P. Devasthale

发表

Carboxylic Acids and Lactones as HMG‐CoA Reductase Inhibitors

X. Ye, P. Devasthale, 2016 .

Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists.

Wei Wang, Jonathan Lippy, Arthur M Doweyko, 2009, Bioorganic & medicinal chemistry letters.

Synthesis and biological evaluation of novel pyrrolidine acid analogs as potent dual PPARα/γ agonists.

Weiqi Wang, A. Doweyko, T. Harrity, 2015, Bioorganic & medicinal chemistry letters.

Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.

Weiqi Wang, A. Doweyko, W. Humphreys, 2005, Journal of medicinal chemistry.

Discovery of tertiary aminoacids as dual PPARα/γ agonists-I

Wei Wang, Wei Sun, Zhengping Ma, 2007 .

The Dual Peroxisome Proliferator-Activated Receptor (cid:1) / (cid:2) Activator Muraglitazar Prevents the Natural Progression of Diabetes in db/db Mice

Simeon I. Taylor, E. Janovitz, E. Tozzo, 2007 .

Monoacylglycerol Acyltransferase 2 (MGAT2) Inhibitors for the Treatment of Metabolic Diseases and Nonalcoholic Steatohepatitis (NASH).

D. Cheng, P. Devasthale, 2018, Journal of medicinal chemistry.

Muraglitazar, a novel dual (alpha/gamma) peroxisome proliferator-activated receptor activator, improves diabetes and other metabolic abnormalities and preserves beta-cell function in db/db mice.

R. Gregg, W. Fenderson, Wen-pin Yang, 2006, Diabetes.

MGAT2 inhibitor decreases liver fibrosis and inflammation in murine NASH models and reduces body weight in human adults with obesity.

C. Chu, E. A. Brown, D. Gordon, 2022, Cell metabolism.

Synthesis Optimization, Scale-Up, and Catalyst Screening Efforts toward the MGAT2 Clinical Candidate, BMS-963272

Lidet K. Negash, A. Mathur, R. Lawrence, 2022, Organic Process Research & Development.

Generation of functional diversity via nitroaldol condensations of α-aminoacid aldehydes — A new and stereocontrolled route to acyclic 1,3-diamino-2-alcohols

S. Hanessian, P. Devasthale, 1996 .

7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site.

Wei Wang, C. Weigelt, K. Kish, 2011, Bioorganic & medicinal chemistry letters.

Chiral DNA gyrase inhibitors. 3. Probing the chiral preference of the active site of DNA gyrase. Synthesis of 10-fluoro-6-methyl-6,7-dihydro-9-piperazinyl- 2H-benzo[a]quinolizin-20-one-3-carboxylic acid analogues.

S. Pillai, L. Mitscher, R. Fecik, 2005, Journal of medicinal chemistry.

Structure-Activity Relationships of Fluoro-4-Quinolones

L. Mitscher, R. Zavod, P. Devasthale, 1990 .

Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778).

C. Weigelt, K. Kish, H. Klei, 2013, Journal of medicinal chemistry.

Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.

A. Doweyko, T. Harrity, Litao Zhang, 2008, Bioorganic & medicinal chemistry letters.

Dactylocyclines, novel tetracycline derivatives produced by a Dactylosporangium sp. III. Absolute stereochemistry of the dactylocyclines.

L. Mitscher, A. Tymiak, D. V. Vander Velde, 1992, The Journal of antibiotics.

Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders.

Kimberly A. Foster, C. Chu, A. Mathur, 2021, Journal of medicinal chemistry.

Design and synthesis of novel, pseudo C2 symmetric inhibitors of HIV protease

Stephen Hanessian, S. Hanessian, Pratik V. Devasthale, 1996 .

Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup.

R. Sridhar, D. Longhi, Christine S. Huang, 2015, Bioorganic & medicinal chemistry letters.

Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta.

Johan Malm, Howard Einspahr, Arthur M Doweyko, 2004, Bioorganic & medicinal chemistry letters.

Muraglitazar, a Novel Dual (α/γ) Peroxisome Proliferator–Activated Receptor Activator, Improves Diabetes and Other Metabolic Abnormalities and Preserves β-Cell Function in db/db Mice

Michael Cap, R. Gregg, W. Fenderson, 2006 .

The Dual Peroxisome Proliferator-Activated Receptor α/γ Activator Muraglitazar Prevents the Natural Progression of Diabetes in db/db Mice

Simeon I. Taylor, E. Janovitz, E. Tozzo, 2007, Journal of Pharmacology and Experimental Therapeutics.

The dual peroxisome proliferator-activated receptor alpha/gamma activator muraglitazar prevents the natural progression of diabetes in db/db mice.

Simeon I. Taylor, E. Janovitz, E. Tozzo, 2007, The Journal of pharmacology and experimental therapeutics.

Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453).

Wei Wang, Jun Li, Ying Wang, 2010, Journal of medicinal chemistry.

Synthesis of conformationally constrained potential inhibitors of mammalian metalloproteinases

Stephen Hanessian, S. Hanessian, Pratik V. Devasthale, 1997 .

Discovery of Novel Pyridinones as MGAT2 Inhibitors for the Treatment of Metabolic Disorders.

Kimberly A. Foster, C. Chu, A. Mathur, 2023, Bioorganic & Medicinal Chemistry Letters.

Identification of a nonbasic melanin hormone receptor 1 antagonist as an antiobesity clinical candidate.

J. Barrish, E. Janovitz, D. Longhi, 2014, Journal of medicinal chemistry.

Non-basic azolotriazinone MCHR1 antagonists for the treatment of obesity: An empirical brain-exposures-driven candidate selection for in vivo efficacy studies.

S. Radhakrishnan, D. Longhi, Christine S. Huang, 2015, Bioorganic & medicinal chemistry letters.

Discovery of 12 (BMS-986172) as a Highly Potent MGAT2 Inhibitor that Achieved Targeted Efficacious Exposures at a Low Human Dose for the Treatment of Metabolic Disorders.

Lidet K. Negash, Kimberly A. Foster, A. Mathur, 2023, Journal of medicinal chemistry.

Dactylocyclines: Novel Tetracycline Glycosides Active Against Tetracycline‐Resistant Bacteria.

J. S. Wells, N. Andersen, L. Mitscher, 1993 .