发明名称 PANCREATIC LIPASE INHIBITOR COMPOUNDS, THEIR SYNTHESIS AND USE
摘要 The subject invention features compounds having the structure:, wherein X is O, S, CH<sb>2</sb> or NR<sb>5</sb>; Y is O or S; R<sb>1</sb> is H, substituted or unsubstituted C<sb>1</sb>­C<sb>15</sb> alkyl, C<sb>1</sb>−C<sb>8</sb> alkylaryl, −C(O)OR<sb>4</sb>, −C(O)NR<sb>4</sb>R<sb>5</sb>, −CR<sb>6</sb>R<sb>6'</sb>OR<sb>4</sb>,−CR<sb>6< /sb>R<sb>6'</sb>OC(O)R4, − CR<sb>6</sb>R<sb>6'</sb>OC(O)NHR<sb>7</sb>, −C(O)NR<sb>1o</sb>R<sb>11</sb>, −C(O)NR<sb>8</sb>R<sb>9 </sb>NR<sb>8</sb>R<sb>9</sb>, −N(R<sb>5</sb>)C(O)NHR<sb>5</sb>, or CH<sb>2</sb>R<sb>4</sb>; R<sb>2</sb> is a substituted or unsubstituted, straight chain C<sb>1</sb>−C<sb>30</sb> alkyl or branched C<sb>3</sb> C<sb>30</sb> alkyl, aryl, alkylaryl, arylalkyl, heteroarylalkyl or cycloalkyl; R<sb>3</sb> is H or substituted or unsubstituted C<sb>1</sb>−C<sb>6</sb> alkyl or C<sb>3</sb>−C<sb>10</sb> cycloalkyl; R<sb>4</sb> is H or a substituted or unsubstituted, straight chain or branched, C<sb>6</sb>−C<sb>30</sb> alkyl, aryl, −CH<sb>2</sb>−aryl, aryl −C<sb>1</sb>−C<sb>15</sb> alkyl, heteroaryl−C<sb>1</sb>−C<sb>15</sb>alkyl or C<sb>3</sb>−C<sb>10</sb> cycloalkyl; R<sb>5</sb> is H or a substituted or unsubstituted, straight chain or branched, C<sb>6</sb>−C<sb>30</sb> alkyl, aryl C<sb>1</sb>−C<sb>30</sb>alkyl, heteroarylalkyl or cycloalkyl; R<sb>6</sb> and R<sb>6'</sb> are each independently H, substituted or unsubstituted C<sb>1</sb>−C<sb>6</sb> alkyl, dialkyl or C<sb>3</sb>−C<sb>10</sb> cycloalkyl or together form a 3−7 membered ring system; R<sb>7</sb> is H or substituted or unsubstituted C<sb>1</sb>−C<sb>12</sb> alkyl or C<sb>3</sb>−C<sb>10</sb> cycloalkyl; R<sb>8</sb> and R<sb>9 </sb>are each independently H, substituted or unsubstituted C<sb>1</sb>−C<sb>6</sb> alkyl, C<sb>1</sb>−C<sb>6</sb> alkoxy, C<sb>1</sb>−C<sb>6 </sb>alkylaryl, or NR<sb>8</sb>R<sb>9</sb> together form a substituted piperazine or piperidine ring or a dihydro−1H−isoquinoline ring system, or a specific enantiomer thereof, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating diabetes or obesity by administering a therapeutically effective amount of the compounds of the invention.
申请公布号 WO03053944(A1) 申请公布日期 2003.07.03
申请号 WO2002US41272 申请日期 2002.12.20
申请人 OSI PHARMACEUTICALS, INC.;WITTER, DAVID;CASTELHANO, ARLINDO, L. 发明人 WITTER, DAVID;CASTELHANO, ARLINDO, L.
分类号 A61K31/519;A61K31/5365;A61K31/542;A61P3/04;A61P3/06;A61P3/10;A61P43/00;C07B61/00;C07D333/38;C07D333/40;C07D409/12;C07D495/04;C07D498/02;C07D498/04;C07D513/02;C07D513/04;(IPC1-7):C07D265/12;C07D279/08;A61K31/536 主分类号 A61K31/519
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