62 results about "Cholesterol absorption inhibitor" patented technology

A pharmaceutical combination comprising an effective amount of at least one cholesterol absorption inhibitor and at least one microsomal triglyceride transfer protein inhibitor (MTP).

To provide a bacterium belonging to the genus Bifidobacterium which is excellent in a survival ability in the gastrointestinal tract, has an effect of inhibiting the cholesterol absorption in the intestinal tract, and is excellent in lipid metabolism ameliorating effects including decreasing the blood cholesterol level and the like, and shows a high survival rate after storage, and a cholesterol absorption inhibitor using the same. The invention provides a cholesterol absorption inhibitor containing, as an active ingredient, at least one microorganism selected from Bifidobacterium animalis subsp. animalis YIT 10394, Bifidobacterium animalis subsp. lactis JCM 1253, Bifidobacterium animalis subsp. lactis JCM 7117, and Bifidobacterium pseudolongum subsp. globosum.

The present invention relates to a method of reducing C-reactive protein in a subject in need of treatment thereof, wherein the subject is at risk of having or the subject has already had a vascular event or suffering from an inflammatory disease or disorder. In one embodiment, the vascular event is a cardiovascular event (e.g., myocardial infarction). In another embodiment, the vascular event is a cerebrovascular event (e.g., stroke (such as transient ischemic attacks (TIAs)). In yet another embodiment the vascular event is a peripheral vascular event (e.g., intermittent claudication). The method comprises administering a therapeutically effective amount of at least one growth hormone secretagogue compound or a pharmaceutically acceptable salt, hydrate or solvate thereof. The growth hormone secretagogue can be coadministered with a second growth hormone secretagogue, HMG CoA reductase inhibitor, an ACAT inhibitor, a CETP inhibitor, an anti-inflammatory agent, an ACE inhibitor, a Beta blocker, a cholesterol absorption inhibitor, a nicotonic acid, a fibric acid derivative, a bile acid sequestering agent or a combination thereof.

The instant invention provides a pharmaceutical composition comprised of a cholesterol absorption inhibitor and an HMG-CoA reductase inhibitor, one or more anti-oxidants, microcrystalline cellulose, hydroxypropyl methylcellulose, magnesium stearate and lactose. The composition need not contain ascorbic acid in order to obtain desirable stability.

The invention relates to compositions containing cholesterol absorption inhibitors alone or in combination with other therapeutic agents for treating non-alcoholic fatty liver disease-associated disorders by administering a therapeutically effective amount of the compositions to a subject in need thereof.

Provided, among other things, is a formulation or kit comprising: (a) a pharmaceutically effective dosage of one or more a glucose-level-controlling bioactive agents selected from an α-glucodase inhibitor, sulfonylurea, meglitinide, thiazolidinediones, biguanide, insulin, dual PPARα / γ agonist, PPARγ agonist or insulin secretagogue; and (b) a pharmaceutically effective dosage of (i) one or more of an antihypertensive bioactive agent selected from an ACE inhibitor, calcium channel blocker, beta blocker, angiotension II receptor antagonist or diuretic, or (ii) one or more of an anti-dyslipidemia bioactive agent selected from a HMG-CoA reductase inhibitor, bile acid sequestrant, fibric acid derivative, sterol, cholesterol absorption inhibitor, MTP inhibitor or nicotinic acid derivative; wherein: in the case of (i) a combination of a first bioactive agent of group (a) that is metformin with a second bioactive agent of group (b), or (ii) a combination of a first bioactive agent of group (a) that is a thiazolidinedione or dual PPARα / γ agonist with an angiotension II receptor antagonist, one or more of the following applies: (I) one of the first bioactive agent or the second bioactive agent is formulated for sustained release, and the other is formulated for immediate release, each formulated for once-a-day dosing; or (II) the co-formulation or kit comprises (A) a biguanide and a thiazolidinedione and (B) one or more group (b) bioactive agents.

This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.

The present invention provides methods for the treatment of obesity using sterol or 5α-stanol absorption inhibitors and compositions and therapeutic combinations including sterol or 5α-stanol absorption inhibitors and at least one obesity control medication.

This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.

This invention provides cholesterol absorption inhibitors of Formula I:and the pharmaceutically acceptable salts thereof, wherein R12 is an alkyl, alkeny or alkynyl group mono- or poly-substituted with —OH, —COOH or a combination of—OH and —COOH, and R9 contains an alkyl, alkeny or alkynyl group substituted with a heterocyclic ring, amino or sulfonyl. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating atherosclerosis and preventing atherosclerotic disease events.

