Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Kia Sepassi"'
Publikováno v:
Pharmaceutics, Vol 15, Iss 7, p 1909 (2023)
Dissolution limitations to oral absorption can occur if the time required for dissolution is longer than the transit time across the small intestine and/or if dissolution is slower than the drug’s permeation through the gut wall. These limitations
Externí odkaz:
https://doaj.org/article/f6ffb8b65cfb4371bf4d03ce21b50a2a
Publikováno v:
Pharmaceutics; Volume 15; Issue 7; Pages: 1909
Dissolution limitations to oral absorption can occur if the time required for dissolution is longer than the transit time across the small intestine and/or if dissolution is slower than the drug’s permeation through the gut wall. These limitations
Autor:
Mark S. Tichenor, John J. M. Wiener, Navin L. Rao, Genesis M. Bacani, Jianmei Wei, Charlotte Pooley Deckhut, J. Kent Barbay, Kevin D. Kreutter, Leon Chang, Kathleen W. Clancy, Heather E. Murrey, Weixue Wang, Kay Ahn, Michael Huber, Elizabeth Rex, Kevin J. Coe, Jiejun Wu, Haopeng Rui, Kia Sepassi, Marcello Gaudiano, Mariette Bekkers, Ivo Cornelissen, Kathryn Packman, Mark Seierstad, Christos Xiouras, Scott D. Bembenek, Richard Alexander, Cynthia Milligan, Sriram Balasubramanian, Alec D. Lebsack, Jennifer D. Venable, Ulrike Philippar, James P. Edwards, Gavin Hirst
Publikováno v:
Journal of Medicinal Chemistry. 65:14326-14336
Bruton's tyrosine kinase (BTK) is a Tec family kinase that plays an essential role in B-cell receptor (BCR) signaling as well as Fcγ receptor signaling in leukocytes. Pharmacological inhibition of BTK has been shown to be effective in treating hemat
Autor:
Alexandra S Needham, Akinola Soyode-Johnson, Kevin J. Coe, Bartosz Balana, Freddy Schoetens, Xiaohui Jiang, Daniel J. Pippel, Kia Sepassi, Chungfang Xia, Stenne Brice M, Brian Scott, Leslie Nguyen, Tatiana Koudriakova, Christa C. Chrovian, Brian Lord, Michael A. Letavic, Jeffrey Schoellerman
Publikováno v:
Journal of Medicinal Chemistry. 63:9181-9196
Selective inhibitors of the GluN2B subunit of N-methyl-d-aspartate receptors in the ionotropic glutamate receptor superfamily have been targeted for the treatment of mood disorders. We sought to identify structurally novel, brain penetrant, GluN2B-se
Autor:
Kia Sepassi, Xiahou Deng, Brad M. Savall, Wall Jessica L, Nicholas I. Carruthers, Hong Ao, Anindya Bhattacharya, Brian Lord, Michael A. Letavic, Tatiana Koudriakova, Kevin J. Coe, Anita Everson, Freddy Schoetens, Devin M. Swanson, Meri De Angelis, Brian Scott, Timothy W. Lovenberg, Jason C. Rech, Judith Skaptason, Qi Wang
Publikováno v:
Journal of Medicinal Chemistry. 59:8535-8548
The synthesis and SAR of a series of 4,5,6,7-tetrahydro-imidazo[4,5-c]pyridine P2X7 antagonists are described. Addressing P2X7 affinity and liver microsomal stability issues encountered with this template afforded methyl substituted 4,5,6,7-tetrahydr
Autor:
Brian Lord, Brian Scott, Kia Sepassi, Akinola Soyode-Johnson, Anindya Bhattacharya, Alexander A. Peterson, Nicholas I. Carruthers, Leah Aluisio, Tatiana Koudriakova, Freddy Schoetens, Christa C. Chrovian, Curt A. Dvorak, David J. Gallacher, Christine F. Gelin, Xiaohu Deng, Michael A. Letavic, Ian Fraser, Kevin J. Coe
Publikováno v:
Journal of medicinal chemistry. 61(1)
A single pot dipolar cycloaddition reaction/Cope elimination sequence was developed to access novel 1,4,6,7-tetrahydro-5H-[1,2,3]triazolo[4,5-c]pyridine P2X7 antagonists that contain a synthetically challenging chiral center. The structure–activity
Autor:
Michael P. Maher, Sandra R. Chaplan, Jing Liu, Jason C. Rech, Brian Scott, William A. Eckert, Bryan James Branstetter, Hong Ao, Anne E. Fitzgerald, Yi Liu, Nyantsz Wu, Michele C. Rizzolio, Anindya Bhattacharya, Jamie M. Freedman, Alec D. Lebsack, Nadia Swanson, J. Guy Breitenbucher, Dong H. Li, Alan D. Wickenden, Kia Sepassi, Mena Kansagara
Publikováno v:
European Journal of Pharmacology. 663:40-50
As an integrator of multiple nociceptive and/or inflammatory stimuli, TRPV1 is an attractive therapeutic target for the treatment of various painful disorders. Several TRPV1 antagonists have been advanced into clinical trials and the initial observat
Autor:
Pascal Bonaventure, Anita M. Everson, S. Timothy Motley, Brian Lord, Jonathan Shelton, Raymond Rynberg, Ian Fraser, Christine Dugovic, Diane Nepomuceno, Leah Aluisio, Michael A. Letavic, John M. Keith, Perry Leung, Michele C. Rizzolio, John R. Atack, Tatiana Koudriakova, Kia Sepassi, Timothy W. Lovenberg, Mark A. Feinstein, Kiev S. Ly, Nicholas I. Carruthers, Kirsten L. Morton, Xiaohui Jiang, Kenway Hoey
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4210-4214
The pre-clinical characterization of novel aryloxypyridine amides that are histamine H(3) receptor antagonists is described. These compounds are high affinity histamine H(3) ligands that penetrate the CNS and occupy the histamine H(3) receptor in rat
Autor:
Philip J. Kuehl, Gang Yang, Samuel H. Yalkowsky, Kia Sepassi, Kelly L. Karlage, Parijat Jain, Tim Brenner, Paul B. Myrdal, Michael Mayersohn
Publikováno v:
Journal of Pharmaceutical Sciences. 97:5222-5228
The objective of these studies was to examine the in vivo performance of oral formulations of chlorpropham (CIPC). In order to develop a new oral formulation several different solubilization techniques were evaluated, namely: cosolvents, surfactants,
Autor:
Kia Sepassi, Samuel H. Yalkowsky
Publikováno v:
Industrial & Engineering Chemistry Research. 46:2220-2223
The octanol−air partition coefficient is commonly used to understand the extent of chemical partitioning between the atmosphere and organic matter in the environment. In this study, octanol−air partition coefficients were estimated by generating