4-amino-N-(4-methyl-4-piperidinyl)-2-methoxybenzamides
AssigneeJanssen Pharmaceutica NV
InventorsJosepha Eduarda Maria Francisca Leysen, Georges Henri Paul Van Daele
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Abstract
Piperidinyl substituted benzamides of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof and the stereoisomeric forms thereof, wherein R.sup.1 is hydrogen or halo; R.sup.2 is halo; R.sup.3 is hydrogen or halo; R.sup.4 and R.sup.5 each independently are hydrogen, C.sub.1-4 alkyl or haloC.sub.1-4 alkyl; and the group NR.sup.4 R.sup.5 may also be azido, Alk is C.sub.2-4 alkanediyl; pharmaceutical compositions containing said compounds of formula (I) as active ingredient; use of said compounds as a medicine; process of preparing said compounds; compounds of formula (I) containing a radioactive isotope; process of marking 5HT.sub.2 -receptor sites; and process for imaging an organ are disclosed.
Claims4
A process of marking a 5HT.sub.2 -receptor with a radiolabeled compound comprising the steps of:
- (a) radiolabeling a compound of the formula:
- ##STR7## a pharmaceutically acceptable acid addition salt thereof or a stereoisomeric form thereof, wherein:
- R.sup.1 represents hydrogen or halo;
- R.sup.2 represents halo;
- R.sup.3 represents hydrogen or halo;
- --NR.sup.4 R.sup.5 represents azido;
- and
- Alk represents C.sub.2-4 alkanediyl,
- (b) administering said radiolabeled compound to biological material,
- (c) irradiating the receptor/marker complex with UV-light, and
- (d) detecting the emissions from the covalently bonded radiolabeled compound.
Dependencies are inferred from the claim text.