Crystalline form VII of cabergoline

Details Crystalline form VII of cabergoline Crystalline form VII of cabergoline

2002-09-18

2004-01-20

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, C546S067000

Reexamination Certificate

active

06680327

ABSTRACT:

The present invention concerns a new crystalline form of cabergoline, a pharmaceutical composition thereof and its use as therapeutically active agent, alone or in combination. Another aspect of the present invention relates to the preparation of this crystalline form. 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 European. J. Med. Chem., 24,421, (1989) and in GB-2,103,603-B.
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 VII is an anhydrous not solvated form too.
Thus, the present invention concerns a new polymorph (Form VII) of cabergoline and the preparation thereof. Another aspect relates to samples of cabergoline Form VII having a % polymorphic purity>90%, preferably >99%. The invention further provides a pharmaceutical composition of cabergoline Form VII and its use as therapeutic agent.


REFERENCES:
patent: 4526892 (1985-07-01), Salvati et al.
patent: 2 103 603 (1983-02-01), None
patent: 99 48484 (1999-09-01), None
patent: 99 59563 (1999-11-01), None
patent: 01/72747 (2001-10-01), None
Chemical Abstracts, vol. 122, No. 21, abstract No. 265741 May 22, 1995.

Affiliated with

Also associated with

Rating

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

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-3193562