1, 2, 3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors

…, TS Angeles, SX Yang, MS Albom, LD Aimone… - Bioorganic & medicinal …, 2007 - Elsevier
KDR kinase inhibition is considered to play an important role in regulating angiogenesis,
which is vital for the survival and proliferation of tumor cells. Recently we disclosed a structure-…

Stimulation-produced descending inhibition from the periaqueductal gray and nucleus raphe magnus in the rat: mediation by spinal monoamines but not opioids

LD Aimone, SL Jones, GF Gebhart - Pain, 1987 - journals.lww.com
: Focal electrical stimulation in the midbrain periaqueductal gray (PAG) or medullary nucleus
raphe magnus (NRM) inhibits spinal nociceptive transmission and nociceptive reflexes. The …

Discovery of clinical candidate CEP-37440, a selective inhibitor of focal adhesion kinase (FAK) and anaplastic lymphoma kinase (ALK)

…, K Wells-Knecht, Z Huang, LD Aimone… - Journal of medicinal …, 2016 - ACS Publications
Analogues structurally related to anaplastic lymphoma kinase (ALK) inhibitor 1 were optimized
for metabolic stability. The results from this endeavor not only led to improved metabolic …

Stimulation-produced spinal inhibition from the midbrain in the rat is mediated by an excitatory amino acid neurotransmitter in the medial medulla

LD Aimone, GF Gebhart - Journal of Neuroscience, 1986 - Soc Neuroscience
LD Aimone and GF Gebhart … Correspondence should be addressed to LD Aimone at the
above address. … also is unable to block SPA from the PAG (Aimone et al., 1986). Thus, naloxone’…

A Selective, Orally Bioavailable 1,2,4-Triazolo[1,5-a]pyridine-Based Inhibitor of Janus Kinase 2 for Use in Anticancer Therapy: Discovery of CEP-33779

…, MS Albom, JL Mason, LD Aimone… - Journal of medicinal …, 2012 - ACS Publications
Members of the JAK family of nonreceptor tyrosine kinases play a critical role in the growth
and progression of many cancers and in inflammatory diseases. JAK2 has emerged as a …

Discovery and Characterization of 6-{4-[3-(R)-2-Methylpyrrolidin-1-yl) propoxy] phenyl}-2 H-pyridazin-3-one (CEP-26401, Irdabisant): A Potent, Selective Histamine …

…, M Tao, JR Mathiasen, LD Aimone… - Journal of medicinal …, 2011 - ACS Publications
Optimization of a novel series of pyridazin-3-one histamine H 3 receptor (H 3 R) antagonists/inverse
agonists identified 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-…

CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers

…, W Wan, MS Albom, TS Angeles, LD Aimone… - Molecular cancer …, 2012 - AACR
Anaplastic lymphoma kinase (ALK) is constitutively activated in a number of human cancer
types due to chromosomal translocations, point mutations, and gene amplification and has …

A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: Structure− activity relationships for a series of 9-alkoxymethyl-12-(3 …

…, DR Reddy, MA Iqbal, J Singh, LD Aimone… - Journal of medicinal …, 2003 - ACS Publications
A series of potent vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase
inhibitors from a new indenopyrrolocarbazole template is reported. The structure−activity …

Brain-stem relays mediating stimulation-produced antinociception from the lateral hypothalamus in the rat

LD Aimone, CA Bauer, GF Gebhart - Journal of Neuroscience, 1988 - Soc Neuroscience
Several lines of evidence have demonstrated a role for the lateral hypothalamus (LH) in an
endogenous system of descending inhibition. The present study, in rats lightly anesthetized …

Opioid modulation of capsaicin-evoked release of substance P from rat spinal cord in vivo

LD Aimone, TL Yaksh - Peptides, 1989 - Elsevier
Capsaicin has been shown to evoke the release of substance P (SP) from small diameter
primary afferent fibers. Using an in vivo perfusion of the rat spinal cord, this study examined the …