R
Roger M. Freidinger
Researcher at United States Military Academy
Publications - 144
Citations - 6078
Roger M. Freidinger is an academic researcher from United States Military Academy. The author has contributed to research in topics: Receptor & Cholecystokinin. The author has an hindex of 38, co-authored 144 publications receiving 5882 citations. Previous affiliations of Roger M. Freidinger include Merck & Co..
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Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists
Ben E. Evans,Kenneth E. Rittle,Mark G. Bock,Robert M. DiPardo,Roger M. Freidinger,W. L. Whitter,George F. Lundell,Daniel F. Veber,Paul S. Anderson,Raymond S.L. Chang,Victor J. Lotti,D. J. Cerino,Tsing-Bau Chen,Paul J. Kling,K. A. Kunkel,James P. Springer,J. Hirshfield +16 more
TL;DR: 3-(Acylamino)-5-phenyl-2H-1,4-benzodiazepines, antagonists of the peptide hormone cholecystokinin (CCK), are described, and the method of development of these compounds is discussed in terms of its relevance to the general problem of drug discovery.
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Design of potent, orally effective, nonpeptidal antagonists of the peptide hormone cholecystokinin
Ben E. Evans,Mark G. Bock,Kenneth E. Rittle,Robert M. DiPardo,Willie L. Whitter,Daniel F. Veber,Paul S. Anderson,Roger M. Freidinger +7 more
TL;DR: The design and synthesis of nonpeptidal antagonists of the peptide hormone cholecystokinin are described, and several of these compounds have high specificity and nanomolar binding affinity and are active after oral administration.
Journal ArticleDOI
Benzodiazepine gastrin and brain cholecystokinin receptor ligands; L-365,260
Mark G. Bock,Robert M. DiPardo,Ben E. Evans,Kenneth E. Rittle,Willie L. Whitter,Daniel F. Veber,Paul S. Anderson,Roger M. Freidinger +7 more
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Protected lactam-bridged dipeptides for use as conformational constraints in peptides
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In Vitro and in Vivo Evaluation of Dihydropyrimidinone C-5 Amides as Potent and Selective α1A Receptor Antagonists for the Treatment of Benign Prostatic Hyperplasia
James C. Barrow,Philippe G. Nantermet,Harold G. Selnick,Kristen L. Glass,Kenneth E. Rittle,Kevin F. Gilbert,Thomas G. Steele,Carl F. Homnick,Roger M. Freidinger,Rick W. Ransom,Paul J. Kling,Duane R. Reiss,Theodore P. Broten,Terry W. Schorn,Raymond S.L. Chang,Stacey O'Malley,Timothy V. Olah,Joan D. Ellis,A. Barrish,Kelem Kassahun,Paula Leppert,Dhanapalan Nagarathnam,Carlos Forray +22 more
TL;DR: While many of the compounds tested displayed poor pharmacokinetics, compound 48 was found to be more potent than terazosin in both a rat model of prostate tone and a dog model of intra-urethral pressure without significantly affecting blood pressure.