62 results about "Cholesterol absorption inhibitor" patented technology

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.

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 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 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 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.