C07D515/10

BENZOTRIAZOLE COMPOUND

The present invention aims to provide a medicament capable of treating and/or preventing diseases associated with oxidative stress by inhibiting the protein-protein interaction between Keap1 and Nrf2 and activating Nrf2. The present invention relates to a compound represented by the following formula (1):

##STR00001## wherein each symbol is as described in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. In addition, the present invention also relates to a medicament containing the aforementioned compound, for the prophylaxis and/or treatment of diseases involving oxidative stress selected from the group consisting of chronic kidney disease, non-alcoholic steatohepatitis, chronic obstructive pulmonary disease, radiation skin disorder, radiation mucosal disorder, cardiac failure, pulmonary arterial hypertension, Parkinson's disease, Friedreich's ataxia, multiple sclerosis, age-related macular degeneration, retinitis pigmentosa and glaucoma.

1,1,1-TRIFLUORO-3-HYDROXYPROPAN-2-YL CARBAMATE DERIVATIVES AND 1,1,1-TRIFLUORO-4-HYDROXYBUTAN-2-YL CARBAMATE DERIVATIVES AS MAGL INHIBITORS

The present invention provides, in part, compounds of Formula I:

##STR00001##

and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, traumatic brain injury, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.

1,1,1-TRIFLUORO-3-HYDROXYPROPAN-2-YL CARBAMATE DERIVATIVES AND 1,1,1-TRIFLUORO-4-HYDROXYBUTAN-2-YL CARBAMATE DERIVATIVES AS MAGL INHIBITORS

The present invention provides, in part, compounds of Formula I:

##STR00001##

and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, traumatic brain injury, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.

CYCLIZED SULFAMOYLARYLAMIDE DERIVATIVES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B

Inhibitors of HBV replication of Formula (I-A)

##STR00001##

including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R.sup.a to R.sup.d, and R.sup.1 to R.sup.8 have the meaning as defined herein.

The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.

CYCLIZED SULFAMOYLARYLAMIDE DERIVATIVES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B

Inhibitors of HBV replication of Formula (I-A)

##STR00001##

including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R.sup.a to R.sup.d, and R.sup.1 to R.sup.8 have the meaning as defined herein.

The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.

COVALENT FLUORESCENT PROBES FOR CANNABINOID RECEPTOR 2

The present invention provides covalent fluorescent probes for cannabinoid receptor 2 (CB2) having the general formula (I)

##STR00001##

wherein X, n, p, and R.sup.1 to R.sup.4 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

BENZOTRIAZOLE COMPOUND

The present invention aims to provide a medicament capable of treating and/or preventing diseases associated with oxidative stress by inhibiting the protein-protein interaction between Keap1 and Nrf2 and activating Nrf2. The present invention relates to a compound represented by the following formula (1):

##STR00001##

wherein each symbol is as described in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. In addition, the present invention also relates to a medicament containing the aforementioned compound, for the prophylaxis and/or treatment of diseases involving oxidative stress selected from the group consisting of chronic kidney disease, non-alcoholic steatohepatitis, chronic obstructive pulmonary disease, radiation skid: disorder, radiation mucosal disorder, cardiac failure, pulmonary arterial hypertension, Parkinson's disease, Friedreich's ataxia, multiple sclerosis, age-related macular degeneration, retinitis pigmentosa and glaucoma.

Substituted Bicyclic Heteroaryl Sulfonamide Derivatives for the Treatment of Cancer

The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof; wherein X.sup.1 is CR.sup.7 or N, X.sup.2 is CR.sup.8 or N, X.sup.3 is CR.sup.9 or N and wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are as defined in the claims, as well as methods of using the compounds for the treatment of neoplastic diseases such as cancer.

Substituted Bicyclic Heteroaryl Sulfonamide Derivatives for the Treatment of Cancer

The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof; wherein X.sup.1 is CR.sup.7 or N, X.sup.2 is CR.sup.8 or N, X.sup.3 is CR.sup.9 or N and wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are as defined in the claims, as well as methods of using the compounds for the treatment of neoplastic diseases such as cancer.