Stable hydrate of a muscarinic receptor antagonist
AssigneeNovartis International Pharmaceutical Ltd.
InventorsPeter James Dunn, John George Matthews, Trevor Jack Newbury, Garry O'Connor
Life of this patent
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Abstract
A stable solid hydrate of a muscarinic receptor antagonist is useful in the treatment of irritable bowel syndrome, diverticular disease, oesophageal achalasia, chronic obstructive airways disease, over active bladder (including symptoms of incontinence, urge and frequency), urinary incontinence, neurogenic urinary urgency or pollakiuria, treatment of bladder functional disorder, urinary leakage, painful or difficult urination caused by neurogenic bladder, spastic or hypertonic bladder, dysfunctional bladder syndrome, gastrointestinal disorders including gastrointestinal hyperactivity, and relaxing effect on intestinal smooth muscle cells.
Claims23
A stable solid hydrate of darifenacin.
A hydrate according any of the preceding claims characterised by an infra-red spectrum, run using single reflection ATR (attenuated total reflectance), which shows significant absorption bands at νmax (cm−1):
- 3625, 3516, 3440, 2948, 2806, 1699, 1622, 1597, 1578, 1488, 1471, 1445, 1378, 1353, 1325, 1312, 1280, 1242, 1196, 1152, 1119, 1102, 1086, 1024, 981, 939, 925, 900.
A hydrate according to any of the preceding claims which is characterised by a powder X-ray diffraction pattern obtained using copper radiation (λ=0.15405 nm) which shows main peaks at 8.39, 10.519, 13.272, 13.693, 15.908, 16.289, 16.855, 19.637, 21.135, 21.55, 21.722, 23.006, and 26.284 degrees 2θ.
A hydrate according to any of the preceding claims which is characterised by a differential scanning calorimetry. (DSC) trace showing a sharp endotherm at 101° C. at a scan rate of 20° C./min.
A pharmaceutical composition comprising a hydrate according to any of the preceding claims together with a pharmaceutically acceptable excipient, diluent or carrier.
A solvate of darifenacin of the formula (VIII):
Dependencies are inferred from the claim text.