59 results about "Peroxisome proliferators" patented technology

The present invention refers to steroid derivatives for use as medicaments. More specifically, the invention also relates to the use of a steroid derivative of 5-androstene-, 5-pregnenolone or corresponding saturated derivatives (androstane- or pregnane-) in the manufacture of a medicament for the treatment of a benign and/or malignant tumour, which medicament is capable of interrupting disturbances in Wnt-signaling, such as cell-cycle arrest in G1-phase, and/or providing an angiostatic effect. Examples of such steroid derivatives are -5-androstene-17-ol, androstane-17-ol-pregnane-17-ol or pregnane-17-ol derivatives. In a further aspect, the invention relates to a method of producing a medicament for the treatment of a benign and/or malignant tumour and/or an inflammatory condition comprising the steps of contacting 5-androstane-3β,17-diol or androstane-3β-diol, an enzyme and a sulfotransferase to provide 5-androstene-17-ol-3β-sulfate or corresponding andros tane derivative (17-AEDS or 17-AADS); and mixing the 17-AEDS or 17-AADS so produced with a suitable carrier; whereby a medicament which is capable of acting as a ligand to peroxisome proliferators-activated receptor-(PPAR) is produced.

Implantable medical devices having an anti-restenotic coatings are disclosed. Specifically, implantable medical devices having coatings of peroxisome proliferator-activated receptor gamma (PPAR.gamma.) agonists are disclosed. The anti-restenotic PPAR.gamma. ligands include thiazolidinedione compounds including ciglitazone. The anti-restenotic medial devices include stents, catheters, micro-particles, probes and vascular grafts. The medical devices can be coated using any method known in the art including compounding the thiazolidinedione with a biocompatible polymer prior to applying the coating. Moreover, medical devices composed entirely of biocompatible polymer-thiazolidinedione blends are disclosed. Additionally, medical devices having a coating comprising at least one thiazolidinedione in combination with at least one additional therapeutic agent are also disclosed. Furthermore, related methods of using and making the anti-restenotic implantable devices are also disclosed.

The present invention relates to the field of medical treatments for diseases and disorders. More specifically, the present invention relates to the use of the lanthionine synthetase component C-like (LANCL) proteins as therapeutic targets for novel classes of anti-inflammatory, immune regulatory and antidiabetic drugs. This includes but it is not limited to abscisic acid (ABA), ABA analogs, benzimidazophenyls, repurposed drugs or drug combinations, including thiazolidinediones (TZDs); naturally occurring compounds such as conjugated diene fatty acids, conjugated triene fatty acids, isoprenoids, and natural and synthetic agonists of peroxisome proliferator-activated receptors that activate this receptor through an alternative mechanism of action involving LANCL2 or other membrane proteins to treat or prevent the common inflammatory pathogenesis underlying type 2 diabetes, atherosclerosis, cancer, some inflammatory infectious diseases such as influenza and autoimmune diseases including but not limited to inflammatory bowel disease (Crohn's disease and Ulcerative colitis), rheumatoid arthritis, multiple sclerosis and type 1 diabetes and other chronic inflammatory conditions.

Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.

The present invention provides a novel phenylpropionic acid derivative and a PPAR-γ modulator comprising the same as an active ingredient. The phenylpropionic acid derivative of the present invention has modulatory action on function of PPAR-γ and then exhibits hypoglycemic, hypolipidemic and insulin resistance-reducing effects on PPAR-mediated diseases or disorders. Therefore, the present invention is prophylactically or therapeutically effective for diabetes and metabolic diseases.

Omega-3 lipid compounds of the general formula (I):

Disclosed is the preparation and pharmaceutical use of substituted arylalcanoic acid derivatives of Formula I, wherein ring A, ring B, R¹, R², R³, R⁴, R⁵, X, Alk¹, Alk², Ar¹, and Ar² are as defined in the specification. These compounds, as selective agonists activating peroxisome proliferator-activated receptors (PPAR), in particularly the RXR/PPARalpha, RXR/PPARgamma, and RXR/PPARdelta heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders with improved side effects profile commonly associated with conventional PPARgamma agonists.

An ester formed from an inositol or an inositol derivative and niacin, wherein the inositol or the inositol derivatives comprises a stereoisomer selected from allo-inositol, cis-inositol, epi-inositol, muco-inositol, neo-inositol, scyllo-inositol, D-chiro-inositol and L-chiro-inositol, or pharmaceutically acceptable salts thereof. Examples of esters include inositol hexaniacinates such as allo-inositol hexaniacinate and cis-inositol hexaniacinate. The esters can be used to treat any disorder that is treatable with niacin therapy such as dyslipidemia, hypercholesterolemia, hyperlipidemia or cardiovascular disease. The esters can be administered with other agents such as HMG-CoA reductase inhibitors, statins, fibrates, activators of peroxisome proliferator activated receptors poli-cosanol, phytosterols, tocotrienols, calcium, bile acid sequestrants, guar gum and free niacin. The invention includes pharmaceutical compositions containing these compounds.

