公开(公告)号：WO2008103574A2

公开(公告)日：2008-08-28

申请号：PCT/US2008/053653

申请日：2008-02-12

Applicant: ELI LILLY AND COMPANY ,  PFEIFER, Lance, Allen ,  MA, Tianwei ,  MANTLO, Nathan, Bryan ,  MICHAEL, Laura, Frey ,  MOKUBE, Fese, Mambo ,  MONTROSE-RAFIZADEH, Chahrzad

Inventor： PFEIFER, Lance, Allen ,  MA, Tianwei ,  MANTLO, Nathan, Bryan ,  MICHAEL, Laura, Frey ,  MOKUBE, Fese, Mambo ,  MONTROSE-RAFIZADEH, Chahrzad

CPC classification number: C07D401/06 ,  C07D249/12

Abstract: The present invention is directed to compounds of the structural Formula: wherein: R 1 is H or -C 1 -C 3 alkyl; R 2 is selected from the group consisting of -H, -C 1 -C 4 alkyl, -C 1 -C 3 alkyl-CF 3 , phenyl, and pyridinyl; and R 3 is selected from the group consisting of -H, -C 1 -C 4 alkyl, -C 1 -C 3 alkyl-O-CH 3 , -CH 2 -cyclopropyl, -CH 2 -C=CH 2 , -CH 2 CH 2 -(2-F-phenyl), and phenyl substituted with from 1 to 2 fluorines; provided that when R 1 and R 2 are each H, then R 3 is selected from the group consisting of -C 1 -C 4 alkyl, -C 1 -C 3 alkyl-O-CH 3 , -CH 2 -cyclopropyl, -CH 2 -C=CH 2 , -CH 2 CH 2 -(2-F-phenyl), and phenyl substituted with from 1 to 2 fluorines; or stereoisomers and pharmaceutically acceptable salts thereof.

Abstract translation: 本发明涉及结构式的化合物：其中：R 1是H或-C 1 -C 3烷基; R 2选自-H，-C 1 -C 4烷基，-C 1 H 2 -C 3 -C 3烷基-C≡C3，苯基和吡啶基; 和R 3选自-H，-C 1 -C 4烷基，-C 1 -C 4烷基， C 1 -C 3烷基-O-CH 3，-CH 2 - 环丙基，-CH 2 - C = CH 2，-CH 2 CH 2 - （2-F-苯基）和被1至2个氟取代的苯基; 条件是当R 1和R 2各自为H时，R 3选自-C 1， C 1 -C 4烷基，-C 1 -C 3烷基-O-CH 3 - ， - CH 2 - 2 - 环丙基，-CH 2 -C = CH 2 CH 2，-CH 2 CH 2 （2-F-苯基）和被1至2个氟取代的苯基; 或立体异构体及其药学上可接受的盐。

公开(公告)号：WO2008103574A3

公开(公告)日：2008-12-18

申请号：PCT/US2008053653

申请日：2008-02-12

Applicant: LILLY CO ELI ,  PFEIFER LANCE ALLEN ,  MA TIANWEI ,  MANTLO NATHAN BRYAN ,  MICHAEL LAURA FREY ,  MOKUBE FESE MAMBO ,  MONTROSE-RAFIZADEH CHAHRZAD

Inventor： PFEIFER LANCE ALLEN ,  MA TIANWEI ,  MANTLO NATHAN BRYAN ,  MICHAEL LAURA FREY ,  MOKUBE FESE MAMBO ,  MONTROSE-RAFIZADEH CHAHRZAD

IPC: C07D249/12 ,  A61K31/4196 ,  A61K31/4439 ,  A61P3/00 ,  C07D401/06

CPC classification number: C07D401/06 ,  C07D249/12

Abstract: The present invention is directed to compounds of the structural Formula: wherein: R1 is H or -C1-C3 alkyl; R2 is selected from the group consisting of -H, -C1-C4 alkyl, -C1-C3 alkyl-CF3, phenyl, and pyridinyl; and R3 is selected from the group consisting of -H, -C1-C4 alkyl, -C1-C3 alkyl-O-CH3, -CH2-cyclopropyl, -CH2-C=CH2, -CH2CH2-(2-F-phenyl), and phenyl substituted with from 1 to 2 fluorines; provided that when R1 and R2 are each H, then R3 is selected from the group consisting of -C1-C4 alkyl, -C1-C3 alkyl-O-CH3, -CH2-cyclopropyl, -CH2-C=CH2, -CH2CH2-(2-F-phenyl), and phenyl substituted with from 1 to 2 fluorines; or stereoisomers and pharmaceutically acceptable salts thereof.

