Polymorphic forms of cipamfylline

Details Polymorphic forms of cipamfylline Polymorphic forms of cipamfylline

2000-08-15

2003-06-24

Berch, Mark L (Department: 1624)

Organic compounds -- part of the class 532-570 series

Organic compounds

Chalcogen bonded directly to ring carbon of the purine ring...

Reexamination Certificate

active

06583283

ABSTRACT:

FIELD OF THE INVENTION
This invention relates to novel crystalline polymorphic forms of Cipamfylline, and to methods for preparing them.
BACKGROUND OF THE INVENTION
The capacity to occur in different crystal structures is known as polymorphism and is known to occur in many organic compounds. These different crystalline forms are known as “polymorphic modifications” or “polymorphs” and are realized in their crystalline state. While polymorphic modifications have the same chemical composition, they differ in packing, geometrical arrangement, and other descriptive properties of the crystalline solid state. As such, these modifications may have different solid-state physical properties such as shape, color density, hardness, deformability, stability, and dissolution properties, etc. Polymorphism of an organic drug molecule and its consequences will be appreciated by the skilled artisan.
Cipamfylline, 1,3-di-cyclopropylmethyl-8-amino xanthine, has the chemical formula C
13
H
17
N
5
O
2
, m.w. of 275.31, and the following structural formula:
Its synthesis is described in Example 9, in Maschler et al., Great Britain Patent Application No. 8906792.0 filed on Mar. 23, 1989, in its corresponding EPO patent EP 389282, and corresponding U.S. Pat. No. 5,734,051 whose disclosures are incorporated herein by reference in their entirety.
Cipamfylline is a PDE
4
inhibitor and is useful in the treatment, including prophylaxis, of disease states mediated thereby.
Cipamfylline was also disclosed to have TNF inhibiting activity in Esser et al., PCT/US91/08734 (also published as EP 558659), and is therefore useful in the treatment, including prophylaxis of TNF mediated disease states. Suitable assays, dosage forms, and dosage ranges, etc. for the polymorphs of this invention for use in the therapeutic treatment of diseases may be found in either the Maschler et al., or the Esser et al. patent applications whose disclosures are incorporated herein by reference in their entirety.
SUMMARY OF THE INVENTION
This invention relates to a novel crystalline polymorph of the 1,3-di-cyclopropylmethyl-8-amino xanthine, referred to hereinafter as Form I, which form of such compound is useful in the treatment of PDE
4
or TNF mediated diseases.
This invention also relates to a novel crystalline polymorph of the 1,3-di-cyclopropylmethyl-8-amino xanthine, referred to hereinafter as Form II, which form of such compound is useful in the treatment of PDE
4
or TNF mediated diseases.
This invention also relates to a novel crystalline polymorph of the 1,3-di-cyclopropylmethyl-8-amino xanthine, referred to hereinafter as Form IV, which form of such compound is useful in the treatment of PDE
4
or TNF mediated diseases.


REFERENCES:
patent: 5734051 (1998-03-01), Spicer et al.
patent: 5981535 (1999-11-01), Spicer et al.
patent: WO 92/05175 (1992-04-01), None
patent: WO 92/05176 (1992-04-01), None

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