公开(公告)号：EP1392637A2

公开(公告)日：2004-03-03

申请号：EP02739503.7

申请日：2002-05-30

申请人： ELI LILLY AND COMPANY ,  LIGAND PHARMACEUTICALS INCORPORATED

发明人： BROOKS, Dawn, Alisa ,  WARSHAWSKY, Alan, M. ,  MONTROSE-RAFEZADEH, Chahrzad ,  REIFEL-MILLER, Anne ,  PRIETO, Lourdes ,  ROJO, Isabel ,  MARTIN, Jose, Alfredo ,  GONZALES GARCIA, Maria, Rosario ,  TORRADO, Alicia ,  FERRITTO CRESPO, Rafael ,  LAMAS-PETEIRA, Carlos ,  MARTIN-ORTEGA FINGER, Maria ,  ARDECKY, Robert, J.

IPC分类号： C07C59/68 ,  C07C59/90 ,  C07C59/72 ,  C07C239/12 ,  C07D311/30 ,  C07D307/91 ,  C07C219/10 ,  C07D213/30 ,  C07D215/14 ,  C07D295/08 ,  C07C217/94 ,  A61K31/192 ,  A61K31/195 ,  A61P9/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/00

CPC分类号： C07D209/48 ,  C07C59/68 ,  C07C59/72 ,  C07C59/90 ,  C07C217/20 ,  C07C217/84 ,  C07C217/92 ,  C07C219/10 ,  C07C233/25 ,  C07C233/29 ,  C07C233/60 ,  C07C233/75 ,  C07C235/56 ,  C07C235/64 ,  C07C239/12 ,  C07C255/54 ,  C07C2601/08 ,  C07D209/08 ,  C07D213/30 ,  C07D215/14 ,  C07D217/02 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D257/04 ,  C07D277/64 ,  C07D295/096 ,  C07D295/112 ,  C07D295/185 ,  C07D307/79 ,  C07D307/83 ,  C07D307/91 ,  C07D307/93 ,  C07D311/30 ,  C07D317/20 ,  C07D317/22 ,  C07D317/54 ,  C07D317/64 ,  C07D333/16 ,  C07D333/76 ,  C07D335/02

摘要： Disclosed is a compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aromatic group. Q is a covalent bond, -CH2-or-CH2CH2-; W is a substituted or unsubstituted alkylene or a substituted or unsubstituted heteroalkylene linking group from two to ten atoms in length, preferably from two to seven atoms in length. Phenyl Ring A is optionally substituted with up to four substituents in addition to R1 and W. R1 is (CH2)n-CH(OR2)-(CH2)mE, -(CH)=C(OR2)-(CH2)mE, -(CH2)n-CH(Y)-(CH2)mE or (CH)=C(Y)-(CH2)mE; wherein E is COOR3, C1-C3 alkylnitrile, carboxamide, sulfonamide, acylsulfonamide or tetrazole and wherein sulfonamide, acylsulfonamide and tetrazole are optionally substituted with one or more substituents independently selected from: C1-C6 alkyl, haloalkyl and aryl-C0-4-alkyl; R2 is H, an aliphatic group, a substituted aliphatic group, haloalkyl, an aromatic group, a substituted aromatic group, -COR4, -COOR4, -CONR5R6, -C(S)R4, -C(S)OR4 or C(S)NR5R6. R3 is H, an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. Y is O-, CH2-, -CH2CH2- or CH=CH- and is bonded to a carbon atom in Phenyl Ring A that is ortho to R1. R4-R6 are independently H, an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. n and m are independently 0, 1 or 2.

