Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – N-c doai
Reexamination Certificate
2003-01-23
2004-12-28
Zucker, Paul A. (Department: 1621)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
N-c doai
C560S136000
Reexamination Certificate
active
06835748
ABSTRACT:
This invention is in particular related to the use of rivastigmine in the manufacture of a medicament for the treatment of ocular disorders selected from glaucoma and neurodegenerative disease conditions of the retina and the optic nerve.
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 typically able to reduce the intraocular pressure (IOP). For example, increased IOP be treated with certain &bgr;-adrenoceptor blockers.
More recently, the phenomenon of so-called normal tension glaucoma (“low tension” or “normal tension glaucoma” is used synonymously) has now been clinically established in ophthalmology [J. Flammer, Fortschr. Ophthalmol. 87, 187(1990)]. Normal tension glaucoma is characterized by an intraocular pressure which is typically 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, which may be caused e.g. by atherosclerosis, hypotension, orthostasis, functional vasospasms and neurodegenerative factors.
It has now surprisingly been found that rivastigmine, its racemate, its analogs and/or its pharmaceutically acceptable salts are highly effective in the treatment of glaucoma and disorders of neurological pathogenesis (neurodegeneration), such as normal tension glaucoma.
Accordingly, a first aspect of the present invention is related to the use of a compound of formula (I),
wherein
R1 is hydrogen, lower alkyl, cyclohexyl, allyl or benzyl,
R2 is hydrogen, methyl, ethyl or propyl or
R1 and R2 together with the nitrogen to which they are attached form a morpholino or piperidino radical,
R3 is hydrogen or lower alkyl,
R4 and R5 are the same or different and each is a lower alkyl, and the dialkylaminoalkyl group is in the meta, ortho or para position,
in free base or pharmaceutically acceptable acid addition salt form,
in the preparation of a pharmaceutical composition for the treatment of an ocular disorder selected from the group consisting of glaucoma, normal tension glaucoma and neurodegenerative disease conditions of the retina and the optic nerve.
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Hess Susan
Novartis AG
Zucker Paul A.
LandOfFree
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