Arylpiperazinyl-cyclohexyl indole derivatives for the treatment of depression
First Claim
Patent Images
1. A compound of the formula:
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wherein;
R1, R2 and R3 are each, independently, hydrogen, halogen, CF3, alkyl, alkoxy, MeSO2, or any two of R1, R2 and R3 taken together with the ortho and meta carbon atoms of the ring to which they are attached can form a 5-7 membered carbocyclic or a 5-6 membered heterocyclic ring which includes up to two non-carbon ring atoms each of which independently is either N or O;
R4 is hydrogen, halogen, or alkyl;
R5 is hydrogen, alkyl, alkylaryl, or aryl; and
R6 is hydrogen, halogen, CF3, CN, carbamido, or alkoxy;
X1, X2 and X3 are each carbon or one of X1, or X2 may be nitrogen;
Y is nitrogen; and
Z is carbon or nitrogen;
with the proviso that if one of X1 or X2 is N then at least one of R1, R2 and R3 is not H;
or pharmaceutically acceptable salts thereof.
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Accused Products
Abstract
Compounds are provided which are useful for the treatment of serotonin-affected neurological disorders which comprise
Wherein:
R1, R2 and R3 are each, independently, hydrogen, halogen, CF3, alkyl, alkoxy, MeSO2, or together can form a 5-7 membered carbocyclic or heterocyclic ring;
R4 is hydrogen, halogen, or alkyl;
R5 is hydrogen, alkyl, alkylaryl, or aryl;
R6 is hydrogen, halogen, CF3, CN, carbamide, or alkoxy;
X1, X2 and X3 are each carbon or one of X1, X2 or X3 may be nitrogen;
Y is carbon or nitrogen; and
Z is carbon or nitrogen; or
pharmaceutically acceptable salts thereof.
45 Citations
68 Claims
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1. A compound of the formula:
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wherein; R1, R2 and R3 are each, independently, hydrogen, halogen, CF3, alkyl, alkoxy, MeSO2, or any two of R1, R2 and R3 taken together with the ortho and meta carbon atoms of the ring to which they are attached can form a 5-7 membered carbocyclic or a 5-6 membered heterocyclic ring which includes up to two non-carbon ring atoms each of which independently is either N or O;
R4 is hydrogen, halogen, or alkyl;
R5 is hydrogen, alkyl, alkylaryl, or aryl; and
R6 is hydrogen, halogen, CF3, CN, carbamido, or alkoxy;
X1, X2 and X3 are each carbon or one of X1, or X2 may be nitrogen;
Y is nitrogen; and
Z is carbon or nitrogen;
with the proviso that if one of X1 or X2 is N then at least one of R1, R2 and R3 is not H;
or pharmaceutically acceptable salts thereof.- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66)
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67. A pharmaceutical composition comprising a compound of the formula:
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wherein; R1, R2 and R3 are each, independently, hydrogen, halogen, CF3, alkyl, alkoxy, MeSO2, or any two of R1, R2 and R3 taken together with the ortho and meta carbon atoms of the ring to which they are attached can form a 5-7 membered carbocyclic or a 5-6 membered heterocyclic ring which includes up to two non-carbon ring atoms each of which independently is either N or O;
R4 is hydrogen, halogen, or alkyl;
R5 is hydrogen, alkyl, alkylaryl, or aryl; and
R6 is hydrogen, halogen, CF3, CN, carbamido, or alkoxy;
X1, X2 and X3 are each carbon or one of X1, or X2 may be nitrogen;
Y is nitrogen; and
Z is carbon or nitrogen;
with the proviso that if one of X1 or X2 is N then at least one of R1, R2 and R3 is not H;
or pharmaceutically acceptable salts thereof.
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68. A method for treating depression in a patient in need thereof comprising administering to said patient an antidepressant effective amount of a compound of the formula:
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wherein; R1, R2 and R3 are each, independently, hydrogen, halogen, CF3, alkyl, alkoxy, MeSO2, or any two of R1, R2 and R3 taken together with the ortho and meta carbon atoms of the ring to which they are attached can form a 5-7 membered carbocyclic or a 5-6 membered heterocyclic ring which includes up to two non-carbon ring atoms each of which independently is either N or O, R4 is hydrogen, halogen, or alkyl;
R5 is hydrogen, alkyl, alkylaryl, or aryl; and
R6 is hydrogen, halogen, CF3, CN, carbamido, or alkoxy;
X1, X2 and X3 are each carbon or one of X1, or X2 may be nitrogen;
Y is nitrogen; and
Z is carbon or nitrogen;
with the proviso that if one of X1 or X2 is N then at least one of R1, R2 and R3 is not H;
or pharmaceutically acceptable salts thereof.
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Specification
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Current AssigneeWyeth (Pfizer Inc.)
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Original AssigneeAmerican Home Products Corporation (Pfizer Inc.)
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InventorsZhou, Ping, Gilbert, Adam M., Zhou, Dahui, Asselin, Magda, Evrard, Deborah A., Mewshaw, Richard E., Meagher, Kristin L.
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Primary Examiner(s)BERNHARDT, EMILY A
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Application NumberUS09/476,254Time in Patent Office677 DaysField of Search544/362, 544/363, 544/373, 544/353, 544/364, 514/253.04, 514/253.06, 514/253.09, 514/254.09, 514/249US Class Current514/249CPC Class CodesC07D 209/14 Radicals substituted by nit...C07D 209/34 in position 2C07D 401/08 linked by a carbon chain co...C07D 401/12 linked by a chain containin...C07D 403/12 linked by a chain containin...C07D 405/12 linked by a chain containin...C07D 471/04 Ortho-condensed systems
