公开(公告)号：US20090062358A1

公开(公告)日：2009-03-05

申请号：US11828446

申请日：2007-07-26

申请人： Ivan Collado Cano ,  Samuel James Dominianni ,  Garret Jay Etgen, JR. ,  Cristina Garcia-Paredes ,  Richard Duane Johnston ,  Michael Edward Letourneau ,  Nathan Bryan Mantlo ,  Michael John Martinelli ,  Daniel Ray Mayhugh ,  Ashraf Saeed ,  Richard Craig Thompson ,  Xiaodong Wang ,  David Scott Coffey ,  Christopher Randall Schmid ,  Jeffrey Thomas Vicenzi ,  Yanping Xu

发明人： Ivan Collado Cano ,  Samuel James Dominianni ,  Garret Jay Etgen, JR. ,  Cristina Garcia-Paredes ,  Richard Duane Johnston ,  Michael Edward Letourneau ,  Nathan Bryan Mantlo ,  Michael John Martinelli ,  Daniel Ray Mayhugh ,  Ashraf Saeed ,  Richard Craig Thompson ,  Xiaodong Wang ,  David Scott Coffey ,  Christopher Randall Schmid ,  Jeffrey Thomas Vicenzi ,  Yanping Xu

IPC分类号： A61K31/4196 ,  C07D249/12 ,  C07D405/02

CPC分类号： C07C281/06 ,  C07C257/22 ,  C07C281/04 ,  C07D249/12 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06 ,  C07D417/12

摘要： The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C1-C5 alkyl, C1-C5 alkoxy, C3-C6 cycloalkyl, arylC0-C4alkyl and phenyl, or R3 and R4 are combined to form a C3-C4 cycloalkyl.

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，溶剂合物和水合物，R 1是选自C 1 -C 8烷基，芳基-C 0-2 - 烷基，杂芳基-C 0 - C 3 -C 6环烷基芳基-C 0-2 - 烷基或苯基。 W是O或S.R 2是H或选自C 1 -C 6烷基，C 3 -C 6环烷基和杂芳基的取代或未取代的基团。 X是C2-C5亚烷基连接体，连接体的一个碳原子可被O，NH或S取代.Y是C，O，S，NH或单键。 此外，E是（CH 2）n COOH，其中n是0,1,2或3或C（R3）（R4）A，其中A是酸性官能团如羧基，甲酰胺取代或未取代的磺酰胺，或取代或未取代的 未取代的四唑。 R3是H，饱和或不饱和的C1-C5烷基，C1-C5烷氧基。 另外，R 4为H，卤素，取代或未取代的选自C 1 -C 5烷基，C 1 -C 5烷氧基，C 3 -C 6环烷基，芳基C 0 -C 4烷基和苯基，或R 3和R 4的基团，形成C 3 -C 4环烷基。

公开(公告)号：US07304062B2

公开(公告)日：2007-12-04

申请号：US10415673

申请日：2001-11-09

申请人： Samuel James Dominianni ,  Garret Jay Etgen ,  Richard Duane Johnston ,  Nathan Bryan Mantlo ,  Daniel Ray Mayhugh ,  Ashraf Saeed ,  Richard Craig Thompson ,  Xiaodong Wang ,  Christopher Randall Schmid ,  Yanping Xu

发明人： Samuel James Dominianni ,  Garret Jay Etgen ,  Richard Duane Johnston ,  Nathan Bryan Mantlo ,  Daniel Ray Mayhugh ,  Ashraf Saeed ,  Richard Craig Thompson ,  Xiaodong Wang ,  Christopher Randall Schmid ,  Yanping Xu

IPC分类号： A61K31/5377 ,  A61K31/4709 ,  A61K31/4196 ,  C07D413/06 ,  C07D249/12 ,  C07D215/12

CPC分类号： C07C281/06 ,  C07C257/22 ,  C07C281/04 ,  C07D249/12 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06 ,  C07D417/12

摘要： The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C1-C5 alkyl, C1-C5 alkoxy, C3-C6 cycloalkyl, arylC0-C4alkyl and phenyl, or R3 and R4 are combined to form a C3-C4 cycloalkyl.

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，溶剂合物和水合物，R 1是选自C 1 -C 8烷基的取代或未取代的基团， 烷基，芳基-C 0-2 - - 烷基，杂芳基-C 0-2-2 - 烷基，C 3 -C 6环烷基芳基-C 0-2-2 - 烷基或苯基。 W是O或S.R 2是H或选自C 1 -C 6烷基，C 3 -C 3烷基的取代或未取代的基团， C 6环烷基和杂芳基。 X是连接子的一个碳原子可以被O，NH或S取代的C 2 -C 5亚烷基连接基，Y是C，O，S，NH 或单一债券。 此外，E是（CH 2 SO 2）n COOH，其中n是0,1,2或3，或C（R 3）（R 4）A，其中A是 酸性官能团如羧基，羧酰胺取代或未取代的磺酰胺，或取代或未取代的四唑。 R 3是H，饱和或不饱和的C 1 -C 5烷基，C 1 -C 5烷氧基。 另外，R 4是H，卤素，取代或未取代的选自C 1 -C 5烷基，C 1 -C 3烷基， 5个烷氧基，C 3 -C 6环烷基，芳基C 0 -C 4烷基和苯基 ，或R 3和R 4结合形成C 3 -C 4环烷基。