M
Mark G. Bock
Researcher at Novartis
Publications - 24
Citations - 2191
Mark G. Bock is an academic researcher from Novartis. The author has contributed to research in topics: Receptor & Cholecystokinin. The author has an hindex of 13, co-authored 24 publications receiving 2073 citations. Previous affiliations of Mark G. Bock include Merck & Co..
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Journal ArticleDOI
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.
Journal ArticleDOI
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: In this article, 3.3-(Acylamino)-5-phenyl-2H-1,4-benzodiazepines, antagonists of the peptide hormone cholecystokinin (CCK), are described.
Journal ArticleDOI
Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists
B. E. Evans,Kenneth E. Rittle,Mark G. Bock,Robert M. DiPardo,Roger M. Freidinger,Willie L. Whitter,N. P. Gould,George F. Lundell,Carl F. Homnick +8 more
TL;DR: A series of 3-substituted 5-phenyl-1,4-benzodiazepines, nonpeptidal antagonists of the peptide hormone cholecystokinin, serve to illuminate the distinction between central and peripheral CCK receptors, as well as to provide orally effective CCK antagonists of potential pharmacological or therapeutic utility.
Journal ArticleDOI
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.
William D. Shipe,James C. Barrow,Zhi Qiang Yang,Craig W. Lindsley,Craig W. Lindsley,F. Vivien Yang,Schlegel Kelly-Ann,Youheng Shu,Kenneth E. Rittle,Mark G. Bock,Mark G. Bock,George D. Hartman,Cuyue Tang,Jeanine E. Ballard,Yuhsin Kuo,Emily D. Adarayan,Thomayant Prueksaritanont,Matthew M. Zrada,Victor N. Uebele,Cindy E. Nuss,Thomas M. Connolly,Scott M. Doran,Steven V. Fox,Richard L. Kraus,Michael J. Marino,Michael J. Marino,Valerie Kuzmick Graufelds,Hugo M. Vargas,Hugo M. Vargas,Patricia B. Bunting,Martha Hasbun-Manning,Rose M. Evans,Kenneth S. Koblan,John J. Renger +33 more
TL;DR: Structural modification of the p Piperidine leads 1 and 2 afforded the fluorinated piperidine ( S)- 5, a potent and selective antagonist that displayed in vivo CNS efficacy without adverse cardiovascular effects.
Journal ArticleDOI
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.
Zhi-Qiang Yang,James C. Barrow,William D. Shipe,Kelly-Ann S. Schlegel,Youheng Shu,F. Vivien Yang,Craig W. Lindsley,Craig W. Lindsley,Kenneth E. Rittle,Mark G. Bock,Mark G. Bock,George D. Hartman,Victor N. Uebele,Cindy E. Nuss,Steven V. Fox,Richard L. Kraus,Scott M. Doran,Thomas M. Connolly,Cuyue Tang,Jeanine E. Ballard,Yuhsin Kuo,Emily D. Adarayan,Thomayant Prueksaritanont,Matthew M. Zrada,Michael J. Marino,Michael J. Marino,Valerie Kuzmick Graufelds,Anthony G. DiLella,Ian J. Reynolds,Hugo M. Vargas,Hugo M. Vargas,Patricia B. Bunting,Richard Woltmann,Michael M. Magee,Kenneth S. Koblan,John J. Renger +35 more
TL;DR: Compound 30 demonstrated a robust reduction in the number and duration of seizures at 33 nM plasma concentration, with no cardiovascular effects at up to 5.6 microM, and is a useful tool for probing the effects of T-type calcium channel inhibition.