A61K31/50

Quinone-masked probes as labeling reagents for cell uptake measurements

Provided are labeling reagents and methods of using the reagents for cell uptake measurements. The labeling reagents can be quinone-masked probes including fluorophores and/or luminophores.

Inhibitors of indoleamine 2,3-dioxygenase and methods of their use

There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the disclosure.

NLRP3 inflammasome inhibitors

The present invention relates to novel pyridazin-3-yl phenol compounds of Formula (I): ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Z are defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of diseases and disorders mediated by NLRP3.

NLRP3 inflammasome inhibitors

The present invention relates to novel pyridazin-3-yl phenol compounds of Formula (I): ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Z are defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammasome activity. The invention further relates to the processes for their preparation, pharmaceutical compositions and medicaments containing them, and their use in the treatment of diseases and disorders mediated by NLRP3.

USE OF PIMOBENDAN FOR THE REDUCTION OF HEART SIZE AND/OR THE DELAY OF ONSET OF CLINICAL SYMPTOMS IN PATIENTS WITH ASYMPTOMATIC HEART FAILURE DUE TO MITRAL VALVE DISEASE
20170290829 · 2017-10-12 ·

The invention relates to pimobendan for use in a method of reducing the heart size and/or delaying the onset of clinical symptoms in a patient suffering from asymptomatic (occult, preclinical) heart failure, preferably congestive heart failure, due to mitral valve disease (MVD), and/or delaying the onset of heart failure, preferably congestive heart failure, in a patient suffering from asymptomatic (occult, preclinical) heart failure, preferably congestive heart failure, due to mitral valve disease (MVD), wherein the patient is preferably a mammal, more preferably a human, a dog, a cat or a horse, and most preferably a dog.

USE OF PIMOBENDAN FOR THE REDUCTION OF HEART SIZE AND/OR THE DELAY OF ONSET OF CLINICAL SYMPTOMS IN PATIENTS WITH ASYMPTOMATIC HEART FAILURE DUE TO MITRAL VALVE DISEASE
20170290829 · 2017-10-12 ·

The invention relates to pimobendan for use in a method of reducing the heart size and/or delaying the onset of clinical symptoms in a patient suffering from asymptomatic (occult, preclinical) heart failure, preferably congestive heart failure, due to mitral valve disease (MVD), and/or delaying the onset of heart failure, preferably congestive heart failure, in a patient suffering from asymptomatic (occult, preclinical) heart failure, preferably congestive heart failure, due to mitral valve disease (MVD), wherein the patient is preferably a mammal, more preferably a human, a dog, a cat or a horse, and most preferably a dog.

UREA AND BIS-UREA BASED COMPOUNDS AND ANALOGUES THEREOF USEFUL IN THE TREATMENT OF ANDROGEN RECEPTOR MEDIATED DISEASES OR DISORDERS
20170273922 · 2017-09-28 ·

Urea-based and bis-urea based compounds and analogues thereof are disclosed. These compounds are useful in the treatment of androgen-dependent diseases or disorders and androgen receptor-mediated diseases or disorders. Specifically, the compounds are useful in the treatment of diseases or disorders that are AR negative.

UREA AND BIS-UREA BASED COMPOUNDS AND ANALOGUES THEREOF USEFUL IN THE TREATMENT OF ANDROGEN RECEPTOR MEDIATED DISEASES OR DISORDERS
20170273922 · 2017-09-28 ·

Urea-based and bis-urea based compounds and analogues thereof are disclosed. These compounds are useful in the treatment of androgen-dependent diseases or disorders and androgen receptor-mediated diseases or disorders. Specifically, the compounds are useful in the treatment of diseases or disorders that are AR negative.

UREA AND BIS-UREA BASED COMPOUNDS AND ANALOGUES THEREOF USEFUL IN THE TREATMENT OF ANDROGEN RECEPTOR MEDIATED DISEASES OR DISORDERS
20170273922 · 2017-09-28 ·

Urea-based and bis-urea based compounds and analogues thereof are disclosed. These compounds are useful in the treatment of androgen-dependent diseases or disorders and androgen receptor-mediated diseases or disorders. Specifically, the compounds are useful in the treatment of diseases or disorders that are AR negative.

FLUORINATED PYRIDAZIN-3-ONES FOR THE USE THEREOF IN THE TREATMENT OF LUNG DISEASES

The present invention concerns compounds belonging to the family of fluorinated pyridazin-3-ones, for the use thereof in the treatment of broncho-pulmonary conditions. In compounds having a formula, or a pharmaceutically acceptable salt of the compound, the formula includes R1 representing H, an alkyl, an aryl or a heteroaryl; either E2 and E3 representing, separately from each other, H, an alkyl, an aryl or a heteroaryl, or R2 and R3 being bridged within a same cycle or via several cycles; and F representing CF.sub.3, (CF.sub.2)nCF.sub.3 or CF.sub.2H, with n representing an integer of between 1 and 7.