| 摘要 |
The present invention relates to 6-substituted isoquinoline derivatives having the general Formula I wherein X is O, S or NH; Y is OH or NH<SUB>2</SUB>; m is 0, 1 or 2; n is 0 or 1; o is 0 or 1; R<SUB>1 </SUB>is H, when Y is NH<SUB>2</SUB>; or R<SUB>1 </SUB>is H, (C<SUB>1-4</SUB>)alkyl or halogen, when Y is OH; R<SUB>2 </SUB>and R<SUB>3 </SUB>are independently H, (C<SUB>1-4</SUB>)alkyl or halogen; R<SUB>4 </SUB>is H or (C<SUB>1-6</SUB>)alkyl, optionally substituted with halogen, (C<SUB>3-7</SUB>)cycloalkyl, (C<SUB>6-10</SUB>)aryl or a saturated 5- or 6-membered heterocyclic ring comprising 1-3 heteroatoms independently selected from O, S and N, the (C<SUB>6-10</SUB>)aryl and heterocyclic ring being optionally substituted with (C<SUB>1-4</SUB>)alkyl, (C<SUB>1-4</SUB>)alkyloxy or halogen; R<SUB>5 </SUB>is H or (C<SUB>1-4</SUB>)alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that the compounds of Formula I wherein X is O, Y is OH , n is 0 and m+o=2 are excluded, to pharmaceutical compositions comprising the same, as well as to the use of said 6-substituted isoquinoline derivatives for the preparation of a medicament for the treatment of ROCK-I related disorders such as glaucoma, hypertension and atherosclerosis.
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