C07D231/54

Pyrazole derivatives with anticancer activity

The inventors have used a differential nuclear staining (DNS) assay to discover compounds with cytotoxic activity against the CEM cell line that has been determined to be highly sensitive to a variety of anti-cancer compounds. Compounds were synthesized based on a pyrazole backbone structure. Several newly synthesized compounds have been tested to identify the compounds with highest activity. One compound identified is the SSK-3 compound which has been tested on cancer cell lines and determined that it induced apoptosis via phosphatidylserine membrane exposure and activation of caspase 3 in the CEM lymphoma cell line.

Pyrazole derivatives with anticancer activity

The inventors have used a differential nuclear staining (DNS) assay to discover compounds with cytotoxic activity against the CEM cell line that has been determined to be highly sensitive to a variety of anti-cancer compounds. Compounds were synthesized based on a pyrazole backbone structure. Several newly synthesized compounds have been tested to identify the compounds with highest activity. One compound identified is the SSK-3 compound which has been tested on cancer cell lines and determined that it induced apoptosis via phosphatidylserine membrane exposure and activation of caspase 3 in the CEM lymphoma cell line.

Medicament for liver regeneration and for treatment of liver failure

The present invention relates to the use of a compound which inhibits the activity of MKK4 as a medicament for the treatment of a patient suffering from an impaired liver function, to the use of a compound as a medicament for the treatment of liver failure, including acute/fulminant or chronic liver failure and/or for increasing the regeneration of liver tissue in a patient.

Medicament for liver regeneration and for treatment of liver failure

The present invention relates to the use of a compound which inhibits the activity of MKK4 as a medicament for the treatment of a patient suffering from an impaired liver function, to the use of a compound as a medicament for the treatment of liver failure, including acute/fulminant or chronic liver failure and/or for increasing the regeneration of liver tissue in a patient.

Aromatic derivatives, preparation methods, and medical uses thereof
11976058 · 2024-05-07 · ·

The present disclosure relates generally to aromatic derivatives that are inhibitors of FGFR4 and are useful in treating FGFR4-associated diseases or conditions. Compositions containing the compounds of the present disclosure are also provided.

INDAZOLYL- AND INDOLYL-BENZAMIDE DERIVATIVES
20190225587 · 2019-07-25 ·

The invention relates to indazolylbenzamide, indolylbenzamide, benzo[d]imidazolyl-benzamide, and benzo[d]triazolylbenzamide derivatives of formula

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useful in the treatment and/or prevention of diseases and/or conditions related to cell proliferation, such as cancer, infection, inflammation and inflammation-associated disorders, and conditions associated with angiogenesis.

INDAZOLYL- AND INDOLYL-BENZAMIDE DERIVATIVES
20190225587 · 2019-07-25 ·

The invention relates to indazolylbenzamide, indolylbenzamide, benzo[d]imidazolyl-benzamide, and benzo[d]triazolylbenzamide derivatives of formula

##STR00001##

useful in the treatment and/or prevention of diseases and/or conditions related to cell proliferation, such as cancer, infection, inflammation and inflammation-associated disorders, and conditions associated with angiogenesis.

Pyrazole derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto

Pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT.sub.2A receptor. Formula (Ia). Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT.sub.2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together. ##STR00001##

Pyrazole derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto

Pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT.sub.2A receptor. Formula (Ia). Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT.sub.2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together. ##STR00001##

Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain

Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome. ##STR00001##