Bristol-Myers Squibb Compnay

Anthera Pharmaceuticals, Inc.

Scott Chadwick

Purushotham Vemishetti

Patrick Irving Eacho

Emily A Reiff

Debra Odink

Carrie A Costello

Joaquim Trias

Colin Hislop

Marian Mosior

Paul Truex

Sridhar Desikan

Bernadine Fraser

Kenneth Gould

Administration of sPLAinhibitors has been found to decrease cholesterol levels, atherosclerotic plaque formation and aortic aneurysm in mice, and to decrease cholesterol and triglyceride levels in humans. Interestingly, administration of sPLAinhibitors was found to decrease cholesterol levels even when the inhibitors were administered only once per day. Therefore, provided herein are methods of treating dyslipidemia, CVD, and conditions associated with CVD such as atherosclerosis and metabolic syndrome, by administering one or more sPLAinhibitors. Significantly, administration of sPLAinhibitors and various compounds used in the treatment of CVD, such as for example statins, resulted in greater decreases in LDL and LDL particle levels in a synergistic manner. In addition, administration of sPLAinhibitors and statins resulted in a synergistic decrease in plaque content. Therefore, also provided herein are compositions comprising one or more sPLAinhibitors and one or more compounds used in the treatment of CVD, such as for example statins, and methods of using these compositions to treat dyslipidemia, CVD, and conditions associated with CVD such as atherosclerosis and metabolic syndrome.

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The present invention provides novel methods for the synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (III) which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.

Synthesis of a benzoxazinone

Growing community of inventors

Redwood City, CA, United States of America

Scott Chadwick