The present invention relates to a pharmaceutical composition for preventing or treating metabolic diseases, in which a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative and at least another active ingredient, which is selected from the group consisting of dipeptidyl peptidase-4 (DPPIV) inhibitor-based, sulfonylurea-based, thiazolidinedione (TZD)-based, biguanide-based, and sodium/glucose cotransporter 2 (SGLT2) inhibitor-based drugs, may be administered in combination or in the form of a composite preparation. The use of the composition of the present invention can provide a remarkably excellent blood sugar reducing effect in various animal diabetic disease models, and the composition of the present invention can be favorably used as a pharmaceutical composition for preventing or treating metabolic diseases, such as obesity, diabetes type I, diabetes type II, glucose intolerance symptoms, insulin resistance symptoms, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, and syndrome X.

The present invention relates to a pharmaceutical composition for preventing or treating metabolic diseases, in which a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative and at least another active ingredient, which is selected from the group consisting of dipeptidyl peptidase-4 (DPPIV) inhibitor-based, sulfonylurea-based, thiazolidinedione (TZD)-based, biguanide-based, and sodium/glucose cotransporter 2 (SGLT2) inhibitor-based drugs, may be administered in combination or in the form of a composite preparation. The use of the composition of the present invention can provide a remarkably excellent blood sugar reducing effect in various animal diabetic disease models, and the composition of the present invention can be favorably used as a pharmaceutical composition for preventing or treating metabolic diseases, such as obesity, diabetes type I, diabetes type II, glucose intolerance symptoms, insulin resistance symptoms, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, and syndrome X.

Compounds that are not related to NAD, and which target PARP1-histone H4 interaction are provided, as well as compositions of these compounds, and methods for specific inhibition of poly(ADP-ribose) polymerase 1 (PARP-1) using these compounds are provided. These PARP-1 inhibitors may be used to treat cancer in which PARP-1 activation or biologic activity plays a role, including prostate cancer, breast cancer, kidney cancer, ovarian cancer, lymphoma, leukemia, and glioblastoma, among others.

Compounds that are not related to NAD, and which target PARP1-histone H4 interaction are provided, as well as compositions of these compounds, and methods for specific inhibition of poly(ADP-ribose) polymerase 1 (PARP-1) using these compounds are provided. These PARP-1 inhibitors may be used to treat cancer in which PARP-1 activation or biologic activity plays a role, including prostate cancer, breast cancer, kidney cancer, ovarian cancer, lymphoma, leukemia, and glioblastoma, among others.

Amphiphilic compounds with tetradecahydrophenanthrene skeleton and their enantiomers, exhibiting neuroprotective effects, their use in methods of treatment of neuropsychiatric disorders associated with an imbalance in glutamatergic neurotransmitter system, such as ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, post-traumatic stress disorder and diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addiction, multiple sclerosis, epilepsy, glioma, and a pharmaceutical composition containing compound.

Disclosed herein is a lipid having a net charge at physiological pH, and being covalently attached to a lipid moiety. The lipid moiety comprises a hydrocarbon structure having two or more linked hydrocarbon chains, optionally having cis or trans C═C, at least one of said chains being covalently attached to the head group optionally via the linker region. The hydrocarbon chains are bonded to one another at a branch point at an internal carbon of the chain attached to the linker region, which branch point comprises a functional group having an electronegative atom. The hydrocarbon chains each have between 1 and 40 carbon atoms, wherein the hydrocarbon structure in total comprises between 10 and 150 carbon atoms. Advantageously, the hydrocarbon structure may assume a generally flared shape for enhanced delivery of cargo molecules. Further provided are delivery vehicles comprising the lipids.

The present invention relates to a novel process for the esterification of N-acylated amino acids which contain an acid-labile keto protective group under alkaline conditions without using a polar aprotic solvent, in which the N-acylated amino acid with acid-labile keto protective group prepared in situ is esterified using an alkyl halide or a mono- or dialkyl ester of sulfuric acid.

The present invention relates to a novel process for the esterification of N-acylated amino acids which contain an acid-labile keto protective group under alkaline conditions without using a polar aprotic solvent, in which the N-acylated amino acid with acid-labile keto protective group prepared in situ is esterified using an alkyl halide or a mono- or dialkyl ester of sulfuric acid.

A salt represented by formula (I): ##STR00001##
wherein R.sup.1 and R.sup.2 independently represent a hydrogen atom, a hydroxy group or a C.sub.1 to C.sub.12 hydrocarbon group in which a methylene group may be replaced by a —O— or —CO—; m and n independently represent 1 or 2; Ar represents an optionally substituted phenyl group; Q.sup.1 and Q.sup.2 independently represent a fluorine atom or a C.sub.1 to C.sub.6 perfluoroalkyl group, A.sup.1 represents a single bond, a C.sub.1 to C.sub.24 alkanediyl group or the like, and Y represents an optionally substituted C.sub.1 to C.sub.18 alkyl group or monovalent C.sub.3 to C.sub.18 alicyclic hydrocarbon group, and a methylene group therein may be replaced by a —O—, O— or —SO.sub.2—, provided that the alkyl group or the alicyclic hydrocarbon group has at least one substituent, or at least one methylene group contained therein is replaced by a —O—, —CO— or —SO.sub.2—.

A salt represented by formula (I): ##STR00001##
wherein R.sup.1 and R.sup.2 independently represent a hydrogen atom, a hydroxy group or a C.sub.1 to C.sub.12 hydrocarbon group in which a methylene group may be replaced by a —O— or —CO—; m and n independently represent 1 or 2; Ar represents an optionally substituted phenyl group; Q.sup.1 and Q.sup.2 independently represent a fluorine atom or a C.sub.1 to C.sub.6 perfluoroalkyl group, A.sup.1 represents a single bond, a C.sub.1 to C.sub.24 alkanediyl group or the like, and Y represents an optionally substituted C.sub.1 to C.sub.18 alkyl group or monovalent C.sub.3 to C.sub.18 alicyclic hydrocarbon group, and a methylene group therein may be replaced by a —O—, O— or —SO.sub.2—, provided that the alkyl group or the alicyclic hydrocarbon group has at least one substituent, or at least one methylene group contained therein is replaced by a —O—, —CO— or —SO.sub.2—.