Polyguanidines and methods of use thereof are described. In particular, polyguanidines of formula (I), formula (II), and formula (III) are described. The polyguanidines can be used to treat infection, such as bacterial, viral or fungal infection, and as an ex vivo microbial agent.

##STR00001##

Polyguanidines and methods of use thereof are described. In particular, polyguanidines of formula (I), formula (II), and formula (III) are described. The polyguanidines can be used to treat infection, such as bacterial, viral or fungal infection, and as an ex vivo microbial agent.

##STR00001##

A biguanide derivative compound with N1-N5 substitution, which is represented by Formula 1, or a pharmaceutically acceptable salt thereof, a method of preparing the same, and a pharmaceutical composition containing the same as an active ingredient are provided. The biguanide derivative may exhibit excellent effect on activation of AMPK and inhibition of cancer cell proliferation in a low dose, compared to conventional drugs, and thus, may be useful to treat diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer, etc.

A biguanide derivative compound with N1-N5 substitution, which is represented by Formula 1, or a pharmaceutically acceptable salt thereof, a method of preparing the same, and a pharmaceutical composition containing the same as an active ingredient are provided. The biguanide derivative may exhibit excellent effect on activation of AMPK and inhibition of cancer cell proliferation in a low dose, compared to conventional drugs, and thus, may be useful to treat diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer, etc.

A method for preparing polycondensation products of guanidine, aminoguanidine or diaminoguanidine G with one or more benzyl or allyl derivatives BA according to the following reaction scheme is provided: ##STR00001##
wherein X, R.sub.1, Gua, Y and Z are as defined in the specification. In the disclosed method, at least one benzyl or allyl derivative BA is subjected to a polycondensation reaction with excessive guanidine, aminoguanidine or diaminoguanidine G upon elimination of HX.

A method for preparing polycondensation products of guanidine, aminoguanidine or diaminoguanidine G with one or more benzyl or allyl derivatives BA according to the following reaction scheme is provided: ##STR00001##
wherein X, R.sub.1, Gua, Y and Z are as defined in the specification. In the disclosed method, at least one benzyl or allyl derivative BA is subjected to a polycondensation reaction with excessive guanidine, aminoguanidine or diaminoguanidine G upon elimination of HX.

The present invention provides cationic lipids and lipid nanoparticle formulations comprising these lipids, alone or in combination with other lipids. These lipid nanoparticles may be formulated with nucleic acids to facilitate their intracellular delivery both in vitro and for therapeutic applications. The present invention also provides methods of chemical synthesis of these lipids, lipid nanoparticle preparation and formulation with nucleic acids.

The present invention provides cationic lipids and lipid nanoparticle formulations comprising these lipids, alone or in combination with other lipids. These lipid nanoparticles may be formulated with nucleic acids to facilitate their intracellular delivery both in vitro and for therapeutic applications. The present invention also provides methods of chemical synthesis of these lipids, lipid nanoparticle preparation and formulation with nucleic acids.

A compound capable of providing a composition having high storage stability without reacting with a base-reactive compound, even when stored in a mixed state with the base-reactive compound, as well as capable of generating a strong base by irradiation of light (active energy rays) or heating. A base generator comprises the compound and a base-reactive composition comprises the base generator and the base-reactive compound. The compound is represented by the general formula (A).

A compound capable of providing a composition having high storage stability without reacting with a base-reactive compound, even when stored in a mixed state with the base-reactive compound, as well as capable of generating a strong base by irradiation of light (active energy rays) or heating. A base generator comprises the compound and a base-reactive composition comprises the base generator and the base-reactive compound. The compound is represented by the general formula (A).