The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.

Compounds and methods for use to treat a bacterial infection caused by, for example, gram positive bacteria, gram negative bacteria, and/or mycobacteria are provided herein. Also provided herein are compounds and methods for use in potentiating the effect of an antibiotic in the treatment of a bacterial infection. Pharmaceutical compositions including the compounds as described herein are also provided.

Compounds and methods for use to treat a bacterial infection caused by, for example, gram positive bacteria, gram negative bacteria, and/or mycobacteria are provided herein. Also provided herein are compounds and methods for use in potentiating the effect of an antibiotic in the treatment of a bacterial infection. Pharmaceutical compositions including the compounds as described herein are also provided.

The present invention relates in certain aspects to the discovery of novel 2-naphthimidamide compounds that are capable of binding Type II Transmembrane Serine Proteases (TTSPs). In certain embodiments, the compounds of the invention can be used to treat or prevent Influenza A viral infection in a mammal.

The present invention relates in certain aspects to the discovery of novel 2-naphthimidamide compounds that are capable of binding Type II Transmembrane Serine Proteases (TTSPs). In certain embodiments, the compounds of the invention can be used to treat or prevent Influenza A viral infection in a mammal.

The present invention provides a benzoic acid ester compound that has an enteropeptidase inhibitory effect, and use of the compound as a medicament for the treatment or prevention of obesity, diabetes mellitus, or the like.

A compound represented by the formula (I) or a salt thereof has an enteropeptidase inhibitory effect and is useful as a medicament for the treatment or prevention of obesity, diabetes mellitus, or the like:

##STR00001##

[in the formula, each symbol is as defined in the specification].

A compound having a first ligand of the following ##STR00001##
is described. Ring A represents a monocyclic aromatic group or a polycyclic aromatic group. Ring B represents a polycyclic aromatic group. Z is a carbon. Z and the right N are coordinated to a metal to form a five-membered chelate ring. R.sub.1 and R.sub.2 independently represent mono to a maximum possible number of substitutions, or no substitution.

A compound having a first ligand of the following ##STR00001##
is described. Ring A represents a monocyclic aromatic group or a polycyclic aromatic group. Ring B represents a polycyclic aromatic group. Z is a carbon. Z and the right N are coordinated to a metal to form a five-membered chelate ring. R.sub.1 and R.sub.2 independently represent mono to a maximum possible number of substitutions, or no substitution.

The present disclosure provides a group of aromatic (e.g., pyridinyl, pyrimidinyl, pyrazinyl, or phenyl) diamidine analogs and pharmaceutically acceptable salts that are useful for treating a proliferative disease. The proliferative disease may include solid cancer or blood cancer. Compositions, methods of synthesizing the same and methods for treating various cancer using the analogs are disclosed herein. The present disclosure also provides pharmaceutical formulations comprising at least one of the compounds with a pharmaceutically acceptable carrier, diluent or excipient therefor.

Compounds useful in inhibiting endo-exonuclease activity and treating cancer have the formula (I):

##STR00001##

wherein R3 is selected from the group consisting of loweralkyl, oxyalkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, aminoalkyl or a halogen; R4 is selected from the group consisting of H, loweralkyl, oxyalkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, aminoalkyl or a halogen; and wherein R5 is a loweralkyl; or formula (II):

##STR00002##

wherein R1 is selected from the group consisting of loweralkyl, oxyalkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, aminoalkyl or halogen; R2 is selected from the group consisting of H, loweralkyl, oxyalkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, aminoalkyl or halogen; and wherein R5 is a loweralkyl comprising a linear carbon chain of at least two carbons connecting the first “O” to the second “O”.