The present invention is directed to benzoimidazole compounds of the formula:

##STR00001##

and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.

The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

Pyrimidine derivatives of formula (I):

##STR00001##

optionally with a detectable isotope, pharmaceutical composition and method of preparation thereof. Pyrimidine derivatives for use in treatment or prevention of bacterial infection in a host mammal in need of such treatment or prevention and use as inhibitors of biofilm formation on a surface of biomaterial or medical device, particularly of cardiovascular device such as prosthetic heart valve or pacemakers. Pyrimidine derivatives for use as radiotracer in diagnosing or prognosing bacterial infection in a host mammal.

Pyrimidine derivatives of formula (I):

##STR00001##

optionally with a detectable isotope, pharmaceutical composition and method of preparation thereof. Pyrimidine derivatives for use in treatment or prevention of bacterial infection in a host mammal in need of such treatment or prevention and use as inhibitors of biofilm formation on a surface of biomaterial or medical device, particularly of cardiovascular device such as prosthetic heart valve or pacemakers. Pyrimidine derivatives for use as radiotracer in diagnosing or prognosing bacterial infection in a host mammal.

The present invention relates to a process for preparing a compound of formula [I], said process comprising the steps of: formula [II]+formula [III].fwdarw.formula [I] (i) forming a reaction mixture comprising (a) a compound of formula [II], (b) a compound of formula [III] and (c) 1,2-propanediol or polyethylene glycol, or a mixture thereof, and optionally (d) a base; (ii) heating said reaction mixture to a temperature of at least about 150 C. to form a compound of formula [I]; (iii) isolating said compound of formula [I]; and (iv) optionally converting said compound of formula [I] into salt form; wherein: R.sup.1 and R.sup.2 are each independently H, alkyl or haloalkyl; R.sup.3 and R.sup.4 are each independently H, alkyl, haloalkyl or aryl; R.sup.5 is alkyl, alkenyl, cycloalkyl or cycloalkyl-alkyl, each of which may be optionally substituted with one or more OH groups; R.sup.6 is selected from cyclopropylamino, cyclopropylmethylamino, cyclobutylamino, cyclobutylmethylamino and formula (A) where one of X, Y and Z is N and the remainder are CR.sup.9; R.sup.7, R.sup.8 and each R.sup.9 are independently H, alkyl or haloalkyl, wherein at least one of R.sup.7, R.sup.8 and R.sup.9 is other than H. Further aspects of the invention relate to a highly diastereoselective process for the preparation of compounds of formula [III], a process for preparing intermediates of formula [II], and other intermediates useful in the synthesis of compounds of formula [I], and to a process for preparing the crystalline tartrate salt and free base of compounds of formula [I]. ##STR00001##

The present invention relates to a process for preparing a compound of formula [I], said process comprising the steps of: formula [II]+formula [III].fwdarw.formula [I] (i) forming a reaction mixture comprising (a) a compound of formula [II], (b) a compound of formula [III] and (c) 1,2-propanediol or polyethylene glycol, or a mixture thereof, and optionally (d) a base; (ii) heating said reaction mixture to a temperature of at least about 150 C. to form a compound of formula [I]; (iii) isolating said compound of formula [I]; and (iv) optionally converting said compound of formula [I] into salt form; wherein: R.sup.1 and R.sup.2 are each independently H, alkyl or haloalkyl; R.sup.3 and R.sup.4 are each independently H, alkyl, haloalkyl or aryl; R.sup.5 is alkyl, alkenyl, cycloalkyl or cycloalkyl-alkyl, each of which may be optionally substituted with one or more OH groups; R.sup.6 is selected from cyclopropylamino, cyclopropylmethylamino, cyclobutylamino, cyclobutylmethylamino and formula (A) where one of X, Y and Z is N and the remainder are CR.sup.9; R.sup.7, R.sup.8 and each R.sup.9 are independently H, alkyl or haloalkyl, wherein at least one of R.sup.7, R.sup.8 and R.sup.9 is other than H. Further aspects of the invention relate to a highly diastereoselective process for the preparation of compounds of formula [III], a process for preparing intermediates of formula [II], and other intermediates useful in the synthesis of compounds of formula [I], and to a process for preparing the crystalline tartrate salt and free base of compounds of formula [I]. ##STR00001##

The present invention relates to compounds and methods of use thereof for treatment of certain disorders and conditions, for example an addiction or compulsive disorder.

The present invention provides PI3K protein kinase modulators of Formula (I) ##STR00001##
wherein R, n, R.sup.1, R.sup.2, L.sup.1, Cy.sup.1 and Cy.sup.2 are as defined herein, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

The present invention provides PI3K protein kinase modulators of Formula (I) ##STR00001##
wherein R, n, R.sup.1, R.sup.2, L.sup.1, Cy.sup.1 and Cy.sup.2 are as defined herein, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.