日：2007-09-26

申请号：EP05854993.2

申请日：2005-12-19

申请人： ELI LILLY AND COMPANY

发明人： SHEN, Quanrong ,  WARSAWSKY, Alan, M. ,  YEE, Ying, Kwong

IPC分类号： C07D263/56 ,  A61K31/423 ,  A61P17/06

CPC分类号： C07D263/56

摘要： The present invention relates to novel, non-secosteroidal, phenyl-benzoxazole compounds of Formula (I) wherein the variables R, R’, RP, RP3, LP1, LP2, ZP, RB, RB’, LXB and ZXB are as hereinafter defined, their preparation, pharmaceutical compositions, and methods of use.

摘要翻译： 本发明涉及式（I）的新颖非 - 类固醇，苯基 - 苯并恶唑化合物，其中变量R，R'，RP，RP3，LP1，LP2，ZP，RB，RB'，LXB和ZXB如下文所定义 ，它们的制备，药物组合物和使用方法。

公开(公告)号：EP1819693A1

公开(公告)日：2007-08-22

申请号：EP05851697.2

申请日：2005-11-15

申请人： ELI LILLY AND COMPANY

发明人： FRANCISKOVICH, Jeffry, Bernard ,  HERRON, David, Kent ,  KLIMKOWSKI, Valentine, Joseph ,  MARQUART, Angela, Lynn ,  MASTERS, John, Joseph ,  MENDEL, David ,  RATZ, Andrew, Michael ,  SMITH, Gerald, Floyd ,  WILEY, Michael, Robert ,  YEE, Ying, Kwong

IPC分类号： C07D401/00 ,  C07D409/00 ,  C07D401/12 ,  C07D409/12 ,  C07D213/75 ,  C07D409/14 ,  C07C271/16 ,  C07C235/64 ,  A61K31/4465 ,  A61K31/4436 ,  A61P7/02

CPC分类号： C07D213/75 ,  C07C235/64 ,  C07C237/06 ,  C07C271/16 ,  C07C275/10 ,  C07C275/16 ,  C07C275/26 ,  C07C275/28 ,  C07C275/30 ,  C07D211/22 ,  C07D211/46 ,  C07D295/088 ,  C07D295/192 ,  C07D295/205 ,  C07D295/215 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

摘要： This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.

公开(公告)号：EP1687258A2

公开(公告)日：2006-08-09

申请号：EP04800873.4

申请日：2004-11-16

申请人： ELI LILLY AND COMPANY

发明人： BUNEL, Emilio, Enrique ,  GAJEWSKI, Robert, Peter ,  JONES, Charles, David ,  LU, Jianliang ,  NAGPAL, Sunil ,  MA, Tianwei ,  YEE, Ying, Kwong

IPC分类号： C07C235/42 ,  C07C235/84 ,  C07C63/04 ,  C07C69/76 ,  C07D257/06 ,  C07D257/04 ,  A61K31/18 ,  A61K31/255 ,  A61P19/08 ,  A61P19/10

CPC分类号： C07C235/42 ,  C07C65/19 ,  C07C69/92 ,  C07C235/84 ,  C07C2601/08 ,  C07C2601/14 ,  C07D257/04 ,  C07D257/06

摘要： The present invention relates to novel, non-secosteroidal, hydroxyl substituted, carbon- linked diaryl compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1α,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.

摘要翻译： 本发明涉及具有维生素D受体（VDR）调节活性的新型非 - 非甾体羟基取代的碳键二芳基化合物，其比1α，25二羟基维生素D3低钙血红素。 这些化合物可用于治疗骨病和牛皮癣。

公开(公告)号：EP1379506A2

公开(公告)日：2004-01-14

申请号：EP01273729.2

申请日：2001-11-14

申请人： ELI LILLY AND COMPANY

发明人： HERRON, David, Kent ,  JOSEPH, Sajan ,  MARQUART, Angela, Lynn ,  MASTERS, John, Joseph ,  MENDEL, David ,  SMITH, Gerald, Floyd ,  WAID, Philip, Parker ,  WILEY, Michael, Robert ,  YEE, Ying, Kwong

IPC分类号： C07D213/74 ,  C07D401/12 ,  A61P7/00 ,  A61K31/44 ,  A61K31/55

CPC分类号： C07D213/75 ,  C07D213/81 ,  C07D401/12 ,  C07D401/14

摘要： This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) in which R1 is substituted pyririnyl, phenyl, indolyl or indazolyl, A3, A4, A5 and A6, together with the two carbons to which they are attached complete a substituted benzene or a substituted heteroaromatic ring, L is carbonyl or methylene, Q is phenyl, cyclohexan-1,4-diyl or piperidin-1,4-diyl, M is N or CH and R is hydrogen, C1-C3 alkyl, C3-C5 cycloalkyl, C1-C3 acyl, acetyloxyacetyl, aminoacetyl, hydroxyacetyl C1-C4 alkoxy carbonyl C1-C4 alkoxycarbonylmethyl RaRbN-C(O) or RjSOj wherein the substitution is as defined in the description. This application also relates to pharmaceutical compositions of compounds of formula I, its use as an inhibitor of factor Xa, as well as a process for the preparation of compounds of formula I and intermediates therefor.

公开(公告)号：EP1307444A2

公开(公告)日：2003-05-07

申请号：EP01958825.0

申请日：2001-07-18

申请人： ELI LILLY AND COMPANY

发明人： HERRON, David, Kent ,  JOSEPH, Sajan ,  MARQUART, Angela, Lynn ,  MASTERS, John, Joseph ,  MENDEL, David ,  SMITH, Gerald, Floyd ,  WAID, Philip, Parker ,  WILEY, Michael, Robert ,  YEE, Ying, Kwong

IPC分类号： C07D401/14 ,  C07D401/12 ,  C07D213/81 ,  C07D237/24 ,  A61K31/4402 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61P7/02

CPC分类号： C07D401/14 ,  C07D237/24 ,  C07D403/04

摘要： This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

公开(公告)号：EP1007037A1

公开(公告)日：2000-06-14

申请号：EP98932926.3

申请日：1998-06-26

申请人： ELI LILLY AND COMPANY

发明人： BEIGHT, Douglas, Wade ,  CRAFT, Trelia, Joyce ,  FRANCISKOVICH, Jeffry, Bernard ,  GOODSON, Theodore, Junior ,  HALL, Steven, Edward ,  HERRON, David, Kent ,  KLIMKOWSKI, Valentine, Joseph ,  MASTERS, John, Joseph ,  MENDEL, David ,  MILOT, Guy ,  SAWYER, Jason, Scott ,  SHUMAN, Robert, Theodore ,  SMITH, Gerald, Floyd ,  TEBBE, Anne, Louise ,  TINSLEY, Jennifer, Marie ,  WEIR, Leonard, Crayton ,  WIKEL, James, Howard ,  WILEY, Michael, Robert ,  YEE, Ying, Kwong

IPC分类号： A61K31/38 ,  A61K31/40 ,  A61K31/42 ,  A61K31/165 ,  A61K31/445 ,  C07C233/64 ,  C07D209/44 ,  C07D211/32 ,  C07D333/06

CPC分类号： C07C271/66 ,  A61K31/00 ,  C07C257/18 ,  C07C259/18 ,  C07C271/64 ,  C07D209/44 ,  C07D211/60 ,  C07D261/20 ,  C07D333/38

摘要： This application relates to a compound of formula (I) (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.