Zobrazeno 1 - 10
of 36
pro vyhledávání: '"Klaas Schildknegt"'
Autor:
Angela C. Doran, Peter Lockwood, Thomas A. Comery, R. Scott Obach, Aarti Sawant-Basak, Hongying Gao, Jessica Mancuso, Susanna Tse, Klaas Schildknegt
Publikováno v:
Drug Metabolism and Disposition. 46:934-942
SAM-760 [(2-methyl-1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-benzo[d]imidazole)], a 5HT6 antagonist, was investigated in humans for the treatment of Alzheimer's disease. In liver microsomes and recombinant cytochrome P450 (P450) isozymes, SAM-760 was
Autor:
Klaas Schildknegt, Eric Fluhler, Lloyd Stevens, Eric Woolf, Alfin D. N. Vaz, Haihong Shi, Steven G. Terra, Dimitris Papadopoulos, Vaishali Sahasrabudhe, Didier Saur, Daniel Gaunt, Kyle Matschke, Robert J. Fountaine, Susan Zhou, David L. Cutler, Ernesto Callegari, Sangeeta Raje, Christine Alvey
Publikováno v:
Clinical and Translational Science. 11:405-411
Ertugliflozin, a sodium glucose cotransporter-2 inhibitor, is approved in the United States for treatment of type 2 diabetes mellitus. A novel two-period study design with 14 C microtracer dosing in each period was used to determine absolute oral bio
Autor:
Angela C. Doran, Cheng Chang, Shenping Liu, Butler Todd W, Travis T. Wager, Klaas Schildknegt, Lei Zhang, Michael Marconi, Jianke Li, Scot Richard Mente, Katherine Fisher, Ramalakshmi Yegna Chandrasekaran, Joseph R. Hedde, Sarah Grimwood, Chakrapani Subramanyam, Paul Galatsis
Publikováno v:
ACS Chemical Neuroscience. 8:1995-2004
To enable the clinical development of our CNS casein kinase 1 delta/epsilon (CK1δ/e) inhibitor project, we investigated the possibility of developing a CNS positron emission tomography (PET) radioligand. For this effort, we focused our design and sy
Autor:
Christopher Ryan Butler, Timothy J. McCarthy, Ryosuke Arakawa, Deborah L. Smith, Klaas Schildknegt, Justin R. Piro, Lei Zhang, Kevin P. Maresca, Laura A. McAllister, Deane M. Nason, Zhisheng Jia, Sangram Nag, Akihiro Takano, Tarek A. Samad, Christer Halldin, Anabella Villalobos, Steven Victor O'neil, Patrick Trapa
Publikováno v:
Journal of medicinal chemistry. 62(18)
Monoacylglycerol lipase (MAGL), a serine hydrolase extensively expressed throughout the brain, serves as a key gatekeeper regulating the tone of endocannabinoid signaling. Preclinically, inhibition of MAGL is known to provide therapeutic benefits for
Autor:
John F. Traverse, Thomas Raglione, Anthony R. Haight, Scott A. Miller, Brad D. Maxwell, Klaas Schildknegt, Charles S. Elmore, Boris A. Czeskis, Peng Wang, David Hesk
Publikováno v:
Journal of labelled compoundsradiopharmaceuticalsREFERENCES. 62(11)
The International Consortium for Innovation & Quality (IQ) in Pharmaceutical Development recently established a working group focused on the development of a guidance to address Deuterated Active Pharmaceutical Ingredients. Deuteration of an Active P
Autor:
Charles E. Nolan, Christer Halldin, Anabella Villalobos, Kelly R. Bales, Klaas Schildknegt, Ryosuke Arakawa, Akihiro Takano, Lorraine F. Lanyon, Leanne M. Buzon, Shawn D. Doran, Nahid Amini, Laigao Chen, Brian T. O’Neill, Michael Aaron Brodney, Elizabeth Mary Beck, Lei Zhang, Timothy J. McCarthy, Sangram Nag, Jason K. Dutra
Publikováno v:
Journal of medicinal chemistry. 61(8)
Alzheimer’s disease (AD) is characterized by accumulation of β-amyloid (Aβ) plaques and neurofibrillary tau tangles in the brain. β-Site amyloid precursor protein cleaving enzyme 1 (BACE1) plays a key role in the generation of Aβ fragments via
Autor:
Aarti, Sawant-Basak, R Scott, Obach, Angela, Doran, Peter, Lockwood, Klaas, Schildknegt, Hongying, Gao, Jessica, Mancuso, Susanna, Tse, Thomas A, Comery
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 46(7)
SAM-760 [(2-methyl-1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-benzo[d]imidazole)], a 5HT
Autor:
Frank Loganzo, Klaas Schildknegt, Sujiet Puthenveetil, Birte Nolting, Andrew J. Bessire, T. Eric Ballard, Lee R. Roberts, My-Hanh Lam, Chakrapani Subramanyam, Michael Eric Green, Betsy Pierce, Manoj Charati, Justin Cohen
Publikováno v:
Bioconjugate chemistry. 27(7)
Antibody-drug conjugates (ADC) are currently an active area of research, focused primarily on oncology therapeutics, but also to a limited extent on other areas such as infectious disease. The success of this type of targeted drug delivery is depende
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 55:166-170
β-amino acids 1 and 2 are α2δ agonists, which were developed for the treatment of generalized anxiety disorder and insomnia. The stable and radioactive isotope-labeled β-amino acids were required to support pre-clinical and clinical studies. Asym
Autor:
Stephanie L. Coffing, Victor F. Soliman, Evan Smith, Richard V. Coelho, Jiri Aubrecht, Klaas Schildknegt, Jennifer R. Cheung, Mary E. Lame, Tristan S. Maurer, Phoebe Chiang, Deepak Dalvie, Chandra Vage, Amit S. Kalgutkar, Kim F. McClure
Publikováno v:
Drug Metabolism and Disposition. 35:848-858
2-(3-Chlorobenzyloxy)-6-(piperazin-1-yl)pyrazine (3) is a potent and selective 5-HT(2C) agonist that exhibits dose-dependent inhibition of food intake and reduction in body weight in rats, making it an attractive candidate for treatment of obesity. H