Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1991-11-05
1992-08-18
Lee, Mary C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
548517, 548527, 548577, 514429, A61K 3140, C07D40504, C07D40904, C07D20704
Patent
active
051400405
ABSTRACT:
The present invention includes compounds represented by the formula: ##STR1## wherein n is 0 or 1; R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently selected from hydrogen, hydroxyl, amino, alkylamino, alkylsulfonylamino, loweralkyl, loweralkoxy, halo, and thioalkoxy; R.sub.1 and R.sub.2 or R.sub.2 and R.sub.3 taken together can form a methylenedioxy or ethylenedioxy bridge; R.sub.10 is independently selected from hydrogen, loweralkyl, phenyl, and substituted phenyl; R.sub.5 is loweralkyl; R.sub.9 is hydrogen or loweralkyl; R.sub.6 and R.sub.8 are hydrogen; and R.sub.7 is ##STR2## wherein m is 0, 1 or 2; X is CH.sub.2, O, S or N--CH.sub.3 ; or R.sub.7 is ##STR3## wherein s is 0, 1, or 2; Z is C or N; R.sub.11 and R.sub.12 are independently selected from hydrogen, halo, hydroxy, methoxy, thiomethoxy, amino and loweralkyl, or R.sub.11 and R.sub.12 taken together can form a methylenedioxy or ethylenedioxy bridge; or R.sub.7 is ##STR4## wherein t is 0 or 1; or R.sub.5 and R.sub.9 taken together form a pyrrolidine ring and R.sub.6 and R.sub.8 are hydrogen and R.sub.7 is as described above; or R.sub.5 and R.sub.9 taken together form a pyrrolidine ring and then R.sub.6 is hydrogen and R.sub.7 and R.sub.8 taken together may form a phenyl, substituted phenyl, thienyl or furyl ring; or R.sub.5 and R.sub.8 taken together form a pyrrolidine ring and then R.sub.9 and R.sub.6 are hydrogen and R.sub.7 is phenyl, substituted phenyl, thienyl, or furyl; or R.sub.7 and R.sub.9 are hydrogen and R.sub.6 is benzyl, substituted benzyl, thienylmethyl, or furylmethyl; or a pharmaceutically acceptable salt thereof.
REFERENCES:
CA112:76644q Preparation of . . . antagonists. DeBernardis et al. p. 746, 1990.
Basha Fatima Z.
DeBernardis John F.
Zelle Robert E.
Abbott Laboratories
Janssen Jerry F.
Lee Mary C.
McKane Joseph K.
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