Cycloalkyl lactam derivatives as inhibitors of...

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C514S422000

Reexamination Certificate

active

07834194

ABSTRACT:
The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention provides compositions comprising compounds of formula I for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula (I) wherein, R0is (II), or (III) G1is methylene or ethylene; L is a divalent linking group selected from —(C1-C4) alkylene-, —S—, —CH(OH)—, or —O—; A is methylene, —S—, —O—, or —NH—; and the other substituents are as defined in the claims.

REFERENCES:
patent: WO 02/26706 (2002-04-01), None
patent: WO 2004/033427 (2004-04-01), None
patent: WO 2004/041776 (2004-05-01), None
patent: WO 2005/108361 (2005-11-01), None
Bydal et. al. “Inhibition of type 2 17B-hydroxysteroid dehydrogenase by estradiol derivatives bearing a lactone on the D-ring: structure—activity relationships” Steroids 2004, 69, 325-342.
Martin, Yvonne C. et. al. “Do Structurally Similar Molecules Have Similar Biological Activity?” Journal of Medicinal Chemistry 2002, 45, 4350-4358.
Messinger, J. et. al. “New inhibitors of 17-hydroxysteroid dehydrogenase type 1” Molecular and Cellular Endocrinology 2006, 248, 192-198.
Webster et. al. “Discovery and biological evaluation of adamantly amide 11b-HSD1 inhibitors” Bioorganic & Medicinal Chemistry Letters 17 (2007) 2838-2843.
Roche et. al. “Discovery and structure—activity relationships of pentanedioic acid diamides as potent inhibitors of 11b-hydroxysteroid dehydrogenase type I” Bioorganic & Medicinal Chemistry Letters 19 (2009) 2674-2678.
Xiang et. al. “Synthesis and biological evaluation of sulfonamidooxazoles and B-keto sulfones: selective inhibitors of 11B-hydroxysteroid dehydrogenase type I” Bioorganic & Medicinal Chemistry Letters 2005, 15, 2865-2869.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Cycloalkyl lactam derivatives as inhibitors of... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Cycloalkyl lactam derivatives as inhibitors of..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Cycloalkyl lactam derivatives as inhibitors of... will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-4251995

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.