C07D317/66

CATALYST FOR CONVERTING ESTER TO AMIDE USING HYDROXYL GROUP AS ORIENTATION GROUP

Provided is a method for amidating a hydroxy ester compound at a high chemical selectivity. The amidation reaction method for a hydroxy ester compound comprises, in the presence of a catalyst containing a compound of a transition metal of the group 4 or group 5 in the periodic table, reacting at least one kind of hydroxy ester compound selected from the group consisting of an -hydroxy ester compound, a -hydroxy ester compound, a -hydroxy ester compound and a -hydroxy ester compound with an amino compound so as to amidate an ester group having a hydroxyl group at the -, -, - or -position of the hydroxy ester compound.

Sulfonylureas and related compounds and use of same

The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, solvates and prodrugs thereof: ##STR00001##
wherein Q is selected from O, S and Se; J is S or Se; W.sup.1 and W.sup.2, when present, are independently selected from N and C; R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen, C.sub.1-C.sub.12 alkyl, C.sub.2-C.sub.12 alkenyl, C.sub.2-C.sub.12 alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, cycloalkenyl, amino, amido, alkylthio, acyl, arylalkyl and acylamido, all of which may be optionally substituted; and wherein at least one of W.sup.1 and W.sup.2 is present and is a nitrogen atom and when R.sup.1 or R.sup.2 are cyclic then the respective W.sup.1 or W.sup.2 may form part of the ring structure. The present invention also relates to pharmaceutical compositions including such compounds, to methods of treatment using such compounds, in particular in relation to NLRP3 inflammasome mediated disorders, and to associated diagnostic uses.

Sulfonylureas and related compounds and use of same

The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, solvates and prodrugs thereof: ##STR00001##
wherein Q is selected from O, S and Se; J is S or Se; W.sup.1 and W.sup.2, when present, are independently selected from N and C; R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen, C.sub.1-C.sub.12 alkyl, C.sub.2-C.sub.12 alkenyl, C.sub.2-C.sub.12 alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, cycloalkenyl, amino, amido, alkylthio, acyl, arylalkyl and acylamido, all of which may be optionally substituted; and wherein at least one of W.sup.1 and W.sup.2 is present and is a nitrogen atom and when R.sup.1 or R.sup.2 are cyclic then the respective W.sup.1 or W.sup.2 may form part of the ring structure. The present invention also relates to pharmaceutical compositions including such compounds, to methods of treatment using such compounds, in particular in relation to NLRP3 inflammasome mediated disorders, and to associated diagnostic uses.

UREA MOTIF CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS ANTIBACTERIAL DRUGS
20210009550 · 2021-01-14 ·

The invention relates to compounds which are suitable for treating bacterial diseases and to pharmaceutical compositions containing such compounds. The invention further relates to a kit of parts comprising such compounds and to the use of such compounds as disinfectants.

UREA MOTIF CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS ANTIBACTERIAL DRUGS
20210009550 · 2021-01-14 ·

The invention relates to compounds which are suitable for treating bacterial diseases and to pharmaceutical compositions containing such compounds. The invention further relates to a kit of parts comprising such compounds and to the use of such compounds as disinfectants.

Human GLUT5 specific inhibitors and methods of treatment

The present invention relates to compounds which have been discovered to be potent ligands (inhibitors) of human GLUT5 (glucose transporter type 5), a facilitative glucose transporter that transports fructose, and their use as ligands assays which can uncover additional ligands of GLUT5, having the potential for being used as drugs. In addition, the present invention is directed to compounds, chemical compositions and methods for treating disease states and conditions which are mediated through GLUT5, including such disease states and conditions as GLUT5 deficiency syndrome, diabetes (type I and II), cancer, metabolic diseases including metabolic syndrome and fatty liver disease, among others.

Human GLUT5 specific inhibitors and methods of treatment

The present invention relates to compounds which have been discovered to be potent ligands (inhibitors) of human GLUT5 (glucose transporter type 5), a facilitative glucose transporter that transports fructose, and their use as ligands assays which can uncover additional ligands of GLUT5, having the potential for being used as drugs. In addition, the present invention is directed to compounds, chemical compositions and methods for treating disease states and conditions which are mediated through GLUT5, including such disease states and conditions as GLUT5 deficiency syndrome, diabetes (type I and II), cancer, metabolic diseases including metabolic syndrome and fatty liver disease, among others.

Compounds and methods for hematopoietic regeneration

The invention relates to compounds that promote hematopoietic regeneration. The invention further relates to methods of promoting hematopoietic regeneration using the novel compounds of the invention.

Compounds and methods for hematopoietic regeneration

The invention relates to compounds that promote hematopoietic regeneration. The invention further relates to methods of promoting hematopoietic regeneration using the novel compounds of the invention.

Antagonists of the glucagon receptor

The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof and pharmaceutical compositions comprising the same.