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Novel L-xylose derivatives as selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.

• Nicole C Goodwin, Ross Mabon, +14 authors David B. Rawlins
• Journal of medicinal chemistry
• 2009

The prevalence of diabetes throughout the world continues to increase and has become a major health issue. Recently there have been several reports of inhibitors directed toward the sodium-dependent… (More)

Gamma Secretase Modulators: New Alzheimer's Drugs on the Horizon?

• Matthew G Bursavich, Bryce A Harrison, Jean-François Blain
• Journal of medicinal chemistry
• 2016

The rapidly aging population desperately requires new therapies for Alzheimer's disease. Despite years of pharmaceutical research, limited clinical success has been realized, with several failed… (More)

Novel class of LIM-kinase 2 inhibitors for the treatment of ocular hypertension and associated glaucoma.

• Bryce A Harrison, N. Andrew Whitlock, +22 authors David B. Rawlins
• Journal of medicinal chemistry
• 2009

The discovery of a pyrrolopyrimidine class of LIM-kinase 2 (LIMK2) inhibitors is reported. These LIMK2 inhibitors show good potency in enzymatic and cellular assays and good selectivity against ROCK.… (More)

Discovery of LX2761, a Sodium-Dependent Glucose Cotransporter 1 (SGLT1) Inhibitor Restricted to the Intestinal Lumen, for the Treatment of Diabetes.

• Nicole C Goodwin, Zhi-Ming Ding, +16 authors David B. Rawlins
• Journal of medicinal chemistry
• 2017

The increasing number of people afflicted with diabetes throughout the world is a major health issue. Inhibitors of the sodium-dependent glucose cotransporters (SGLT) have appeared as viable… (More)

Decreased intraocular pressure in mice following either pharmacological or genetic inhibition of ROCK.

• N. Andrew Whitlock, Bryce A Harrison, +6 authors Dennis S. Rice
• Journal of ocular pharmacology and therapeutics…
• 2009

PURPOSE Goals of this study were to determine if pharmacological or genetic inhibition of Rho-associated coiled coil containing protein kinases (known as ROCK1 and ROCK2) alters intraocular pressure… (More)

Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma.

• Bryce A Harrison, Zheng Y Almstead, +18 authors David B. Rawlins
• ACS medicinal chemistry letters
• 2015

The structure of LX7101, a dual LIM-kinase and ROCK inhibitor for the treatment of ocular hypertension and associated glaucoma, is disclosed. Previously reported LIM kinase inhibitors suffered from… (More)

Characterization of FRM-36143 as a new γ-secretase modulator for the potential treatment of familial Alzheimer’s disease

• Jean-François Blain, Matthew G Bursavich, +13 authors Gerhard König
• Alzheimer's Research & Therapy
• 2016

Familial Alzheimer’s disease (FAD) is caused by mutations in the amyloid precursor protein (APP) or presenilin (PS). Most PS mutations, which account for the majority of FAD cases, lead to an… (More)

LX2761, a Sodium/Glucose Cotransporter 1 Inhibitor Restricted to the Intestine, Improves Glycemic Control in Mice.

• David R. Powell, Melinda G Smith, +16 authors Zhi-Ming Ding
• The Journal of pharmacology and experimental…
• 2017

LX2761 is a potent sodium/glucose cotransporter 1 inhibitor restricted to the intestinal lumen after oral administration. Studies presented here evaluated the effect of orally administered LX2761 on… (More)

Design, Synthesis, and Evaluation of a Novel Series of Oxadiazine Gamma Secretase Modulators for Familial Alzheimer's Disease.

• Matthew G Bursavich, Bryce A Harrison, +15 authors Duane A Burnett
• Journal of medicinal chemistry
• 2017

Herein we describe the design, synthesis, and evaluation of a novel series of oxadiazine-based gamma secretase modulators obtained via isosteric amide replacement and critical consideration of… (More)

LP-925219 maximizes urinary glucose excretion in mice by inhibiting both renal SGLT1 and SGLT2

• David R. Powell, Melinda G Smith, +13 authors Zhi-Ming Ding
• Pharmacology research & perspectives
• 2015

Sodium-glucose cotransporter 2 (SGLT2) inhibitors are a new class of oral anti-diabetic agents that improve glycemic control by inhibiting SGLT2-mediated renal glucose reabsorption. Currently… (More)

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