发明名称 THERAPEUTIC QUINAZOLINE DERIVATIVES
摘要 <p>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.</p>
申请公布号 EP1218355(A1) 申请公布日期 2002.07.03
申请号 EP20000960850 申请日期 2000.09.19
申请人 ASTRAZENECA AB 发明人 MORTLOCK, ANDREW, AUSTEN;KEEN, NICHOLAS, JOHN
分类号 A61K31/517;A61K31/5377;A61K31/661;A61P35/00;A61P43/00;C07D239/94;C07D401/12;C07D401/14;C07D403/12;C07D403/14;C07D405/14;C07D409/14;C07D413/14;(IPC1-7):C07D239/94 主分类号 A61K31/517
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