16332-18-6Relevant academic research and scientific papers
HETEROCYCLIC COMPOUND
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Paragraph 1011, (2015/04/15)
The present invention provides a compound having a superior JAK inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like, or a salt thereof. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
5-HTX MODULATORS
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Page/Page column 82-83, (2008/06/13)
This invention relates to compounds which bind to serotonin receptors inside or outside the central nervous system, in particular compounds which bind to the 5-HT2 or 5-HT7 receptors, their preparation and use, compositions containing them, and methods of treatment using them.
Structural changes of benzylether derivatives of vesamicol and their influence on the binding selectivity to the vesicular acetylcholine transporter
Wenzel, Barbara,Sorger, Dietlind,Heinitz, Katrin,Scheunemann, Matthias,Schliebs, Reinhard,Steinbach, J?rg,Sabri, Osama
, p. 1197 - 1205 (2007/10/03)
18F labelled vesamicol analogues, which bind to the vesicular acetylcholine transporter (VAChT) in central cholinergic nerve terminals, are expected to be potential radioligands for the visualisation of cholinergic transmission deficits via pos
Piperidine carboxylic acid derivatives of 10H-pyrazino[2,3-b][1,4] benzothiazine as orally-active adhesion molecule inhibitors
Kaneko, Toshihiko,Clark, Richard S. J.,Ohi, Norihito,Ozaki, Fumihiro,Kawahara, Tetsuya,Kamada, Atsushi,Okano, Kazuo,Yokohama, Hiromitsu,Ohkuro, Masayoshi,Muramoto, Kenzo,Takenaka, Osamu,Kobayashi, Seiichi
, p. 675 - 687 (2007/10/03)
Novel piperidine carboxylic acid derivatives of 10H-pyrazino[2,3-b][1,4] benzothiazine were prepared and evaluated for their inhibitory activity on the upregulation of adhesion molecules such as intercellular adhesion molecule-1 (ICAM-1). Replacement of the methanesulfonyl group on the piperidine ring of previously prepared derivatives with a carboxylic acid-containing moiety resulted in a number of potent adhesion molecule inhibitors. Of these, (anti) [3-(10H-pyrazino[2,3-b][1,4]benzothiazin-8-yl)methyl-3-azabicyclo[3.3.1] non-9-yl]acetic acid 2q (ER-49890), showed the most potent oral inhibitory activities against neutrophil migration in an interleukin-1 (IL-1) induced paw inflammation model using mice, and leukocyte accumulation in a carrageenan pleurisy model in the rat, and therapeutic effect on collagen-induced arthritis in rats.
Substituted piperidines - Highly potent renin inhibitors due to induced fit adaptation of tile active site
Vieira, Eric,Binggeli, Alfred,Breu, Volker,Bur, Daniel,Fischli, Walter,Gueller, Rolf,Hirth, Georges,Maerki, Hans Peter,Mueller, Marcel,Oefner, Christian,Scalone, Michelangelo,Stadler, Heinz,Wilhelm, Maurice,Wostl, Wolfgang
, p. 1397 - 1402 (2007/10/03)
The identification, synthesis and activity of a novel class of piperidine renin inhibitors is presented. The most active compounds show activities in the picomolar range and are among the most potent renin inhibitors ever identified.
