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US 5,047,410 AGranted
Indolyl derivatives and their use as 5-HT.sub.3, receptor antagonists
AssigneeIstituto de Angeli S.p.A.
InventorsArturo Donetti, Marco Turconi, Massimo Nicola, Rosamaria Micheletti
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Abstract
New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## , wherein the substituents are defined hereinbelow, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.
Claims8
Compound of general formula (I) ##STR15## wherein A is ##STR16## wherein R.sub.3 is H, halogen, C.sub.1-6 alkoxy
- R.sub.4 is H, C.sub.1-6 alkyl
- X is --O-- or --NH--
- B is a group selected from ##STR17## wherein m is 1, 2
- p is 0, 1, 2,
- q is 0, 1, 2, 3
- R.sub.5 is H, C.sub.1-6 alkyl
- R is H, C.sub.1-6 alkyl optionally substituted by halogen, NR.sub.6 R.sub.7 in which R.sub.6 is H, C.sub.1-6 alkyl, NO.sub.2, CN and R.sub.7 is H, C.sub.1-6 alkyl;
- R.sub.1 is H, C.sub.1-6 alkyl optionally substituted by halogen, CN, or tautomers thereof, optical isomers thereof and acid addition salts thereof.
5 more elements
Dependencies are inferred from the claim text.