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US 4,376,779 AGranted
N -(Substituted)-2-aza-2'-hydroxy-5,6-benzotricyclo[6.3.0.sup.1,8.0.sup.4,1 1 ] undecane centrally-acting analgesics
AssigneeMerck Sharp & Dohme (I.A.) Corp.
InventorsPatrice C. Belanger, Robert N. Young
Life of this patent
Estimating the term…
Abstract
Novel N-(substituted) derivatives of 2-aza-2'-hydroxy-5,6-benzotricyclo[6.3.0.sup.1,8.0.sup.4,11 ] undecane of the formula: ##STR1## are centrally acting analgesics effective in the relief of pain.
Claims13
A compound of the formula ##STR6## where R is hydrogen or methyl;
- R.sup.1 and R.sup.2 are each independently hydrogen or C.sub.1-4 alkyl;
- and
- Y is (a) C.sub.1-4 alkyl;
- (b) C.sub.3-4 cycloalkylmethyl;
- (c) phenyl C.sub.1-4 alkyl;
- or (d) substituted benzyl of formula ##STR7## wherein:
- R.sup.3 is hydrogen or C.sub.1-4 alkyl;
- R.sup.4 is hydrogen;
- and
- R.sup.5 is selected from the group consisting of (1) halo;
- (2) C.sub.1-4 alkyl;
- (3) C.sub.1-4 alkoxy;
- (4) amino, and mono- and di-(C.sub.1-4 alkyl) substituted amino;
- (5) cyano;
- (6) trifluoromethyl;
- (7) trifluoromethylthio;
- (8) C.sub.1-4 -alkylthio;
- (9) C.sub.1-4 alkylsulfoxide;
- (10) C.sub.1-4 alkylsulfone;
- (11) hydroxy;
- and (12) phenyl;
- or a pharmaceutically acceptable acid addition salt thereof.
19 more elements
A method of treating pain comprising administering to a patient in need of such treatment of therapeutically effective amount of a compound of the formula:
- ##STR9## wherein R is hydrogen or methyl;
- R.sup.1 and R.sup.2 are each independently hydrogen or C.sub.1-4 alkyl;
- and
- Y is (a) C.sub.1-4 alkyl;
- (b) C.sub.3-4 cycloalkylmethyl;
- (c) phenyl C.sub.1-4 alkyl;
- or (d) substituted benzyl of formula ##STR10## wherein:
- R.sup.3 is hydrogen or C.sub.1-4 alkyl;
- R.sup.4 is hydrogen;
- and
- R.sup.5 is selected from the group consisting of (1) halo;
- (2) C.sub.1-4 alkyl;
- (3) C.sub.1-4 alkoxy;
- (4) amino, and mono- and di-(C.sub.1-4 alkyl) substituted amino;
- (5) cyano;
- (6) trifluoromethyl;
- (7) trifluoromethylothio;
- (8) C.sub.1-4 alkylthio;
- (9) C.sub.1-4 alkylsulfoxide;
- (10) C.sub.1-4 alkylsulfone;
- (11) hydroxy;
- and (12) phenyl;
- or a pharmaceutically acceptable acid addition salt thereof.
20 more elements
A pharmaceutical composition for use in treating pain comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of the formula:
- ##STR11## wherein R is hydrogen or methyl;
- R.sup.1 and R.sup.2 are each independently hydrogen or C.sub.1-4 alkyl;
- and
- Y is (a) C.sub.1-4 alkyl;
- (b) C.sub.3-4 cycloalkylmethyl;
- (c) phenyl C.sub.1-4 alkyl;
- or (d) substituted benzyl of formula ##STR12## wherein:
- R.sup.3 is hydrogen or C.sub.1-4 alkyl;
- R.sup.4 is hydrogen;
- and
- R.sup.5 is selected from the group consisting of (1) halo;
- (2) C.sub.1-4 alkyl;
- (3) C.sub.1-4 alkoxy;
- (4) amino, and mono- and di-(C.sub.1-4 alkyl) substituted amino;
- (5) cyano;
- (6) trifluoromethyl;
- (7) trifluoromethylothio;
- (8) C.sub.1-4 alkylthio;
- (9) C.sub.1-4 alkylsulfoxide;
- (10) C.sub.1-4 alkylsulfone;
- (11) hydroxy;
- and (12) phenyl;
- or a pharmaceutically acceptable acid addition salt thereof.
20 more elements
Dependencies are inferred from the claim text.