Abstract: Enantiomerically pure compound of formula 1 are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.

Abstract: The invention relates to biocatalytic methods for preparing enantiomerically pure stereoisomers of 1-(2,6-dichloro-3-fluorophenyl)ethanol. Disclosed are methods of preparation of the desired (S)-enantiomer, which methods are based on a combination of enzymatic resolution, chemical esterification and chemical hydrolysis with inversion of 1-(2,6-dichloro-3-fluorophenyl)ethyl esters or stereoselective bio-reduction of 2,6-dichloro-3-fluoro-acetophenone with a biocatalyst such as an enzyme or a microorganism. The chiral (S)-enantiomer can be used in the synthesis of certain enantiomerically enriched, ether linked 2-aminopyridine compounds that potently inhibit auto-phosphorylation of human heptocyte growth factor receptor.

Abstract: Aminopyridine and aminopyrazine compounds of formula (1), compositions including these compounds, and methods of their use are provided. Preferred compounds of formula 1 have activity as protein kinase inhibitors, including as inhibitors of c-MET.

Abstract: The present invention is directed to combination therapies for treating cell proliferative disorders associated with methylthioadenosine phosphorylase (MTAP) deficient cells in a mammal. The combination therapies selectively kill MTAP-deficient cells by administering an inhibitor of de novo inosinate synthesis and administering an anti-toxicity agent, wherein the inhibitors of de novo inosinate synthesis are inhibitors of glycinamide ribonucleotide formyltransferase (“GARFT”) and/or aminoinidazolecarboximide ribonucleotide formyltransferase (“AICARFT”), and the anti-toxicity agent is an MTAP substrate (e.g. methylthioadenosine or “MTA”), a precursor of MTA, an analog of an MTA precursor or a prodrug of an MTAP substrate.

Abstract: Compositions comprising novel di-nitrogen heterocycle compounds containing at least one N-meta-substituted alkaryl group are prepared. The compounds of the present invention are useful as antibacterial and as other pharmaceutical agents and as intermediates for preparation of other pharmaceutical agents. In addition, compounds of the present invention are useful as research reagents.

Abstract: Novel macrocyclic compounds are constructed to include a ring or ring system having two bridgehead atoms with a bridge extending between the bridgehead atoms. Located in at least the bridge are two or more nitrogenous moieties that are derivatized with chemical functional groups. The ring or ring systems can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring. These can also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the library.

Abstract: Provided are compounds of formula (I) ##STR1## wherein X, Y and Z are independently CH or N; n is 0 or 1; R.sub.1 is selected from OH, alkoxy, aryloxy, aralkyloxy and guanidinyl; R.sub.2 and R.sub.3 are independently selected from H, halogen, amino, hydroxyl, nitro, cyano and carboxyl; R.sub.4 is H, alkyl or acyl; R.sub.5 is selected from H, hydroxyl, halogen, nitro, alkyl, alkoxy, amino, cyclic amino, alkylamino, arylamino and aralkylamino wherein the alkyl, aryl and cyclic moieties are optionally substituted; R.sub.6 and R.sub.7 are independently selected from H, alkyl, alkoxy, halogen and amino; and R.sub.8 and R.sub.9 are independently selected from H, C.sub.1-4 alkyl, alkoxy, acyl, acyloxy, alkoxycarbonyl, hydroxyl, halogen, amino and carboxyl. The compounds have therapeutic or prophylactic use for treating bacterial infection in mammals.

Abstract: Compositions are provided comprising novel di-nitrogen heterocycle compounds containing N-(aminoalkyl) and/or N-(amidoalkyl) groups. An additional situs of functionality is also provided. The compounds and compositions of the invention are useful as antibacterial and other pharmaceutical agents and as intermediates for preparation of other pharmaceutical agents. In addition, compounds of the present invention are useful as research reagents including employment as species for effecting combinatorial synthesis.

Abstract: Novel compounds and libraries of compounds based on nitrogen atoms that are joined together with spanner groups include "letters" i.e., functional groups, that are attached to the nitrogen atoms, to the spanner groups or to both the nitrogen atoms and the spanner groups to render the compounds and libraries of such compounds with diverse properties.

Abstract: Novel macrocyclic compounds are constructed to include large cyclic structures that are interrupted by at least one ring system. Each interrupting ring system includes two bridgehead atoms. Bridgehead atoms are bonded to one or more bridges that interconnect one or more ring systems thereby forming a large cyclic structure. Located in each bridge are two or more nitrogenous moieties that are derivatized with chemical functional groups. The ring systems can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring. These can also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the macrocyclic compounds. In accordance with certain embodiments of the invention, libraries of such macrocyclic compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the library.

Abstract: Compositions comprising novel di-nitrogen heterocycle compounds containing N-(aminoalkyl) and/or N-(amidoalkyl) groups are prepared. The compounds of the present invention are useful as antibacterial and other pharmaceutical agents and as intermediates for preparation of other pharmaceutical agents. In addition, compounds of the present invention are useful as research reagents.

Abstract: Compositions comprising novel di-nitrogen heterocycle compounds containing at least one N-meta-substituted alkaryl group are prepared. The compounds of the present invention are useful as antibacterial and as other pharmaceutical agents and as intermediates for preparation of other pharmaceutical agents. In addition, compounds of the present invention are useful as research reagents.

Abstract: Compositions are provided comprising novel di-nitrogen heterocycle compounds containing N-(aminoalkyl) and/or N-(amidoalkyl) groups. An additional situs of functionality is also provided. The compounds and compositions of the invention are useful as antibacterial and other pharmaceutical agents and as intermediates for preparation of other pharmaceutical agents. In addition, compounds of the present invention are useful as research reagents including employment as species for effecting combinatorial synthesis.

Abstract: Compositions comprising novel di-nitrogen heterocycle compounds containing N-(aminoalkyl) and/or N-(amidoalkyl) groups are prepared. The compounds of the present invention are useful as antibacterial and other pharmaceutical agents and as intermediates for preparation of other pharmaceutical agents. In addition, compounds of the present invention are useful as research reagents.