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    PURINE DERIVATIVES AS PURINERGIC RECEPTOR ANTAGONISTS
    5.
    发明授权
    PURINE DERIVATIVES AS PURINERGIC RECEPTOR ANTAGONISTS 有权
    嘌呤衍生物作为拮抗剂嘌呤能受体

    公开(公告)号：EP1349857B1

    公开(公告)日：2010-06-16

    申请号：EP02729444.6

    申请日：2002-01-10

    申请人： VERNALIS RESEARCH LIMITED

    发明人： GILLESPIE, Roger, John ,  LERPINIERE, Joanne ,  DAWSON, Claire, Elizabeth ,  GAUR, Suneel ,  PRATT, Robert, Mark ,  STRATTON, Gemma, Caroline ,  WEISS, Scott, Murray

    IPC分类号： C07D473/00 ,  A61K31/52 ,  A61P25/14 ,  A61P25/16

    CPC分类号： C07D473/00 ,  A61K31/52 ,  C07D473/28 ,  C07D473/32 ,  C07D473/36 ,  C07D473/40

    摘要： Use of a compound of formula (I) wherein R1 is selected from alkyl, aryl, alkoxy, aryloxy, 0thioalkyl, thioaryl, CN, halo, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2R7 and NR4SO2R7; R2 is selected from N, O or S-containing heteroaryl groups, wherein the heteroaryl group is attached via an unsaturated carbon atom which is adjacent to one or two N, O or S-heteroatom(s), other than ortho, ortho-disubstituted heteroaryl groups; R3 is selected from H, alkyl, COR8, CONR9R10, CONR8NR9R10, CO2R11 and SO2R11; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an (NR5R6) group then R5 and R6 may be linked to form a heterocyclic ring; R7 is selected from alkyl and aryl; R8, R9 and R10 are independently selected from H, alkyl and aryl, or R9 and R10 may be linked to form a heterocyclic ring, or where R8, R9 and R10 are in a (CONR8NR9R10) group, R8 and R9 may be linked to form a heterocyclic group; and R11 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial, particularly wherein said disorder is a movement disorder such as Parkinson's disease or said disorder is depression, cognitive or memory impairment, acute or chronic pain, ADHD or narcolepsy, or for neuroprotection in a subject; compounds of formula (I) for use in therapy; and novel compounds of formula (I) per se.

    PURINE DERIVATIVES AS PURINERGIC RECEPTOR ANTAGONISTS
    6.
    发明公开
    PURINE DERIVATIVES AS PURINERGIC RECEPTOR ANTAGONISTS 有权
    嘌呤衍生物作为拮抗剂嘌呤能受体

    公开(公告)号：EP1349857A1

    公开(公告)日：2003-10-08

    申请号：EP02729444.6

    申请日：2002-01-10

    申请人： VERNALIS RESEARCH LIMITED

    发明人： GILLESPIE, Roger, John ,  LERPINIERE, Joanne ,  DAWSON, Claire, Elizabeth ,  GAUR, Suneel ,  PRATT, Robert, Mark ,  STRATTON, Gemma, Caroline ,  WEISS, Scott, Murray

    IPC分类号： C07D473/00 ,  A61K31/52 ,  A61P25/14 ,  A61P25/16

    CPC分类号： C07D473/00 ,  A61K31/52 ,  C07D473/28 ,  C07D473/32 ,  C07D473/36 ,  C07D473/40

    摘要： Use of a compound of formula (I) wherein R1 is selected from alkyl, aryl, alkoxy, aryloxy, 0thioalkyl, thioaryl, CN, halo, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2R7 and NR4SO2R7; R2 is selected from N, O or S-containing heteroaryl groups, wherein the heteroaryl group is attached via an unsaturated carbon atom which is adjacent to one or two N, O or S-heteroatom(s), other than ortho, ortho-disubstituted heteroaryl groups; R3 is selected from H, alkyl, COR8, CONR9R10, CONR8NR9R10, CO2R11 and SO2R11; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an (NR5R6) group then R5 and R6 may be linked to form a heterocyclic ring; R7 is selected from alkyl and aryl; R8, R9 and R10 are independently selected from H, alkyl and aryl, or R9 and R10 may be linked to form a heterocyclic ring, or where R8, R9 and R10 are in a (CONR8NR9R10) group, R8 and R9 may be linked to form a heterocyclic group; and R11 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial, particularly wherein said disorder is a movement disorder such as Parkinson's disease or said disorder is depression, cognitive or memory impairment, acute or chronic pain, ADHD or narcolepsy, or for neuroprotection in a subject; compounds of formula (I) for use in therapy; and novel compounds of formula (I) per se.