C07D279/08

POLYMER COMPRISING A PLURALITY OF PHENOTHIAZINE GROUPS AND METHODS OF MAKING THE SAME

A non-leaching mediator may include a polymer having a polymeric backbone, and a plurality of phenothiazine groups bonded to the polymeric backbone. The plurality of phenothiazine groups may include at least one of a phenothiazine group having the general formula (IV):

##STR00001##

and salts thereof, where n is about 9 and R represents the polymeric backbone to which the phenothiazine group is bonded, and a phenothiazine group having the general formula (V):

##STR00002##

and salts thereof, where n is about 9 and R represents the polymeric backbone to which the phenothiazine group is bonded.

Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use

The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: ##STR00001##
wherein variables A.sup.4, A.sup.5, A.sup.6, A.sup.8, and each of R.sup.a, R.sup.b, R.sup.1, R.sup.2, R.sup.3 and R.sup.7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.

Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use

The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: ##STR00001##
wherein variables A.sup.4, A.sup.5, A.sup.6, A.sup.8, and each of R.sup.a, R.sup.b, R.sup.1, R.sup.2, R.sup.3 and R.sup.7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.

2,3-diaryl-2,3-dihydro-4H-1,3-thiazin-4-one compounds and methods for making

A compound with the following general formula (I) and a general method of making this compound are provided. R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 are each independently selected from the group that includes H, halogen, nitro, cyano, amido, pyridyl, alkyl, aryl, acyl, alkoxy, cycloalkyl, heteroalkyl, heterocyclyl, aralkyl, heteroaryl and heteroaralkyl. ##STR00001##

2,3-diaryl-2,3-dihydro-4H-1,3-thiazin-4-one compounds and methods for making

A compound with the following general formula (I) and a general method of making this compound are provided. R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 are each independently selected from the group that includes H, halogen, nitro, cyano, amido, pyridyl, alkyl, aryl, acyl, alkoxy, cycloalkyl, heteroalkyl, heterocyclyl, aralkyl, heteroaryl and heteroaralkyl. ##STR00001##

Sulfur (VI) fluoride compounds and methods for the preparation thereof

This application describes modified amino acids and polypeptides comprising a SO.sub.2F or CH.sub.2CH.sub.2SO.sub.2F group bound to the side chain of an amino acid or amino acid residue of a polypeptide in place of a hydrogen of a hydroxyl or amino substituent thereof. Methods of covalently binding the polypeptides to receptor sites of receptor proteins are also described herein.

Sulfur (VI) fluoride compounds and methods for the preparation thereof

This application describes modified amino acids and polypeptides comprising a SO.sub.2F or CH.sub.2CH.sub.2SO.sub.2F group bound to the side chain of an amino acid or amino acid residue of a polypeptide in place of a hydrogen of a hydroxyl or amino substituent thereof. Methods of covalently binding the polypeptides to receptor sites of receptor proteins are also described herein.

Ophthalmic devices

A method for preparing an ophthalmic device for slowing, inhibiting or preventing myopia progression involves (a) soaking an ophthalmic device in one or more first solvent solutions to swell the ophthalmic device; (b) soaking the swelled ophthalmic device in one or more second solvents solutions comprising one or more red-light blocking compounds blocking greater than about 5% to about 25% of red-light transmission through the ophthalmic device at a wavelength of from about 550 nanometers (nm) to about 800 nm to de-swell the swelled ophthalmic device and entrap the one or more red-light blocking compounds in the de-swelled ophthalmic device; and (c) sterilizing the de-swelled ophthalmic device.

Ophthalmic devices

A method for preparing an ophthalmic device for slowing, inhibiting or preventing myopia progression involves (a) soaking an ophthalmic device in one or more first solvent solutions to swell the ophthalmic device; (b) soaking the swelled ophthalmic device in one or more second solvents solutions comprising one or more red-light blocking compounds blocking greater than about 5% to about 25% of red-light transmission through the ophthalmic device at a wavelength of from about 550 nanometers (nm) to about 800 nm to de-swell the swelled ophthalmic device and entrap the one or more red-light blocking compounds in the de-swelled ophthalmic device; and (c) sterilizing the de-swelled ophthalmic device.

OPHTHALMIC DEVICES

A method for preparing an ophthalmic device for slowing, inhibiting or preventing myopia progression involves (a) soaking an ophthalmic device in one or more first solvent solutions to swell the ophthalmic device; (b) soaking the swelled ophthalmic device in one or more second solvents solutions comprising one or more red-light blocking compounds blocking greater than about 5% to about 25% of red-light transmission through the ophthalmic device at a wavelength of from about 550 nanometers (nm) to about 800 nm to de-swell the swelled ophthalmic device and entrap the one or more red-light blocking compounds in the de-swelled ophthalmic device; and (c) sterilizing the de-swelled ophthalmic device.