公开(公告)号：US20110212955A1

公开(公告)日：2011-09-01

申请号：US13119904

申请日：2009-07-02

申请人： Hong Boon Lee ,  Kevin Burgess ,  Siang Hui Lim ,  Liangxing Wu

发明人： Hong Boon Lee ,  Kevin Burgess ,  Siang Hui Lim ,  Liangxing Wu

IPC分类号： A61K31/5377 ,  C07D405/14 ,  A61K31/4025 ,  A61K31/4545 ,  C07D413/14 ,  A61K31/496 ,  C07D405/04 ,  C07D413/04 ,  A61P35/00 ,  A61P35/02

CPC分类号： A61K31/352 ,  A61K31/4025 ,  A61K31/4453 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5375 ,  C07D311/82 ,  C07D311/86 ,  C09B11/24 ,  C09B11/26

摘要： The present invention relates to a new class of rosamine derivatives, in one embodiment, the compounds have the structure (I) or any pharmaceutically acceptable salt or solvate thereof, wherein: R1 represents aryl, Het1 or C1-6 alkyl, which latter group is optionally substituted by aryl or Het2; R2a and R2b together form C3.8 n-alkylene, which alkylene group is optionally substituted by one or more substituents selected from halo, C1-4 alkyl, C(O)OH and C(O)O—C1-4, alkyl and which alkylene group is optionally interrupted by X1; R3a and R3b together form C3-6 /7-alkylene, which alkylene group is optionally substituted by one or more substituents selected from halo. C1-4 alkyl, C(O)OH and C(O)O—C1-4 alkyl, and which alkylene group is optionally interrupted by X2; X1 and X2 independently represent O, S, or NR4; R4 represents, independently at each occurrence, H, C(O)OR5, C(O)R6a, C(O)N(R6b)R6c or C1-6, alkyl, which latter group is optionally substituted by one or more substituents selected from halo, aryl and Het3 or is substituted by a single C(O)OR1a group; R4a represents H or C1-4 alkyl; R5 represents aryl, Het4 or C1-6 alkyl optionally substituted by one or more substituents selected from halo, aryl and Het5; R5e to R6d independently represent H or R5; each aryl independently represents a C6-10carbocylic aromatic group, which group may comprise either one or two rings and may be substituted by one or more substituents selected from halo, CN, C1-6 alkyl (which latter group is optionally substituted by one or more substituents selected from halo, OR7, phenyl, napthyl and Het6) and OR8; R7 and R8 independently represent H, C1-4 alkyl (optionally substituted by one or more halo groups or by a single phenyl or C(O)OR8a substituent), Het7, phenyl or naphthyl; R8a represents H or C1-4 alkyl; Het1 to Het7 independently represent 5- to 10-membered aromatic, fully saturated or partially unsaturated heterocyclic groups containing one or more heteroatoms selected from oxygen, nitrogen and/or sulphur, which heterocyclic groups may comprise one or two rings and may be substituted by one or more substituents selected from Halo, CN, C1-6 alkyl (which latter group is optionally substituted by one or more substituents selected from halo, OR9 and phenyl) and OR10; R9 and R10 independently represent H, C1-4 alkyl or phenyl; unless otherwise specified, alkyl groups are optionally substituted by one or more halo atoms; and A′ represents a pharmaceutically acceptable anion. Also disclosed are methods for making and using compounds as well as pharmaceutical compositions.