发明名称 ANTI-NONMELANOMA CARCINOMA COMPOUNDS, COMPOSITIONS, AND METHODS OF USE THEREOF
摘要 <p>Compounds and compositions of Formula (I) are described, useful as anti- proliferative agents, and in particular anti-nonmelanoma carcinoma agents, wherein: Y<SUP>1A</SUP> and Y<SUP>1B</SUP> are independently Y<SUP>1</SUP>; R<SUP>X1</SUP> and R<SUP>X2</SUP> are independently R<SUP>X</SUP>; Y<SUP>1</SUP> is =O, -O(R<SUP>X</SUP>), =S, -N(R<SUP>X</SUP>), -N(O)(R<SUP>X</SUP>), -N(OR<SUP>X</SUP>), -N(O)(OR<SUP>X</SUP>), or -N(N(R<SUP>X</SUP>)( R<SUP>X</SUP>)); R<SUP>X</SUP> is independently R<SUP>1</SUP>, R<SUP>2</SUP>, R<SUP>4</SUP>, W<SUP>3</SUP>, or a protecting group; R<SUP>1</SUP> is independently -H or alkyl of 1 to 18 carbon atoms; R<SUP>2</SUP> is independently R<SUP>3</SUP> or R<SUP>4</SUP> wherein each R<SUP>4</SUP> is independently substituted with 0 to 3 R<SUP>3</SUP> groups or taken together at a carbon atom, two R<SUP>2</SUP> groups form a ring of 3 to 8 carbons and the ring may be substituted with 0 to 3 R<SUP>3</SUP> groups; R<SUP>3</SUP> is R<SUP>3a</SUP>, R<SUP>3b</SUP>, R<SUP>3c</SUP> or R<SUP>3d</SUP>, provided that when R<SUP>3</SUP> is bound to a heteroatom, then R<SUP>3</SUP> is R<SUP>3c</SUP> or R<SUP>3d</SUP>; R<SUP>3a</SUP> is -H, -F, -CI, -Br, -I, -CF<SUB>3</SUB>, -CN, N<SUB>3</SUB>, -NO<SUB>2</SUB>, or -OR<SUP>4</SUP>; R<SUP>3b</SUP> is =O, -O(R<SUP>4</SUP>), =S, -N(R<SUP>4</SUP>), -N(O)(R<SUP>4</SUP>), -N(OR<SUP>4</SUP>), -N(O)(OR<SUP>4</SUP>), or -N(N(R<SUP>4</SUP>) (R<SUP>4</SUP>)); R<SUP>3c</SUP> is - R<SUP>4</SUP>, -N(R<SUP>4</SUP>)(R<SUP>4</SUP>), -SR<SUP>4</SUP>, -S(O)R<SUP>4</SUP>, -S(O)<SUB>2</SUB>R<SUP>4</SUP>, -S(O)(OR<SUP>4</SUP>), -S(O)<SUB>2</SUB>(OR<SUP>4</SUP>), - OC(R<SUP>3b</SUP>)R<SUP>4</SUP>, OC(R<SUP>3b</SUP>)OR<SUP>4</SUP>, -OC(R<SUP>3b</SUP>)(N(R<SUP>4</SUP>)(R<SUP>4</SUP>)), -SC(R<SUP>3b</SUP>)R<SUP>4</SUP>, -SC(R<SUP>3b</SUP>)OR<SUP>4</SUP>, - SC(R<SUP>3b</SUP>)(N(R<SUP>4</SUP>)(R<SUP>4</SUP>)), -N(R<SUP>4</SUP>)C(R<SUP>3b</SUP>)R<SUP>4</SUP>, -N(R<SUP>4</SUP>)C(R<SUP>3b</SUP>)OR<SUP>4</SUP>, -N(R<SUP>4</SUP>)C(R<SUP>3b</SUP>)(N(R<SUP>4</SUP>)(R<SUP>4</SUP>)), W<SUP>3</SUP> -or R<SUP>5</SUP>W<SUP>3</SUP> ; R<SUP>3d</SUP> is -C(R<SUP>3b</SUP>)R<SUP>4</SUP>, -C(R<SUP>3b</SUP>)OR<SUP>4</SUP>, -C(R<SUP>3b</SUP>)W<SUP>3</SUP>, -C(R<SUP>3b</SUP>)OW<SUP>3</SUP> or -C(R<SUP>3b</SUP>)(N(R<SUP>4</SUP>)(R<SUP>4</SUP>)); R<SUP>4</SUP> is -H, or an alkyl of 1 to 18 carbon atoms, alkenyl of 2 to 18 carbon atoms, or alkynyl of 2 to 18 carbon atoms; R<SUP>5 </SUP>is alkylene of 1 to 18 carbon atoms, alkenylene of 2 to 18 carbon atoms, or alkynylene of 2 to 18 carbon atoms; W<SUP>3</SUP> is W<SUP>4</SUP> or W<SUP>5</SUP>; W<SUP>4</SUP> is R<SUP>6</SUP>, -C(R<SUP>3b</SUP>)R<SUP>6</SUP>, -C(R<SUP>3b</SUP>)W<SUP>5</SUP>, -SO<SUB>M2</SUB>R<SUP>6</SUP>, or -SO<SUB>M2</SUB>W<SUP>5</SUP>, wherein R<SUP>6</SUP> is R<SUP>4</SUP> wherein each R<SUP>4</SUP> is substituted with 0 to 3 R<SUP>3</SUP> groups; W<SUP>5</SUP> is carbocycle or heterocycle wherein W<SUP>5</SUP> is independently substituted with 0 to 3 R<SUP>2</SUP> groups; and M2 is 0, 1 or 2; and pharmaceutically acceptable salts thereof.</p>
申请公布号 WO2007002808(A1) 申请公布日期 2007.01.04
申请号 WO2006US25311 申请日期 2006.06.29
申请人 GILEAD SCIENCES, INC.;SHIBATA, RIRI 发明人 SHIBATA, RIRI
分类号 C07F9/6561;A61K31/675;A61P35/00 主分类号 C07F9/6561
代理机构 代理人
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