发明名称 PYRROLOPYRIMIDINE A2B SELECTIVE ANTAGONIST COMPOUNDS, THEIR SYNTHESIS AND USE
摘要 The subject invention provides compounds having the structure: wherein, R<SUB>1 </SUB>is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, -C(-O)NR<SUB>a</SUB>R<SUB>b</SUB>, -NR<SUB>a</SUB>R<SUB>b</SUB>, -NR<SUB>a</SUB>C(-O)NR<SUB>a</SUB>R<SUB>b</SUB>, -NR<SUB>a</SUB>C(-O)OR<SUB>a</SUB>, -OC(-O)NR<SUB>a</SUB>R<SUB>b</SUB>, or -NH C(-O) R<SUB>a</SUB>; R<SUB>2 </SUB>is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, -C(-O)NR<SUB>a</SUB>R<SUB>b</SUB>, -NR<SUB>a</SUB>R<SUB>b</SUB>, -NR<SUB>a</SUB>C(-O)NR<SUB>a</SUB>R<SUB>b</SUB>, -NR<SUB>a</SUB>C(-O)OR<SUB>a</SUB>, -OC(-O)NR<SUB>a</SUB>R<SUB>b</SUB>, or -NHC(-O)R<SUB>a</SUB>, or R<SUB>1</SUB>, R<SUB>2 </SUB>and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with -(CH<SUB>2</SUB>)<SUB>2</SUB>OH or -CH<SUB>2</SUB>C(-O)OH; R<SUB>3 </SUB>is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C<SUB>1</SUB>-C<SUB>15</SUB>)alkyl, (C<SUB>1</SUB>-C<SUB>15</SUB>)alkoxy, or -NR<SUB>a</SUB>R<SUB>b</SUB>; R<SUB>4 </SUB>is hydrogen or substituted or unsubstituted (C<SUB>1</SUB>-C<SUB>15</SUB>)alkyl; R<SUB>5 </SUB>is -(CH<SUB>2</SUB>)<SUB>m</SUB>OR<SUB>6</SUB>, -CHNOR<SUB>7</SUB>, -C(-O)NR<SUB>8</SUB>R<SUB>9</SUB>, -(CH<SUB>2</SUB>)<SUB>m</SUB>C(-O)OR<SUB>10</SUB>, -(CH<SUB>2</SUB>)<SUB>k</SUB>C(-O)NR<SUB>11</SUB>R<SUB>12</SUB>; wherein R<SUP>6 </SUP>is a substituted or unsubstituted (C<SUB>1</SUB>-C<SUB>30</SUB>)alkyl, (C<SUB>3</SUB>-C<SUB>10</SUB>)cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R<SUB>7 </SUB>is hydrogen, or a substituted or unsubstituted (C<SUB>1</SUB>-C<SUB>30</SUB>)alkyl, (C<SUB>1</SUB>-C<SUB>30</SUB>)alkylaryl; R<SUB>8 </SUB>and R<SUB>9 </SUB>are each independently hydrogen, or a substituted or unsubstituted (C<SUB>1</SUB>-C<SUB>30</SUB>)alkyl, (C<SUB>1</SUB>-C<SUB>30</SUB>)alkylaryl, (C<SUB>1</SUB>-C<SUB>30</SUB>)alkylamino, (C<SUB>1</SUB>-C<SUB>30</SUB>)alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R<SUB>8</SUB>, N, and R<SUB>9 </SUB>together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R<SUB>10 </SUB>is hydrogen or a substituted or unsubstituted (C<SUB>1</SUB>-C<SUB>30</SUB>)alkyl, (C<SUB>3</SUB>-C<SUB>10</SUB>)cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R<SUB>11</SUB>, N and R<SUB>12 </SUB>together form a 4-8 membered heterocyclic ring; R<SUB>a </SUB>and R<SUB>b </SUB>are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3, or a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A<SUB>2b </SUB>adenosine receptor in a subject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.
申请公布号 US2008261943(A1) 申请公布日期 2008.10.23
申请号 US20070536119 申请日期 2007.06.19
申请人 OSI PHARMACEUTICALS, INC. 发明人 CASTELHANO ARLINDO;MCKIBBEN BRYAN;STEINIG ARNO
分类号 A61K31/519;A61P1/04;A61P1/12;A61P3/10;A61P9/00;A61P9/10;A61P9/12;A61P11/06;A61P13/00;A61P17/00;A61P17/04;A61P19/02;A61P27/02;A61P29/00;A61P35/00;A61P35/04;A61P37/08;A61P43/00;C07D487/04 主分类号 A61K31/519
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