摘要 |
<p>The invention relates to 4-cycloalkyl-pyrimidine-2-carbonitrile derivatives having the general formula (I) wherein n is 0, 1, 2 or 3; R<SUB>1</SUB> is H or (C<SUB>1-6</SUB>)alkyl; R<SUB>2</SUB> is (C<SUB>2-6</SUB>)alkyl, optionally substituted with one or more halogens, OH, (C<SUB>1-4</SUB>)alkyloxy or NR<SUB>3</SUB>R<SUB>4</SUB>; R<SUB>3</SUB> and R<SUB>4</SUB> are independently H, (C<SUB>1-4</SUB>)alkyl, (C<SUB>3-8</SUB>)cycloalkyl, (C<SUB>3-8</SUB>)cycloalkyl(C<SUB>1-4</SUB>)alkyl, (C<SUB>6-10</SUB>)aryl, (C<SUB>6-10</SUB>)aryl(C<SUB>1-4</SUB>)alkyl, (C<SUB>2-9</SUB>)heteroaryl, (C<SUB>2-9</SUB>)heteroaryl(C<SUB>1-4</SUB>)alkyl or (C<SUB>1-4</SUB>)alkyl substituted with a 4-8 membered saturated heterocyclic ring comprising 1-3 heteroatoms selected from O, S and NR<SUB>5</SUB>; or R<SUB>3</SUB> and R<SUB>4</SUB> together with the nitrogen to which they are bound form a 4-8 membered saturated heterocyclic ring, which ring optionally comprises NR<SUB>5</SUB>, and which ring is optionally substituted with (C<SUB>6-10</SUB>)aryl, (C<SUB>6-10</SUB>)aryloxy, (C<SUB>6-10</SUB>)aryl(C<SUB>1-4</SUB>)alkyloxy, (C<SUB>2-9</SUB>)heteroaryl, NR<SUB>6</SUB>,R<SUB>7</SUB>, CONR<SUB>6</SUB>R<SUB>7</SUB> or NR<SUB>6</SUB>COR<SUB>7</SUB>; R<SUB>5</SUB> is H, (C<SUB>1-4</SUB>)alkyl, (C<SUB>6-10</SUB>)aryl, (C<SUB>6-10</SUB>)aryl(C<SUB>1-4</SUB>)alkyl, (C<SUB>2-5</SUB>) heteroaryl or (C<SUB>2-5</SUB>)heteroaryl(C<SUB>1-4</SUB>)alkyl; R<SUB>6</SUB> and R<SUB>7</SUB> are independently H or (C<SUB>1-4</SUB>)alkyl; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said compounds as well as to the use thereof in the treatment of osteoporosis, atherosclerosis and related disorders.</p> |