Janssen laboratories

A series of benzimidazole and benzimidazolone derivatives from the Janssen laboratories has provided an unusually large number of biologically active compounds, particularly in the area of the central nervous system. Reaction of imidazolone itself with isopropenyl acetate leads to the singly protected imidazolone derivative 51. Alkylation of this with 3-chloro-l-bromopropane affords the functionalized derivative Use of this... 

Haloperidol was discovered in the Janssen Laboratories in 1958 (280,315,320,322). It is a butyrophenone derivative and was pursued because of its ability to block the behavioral activating effects of amphetamine in rat models. The amphetamine models were used as screening tools, because symptoms observed in paranoid schizophrenia were noted to be similar to those that developed in chronic amphetamine abusers. The behavioral profile of haloperidol was qualitatively similar to that of CPZ, but haloperidol required up to 50-fold lower doses to exert the same behavioral effects as CPZ. Around this time, the term "major tranquilizer" began to be replaced by the term "neuroleptic." The compound was pursued very vigorously, and the initial clinical results were published only 10 months after the initial synthesis of the compound. Haloperidol is still one of the most widely pre-... 

The circumstances which led to the discovery of tetramisole (II, Ar = C5H5), a new broad-spectrum anthelmintic, were described in two papers from the Janssen Laboratories. f2-Acetylimino-3-[2-hy-droxy-2-(2-thienyl)ethylJthiazoline (Thiazothienol, IV), which was under investigation as an anthelmintic in poultry and sheep, was found to undergo metabolism in these species to the more potent 6-(2-thienyl)-5,6-dihydroimidazo[2,l-b]thiazole (III, Ar = 2-thienyl). This metabolic transformation was not observed in rats or mice. 

Department of Cellular and Molecular Medicine, University of Leuven, Leuven, Belgium Michael R. Jackson Conrad Prebys Center for Chemical Genomics, Sanford-Burnham Medical Research Institute, La Jolla, CA, USA Veerle Janssens Laboratory of Protein Phosphorylation and Proteomics,... 

In the class of the butyrophenones, which has yielded a number of interesting psycho-active agents [119] - chiefly as a result of research done in the Janssen laboratories-two hypotensive compounds are also worth mentioning. They are the co-piperidino-butyrophenone (XII)-which, combined with the Rauwolfia alkaloid rescinnamine and the benzyl-piperazine trimetazidine, is marketed... 

Joseph SJ, P Hugenholtz, P Sangwan, CA Osborne, PH Janssen (2003) Laboratory cultivation of widespread and previously uncultured soil bacteria. Appl Environ Microbiol 69 7210-7215. 

Dick B. Janssen, Biochemical Laboratory, Groningen Biomolecular Sciences and Biotechnology Institute, University of Groningen, Nijenborgh 4, 9747 AG, Groningen, The Netherlands... 

Lores Laboratories GlaxoSmithKline Janssen Pharmaceutica Otsuka... 

Speakers Bureau Abbott Laboratories GlaxoSmithKline Janssen Pharmaceutica Pfizer Pharmaceuticals... 

Persoone, G. Janssen, C.R. Field validation of predictions based on laboratory toxicity tests. In Freshwater Field Tests for Hazard Assessment of Chemicals Hill, I.A., Helmbach, F., Leeuwangh, P., Matthiessen, P., Eds. CRC Press, Inc. Boca Raton, EL, 1994 379-397. 

Janssen, C.L., Nielsen, I.B., Leininger, M.L., Valeev, E.F., Seidl, E.T. mpqc, the massively parallel quantum chemistry program, version 3.0.0a, Sandia National Laboratories, Livermore, CA, 2006. 

Semprini L, Hopkins GD, Janssen DB, et al. 1991. In-situ biotransformation of carbon tetrachloride under anoxic conditions. Ada, OK U.S. Environmental Protection Agency, Robert S. Kerr Environmental Research Laboratory, EPA/600/2-90/060. 

Two different approaches have been taken by researchers to determine the secondary mineralogy of CCBs (1) direct observation, which is accomplished via analysis of weathered ash materials, and (2) prediction, based on chemical equilibrium solubility calculations for ash pore-waters and/or experimental ash leachate or extractant solutions. Because the secondary phases are typically present in very low abundance, their characterization by direct analysis is difficult. On the other hand, predictions based on chemical equilibrium modelling or laboratory leaching experiments may not be reliable indicators of element leachability or accurately indicate the secondary phases that will form under field conditions (Eighmy et al. 1994 Janssen-Jurkovicova et al. 1994). 

Monique M. I,. Janssens, Janssen Research Foundatian.Ber.se. Belgium, Histamine and Histamine Antagonists Hiremagular N. Jayaram, Indiana University School of Medicine, Indianapolis, IN, http //www.medicinc.iu.edu/. Enzyme Therapeutic A. Jayaraman, AT T Bell Laboratories, Mimas Hill, NJ, hltp //www. 

Chemicals were purchased from Aldrich, Fluka, Janssen, and Merck. Merrifield resin (1-2% cross-linked, 200-400 mesh) was obtained from Novabiochem or Polymer Laboratories. To obtain the molecular mass of the resin and to calculate the elemental analysis the following calculation has to be performed ... 

The vaginal retention and antiviral (anti-HIV) effect of different N-9 formulations were compared [43] Advantage 24 (cream) (Lake Pharmaceutics, Columbia Laboratories Inc., Livingston, NJ, USA), Conceptrol (cream) (Ortho Pharmaceuticals, Family Health International, Research Triangle Park, NC, USA), Deflon Foam (foam) (Ortho Pharmaceuticals, Janssen-Ortho Inc., Toronto, Ontario, Canada), Semicid (suppository) (Whitehall Pharmaceuticals, Whitehall-Robbins Healthcare, Madison, NJ, USA), and VCF (film) (Apothecus Pharmaceutical Corporation, Oyster Bay, NY, USA). Even though there was a great variability... 

Muyssen, B.T. and Janssen, C.R. (2001) Zinc acclimation and its effect on the zinc tolerance of Raphidocelis subcapitata and Chlorella vulgaris in laboratory experiments, Chemosphere 45 (4-5), 507-514. 

Janssens de Bisthoven L, Gerhardt A, Soares AMVM. 2004. Effects of acid mine drainage on Chironomus spp. (Diptera) in laboratory and in situ bioassays with the multispecies freshwater biomonitor. Environ Toxicol Chem 23 1123-1128. 

And while it is also true that thirty pharmaceutical companies alone account for 60 percent of worldwide ethical drug sales, the sums of money invested in research do not always get their full return. Thus it is that a small company like Janssen s laboratory, Janssen Pharmaceuticals, in Belgium, which was acquired in 1979 by Johnson and Johnson and which has among its discoveries diphenoxylate (1963) and loperamide (1975), has proved more innovative over the last fifteen years than the Rhone-Poulenc group, which has produced no major new molecule during the same time, although it devotes far more money to its research. 

Janssen and Eddy(41) have given a semiquantitative estimate of the influence of systematic chemical modifications on analgesic potency in mice and rats of a series of N-substituted norpethidines and reversed esters of pethidine. Their estimates, based on the results of the hot-plate test obtained in three separate laboratories, are illustrated in Scheme 6.3. 

All itraconazole clinical trials sponsored by Janssen Research Foundation for the treatment of onychomycosis, in which there was an assessment of laboratory safety, have been analysed (39). There were no significant differences in the number of code 4 abnormalities (baseline... 

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