摘要翻译： 公开了由结构式（I）表示的化合物：Ar是取代或未取代的芳基。 Q是共价键，-CH 2 - 或-CH 2 CH 2 - ; - W是长度为2至10个原子，优选2至7个长度的取代或未取代的亚烷基或取代或未取代的亚烷基连接基团。 苯环A任选被至多四个取代基取代，除R 1和W之外，R 1是（CH 2 2） - （CH 2） - （CH 2）2 - ， - （CH 2）n - CH 2 - （CH 2）2 - ， - （CH 2 CH 2） - （CH 2 CH 2） 或（CH）-C（Y） - （CH 2） - （CH 2）n - （CH 2） / SUB>）_{米电子; 其中E是COOR 3，C 1 -C 3烷基腈，甲酰胺，磺酰胺，酰基磺酰胺或四唑，并且其中磺酰胺，酰基磺酰胺和四唑是任选的 被一个或多个独立地选自C 1 -C 6烷基，卤代烷基和芳基-C 0-4烷基的取代基取代; R 2是H，脂族基团，取代的脂族基团，卤代烷基，芳族基团，取代的芳族基团，-COR 4，-COOR 4， -CONR 5 R 6，-C（S）R 4，-C（S）OR 4， / SUB或C（S）NR 5 R 6，R 3是H，脂族基团，取代的脂族基团，芳香族基团 基团或取代的芳族基团。 Y是O-，CH 2 - ， - CH 2 CH 2 - 或CH-CH-，并且与苯基中的碳原子键合 与R 1邻位的环A。 R 4 -R 6独立地是H，脂族基团，取代的脂族基团，芳族基团或取代的芳族基团。 n和m独立地为0,1或2}

公开(公告)号：EP1206457A1

公开(公告)日：2002-05-22

申请号：EP00959401.1

申请日：2000-08-23

申请人： ELI LILLY AND COMPANY ,  LIGAND PHARMACEUTICALS INCORPORATED

发明人： BROOKS, Dawn A. ,  RITO, Christopher, J. ,  SHUKER, Anthony, J. ,  DOMINIANNI, Samuel, J. ,  WARSHAWSKY, Alan, M. ,  GOSSETT, Lynn, S. ,  MATTHEWS, Donald, P. ,  HAY, David, A. ,  ARDECKY, Robert, J. ,  MICHELLYS, Pierre-Yves ,  TYHONAS, John. S.

IPC分类号： C07D263/32 ,  C07D277/24 ,  C07D413/10 ,  A61K31/421 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/506 ,  A61P3/10 ,  A61P9/00

CPC分类号： C07D413/10 ,  C07D263/32 ,  C07D277/24

摘要： Compounds represented by Formula (I) wherein n is 2, 3, or 4; V is O or S; W is O, S, or SO2 and at least one R5 is a substituted or unsubstituted aryl or a substituted or unsubstituted heteroaryl; are modulators of peroxisome proliferator activated receptors and are useful in the treatment of type II diabetes and of cardiovascular diseases.

公开(公告)号：EP1206457B1

公开(公告)日：2003-10-15

申请号：EP00959401.1

申请日：2000-08-23

申请人： ELI LILLY AND COMPANY ,  LIGAND PHARMACEUTICALS INCORPORATED

发明人： BROOKS, Dawn A. ,  RITO, Christopher, J. ,  SHUKER, Anthony, J. ,  DOMINIANNI, Samuel, J. ,  WARSHAWSKY, Alan, M. ,  GOSSETT, Lynn, S. ,  MATTHEWS, Donald, P. ,  HAY, David, A. ,  ARDECKY, Robert, J. ,  MICHELLYS, Pierre-Yves ,  TYHONAS, John. S.

IPC分类号： C07D263/32 ,  C07D277/24 ,  C07D413/10 ,  A61K31/421 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/506 ,  A61P3/10 ,  A61P9/00

CPC分类号： C07D413/10 ,  C07D263/32 ,  C07D277/24

摘要： Compounds represented by Formula (I) wherein n is 2, 3, or 4; V is O or S; W is O, S, or SO2 and at least one R5 is a substituted or unsubstituted aryl or a substituted or unsubstituted heteroaryl; are modulators of peroxisome proliferator activated receptors and are useful in the treatment of type II diabetes and of cardiovascular diseases.

