Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1996-06-04
1998-06-30
Fay, Zohreh
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
514573, A61K 31215, A61K 3119
Patent
active
057734720
DESCRIPTION:
BRIEF SUMMARY
The present invention is related to the use of thiol-binding prostaglandins or prostaglandin-like substances containing alpha beta unsaturated ketone, esp. prostaglandins of type A or J and derivatives or analogues thereof, for the preparation of ophthalmically compatible compositions for prevention of cataract.
Cataract is a general name for opacification of the crystalline lens. There are many causes of cataract and there are several kinds of cataract. Thus cataract may develop due to metabolic diseases such as diabetes mellitus and it may develop due to various kinds of irradiation, e.g. x-ray, ultra-violet and infrared. The most common form of cataract, however, is senile cataract, which can be regarded as a normal physiologic ageing of the lens. Also local diseases and trauma of the eye may cause cataract formation, e.g. chronic iritis and traumatic lesions of the lens. The opacification may be localised to the entire crystalline lens or it may be localised to a certain part of the lens, for example to the nucleus or the cortex, or it may be localised superficially e.g. subcapsularly in the anterior part or the posterior part of the lens. There are also congenital forms of cataract.
Certain drugs may cause cataract as side effect. Such drugs comprise for example corticosteroids, and cholinesterase inhibitors. Presently the only way to treat cataract is operation. Thus, the opacified lens is removed and an artificial intraocular lens is implanted. While such operations usually are successful and restore the vision of the patients, sight-threatening complications may occur. For example sight-threatening endophthalmitis occurs in about 0.1-0.3% of the operations, corresponding to more than 10000 cases per year world-wide. Furthermore, there are several risk factors e.g. glaucoma, diabetes and myopia that may affect the outcome of the surgery negatively. Thus there are patients in whom cataract surgery poses a particular risk and postponement of the operation may be desorable.
While treatment or prevention of cataract has been studied intensely and several drugs have been suggested to revert or halt cataract formation, there is still controversy whether such drugs are effective or not. So far there is no scientific evidence that such drugs have a true therapeutic effect. The formation of large protein aggregates and the relevance of an increase in T.sub.c, the highest critical temperature for phase separation, as well as the effect of certain reagents has been studied for instance by Pande et al in Exp Eye Res 57 (1993) 257-264, Pande in Exp Eye Res 681 (Suppl 1) 197 and Truscott et al in Exp Eye Res 49 (1989) 927-940.
We have now unexpectedly found that certain prostaglandins and prostaglandin-like substances, which in the present application are covered by the term "prostaglandins", effectively prevent or retard the formation of cataract in vitro. More specifically such compounds containing an alpha beta unsaturated ketone (enone), and particularly in the cyclopentane ring, have been found effective. The group of prostaglandins comprises particularly prostaglandins of type A and J (for definitions see below) as well as various derivatives and analogues thereof. However, all prostaglandins carry an alpha beta unsaturated ketone in the lower side chain (omega chain) after the first metabolic degradation and could therefore have a similar effect and accordingly be of potential interest, but prostaglandins and prostaglandin analogues with the alpha beta unsaturated ketone in the cyclopentane ring are at present preferred to be used according to the present invention.
The general structure of prostaglandins is illustrated below: ##STR1##
Prostaglandins A, B, C, D, E, F and J contain a cyclopentane ring and two side chains, the upper being the alpha chain and the lower the omega chain. The total number of carbon atoms is 20, the numbering starting from the carboxylic group on the alpha chain. The alpha chain carries a double bond in the cis geometry between carbon atoms 5 and 6, while the omega chain carries
REFERENCES:
Chemical Abstract 117:21186 (1991)--Ueno.
Resul Bahram
Stjernschantz Johan
Fay Zohreh
Pharmacia AB
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