C07D285/24

OREXIN RECEPTOR ANTAGONISTS

The disclosures herein relate to novel compounds of formula

##STR00001##

wherein W, X and Y.sub.1, Y.sub.2, Y.sub.3 and Y.sub.4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.

3-amino-4H-benzo[e][1,2,4]thiadiazine 1,1-dioxide derivatives as inhibitors of MRGX2

Disclosed are compounds of Formula (1), tautomers thereof, and pharmaceutically acceptable salts of the compounds or tautomers, wherein L, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula (1), to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders or conditions associated with MRGX2. ##STR00001##

3-amino-4H-benzo[e][1,2,4]thiadiazine 1,1-dioxide derivatives as inhibitors of MRGX2

Disclosed are compounds of Formula (1), tautomers thereof, and pharmaceutically acceptable salts of the compounds or tautomers, wherein L, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula (1), to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders or conditions associated with MRGX2. ##STR00001##

C6-spiro iminothiadiazine dioxides as BACE inhibitors, compositions, and their use

In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): (structurally represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds, wherein R1, R2, R3, X, Y, s, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed. ##STR00001##

C6-spiro iminothiadiazine dioxides as BACE inhibitors, compositions, and their use

In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): (structurally represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds, wherein R1, R2, R3, X, Y, s, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed. ##STR00001##

Orexin receptor antagonists

The disclosures herein relate to novel compounds of formula wherein W, X and Y.sub.1, Y.sub.2, Y.sub.3 and Y.sub.4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors. ##STR00001##

Orexin receptor antagonists

The disclosures herein relate to novel compounds of formula wherein W, X and Y.sub.1, Y.sub.2, Y.sub.3 and Y.sub.4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors. ##STR00001##

NOVEL THERAPEUTICS FOR THE TREATMENT OF GLAUCOMA

The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and/or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a KATP channel to reduce an intraocular pressure.

NOVEL THERAPEUTICS FOR THE TREATMENT OF GLAUCOMA

The present invention provides benzothiadiazine and chroman derivatives and particularly diazoxide and cromakalim derivatives for use in treating glaucoma, retinopathy, treating age related macular degeneration, treating, stabilizing and/or inhibiting blood and lymph vascularization, and reducing intraocular pressure by administering a pharmaceutically effective amount of a prodrug disposed in an ophthalmically acceptable carrier to the eye, wherein the prodrug specifically modulates a KATP channel to reduce an intraocular pressure.

MRGPRX2 MODULATORS AND RELATED METHODS OF TREATMENT

Disclosed herein are compounds having the structure of Formula (I):

##STR00001##

or a pharmaceutically acceptable salt, solvate, hydrate, isomer, tautomer, racemate, or isotope thereof, wherein L.sup.1, L.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, and m are as defined herein. Pharmaceutical compositions comprising them, processes for preparing them, and uses of them to treat or prevent diseases, disorders, and conditions are also provided. The compounds are modulators of MRGPRX2 or the MRGPRX2 ortholog and are useful in the treatment of diseases, disorders, and conditions related to MRGPRX2 or the MRGPRX2 ortholog activity.