The present invention is directed to a compound of formula I, and pharmaceutically acceptable salts, solvates, hydrates or stereoisomer thereof, which are useful in treating Syndrome X, Type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to Syndrome X as well as cardiovascular diseases.

The invention relates to benzimidazolyl thiazolidinone compounds and a synthesis method thereof. The compounds have a structure shown by a general formula (I), wherein R1 and R2 may be methyl, ethyl, benzyl, alkyl or hydrogen; and n is an integer between 1 and 5. The benzimidazolyl thiazolidinone compounds provided by the invention are high-affinity ligands having specificity against peroxisome proliferator-activated receptor (PPAR-gamma), by improving glucose absorption by cells and lowering output of glycogen, the sensitivity of cells to insulin is increased and the antagonism of tissues against glucose; and the compounds, compared with the conventional thiazolidinones PPAR-gamma activating agent, has high lipid solubility, is easier to pass through blood brain barrier, improves the sensitivity of insulin in brain, and can be used for treating neurological diseases caused by diabetes and neuroprotection.

An injectable composition comprising peroxisome proliferator-activated receptor-gamma for subcutaneous administration and a method for improving imperfections of the skin, wherein the injectable composition is subcutaneously administered at the area of skin imperfections comprising the steps: a) identifying an area of skin imperfections, b) administering a safe and cosmetically effective amount of the composition subcutaneously to the area of skin imperfections.

The invention discloses a novel thiazolidine derivant and a preparation method, a medicine combination and a purpose thereof, which specifically relate to the thiazolidine derivant shown as the formula I and the formula II, officinal salt of the derivant, a precursor or a derivant with the same biological function with the thiazolidine derivant, the preparation method of the thiazolidine derivant, the combination of one or a plurality of thiazolidine derivants and the purpose of the compound in treatment on diseases related with glucokinase and a peroxisome proliferators activated receptor, such as diabetes mellitus and obesity.

The present invention provides a compound of formula (I):

• • wherein R¹-R⁵, R²⁵, R²⁶, Y, y, and X² are as defined herein. The compounds activate human peroxisome proliferater activated receptors (hPPARs) and are useful for the treatment of associated disorders such as dyslipidemia, syndrome X, hypercholesteremia, type II diabetes mellitus, type I diabetes, insulin resistance, hyperlipidemia, and obesity.

This invention features the identification of novel target genes for peroxisome proliferator-activated receptors alpha (PPARα) in human, and their use in treating or monitoring the treatment of metabolic abnormalities, as well as in identifying compounds useful for treating metabolic abnormalities.

The present invention relates to directed differentiation and maturation of mammalian hepatocytes, such as human hepatocytes. The hepatocyte obtained in accordance with the present invention show a phenotype which is more similar to that of primary hepatocytes than previously shown. In particular, the present invention relates to exposure of mammalian hepatocytes, such as human hepatocytes, to at least one maturation factor selected from the group consisting of Src kinase inhibitors, vitamin D including precursors, metabolites and analogs thereof, hypoxia inducing compounds, sphingosine and sphingosine derivatives, activators of peroxisome proliferator-activated receptors (PPARs), platelet-activating factor (PAF), PKC inhibitors, and combinations thereof.

The invention provides novel pharmacologic action of non-steroidal anti-in-flammatory medicines, i.e. the action for preventing and treating the diabetic encephalopathy. The non-steroidal anti-inflammatory medicines (ibuprofen) can be used for obviously improving the injury of the cognitive function caused by the diabetes mellitus, obviously increasing the protein expression and the mRNA (messenger ribose nucleic acid) level of intracerebral peroxisome proliferators-activated receptor gamma (PPAR gamma), obviously reducing the activity, the protein expression and the mRNA level of cerebral cortex beta amyloid precursor protein gamma-beta amyloid cleaving enzyme 1 (beta amyloid cleaving enzyme 1), the level of end-stage advanrced glycation end products (AGEs), and the protein expression of cyclo-oxygenase 2 (COX-2) and inducible nitric oxide synthase (iNOS), and obviously increasing the level of superoxide dismutase (SOD) reduced glutathione (GSH) in blood serum, etc. The non-steroidal anti-in-flammatory medicines can be used for preventing and treating the diabetic complication, i.e. the diabetic encephalopathy.

Ligands of nuclear receptors PPAR's (peroxisome proliferator-activated receptors) which are compounds selected from the group consisting of ascofuranone; and ascofuranone homologs and ascochlorin homologs having at least an orcyl aldehyde moiety wherein the hydrogen atom(s) of the hydroxyl group(s) at the 2-position and/or the 4-position of the orcyl aldehyde moiety are substituted by C1-15 alkyl, C1-15 alkenyl, CH2COOH, CH2COO(C1-15 alkyl), C(C=O)(C1-15 alkyl), C(=O)(CH2)1-15COOH, nicotinoyl, isonicotinoyl, etc. These ligands are usable in preventing and/or treating diabetes; hypertension or cerebrovascular disorders; arteriosclerosis; complications of diabetes; chronic inflammation; cachexia; digestive cancers, etc.