Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1998-05-21
2001-05-01
McKane, Joseph K. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C549S416000, C549S418000, C536S004100, C514S475000
Reexamination Certificate
active
06225342
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to compounds, and plant extracts containing compounds which are indicated as having an inhibiting effect on cell proliferation. More specifically, the invention relates to glycosidic compounds derivable from Calendula species, the plant glycosides having a cytostatic effect on cells, and their use as cytostatic agents, in particular in the treatment of psoriasis.
BACKGROUND OF THE INVENTION
Crude Calendula plant extracts have been used in medicinal folklore for the treatment of several ailments for centuries. Such extracts have, for example, been used as or in anti-inflammatory medicaments and the like.
International Patent application WO 91/15218 teaches a therapeutic composition against psoriasis comprising as active ingredient a solvent extract of at least six different herbs. This application teaches that marigold decoctions can be used against gastric and intestinal ulcers externally as well as for packing slowly healing wounds and ulcers. Nowhere is it stated that marigold extract is in fact used by itself as the active component in a therapeutical composition against psoriasis.
Pizza C., and de Tommasi N., Phytochemistry, Vol. 27, number 7, pp 2205-2208 (1988) teaches the isolation and structure of a sesquiterpene glycoside from Calendula Arvensis. It is stated that Calendula Arvensis L. (compositae) is a herbaceous plant used in Italian folk medicine as an anti-inflammatory and anti-pyretic remedy. There is no suggestion that the sesquiterpene glycosides obtained has cytostatic activity or could be used in the treatment of psoriasis.
Mascolo N. et al., Phytotherapy Research, Vol. 1, pp 28-31 (1987) teaches that marigold extract is known for anti-inflammatory activity. There is no mention of marigold extract being used as an anti-psoriatic agent.
Gracza L. Planta Medica 53, page 227 (1987) discloses various oxygen containing terpene derivatives from Calendula Officinalis. The uses of these are indicated for leukorrhoea and trichomonacide activity. There is no mention of using the terpene derivatives as anti-psoriatic agents.
Fazakas B. and Rácz, G. Farmacia Vol. XIII, number 2, page 91 (1965) also teaches that extracts from the flowers of Calendula Officinalis are employed in traditional herbal medicine for leukorrhoea (excessive fluor albus) and showed a good trichomonacide activity.
Gracza L. and Szász K. Acta Pharm. Hung. 38, pp 118-125 (1968) reports on a chemical analysis of the petals of marigold (Calendula Officinalis) with the aim of separating and identifying the solution or solutions which are responsible for the trichomonacide effect reported by Fazakas and Rácz (supra). The most active liquid compounds isolated were described as terpenic alcohols and terpenic lactons according to spectroscopic data.
Jakupovic et al. Planta Medica 54 (3) pp 254-256 (1988) teaches the extraction and isolation of five sesquiterpene glycosides from
Calendula oersica.
There is no mention of potential or actual uses for the extracted and isolated molecules.
Ahmed A Ahmed et al., Journal of Natural Products Vol. 56, number 10, pp 1821-1824 (1993) relates to extraction products from
Calendula arvensis.
The products are described as four new sesquiterpene glycosides and three known ones. There is no reference to possible uses therefor.
EP 364442 B1 describes a therapeutic composition against psoriasis comprising an oil extract of at least three herbs selected from a range of herbs which range may include Calendula. However, it is stated that separate extractions of herbs did not provide a curative effect against psoriasis when used singly. Furthermore, it is stated that decoctions of Calendula per se are used for inter alia gastric and intestinal ulcer treatment. Calendula decoctions are not described as being beneficial for the treatment of skin diseases involving abnormal rates of proliferation of skin cells (e.g. hyperproliferation), in diseases such as psoriasis.
