139362-30-4Relevant articles and documents
Novel 3-(4-piperidinylthio)-1H-indoles as potent nonopioid orally active central analgesics
Potin, Dominique,Parnet, Veronique,Teulon, Jean-Marie,Camborde, Francoise,Caussade, Francois,Meignen, Joelle,Provost, Daniel,Cloarec, Alix
, p. 805 - 809 (2000)
A series of 3-(4-piperidinylthio)-1H-indoles was synthesized and evaluated in mice in the phenylbenzoquinone(PBQ)-induced writhing and hot plate tests. Most of these compounds are good analgesics with activities comparable to that of morphine. Among them compound 1i (UP 237-61), which has a strong serotonin binding profile, has an interesting antinociceptive activity which is not reserved by naloxone. (C) 2000 Elsevier Science Ltd. All rights reserved.
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.
Piperidinylthioindole derivatives, their methods of preparation and pharmaceutical compositions in which they are present, useful especially as analgesics
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, (2008/06/13)
The present invention relates to the derivatives of the formula STR1 and their addition salts, and to their use in therapeutics, especially as drugs with analgesic properties.
Piperidinylthioindole derivatives, their methods of preparation and pharmaceutical compositions in which they are present, useful especially as analgesics
-
, (2008/06/13)
The present invention relates to the derivatives of the formula STR1 and their addition salts, and to their use in therapeutics, especially as drugs having analgesic properties.
