Molecule having the structural formula (I): (I) for use as targeting probe of translating ribosomes and ribosome-interacting proteins. ##STR00001##

Disclosed are compounds of formula (I), and pharmaceutically acceptable salts thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the compounds and compositions in the treatment or prevention of a disease or condition characterized by aberrant complement system activity.

##STR00001##

The present invention provides compounds useful as inhibitors of PDK1. The present invention also provides compositions thereof, and methods of treating PDK1-mediated diseases.

The present invention provides compounds useful as inhibitors of PDK1. The present invention also provides compositions thereof, and methods of treating PDK1-mediated diseases.

The present invention relates to dual delta (δ) and gamma (γ) PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them.

The present invention relates to dual delta (δ) and gamma (γ) PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of Pi3K kinase mediated diseases or disorders with them.

Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.

Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.

The present invention relates to a process for preparing a compound of formula [I], or a pharmaceutically acceptable salt thereof, said process comprising the steps of: (i) forming a reaction mixture comprising a compound of formula [II] and a compound of formula [III]; (ii) heating said reaction mixture to a temperature of at least about 130° C. to form a compound of formula [I]; (iii) isolating said compound of formula [I] from the mixture and optionally recovering unreacted compound of formula [III]; 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 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 process for preparing intermediates of formula [II], and other intermediates useful in the synthesis of compounds of formula [I].

##STR00001##

The present invention relates to a process for preparing a compound of formula [I], or a pharmaceutically acceptable salt thereof, said process comprising the steps of: (i) forming a reaction mixture comprising a compound of formula [II] and a compound of formula [III]; (ii) heating said reaction mixture to a temperature of at least about 130° C. to form a compound of formula [I]; (iii) isolating said compound of formula [I] from the mixture and optionally recovering unreacted compound of formula [III]; 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 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 process for preparing intermediates of formula [II], and other intermediates useful in the synthesis of compounds of formula [I].

##STR00001##