The present invention related to novel sulfonamides or amides as TLR-4 antagonists, and pharmaceutical formulations containing the same and the methods of use thereof. Uses of the present novel sulfonamides or amides include, but are not limited to, the prophylaxis and/or treatment of autoimmune, inflammation, or infection related disorders.

An electrophotographic photosensitive member (1) includes a conductive substrate (2) and a photosensitive layer (3). The photosensitive layer (3) is a single-layer photosensitive layer (3c) and contains a charge generating material, a hole transport material, an electron transport material, and a binder resin. The binder resin includes a polyarylate resin represented by general formula (1). ##STR00001##
In general formula (1), Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 each represent a methyl group or a hydrogen atom. r, s, t, and u each represent a number greater than or equal to 15 and less than or equal to 35. X and Y each represent a divalent group represented by chemical formula (2A), chemical formula (2B), chemical formula (2C), or chemical formula (2D), and X and Y are different from each other ##STR00002##

An electrophotographic photosensitive member (1) includes a conductive substrate (2) and a photosensitive layer (3). The photosensitive layer (3) is a single-layer photosensitive layer (3c) and contains a charge generating material, a hole transport material, an electron transport material, and a binder resin. The binder resin includes a polyarylate resin represented by general formula (1). ##STR00001##
In general formula (1), Q.sup.1, Q.sup.2, Q.sup.3, and Q.sup.4 each represent a methyl group or a hydrogen atom. r, s, t, and u each represent a number greater than or equal to 15 and less than or equal to 35. X and Y each represent a divalent group represented by chemical formula (2A), chemical formula (2B), chemical formula (2C), or chemical formula (2D), and X and Y are different from each other ##STR00002##

The present invention relates to a sodium salt of N-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-1-isopropyl-1H-pyrazole-3-sulfonamide and to hydrates, solvates and polymorphic forms thereof. The present invention further relates to pharmaceutical compositions comprising this compound and the use of this compound in the treatment and prevention of medical disorders and diseases, most especially by NLRP3 inhibition.

Substituted hydroquinones and quinones and methods of synthesizing such compounds are disclosed herein. The substituted hydroquinones have the formula:

##STR00001##

while the substituted quinones have the corresponding oxidized structure (1,4-benzoquinones). One, two, three, or all four of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 comprise a thioether moiety and a sulfonate moiety, and wherein each R.sup.1, R.sup.2, R.sup.3 and R.sup.4 that does not comprise a thioether and a sulfonate moiety sulfonate moiety is independently a hydrogen, an alkyl or an electron withdrawing group.

The substituted hydroquinones and quinones are soluble in water, stable in aqueous acid solutions, and have a high reduction potential in the oxidized form. Accordingly, they can be used as redox mediators in emerging technologies, such as in mediated fuel cells or organic-mediator flow batteries.

Substituted hydroquinones and quinones and methods of synthesizing such compounds are disclosed herein. The substituted hydroquinones have the formula:

##STR00001##

while the substituted quinones have the corresponding oxidized structure (1,4-benzoquinones). One, two, three, or all four of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 comprise a thioether moiety and a sulfonate moiety, and wherein each R.sup.1, R.sup.2, R.sup.3 and R.sup.4 that does not comprise a thioether and a sulfonate moiety sulfonate moiety is independently a hydrogen, an alkyl or an electron withdrawing group.

The substituted hydroquinones and quinones are soluble in water, stable in aqueous acid solutions, and have a high reduction potential in the oxidized form. Accordingly, they can be used as redox mediators in emerging technologies, such as in mediated fuel cells or organic-mediator flow batteries.

The present invention relates to compounds of formula (I): wherein Q is O or S; R.sup.1 is a cyclic group substituted with at least one group X, wherein R.sup.1 may optionally be further substituted; X is any group comprising a carbonyl group; and R.sup.2 is a cyclic group substituted at the -position, wherein R.sup.2 may optionally be further substituted. 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 dual action of NLRP.sub.3 inhibition and the stimulation of insulin secretion.

##STR00001##

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##

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##

The present invention provides processes for preparation of substituted pyrazole compounds of formula II, that can be used as intermediates for preparation of substituted piperidine urea compounds useful for the treatment of dilated cardiomyopathy (DCM). R.sup.2 is independently selected from F, C1-C4 alkyl, C1-C4 haloalkyl, R.sup.3 is independently selected from H, F, C1-C4 alkyl, C1-C4 haloalkyl, R.sup.4 is C1-C4 alkyl, R.sup.6 is H or a protecting group and R.sup.7 is selected from H, CI or trialkylsilyl. ##STR00001##