2-homopiperazine-1-yl-4H-1, 3-bensothiazine-4-one derivatives of formula (I) are provided. They are useful in the treatment of bacterial infections, in particular tuberculosis, buruli ulcer and leprosy. A process for the preparation of 2-(homo)piperazine 1, 3-benzothiazine-4-one hydrochlorides is also provided.

The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof.

##STR00001##

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.

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.

A compound, having the following formula: ##STR00001## or resonance form thereof, or salt thereof, or salt of resonance form thereof is provided, wherein E includes an electrophilic site, and wherein R.sup.1-R.sup.4 and n are defined herein. Compositions and methods including the compound are also provided.

A compound, having the following formula: ##STR00001## or resonance form thereof, or salt thereof, or salt of resonance form thereof is provided, wherein E includes an electrophilic site, and wherein R.sup.1-R.sup.4 and n are defined herein. Compositions and methods including the compound are also provided.

This application describes a compound represented by Formula (I): (I) wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X.sup.1 is a covalent bond or CH.sub.2CH.sub.2, X.sup.2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.

The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: ##STR00001##
wherein Q, R.sup.1, X.sup.1, X.sup.2, Y and R.sup.2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: ##STR00001##
wherein Q, R.sup.1, X.sup.1, X.sup.2, Y and R.sup.2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

Provided is a low-molecular compound or a salt thereof, or a solvate thereof which has the ability to activate Nrf2.

The present invention provides a compound represented by the formula (1) or a salt thereof, or a solvate thereof, wherein X.sub.a1 is CR.sub.a1 or N, X.sub.a3 is CR.sub.a3 or N, R.sub.a1, R.sub.a2 and R.sub.a3 are each independently selected from the group consisting of hydrogen, halogen and C.sub.1-C.sub.6 alkoxy, X.sub.b1, X.sub.b2 and X.sub.b3 are each independently selected from the group consisting of CH.sub.2, O, NH, S and C=O, Y is C.sub.6-C.sub.10 aryl optionally having a substituent or 5- to 10-membered heteroaryl optionally having a substituent, and Z is C.sub.6-C.sub.10 aryl optionally having a substituent, 5- to 10-membered heteroaryl optionally having a substituent or C.sub.1-C.sub.6 alkyl optionally having a substituent.

##STR00001##