A61K31/4245

TARGETING THE NEUROLIGIN-3 BINDING PARTNER CSPG4 IN GLIOMA
20220387441 · 2022-12-08 ·

Compositions and methods are provided for decreasing processing of chondroitin sulfate proteoglycan 4 (CSPG) in treatment of gliomas, which treatment may be combined with administration of an immune-oncology agent.

TARGETING THE NEUROLIGIN-3 BINDING PARTNER CSPG4 IN GLIOMA
20220387441 · 2022-12-08 ·

Compositions and methods are provided for decreasing processing of chondroitin sulfate proteoglycan 4 (CSPG) in treatment of gliomas, which treatment may be combined with administration of an immune-oncology agent.

COMBINATION THERAPY METHODS, COMPOSITIONS AND KITS
20220378866 · 2022-12-01 ·

Combination therapy methods, compositions and kits Invention relates to combinations comprising: a) a compound of formula (I)

##STR00001##

or a pharmaceutically or veterinary acceptable salt thereof, wherein:
R.sub.1 R.sub.2 and R.sub.3 have particular meaning; and (b) one or more drugs selected from the group consisting of i) a compound of formula (IV), or a pharmaceutically or veterinary acceptable salt thereof,

##STR00002##

wherein R.sub.5 and R.sub.6 have particular meaning, ii) a sphingosine-1-phosphate receptor inhibitor (S1PR modulator), and iii) a Signal transducer and activator of transcription 3 (STAT3) inhibitor. Particular combinations and single pharmaceutical compositions and kits of parts are disclosed. These combinations, single pharmaceutical compositions and kits of parts are for use in the treatment and/or prevention of an inflammatory neurological disease or condition which can result in the destruction or degeneration of axons or myelin in a subject in need thereof

COMBINATION THERAPY METHODS, COMPOSITIONS AND KITS
20220378866 · 2022-12-01 ·

Combination therapy methods, compositions and kits Invention relates to combinations comprising: a) a compound of formula (I)

##STR00001##

or a pharmaceutically or veterinary acceptable salt thereof, wherein:
R.sub.1 R.sub.2 and R.sub.3 have particular meaning; and (b) one or more drugs selected from the group consisting of i) a compound of formula (IV), or a pharmaceutically or veterinary acceptable salt thereof,

##STR00002##

wherein R.sub.5 and R.sub.6 have particular meaning, ii) a sphingosine-1-phosphate receptor inhibitor (S1PR modulator), and iii) a Signal transducer and activator of transcription 3 (STAT3) inhibitor. Particular combinations and single pharmaceutical compositions and kits of parts are disclosed. These combinations, single pharmaceutical compositions and kits of parts are for use in the treatment and/or prevention of an inflammatory neurological disease or condition which can result in the destruction or degeneration of axons or myelin in a subject in need thereof

PROSTAGLANDIN E2 (PGE2) EP4 RECEPTOR ANTAGONISTS

The present invention relates to novel compounds of formula (I) and pharmaceutical compositions containing these compounds. The compounds provided herein can act as prostaglandin E2 (PGE2) EP4 receptor antagonists, which renders them highly advantageous for use in therapy, particularly in the treatment or prevention of cancer, a neovascular eye disease, inflammatory pain, or an inflammatory disease, such as, e.g., multiple sclerosis, rheumatoid arthritis or endometriosis.

##STR00001##

PROSTAGLANDIN E2 (PGE2) EP4 RECEPTOR ANTAGONISTS

The present invention relates to novel compounds of formula (I) and pharmaceutical compositions containing these compounds. The compounds provided herein can act as prostaglandin E2 (PGE2) EP4 receptor antagonists, which renders them highly advantageous for use in therapy, particularly in the treatment or prevention of cancer, a neovascular eye disease, inflammatory pain, or an inflammatory disease, such as, e.g., multiple sclerosis, rheumatoid arthritis or endometriosis.

##STR00001##

1,2,4-oxadiazole derivatives as immunomodulators

The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I) ##STR00001## In the formula Q is O, R.sub.1 is the side chain of Ser, R.sub.2 is —CO-Thr, R.sub.3 is the side chain of Asn or Glu, and R.sub.4, R.sub.5 and R.sub.6 are each H.

1,2,4-oxadiazole derivatives as immunomodulators

The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I) ##STR00001## In the formula Q is O, R.sub.1 is the side chain of Ser, R.sub.2 is —CO-Thr, R.sub.3 is the side chain of Asn or Glu, and R.sub.4, R.sub.5 and R.sub.6 are each H.

Compounds and compositions for inducing chondrogenesis

The present invention provides compounds of formula I: ##STR00001##
or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds, and methods of using such compounds for treatment of joint damage or joint injury in a mammal, and for inducing differentiation of mesenchymal stem cells into chondrocytes.

Compounds and compositions for inducing chondrogenesis

The present invention provides compounds of formula I: ##STR00001##
or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds, and methods of using such compounds for treatment of joint damage or joint injury in a mammal, and for inducing differentiation of mesenchymal stem cells into chondrocytes.