33 results about "Fatty Acid Synthases" patented technology

A compound of formula Ior a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as Fatty Acid Synthase inhibitors, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus, cancer and infection and pharmaceutical compositions containing them.

The present inventors focused on certain nutritional compositions known to have activity of controlling blood glucose levels. These foods were administered to rats for long periods, and real-time PCR was used to analyze the expression of genes associated with lipid metabolism in the liver and adipose tissues. As a result, the present inventors found that the expression of the PPARα gene is enhanced by these foods, and that this is accompanied by suppressed expression of fatty acid synthase and enhanced expression of a group of PPARα target genes associated with fatty acid metabolism. The present inventors also confirmed the effect of these foods in enhancing the expression of PPARγ and adiponectin, and discovered that these foods have the activity of enhancing the production of PPAR and PPAR-associated factors.

A pharmaceutical composition comprising a pharmaceutical diluent and a compound of formula IV wherein R21=H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, —CH2OR25, —C(O)R25, —CO(O)R25, —C(O)NR25R26, —CH2C(O)R25, or —CH2C(O)NHR25, where R25 and R26 are each independently H, C1-C10 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing one or more halogen atoms. R22=—OH, —OR27, —OCH2C(O)R27, —OCH2C(O)NHR27, —OC(O)R27, —OC(O)OR27, —OC(O)NHNH—R5, or —OC(O)NR27R28, where R27 and R28 are each independently H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, and where R27 and R28 can each optionally contain halogen atoms; R23 and R24, the same or different from each other, are C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl. Methods of using such formulations for the treatment of cancer, to effect weight loss, to treat microbially-based infections, to inhibit neuropeptide-Y and / or fatty acid synthase, and to stimulate CPT-1.

The invention relates to cyclopentanecarboxamide derivatives of formula 1, to their use as Fatty Acid Synthase inhibitors, to methods for their therapeutic use and to pharmaceutical compositions containing them, wherein R1, R2, R3, LO, W, AR1, n are as defined in claim 1.

The present invention relates to proteins involved in fatty acid synthesis, such as fatty acid synthases (FAS) variants, comprising one or more polypeptide chains, wherein said polypeptide chain(s) comprise one or more subunits comprising a malonyl / palmitoyl transferase domain (MPT domain), acetyl transferase domain (AT domain), and ketoacyl synthase domain (KS domain), and at least one amino acid substitution in the MPT domain at a position corresponding to R130, in the AT domain at a position corresponding to I306, and / or in the KS domain, preferably in the acyl binding channel and / or at KS domain binding site to ACP, to modulate affinities of acyl intermediates, and optionally further amino acid substitution(s). The present invention relates to the respective polypeptide domains. The present invention further relates to nucleic acid molecules encoding the proteins (or the polypeptide domains) and to host cells containing said nucleic acid molecules. The present invention further relates to a method for the production of short fatty acids, CoA esters of short fatty acids, ethyl esters of short fatty acids, esters of short fatty acids with other metabolites, and / or enzyme bound short fatty acids (C6 to C12), comprising the expression of said nucleic acid molecules, preferably in said host cells. The present invention further relates to a method for the production of biofuels, flavoring compounds and / or fine chemicals, comprising the expression of said nucleic acid molecules, preferably in said host cells. The present invention also relates to the use of the proteins, nucleic acids molecule or host cells for the bulk production of short fatty acids (C6 to C12), the specific production of C6 fatty acids and / or C8 fatty acids, the bulk production of CoA esters of short fatty acids (C6 to C12), the specific production of C6-CoA esters and / or C8-CoA esters, the bulk production of ethyl esters of short fatty acids (C6 to C12), the specific production of C6 fatty acid ethyl esters and / or C8 fatty acid ethyl esters, the bulk production of esters of short fatty acids (C6 to C12) with other metabolites, the specific production of C6 fatty acid esters with other metabolites and / or C8 fatty acid esters with other metabolites, the bulk production of enzyme bound short fatty acids (C6 to C12), the specific production of enzyme bound C6 fatty acids and / or enzyme bound C8 fatty acids, the production of biofuels, fine chemicals and / or flavoring substances.

The invention relates to a general formula I pyrrole derivation capable of inhibiting the fatty acid synthase, or all possible isomers thereof, or medicated salts or solvates thereof, wherein the definition of each substituting group in general formula I is shown in the instruction; the invention also relates to a preparation process for general formula I pyrrole derivation; the invention comprises the compound, or all possible isomers thereof, or medicated salts or medicine combinations of solvates thereof, and the usage that the compound can be used to prepare the medicaments for the bacteria infection.

