K. Quinn

发表

A formulation strategy for gamma secretase inhibitor ELND006, a BCS class II compound: development of a nanosuspension formulation with improved oral bioavailability and reduced food effects in dogs.

E. Merisko-Liversidge, G. Liversidge, G. Tonn, 2012, Journal of pharmaceutical sciences.

Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents.

H. Sham, N. Yao, T. Yednock, 2010, Bioorganic & medicinal chemistry letters.

Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.

R. Neitz, H. Sham, N. Yao, 2011, Bioorganic & medicinal chemistry letters.

Design, synthesis and optimization of bis-amide derivatives as CSF1R inhibitors.

A. K. Agarwal, C. Higgs, S. Bernales, 2017, Bioorganic & medicinal chemistry letters.

Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors.

R. Motter, M. Adler, H. Sham, 2013, Bioorganic & medicinal chemistry letters.

Highly selective c-Jun N-terminal kinase (JNK) 3 inhibitors with in vitro CNS-like pharmacokinetic properties II. Central core replacement.

R. Neitz, H. Sham, T. Yednock, 2011, Bioorganic & medicinal chemistry letters.

Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.

G. Tóth, R. Neitz, H. Sham, 2010, Bioorganic & medicinal chemistry letters.

Triazolopyridazine LRRK2 kinase inhibitors.

M. Adler, H. Sham, M. Franzini, 2013, Bioorganic & medicinal chemistry letters.

Novel cinnoline-based inhibitors of LRRK2 kinase activity.

R. Neitz, M. Adler, H. Sham, 2013, Bioorganic & medicinal chemistry letters.

Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.

G. Tóth, H. Sham, N. Yao, 2011, Bioorganic & medicinal chemistry letters.

Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors.

H. Sham, T. Yednock, M. Bova, 2009, Bioorganic & medicinal chemistry letters.

Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.

R. Motter, D. Kholodenko, H. Sham, 2010, Bioorganic & medicinal chemistry letters.

Functional gamma‐secretase inhibitors reduce beta‐amyloid peptide levels in brain

F. D. Miller, R. Motter, D. Kholodenko, 2000, Journal of neurochemistry.

Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors.

Devleena Shivakumar, J. Lindquist, D. T. Hung, 2016, Bioorganic & medicinal chemistry letters.

Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease

R. Motter, D. Kholodenko, R. Barbour, 2010, Alzheimer's Research & Therapy.

Chronic γ-secretase inhibition reduces amyloid plaque-associated instability of pre- and postsynaptic structures

Richard M. Page, T Bonhoeffer, T. Bonhoeffer, 2013, Molecular Psychiatry.

Dual Inhibition of Bruton’s Tyrosine Kinase and Phosphoinositide-3-Kinase p110δ as a Therapeutic Approach to Treat Non-Hodgkin’s B Cell Malignancies

Emma McCullagh, D. T. Hung, S. Bernales, 2017, The Journal of Pharmacology and Experimental Therapeutics.

Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.

John-Michael Sauer, Zhao Ren, Dean R Artis, 2011, Bioorganic & medicinal chemistry letters.

Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): metabolically stable γ-secretase Inhibitor

R. Motter, D. Kholodenko, H. Sham, 2013, Journal of medicinal chemistry.

Discovery of pyrazolopyrimidine derivatives as novel inhibitors of ataxia telangiectasia and rad3 related protein (ATR).

J. Lindquist, Manvendra Singh, A. Protter, 2017, Bioorganic & medicinal chemistry letters.

Bioactivation of sitaxentan in liver microsomes, hepatocytes, and expressed human P450s with characterization of the glutathione conjugate by liquid chromatography tandem mass spectrometry.

M. Svensson, G. Tonn, Shawn Gauby, 2013, Chemical research in toxicology.

Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.

H. Sham, L. Latimer, M. Bova, 2013, Bioorganic & medicinal chemistry letters.

Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region.

G. Tóth, H. Sham, N. Yao, 2010, Bioorganic & medicinal chemistry letters.

Effects of single and multiple dose oral administration of ELND006, a novel APP-selective gamma-secretase inhibitor, on amyloid-β concentrations in the brain and CSF of cynomolgus monkeys

R. Motter, D. Kholodenko, J. Sauer, 2010, Alzheimer's & Dementia.

APP-selective gamma secretase inhibitor ELND006 effects on brain parenchymal and vascular amyloid beta in the PDAPP mouse model of Alzheimer's disease

R. Motter, D. Kholodenko, K. Khan, 2010, Alzheimer's & Dementia.

Pharmacokinetic and pharmacodynamic investigation of ELND006, a novel APP-selective gamma-secretase inhibitor, on amyloid-β concentrations in the brain, CSF and plasma of multiple nonclinical species following oral administration

R. Motter, D. Kholodenko, K. Hu, 2010, Alzheimer's & Dementia.

Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: prime side chromane-containing inhibitors.

R. Neitz, M. Adler, H. Sham, 2012, Bioorganic & medicinal chemistry letters.

Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent γ-secretase inhibitors.

H. Sham, M. Bova, J. Sauer, 2011, Bioorganic & Medicinal Chemistry Letters.

Amino-caprolactam γ-secretase inhibitors showing potential for the treatment of Alzheimer's disease.

M. Bova, J. Sauer, G. Basi, 2011, Bioorganic & medicinal chemistry letters.

Development of ALZET® osmotic pump compatible solvent compositions to solubilize poorly soluble compounds for preclinical studies

K. Quinn, R. Gullapalli, E. Goldbach, 2012, Drug delivery.

Discovery of a potent, orally bioavailable pyrimidine VLA-4 antagonist effective in a sheep asthma model.

W. Dunn, L. Mutter, C. Vandevert, 2011, Bioorganic & Medicinal Chemistry Letters.

N-Bridged bicyclic sulfonamides as inhibitors of gamma-secretase.

H. Sham, M. Bova, J. Sauer, 2009, Bioorganic & medicinal chemistry letters.

Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors.

Devleena Shivakumar, J. Lindquist, S. Bernales, 2016, Bioorganic & medicinal chemistry letters.

R. Motter, D. Kholodenko, H. Sham, 2013, Journal of medicinal chemistry.

Novel cinnoline-based inhibitors of LRRK2 kinase activity.

M. Adler, H. Sham, M. Franzini, 2013, Bioorganic & medicinal chemistry letters.

JPET # 238022 1 Dual Inhibition of Bruton ’ s Tyrosine Kinase and Phosphoinositide-3-Kinase p 110 δ as a Therapeutic Approach to Treat Non-Hodgkin ’ s B cell Malignancies

Emma McCullagh, L. Delgado, R. Rai, 2017 .

Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents.

John-Michael Sauer, Gergely Toth, G. Tóth, 2009, Bioorganic & medicinal chemistry letters.

Discovery of Pyrazolopyrimidine Derivatives as Novel Dual Inhibitors of BTK and PI3Kδ.

Emma McCullagh, S. Bernales, Anamika Thakur, 2016, ACS medicinal chemistry letters.