Abstract translation: 本发明涉及结构式的化合物：其中：R 1是H或-C 1 -C 3烷基; R 2选自-H，-C 1 -C 4烷基，-C 1 -C 3烷基-CF 3，苯基和吡啶基; 并且R 3选自-H，-C 1 -C 4烷基，-C 1 -C 3烷基-O-CH 3，-CH 2 - 环丙基，-CH 2 -C = CH 2，-CH 2 CH 2 - （2-F-苯基） 和被1至2个氟取代的苯基; 条件是当R 1和R 2各自为H时，R 3选自-C 1 -C 4烷基，-C 1 -C 3烷基-O-CH 3，-CH 2 - 环丙基，-CH 2 -C = CH 2，-CH 2 CH 2 - （2-F-苯基）和被1至2个氟取代的苯基; 或其立体异构体及其药学上可接受的盐。

公开(公告)号：WO2006083645A3

公开(公告)日：2006-12-28

申请号：PCT/US2006002606

申请日：2006-01-25

Applicant: LILLY CO ELI ,  ABU-RADDAD EYAS JAMAL ,  DERBY MICHAEL ARTHUR ,  HARRIS CYNTHIA JOYCE ,  HOWEY DANIEL CHARLES ,  MICHAEL LAURA FREY

Inventor： ABU-RADDAD EYAS JAMAL ,  DERBY MICHAEL ARTHUR ,  HARRIS CYNTHIA JOYCE ,  HOWEY DANIEL CHARLES ,  MICHAEL LAURA FREY

IPC: A61K31/4196 ,  A61P3/06 ,  A61P3/10

CPC classification number: A61K31/4196

Abstract: The present invention provides dosing regimens for PPAR-alpha agonist and compositions thereof. A further embodiment of the present invention is a solid oral formulation of Propanoic Acid, 2-[4-[3-[2,5-dihydro-l-[(4-methylphenyl)methyl]-5-oxo- lH-l,2,4-triazol-3-yl]propyl]phenoxy]-2-methyl- comprising 75 µg or less of Propanoic Acid, 2-[4-[3-[2,5-dihydro-l-[(4-methylphenyl)methyl]-5-oxo-lH-l,2,4-triazol-3- yl]propyl]phenoxy]-2-methyl- per dosage unit.

Abstract translation: 本发明提供PPAR-α激动剂及其组合物的给药方案。 本发明的另一个实施方案是丙酸2- [4- [3- [2,5-二氢-1 - [（4-甲基苯基）甲基] -5-氧代-1H- 2,4-三氟-3-基]丙基]苯氧基] -2-甲基 - 包含75μg或更少的丙酸，2- [4- [3- [2,5-二氢-1 - [（4-甲基苯基） ）甲基] -5-氧代-1H-1,2,4-三唑-3-基]丙基]苯氧基] -2-甲基 - 。

公开(公告)号：WO2006083645A2

公开(公告)日：2006-08-10

申请号：PCT/US2006/002606

申请日：2006-01-25

Applicant: ELI LILLY AND COMPANY ,  ABU-RADDAD, Eyas, Jamal ,  DERBY, Michael, Arthur ,  HARRIS, Cynthia, Joyce ,  HOWEY, Daniel, Charles ,  MICHAEL, Laura, Frey

Inventor： ABU-RADDAD, Eyas, Jamal ,  DERBY, Michael, Arthur ,  HARRIS, Cynthia, Joyce ,  HOWEY, Daniel, Charles ,  MICHAEL, Laura, Frey

IPC: A61K31/4196 ,  A61P3/06 ,  A61P3/10

CPC classification number: A61K31/4196

Abstract: The present invention provides dosing regimens for PPAR-alpha agonist and compositions thereof. A further embodiment of the present invention is a solid oral formulation of Propanoic Acid, 2-[4-[3-[2,5-dihydro-l-[(4-methylphenyl)methyl]-5-oxo- l H -l,2,4-triazol-3-yl]propyl]phenoxy]-2-methyl- comprising 75 µg or less of Propanoic Acid, 2-[4-[3-[2,5-dihydro-l-[(4-methylphenyl)methyl]-5-oxo-l H -l,2,4-triazol-3- yl]propyl]phenoxy]-2-methyl- per dosage unit.

Abstract translation: 本发明提供了PPAR-α激动剂及其组合物的给药方案。 本发明的另一个实施方案是丙酸2- [4- [3- [2,5-二氢-1 - [（4-甲基苯基）甲基] -5-氧代-1,3-丙二醇的固体口服制剂， H-1,2,4-三唑-3-基]丙基]苯氧基] -2-甲基 - 包含75微克或更少的丙酸，2- [4- [3- [2,5 - 二氢-1 - [（4-甲基苯基）甲基] -5-氧代-1H-1,2,4-三唑-3-基]丙基]苯氧基] -2-甲基 - 剂量单位。