发明名称 Substituted indoles and their use as integrin antagonists
摘要 The present invention relates to novel substituted indole compounds that are antagonists of alpha V (alphav) integrins, for example alphavbeta<SUB>3 </SUB>and alpha<SUB>v</SUB>beta<SUB>5 </SUB>integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by alpha<SUB>v</SUB>beta<SUB>3 </SUB>and alpha<SUB>v</SUB>beta<SUB>5 </SUB>integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R<SUP>1</SUP>, R<SUP>2</SUP>, R<SUP>3</SUP>, R<SUP>4</SUP>, R<SUP>5</SUP>, R<SUP>6</SUP>, R<SUP>7</SUP>, R<SUP>8</SUP>, R<SUP>9</SUP>, R<SUP>10</SUP>, R<SUP>11</SUP>, , R<SUP>12</SUP>, R<SUP>13</SUP>, R<SUP>14</SUP>, D, X, W, a, m, n, i, j, k and v are defined herein.
申请公布号 US2005250771(A1) 申请公布日期 2005.11.10
申请号 US20040005294 申请日期 2004.12.06
申请人 发明人 LU TIANBO;TOMCZUK BRUCE E.;LAFRANCE LOUIS V.;MARKOTAN THOMAS P.;MARUGAN SANCHEZ JUAN J.;MARDER VICTOR J.;U'PRICHARD DAVID C.;ANACLERIO BETH M.;GUO ZIHONG;PAN WENZI;LEONARD KRISTI A.
分类号 A61K31/404;A61K31/4375;A61K31/4439;A61K31/4709;A61K31/5383;A61P3/06;A61P3/10;A61P7/06;A61P9/00;A61P9/10;A61P19/10;A61P25/00;A61P25/04;A61P25/08;A61P25/18;A61P25/22;A61P27/02;A61P29/00;A61P35/00;A61P43/00;C07D209/08;C07D213/74;C07D401/12;C07D401/14;C07D403/12;C07D471/04;C07D498/04;(IPC1-7):A61K31/538;A61K31/506;A61K31/474;A61K31/443;A61K31/405;C07D413/02;C07D43/02 主分类号 A61K31/404
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