C07D211/48

COMPOSITIONS OF SPHINGOSINE-1-PHOSPHATE RECEPTOR 2 (S1PR2) BINDING AGENTS AND USES THEREOF
20200369626 · 2020-11-26 · ·

Described are compounds for the binding of S1PR2, and imaging agents and pharmaceutical compositions including said compounds. Also described are methods employing the compounds, imaging agents, and pharmaceutical compositions. These methods include imaging and/or treatment of diseases associated with S1PR2.

COMPOSITIONS OF SPHINGOSINE-1-PHOSPHATE RECEPTOR 2 (S1PR2) BINDING AGENTS AND USES THEREOF
20200369626 · 2020-11-26 · ·

Described are compounds for the binding of S1PR2, and imaging agents and pharmaceutical compositions including said compounds. Also described are methods employing the compounds, imaging agents, and pharmaceutical compositions. These methods include imaging and/or treatment of diseases associated with S1PR2.

Phenyl derivative

The compound of the formula (I-1): ##STR00001##
wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P.sub.2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P.sub.2-mediated diseases such as diseases resulting from vascular constriction, fibrosis, and respiratory diseases.

Phenyl derivative

The compound of the formula (I-1): ##STR00001##
wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P.sub.2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P.sub.2-mediated diseases such as diseases resulting from vascular constriction, fibrosis, and respiratory diseases.

COMPOSITIONS FOR TREATING NEURODEGENERATIVE DISEASES

The present disclosure relates to novel compounds, pharmaceutical compositions containing the compounds and methods of using the compounds and pharmaceutical compositions for treating neurodegenerative diseases, including Alzheimer's disease and cognitive decline. Methods for inhibiting synapse number decline or membrane trafficking abnormalities associated with exposure of a neuronal cell to Abeta species are also disclosed.

COMPOSITIONS FOR TREATING NEURODEGENERATIVE DISEASES

The present disclosure relates to novel compounds, pharmaceutical compositions containing the compounds and methods of using the compounds and pharmaceutical compositions for treating neurodegenerative diseases, including Alzheimer's disease and cognitive decline. Methods for inhibiting synapse number decline or membrane trafficking abnormalities associated with exposure of a neuronal cell to Abeta species are also disclosed.

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.

ARYL ALKYNAMIDE DERIVATIVES

[Problem] A compound which is useful as a STING inhibitor is provided.

[Means for Solution] The present inventors have found aryl alkynamide derivatives having an inhibitory action on STING. The aryl alkynamide derivatives of the present invention have an inhibitory action on STING and can be used as an agent for treating an autoimmune disease, a neurodegenerative disease, a type I interferonopathy and/or other STING-mediated disease.

ARYL ALKYNAMIDE DERIVATIVES

[Problem] A compound which is useful as a STING inhibitor is provided.

[Means for Solution] The present inventors have found aryl alkynamide derivatives having an inhibitory action on STING. The aryl alkynamide derivatives of the present invention have an inhibitory action on STING and can be used as an agent for treating an autoimmune disease, a neurodegenerative disease, a type I interferonopathy and/or other STING-mediated disease.