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Pharmaceutical composition comprising hydroxylated nebivolol

A technology of composition and flavonoids, which is applied in the direction of drug combination, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve problems such as increased oxidative stress, increased platelet aggregation, and reduced NO release

Inactive Publication Date: 2008-03-19
MYLAN LAB INC (US)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, in conditions of hypertension and hyperlipidemia, dysfunction of the endothelium causes a marked decrease in NO release, which results in: 1) increased vasoconstriction and vasospasm; 2) more infiltration of monocytes and LDL; 3 ) proliferation of vascular smooth muscle cells; 4) increased oxidative stress; and 5) increased platelet aggregation

Method used

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  • Pharmaceutical composition comprising hydroxylated nebivolol
  • Pharmaceutical composition comprising hydroxylated nebivolol
  • Pharmaceutical composition comprising hydroxylated nebivolol

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Embodiment Construction

[0025] definition

[0026] For convenience, before further describing the invention, certain terms used in the specification, examples and appended claims are collected here. These definitions should be read and understood by those skilled in the art in light of the remainder of this disclosure. Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art.

[0027] The articles "a" and "an" are used herein to refer to one or more than one (ie, at least one) of the grammatical object of the article. By way of example, "an element" means one element or more than one element.

[0028] "About the same time" means that within about 30 minutes of administering one compound (nebivolol) to the patient, the other active compound is administered to the patient. "About the same time" also includes administering the compounds simultaneously.

[0029] The phrase "angiotensin converting enzyme ...

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Abstract

Hydroxylated nebivolol metabolites increase NO release in human endothelial cell preparations in a concentration-dependent manner after acute administration. In addition, hydroxylated nebivolol metabolites (including but not limited to 4-hydroxy-6,6'difluoro) have the ability to increase NO release in human endothelial cells after chronic administration. The present invention provides hydroxylated nebivolol metabolites for use in the treatment of cardiovascular diseases. Furthermore, the present invention provides methods of treating and / or preventing vascular diseases by administering at least one hydroxylated metabolite of nebivolol capable of releasing a therapeutically effective amount of nebivolol to targets affected by vascular diseases. Nitric oxide.

Description

[0001] John P.O’Donnell, Walter Owens, Joseph Duncan, Andrew Shaw, all of Morgantown, WV; Jinn Wu of Princeton Junction, NJ [0002] Pursuant to 35 USC §119, this application claims priority to US Provisional Application Serial No. 60 / 648,551 filed January 31, 2005 and US Provisional Application Serial No. 60 / 755,856 filed January 3, 2006. technical field [0003] Metabolites of nebivolol possess pharmacological properties that may be beneficial in the treatment of various diseases such as cardiovascular diseases, which may include hypertension, atherosclerosis, and congestive heart failure . In particular, nebivolol and its key metabolites have effects on NO metabolism independent of β 1 - Selective interaction and beneficial effect of nebivolol metabolites on endothelial NO release associated with their use in the treatment of cardiovascular diseases. Described are hydroxylated nebivolol metabolites, compositions containing at least one hydroxylated nebivolol metabolite, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/353C07D311/58A61P9/00A61P9/08
Inventor J·P·奥唐奈W·欧文斯J·邓肯A·肖J·吴
Owner MYLAN LAB INC (US)
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