C07C275/28

NOVEL COMPOUND HAVING ANTICANCER ACTIVITY, AND METHOD FOR PRODUCING SAME
20220204497 · 2022-06-30 ·

The present invention pertains to a novel compound having anticancer activity, and a method for producing same, and more specifically, to a novel compound that exhibits excellent anticancer activity by inhibiting the expression of AIMP2-DX2, and a method for producing same. The compound represented by chemical formula 1 according to the present invention is highly effective in inhibiting the expression of AIMP2-DX2, and thus can be very advantageously used for the development of agents for treating various diseases, in particular cancer, caused by AIMP2-DX2.

Urea derivatives and methods of use thereof

The present disclosure relates to compounds of Formula (I): and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein inhibit the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inter alia autoinflammatory and autoimmune diseases and cancers. ##STR00001##

Urea derivatives and methods of use thereof

The present disclosure relates to compounds of Formula (I): and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein inhibit the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inter alia autoinflammatory and autoimmune diseases and cancers. ##STR00001##

SOLID DRUG FORM OF N-(2,6-BIS(1-METHYLETHYL)PHENYL)-N'-((1-(4-(DIMETHYLAMINO)PHENYL)CYCLOPENTYL)METHYL)UREA HYDROCHLORIDE AND COMPOSITIONS, METHODS AND KITS RELATED THERETO

A novel solid drug form of N-(2,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride (also referred to “ATR-101”) suitable for oral dosing, and to compositions, methods and kits relating thereto. ATR-101 has particular utility in the treatment of, for example, aberrant adrenocortical cellular activity, including adrenocortical carcinoma (ACC), congenital adrenal hyperplasia (CAH) and Cushing's syndrome.

SOLID DRUG FORM OF N-(2,6-BIS(1-METHYLETHYL)PHENYL)-N'-((1-(4-(DIMETHYLAMINO)PHENYL)CYCLOPENTYL)METHYL)UREA HYDROCHLORIDE AND COMPOSITIONS, METHODS AND KITS RELATED THERETO

A novel solid drug form of N-(2,6-bis(1-methylethyl)phenyl)-N′-((1-(4-(dimethylamino)phenyl)cyclopentyl)methyl)urea hydrochloride (also referred to “ATR-101”) suitable for oral dosing, and to compositions, methods and kits relating thereto. ATR-101 has particular utility in the treatment of, for example, aberrant adrenocortical cellular activity, including adrenocortical carcinoma (ACC), congenital adrenal hyperplasia (CAH) and Cushing's syndrome.

UREA DERIVATIVE

An object of the present invention is to find a novel pharmaceutical that has an excellent tryptophanase inhibitory effect and suppresses worsening of renal function to preserve the kidney by reducing production of indoxyl sulfate in the blood. The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound represented by the following formula, or a pharmacologically acceptable salt thereof:

##STR00001##

wherein R.sup.1 and R.sup.2 are the same or different, and represent a C.sub.1-C.sub.6 alkyl group or the like, and Ar represents an optionally substituted phenyl group or an optionally substituted thienyl group.

Synthetic receptors for hydrosulfide

A method for detecting for the presence of H.sub.2S or HS.sup.− anion in a system, comprising contacting a sample from the system with a compound, or a protonate or salt thereof, having a structure represented by: ##STR00001## wherein Y represents an aromatic group or a substituted aromatic group; n is 1 or 2; R is independently H, alkyl, substituted alkyl, a polyether moiety, carboxyl, substituted carboxyl, carbamate, substituted carbonate, carbonyloxy, alkoxy, substituted alkoxy, haloalkyl, halogen, nitro, amino, amido, aryloxy, cyano, hydroxyl, or sulfonyl; R.sup.1 is H, substituted lower alkyl, lower alkyl, substituted aralkyl or aralkyl; R.sup.2 is selected from H, acyl, substituted aralkyl, aralkyl, phosphonyl, —SO.sub.2R.sup.3; —C(O)R.sup.5; —C(O)OR.sup.7 or —C(O)NR.sup.9R.sup.10; R.sup.3; R.sup.5; R.sup.7; R.sup.9 and R.sup.10 are each independently selected from H, substituted lower alkyl, lower alkyl, substituted aralkyl, aralkyl, substituted aryl or aryl.

N-TRIFLUORMETHYLCARBONYL COMPOUNDS AND METHODS FOR THEIR SYNTHESIS

The present invention relates to the synthesis of N-trifluoromethylcarbonyl compounds starting from isothiocyanates, which can be converted into N-trifluoromethylcarbamoyl fluorides or similar compounds, which later on can be derivatized further to amides, ureas, carbamates, thiocarbamates and selenocarbamates.

N-TRIFLUORMETHYLCARBONYL COMPOUNDS AND METHODS FOR THEIR SYNTHESIS

The present invention relates to the synthesis of N-trifluoromethylcarbonyl compounds starting from isothiocyanates, which can be converted into N-trifluoromethylcarbamoyl fluorides or similar compounds, which later on can be derivatized further to amides, ureas, carbamates, thiocarbamates and selenocarbamates.

METHOD FOR CONVERTING MONOISOCYANATES TO UREAS

Organic isocyanates are converted to ureas by heating in the presence of certain cobalt, magnesium, chromium and lanthanide series organometallic catalysts. The process requires no water or other reactants. The process is particularly useful for removing small quantities of monoisocyanates from a solvent stream recovered from a polyisocyanate manufacturing process. The urea compounds in some instances can be recycled back into the polyisocyanate manufacturing process and reacted with polyisocyanate compounds to form biurets.