Patent classifications
C07D221/20
Methods and compositions for targeting Tregs using CCR8 inhibitors
The present invention provides compounds of Formula (I) which can be used as CCR8 inhibitors, which can be used as treatment or prevention of cancer using CCR8 inhibitors targeted tumor specific T regulatory cells.
##STR00001##
Pharmaceutical combination of an EP4 antagonist and immune checkpoint inhibitors for the treatment of tumours
The present invention provides a pharmaceutical combination comprising the EP4 antagonist of Formula (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)-benzoic acid or a pharmaceutically acceptable salt thereof and at least one immune checkpoint inhibitor, preferably the sodium salt of (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl) benzoic acid. A polymorphic form A of sodium salt of (R)-4-(1-(6-(4-(trifluoromethyl) benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)benzoate characterized by a powder XRD spectrum with peaks at values of the angle 2θ+0.2° of 4.3, 5.0, 5.8, 6.4, 7.1, 8.3, 8.7, 12.8, 15.3, 15.9 is also described. The combination and the polymorphic form A are described for use in the treatment of tumours.
Pharmaceutical combination of an EP4 antagonist and immune checkpoint inhibitors for the treatment of tumours
The present invention provides a pharmaceutical combination comprising the EP4 antagonist of Formula (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)-benzoic acid or a pharmaceutically acceptable salt thereof and at least one immune checkpoint inhibitor, preferably the sodium salt of (R)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl) benzoic acid. A polymorphic form A of sodium salt of (R)-4-(1-(6-(4-(trifluoromethyl) benzyl)-6-azaspiro[2.5]octane-5-carboxamido)cyclopropyl)benzoate characterized by a powder XRD spectrum with peaks at values of the angle 2θ+0.2° of 4.3, 5.0, 5.8, 6.4, 7.1, 8.3, 8.7, 12.8, 15.3, 15.9 is also described. The combination and the polymorphic form A are described for use in the treatment of tumours.
GLUCOCEREBROSIDASE MODULATORS AND USES THEREOF
The invention provides compounds for modulating glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.
GLUCOCEREBROSIDASE MODULATORS AND USES THEREOF
The invention provides compounds for modulating glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.
DEUTERATED ORGANIC COMPOUND, MIXTURE AND COMPOSITION CONTAINING SAID COMPOUND, AND ORGANIC ELECTRONIC DEVICE
The present disclosure discloses a deuterated organic compound and a formulation and an organic electronic device containing the same, wherein the deuterated organic compound has the following structural formula:
##STR00001##
wherein Ar is an aromatic or heteroaromatic structural unit, D is an electron donor group, A is an electron acceptor group, n and m are an integer between 1 and 6; and wherein for the organic compound, (S1-T1)≦0.25 eV, and at least one H atom of the organic compound is substituted by deuterium. The present disclosure achieves the improvement of the electroluminescence quantum efficiency and the lifetime of the organic compound by replacing the H atom in the organic compound with deuterium and having (S1-T1)≦0.35 eV, and the material of the present disclosure has a great application potential and application range due to its low cost and relatively simple synthesis process.
SHP2 PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF
The present disclosure relates to novel compounds including formula (X) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.
##STR00001##
SHP2 PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF
The present disclosure relates to novel compounds including formula (X) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.
##STR00001##
INDENOAZANAPHTHALENES
The present invention relates indenoazanaphthalenes, particularly for use in electronic devices. The invention further relates to a method for producing the indenoazanaphthalenes according to the invention, and to electronic devices comprising the same.
INDENOAZANAPHTHALENES
The present invention relates indenoazanaphthalenes, particularly for use in electronic devices. The invention further relates to a method for producing the indenoazanaphthalenes according to the invention, and to electronic devices comprising the same.