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MLi-2, a Potent, Selective, and Centrally Active Compound for Exploring the Therapeutic Potential and Safety of LRRK2 Kinase Inhibition

The Journal of pharmacology and experimental therapeutics, 2015-12, Vol.355 (3), p.397-409

2015

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fMRI study of olfactory processing in mice under three anesthesia protocols: Insight into the effect of ketamine on olfactory processing

NeuroImage (Orlando, Fla.), 2020-06, Vol.213, p.116725-116725, Article 116725

2020

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The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients

Science translational medicine, 2016-11, Vol.8 (363), p.363ra150

2016

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Increased seizure threshold and severity in young transgenic CRND8 mice

Neuroscience letters, 2004-09, Vol.367 (2), p.164-167

2004

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Discovery of a 3‑(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity

Journal of medicinal chemistry, 2017-04, Vol.60 (7), p.2983-2992

2017

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Pharmacological BACE Inhibition Improves Axonal Regeneration in Nerve Injury and Disease Models

Neurotherapeutics, 2020-07, Vol.17 (3), p.973-988

2020

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Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors

Bioorganic & medicinal chemistry letters, 2022-01, Vol.56, p.128463-128463, Article 128463

2022

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Chronic Verubecestat Treatment Suppresses Amyloid Accumulation in Advanced Aged Tg2576-AβPPswe Mice Without Inducing Microhemorrhage

Journal of Alzheimer's disease, 2017-01, Vol.59 (4), p.1393-1413

2017

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MitoPark mice, an animal model of Parkinson's disease, show enhanced prepulse inhibition of acoustic startle and no loss of gating in response to the adenosine A(2A) antagonist SCH 412348

Psychopharmacology, 2014-04, Vol.231 (7), p.1325-1337

2014

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Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor

Bioorganic & medicinal chemistry letters, 2012-04, Vol.22 (7), p.2444-2449

2012

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In Vivo Characterization of a Novel γ-Secretase Inhibitor SCH 697466 in Rodents and Investigation of Strategies for Managing Notch-Related Side Effects

Interdisciplinary perspectives on infectious diseases, 2013, Vol.2013 (2013), p.1-14

2013

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Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS Aβ Reduction

ACS medicinal chemistry letters, 2012-11, Vol.3 (11), p.897-902

2012

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Discovery of a Tetrahydrobenzisoxazole Series of γ‑Secretase Modulators

ACS medicinal chemistry letters, 2017-10, Vol.8 (10), p.1002-1006

2017

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Design and synthesis of water soluble β-aminosulfone analogues of SCH 900229 as γ-secretase inhibitors

Bioorganic & medicinal chemistry letters, 2016-12, Vol.26 (23), p.5836-5841

2016

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In Vivo Characterization of a Novel -Secretase Inhibitor SCH 697466 in Rodents and Investigation of Strategies for Managing Notch-Related Side Effects

International journal of alzheimer's disease, 2013, Vol.2013, p.1-14

2013

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Structure activity relationship studies of tricyclic bispyran sulfone γ-secretase inhibitors

Bioorganic & medicinal chemistry letters, 2013-02, Vol.23 (3), p.844-849

2013

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The anxiolytic-like profile of the nociceptin receptor agonist, endo-8-[bis(2-chlorophenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octane-3-carboxamide (SCH 655842): Comparison of efficacy and side effects across rodent species

European journal of pharmacology, 2011-07, Vol.661 (1), p.63-71

2011

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Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active γ-secretase inhibitors

Bioorganic & medicinal chemistry, 2008-01, Vol.18 (1), p.215-219

2008

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Characterization of the selective mGluR1 antagonist, JNJ16259685, in rodent models of movement and coordination

Pharmacology, biochemistry and behavior, 2011-04, Vol.98 (2), p.181-187

2011

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Age-progressing cognitive impairments and neuropathology in transgenic CRND8 mice

Behavioural brain research, 2005-05, Vol.160 (2), p.344-355

2005

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Ts65Dn mice, a model for Down syndrome, have deficits in context discrimination learning suggesting impaired hippocampal function

Behavioural brain research, 2001-01, Vol.118 (1), p.53-60

2001

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Age-Related Deficits in Context Discrimination Learning in Ts65Dn Mice That Model Down Syndrome and Alzheimer's Disease

Behavioral neuroscience, 2001-12, Vol.115 (6), p.1239-1246

2001

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Novel orally active morpholine N-arylsulfonamides γ-secretase inhibitors with low CYP 3A4 liability

Bioorganic & medicinal chemistry letters, 2009-11, Vol.19 (21), p.6032-6037

2009

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MLi-2, a Potent, Selective, and Centrally Active Compound for Exploring the Therapeutic Potential and Safety of LRRK2 Kinase Inhibition

fMRI study of olfactory processing in mice under three anesthesia protocols: Insight into the effect of ketamine on olfactory processing

The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients

Increased seizure threshold and severity in young transgenic CRND8 mice

Discovery of the 3‑Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)–A β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer’s Disease

Discovery of a 3‑(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity

Pharmacological BACE Inhibition Improves Axonal Regeneration in Nerve Injury and Disease Models

Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors

Chronic Verubecestat Treatment Suppresses Amyloid Accumulation in Advanced Aged Tg2576-AβPPswe Mice Without Inducing Microhemorrhage

MitoPark mice, an animal model of Parkinson's disease, show enhanced prepulse inhibition of acoustic startle and no loss of gating in response to the adenosine A(2A) antagonist SCH 412348

Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor

Structure-Based Design of an Iminoheterocyclic β‑Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates

In Vivo Characterization of a Novel γ-Secretase Inhibitor SCH 697466 in Rodents and Investigation of Strategies for Managing Notch-Related Side Effects

Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS Aβ Reduction

Discovery of a Tetrahydrobenzisoxazole Series of γ‑Secretase Modulators

Design and synthesis of water soluble β-aminosulfone analogues of SCH 900229 as γ-secretase inhibitors

In Vivo Characterization of a Novel -Secretase Inhibitor SCH 697466 in Rodents and Investigation of Strategies for Managing Notch-Related Side Effects

Structure activity relationship studies of tricyclic bispyran sulfone γ-secretase inhibitors

The anxiolytic-like profile of the nociceptin receptor agonist, endo-8-[bis(2-chlorophenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octane-3-carboxamide (SCH 655842): Comparison of efficacy and side effects across rodent species

Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active γ-secretase inhibitors

Characterization of the selective mGluR1 antagonist, JNJ16259685, in rodent models of movement and coordination

Age-progressing cognitive impairments and neuropathology in transgenic CRND8 mice

Ts65Dn mice, a model for Down syndrome, have deficits in context discrimination learning suggesting impaired hippocampal function

Age-Related Deficits in Context Discrimination Learning in Ts65Dn Mice That Model Down Syndrome and Alzheimer's Disease

Novel orally active morpholine N-arylsulfonamides γ-secretase inhibitors with low CYP 3A4 liability

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