Zobrazeno 1 - 8
of 8
pro vyhledávání: '"C J, Woyden"'
Autor:
C. J. Woyden, Roger M. Freidinger, Mark G. Bock, Duane R. Reiss, Joseph M. Pawluczyk, Michelle S. Kuo, Amy G. Quigley, Douglas J. Pettibone, Maribeth T. Guidotti, E V Lis, D. S. Perlow, Peter D. Williams
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:3081-3086
Structure-activity studies on the oxytocin antagonist 1 (L-371,257) have identified a new series of high affinity, receptor-selective OT antagonists in which the N-acetyl-4-piperidinyl ether terminus in 1 has been replaced with a 1-(aryl)ethoxy group
Autor:
Steven N. Gallicchio, James P. Guare, C. J. Woyden, Duane R. Reiss, Carl F. Homnick, Roger M. Freidinger, S Vickers, Michelle S. Kuo, E V Lis, Stuart R. Michelson, Douglas J. Pettibone, Peter D. Williams, Joseph M. Pawluczyk, Erb Jm, Doug W. Hobbs, Ian M. Bell, Rita A. Halpin, David J. Mathre, Maribeth T. Guidotti
Publikováno v:
Journal of Medicinal Chemistry. 41:2146-2163
The previously reported oxytocin antagonist L-371,257 (2) has been modified at its acetylpiperidine terminus to incorporate various pyridine N-oxide groups. This modification has led to the identification of compounds with improved pharmacokinetics a
Autor:
C. J. Woyden, M. J. Novy, Mark G. Bock, Bradley V. Clineschmidt, B. E. Evans, E V Lis, Terry W. Schorn, K. L. Thompson, Peter K. S. Siegl, Douglas J. Pettibone, Duane R. Reiss, Peter D. Williams, Doug W. Hobbs, M. A. Cukierski, Maribeth T. Guidotti, Roger M. Freidinger, D. F. Veber, G. J. Haluska, M. J. Cook, M. J. Kaufman, S.-H. L. Chiu
Publikováno v:
Drug Development Research. 30:129-142
L-368,899 [1S-(-7,7-dimethyl-2-endo-(2S-amino-4-(methylsulfonyl)butyramido)-bicyclo(2.2.1)-heptan-1-yl)methanesulfonyl)-4-(2-methylphenyl)piperazine] was characterized in vitro and in vivo as a potent and selective, orally bioavailable oxytocin (OT)
Autor:
Douglas J. Pettibone, Peter D. Williams, C. J. Woyden, Roger M. Freidinger, Erb Jm, E V Lis, Duane R. Reiss, Bradley V. Clineschmidt, D. F. Veber, Maribeth T. Guidotti, Joseph M. Pawluczyk
Publikováno v:
ChemInform. 27
Autor:
C. J. Woyden, Stacey O'Malley, James C. Barrow, Roger M. Freidinger, Raymond S.L. Chang, Kristen L. Glass, Harold G. Selnick
Publikováno v:
ChemInform. 31
Several 1,3-diaminocyclopentane linked α 1a -receptor antagonists were prepared using a divergent chemical strategy that allows for rapid analysis of all stereochemical permutations for their effect on α 1 -receptor binding.
Autor:
Michelle R. Levy, K.J. Stauffer, Roger M. Freidinger, E V Lis, Mark G. Bock, Stuart R. Michelson, Douglas J. Pettibone, D. S. Perlow, Christopher A. Salvatore, Marlene A. Jacobson, B. E. Evans, Joseph M. Pawluczyk, Amy G. Quigley, C. J. Woyden, Maribeth T. Guidotti, Peter D. Williams, Michelle S. Kuo, Steven N. Gallicchio, Duane R. Reiss
Publikováno v:
Bioorganicmedicinal chemistry letters. 9(9)
Structure-activity studies on the oxytocin antagonist 1 (L-371,257; Ki = 9.3 nM) have led to the identification of a related series of compounds containing an ortho-trifluoroethoxyphenylacetyl core which are orally bioavailable and have significantly
Autor:
D J, Pettibone, M, Guidotti, C M, Harrell, J R, Jasper, E V, Lis, J A, O'Brien, D R, Reiss, C J, Woyden, M G, Bock, B E, Evans
Publikováno v:
Advances in experimental medicine and biology. 395
From a targeted screening effort and medicinal chemistry program, L-368,899 was selected as the first orally-active oxytocin (OT) antagonist to enter clinical trials. In animal studies, L-368,899 was shown to be a potent and selective OT antagonist a
Autor:
D J, Pettibone, B V, Clineschmidt, M T, Kishel, E V, Lis, D R, Reiss, C J, Woyden, B E, Evans, R M, Freidinger, D F, Veber, M J, Cook
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 264(1)
L-366,509, a member of a novel class of nonpeptidyl compounds, has been characterized as an orally active oxytocin (OT) antagonist. L-366,509 exhibits a moderate binding affinity (K(i) values, 370-780 nM) for the rat, rhesus and human uterine OT rece