Compounds of formula (I), wherein R1, R2, R, X1, X2, X3, X4, n1, n2, n3 and n4 have the meanings indicated in claim 1, are inhibitors of fatty acid synthase and are especially useful in the treatment of Diseases such as cancer, cardiovascular disease, damage to the central nervous system, and different forms of inflammation.

The present disclosure generally relates to novel compounds as a fatty acid synthase inhibitor useful for the treatment of infection diseases, cancers, or metabolic diseases that malfunction of fatty acid synthase is involved. In particular this present invention directs to malonyl-coenzyme A (CoA) mimetics and methods of use thereof. The invention described herein also pertains to pharmaceutical compositions and methods for treating diseases in mammals using compounds disclosed herein.

The present invention relates to an autoantibody specifically recognizing the epitope sequence of FASN (fatty acid synthase), more particularly, to the autoantibody or a fragment comprising an antigen-binding site thereof, a diagnostic composition for hepatocellular carcinoma comprising an agent capable of assessing the expression level of the autoantibody, a hybridoma cell line producing the autoantibody, a diagnostic kit for hepatocellular carcinoma comprising the composition, a method for detecting the autoantibody of hepatocellular carcinoma patient using the composition, and a method for screening a therapeutic agent for hepatocellular carcinoma by administering candidate materials for hepatocellular carcinoma treatment to confirm a reduction in the expression level of autoantibody.

Compounds of formula (I), wherein R, X1, X2, X3, X4, R1, R2 and q have the meanings indicated in claim 1, are inhibitors of fatty acid synthase and are especially useful in the treatment of diseases such as cancer , cardiovascular disease, central nervous system injury and different forms of inflammation.

Compounds of the formula (I) in which R1, R2, R, X1, X2, X3, X4, n1, n2, n3 and n4 have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

The expression of a mRNA encoding a putative 76 amino acid, secreted protein (“Enho1”) was found to negatively correlate with fasting triglyceride and cholesterol levels. A recombinant adenovirus was used to increase the expression of Enho1 mRNA in two mouse models of obesity, KK-Ay and Lepob / Lepob mice. Over-expression of Enho1 by adenovirus injection significantly, and reproducibly, reduced fasting triglyceride and cholesterol levels in both models. In addition, transgenic mice strains were made that over express Enho1 protein. Additionally, the expression of a key gene involved in lipogenesis (fatty acid synthase) and FAS protein levels were reduced by ENHO1 adenoviral treatment in Lepob / Lepob mice. Full-length ENHO1 peptide, or peptide derivatives, homologues, analogues, or mimetics thereof, delivered by oral intake, injection, subcutaneous patch, or intranasal routes, could be used as therapeutic or diagnostic agents for hypercholesterolemia, hypertriglyceridemia, insulin resistance, obesity, diabetes, and / or energy imbalance.

The invention discloses a fatty acid synthase inhibitor, its production method and application, and its purpose is to provide a fatty acid synthase inhibitor, its production method and its prevention and adjuvant treatment of related diseases with fatty acid synthase as the target in the application. The fatty acid synthase inhibitor is obtained by treating tea warm extract or catechin compounds with acid. The preparation method of the fatty acid synthase inhibitor provided by the invention is to react the warm tea extract or catechin compounds with acid at 25-120°C to obtain the fatty acid synthase inhibitor. The present invention has significant potential applications in the prevention and auxiliary treatment of diseases targeted at fatty acid synthase, especially in the medicines and health products for weight control, prevention and auxiliary treatment of obesity-related diseases, and prevention and auxiliary treatment of cancer value.

The invention discloses a preparation method and application of an apocynum venetum extract. The method comprises the following steps of: crushing apocynum venetum leaves, carrying out reflux extraction at room temperature or heated temperature by using ethanol, filtering, merging extracting solutions, carrying out vacuum concentration until no ethanol smell exists to obtain an ethanol extract; and diluting the ethanol extract by using water, degreasing by using petroleum ether, extracting the ethanol extract by using ethyl acetate or n-butyl alcohol as a solvent, recovering the solvent at reduced pressure, and drying to obtain the apocynum venetum extract. Proved by tests, the apocynum venetum extract obtained by using the method disclosed by the invention is an extract capable of inhibiting the activity of fatty acid synthase so as to be a natural, plant-sourced and nontoxic fatty acid synthase inhibitor.