C07C311/58

MODULATORS OF MAS-RELATED G-PROTEIN RECEPTOR X4 AND RELATED PRODUCTS AND METHODS

Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I).

##STR00001##

or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q.sub.1, Q.sub.2, Z, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS

The present invention relates to compounds of formula (I): Formula (I) wherein Q is selected from O or S; L is a saturated or unsaturated, optionally substituted C.sub.1-C.sub.12 hydrocarbylene group optionally including one or more heteroatoms N, O or S; R.sup.1 is NR.sup.3R.sup.4, OR.sup.5, (CNR.sup.6)R.sup.7, (CO)R.sup.8, CN, N.sub.3, a quaternary ammonium group or an optionally substituted heterocycle; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are each independently hydrogen or a saturated or unsaturated, optionally substituted C.sub.1-C.sub.10 hydrocarbyl group optionally including one or more heteroatoms N, O or S; wherein optionally L and R.sup.3, or L and R.sup.4, or R.sup.3 and R.sup.4, or L and R.sup.5, or L and R.sup.6, or L and R.sup.7, or R.sup.6 and R.sup.7, or L and R.sup.8 together with the atom(s) to which they are attached may form a 3- to 12-membered, saturated or unsaturated, optionally substituted cyclic group; and R.sup.2 is a cyclic group substituted at the a-position, wherein R.sup.2 may optionally be further substituted; provided that the atom of L which is attached to the sulfur atom of the sulfonylurea group is a carbon atom and is not a ring atom of a heterocyclic or aromatic group. 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##

Protoporphyrinogen oxidase inhibitors

The present invention relates to protoporphyrinogen IX oxidase (PPO) inhibitors of the general formula (I) ##STR00001## where the variables are defined herein. The invention features processes and intermediates for preparing the compounds of formula (I), compositions comprising them, and their use as herbicidese.g., for controlling harmful plants. The invention also features methods for controlling unwanted vegetation comprising allowing an herbicidal effective amount of at least one PPO inhibitor of formula (I) to act on plants, their seed, and/or their habitat.

THROMBOXANE RECEPTOR ANTAGONISTS
20190336513 · 2019-11-07 ·

The invention relates to novel chemical entities that act as thromboxane (TX) A.sub.2 receptor, or T prostanoid receptor (TP), antagonists and to their use in the treatment of human diseases in which thromboxane (TX) A and of all other agents that act as incidental ligands of TP, including the endoperoxide prostaglandin (PG)G.sub.2/PGH.sub.2, 20-hydroxyeicosatetraenoic acid (20-HETE) and the free-radical derived isoprostanes (e.g., 8-iso-prostaglandin (PG)F.sub.2), play a role. Compounds of the invention preferably include a benzenesulfonyl urea in which the benzene is substituted by a substituted biphenylyloxy group (e.g., at the 2 position) and by a nitrile group (e.g., at the 5 position), which compounds show promising results as TP-isoform selective TP antagonists.

THROMBOXANE RECEPTOR ANTAGONISTS
20190336513 · 2019-11-07 ·

The invention relates to novel chemical entities that act as thromboxane (TX) A.sub.2 receptor, or T prostanoid receptor (TP), antagonists and to their use in the treatment of human diseases in which thromboxane (TX) A and of all other agents that act as incidental ligands of TP, including the endoperoxide prostaglandin (PG)G.sub.2/PGH.sub.2, 20-hydroxyeicosatetraenoic acid (20-HETE) and the free-radical derived isoprostanes (e.g., 8-iso-prostaglandin (PG)F.sub.2), play a role. Compounds of the invention preferably include a benzenesulfonyl urea in which the benzene is substituted by a substituted biphenylyloxy group (e.g., at the 2 position) and by a nitrile group (e.g., at the 5 position), which compounds show promising results as TP-isoform selective TP antagonists.

PROTOPORPHYRINOGEN OXIDASE INHIBITORS

The present invention relates to protoporphyrinogen IX oxidase (PPO) inhibitors of the general formula (I)

##STR00001##

where the variables are defined herein. The invention features processes and intermediates for preparing the compounds of formula (I), compositions comprising them, and their use as herbicidese.g., for controlling harmful plants. The invention also features methods for controlling unwanted vegetation comprising allowing an herbicidal effective amount of at least one PPO inhibitor of formula (I) to act on plants, their seed, and/or their habitat.

Heat-sensitive recording material

A heat-sensitive recording material includes a heat-sensitive recording layer containing a basic dye and a developer and provided on a supporting body, in which the developer is at least one type of an N-substituted amino acid derivative represented by the following General Formula: (RX).sub.mY(Z).sub.m . . . (1) (In Formula (1), R represents an alkyl group or an aryl group which may have a substituent. X is a group bonded to the N-terminus of Y, and represents OCO, SO.sub.2NHCO, NHCO, NHCS, or SO.sub.2. Y represents an amino acid residue or a peptide residue. Z represents a group bonded to the C-terminus of Y and represents an OH group or an OR group. When Y is an amino acid residue other than a cystine residue or when Y is a peptide residue not having a cystine residue, m=1, and when Y is a peptide residue having n cystine residues, m=n+1 and n is 1 or 2.)

MODULATORS OF MAS-RELATED G-PROTEIN RECEPTOR X4 AND RELATED PRODUCTS AND METHODS

Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I):

##STR00001##

or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q.sub.1, Q.sub.2, Z, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

Inhibitors of human immunodeficiency virus replication

Compounds of Formula I with activity against HIV, including pharmaceutical compositions and methods for using these compounds in treating human immunodeficiency virus (HIV) infection, are set forth: ##STR00001##

Inhibitors of human immunodeficiency virus replication

Compounds of Formula I with activity against HIV, including pharmaceutical compositions and methods for using these compounds in treating human immunodeficiency virus (HIV) infection, are set forth: ##STR00001##