Crystalline form II of cabergoline

Details Crystalline form II of cabergoline Crystalline form II of cabergoline

2003-10-31

2004-10-05

Aulakh, Charanjit S. (Department: 1625)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C546S069000

Reexamination Certificate

active

06800635

ABSTRACT:

STATEMENTS REGARDING FEDERALLY SPONSORED RESEARCH OR DEVELOPMENT
Not applicable.
REFERENCE TO A MICROFICHE APPENDIX
Not applicable.
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention concerns a new crystalline form of cabergoline, a pharmaceutical composition thereof and its use as a therapeutically active agent, alone or in combination. Another aspect of the present invention relates to the preparation of this crystalline form.
2. Description of the Related Art
Cabergoline is an ergoline derivative interacting with D2 dopamine receptors and is endowed with different useful pharmaceutical activities and it is used in the treatment of hyperprolactinemia, central nervous system disorders (CNS) and other related diseases.
Cabergoline is the generic name of 1((6-allylergolin-8Beta-yl)-carbonyl)-1-(3-dimethylaminopropyl)-3-ethylurea, described and claimed in U.S. Pat. No. 4,526,892. The synthesis of Cabergoline molecule is reported also in Eur. J. Med. Chem., 24, 421, (1989) and in GB 2,103,603.
BRIEF SUMMARY OF THE INVENTION
During our work we discovered that cabergoline can exist in at least two crystalline forms under ambient conditions. One form (coded Form I) is an anhydrous not solvated form and, to our knowledge, it is the only form reported in the literature to date. Form II is an anhydrous not solvated form too.
Thus, the present invention concerns a new polymorph (Form II) of cabergoline and the preparation thereof. Another aspect relates to samples of cabergoline Form II having a % polymorph purity >90%, preferably >99%. The invention further provides a pharmaceutical composition of cabergoline Form II and its use as therapeutic agent.


REFERENCES:
patent: 4526892 (1985-07-01), Salvati et al.
patent: 6673806 (2004-01-01), Tomasi et al.
patent: 2003/0144516 (2003-07-01), Candiani et al.
patent: 2003/0149067 (2003-08-01), Tomasi et al.
patent: 2003/0187013 (2003-10-01), Tomasi et al.
patent: 2103603 (1983-02-01), None
patent: WO 01/72741 (2001-10-01), None
P. Sabatino et al, “X-ray Crystal Structure and Conformational Analysis of N-(3-diamethylaminopropyl)-N-ethylaminocarbonyl)-6(2-propenyl)ergoline-8-beta-carboxamide (cabergoline)”, II Farmco, vol. 50—No. 3, pp. 175-178, 1995.
E. Brambilla et al, “Synthesis and Nidtion Activity of a New Class of Ergoline Derivative”, European Journal of Medicinal Chemistry, vol. 24, pp. 421-426, 1989.
International Search Report, 3 pages, (Jul. 2001).

Affiliated with

Also associated with

Rating

Crystalline form II of cabergoline does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Crystalline form II of cabergoline, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Crystalline form II of cabergoline will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-3320104