- Novel chemical transformations of tenoxicam
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Both N- and O-substituted derivatives of the anti-inflammatory drug tenoxicam (= 4-hydroxy-2-methyl-N-(pyridin-2-yl)-2H-thieno[2,3-e][1,2]thiazine- 3-carboxamide 1,1-dioxide; 1) were synthesized, and various chemical transformations were investigated. Bot
- Koczian, Kristof,Koekoesi, Jozsef,Mazak, Karoly,Noszal, Bela
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p. 2355 - 2363
(2007/10/03)
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- Analogues and Derivatives of Tenoxicam. 1. Synthesis and Antiinflammatory Activity of Analogues with Different Residues on the Ring Nitrogen and the Amide Nitrogen
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The synthesis of tenoxicam, 4-hydroxy-2-methyl-N-2-pyridyl-2H-thieno-1,2-thiazine-3-carboxamide 1,1-dioxide (1e), and of the analogues with various residues on the ring nitrogen and the amide nitrogen is described.This new class of "oxicams" has pronounced antiinflammatory and analgesic properties.The very specific structure-activity relationship of isomeric and isosteric groups at the amide nitrogen has been evaluated.The substituent in position 2 also has a great influence on the pharmacological properties.Tenoxicam is presently underrgoing clinical trials.
- Binder, Dieter,Hromatka, Otto,Geissler, Franz,Schmied, Karl,Noe, Christian R.,et al.
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p. 678 - 682
(2007/10/02)
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- Thienothiazines
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The present invention relates to compounds of the formula STR1 wherein A together with the two carbon atoms to which it is attached forms the group STR2 AND THE BROKEN LINE REPRESENTS THE DOUBLE BOND IN GROUP (A); R1 represents a lower alkyl group; R2 represents the residue of an aromatic heterocyclic ring containing from 1 to 4 hetero atoms, which may be substituted by one or two lower alkyl groups, or a phenyl group which may be substituted by halogen, hydroxy, lower alkyl, trifluoromethyl or lower alkoxy and R3 and R4 each represent a hydrogen atom or a lower alkyl group. Also provided are methods for their preparation. The thienothiazine derivatives provided by this invention have anti-flammatory, analgesic and antirheumatic activity.
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