Discovery of evobrutinib: an oral, potent, and highly selective, covalent Bruton's tyrosine kinase (BTK) inhibitor for the treatment of immunological diseases

RD Caldwell, H Qiu, BC Askew, AT Bender, N Brugger… - 2019 - ACS Publications
Bruton’s tyrosine kinase (BTK) inhibitors such as ibrutinib hold a prominent role in the
treatment of B cell malignancies. However, further refinement is needed to this class of agents, …

Nonpeptide αvβ3 Antagonists. Part 11:  Discovery and Preclinical Evaluation of Potent αvβ3 Antagonists for the Prevention and Treatment of Osteoporosis

PJ Coleman, KM Brashear, BC Askew… - Journal of medicinal …, 2004 - ACS Publications
3-(S)-Pyrimidin-5-yl-9-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-nonanoic acid (5e) and 3-(S)-(methylpyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-nonanoic
acid (5f) were …

[HTML][HTML] Ocular distribution and pharmacodynamics of SF0166, a topically administered αvβ3 integrin antagonist, for the treatment of retinal diseases

BC Askew, T Furuya, DS Edwards - Journal of Pharmacology and …, 2018 - ASPET
SF0166, a small-molecule α v β 3 antagonist, has physiochemical properties that allow
distribution to the posterior segment of the eye after topical administration in an ophthalmic …

11β-Hydroxysteroid dehydrogenase-1 as a therapeutic target for metabolic diseases

C Fotsch, BC Askew, JJ Chen - Expert Opinion on Therapeutic …, 2005 - Taylor & Francis
11β-Hydroxysteroid dehydrogenase-1 (11βHSD1) is a therapeutic target for Type 2 diabetes
that has stimulated the interest of many pharmaceutical companies. Mounting evidence …

Non-peptide αvβ3 antagonists. Part 4: potent and orally bioavailable chain-shortened RGD mimetics

PJ Coleman, BC Askew, JH Hutchinson… - Bioorganic & medicinal …, 2002 - Elsevier
Potent non-peptidic α v β 3 antagonists have been prepared where deletion of an amide
bond from an earlier series of linear RGD-mimetics provides a novel series of chain-shortened …

Nonpeptide αvβ3 antagonists. Part 9: Improved pharmacokinetic profile through the use of an aliphatic, des-amide backbone

…, BC Askew, LT Duong, C Fernandez-Metzler… - Bioorganic & medicinal …, 2004 - Elsevier
A series of α v β 3 receptor antagonists lacking the amide bond of previously-reported ‘chain-shortened’
compounds is described. Replacement of the lone amide bond with two …

Non-Peptide αvβ3 antagonists. Part 3: Identification of potent RGD mimetics incorporating novel β-Amino acids as aspartic acid replacements

…, MJ Breslin, CA McVean, BC Askew… - Bioorganic & medicinal …, 2002 - Elsevier
Potent non-peptidic α v β 3 antagonists have been prepared incorporating various β-amino
acids as aspartic acid mimetics. Modification of the β-alanine 3-substituents alters the …

Nonpeptide glycoprotein IIb/IIIa inhibitors. 15. Antithrombotic efficacy of L-738,167, a long-acting GPIIb/IIIa antagonist, correlates with inhibition of adenosine …

…, MA Holahan, MT Stranieri, JD Glass, BC Askew… - … of Pharmacology and …, 1997 - ASPET
The nonpeptide platelet glycoprotein IIb/IIIa antagonist, L-738,167, was characterized in
dog and nonhuman primate. In an anesthetized canine model of coronary artery electrolytic …

Nonpeptide glycoprotein IIb/IIIa inhibitors: 14: oral antithrombotic efficacy of L-738,167 in a conscious canine model of coronary artery electrolytic injury.

…, AA Wallace, GL Stump, EL Hand, BC Askew… - Circulation, 1997 - europepmc.org
Background A conscious dog model of left circumflex coronary artery electrolytic injury was
used to assess the oral antithrombotic efficacy of L-738,167, a potent nonpeptide antagonist …

Disposition of L-738,167, a potent and long-acting fibrinogen receptor antagonist, in dogs: dose-dependent pharmacokinetics

…, LM Gorham, JA Naue, TG Hamill, BC Askew… - Drug metabolism and …, 1997 - ASPET
l-738,167 is a potent and long-acting fibrinogen receptor antagonist and may be useful for
treatment of chronic thrombotic occlusive disorders. The purposes of this study were to …