发明名称 ПРОИЗВОДНЫЕ ГЕТЕРОЦИКЛИЧЕСКИХ АМИДОВ, ОБЛАДАЮЩИЕ ИНГИБИТОРНОЙ АКТИВНОСТЬЮ В ОТНОШЕНИИ ГЛИКОГЕНФОСФОРИЛАЗЫ
摘要 Heterocyclic amides of formula (1) wherein: Z is CH or nitrogen; R<SUP>4 </SUP>and R<SUP>5 </SUP>together are either -S-C(R<SUP>6</SUP>)-C(R<SUP>7</SUP>)- or -C(R<SUP>7</SUP>)-C(R<SUP>6</SUP>)-S-; R<SUP>6 </SUP>and R<SUP>7 </SUP>are selected from for example hydrogen, halo, C<SUB>1-4</SUB>alkyl, and C<SUB>1-4</SUB>alkanoyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R<SUP>1 </SUP>is selected from for example halo, nitro, cyano, hydroxy, carboxy; r is 1 or 2; Y is -NR<SUP>2</SUP>R<SUP>3 </SUP>or -OR<SUP>3</SUP>; R<SUP>2 </SUP>and R<SUP>3 </SUP>are selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C<SUB>1-4</SUB>alkyl(optionally substituted by 1 or 2 R<SUP>8 </SUP>groups); R<SUP>4 </SUP>is selected from for example hydrogen, halo, nitro, cyano, hydroxy, C<SUB>1-4</SUB>alkyl, and C<SUB>1-4</SUB>alkanoyl; R<SUP>8 </SUP>is selected from for example hydroxy, -COCOOR<SUP>9</SUP>, -C(O)N(R<SUP>9</SUP>)(R<SUP>10</SUP>), -NHC(O)R<SUP>9</SUP>, (R<SUP>9</SUP>)(R<SUP>10</SUP>)N- and -COOR<SUP>9</SUP>; R<SUP>9 </SUP>and R<SUP>10 </SUP>are selected from for example hydrogen, hydroxy, C<SUB>1-4</SUB>alkyl (optionally substituted by 1 or 2 R<SUP>13</SUP>); R<SUP>13 </SUP>is selected from hydroxy, halo, trihalomethyl and C<SUB>1-4</SUB>alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are described.
申请公布号 RU2004125145(A) 申请公布日期 2005.06.10
申请号 RU20040125145 申请日期 2003.03.04
申请人 АстраЗенека АБ (SE) 发明人 УИТМОР Пол Роберт Оуэн (GB);БЕННЕТТ Стюарт Норман Лайл (GB);СИМПСОН Айан (GB)
分类号 A61K31/407;A61K31/4439;A61K31/496;A61K31/5377;A61P3/04;A61P3/10;A61P9/10;C07D495/04 主分类号 A61K31/407
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