摘要 |
<p>Indazolecarboxamides are used as antagonists and partial agonists for the serotonin receptor 5-HT4 and provide therapeutic methods for treatment of disorders caused by or affected by dysfunction of the 5-HT4 receptor. The indazolecarboxamides are of the formula <CHEM> wherein: R is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl; R<1> is hydrogen, halo, C1-C4 alkyl, hydroxy, C1-C4 alkoxy or alkylthio, cyano, trifluoromethyl, carboxamido, mono- or di(C1-C4 alkyl)carboxamido; m, n and o are independently 0-5, provided that the sum of m, n and o is 2-5; R<2> is hydrogen or C1-C4 alkyl; R<3> and R<4> combine with the nitrogen atom to which they are attached to form 1-pyrrolidinyl, 1-piperazinyl, 1,2,3,4-tetrahydro-2-isoquinolinyl, 2,3-dihydro-1-indolinyl, 4-morpholinyl, 1-piperidinyl or 1-hexamethyleneiminyl, substituted with phenyl, naphthyl, (phenyl or naphthyl) (C1-C3 alkyl), (phenyl or naphthyl) (C1-C3 alkanoyl), amino, mono- or di(C1-C4 alkyl)amino, or a group of the formula -NH-Y-R<5>; provided that a piperazinyl or morpholinyl group may not be substituted with amino, mono- or di(C1-C4 alkyl)amino, or -NH-Y-R<5>; wherein a phenyl or naphthyl group is unsubstituted or substituted with 1-3 halo, C1-C3 alkyl or C1-C3 alkoxy groups; Y is carbonyl, sulfonyl, aminocarbonyl or oxycarbonyl; R<5> is C1-C6 alkyl, C3-C8 cycloalkyl, C6-C11 bicyclo- or tricycloalkyl, (phenyl or naphthyl)(C1-C3 alkyl), phenyl or naphthyl; wherein a cycloalkyl, bicyclo- or tricycloalkyl, phenyl or naphthyl group is unsubstituted or substituted with 1-3 hydroxy, halo, C1-C3 alkyl or C1-C3 alkoxy groups; or a pharmaceutically acceptable salt thereof.</p> |
申请人 |
ELI LILLY AND COMPANY |
发明人 |
CATLOW, JOHN THOMAS;COHEN, MARLENE LOIS;MARTINELLI, MICHAEL JOHN;SCHAUS, JOHN MEHNERT;SWANSON, STEVEN PHILLIP;THOMPSON, DENNIS CHARLES;WILSON, THOMAS MICHAEL |