Provided are a long-acting prodrug of Rasagiline, which has application in the treatment of Central Nervous System diseases such as Parkinson's disease, preparation method and use thereof. The long-acting prodrug of Rasagiline has a structure of formula (I), wherein T is absent, or T is selected from ##STR00001##
each of R.sub.1 and R.sub.2 is independently selected from H, D, and alkyl; W is absent, or W is selected from (CH.sub.2).sub.n, wherein n is an integer selected from 1 to 15; X is absent, or X is selected from (CH.sub.2).sub.m, wherein m is an integer selected from 1 to 10; Y is absent, or Y is selected from —C(═O)NH—, —NHC(═O)—; R.sub.3 is selected from substituted or unsubstituted C.sub.1-C.sub.30 alkyl, substituted or unsubstituted C.sub.2-C.sub.30 alkenyl, substituted or unsubstituted C.sub.2-C.sub.30 alkynyl, substituted or unsubstituted C.sub.3-C.sub.30 cycloalkyl, cholane aliphatic group, —R.sup.3a—C(═O)O—R.sup.3b, —R.sup.3a—OC(═O)—R.sup.3b, —R.sup.3a—C(═O)NH—R.sup.3b, —R.sup.3a—NHC(═O)—R.sup.3b, —R.sup.3a—S(═O).sub.1-2O—R.sup.3b and —R.sup.3a—OS(═O).sub.1-2—R.sup.3b. ##STR00002##

Ophthalmic formulations for acute and transient treatment of night vision disturbance syndrome (NVD) are presented. Preferred formulations comprise carbachol at very low concentrations that were demonstrated to unexpectedly provide an acute and transient therapeutic effect for a desirable magnitude and period of time.

Ophthalmic formulations for acute and transient treatment of night vision disturbance syndrome (NVD) are presented. Preferred formulations comprise carbachol at very low concentrations that were demonstrated to unexpectedly provide an acute and transient therapeutic effect for a desirable magnitude and period of time.

The present invention relates to a composition for treating K.sub.Ca3.1 channel-mediated diseases, comprising a phenylalkyl carbamate compound and, more specifically, to a pharmaceutical composition comprising, as an active ingredient, a phenylalkyl carbamate compound, the representative example of which is solriamfetol conventionally used as a therapeutic agent for narcolepsy, i.e., 2-amino-3-phenylpropyl carbamate, the pharmaceutical composition being able to be used for treating K.sub.Ca3.1 channel-mediated diseases, for example, fibrotic diseases, autoimmune diseases, and cancer diseases, by inhibiting the activation of K.sub.Ca3.1 channels in the cell membrane.

The present invention includes compositions and methods for providing a therapeutically acceptable dose of an active pharmaceutical agent for once a day delivery of the active pharmaceutical compound in an amount effective to treat at least one of: Sjogren's syndrome, Xerostomia, dry mouth, hypo-salivation, or dental carries due to reduced or compromised salivation, wherein both the peak and trough times in the blood level at 8 hours is greater than 25% of the peak value in the blood level concentration.

Problem: To provide a topical composition having excellent permeability in the stratum corneum. Solution: A topical composition is prepared that comprises: (A) one antifungal agent or two or more antifungal agents selected from the group consisting of tolnaftate and pharmaceutically acceptable salts thereof; and (B) at least one compound selected from the group consisting of ester compounds of fatty acids having from 8 to 18 carbon atoms and dihydric alcohols having from 2 to 4 carbon atoms, lysine acyl glutamate, lysine diacyl glutamate, pharmaceutically acceptable salts of lysine acyl glutamate or lysine diacyl glutamate, diethylene glycol-based glycol ethers, cyclohexanedicarboxylic acid polyoxyethylene alkyl ethers, mannosylerythritol lipids, and sucrose fatty acid esters.

Problem: To provide a topical composition having excellent permeability in the stratum corneum. Solution: A topical composition is prepared that comprises: (A) one antifungal agent or two or more antifungal agents selected from the group consisting of tolnaftate and pharmaceutically acceptable salts thereof; and (B) at least one compound selected from the group consisting of ester compounds of fatty acids having from 8 to 18 carbon atoms and dihydric alcohols having from 2 to 4 carbon atoms, lysine acyl glutamate, lysine diacyl glutamate, pharmaceutically acceptable salts of lysine acyl glutamate or lysine diacyl glutamate, diethylene glycol-based glycol ethers, cyclohexanedicarboxylic acid polyoxyethylene alkyl ethers, mannosylerythritol lipids, and sucrose fatty acid esters.

The invention relates to methods for decreasing adverse effects associated with solriamfetol ([R]-2-amino-3-phenylpropylcarbamate) therapy in subjects with impaired renal function. In particular, the invention provides an optimized dose escalation scheme for subjects with moderate renal impairment which results in the subjects having increased tolerance to adverse effects associated with the administration of solriamfetol. The invention also provides adjusted dosing for safe therapeutic use of solriamfetol in subjects having severe renal impairment.

The invention relates to methods for decreasing adverse effects associated with solriamfetol ([R]-2-amino-3-phenylpropylcarbamate) therapy in subjects with impaired renal function. In particular, the invention provides an optimized dose escalation scheme for subjects with moderate renal impairment which results in the subjects having increased tolerance to adverse effects associated with the administration of solriamfetol. The invention also provides adjusted dosing for safe therapeutic use of solriamfetol in subjects having severe renal impairment.

Disclosed are hydroquinone compounds, preparation methods therefor, and uses thereof in anti-tumor or immunomodulation. The structural formula of the hydroquinone compounds are shown by formula I, ##STR00001##
wherein X is C═O or CH.sub.2; Y is NH, O or absent; R is: a substituted or unsubstituted alkyl group having at least one carbon atom, a substituted or unsubstituted cycloalkyl group having at least three carbon atoms, a substituted or unsubstituted alkenyl group or alkynyl group having at least two carbon atoms; and a substituted or unsubstituted aryl group or heteroaryl group containing at least four carbon atoms. The compounds provided slowly release 2-tert-butyl-4-methoxyphenol in vivo and maintain stable plasma concentration of 2-tert-butyl-4-methoxyphenol (T1/2=12-24 h). The compounds provided by the present invention protect the phenolic hydroxyl group of 2-tert-butyl-4-methoxyphenol, avoids environmental oxidation and increase the environmental stability of drugs containing the compounds.