Patent number: 4978669
Abstract: Compounds of formula I are useful for suppressing appetite, for altering macronutrient preferences, for suppressing obsessive-compulsive behavior, and for inhibiting cravings and substance abuse: ##STR1## wherein R.sub.1 and R.sub.3 are each independently H, hydroxy-alkyl, alpha-cyanoalkyl, SO.sub.3 H, SO.sub.2 NH.sub.2, or C(O)R, where R is OH, NH.sub.2, lower alkoxy, benzyloxy, or aliphatic amino acyl;R.sub.2 and R.sub.9 are each independently H, lower alkyl, benzyl, succinyl, or C(O)R.sub.4, where R.sub.4 is H, lower alkyl, hydrocarboxy-lower alkylene, or lower alkoxycarboxy-lower alkylene; andR.sub.5, R.sub.6, R.sub.7, and R.sub.8 are each independently H, halo, lower alkyl, hydroxy, lower alkoxy, or two adjacent radicals form methylenedioxy or ethylenedioxy;with the proviso that R.sub.1, R.sub.2, R.sub.3, R.sub.5, R.sub.6, R.sub.7, R.sub.8, and R.sub.9 are not simultaneously H.
Type:
Grant
Filed:
June 8, 1989
Date of Patent:
December 18, 1990
Assignee:
Neurex Corporation
Inventors:
Jack D. Barchas, Glen R. Elliott, Peter I. Adriaenssens, Robert S. Bitner, Stephen S. Bowersox, Laszlo Nadasdi
Patent number: 4585796
Abstract: The tertiary amines of the formula ##STR1## wherein n represents a whole number of 1 to 5;X.sup.1 represents phenyl or phenyl mono-, di- or tri-substituted by R.sup.1, R.sup.2 and R.sup.3 ;X.sup.2 represents hydrogen, lower-alkyl, phenyl or phenyl mono-, di- or tri-substituted by R.sup.1, R.sup.2 and R.sup.3 ;Y represents hydrogen, lower-alkyl, hydroxymethyl, carboxy or lower-alkoxycarbonyl;Z represents a group of the formula ##STR2## R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, halogen, hydroxy, benzyloxy, lower-alkyl, lower-alkoxy, hydroxymethyl, amino, acylamino, lower-alkoxybenzylamino, nitro, carbamoyl, trifluoromethyl or lower-alkylsulphonylmethyl;R.sup.4, R.sup.5 and R.sup.51 represent hydrogen, lower-alkyl, lower-alkoxy, lower alkanoyl, carboxy, cyano, hydroxy, hydroxy-lower-alkyl, acyloxy or a group --C(R.sup.6).dbd.C(R.sup.7)COOR.sup.8, --SO.sub.2 R.sup.9, --C(O)R.sup.9 or --CH.sub.2 R.sup.10, with the proviso that R.sup.4 does not represent hydrogen when R.sup.
Type:
Grant
Filed:
August 1, 1983
Date of Patent:
April 29, 1986
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Leo Alig, Marcel Muller