Aceclidine derivatives, compositions thereof and methods of use thereof
The present invention is directed to derivatives of aceclidine. The present invention is further directed to ophthalmological compositions comprising a therapeutically effective amount of a compound of the present invention and one or more pharmaceutically acceptable excipients. The present invention is further directed to a methods of treating presbyopia or glaucoma or reducing hyperemia comprising administering to a patient in need thereof a therapeutically effective amount of a compound of the present invention.
1. A pharmaceutically acceptable salt of a compound comprising a cation of formula (I),
wherein R 1 is an alkyl, and
wherein R 2 is an amine or tert-butyl.
2. An ophthalmological composition comprising a therapeutically effective amount of (i) a pharmaceutically acceptable salt of a compound comprising a cation of formula (I):
wherein R 1 is an alkyl, and
wherein R 2 is an amine or tert-butyl, or
(ii) a compound of formula (III)
or a pharmaceutically acceptable salt thereof,
wherein the pH of the composition is at least 3 log units less than the pKa of the compound.
3. The composition of claim 2 , further comprising a cyclodextrin.
4. The composition of claim 3 , wherein the cyclodextrin is selected from an alpha-cyclodextrin, a beta-cyclodextrin and a gamma-cyclodextrin.
5. A method of treating presbyopia or glaucoma comprising administering to a patient in need thereof a therapeutically effective amount of (i) a pharmaceutically acceptable salt of a compound comprising a cation of formula (I):
wherein R 1 is an alkyl, and
wherein R 2 is an amine or tert-butyl, or
(ii) a compound of formula (III)
or a pharmaceutically acceptable salt thereof.
6. A method of reducing hyperemia comprising administering to a patient in need thereof a therapeutically effective amount of (i) a pharmaceutically acceptable salt of a compound comprising a cation of formula (I):
wherein R 1 is an alkyl, and
wherein R 2 is an amine or tert-butyl, or
(ii) a compound of formula (III)
or a pharmaceutically acceptable salt thereof.