Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1989-01-30
1990-10-02
Gerstl, Robert
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
540488, 540548, C07D48804, A61K 3155
Patent
active
049607677
ABSTRACT:
This invention relates to isoxazolobenzoxazepines having the following formula ##STR1## wherein X.sub.1 is H; X.sub.2 is H or OH; or X.sub.1 and X.sub.2 taken together are carbonyl oxygen or ##STR2## R is (1) H, (2) loweralkyl, (3) arylloweralkyl, (4) loweralkynyl, (5) loweralkenyl, (6) ##STR3## where R.sub.1 and R.sub.2 are independently (a) H, (b) lower alkyl, (c) arylloweralkyl, (d) ##STR4## where Z is H, halogen, loweralkyl, loweralkoxy, CF.sub.3, nitro or amino and n' is an integer of 1 to 3; (e) ##STR5## where n" is an integer of 1 to 3; or (f) R.sub.1 and R.sub.2 taken together with the nitrogen atom are substituted or unsubstituted piperidino or pyrrolidino of the formula ##STR6## where R.sub.3 is H, loweralkyl or aryl, and m is an integer of 1 or 2; (7) ##STR7## where R.sub.4 is H or loweralkyl and m' is an integer of 3 or 4; (8) ##STR8## where Z and n' are as previously defined; (9) ##STR9## where m'" is an integer of 1, 2, or 3 (10) ##STR10## where R.sub.5 and R.sub.6 are lower alkyl, aryl lower alkyl or are independently taken together with the N atom to form a substituted or unsubstituted piperidino or pyrrolidino group of the formula ##STR11## where R.sub.3 and m are as previously defined (11) ##STR12## where R.sub.7 is loweralkyl, aryl, or arylloweralkyl; (12) ##STR13## where R.sub.5 and R.sub.6 are as previously defined; Y is H, halogen, loweralkyl, loweralkoxy, CF.sub.3, nitro or amino and n is an integer of 1 to 3, and the pharmaceutically acceptable acid addition salts thereof and where applicable to the geometric, stereo and optical isomers thereof.
REFERENCES:
patent: 4476133 (1984-10-01), Hirai
Kapples Kevin J.
Shutske Gregory M.
Gerstl Robert
Hoechst-Roussel Pharmaceuticals Inc.
Rosenstock Jerome
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