Patent classifications
C07F9/65128
SMALL MOLECULE MODULATORS OF HUMAN STING
The present invention relates to compounds of formula (I). The compounds maybe used to modulate the Stimulator of Interferon Genes (STING) protein and thereby treat diseases such as cancer and microbial infections.
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Organic Electronic Device Comprising an Organic Semiconductor Layer and a Device
The present invention relates to a compound of formula 1 and an organic electronic device comprising an organic semiconductor layer, wherein at least one organic semiconductor layer comprises a compound of formula (1), wherein X is selected from O, S or Se; Ar.sup.1 is selected from unsubstituted or substituted C.sub.2 to C.sub.60 heteroarylene, and wherein the substituted C.sub.2 to C.sub.60 heteroarylene comprises at least about one to about six substituents, wherein the substituent of the substituted C.sub.2 to C.sub.60 heteroarylene are independently selected from C.sub.1 to C.sub.12 alkyl, C.sub.1 to C.sub.12 alkoxy, CN, OH, halogen, C.sub.6 to C.sub.36 arylene, or C.sub.2 to C.sub.25 heteroarylene; n is 1 or 2; L.sup.1 is selected from a single bond, C.sub.1 to C.sub.4 alkyl, substituted or unsubstituted C.sub.6 to C.sub.36 arylene, wherein the substituent of substituted C.sub.6 to C.sub.36 arylene is selected from C.sub.1 to C.sub.12 alkyl, C.sub.6 to C.sub.18 arylene; L.sup.2 is selected from a single bond or C.sub.1 to C.sub.6 alkyl; R.sup.1, R.sup.2 are independently selected from substituted or unsubstituted C.sub.1 to C.sub.16 alkyl, wherein the substituent of substituted C.sub.1 to C.sub.16 alkyl is selected from C.sub.6 to C.sub.18 arylene or C.sub.2 to C.sub.12 heteroarylene; wherein the compound of formula 1 comprises at least about 4 of C.sub.6-arylene rings and a molecular mass of at least about 400 g/mol to about 1800 g/mol.
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Nucleoside prodrugs and uses related thereto
Disclosed are acyclic nucleoside prodrugs with improved metabolic stability and oral bioavailability. In general, the prodrugs are derivatives of acyclic nucleoside phosphonates containing a lipid-like moiety that can increase oral absorption and subsequent stability in the liver and plasma. Preferably, the lipid-like moiety can resist enzyme-mediated ?-oxidation, such as ?-oxidation catalyzed by cytochrome P450 enzymes. Also disclosed are pharmaceutical formulations of the acyclic nucleoside prodrugs. The acyclic nucleoside prodrugs and pharmaceutical formulations thereof can be used to treat viral infections, such as HIV infections, and/or viral-associated cancer, such as HPV-associated cancers.
SOS1 INHIBITOR CONTAINING PHOSPHORUS
The present application relates to the field of pharmaceutical chemistry, relates to an SOS1 inhibitor containing phosphorus, i.e., a compound of formula (I) and a preparation method therefor, and a pharmaceutical composition containing the compound, and relates to use thereof in the preparation of a drug for treating a disease and/or disorder related to SOS1 or regulated by SOS1.
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Nucleoside Prodrugs and Uses Related Thereto
Disclosed are acyclic nucleoside prodrugs with improved metabolic stability and oral bioavailability. In general, the prodrugs are derivatives of acyclic nucleoside phosphonates containing a lipid-like moiety that can increase oral absorption and subsequent stability in the liver and plasma. Preferably, the lipid-like moiety can resist enzyme-mediated -oxidation, such as -oxidation catalyzed by cytochrome P450 enzymes. Also disclosed are pharmaceutical formulations of the acyclic nucleoside prodrugs. The acyclic nucleoside prodrugs and pharmaceutical formulations thereof can be used to treat viral infections, such as HIV infections, and/or viral-associated cancer, such as HPV-associated cancers.
KINASE INHIBITORS
Compounds of formula I,
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have anti-inflammatory activity. Exemplary mechanisms of action include inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases. The compounds have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
Heterocyclic compound and organic light emitting device using the same
The present specification provides a heterocyclic compound, and an organic light emitting device including: a first electrode, a second electrode, and organic material layers formed of one or more layers including a light emitting layer disposed between the first electrode and the second electrode, in which one or more layers of the organic material layers include the heterocyclic compound or a compound in which a heat-curable or photo-curable functional group is introduced into the heterocyclic compound.
ENPP1 Inhibitors and Methods of Modulating Immune Response
Compounds, compositions and methods are provided for the inhibition of ENPP1. Aspects of the subject methods include contacting a sample with an ENPP1 inhibitor compound to inhibit the cGAMP hydrolysis activity of ENPP1. In some cases, the ENPP1 inhibitor compound is cell impermeable. ENPP1 inhibitor compounds can act extracellularly to block the degradation of cGAMP. Also provided are pharmaceutical compositions and methods for treating cancer. Aspects of the methods include administering to a subject a therapeutically effective amount of an ENPP1 inhibitor to treat the subject for cancer. In certain cases, the cancer is a solid tumor cancer. Also provided are methods of administering radiation therapy to a subject in conjunction with administering an ENPP1 inhibitor to the subject. The radiation therapy can be administered in the subject methods at a dosage and/or frequency effective to reduce radiation damage to the subject, but still instigate an immune response.
PURINE DERIVATIVES AS CD73 INHIBITORS FOR THE TREATMENT OF CANCER
Provided are novel compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are inhibitors of CD73 and are useful in the treatment of cancer.
TRYPTANTHRIN DERIVATIVES AND USES THEREOF
The present disclosure provides tryptanthrin derivatives that are modulators of IDO2 and pharmaceutical compositions comprising these compounds. The present disclosure further provides methods of using these compounds for the treatment of disease.