Zobrazeno 1 - 10
of 58
pro vyhledávání: '"R. Mudra"'
Autor:
Kannan Thirunavukkarasu, Mark Chambers, Daniel R. Mudra, Michael Robert Wiley, Craig A. Swearingen, Lisa A. Adams, Timothy B. Durham, Jothirajah Marimuthu, C. Lin, James Lee Toth, Chin Liu
Publikováno v:
Journal of Medicinal Chemistry. 60:5933-5939
Aggrecanase-1 and -2 (ADAMTS-4 and ADAMTS-5) are zinc metalloproteases involved in the degradation of aggrecan in cartilage. Inhibitors could provide a means of altering the progression of osteoarthritis. We report the identification of 7 which had g
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b1aa6bde3d0801758aea530059c1a40
https://doi.org/10.1021/acs.jmedchem.7b00650
https://doi.org/10.1021/acs.jmedchem.7b00650
Autor:
Thomas James Beauchamp, Thomas J. Bleisch, Norman Earle Hughes, Daniel R. Mudra, Srinivasan Chandrasekhar, Bryan H. Norman, Hai Bui, Jim D. Durbin, Spencer B. Jones, Yen Dao, Kannan Thirunavukkarasu, Mark Chambers, Denis J. McCann, J.L. Oskins, Joseph Michael Gruber, Lance Allen Pfeifer, Craig A. Swearingen, Christopher John Rito, V. Joseph Klimkowski, C. Lin
Publikováno v:
ACS Medicinal Chemistry Letters. 7:857-861
In an effort to develop a novel therapeutic agent aimed at addressing the unmet need of patients with osteoarthritis pain, we set out to develop an inhibitor for autotaxin with excellent potency and physical properties to allow for the clinical inves
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::095ce4b285974ea117e2612b0b46c193
https://doi.org/10.1021/acsmedchemlett.6b00207
https://doi.org/10.1021/acsmedchemlett.6b00207
Autor:
Kannan Thirunavukkarasu, Mark Chambers, Daniel R. Mudra, Craig A. Swearingen, Lisa A. Adams, Jennifer M. Weller, P.G. Mitchell, Timothy B. Durham, Chin Liu, C. Lin, James Lee Toth, Michael Robert Wiley, Jothirajah Marimuthu
Publikováno v:
Journal of Medicinal Chemistry. 59:5810-5822
The development of reliable relationships between in vivo target engagement, pharmacodynamic activity, and efficacy in chronic disease models is beneficial for enabling hypothesis-driven drug discovery and facilitating the development of patient-focu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f252c22eeb38a66a724a46f915a1a225
https://doi.org/10.1021/acs.jmedchem.6b00398
https://doi.org/10.1021/acs.jmedchem.6b00398
Autor:
Daniel R. Mudra, Matthew J. Fisher, Maria-Jesus Blanco, Warshawsky Alan M, Xiao-Peng Yu, Tatiana Natali Vetman, Anita K. Harvey, Srinivasan Chandrasekhar, Xushan Wang, Kuklish Steven Lee, J.L. Oskins, Mark Chambers, C. Lin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:2303-2307
Continued SAR optimization of a series of 3-methylpyridine-2-carbonyl amino-2,4-dimethyl-benzoic acid led to the selection of compound 4f for clinical studies. Compound 4f showed an IC50 of 123nM for inhibition of PGE2-induced TNFα reduction in an e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::14c5fc831a41c4d4dae2d9bc322b91a3
https://doi.org/10.1016/j.bmcl.2016.03.041
https://doi.org/10.1016/j.bmcl.2016.03.041
Autor:
Srinivasan Chandrasekhar, Tatiana Natali Vetman, Xushan Wang, Anita K. Harvey, Matthew Allen Schiffler, Maria-Jesus Blanco, Xiao-Peng Yu, Warshawsky Alan M, Matthew J. Fisher, Daniel R. Mudra
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:105-109
A novel series of EP4 antagonists, based on a quinoline scaffold, has been discovered. Medicinal chemistry efforts to optimize the potency of the initial hit are described. A highly potent compound in a clinically relevant human whole blood assay was
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8005a33b12336736a42cb91a1af334d7
https://doi.org/10.1016/j.bmcl.2015.11.023
https://doi.org/10.1016/j.bmcl.2015.11.023
Tackling translational medicine with a focus on the drug discovery development-interface, this book integrates approaches and tactics from multiple disciplines, rather than just the pharmaceutical aspect of the field. The authors of each chapter addr
Autor:
Majid Vakilynejad, Arijit Chakravarty, Tonika Bohnert, Anu Shilpa Krishnatry, Jerome T. Mettetal, Tristan S. Maurer, Christopher R. Gibson, Daniel R. Mudra, Edgar Schuck, Yaming Su, Marjoleen J.M.A Nijsen, Tycho Heimbach, Shining Wang, Virna J A Schuck, Cheng-Pang Hsu, Harvey Wong, Patrick Trapa, Joseph Raybon, Patricia Schroeder, Satyendra Suryawanshi, Jing Lin, Bianca M. Liederer, Valeriu Damian-Iordache, Alice Tsai
Publikováno v:
The AAPS Journal. 17:462-473
The application of modeling and simulation techniques is increasingly common in preclinical stages of the drug discovery and development process. A survey focusing on preclinical pharmacokinetic/pharmacodynamics (PK/PD) analysis was conducted across
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::987c55984d67b4b816af57121c982893
https://doi.org/10.1208/s12248-014-9716-2
https://doi.org/10.1208/s12248-014-9716-2
Autor:
Bianca M. Liederer, Edgar Schuck, Daniel R. Mudra, Jing Lin, Patricia Schroeder, Fan Wu, Harvey Wong, Cheng-Pang Hsu, Anu Shilpa Krishnatry, Haiqing Wang, Jerome T. Mettetal, Tonika Bohnert, Christopher R. Gibson, Alice Tsai, Marjoleen J.M.A Nijsen, Qiang Lu, Valeriu Damian-Iordache, Satyendra Suryawanshi, Patrick Trapa
Publikováno v:
Drug discovery today. 22(10)
With inadequate efficacy being the primary cause for the attrition of drug candidates in clinical development, the need to better predict clinical efficacy earlier in the drug development process has increased in importance in the pharmaceutical indu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b75af1e43e6e3a51f39468fbc00dc204
https://pubmed.ncbi.nlm.nih.gov/28476536
https://pubmed.ncbi.nlm.nih.gov/28476536
Publikováno v:
Translating Molecules into Medicines ISBN: 9783319500409
Drug discovery requires the convergence of molecular attributes including magnitude and duration of exposure, tissue distribution, target engagement, and pharmacological action. To this end, during lead optimization, discovery scientists must leverag
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::21af9e38b0830e72eba559e1e11e471c
https://doi.org/10.1007/978-3-319-50042-3_6
https://doi.org/10.1007/978-3-319-50042-3_6
Publikováno v:
AAPS Advances in the Pharmaceutical Sciences Series ISBN: 9783319500409
Translating Molecules into Medicines
Translating Molecules into Medicines
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d9503f5cdd20f18b5255c82a24474927
https://doi.org/10.1007/978-3-319-50042-3
https://doi.org/10.1007/978-3-319-50042-3