申请人:Pulmagen Therapeutics (Asthma) Limited
公开号:US07858640B2
公开(公告)日:2010-12-28
Compounds of formula [1] are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory components; in which: R1-R9 are various substituents; A is —CHR10—, —C(O)—, —S(O)n—, —O—, or —NR10— wherein n is an integer from 0-1 and R10 is selected from various substituents; B is a direct bond or a divalent radical; R11 and R12 are selected from cvarious substituents; X is a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, sulfonic acid group, or a group of formula C═(O)NHSO2R6 or SO2NHC(═O)R6; and Y is aryl, heteroaryl, aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group.
化合物的化学式[1]是CRTH2拮抗剂,可用于治疗具有炎症成分的疾病;其中:R1-R9是不同的取代基;A是-CHR10-,-C(O)-,-S(O)n-,-O-或-NR10-,其中n是0-1的整数,R10是选择的不同取代基;B是直接键或二价基团;R11和R12是选择的不同取代基;X是羧酸,四唑,3-羟基异噁唑,羟肟酸,磷酸酯,膦酸盐,膦酰胺,磺酸基或公式C =(O)NHSO2R6或SO2NHC(= O)R6的基团;Y是芳基,杂环芳基,芳基融合杂环烷基,杂环芳基融合环烷基,杂环芳基融合杂环烷基或芳基融合环烷基基团。