发明申请
- 专利标题: Quinolines and Their Therapeutic Use
- 专利标题(中): 喹啉及其治疗用途
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申请号: US12066603申请日: 2006-09-29
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公开(公告)号: US20090156600A1公开(公告)日: 2009-06-18
- 发明人: Michael Colin Cramp , Rosa Arienzo , George Hynd , Peter Crackett , Yann Griffon , Trevor Keith Harrison , Nicholas Charles Ray , Harry Finch , John Gary Montana
- 申请人: Michael Colin Cramp , Rosa Arienzo , George Hynd , Peter Crackett , Yann Griffon , Trevor Keith Harrison , Nicholas Charles Ray , Harry Finch , John Gary Montana
- 优先权: GB0519969.0 20050930; GB0610551.4 20060526
- 国际申请: PCT/GB06/03644 WO 20060929
- 主分类号: A61K31/5377
- IPC分类号: A61K31/5377 ; C07D215/233 ; A61P11/06 ; C07D413/14 ; A61K31/47
摘要:
Compounds of formula [1] are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory component; in which: R1, R2, R3, R4 and R5 are independently hydrogen, C1-C6alkyl, C1-C6-fluoroalkyl, cyclopropyl, halo, —S(O)nR6, —SO2NR7R8, —NR7R8, —NR7C(O)R6, —CO2R7, —C(O)NR7R8, —C(O)R76, —NO2, —CN or a group —OR9; wherein each R6 is independently C1-C6alkyl, C1-C6-fluoroalkyl, cycloalkyl, aryl, or heteroaryl; R7, R8 are independently C1-C6alkyl, C1-C6-fluoroalkyl, cycloalkyl, cycloalkyl-(C1-C6alkyl)-, aryl, heteroaryl or hydrogen; R9 is hydrogen, C1-C6alkyl, C1-C6-fluoroalkyl, cycloalkyl, cylcoalkyl-(C1-C6alkyl)-, or a group —SO2R6; A is —CHR10—, —C(O)—, —S(O)n—, —O—, or —NR10— wherein n is an integer from 0-2 and R10 is hydrogen C1-C3alkyl, or C1-C6-fluoroalkyl group; B is a direct bond, or a divalent radical selected from —CH2—, —CH2CH2—, —CHR11—, —CR11R12—, —CH2CHR11—, CH2CR11R12—, —CHR11CHR12—, and divalent radicals of formula —(CR11R12)p-Z- wherein Z is attached to the ring carrying R1, R2 and R3; wherein R11 is C1-C3alkyl, cyclopropyl, C1-C6-fluoroalkyl; R12 is methyl or fluoromethyl; p is independently 1 or 2; and Z is —O—, —NH—, or —S(O)n—, wherein n is an integer from 0-2; X is a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, or 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.
公开/授权文献
- US07858640B2 Quinolines and their therapeutic use 公开/授权日:2010-12-28
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