Research Topics
| Scott H WattersonSummaryAffiliation: Bristol-Myers Squibb Country: USA Publications
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Detail Information
Publications
Novel diamide-based inhibitors of IMPDHHenry H Gu
Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 12:1323-6. 2002..A series of novel amide-based small molecule inhibitors of inosine monophosphate dehydrogenase is described. The synthesis and the structure-activity relationships (SARs) derived from in vitro studies are presented...- Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066)Scott H Watterson
Bristol Myers Squibb Research and Development, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 21:7006-12. 2011..Compound 4m demonstrated potent in vitro potency, acceptable pharmacokinetic and physicochemical properties, and efficacy when dosed orally in a mouse model of inflammatory bowel disease... - Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419)Scott H Watterson
Bristol Myers Squibb Pharmaceutical Research Institute, Post Office Box 4000, Princeton, New Jersey 08543, USA
J Med Chem 50:3730-42. 2007..This article will detail the discovery and SAR leading to a novel and potent acridone-based IMPDH inhibitor 4m and its efficacy and GI tolerability when administered orally in a rat adjuvant arthritis model... - Novel amide-based inhibitors of inosine 5'-monophosphate dehydrogenaseScott H Watterson
Bristol Myers Squibb PRI, PO Box 4000, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 12:2879-82. 2002..A series of novel amide-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. The synthesis and the structure-activity relationships (SARs) derived from in vitro studies are described... - Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinScott H Watterson
Bristol Myers Squibb Research and Development, P O Box 4000, Princeton, New Jersey 08543, USA
J Med Chem 53:3814-30. 2010..4]nonan-7-yl)nicotinic acid (2e) was selected to advance into clinical trials... - Novel indole-based inhibitors of IMPDH: introduction of hydrogen bond acceptors at indole C-3Scott H Watterson
Bristol Myers Squibb PRI, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 13:1273-6. 2003..Various hydrogen bond acceptors at C-3 of the indole were explored. The synthesis and the structure-activity relationships (SARs) derived from in vitro studies are outlined... - Inhibitors of inosine monophosphate dehydrogenase: SARs about the N-[3-Methoxy-4-(5-oxazolyl)phenyl moietyEdwin J Iwanowicz
Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 13:2059-63. 2003..The syntheses and in vitro inhibitory values for IMPDH II, and T-cell proliferation (for select analogues) are given... - A survey of cyclic replacements for the central diamide moiety of inhibitors of inosine monophosphate dehydrogenaseT G Murali Dhar
Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 12:3125-8. 2002.... - 3-cyanoindole-based inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationshipsT G Murali Dhar
Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 13:3557-60. 2003..The synthesis and the structure-activity relationships (SAR), derived from in vitro studies, for this new series of inhibitors is given... - Quinolone-based IMPDH inhibitors: introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analoguesT G Murali Dhar
Bristol Myers Squibb PRI, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 13:547-51. 2003..This led to the identification of compound 27 as a potent inhibitor of IMPDH with significantly improved aqueous solubility over the lead compound 1... - Novel inhibitors of IMPDH: a highly potent and selective quinolone-based seriesScott H Watterson
Bristol Myers Squibb PRI, PO Box 400, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 13:543-6. 2003..A series of novel quinolone-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. The synthesis and the structure-activity relationships (SARs) derived from in vitro studies are described... - Novel guanidine-based inhibitors of inosine monophosphate dehydrogenaseEdwin J Iwanowicz
Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 12:2931-4. 2002..The synthesis and the structure-activity relationships (SARs), derived from in vitro studies, for this new series of inhibitors is given... - Novel tricyclic inhibitors of IkappaB kinaseJames Kempson
Departments of Discovery Chemistry, Discovery Biology, and Metabolism and Pharmacokinetics and Synthesis and Analysis Technology Team, Bristol Myers Squibb Research and Development, Princeton, New Jersey 08543 4000, USA
J Med Chem 52:1994-2005. 2009..This, combined with an iterative rat cassette dosing strategy, was used to identify compounds with improved pharmacokinetic (PK) profiles to advance for in vivo evaluation... - Rapid synthesis of triazine inhibitors of inosine monophosphate dehydrogenaseWilliam J Pitts
Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 12:2137-40. 2002..A series of novel triazine-based small molecule inhibitors (IV) of inosine monophosphate dehydrogenase was prepared. The synthesis and the structure-activity relationships (SAR) derived from in vitro studies are described... - Periodic, partial inhibition of IkappaB Kinase beta-mediated signaling yields therapeutic benefit in preclinical models of rheumatoid arthritisKathleen M Gillooly
Departments of Immunology and Inflammation Drug Discovery, Bristol Myers Squibb Research and Development, Princeton, New Jersey, USA
J Pharmacol Exp Ther 331:349-60. 2009..Thus, only partial and transient inhibition of IKKbeta is sufficient to yield dramatic benefit in vivo, and this understanding will be important in the clinical development of IKKbeta inhibitors... - Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritisAlaric J Dyckman
Bristol Myers Squibb, Research and Development, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 21:383-6. 2011..The synthesis, structure-activity relationships (SAR) and biological evaluation of thiazole based tricyclic inhibitors of IKK2 are described. Compound 9 was determined to be orally efficacious in a murine model of rheumatoid arthritis... - Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitorsPing Chen
Discovery Chemistry, Bristol Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543, USA
Bioorg Med Chem Lett 13:1345-8. 2003..Subsequent optimization of 1 afforded a series of novel 2-isoquinolinoaminooxazole-based inhibitors, represented by 17, with single-digit nanomolar potency against the enzyme... - Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinaseJames Kempson
Bristol Myers Squibb Research and Development, Princeton, NJ 08543 4000, USA
Bioorg Med Chem Lett 19:2646-9. 2009..A new series of tricyclic-based inhibitors of IKK have been derived from an earlier lead compound. The synthesis and structure-activity relationships (SAR) are described. Compound 4k inhibited TNF production in rats stimulated with LPS... - Discovery of N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a novel and potent inhibitor of inosine monophosphate dehydrogenase with excellent in vivo activityT G Murali Dhar
J Med Chem 45:2127-30. 2002..One of the analogues (compound 23) showed excellent in vivo activity in the inhibition of antibody production in mice and in the adjuvant induced arthritis model in rats...