Patent classifications
C07D277/46
DEUTERATED AND TRITIATED N-(4,5-DIMETHYLTHIAZOLO-2(3H)-YLIDEN)-2,2,3,3-TETRAMETHYLCYCLOPROPANE-1-CARBOXAMIDE DERIVATIVES AND THE USE THEREOF
Compounds of general formula I
##STR00001##
X.sup.1 is a CD.sub.2 group or a CT.sub.2 group; X.sup.2 is oxygen or a group (CZ.sup.1Z.sup.2).sub.n, wherein Z.sup.1 and Z.sup.2 on each occurrence independently each are hydrogen, deuterium, or tritium and n is an integer from 1 to 12; X.sup.3 is a CD.sub.2 group or a CT.sub.2 group; and R is selected from the group consisting of hydroxy, -NO.sub.2, halogen, a diazonium ion, a diazonium salt, a trialkylammonium ion, a trialkylammonium salt, a dialkoxyarene, a sulphoxide, a boronic acid, a boronic acid ester, an organotin compound, an iodonium ion, an iodonium salt, an iodonium ylide, and a sulphonate.
Aminothiazole compounds as c-Kit inhibitors
The invention relates to c-Kit inhibitors useful in the treatment of cancers, and other serine-threonine kinase mediated diseases, having the Formula: ##STR00001##
wherein A, L, R.sub.1, R.sub.2, R.sub.3, and n are described herein.
Aminothiazole compounds as c-Kit inhibitors
The invention relates to c-Kit inhibitors useful in the treatment of cancers, and other serine-threonine kinase mediated diseases, having the Formula: ##STR00001##
wherein A, L, R.sub.1, R.sub.2, R.sub.3, and n are described herein.
EIF4E inhibitors and uses thereof
The present invention provides compounds inhibiting eIF4E activity, and compositions and methods of using thereof.
SUBSTITUTED AMINOTHIAZOLES AS DGKZETA INHIBITORS FOR IMMUNE ACTIVATION
The present invention covers aminothiazole compounds of general formula (I), in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of diacylglycerol kinase zeta (DGKζ) regulated disorders, as a sole agent or in combination with other active ingredients.
##STR00001##
SUBSTITUTED AMINOTHIAZOLES AS DGKZETA INHIBITORS FOR IMMUNE ACTIVATION
The present invention covers aminothiazole compounds of general formula (I), in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of diacylglycerol kinase zeta (DGKζ) regulated disorders, as a sole agent or in combination with other active ingredients.
##STR00001##
NEPRILYSIN INHIBITORS
In one aspect, the invention relates to compounds having the formula:
##STR00001##
where R.sup.1-R.sup.6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
NEPRILYSIN INHIBITORS
In one aspect, the invention relates to compounds having the formula:
##STR00001##
where R.sup.1-R.sup.6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.