Crystalline drug form
AssigneePfizer Inc.
InventorsTerence Vernon Silk, Julian Duncan Smith
Life of this patent
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Abstract
The present invention relates to a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-β-D-ribofuranosyluronamide)-N-(2-{N′-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide and to a process for the preparation of, compositions containing and the uses of such a crystalline form.
Claims16
A method of agonising an A2a receptor in a mammal comprising administering to said mammal in need thereof an effective amount of a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-β-D-ribofuranosyluronamide)-N-(2-{N′-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide.
A method of treating an inflammatory disease in a mammal comprising administering to said mammal in need of such treatment an effective amount of a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-β-D-ribofuranosyluronamide)-N-(2-{N′-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide.
A method of treating a respiratory disease in a mammal comprising administering to said mammal in need of such treatment an effective amount of a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-β-D-ribofuranosyluronamide)-N-(2-{N′-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide.
A method of treating septic shock, male erectile dysfunction, male factor infertility, female factor infertility, hypertension, stroke, epilepsy, cerebral ischaemia, peripheral vascular disease, post-ischaemic reperfusion injury, diabetes, rheumatoid arthritis, multiple sclerosis, psoriasis, dermatitis, allergic dermatitis, eczema, ulcerative colitis, Crohns disease, inflammatory bowel disease, Heliobacter pylori gastritis, non-Heliobacter pylori gastritis, non-steroidal anti-inflammatory drug-induced damage to the gastro-intestinal tract or a psychotic disorder, or for wound healing in a mammal comprising administering to said mammal in need of such treatment an effective amount of a combination of a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-β-D-ribofuranosyluronamide)-N-(2-{N′-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide.
A process for preparing a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-β-D-ribofuranosyluronamide)-N-(2-{N′-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide, comprising the steps of:
- (a) dissolving amorphous 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-β-D-ribofuranosyluronamide)-N-(2-{N′-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide in an organic solvent which contains at least 2% w/w dissolved water to obtain a solution;
- and
- (b) heating the solution to a temperature of at least 50° C. until crystallisation occurs.
Dependencies are inferred from the claim text.