公开(公告)号：US06417212B1

公开(公告)日：2002-07-09

申请号：US09644457

申请日：2000-08-23

申请人： Dawn A. Brooks ,  Christopher J. Rito ,  Anthony J. Shuker ,  Samuel J. Dominianni ,  Alan M. Warshawsky ,  Lynn S. Gossett ,  Donald P. Matthews ,  David A. Hay ,  Robert J. Ardecky ,  Pierre-Yves Michellys ,  John S. Tyhonas

发明人： Dawn A. Brooks ,  Christopher J. Rito ,  Anthony J. Shuker ,  Samuel J. Dominianni ,  Alan M. Warshawsky ,  Lynn S. Gossett ,  Donald P. Matthews ,  David A. Hay ,  Robert J. Ardecky ,  Pierre-Yves Michellys ,  John S. Tyhonas

IPC分类号： C07D26336

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

摘要： The present invention is directed to compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof, and methods of making, methods of using and pharmaceutical compositions having compounds represented by Structural Formula I and pharmaceutically acceptable salts, solvates and hydrates thereof: In Structural Formula I, n is 2, 3, or 4; V is O or S; W is O, S, or SO2; R1 is H, a C1-C4 alkyl, phenyl or trifluoromethyl; R2 are each, independently, H, a C1-C6 alkyl, an aryl-C1-C6 alkyl, a cycloalkyl-C1-C4 alkyl, an aryl, a cycloalkyl, or together with the phenyl to which they are bound form naphthyl or 1,2,3,4-tetrahydronaphthyl; R3 are each, independently, H, a C1-C6 alkyl, an aryl-C1-C6 alkyl, a cycloalkyl-C1-C4 alkyl, an aryl, or a cycloalkyl; R4 are each, independently, H, a C1-C4 alkyl, an aryl, or benzyl; R5 are each, independently, H, a substituted or unsubstituted aryl or a heteroaryl, provided that at least one R5 is a substituted or unsubstituted aryl or a substituted or unsubstituted heteroaryl; and R6 is H, a C1-C4 alkyl, or an aminoalkyl.

摘要翻译： 本发明涉及由结构式I表示的化合物及其药学上可接受的盐，溶剂合物和水合物及其制备方法，使用方法和具有由结构式I表示的化合物的药物组合物及其药学上可接受的盐，溶剂化物和水合物： 在结构式I中，n为2,3或4; V为O或S; W是O，S或SO 2; R1是H，C1-C4烷基，苯基或三氟甲基; R 2各自独立地为H，C 1 -C 6烷基，芳基-C 1 -C 6烷基，环烷基-C 1 -C 4烷基，芳基，环烷基，或与它们所连接的苯基一起形成萘基或1 ，2,3,4-四氢萘基; R 3各自独立地为H，C 1 -C 6烷基，芳基-C 1 -C 6烷基，环烷基-C 1 -C 4烷基，芳基或环烷基; R 4各自独立地为H，C 1 -C 4烷基，芳基或苄基; R5各自独立地为H，取代或未取代的芳基或杂芳基，条件是至少一个R 5为取代或未取代的芳基或取代或未取代的杂芳基; 并且R 6是H，C 1 -C 4烷基或氨基烷基。

公开(公告)号：US06437146B1

公开(公告)日：2002-08-20

申请号：US09787433

申请日：2001-04-20

申请人： Kouji Hattori ,  Akira Tanaka ,  Yutaka Kono ,  Shoko Nakazato

发明人： Kouji Hattori ,  Akira Tanaka ,  Yutaka Kono ,  Shoko Nakazato

IPC分类号： C07D26336

CPC分类号： C07D413/12 ,  C07D263/32 ,  C07D413/10

摘要： Oxazole compounds of formula (I), wherein R1 is aryl which may be substituted with halogen(s), R2 is aryl which may be substituted with halogen(s), X is single bond, (a) or SO2, R3 and R4 are independently hydrogen or suitable substituent, (wherein X is (a), neither R3 nor R4 is hydrogen), R3 and R4 may be linked together to form (b), (b) is N-containing heterocyclic group which may be substituted with one or more suitable substituent(s), R5 is hydrogen, etc., A1 is lower alkylene or single bond, (c) is cyclo(C3-C9)alkane or cyclo(C5-C9)alkene, or a pro-drug thereof, or a pharmaceutically acceptable salt thereof, which are useful as medicament.

摘要翻译： 式（I）的恶唑化合物，其中R 1为可被卤素取代的芳基，R 2为可被卤素取代的芳基，X为单键，（a）或SO 2，R 3和R 4为 （其中X是（a），R3和R4都不是氢），R3和R4可以连接在一起形成（b），（b）是可以被一个取代的含氮杂环基 或更合适的取代基，R5是氢等，A1是低级亚烷基或单键，（c）是环（C 3 -C 9）烷烃或环（C 5 -C 9）烯烃或其前药， 或其药学上可接受的盐，其可用作药物。