254 results about "Cholesteryl ester" patented technology

Cholesteryl ester transfer protein inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.

The present invention relates to a compound of the general formula (1):

wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted heterocyclic group, and the like; R¹ is an optionally substituted alkyl group, wherein the alkyl group further may optionally be substituted by an optionally substituted homocyclic group, and the like; and R² is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.

Cholesteryl ester transfer protein inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.

Cholesteryl ester transfer protein inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.

A pharmaceutical composition comprises a solid amorphous dispersion of a cholesteryl ester transfer protein inhibitor and a concentration-enhancing polymer.

Cholesteryl ester transfer protein inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.

Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), A¹ is a cyclic group, and B is a cyclic group which is attached to the heterocyclic ring directly or through a methylene group.

The present invention relates to a composition comprising: a C12 to C24 branched or unbranched hydrocarbon; a mid-chain triglyceride; a C26 to C36 branched or unbranched hydrocarbon; a cholesteryl ester; an ester of a C10 to C24 fatty acid and a C10 to C20 alcohol; an ester of a C10 to C24 fatty acid and a C21 to C34 alcohol; glycerol; and a polar lipid; and to methods of making and methods of using the composition to treat lipid tear deficiency (LTD), aqueous tear deficiency (ATD), a combination of LTD and ATD, and other dry eye conditions. The composition is substantially free of water and substantially free of an artificial surfactant. A method of administering an ointment comprising a lipid composition to treat dry eye, while achieving sustained release of the ointment and preventing a blurring of vision by the ointment, comprises applying the ointment to the inferior lid margin of the outside skin of the lower eyelid or to the superior lid margin of the outside skin of the upper eyelid, and allowing the ointment to diffuse onto the eye. Also disclosed is the use of kinetic analysis of tear interference images to analyze an individual's precorneal lipid film spread to identify LTD or to evaluate response to LTD treatment in order to adjust percentages of lipids in the composition.

The invention relates to the pharmaceutical field, in particular to application of a series of pentacyclic triterpenoid compounds as a cholesterol ester transfer protein (CETP) inhibitor, in particular to application in factors of preparing medicines for treating cardiovascular and cerebrovascular diseases, atherosclerosis diseases and hyperlipemia. The invention further discloses a series of novel pentacyclic triterpenoid compounds, application of the compounds as the CETP inhibitor and a pharmaceutical composition.

The present invention relates to a compound of the general formula (1):

wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R¹ is an optionally substituted alkyl group, and the like; and R² is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.

It has been discovered that certain selected ethers of probucol, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.

A composition comprises (1) a solid amorphous adsorbate comprising a cholesteryl ester transfer protein (CETP) inhibitor and a substrate; and (2) an HMG-CoA reductase inhibitor. The solid amorphous adsorbate provides concentration enhancement of the CETP inhibitor relative to a control composition consisting essentially of the unadsorbed CETP inhibitor alone, resulting in improved bioavailability.

The present invention provides a method of administering vitamin B6 related compounds for treatment of hypertriglyceridemia. Vitamin B6 related compounds include pyridoxal, pyridoxal-5′-phosphate, pyridoxamine, a 3-acylated analogue of pyridoxal, a 3-acylated analogue of pyridoxal-4,5-aminal, and mixtures thereof. Embodiments of the present invention also comprise co-administering a lipid lowering agent, such as a nicotinic acid, a fibrate, a HMG CoA reductase inhibitor, a cholesteryl ester transfer protein inhibitor, and combinations thereof.

A computer-based method for determining a prediction of risk and/or an indication of extent of coronary stenosis in a human subject, comprises the steps of: (a) inputting the level of at least one cholesteryl ester measured in a blood sample collected from said subject; and then (b) inputting the age and gender of said subject; and then (c) generating in said computer from said cholesteryl ester level input, said age input and said gender input a prediction of risk and/or an indication of extent of coronary stenosis blood sample by mass spectrometry.

A novel compound of the formula (I):

wherein R¹ is alkoxycarbonyl or the like, R² is alkyl or the like; R³ is hydrogen or the like; R⁴ is alkylene or the like; R⁵ is optionally substituted heterocyclic group; R⁶, R⁷, and R⁸ are independently hydrogen; alky, alkoxy, or the like; R¹⁰ is optionally substituted aromatic ring, or the like; or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP).

This invention relates to inhibitors of CETP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders mediated by CETP.