C07D253/08

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.

Process for the synthesis of amide bonds with the aid of novel catalysts

The invention relates to a process for the production of amide bonds, in particular peptide bonds, with the aid of novel amide linking reagents containing an anion of the formula (I), to the novel reagents, and to the preparation thereof.

Process for the synthesis of amide bonds with the aid of novel catalysts

The invention relates to a process for the production of amide bonds, in particular peptide bonds, with the aid of novel amide linking reagents containing an anion of the formula (I), to the novel reagents, and to the preparation thereof.

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.

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.

PROCESS FOR THE SYNTHESIS OF AMIDE BONDS WITH THE AID OF NOVEL CATALYSTS

The invention relates to a process for the production of amide bonds, in particular peptide bonds, with the aid of novel amide linking reagents containing an anion of the formula (I), to the novel reagents, and to the preparation thereof.

PROCESS FOR THE SYNTHESIS OF AMIDE BONDS WITH THE AID OF NOVEL CATALYSTS

The invention relates to a process for the production of amide bonds, in particular peptide bonds, with the aid of novel amide linking reagents containing an anion of the formula (I), to the novel reagents, and to the preparation thereof.

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.

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.

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.