C07D231/18

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:

##STR00001## or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

USE OF N-FUNCTIONALIZED ALKOXY PYRAZOLE COMPOUNDS AS NITRIFICATION INHIBITORS

The present invention relates to the use of novel nitrification inhibitors of formula (I), which are N-functionalized alkoxy pyrazole compounds. Moreover, the invention relates to the use of compounds of formula (I) as nitrification inhibitors, i.e. for reducing nitrification, as well as agrochemical mixtures and compositions comprising the nitrification inhibitors of formula (I).

UBE2K MODULATORS AND METHODS FOR THEIR USE

Provided are compounds of Formula (I):

##STR00001##

and pharmaceutically acceptable salts and compositions thereof, which are useful for treating conditions associated with modulation of UBE2K.

METHODS OF REDUCING INFLAMMATION OF THE DIGESTIVE SYSTEM WITH INHIBITORS OF HIF-2- ALPHA

The present disclosure provides methods of reducing inflammation of the digestive system in a subject in need thereof, including subjects suffering from inflammatory bowel disease. Compositions for use in these methods are also provided.

NOVEL COMPOUNDS
20200399243 · 2020-12-24 ·

The present invention relates to compounds of formula (1): wherein Q is selected from O or S; R.sup.1 is a 5-membered nitrogen-containing heteroaryl group substituted with R.sup.6 and optionally further substituted; R.sup.2 is an alpha, alpha-substituted cyclic group which may optionally be further substituted; R.sup.3 and R.sup.4 are each independently hydrogen, halogen, OH, NH.sub.2, CN, R.sup.5, OR.sup.5, NHR.sup.5 or N(R.sup.5).sub.2; or R.sup.3 and R.sup.4 together with the carbon atom to which they are attached may form a 3 to 7 membered saturated or unsaturated, optionally substituted cyclic group; R.sup.5 is independently an optionally substituted C.sub.1-C.sub.4 alkyl group; and R.sup.6 is any group comprising a nitrogen atom. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.sub.3.

##STR00001##

NOVEL COMPOUNDS
20200399243 · 2020-12-24 ·

The present invention relates to compounds of formula (1): wherein Q is selected from O or S; R.sup.1 is a 5-membered nitrogen-containing heteroaryl group substituted with R.sup.6 and optionally further substituted; R.sup.2 is an alpha, alpha-substituted cyclic group which may optionally be further substituted; R.sup.3 and R.sup.4 are each independently hydrogen, halogen, OH, NH.sub.2, CN, R.sup.5, OR.sup.5, NHR.sup.5 or N(R.sup.5).sub.2; or R.sup.3 and R.sup.4 together with the carbon atom to which they are attached may form a 3 to 7 membered saturated or unsaturated, optionally substituted cyclic group; R.sup.5 is independently an optionally substituted C.sub.1-C.sub.4 alkyl group; and R.sup.6 is any group comprising a nitrogen atom. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.sub.3.

##STR00001##

PYRAZOLYL SUBSTITUTED CARBONIC ACID DERIVATIVES AS MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).

##STR00001##

PYRAZOLYL SUBSTITUTED CARBONIC ACID DERIVATIVES AS MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

Pyrazole derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH) and related disorders; platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation in an angioplasty or coronary bypass surgery individual or in an individual suffering from atrial fibrillation; atherosclerosis; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder such as diabetic peripheral neuropathy, diabetic nephropathy or diabetic retinopathy; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; ischemia-reperfusion injury; restenosis; atherosclerosis; acne; type 1 diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).

##STR00001##

SUBSTITUTED HETEROCYCLES AS c-MYC TARGETING AGENTS

Disclosed are substituted heterocycle compounds including substituted pyrazoles, substituted pyrimidines, and substitute triazoles. The substituted heterocycles disclosed herein are shown to be useful in inhibiting c-MYC and may be utilized as therapeutics for treating cancer and cell proliferative disorders.

SUBSTITUTED HETEROCYCLES AS c-MYC TARGETING AGENTS

Disclosed are substituted heterocycle compounds including substituted pyrazoles, substituted pyrimidines, and substitute triazoles. The substituted heterocycles disclosed herein are shown to be useful in inhibiting c-MYC and may be utilized as therapeutics for treating cancer and cell proliferative disorders.