Event
Bristol-Myers Squibb Lectures in Organic Chemistry: Gunda Georg (University of Minnesota) & Richard Fox (BMS)
Discovery and development of a male pill by targeting the retinoid signaling pathway with YCT-529 for effective, reversible oral contraception
Gunda Georg
University of Minnesota
Discovery and development of a male pill by targeting the retinoid signaling pathway with YCT-529 for effective, reversible oral contraception
To lower the high levels of unintended pregnancies observed worldwide, additional effective contraceptive methods for women and men are desirable. Multiple contraceptive methods are available for women; however, male contraception options are limited to condom use and vasectomy. A novel male birth control method would provide an alternate method for family planning and lessen the gender gap in contraceptive responsibility. Hormonal male contraceptives have been investigated for many years, but no drug has reached the market yet. Therefore, investigations have been initiated in several laboratories to discover non-hormonal contraceptive agents. The talk will discuss the discovery and development of a selective retinoic acid receptor alpha antagonist, including preclinical efficacy studies of the clinical candidate YCT-529 in mouse and non-human primates and initial results from the first non-hormonal male contraceptive to reach the clinical stage.
Richard Fox
BMS
Evolution of a Concise Approach to Chiral Cyclohexyl Based Drug Candidate BMS-986278
Development of efficient and sustainable syntheses of new clinical candidates is a vital portion of process development for every pharmaceutical company. An approach to an efficient synthesis combines retrosynthesis (i.e., the ideas of the innovator) and subsequent process development (i.e., the decisions made on selected ideas. This presenation will disclose the discovery of an ERED/KRED biocatalytic cascade to enable efficient installation of two challenging stereocenters on a cyclohexyl ring, as well as the overall strategy and key-decisions that led to the development of an improved 4th generation route to BMS-986278, a potent small-molecule LPA1 antagonist. The talk will discuss how the culmination of these decisions and innovations led to an increase in overall yield by >3x, completely eliminated the use of halogenated solvents and reduced the overall Process Mass Intensity (PMI) and projected raw material costs by 89%, and 80%, respectively.