Patent classifications
C07D239/28
METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.
HERBICIDAL COMPOUNDS
The present invention relates to compounds of Formula (I), or an agronomically acceptable salt of said compounds wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I) and to the use of compounds of Formula (I) for controlling weeds, in particular in crops of useful plants.
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PYRIDINE AND PYRIMIDINE CARBOXYLATE HERBICIDES AND METHODS OF USE THEREOF
Provided herein are pyridine and pyrimidine carboxylates and their derivatives, and compositions and methods of use thereof as herbicides.
PYRIDINE AND PYRIMIDINE CARBOXYLATE HERBICIDES AND METHODS OF USE THEREOF
Provided herein are pyridine and pyrimidine carboxylates and their derivatives, and compositions and methods of use thereof as herbicides.
Compounds as autotaxin inhibitors and pharmaceutical compositions comprising the same
The present invention relates to novel compounds as autotoxin inhibitors for treatment and prophylaxis of conditions or a disorder caused by autotaxin activation or increased concentration of lysophosphatidic acid, and also a pharmaceutical composition containing the same. The novel compounds of the present invention are autotoxin inhibitors, and by inhibiting the production of lysophosphatidic acid, they are useful for treatment or prophylaxis of cardiovascular disorder, cancer, metabolic disorder, kidney disorder, liver disorder, inflammatory disorder, nervous system disorder, respiratory system disorder, fibrotic disease, ocular disorder, cholestatic and other forms of chronic pruritus, or acute or chronic organ transplant rejection.
2-phenylpyrimidine-4-carboxamides as AHR inhibitors
The present invention covers 2-phenylpyrimidine-4-carboxamide compounds of general formula (I): (I) 5 in which X, Y, Z, R1, R2, R4, R5 and R6 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with 10 dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients. ##STR00001##
2-phenylpyrimidine-4-carboxamides as AHR inhibitors
The present invention covers 2-phenylpyrimidine-4-carboxamide compounds of general formula (I): (I) 5 in which X, Y, Z, R1, R2, R4, R5 and R6 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with 10 dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients. ##STR00001##
TRIARYL COMPOUNDS FOR TREATMENT OF PD-L1 DISEASES
Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I)
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including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.2a, R.sup.2b, R.sup.3, R.sup.3a, R.sup.4, R.sup.6, R.sup.7, R.sup.8, A, Z, X.sup.1 and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
P38ALPHA MITOGEN-ACTIVATED PROTEIN KINASE INHIBITORS
Disclosed herein are p38α mitogen-activated protein kinase inhibitors, pharmaceutical compositions thereof, and therapeutic methods of using the p38α mitogen-activated protein kinase inhibitors.
ACSS2 INHIBITORS AND METHODS OF USE THEREOF
The present invention relates to novel ACSS2 inhibitors having activity as anti-cancer therapy, treatment of alcoholism, and viral infection (e.g., CMV), composition and methods of preparation thereof, and uses thereof for treating viral infection, alcoholism, alcoholic steatohepatitis (ASH), non-alcoholic steatohepatitis (NASH), obesity/weight gain, anxiety, depression, post-traumatic stress disorder, inflammatory/autoimmune conditions and cancer, including metastatic cancer, advanced cancer, and dmg resistant cancer of various types.