C07D253/08

Substituted pyrido[3,4-d]pyrimidines and pyrido[4,3-d]pyrimidines as p70S6K inhibitors

Novel azaquinazoline carboxamide derivatives of formula (I) ##STR00001##
wherein W.sup.1, W.sup.2, W.sup.3, W.sup.4, R.sup.1, R.sup.2, R.sup.3 and m which are defined above, are p70S6K inhibitor, and can be employed, inter alia, for the treatment of hyperproliferative disorders.

4-OXO-3,4-DIHYDRO-1,2,3-BENZOTRIAZINE MODULATORS OF GPR139

The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1:

##STR00001##

which are agonists of GPR139, certain compounds encompassed by formula 1, pharmaceutical compositions thereof, processes for making the compounds, and intermediates thereof.

4-OXO-3,4-DIHYDRO-1,2,3-BENZOTRIAZINE MODULATORS OF GPR139

The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1:

##STR00001##

which are agonists of GPR139, certain compounds encompassed by formula 1, pharmaceutical compositions thereof, processes for making the compounds, and intermediates thereof.

RADIOLABELLED mGluR2/3 PET LIGANDS

The present invention relates to novel, radiolabeled mGluR2/3 ligands, selective versus other mGlu receptors which are useful for imaging and quantifying the metabotropic glutamate receptor mGlu2 and 3 in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a mammal, in vitro or in vivo and to precursors of said compounds.

RADIOLABELLED mGluR2/3 PET LIGANDS

The present invention relates to novel, radiolabeled mGluR2/3 ligands, selective versus other mGlu receptors which are useful for imaging and quantifying the metabotropic glutamate receptor mGlu2 and 3 in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a mammal, in vitro or in vivo and to precursors of said compounds.

4-OXO-3,4-dihydro-1,2,3-benzotriazine modulators of GPR139

The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1: ##STR00001##
which are agonists of GPR139, certain compounds encompassed by formula 1, pharmaceutical compositions thereof, processes for making the compounds, and intermediates thereof.

4-OXO-3,4-dihydro-1,2,3-benzotriazine modulators of GPR139

The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1: ##STR00001##
which are agonists of GPR139, certain compounds encompassed by formula 1, pharmaceutical compositions thereof, processes for making the compounds, and intermediates thereof.

SUBSTITUTED BENZAZINONES AS ANTIBACTERIAL COMPOUNDS

The present invention relates to LpxC antibacterial compounds of Formula (IA):

##STR00001##

corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, compound preparation, treatment methods and uses for bacterial infections, especially those caused by gram-negative bacteria.

SUBSTITUTED BENZAZINONES AS ANTIBACTERIAL COMPOUNDS

The present invention relates to LpxC antibacterial compounds of Formula (IA):

##STR00001##

corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, compound preparation, treatment methods and uses for bacterial infections, especially those caused by gram-negative bacteria.

NEPRILYSIN INHIBITORS

In one aspect, the invention relates to compounds having the formula XII:

##STR00001##

where R.sup.a, R.sup.b, R.sup.2, R.sup.7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.