公开(公告)号：EP1836151B1

公开(公告)日：2009-04-01

申请号：EP05854992.4

申请日：2005-12-19

申请人： ELI LILLY AND COMPANY

发明人： GOSSETT, Lynn, Stacy ,  LOPEZ, Jose, Eduardo ,  WARSHAWSKY, Alan, M. ,  YEE, Ying, Kwong

IPC分类号： C07C65/40 ,  C07C65/24 ,  A61K31/165 ,  A61K31/19 ,  A61P3/14

CPC分类号： C07C235/42 ,  C07C65/24 ,  C07C65/40 ,  C07C217/80 ,  C07C271/30

摘要： The present invention relates to novel, non-secosteroidal, phenyl-naphthalene compounds of Formula (I): wherein R, R1, RP, Z P , L P1 , L P2 L NP , RP 3 , RN, and Z NP are defined herein, their preparation, pharmaceutical compositions, and methods of use.

公开(公告)号：EP1480640B1

公开(公告)日：2007-08-15

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.

公开(公告)号：EP1687299A1

公开(公告)日：2006-08-09

申请号：EP04810028.3

申请日：2004-11-16

申请人： ELI LILLY AND COMPANY

发明人： HENRY, James, Robert ,  LI, Yihong ,  SCHKERYANTZ, Jeffrey, Michael ,  WARSHAWSKY, Alan, M.

IPC分类号： C07D413/12 ,  C07D417/12 ,  C07D401/12 ,  C07D413/14 ,  C07D217/24 ,  A61K31/472 ,  A61K31/4725

CPC分类号： C07D413/12 ,  C07D217/06 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

摘要： 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.

公开(公告)号：EP1687292A2

公开(公告)日：2006-08-09

申请号：EP04819516.8

申请日：2004-11-16

申请人： ELI LILLY AND COMPANY

发明人： LU, Jianliang ,  MA, Tainwei ,  NAGPAL, Sunil ,  SHEN, Quanrong ,  WARSHAWSKY, Alan, M. ,  YEE, Ying, Kwong ,  RUPP, Michael, John

IPC分类号： C07D333/70 ,  C07D333/68 ,  A61K31/559 ,  A61P3/14

CPC分类号： C07D333/68 ,  C07D333/70

摘要： The present invention relates to novel, non-secosteroidal, phenyl-benzothiophene 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：EP1687289A1

公开(公告)日：2006-08-09

申请号：EP04800486.5

申请日：2004-11-16

申请人： ELI LILLY AND COMPANY

发明人： LU, Jianliang ,  MA, Tianwei ,  NAGPAL, Sunil ,  SHEN, Quanrong ,  WARSHAWSKY, Alan, M. ,  OCHOADA, Jason, Matthew ,  YEE, Ying, Kwong

IPC分类号： C07D307/77 ,  C07D405/12 ,  C07D407/10 ,  C07D407/12 ,  A61K31/12

CPC分类号： C07D405/12 ,  C07D307/80 ,  C07D407/12

摘要： The present invention relates to novel, non-secosteroidal, phenyl-benzofuran 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 - 类固醇，苯基 - 苯并呋喃化合物，其比1α，25二羟基维生素D 3更低的高钙血症。 这些化合物可用于治疗骨疾病和牛皮癣。

公开(公告)号：EP1697304B1

公开(公告)日：2008-02-20

申请号：EP04820002.6

申请日：2004-11-16

申请人： ELI LILLY AND COMPANY

发明人： CANADA, Emily, Jane ,  GOSSETT, Lynn, Stacy ,  MANTELO, Nathan, Bryan ,  SHI, Qing ,  WANG, Minmin ,  WARSHAWSKY, Alan, M. ,  XU, Yanping

IPC分类号： C07C233/73 ,  C07C271/16 ,  C07C311/04 ,  C07C317/44 ,  C07C323/62 ,  C07D209/42 ,  C07D209/46 ,  C07D213/81 ,  C07D217/06 ,  C07D333/70 ,  A61K31/166 ,  A61K31/265 ,  A61K31/18 ,  A61K31/381 ,  A61K31/4035

CPC分类号： C07D213/81 ,  C07C211/29 ,  C07C233/73 ,  C07C235/46 ,  C07C235/48 ,  C07C235/54 ,  C07C235/84 ,  C07C271/16 ,  C07C311/04 ,  C07C311/17 ,  C07C317/44 ,  C07C323/62 ,  C07D209/30 ,  C07D209/42 ,  C07D213/56 ,  C07D333/70

摘要： 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.

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.