Phenoxy-pyrrolidine derivative and its use and compositions
Inventors
Assignees
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Publication Number
US-8980936-B2
Publication Date
2015-03-17
Expiration Date
Abstract
The present invention is directed to the compound 2-(4-(hydroxymethyl)phenoxy)-1-(3-(2-(trifluoromethyl)phenoxy)pyrrolidin-1-yl)ethanone, its use as an inhibitor of stearoyl CoA desaturase and to pharmaceutical compositions containing this compound.
Core Innovation
The document describes a phenoxy-pyrrolidine derivative of Formula I, specifically (S)-2-(4-(hydroxymethyl)phenoxy)-1-(3-(2-(trifluoromethyl)phenoxy)pyrrolidin-1-yl)ethanone, as an inhibitor of stearoyl-CoA desaturase (SCD1). The activity is linked to inhibition of SCD1-related lipid biology, including effects on cholesterol esters and wax esters and reduction of sebaceous gland size. Reducing SCD1 activity reduces sebum production and secretion, including in settings associated with excess sebum.
The problem addressed is related to excess sebum production and secretion, with treatment motivations connected to limitations of isotretinoin and other therapies described in the background. The document positions SCD1 inhibition as a therapeutic approach for dermatologic and cosmetic conditions mediated by stearoyl-CoA desaturase and associated with excess sebum. Conditions explicitly discussed include acne, oily skin/hair, and seborrheic dermatitis.
The document provides pharmaceutical compositions containing the Formula I compound, or pharmaceutically acceptable salt, solvate, or hydrate, and describes treatment uses for reducing sebum production and secretion. It includes broad chemical scope language covering salts, solvates, hydrates, stereoisomers, enantiomers, and isotopically labeled variations, and describes administration forms including topical, oral, and parenteral routes.
Claims Coverage
The independent claim covers administering a Formula I compound, or pharmaceutically acceptable salt, solvate, or hydrate, in an amount effective to treat Propionibacterium acnes growth by reducing sebum production and secretion, with dependent claims specifying human subjects and administration routes.
Treating Propionibacterium acnes growth by reducing sebum production and secretion
A method of treating Propionibacterium acnes growth by reducing a subject’s sebum production and secretion by administering a compound of Formula I or a pharmaceutically acceptable salt, solvate or hydrate in an amount effective to treat Propionibacterium acnes growth.
Human subject treatment
The method is performed with a human as the subject for treating Propionibacterium acnes growth by reducing sebum production and secretion.
Administration route selection
The compound is administered topically, orally, or parenterally to treat Propionibacterium acnes growth by reducing sebum production and secretion.
Overall, the claim set is directed to treating Propionibacterium acnes growth by administering a Formula I phenoxy-pyrrolidine, or pharmaceutically acceptable salt, solvate, or hydrate, in an amount effective to reduce sebum production and secretion, with dependent coverage narrowed to human subjects and specified administration routes.
Stated Advantages
Reduces sebum production and secretion.
Treats Propionibacterium acnes growth by reducing sebum production and secretion.
Documented Applications
Treatment of conditions associated with excess sebum production and secretion, including acne, oily skin/hair, and seborrheic dermatitis.
Reducing sebum production and secretion in relation to stearoyl-CoA desaturase (SCD1) mediated biology.
Methods for treating Propionibacterium acnes growth by reducing a subject’s sebum production and secretion.
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