The present invention is directed to a method of preparing bromoisoquinoline derivatives, in particular 5- or 8-bromoisoquinoline derivatives. Bromoisoquinoline derivatives, and in particular 5-bromoisoquinoline and 5-bromo-8-nitroisoquinoline derivatives, are key intermediates in the synthesis of pharmaceutical compounds.

Optically active 1-(p-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline having the formula (I) is prepared by asymmetric hydrogenation of the corresponding 3,4,5,6,7,8-hexahydro-compound or of the new 1-(p-methoxybenzyl)-3,4,5,6,7,8-hexahydroisoquinoline dihydrogenated phosphate in the present of chiral iridium-phosphine complexes. This product is an intermediate product in the synthesis of cough-relieving dextromethorphanne and analgesic levorphanol. ##STR1##

Compounds having the formula: ##STR1## are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions, methods for the preparation of urokinase-inhibitors, and a method of inhibiting urokinase in a mammal.

Methods of preparing an amino-substituted-tetrahydroisoquinoline-sulfonamide hydroxamic acid include the steps of providing an amino-substituted-tetrahydroisoquinoline-carboxylate attached to a solid support; reacting the ring nitrogen of the amino-tetrahydroisoquinoline-carboxylate with a sulfonyl chloride; and cleaving the intermediate from the solid support to form an amino-tetrahydroisoquinoline-sulfonamide hydroxamic acid.

1,2,3,4-Tetrahydroisoquinoline compounds having 7 and 8 halo substituents are inhibitors of phenylethanolamine N-methyltransferase.

Substituted carbocyclic sulphonamide derivatives of formula (I), in which n is 0 or 1 and the other variables are as defined in the claims, are selective 5-HT.sub.7 receptor antagonists and are thereby effective in the treatment of a variety of neurological conditions, including depression and sleep disorders. ##STR00001##

The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders.

The present invention relates to novel substituted tetrahydroisoquinoline compounds, pharmaceutical compositions containing the compounds, methods of making the compounds, and methods of using the compounds to destroy a target cell, such as a cancer cell, and to treat or prevent a cancerous condition.

The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline propyl sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders.

An objective of the present invention is to provide compounds having Rho kinase inhibitory activity. The compounds according to the present invention are those represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: Het--X--Z (I) wherein Het represents a monocyclic or bicyclic heterocyclic group containing at least one nitrogen atom, for example, pyridyl or phthalimide; X represents group (i) --NH--C(.dbd.O)--NH--Q1-, group (ii) --NH--C(.dbd.O)--Q2-, wherein Q1 and Q...