C07D237/20

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.

Compounds and their use

The specification generally relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where A, U, V, W, X, Y, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meanings defined herein. Such compounds are modulators of RXFP1 and may be useful as therapeutic agents. The specification also relates to the use of such compounds to treat or prevent diseases and conditions including heart failure, heart failure with preserved ejection fraction, heart failure with mid-range ejection fraction, heart failure with reduced ejection fraction, chronic kidney disease and acute kidney injury. The specification further relates to compositions comprising such compounds, intermediates useful in processes for preparing such compounds, and processes for preparing such compounds using such intermediates.

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.

Benzenesulfonyl-Asymmetric Ureas and Medical Uses Thereof
20170275301 · 2017-09-28 ·

Benzenesulfonyl-asymmetric ureas are provided for the treatment of conditions modulated by the ghrelin receptor.

Benzenesulfonyl-Asymmetric Ureas and Medical Uses Thereof
20170275301 · 2017-09-28 ·

Benzenesulfonyl-asymmetric ureas are provided for the treatment of conditions modulated by the ghrelin receptor.

Flap modulators

The present invention relates to compounds of Formula (I), or a form thereof wherein ring A.sub.1, R.sub.1, R.sub.2, R.sub.3, R.sub.3′, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention. ##STR00001##

Flap modulators

The present invention relates to compounds of Formula (I), or a form thereof wherein ring A.sub.1, R.sub.1, R.sub.2, R.sub.3, R.sub.3′, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention. ##STR00001##

Diamino-pyridine, pyrimidine, and pyridazine modulators of the histamine H4 receptor

Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H.sub.4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H.sub.4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.

Diamino-pyridine, pyrimidine, and pyridazine modulators of the histamine H4 receptor

Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H.sub.4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H.sub.4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.

FLAP modulators

The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R.sub.1, L and R.sub.2 are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention. ##STR00001##