DE 3836519 C2 alleges that a pharmaceutical preparation containing freshly cut composite inflorescences of
Calendula officinalis
with milking grease as a salve base is useful in treating psoriasis. However, the composition is described as being able to give rise to allergy which can lead to discontinuation of treatment, and there is no indication of, or the identification of, the active component of the composition. There is no indication of cytostatic activity and further more it is not apparent which component or mixture of components in the alleged pharmaceutical preparation based on
Calendula officinalis
is/are the active component(s). In addition, there does not appear to be any actual evidence which demonstrates that the composition was employed in the treatment of psoriasis.
There exists a need for the development of new cytostatic drugs which are effective in combatting the onset, maintenance and/or development of disease involving hyperproliferation of dermis cells, in particular for psoriasis treatment.
SUMMARY OF INVENTION
It is an object of the present invention to provide use of active compounds or purified plant extracts comprising at least one active compound in the preparation of a medicament for the treatment of disease involving hyperproliferation of dermis cells, in particular in the treatment of psoriasis.
A second object of the invention is to provide isolated and/or purified active compounds of Calendula for use in the treatment of disease involving hyperproliferation of dermis cells, in particular in the treatment of psoriasis.
A third object of the invention is to provide isolated compounds for use in the treatment of disease involving hyperproliferation of dermis cells, in particular in the treatment of psoriasis.
These and other objects of the invention will become apparent from the following description and examples.
DETAILED DESCRIPTION OF THE INVENTION
According to one aspect of the present invention there is provided use of a compound of general Formula (I):
wherein
R
1
and R
2
are independently selected from H, OH,
and related esters thereto;
R3 is selected from OH,
and related esters thereto;
R
4
is selected from C
6
-C
12
saturated or unsaturated monocyclic or polycyclic aliphatic ring systems optionally substituted by C
1
-C
6
alkyl, H, OH, ═CH
3
or C
1
-C
4
alkyl carboxyloxy or R
4
represents a C
1
-C
6
straight-or branched-chain alkalene group substituted with such a ring system;
R
5
is selected from —CH
3
, —CHO, —COOH and —CH
2
OH and related esters and ethers derived therefrom;
R
6
is selected from —OH;
in the preparation of a medicament for the treatment of disease involving hyperproliferation of dermis cells.
For the purposes of the present invention “related esters and ethers” refers to all defined esters of R groups mentioned herein and in general to saturated or unsaturated straight- or branched chain C
1
-C
20
carboxy alkyl esterifying acids. Suitable examples include esterifying acids comprising methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, and all isomers of pentanyl, pentenyl, hexanyl and hexenyl alkyl groups. Also included within the term “related esters” are aromatic acids such as benzoic acid and cinnamic acid. C
1
-C
20
alkyl ethers comprising straight- or branched-chain alkyl groups as defined for “related esters” above are also encompassed herein.
In a preferment there is provided use of a compound of general Formula (I) wherein
R
1
and R
2
are independently selected from H, —OH
R
3
is selected from —OH,
R
4
is selected from the group
R
5
is selected from the group CH
3
, —CHO, —COOH and —CH
2
OH; and
R
6
is selected from OH,
In a further preferment there is provided use of a compound extractable from Calendula species of general Formula (I) wherein
R
1
and R
2
are independently selected from H and OH (&bgr;OH or &agr;OH);
R
3
is selected from OH,
R
4
is selected from
R
5
is CH
3
; and
R
6
is selected from OH,
Most preferably, there is provided use of a compound of Formula (I) extractable from a Calendula species wherein
R
1
and R
2
are independentl
Anand Chaman Lal
Gray Alexander Irvine
Habtemarium Solomon
Stimson William Howard
Waterman Peter George
Alston & Bird LLP
McKane Joseph K.
Solola Taofiq A.
University of Strathclyde
LandOfFree
Use of calendula glycosides for the treatment of psoriasis does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Use of calendula glycosides for the treatment of psoriasis, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Use of calendula glycosides for the treatment of psoriasis will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2568557