发明名称 Therapeutic quinazoline derivatives
摘要 A compound of formula (I) or a salt, ester, amide or prodrug thereof; where X is O, or S, S(O), S(O)<SUB>2 </SUB>or NR<SUP>6 </SUP>where R<SUP>6 </SUP>is hydrogen of C<SUB>1-6</SUB>alkyl; R<SUP>5 </SUP>is an optionally substituted 6-membered aromatic ring containing at least one nitrogen atom, and R<SUP>1</SUP>, R<SUP>2</SUP>, R<SUP>3</SUP>, R<SUP>4 </SUP>are independently selected from halogeno, cyano, nitro, C<SUB>1-3</SUB>alkylsulphanyl, -N(OH)R<SUP>7</SUP>- (wherein R<SUP>7 </SUP>is hydrogen, or C<SUB>1-3</SUB>alkyl), or R<SUP>9</SUP>X<SUP>1</SUP>- (wherein X<SUP>1 </SUP>represents a direct bond, -O-, -CH<SUB>2</SUB>-, -OC(O), -C(O)-, -S-, -SO-, -SO<SUB>2</SUB>-, -NR<SUP>10</SUP>C(O)-, -C(O)NR<SUP>11</SUP>-, -SO<SUB>2</SUB>NR<SUP>12</SUP>-, -NR<SUP>13</SUP>SO<SUB>2</SUB>- or NR<SUP>14</SUP>- (wherein R<SUP>10</SUP>, R<SUP>11</SUP>, R<SUP>12</SUP>, R<SUP>13 </SUP>and R<SUP>14 </SUP>each independently represents hydrogen, C<SUB>1-3</SUB>alkyl or C<SUB>1-3</SUB>alkoxyC<SUB>2-3</SUB>alkyl), and R<SUP>9 </SUP>is hydrogen, optionally substituted hydrocarbyl, optionally substituted heterocyclyl or optionally substituted alkoxy; provided that at least one of R<SUP>2 </SUP>or R<SUP>3 </SUP>is other than hydrogen. These compounds inhibit aurora 2 kinase and are useful in the preparation of medicaments for the treatment of proliferative disease such as cancer.
申请公布号 US7235559(B1) 申请公布日期 2007.06.26
申请号 US20000088856 申请日期 2000.09.19
申请人 ASTRAZENECA AB 发明人 MORTLOCK ANDREW AUSTEN;KEEN NICHOLAS JOHN
分类号 A61P35/00;A61K31/517;A61K31/5377;A61K31/661;A61P43/00;C07D239/94;C07D401/12;C07D401/14;C07D403/12;C07D403/14;C07D405/14;C07D409/14;C07D413/14 主分类号 A61P35/00
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