GHRELIN RECEPTOR MODULATORS

摘要

Compounds of Formula (IA) or (IB) modulate ghrelin receptor activity, and are useful in the treatment of, for example, obesity and eating disorders: wherein W is, in either orientation, -C(=O)N(R<SUB>3</SUB>)-, or -C(=O)O-; R is hydrogen or C<SUB>1</SUB>-C<SUB>4</SUB> alkyl; R<SUB>1</SUB> is selected from hydrogen, (C<SUB>1</SUB>-C<SUB>4</SUB>)alkyl, cycloalkyl, fully or partially fluorinated (C<SUB>1</SUB>-C<SUB>4</SUB>)alkyl, or -OR<SUB>10</SUB>; and R<SUB>2</SUB> is selected from (i) hydrogen and (ii) (C<SUB>1</SUB>-C<SUB>4</SUB>)alkyl, cycloalkyl, cycloalkenyl, and non aromatic heterocyclyl, each optionally substituted by -F, -CN, C<SUB>1</SUB>-C<SUB>4</SUB> alkyl, cyclopropyl, -NR<SUB>7</SUB>COR<SUB>0</SUB>, -NR<SUB>7</SUB>SO<SUB>2</SUB>R<SUB>0</SUB>, -COR<SUB>0</SUB>, -COOH, -SOR<SUB>9</SUB>, -SO<SUB>2</SUB>R<SUB>0</SUB>, -OR<SUB>10</SUB>, -NR<SUB>7</SUB>R<SUB>8</SUB>, or -NR<SUB>7</SUB>COOR<SUB>8</SUB>; and (iii) aryl, aryl-(C<SUB>1</SUB>-C<SUB>2</SUB>)alkyl-, heteroaryl and heteroaryl-(C<SUB>1</SUB>-C<SUB>2 </SUB>alkyl)- each optionally substituted in the ring part or R<SUB>1</SUB> and R<SUB>2</SUB>, together with the nitrogen to which they are attached, form an optionally substituted cyclic amino group; R<SUB>3</SUB> is selected from hydrogen, (C<SUB>1</SUB>-C<SUB>4</SUB>)alkyl, cycloalkyl, fully or partially fluorinated (C<SUB>1</SUB>-C<SUB>4</SUB>)aIkyl, or -OR<SUB>10</SUB>; and R<SUB>4 </SUB>is selected from (iv) hydrogen and (v) (C<SUB>1</SUB>-C<SUB>4</SUB>)alkyl, cycloalkyl, and non aromatic heterocyclyl, each optionally substituted by -F, -CN, -NR<SUB>7</SUB>COR<SUB>0</SUB>, -NR<SUB>7</SUB>SO<SUB>2</SUB>R<SUB>0</SUB>, -COR<SUB>0</SUB>, - COOH, -SOR<SUB>9</SUB>, -SO<SUB>2</SUB>R<SUB>0</SUB>, -OR<SUB>10</SUB>, -NR<SUB>7</SUB>R<SUB>8</SUB>, or -NR<SUB>7</SUB>COOR<SUB>8</SUB>; and (vi) aryl, aryl-(C<SUB>1</SUB>-C<SUB>2</SUB>)alkyl-, heteroaryl and heteroaryl-(C<SUB>1</SUB>-C<SUB>2</SUB> alkyl)- each optionally substituted in the ring part thereof; or R<SUB>3</SUB> and R<SUB>4</SUB>, together with the nitrogen to which they are attached, form an optionally substituted cyclic amino group; L is a linker radical of formula -(CR<SUB>11</SUB>R<SUB>13</SUB>)<SUB>a</SUB>B(CR<SUB>12</SUB>R<SUB>14</SUB>)b- as defined in the specification; R<SUB>0</SUB>, R<SUB>7</SUB>, R<SUB>8</SUB>, R<SUB>9</SUB> and R<SUB>10</SUB> are as defined in the specification.