Hyundai Pharm. Co.

Seoul, South Korea

Hyundai Pharm. Co.

Seoul, South Korea
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The present invention relates to: a cyclohexene derivative; a preparation method therefor; and a pharmaceutical composition for preventing or treating metabolic diseases, containing the same as an active ingredient. The cyclohexene derivative according to the present invention increases the intracellular activity of cyclic adenosine monophosphate (cAMP) by activating G protein-coupled receptor 119 (GPR-119) and simultaneously exhibits weight loss and hypoglycemic effects by inducing the release of glucagon-like peptide-1 (GLP-1), which is a neuroendocrine protein, and thus can be useful as a pharmaceutical composition for preventing or treating metabolic diseases such as obesity, type 1 diabetes, type 2 diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia and syndrome X.


The present invention relates to a compound inhibiting CDK5-mediated PPARG phosphorylation and a pharmaceutical composition for treating PPARG-related diseases containing the same as an active ingredient. A compound represented by formula 1 or an optical isomer thereof according to the present invention binds to PPARG at a high affinity level, but does not act as an agonist, thereby inducing no gene transcription; blocks CDK5, which is a cause of PPARG phosphorylation, thereby causing no side effects of existing anti-diabetics; can be formulated into drugs due to improved pharmacological properties thereof; and can be favorably used as a pharmaceutical composition for treating PPARG-related diseases due to an excellent treatment effect on PPARG-related diseases.


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 cyclohexene derivative; a preparation method therefor; and a pharmaceutical composition for preventing or treating metabolic diseases, containing the same as an active ingredient. The cyclohexene derivative according to the present invention increases the intracellular activity of cyclic adenosine monophosphate (cAMP) by activating G protein-coupled receptor 119 (GPR-119) and simultaneously exhibits weight loss and hypoglycemic effects by inducing the release of glucagon-like peptide-1 (GLP-1), which is a neuroendocrine protein, and thus can be useful as a pharmaceutical composition for preventing or treating metabolic diseases such as obesity, type 1 diabetes, type 2 diabetes, inadequate glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia and syndrome X.


The present invention relates to a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient for the prevention and treatment of metabolic disease. The novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention has excellent activities of activating GPR40 protein and promoting insulin secretion accordingly but has no toxicity when co-administered with other drugs. That is, the novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention can be co-administered with other drugs and can promote the activation of GPR40 protein significantly, so that the composition comprising the same as an active ingredient can be efficiently used as a pharmaceutical composition for the prevention and treatment of metabolic disease such as obesity, type I diabetes, type II diabetes, incompatible glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, and syndrome X, etc.


The present invention relates to a compound inhibiting CDK5-mediated PPARG phosphorylation and a pharmaceutical composition for treating PPARG-related diseases containing the same as an active ingredient. A compound represented by formula 1 or an optical isomer thereof according to the present invention that binds to PPARG at a high affinity level, but does not act as an agonist, thereby inducing no gene transcription; blocks CDK5, which is a cause of PPARG phosphorylation, thereby causing no side effects of existing anti-diabetic drugs; can be formulated into drugs due to improved pharmacological properties thereof; and can be favorably used as a pharmaceutical composition for treating PPARG-related diseases due to favorable treatment effects on PPARG-related diseases.


Provided is a skin external composition, which includes tranexamic acid or a salt thereof and a skin penetration enhancer, thereby showing remarkably increased skin permeability and improved sense of use, skin irritation, and storage stability.


The present invention relates to a pharmaceutical composition containing acebrophylline thereby having both immediate and extended release characteristics, and more specifically, to a sustained-release pharmaceutical composition containing acebrophylline and a hydrophillic sustained-release agent having a viscosity of no more than 13,000 cps.


The present invention relates to a pharmaceutical composition containing acebrophylline thereby having both immediate and extended release characteristics, and more specifically, to a sustained-release pharmaceutical composition containing acebrophylline and a hydrophobic sustained-release agent.


The present invention relates to a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient for the prevention and treatment of metabolic disease. The novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention has excellent activities of activating GPR40 protein and promoting insulin secretion accordingly but has no toxicity when co-administered with other drugs. That is, the novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention can be co-administered with other drugs and can promote the activation of GPR40 protein significantly, so that the composition comprising the same as an active ingredient can be efficiently used as a pharmaceutical composition for the prevention and treatment of metabolic disease such as obesity, type I diabetes, type II diabetes, incompatible glucose tolerance, insulin resistance, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, dyslipidemia, and syndrome X, etc.

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