The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

Provided are STAT3 inhibitors and methods of treating inflammation or a hyperproliferative disease such as, e.g., cancer. In some aspects, compounds may be used to treat breast cancer, a head/neck cancer, a lung cancer, a prostate cancer, or pancreatic cancer.

Disclosed are compounds of the following formula I:

##STR00001##

wherein: m represents an integer being equal to 0, 1, 2, 3, 4, 5 or 6, X represents a simple bond or a radical CHR.sub.1 wherein R.sub.1 represents: a hydrogen atom, or a linear or branched, possibly interrupted by up to 3 heteroatoms selected from O, S or N and/or possibly substituted, (C.sub.1-C.sub.12)-alkyl, R.sub.2, R.sub.3 and R.sub.4 represent independently from each other: a hydrogen atom, or a linear or branched (C.sub.1-C.sub.12)-alkyl or (C.sub.1-C.sub.12)-acyl R.sub.5 represents: a hydrogen atom, or a linear or branched, possibly substituted, (C.sub.1-C.sub.13)-alkyl possibly interrupted by up to 3 heteroatoms selected from O, S or N, R.sub.6 represents: a hydrogen atom, or a linear or branched possibly substituted (C.sub.1-C.sub.12)-alkyl, possibly substituted and possibly interrupted by up to 3 heteroatoms selected from O, S or N, for their use as antibacterial drugs.

Disclosed are compounds of the following formula I:

##STR00001##

wherein: m represents an integer being equal to 0, 1, 2, 3, 4, 5 or 6, X represents a simple bond or a radical CHR.sub.1 wherein R.sub.1 represents: a hydrogen atom, or a linear or branched, possibly interrupted by up to 3 heteroatoms selected from O, S or N and/or possibly substituted, (C.sub.1-C.sub.12)-alkyl, R.sub.2, R.sub.3 and R.sub.4 represent independently from each other: a hydrogen atom, or a linear or branched (C.sub.1-C.sub.12)-alkyl or (C.sub.1-C.sub.12)-acyl R.sub.5 represents: a hydrogen atom, or a linear or branched, possibly substituted, (C.sub.1-C.sub.13)-alkyl possibly interrupted by up to 3 heteroatoms selected from O, S or N, R.sub.6 represents: a hydrogen atom, or a linear or branched possibly substituted (C.sub.1-C.sub.12)-alkyl, possibly substituted and possibly interrupted by up to 3 heteroatoms selected from O, S or N, for their use as antibacterial drugs.

Disclosed are a preparation method for a 1,3-disubstituted allene compound at room temperature based on a metal carbene catalyst, comprising: reacting terminal alkynes, aldehydes and amines in an organic solvent under the action of a gold catalyst and a molecular sieve, and then synthesizing a 1,3-disubstituted allene compound at room temperature. The method of the present invention is simple to operate, raw materials and reagents are easily obtained, reaction conditions are mild, substrate universality is wide, functional group compatibility is good, yield is high (36-93%), the method is scalable (11 g), and practicability is strong. The 1,3-disubstituted allene compound obtained in the present invention may be used as an important intermediate to construct -caprolactone, trans-allyl alcohol, other allene-derived compounds and natural product molecules and the like.

Disclosed are a preparation method for a 1,3-disubstituted allene compound at room temperature based on a metal carbene catalyst, comprising: reacting terminal alkynes, aldehydes and amines in an organic solvent under the action of a gold catalyst and a molecular sieve, and then synthesizing a 1,3-disubstituted allene compound at room temperature. The method of the present invention is simple to operate, raw materials and reagents are easily obtained, reaction conditions are mild, substrate universality is wide, functional group compatibility is good, yield is high (36-93%), the method is scalable (11 g), and practicability is strong. The 1,3-disubstituted allene compound obtained in the present invention may be used as an important intermediate to construct -caprolactone, trans-allyl alcohol, other allene-derived compounds and natural product molecules and the like.

The present invention provides a compound having a lysine-specific demethylase 1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for cancer, and central nervous system diseases, and the like. The present invention relates to a compound represented by the formula ##STR00001##
wherein A is a hydrocarbon group or heterocyclic group optionally having substituent(s); R is H, a hydrocarbon group or heterocyclic group optionally having substituent(s); A and R are optionally bonded to each other to form a ring optionally having substituent(s); Q.sup.1, Q.sup.2, Q.sup.3 and Q.sup.4 are each a hydrogen atom or a substituent; Q.sup.1 and Q.sup.2, and Q.sup.3 and Q.sup.4, are each optionally bonded to each other to form a ring optionally having substituent(s); X is H, an acyclic hydrocarbon group or saturated cyclic group optionally having substituent(s); Y.sup.1, Y.sup.2 and Y.sup.3 are each H, a hydrocarbon group or heterocyclic group optionally having substituent(s); X and Y.sup.1, and Y.sup.1 and Y.sup.2, are each optionally bonded to each other to form a ring optionally having substituent(s); and Z.sup.1, Z.sup.2 and Z.sup.3 are each H or a substituent, or a salt thereof.

The present invention provides a compound having a lysine-specific demethylase 1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for cancer, and central nervous system diseases, and the like. The present invention relates to a compound represented by the formula ##STR00001##
wherein A is a hydrocarbon group or heterocyclic group optionally having substituent(s); R is H, a hydrocarbon group or heterocyclic group optionally having substituent(s); A and R are optionally bonded to each other to form a ring optionally having substituent(s); Q.sup.1, Q.sup.2, Q.sup.3 and Q.sup.4 are each a hydrogen atom or a substituent; Q.sup.1 and Q.sup.2, and Q.sup.3 and Q.sup.4, are each optionally bonded to each other to form a ring optionally having substituent(s); X is H, an acyclic hydrocarbon group or saturated cyclic group optionally having substituent(s); Y.sup.1, Y.sup.2 and Y.sup.3 are each H, a hydrocarbon group or heterocyclic group optionally having substituent(s); X and Y.sup.1, and Y.sup.1 and Y.sup.2, are each optionally bonded to each other to form a ring optionally having substituent(s); and Z.sup.1, Z.sup.2 and Z.sup.3 are each H or a substituent, or a salt thereof.

Provided are STAT3 inhibitors and methods of treating inflammation or a hyperproliferative disease such as, e.g., cancer. In some aspects, compounds may be used to treat breast cancer, a head/neck cancer, a lung cancer, a prostate cancer, or pancreatic cancer.

The invention relates to a method for synthesizing an intermediate of Apixaban comprising reacting a compound of formula I with 5-chloro-valeryl chloride in the presence of inorganic base in an inert solvent to obtain a compound of formula II, with the reaction formula of (A), wherein R is selected from nitro group and the group (B). The method is mild in reaction condition, simple in operation, easy in purification, inexpensive in production cost, environmental-friendly, and suitable for industrial production. ##STR00001##