C07D209/40

INHIBITORS OF APOL1 AND METHODS OF USING SAME

The disclosure provides compounds of Formula I,

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deuterated derivatives of those compounds, and pharmaceutically acceptable salts of those compounds and derivatives, compositions comprising the same, and methods of using the same, including use in treating APOL1 mediated kidney disease.

BENZOPYRAZOLE COMPOUNDS AND ANALOGUES THEREOF

Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising a compound of formula I, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by aberrant complement system activity.

##STR00001##

BENZOPYRAZOLE COMPOUNDS AND ANALOGUES THEREOF

Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising a compound of formula I, and methods involving use of the compounds and compositions in the treatment and prevention of diseases and conditions characterized by aberrant complement system activity.

##STR00001##

ACLY inhibitors and uses thereof

The present invention provides compounds useful as inhibitors of ATP citrate lyase (ACLY), compositions thereof, and methods of using the same.

Indirubin derivatives, and uses thereof

Indirubin is the major active anti-tumor component of a traditional Chinese herbal medicine used for treatment of chronic myelogenous leukemia (CML). Indirubin derivatives (IRDs) potently reduce the viabilities of various cancer cells and affect kinase activities. IRDs disclosed herein provide new therapeutics for cancer and conditions regulated by the kinase activities.

Indirubin derivatives, and uses thereof

Indirubin is the major active anti-tumor component of a traditional Chinese herbal medicine used for treatment of chronic myelogenous leukemia (CML). Indirubin derivatives (IRDs) potently reduce the viabilities of various cancer cells and affect kinase activities. IRDs disclosed herein provide new therapeutics for cancer and conditions regulated by the kinase activities.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

ISOINDOLINE DERIVATIVES

An isoindoline derivative of formula

##STR00001##

wherein
X is N, C—CN or C—COR.sup.2;
Y is a radical having an acidic group or a basic group;
R.sup.1 is independently from one another halogen or C.sub.1-C.sub.4-alkyl, said alkyl is unsubstituted or substituted with halogen;
R.sup.2 is C.sub.1-C.sub.4-alkyl, said alkyl is unsubstituted or substituted with halogen; and
n is 0, 1, 2, 3 or 4,
with the proviso that Y does not include an acidic group if X is C—CN or C—COR.sup.2, and compositions containing the same are provided. The isoindoline derivative and the pigment composition are suitable, for example, for coloring high molecular mass organic material, especially paints, printing inks, resist formulations for color filter applications, electrophotographic toners, cosmetics, plastics, films or fibers.

ISOINDOLINE DERIVATIVES

An isoindoline derivative of formula

##STR00001##

wherein
X is N, C—CN or C—COR.sup.2;
Y is a radical having an acidic group or a basic group;
R.sup.1 is independently from one another halogen or C.sub.1-C.sub.4-alkyl, said alkyl is unsubstituted or substituted with halogen;
R.sup.2 is C.sub.1-C.sub.4-alkyl, said alkyl is unsubstituted or substituted with halogen; and
n is 0, 1, 2, 3 or 4,
with the proviso that Y does not include an acidic group if X is C—CN or C—COR.sup.2, and compositions containing the same are provided. The isoindoline derivative and the pigment composition are suitable, for example, for coloring high molecular mass organic material, especially paints, printing inks, resist formulations for color filter applications, electrophotographic toners, cosmetics, plastics, films or fibers.