To provide a bacterium belonging to the genus Bifidobacterium which is excellent in a survival ability in the gastrointestinal tract, has an effect of inhibiting the cholesterol absorption in the intestinal tract, and is excellent in lipid metabolism ameliorating effects including decreasing the blood cholesterol level and the like, and shows a high survival rate after storage, and a cholesterol absorption inhibitor using the same. The invention provides a cholesterol absorption inhibitor containing, as an active ingredient, at least one microorganism selected from Bifidobacterium animalis subsp. animalis YIT 10394, Bifidobacterium animalis subsp. lactis JCM 1253, Bifidobacterium animalis subsp. lactis JCM 7117, and Bifidobacterium pseudolongum subsp. globosum.

The invention is directed to methods for treating and / or controlling obesity in a patient. The methods involve combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, AEGR-733 and implitapide) and a cholesterol absorption inhibitor (CAI) (for example, ezetimibe).

The invention provides methods and compositions for treating hyperlipidemia and disorders associated with hyperlipidemia in a mammal. Compositions useful in the practice of the invention include a microsomal triglyceride transport protein inhibitor (“MTPI”) and at least two other cholesterol lowering drugs selected from the group consisting of a cholesterol absorption inhibitor (“CAI”), a HMG-CoA reductase inhibitor, a bile acid sequestrant, a fibric acid derivative, niacin, and squalene synthetase inhibitor.

The present invention provides compositions, therapeutic combinations and methods including: (a) at least one peroxisome proliferator-activated receptor activator; and (b) at least one substituted azetidinone or substituted β-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols.

The present invention is directed to systems, apparatus and methods for creating derivatives of at least one form of HDL without substantially affecting LDL. These derivatives of HDL are particles with reduced lipid content, particularly reduced cholesterol content. These particles have the capacity to bind cholesterol and are administered to a patient to enhance cellular cholesterol efflux and reduce cholesterol levels in cells, tissues, organs, and blood vessels. The present method is useful for treating atherogenic vascular disease and may be combined with other therapies such as statins, inhibitors of cholesterol absorption, niacin, anti-inflammatories, exercise and dietary restriction.

The present invention provides methods of treating diabetes and associated conditions by administering a composition including at least one sterol or 5α-stanol absorption inhibitor or compositions or therapeutic combinations including: (a) at least one antidiabetic medication; and (b) at least one sterol or 5α-stanol absorption inhibitor.

Amorphous HMG CoA reductase inhibitors, especially amorphous atorvastatin, are described. Also described are pharmaceutical combinations comprising amorphous HMG CoA reductase inhibitors in combination with cholesterol absorption inhibitors or fibrates. A method of manufacturing the compositions using a hot melt extrusion process are also described.

The purpose in this invention is to providing drugs for treating or preventing duplication of hypertension with serum hyperuricemia and / or hypercholesterolemia that is much frequency among the duplication onset in geriatric diseases. This invention is related to drugs for treating or preventing duplication of hypertension with serum hyperuricemia and / or hypercholesterolemia of which active principles are 2-propyl-3- {[2'-(1H-tetrazole -5-yl) biphenyl -4-yl]methyl}-5, 6, 7, 8-tetrahydrocyclohepta imidazole -4-(3H) - one and that prodrug or that salt. Pratosartan is able to use in combination with one or more than two diuretics chosen from sulfonamide-, phenoxyacetic acid- and thiazide-type diuretics, triamterene, amiloride, spironolactone, potassium canrenoate and traxanox sodium. Also, pratosartan is able to use in combination with one or more than two hypolipidemic drugs chosen from statins, fibrates, cholesterol absorption inhibitors, cholesterol sequestrants and cholesterol excretion enhancers.

The present invention discloses a fire-new sucrose absorbing depressor, which is the common microelement complex in arabinose and living body. No matter the complex is pure compound or mixture containing other natural products, the pure compound and the mixture has equal effect. The complex can be used for reducing glycemia, losing weight and other purposes. A simpler arabinose separation method is also provided by the present invention.

The instant invention provides novel cholesterol absorption inhibitors of Formula I and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.

The invention discloses a compound preparation for treating cardiovascular and cerebrovascular diseases. The compound preparation comprises a cholesterol reuptake inhibitor, an HMG-CoA (3-hydroxy-3-methyl-glutaryl) reductase inhibitor and a calcium ion antagonist, and has the effect of jointly lowering blood pressure and lipid. According to the compound preparation, isolating layers or / and coatings are arranged for active ingredients or a part of active ingredients, and the usage amount of antioxidants in a precipitation is reduced, therefore, the medicine therapeutic range is expanded, the stability and safety of the medicine are improved; simultaneously, the medication compliance of a patient suffering from hypertension and hyperlipemia is improved.

