2,1-benzothiazepine-2,2-dioxide-5-carboxylic acid derivatives

Details 2,1-benzothiazepine-2,2-dioxide-5-carboxylic acid derivatives 2,1-benzothiazepine-2,2-dioxide-5-carboxylic acid derivatives

1987-01-12

1989-02-07

Ford, John M.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

540552, C07D28102, A61K 3155

Patent

active

048031976

ABSTRACT:
Disclosed are the compound of the formula ##STR1## wherein n represents zero, 1 or 2; Ar represents a carbocyclic or heterocyclic aryl radical; R and R.sub.1 independently represent hydrogen, lower alkyl or Ar-lower alkyl; R.sub.2 and R.sub.3 independently represent hydrogen, lower alkyl, halogen, trifluoromethyl or lower alkoxy; or R.sub.2 and R.sub.3 together on adjacent carbon atoms represent lower alkylenedioxy; R.sub.4 represents hydroxy or NR.sub.5 R.sub.6 wherein R.sub.5 and R.sub.6 independently represent hydrogen, lower alkyl or AR-lower alkyl,; or R.sub.5 and R.sub.6 together with the nitrogen to which they are attached represent pyrrolidino or piperidino; pharmaceutically acceptable salts thereof; lower alkyl enol ethers and lower alkanoyl enol esters of compounds of formual I wherein R.sub.4 represents hydroxy; as e.g. antiinflammatory agents; methods for preparing said compounds and pharmaceutical compositions comprising said compounds.

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patent: 4582850 (1986-04-01), Liauw
patent: 4605665 (1986-08-01), Liauw
Shen et al., "Non-Steroidal Inhibitors of Arachidonic Acid Metabolism" Butterfield Publishers, Kent, England (1980), pp. 315-317 and 331-335.
J. C. S. Chem. Communications 1981 (20), 1087-8, R. A. Abramovitch et al.
R. A. Abramovitch et al., J. Org. Chem. 49, 3114-21 (1984).
J. Med. Chemistry, 14, 973 (1971).

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