Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-07-30
1999-03-30
Fay, Zohreh
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514311, 514382, 514385, 514913, A61K 3144, A61K 3147, A61K 3141, A61K 31415
Patent
active
058890203
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/IB95/00056 filed on Jan. 26, 1995.
The present invention describes the use of an angiotensin II antagonist or of a pharmaceutically acceptable salt thereof in the preparation of a pharmaceutical composition for the treatment of normal tension glaucoma and neurodegenerative processes.
The term glaucoma includes symptoms of the eye which are especially to be attributed to increased intraocular pressure. Frequently, an obstruction to drainage of the aqueous humour leads to an increase in the intraocular pressure. Chronically raised intraocular pressure has a harmful effect on the optic nerve and the retina, which can terminally lead to blindness. Accordingly, for the treatment of glaucoma, active ingredients are used which are able to reduce significantly the intraocular pressure. Renin inhibitors have been mentioned, for example, as suitable agents for lowering the intraocular pressure (cf. Watkins, U.S. Pat. No. 4,906,613). Increased intraocular pressure can also be treated with certain .beta.-adrenoceptor blockers.
More recently, the phenomenon of so-called normal tension glaucoma ("low tension" or "normal tension glaucoma" is used synonymously) has now been 87, 187(1990)!. Normal tension glaucoma is characterized by an intraocular pressure which is in the normal range, i.e. is not increased, but in which the optic disc (papilla nervi optici) is pathologically excavated and the field of vision is impaired. The pathogenetic factors are especially circulatory problems in the ocular blood vessels caused by atherosclerosis, hypotension, orthostasis, functional vasospasms and neurodegenerative factors.
Accordingly, a therapy for the treatment of normal tension glaucoma therefore starts with the possible factors involved mentioned above. Actually, this means that active ingredients which are able to guarantee or to improve the circulation in the ocular blood vessels are suitable agents for the treatment of normal tension glaucoma and of neurodegenerative factors.
It has now surprisingly been found that angiotensin II antagonists, preferably those having pronounced selectivity for the AT.sub.1 receptor (also called A II blockers in the following), in general and already preclinically established A II blockers such as, for example, valsartan or losartan in particular, extremely improve the circulation in the eye generally and the ocular blood microcirculation in the choroidal and retinal ocular tissue especially. A II blockers are also suitable for treating narrowed visual field or disorders on account of neurological pathogenesis. Such A II blockers are therefore suitable agents for treating the disease of normal tension glaucoma and neurodegenerative processes.
Such A II blockers typically have a preference of .gtoreq.99% and preferably of .gtoreq.99.99% for the AT.sub.1 receptor in comparison to the AT.sub.2 receptor.
In addition to the A II blockers mentioned, there are also mixed or dual angiotensin II antagonists. Dual angiotensin II antagonists have preferences of the same order of magnitude for the AT.sub.1 and the AT.sub.2 receptor, the relative extent varying greatly. A dual A II blocker having a preference for the AT.sub.1 receptor of .gtoreq.50%, preferably .gtoreq.90% and especially preferably of .gtoreq.95%, is also suitable for treating the disease of normal tension glaucoma.
AT.sub.2 receptor antagonists having a preference of >99% for the AT.sub.2 receptor do not have the abovementioned effect on the microcirculation in the eye and are therefore unsuitable for use in the treatment of normal tension glaucoma
In the following, if angiotensin II antagonists are being discussed, both A II blockers having the mentioned selectivity for the AT.sub.1 receptor, and dual angiotensin II antagonists having the mentioned preference for the AT.sub.1 receptor are meant.
The present invention therefore relates to the use of an angiotensin II antagonist or of a pharmaceutically acceptable salt thereof in the preparation of a pharmaceutical composition for the treatment of normal
REFERENCES:
Could the Pharmacological Differences Observed Between Antiotensin II Antagonists and Inhibitors of Angiotensin Converting Enzyme be Clinically Beneficial?, Pharmacological & Toxicology 1992, 71, pp. 241-249.
The Ocular Hypotensive Effect of DUP 753, A Non-Peptide Agiotension II Antagonist, S. Wilson, et al., Dept. of Pharmacology, Texas College of Osteopathic Medicine, Fort Worth, TX 76107 (Abstract). Ocular Tissues, P., Mallorga, et al., Current Eye Research, IRL Press, vol. 8, 1989, p. 841.
Angiotensin Receptor Subtypes in the Albino Rabbit Eye, Mallorga, P., et al., Society for Neuroscience Abstracts, vol. 17, p. 810,1991.
Nonpeptide Angiotensin II Receptor Antagonists: A New Concept for Pharmacologic Control of the Renin System, American Journal of Hypertension, vol. 4, No. 4, Part 2, Apr., 1991.
Are Large Optic Nerve Heads Susceptible to Glaucomatous Damage at Normal Intraocular Pressure?, Burk, Reinhard O.W., et al., Graefe's Archive Ophthalmology, vol. 230, No. 6, 1992.
Optic Nerve Compression By CartotidArteries in Low-Tension Glaucoma,, Gutman, Isaac, et al., Graefe's Archive for Clinical and Experimental Ophthalmology, Dec., 1993.
Chemical Abstracts 119:174228 (1993), Cash et al.
Huxley Alica
Mathis Georg
Ciba Vision Corporation
Fay Zohreh
Lee Michael U.
Meece R. Scott
LandOfFree
Treatment of normotensive glaucoma with angiotensin II antagonis does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Treatment of normotensive glaucoma with angiotensin II antagonis, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Treatment of normotensive glaucoma with angiotensin II antagonis will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1215443