Novel compounds

Abstract

Compounds of formula (I) wherein R 1 is 2-indanyl, R 2 is 1-methylpropyl, R 3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R 4 represents methyl and R 5 represents hydrogen or methyl or, R 4 and R 5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.

1 . A method of treating benign prostatic hyperplasia, which method comprises administering to a human in need thereof an effective amount of (3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethyl-3-pyridinyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]-2,5-piperazinedione or a pharmaceutically acceptable salt thereof wherein said pharmaceutically acceptable salt is an acid addition salt where the acid is selected from hydrochloric, hydrobromic, nitric, phosphoric, sulphuric, methanesulfonic, ethanesulfonic, benzenesulfonic, p-toluenesulfonic, citric, tartaric, lactic, pyruvic, acetic, succinic, fumaric and maleic acid. 
     
     
         2 . A method of treating benign prostatic hyperplasia, which method comprises administering to a human in need thereof an effective amount of (3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethyl-3-pyridinyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]-2,5-piperazinedione benzenesulfonate salt. 
     
     
         3 . A method of treating benign prostatic hyperplasia, which method comprises administering to a human in need thereof an effective amount of a solvate of (3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethyl-3-pyridinyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]-2,5-piperazinedione benzenesulfonate salt with a pharmaceutically acceptable solvent selected from the group consisting of ethanol, iso-propanol, acetone and ethyl acetate. 
     
     
         4 . A method of treating benign prostatic hyperplasia, which method comprises administering to a human in need thereof an effective amount of a hydrate of (3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethyl-3-pyridinyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]-2,5-piperazinedione benzenesulfonate salt.