A61K31/54

KDM1A inhibitors for the treatment of disease

Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.

Triterpenoids with HIV maturation inhibitory activity

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: ##STR00001##
with X selected from C.sub.4-8 cycloalkyl, C.sub.4-8 cycloalkenyl, C.sub.4-9 spirocycloalkyl, C.sub.4-9 spirocycloalkenyl, C.sub.4-8 oxacycloalkyl, C.sub.4-8 dioxacycloalkyl, C.sub.6-8 oxacycloalkenyl, C.sub.6-8 dioxacycloalkenyl, C.sub.6 cyclodialkenyl, C.sub.6 oxacyclodialkenyl, C.sub.6-9 oxaspirocycloalkyl and C.sub.6-9 oxaspirocycloalkenyl ring, such that X is substituted with A, wherein A is —C.sub.1-6 alkyl-halo. These compounds are useful for the treatment of HIV and AIDS.

Triterpenoids with HIV maturation inhibitory activity

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: ##STR00001##
with X selected from C.sub.4-8 cycloalkyl, C.sub.4-8 cycloalkenyl, C.sub.4-9 spirocycloalkyl, C.sub.4-9 spirocycloalkenyl, C.sub.4-8 oxacycloalkyl, C.sub.4-8 dioxacycloalkyl, C.sub.6-8 oxacycloalkenyl, C.sub.6-8 dioxacycloalkenyl, C.sub.6 cyclodialkenyl, C.sub.6 oxacyclodialkenyl, C.sub.6-9 oxaspirocycloalkyl and C.sub.6-9 oxaspirocycloalkenyl ring, such that X is substituted with A, wherein A is —C.sub.1-6 alkyl-halo. These compounds are useful for the treatment of HIV and AIDS.

Heterocyclic compounds

Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.

Heterocyclic compounds

Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.

OXATHIAZIN COMPOUNDS FOR INHIBITING GAPDH

A method of inhibiting GAPDH with certain oxathiazin-like compounds and/or related compounds.

OXATHIAZIN COMPOUNDS FOR INHIBITING GAPDH

A method of inhibiting GAPDH with certain oxathiazin-like compounds and/or related compounds.

ANTI-INFLAMMATORY IMMUNOENHANCER

The present invention provides an anti-inflammatory type immune-enhancing agent that simultaneously induces an anti-inflammatory action and an immune-enhancing action. An anti-inflammatory type immune-enhancing agent containing at least one kind selected from a heterocyclic compound represented by the formula (I)

##STR00001##

wherein each symbol is as described in the DESCRIPTION, or a salt thereof, and an isothiocyanate compound represented by the formula S═C═N—R.sup.5 (II) wherein the symbol is as described in the DESCRIPTION, as an active ingredient.

ANTI-INFLAMMATORY IMMUNOENHANCER

The present invention provides an anti-inflammatory type immune-enhancing agent that simultaneously induces an anti-inflammatory action and an immune-enhancing action. An anti-inflammatory type immune-enhancing agent containing at least one kind selected from a heterocyclic compound represented by the formula (I)

##STR00001##

wherein each symbol is as described in the DESCRIPTION, or a salt thereof, and an isothiocyanate compound represented by the formula S═C═N—R.sup.5 (II) wherein the symbol is as described in the DESCRIPTION, as an active ingredient.

NON-CATALYTIC SUBSTRATE-SELECTIVE p38alpha-SPECIFIC MAPK INHIBITORS WITH ENDOTHELIAL-STABILIZING AND ANTI-INFLAMMATORY ACTIVITY, AND METHODS OF USE THEREOF

Compounds that inhibit p38α MAPK protein, and methods of using the same, are provided for treating or preventing diseases such as cancer or inflammatory diseases.