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US 5,204,341 AGranted
1-arylsulphonyl-2-pyrrolidone derivatives, their preparation process and the new intermediates obtained, their use as medicaments and the pharmaceutical compositions containing them
AssigneeRoussel Uclaf
InventorsEmilio Toja, Carla Bonetti, Fernando Barzaghi, Giulio Galliani
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Abstract
1-arylsulphonyl-2-pyrrolidone derivatives for treating spasmodic disorders in gastro-enterology, in gynaecology, in obstetrics, in urology; intermediates in the preparation of such products; methods for preparing such products and pharmaceutical preparations containing such products.
Claims14
A compound of formula (I):
- ##STR14## in which the OH radical is in the 3 or 4 position,
- X represents oxygen or sulphur,
- R represents a radical ##STR15## R.sub.1 and R.sub.2 are identical or different from each other, and each represents a saturated or unsaturated alkyl radical containing up to 8 carbon atoms or form together with the nitrogen atom to which they are linked a heterocyclic radical selected from the group consisting of piperidyl, piperazinyl, hexahydro azepinyl, morpholinyl and pyrrolidinyl;
- or a compound of formula (I) having a functional derivative of the hydroxyl in the 3 or 4 position which is metabolized in vivo into the corresponding hydroxylated derivative.
1 more element
A compound selected from the group consisting of:
- 4-hydroxy-1[[4-(1-piperidinyl)-phenyl]-sulphonyl]-2-pyrrolidinethione;
- 1-[[4-(hexahydro-1H-azepin-1-yl)-phenyl]-sulphonyl]-4-hydroxy-2-pyrrolidino ne;
- and
- 1-[[4-(hexahydro-1H-azepin-1-yl)-phenyl]-sulphonyl]-4-hydroxy-2-pyrrolidine thione.
1 more element
Dependencies are inferred from the claim text.