David A. Mareska
Amgen
22 Papers
401 Citations
David A. Mareska is an academic researcher from Amgen. The author has contributed to research in topics: Cancer & Carboxamide. The author has an hindex of 8, co-authored 21 publications.
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Papers
Patent
P38 inhibitors and methods of use thereof
Mark Munson,David A. Mareska,Youngboo Kim,Robert D. Groneberg,James P. Rizzi,Martha Rodriguez,Ganghyeok Kim,Guy Vigers,Chang Rao,Devan Balachari,Darren Harvey +10 more
- 25 Feb 2004
TL;DR: In this article, an invention related to inhibitors of p38, and methods for producing these inhibitors are described. And pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders mediated by p38 are provided.
326
Potent nonpeptide antagonists of the bradykinin B1 receptor: structure-activity relationship studies with novel diaminochroman carboxamides.
Kaustav Biswas,Aiwen Li,Jian J. Chen,Derin C. D'amico,Christopher H. Fotsch,Nianhe Han,Jason Brooks Human,Qingyian Liu,Mark H. Norman,Bobby Riahi,Chester Chenguang Yuan,Hideo Suzuki,David A. Mareska,James Zhan,David E. Clarke,Andras Toro,Robert D. Groneberg,Burgess Laurence E,Dianna Lester-Zeiner,Gloria Biddlecome,Barton H. Manning,Leyla Arik,Hong Dong,Ming Huang,Augustus Kamassah,Richard Loeloff,Hong Sun,Feng-Yin Hsieh,Gondi N. Kumar,Gordon Ng,Randall W. Hungate,Benny C. Askew,Eileen Johnson +32 more
TL;DR: The most potent analog at the human receptor, compound 38, was also active in a rabbit B1 receptor cellular assay and displayed in vivo activity in two rabbit models, a pharmacodynamic model with a blood pressure readout and an efficacy model of inflammatory pain.
28
Identification of a Nonpeptidic and Conformationally Restricted Bradykinin B1 Receptor Antagonist with Anti-Inflammatory Activity
Derin C. D'amico,Toshi Aya,Jason Brooks Human,Christopher H. Fotsch,Jian J. Chen,Kaustav Biswas,Bobby Riahi,Mark H. Norman,Christopher A. Willoughby,Randall W. Hungate,Paul J. Reider,Gloria Biddlecome,Dianna Lester-Zeiner,Carlo van Staden,Eileen Johnson,Augustus Kamassah,Leyla Arik,Judy Wang,Vellarkad N. Viswanadhan,Robert D. Groneberg,James Zhan,Hideo Suzuki,Andras Toro,David A. Mareska,David E. Clarke,Darren Martin Harvey,Burgess Laurence E,Laird Ellen,Benny C. Askew,Gordon Ng +29 more
TL;DR: The discovery of chroman 28, a potent and selective antagonist of human, nonhuman primate, rat, and rabbit bradykinin B1 receptors, is reported and a novel method to calculate entropy is introduced and ascribed approximately 30% of the gained affinity to decreased conformational entropy.
27
Patent
Piperidine-containing compounds and use thereof
Martha E. Rodriguez,David A. Mareska,Jeremy J. Hans,Darren Harvey,Robert D. Groneberg,Michael O'sullivan +5 more
- 07 Jan 2010
TL;DR: A method for preventing and/or treating a metabolic disease, cerebrovascular disease, etc. which comprises administering to a mammal an effective amount of the compound of the formula (I) wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof has an anti-diabetic effect and a neuroprotective effect as discussed by the authors.
23
A new class of bradykinin 1 receptor antagonists containing the piperidine acetic acid tetralin core.
Christopher H. Fotsch,Gloria Biddlecome,Kaustav Biswas,Jian Jeff Chen,Derin C. D'amico,Robert D. Groneberg,Nianhe Bruce Han,Feng-Yin Hsieh,Augustus Kamassah,Gondi N. Kumar,Dianna Lester-Zeiner,Qingyian Liu,David A. Mareska,Babak Riahi,Yueh-Ju Judy Wang,Kevin Yang,James Zhan,Joe Zhu,Eileen Johnson,Gordon Ng,Benny C. Askew +20 more
TL;DR: A new class of B1 receptor antagonists that contain the piperidine acetic acid tetralin core are described, and one of these compounds shows modest oral bioavailability in rats.
22