Antidepressant azaheterocyclylmethyl derivatives of 1,4,5-trioxa-phenanthrene
AssigneeWyeth
InventorsMegan Tran, Gary P. Stack
Life of this patent
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Abstract
Compounds of the formula useful for the treatment of diseases such as depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder (including trichotillomania), social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.
Claims17
A compound of formula I
- wherein
- R1, R3, R4, R5 and R7 are, independently, hydrogen, halo, cyano, carboxamido, carboalkoxy of two to six carbon atoms, trifluoromethyl, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, alkanoyloxy of 2 to 6 carbon atoms, amino, mono- or di-alkylamino in which each alkyl group has 1 to 6 carbon atoms, alkanamido of 2 to 6 carbon atoms, or alkanesulfonamido of 1 to 6 carbon atoms;
- R2 and R6 are hydrogen or alkyl of 1 to 6 carbon atoms;
- Z is CR7 or N;
- X is O, S, H2 or F2;
- the dotted lines at a and b represent independently optional double bonds;
- and
- n is an integer 0, 1 or 2;
- or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising a compound of formula I
- wherein
- R1, R3, R4, R5 and R7 are, independently, hydrogen, halo, cyano, carboxamido, carboalkoxy of two to six carbon atoms, trifluoromethyl, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, alkanoyloxy of 2 to 6 carbon atoms, amino, mono- or di-alkylamino in which each alkyl group has 1 to 6 carbon atoms, alkanamido of 2 to 6 carbon atoms, or alkanesulfonamido of 1 to 6 carbon atoms;
- R2 and R6 are hydrogen or alkyl of 1 to 6 carbon atoms;
- Z is CR7 or N;
- X is O, S, H2 or F2;
- The dotted lines at a and b represent independently optional double bonds;
- and
- n is an integer 0, 1 or 2;
- or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient.
A method of treating a subject suffering from a disorder selected from the group consisting of depression, anxiety, panic disorder, obsessive compulsive disorder, social anxiety disorder and generalized anxiety disorder, which comprises providing to the subject suffering from said condition, a therapeutically effective amount of a compound of formula I
- wherein
- R1, R3, R4, R5 and R7 are, independently, hydrogen, halo, cyano, carboxamido, carboalkoxy of two to six carbon atoms, trifluoromethyl, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, alkanoyloxy of 2 to 6 carbon atoms, amino, mono- or di-alkylamino in which each alkyl group has 1 to 6 carbon atoms, alkanamido of 2 to 6 carbon atoms, or alkanesulfonamido of 1 to 6 carbon atoms;
- R2 and R6 are hydrogen or alkyl of 1 to 6 carbon atoms;
- Z is CR7 or N;
- X is O, S, H2 or F2;
- The dotted lines at a and b represent independently optional double bonds;
- and
- n is an integer 0, 1 or 2;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.