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US 6,583,283 B1Granted
Polymorphic forms of cipamfylline
AssigneeSmithKline Beecham Corporation
InventorsDrake S Eggleston, Ian Robert Lynch
Life of this patent
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Abstract
This invention relates to novel crystalline polymorphic forms, Form I, II and IV of Cipamfylline, methods of preparation, and use thereof in the treatment of PDE4 and TNF mediated diseases. Cipamfylline is 1,3-di-cyclopropylmethyl-8-amino xanthine, and is represented by formula (I):
Claims4
A process for producing a crystalline polymorph of 1,3-di-cyclopropylmethyl-8-amino xanthine, Form I, which process comprises
- a) dissolving 1,3-di-cyclopropylmethyl-8-amino xanthine in 1-propanol or in a 1-propanol:water admixture;
- and
- b) cooling the solution to crystallize out of solution the desired polymorphic Form I, as characterized in any one of FIGS. 1, 4, 20, or wherein Form I exhibits a single crystal X-ray crystallographic analysis with (a) crystal parameters that are approximately equal to the following:
- Crystal shape (mm) Flat needles Crystal dimensions 1.0 × 0.12 × 0.08 mm Crystal color Colorless Space Group P1 triclinic #2 Temperature 295 K Cell Constants a = 10.829(2)Å b = 12.636(2)Å c = 5.105(3)Å alpha (α) = 99.48(4) beta (β) = 91.53(4) gamma (γ) = 83.84(3) Volume 685.0(8)Å3 Molecules/unit cell (Z) 4 Density, (ρ) g/cm=3 1.354 μ 7.362 cm−1 F(000) 292
- the atomic positions of all atoms relative to the origin of the unit cell as represented in the tables of FIGS. 12 to 15.
2 more elements
Dependencies are inferred from the claim text.