发明名称 Purine derivatives as purinergic receptor antagonists.
摘要 Use of a compound of formula (I) wherein R<SUB>1 </SUB>is selected from alkyl, aryl, alkoxy, aryloxy, 0thioalkyl, thioaryl, CN, halo, NR<SUB>5</SUB>R<SUB>6</SUB>, NR<SUB>4</SUB>COR<SUB>5</SUB>, NR<SUB>4</SUB>CONR<SUB>5</SUB>R<SUB>6</SUB>, NR<SUB>4</SUB>CO<SUB>2</SUB>R<SUB>7 </SUB>and NR<SUB>4</SUB>SO<SUB>2</SUB>R<SUB>7</SUB>; R<SUB>2 </SUB>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; R<SUB>3 </SUB>is selected from H, alkyl, COR<SUB>8</SUB>, CONR<SUB>9</SUB>R<SUB>10</SUB>, CONR<SUB>8</SUB>NR<SUB>9</SUB>R<SUB>10</SUB>, CO<SUB>2</SUB>R<SUB>11 </SUB>and SO<SUB>2</SUB>R<SUB>11</SUB>; R<SUB>4</SUB>, R<SUB>5 </SUB>and R<SUB>6 </SUB>are independently selected from H, alkyl and aryl or where R<SUB>5 </SUB>and R<SUB>6 </SUB>are in an (NR<SUB>5</SUB>R<SUB>6</SUB>) group then R<SUB>5 </SUB>and R<SUB>6 </SUB>may be linked to form a heterocyclic ring; R<SUB>7 </SUB>is selected from alkyl and aryl; R<SUB>8</SUB>, R<SUB>9 </SUB>and R<SUB>10 </SUB>are independently selected from H, alkyl and aryl, or R<SUB>9 </SUB>and R<SUB>10 </SUB>may be linked to form a heterocyclic ring, or where R<SUB>8</SUB>, R<SUB>9 </SUB>and R<SUB>10 </SUB>are in a (CONR<SUB>8</SUB>NR<SUB>9</SUB>R<SUB>10</SUB>) group, R<SUB>8 </SUB>and R<SUB>9 </SUB>may be linked to form a heterocyclic group; and R<SUB>11</SUB>, 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 A<SUB>2A </SUB>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.
申请公布号 ZA200305116(B) 申请公布日期 2004.07.01
申请号 ZA20030005116 申请日期 2003.07.01
申请人 VERNALIS RESEARCH LIMITED 发明人 ROGER JOHN GILLESPIE;JOANNE LERPINIERE;CLAIRE ELIZABETH DAWSON;SUNEEL GAUR;ROBERT MARK PRATT;GEMMA CAROLINE STRATTON;SCOTT MURRAY WEISS
分类号 A61K31/198;A61K31/52;A61K31/695;A61K45/00;A61P25/00;A61P25/04;A61P25/08;A61P25/14;A61P25/16;A61P25/24;A61P25/28;A61P43/00;C07D473/00;C07D473/28;C07D473/32;C07D473/36;C07D473/40 主分类号 A61K31/198
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