The invention provides a liquid chromatography detection method for ezetimibe optical isomers; the detection method comprises the following chromatographic conditions: chromatographic columns comprise a silica gel column, an amino column, a cyano column and a chiral column; mobile phases comprise n-hexane (A)-isopropanol (B), n-hexane (A)-ethanol (B), n-heptane (A)-isopropanol (B), n-heptane (A)-ethanol (B), n-hexane (A)-tetrahydrofuran (B), or n-heptane (A)-tetrahydrofuran (B); the ratio of the mobile phases is (A:B)=95:5-50:50; the mobile phase flow rate is 0.2-2.0 mL / min; the detection wavelength is 200-400 nm; the column temperature is 25-40 DEG C; the sample injection volume is 1-40 [mu]L; a detector is an ultraviolet detector or a diode array detector. The detection method provided by the invention has the advantages of relatively high sensitivity and specificity, and concise operation, has the separation degree conforming to standards, can rapidly and accurately detect five kinds of optical isomers of ezetimibe, and has quite important significance on quality control of the cholesterol absorption inhibitor ezetimibe.

Embodiments of the present invention relate generally the use of certain compositions, e.g., compositions comprising a glutathione precursor and a selenium source, in the therapy of subjects suffering from diseases associated with hyperiipidemia and / or hypercholesterolemia. Related embodiments of the present invention relate to treatment and / or reducing the incidence of the side effects of statin therapy comprising administering to a subject in need, a composition comprising a glutathione precursor and a selenium source. Embodiments of the invention also relate to the use of the compositions in combination therapy with other agents such as statins, cholesterol absorption inhibitors, bile acid binding resins, or fibrates. In other embodiments, the invention relates to the use of such compositions comprising the glutathione precursor and the selenium source in the therapy of subjects suffering from erectile dysfunction and / or viral diseases such as Ebola virus disease (EVD) or Ebola hemorrhagic fever (EHF).

The present invention provides compositions, therapeutic combinations and methods including: (a) at least one bile acid sequestrant; and (b) at least one substituted azetidinone or substituted β-lactam sterol absorption inhibitor which can be useful for treating vascular conditions, diabetes, obesity and lowering plasma levels of sterols.

The invention is directed in part to methods for treating and / or controlling hepatitis C in a patient. The methods are directed in part to combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, AEGR-733 and implitapide) and at least one other active agent.

The present invention provides, in one aspect, a method of inhibiting the expression of a multi-drug resistance gene in an animal cell which comprises administering to an animal an effective amount of at least one cholesterol absorption inhibitor. In another aspect, it provides a method of inhibiting the production of a protein expressed by a multi-drug resistance gene in an animal cell which comprises administering to an animal an effective amount of at least one cholesterol absorption inhibitor. In another aspect, the present invention provides a method of enhancing the effectiveness of a chemotherapeutic agent in an animal having cancer, which comprises administering to said animal an effective amount of the chemotherapeutic agent and at least one cholesterol absorption inhibitor. Further, there are provided compositions and kits for use in cancer treatment which comprise at least one chemotherapeutic agent and at least one cholesterol absorption inhibitor.

The invention provides a liquid chromatography detection method of 4-[(4-fluorophenylimino) methyl]-phenol. The liquid chromatography detection method is implemented under the following chromatographic conditions: a chromatographic column is formed by a silica gel column, an amino column, a cyano column, a phenyl column and a chiral column, a mobile phase is formed by n-hexane (A) and isopropanol (B), n-hexane (A) and ethanol (B), n-heptane (A) and isopropanol (B), or n-heptane (A) and ethanol (B), a ratio of A to B in the mobile phase is (95:5) to (70:30), the mobile speed of the mobile phase is 0.2-2.0mL / min, the detection wavelength is 200-400nm, the column temperature is 25-40 DEG C, and an ultraviolet detector or a diode array detector is adopted. The detection method is normal-phase liquid chromatography. The detection method is high in sensitivity and specificity, is simple and convenient in operation, has a degree of separation meeting the standards, can be used for rapidly and accurately detecting related substances and the content of 4-[(4-fluorophenylimino) methyl]-phenol, can be applied to quality control of 4-[(4-fluorophenylimino) methyl]-phenol, and has important significance to synthesis of a cholesterol absorption inhibitor, namely ezetimibe.

The invention relates to an ezetimibe analogue and a preparation method thereof. The structure general formula of the ezetimibe analogue is shown in a structural formula, wherein in the formula, R1, R2 and R3 are selected from fluorine atom, hydroxyl, hydrogen atom and methoxy independently. The ezetimibe analogue is an ideal inhibitor for sucking cholesterol, and the cholesterol inhibitor can obviously prevent Caco-2 cells from sucking the cholesterol, so that the ezetimibe analogue has the prospect of becoming the inhibitor for sucking the cholesterol.