Výsledky vyhledávání - "Diseroad Benjamin Alan"

Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1S,3R)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor

Publikováno v: Journal of Medicinal Chemistry. 62:8711-8732

Clinical development of catechol-based orthosteric agonists of the dopamine D1 receptor has thus far been unsuccessful due to multiple challenges. To address these issues, we identified LY3154207 (...

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::5a353395d3c6f7ca6dfa78c95a347dd4
https://doi.org/10.1021/acs.jmedchem.9b01234

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Synthesis and Pharmacological Characterization of C4β-Amide-Substituted 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1S,2S,4S,5R,6S)-2-Amino-4-[(3-methoxybenzoyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2794193), a Highly Potent and Selective mGlu3 Receptor Agonist

Publikováno v: Journal of Medicinal Chemistry. 61:2303-2328

Multiple therapeutic opportunities have been suggested for compounds capable of selective activation of metabotropic glutamate 3 (mGlu3) receptors, but small molecule tools are lacking. As part of our ongoing efforts to identify potent, selective, an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::34fd3a986aac486e41e6ea738f1a4465
https://doi.org/10.1021/acs.jmedchem.7b01481

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Discovery of LY3104607: A Potent and Selective G Protein-Coupled Receptor 40 (GPR40) Agonist with Optimized Pharmacokinetic Properties to Support Once Daily Oral Treatment in Patients with Type 2 Diabetes Mellitus

Publikováno v: Journal of medicinal chemistry. 61(3)

As a part of our program to identify potent GPR40 agonists capable of being dosed orally once daily in humans, we incorporated fused heterocycles into our recently disclosed spiropiperidine and tetrahydroquinoline acid derivatives 1, 2, and 3 with th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba33126a14f55ea8f6b1d4d12011e1a1
https://pubmed.ncbi.nlm.nih.gov/29236497

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A molecular picture of the problems in ensuring structural purity of tazofelone

Autor: Sreenivas R. Lingireddy, Suk-Fai Lau, Diseroad Benjamin Alan, Sarah L. Price, Jennifer A. McMahon, Louise S. Price, Susan M. Reutzel-Edens

Publikováno v: Journal of Molecular Structure. 1078:26-42

Almost twenty years after the crystal polymorphism of tazofelone was first studied at Lilly, the compound was revisited by calculating the crystal energy landscape and complementing the calculations with experimental work for calibration purposes. Th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e5219090b381e82e64746cfddb522fb
https://doi.org/10.1016/j.molstruc.2014.01.014

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Salt Disproportionation in the Solid State: Role of Solubility and Counterion Volatility

Autor: Diseroad Benjamin Alan, Raj Suryanarayanan, Gregory A. Stephenson, Naveen K. Thakral, Aktham Aburub, Timothy Andrew Woods, Jeffrey A. Peterson, Robert J. Behme

Publikováno v: Molecular pharmaceutics. 13(12)

Disproportionation propensity of salts (HCl, HBr, heminapadisylate) and adipic acid cocrystal of corticotropin releasing hormone receptor-1 antagonist was studied using model free kinetics. Using thermogravimetic weight loss profile or heat flow curv

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f4aef677085b85cb39b5161e8cabdf33
https://pubmed.ncbi.nlm.nih.gov/27766882

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Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8

Publikováno v: Journal of medicinal chemistry. 59(10)

Transmembrane AMPA receptor regulatory proteins (TARPs) are a family of scaffolding proteins that regulate AMPA receptor trafficking and function. TARP γ-8 is one member of this family and is highly expressed within the hippocampus relative to the c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::11f6a1cbca71f336baac901c8fde85e1
https://pubmed.ncbi.nlm.nih.gov/27067148

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Isolation, identification, and synthesis of two oxidative degradation products of olanzapine (LY170053) in solid oral formulations

Autor: Speakman Jeffrey Lynn, Gary G. Cooke, Steven R. Maple, Diseroad Benjamin Alan, Heiko Brunner, Charles Arthur Bunnell, Steven W. Baertschi, Patrick J. Jansen, Craig A. J. Kemp, Karen A. McCune, Douglas E. Dorman

Publikováno v: Journal of pharmaceutical sciences. 97(2)

Two impurities found in both stressed and aged solid-state formulations of olanzapine have been identified as (Z)-1,3-dihydro-4-(4-methyl-1-piperazinyl)-2-(2-oxopropylidene)-2H-1,5-benzodiazepin-2-one (1) and (Z)-1-[1,2-dihydro-4-(4-methyl-1-piperazi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8f84b9c49af627ae4359eb20fb124f37
https://pubmed.ncbi.nlm.nih.gov/17879984

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