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 disclosure provides, inter alia, alpha-5 beta-1 inhibitors, pharmaceutical compositions comprising alpha-5 beta-1 inhibitors, methods for treating diseases using alpha-5 beta-1 inhibitors, and processes for making alpha-5 beta-1 inhibitors.

The disclosure provides, inter alia, alpha-5 beta-1 inhibitors, pharmaceutical compositions comprising alpha-5 beta-1 inhibitors, methods for treating diseases using alpha-5 beta-1 inhibitors, and processes for making alpha-5 beta-1 inhibitors.

The present invention relates to certain compounds of formula (I) wherein—Ar is (Ar1) or (Ar2) and to their uses as antibacterial agents. The invention further relates to methods of treatment of bacterial infection with such compounds, optionally in combination with other antimicrobials and to compositions and pharmaceutical formulations containing such compounds. The invention additionally relates to coatings containing such compounds and to items having such coatings.

##STR00001##

An antibacterial compound of formula I, wherein X is selected from fluoro or bromo, effective against Gram negative and Gram positive bacteria, and in particular against non-fermenting multiresistant bacteria affecting patients suffering from cystic fibrosis and which are responsible of severe hospital-acquired infections in immunodepressed patients; its preparation process and pharmaceutical composition comprising said compound. ##STR00001##

An antibacterial compound of formula I, wherein X is selected from fluoro or bromo, effective against Gram negative and Gram positive bacteria, and in particular against non-fermenting multiresistant bacteria affecting patients suffering from cystic fibrosis and which are responsible of severe hospital-acquired infections in immunodepressed patients; its preparation process and pharmaceutical composition comprising said compound. ##STR00001##

The present invention provides a compound that is highly safe and useful in the prevention, alleviation, and/or treatment of various diseases involving enteropeptidase inhibition and/or trypsin inhibition, a pharmaceutical composition containing the compound, a method for producing the compound, and the like. Specifically, the present invention provides a compound represented by the following general formula (I):

##STR00001##

[wherein: A.sup.1 and A.sup.2 each independently represent an inhibitor residue having at least one activity selected from an enteropeptidase inhibitory activity and a trypsin inhibitory activity; and Z represents a spacer that links A.sup.1 to A.sup.2] or a pharmaceutically acceptable salt thereof.

The present invention provides a compound that is highly safe and useful in the prevention, alleviation, and/or treatment of various diseases involving enteropeptidase inhibition and/or trypsin inhibition, a pharmaceutical composition containing the compound, a method for producing the compound, and the like. Specifically, the present invention provides a compound represented by the following general formula (I):

##STR00001##

[wherein: A.sup.1 and A.sup.2 each independently represent an inhibitor residue having at least one activity selected from an enteropeptidase inhibitory activity and a trypsin inhibitory activity; and Z represents a spacer that links A.sup.1 to A.sup.2] or a pharmaceutically acceptable salt thereof.

The present invention relates to a biguanide derivative compound capable of effectively preventing and treating immune diseases. The biguanide-based derivative compound according to the present invention inhibits the generation of IL-17 and TNF-, which are inflammatory cytokines, increases the activity of regulatory T cells having an immunomodulatory function, and exhibits excellent therapeutic effects in animal models of immune diseases. Accordingly, the biguanide-based derivative compound can be usefully used as an immunosuppressant or a pharmaceutical composition capable of preventing or treating various immune diseases, such as autoimmune diseases, inflammatory diseases, and transplant rejection, caused by the dysregulation of immune responses.

The present invention relates to a biguanide derivative compound capable of effectively preventing and treating immune diseases. The biguanide-based derivative compound according to the present invention inhibits the generation of IL-17 and TNF-, which are inflammatory cytokines, increases the activity of regulatory T cells having an immunomodulatory function, and exhibits excellent therapeutic effects in animal models of immune diseases. Accordingly, the biguanide-based derivative compound can be usefully used as an immunosuppressant or a pharmaceutical composition capable of preventing or treating various immune diseases, such as autoimmune diseases, inflammatory diseases, and transplant rejection, caused by the dysregulation of immune responses.