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US 6,410,550 B1Granted
Aryl fused azapolycyclic compounds
AssigneePfizer Inc.
InventorsJotham Wadsworth Coe, Paige Roanne Palmer Brooks
Life of this patent
Estimating the term…
Abstract
Compounds of the formula and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are defined as in the specification, intermediates in the synthesis of such compounds. pharmaceutical compositions containing such compounds and methods of using such compounds, in the treatment of neurological and psychological disorders.
Claims15
A compound of the formula
- R1 is hydrogen, (C1-C6)alkyl, unconjugate (C3-C6)alkenyl, XC(═O)R13, benzyl or —CH2CH2—O—(C1-C4)alkyl;
- R2 and R3, together with the carbons to which they are attached, form a four to seven membered monocyclic, or ten to fourteen membered bicyclic, carbocyclic ring that can be saturated or unsaturated, wherein from one to three of the nonfused carbon atoms of said monocyclic rings, and from one to five of the carbon atoms of said bicyclic rings that are not part of the benzo rings shown in formula I, may optionally and independently be replaced by a nitrogen, oxygen or sulfur, and wherein said monocyclic and bicyclic rings may optionally be substituted with one or more substituents that are selected, independently, from (C1-C6) alkyl optionally substituted with from one to seven fluorine atoms;
- (C1-C6)alkoxy optionally substituted with from one to seven fluorine atoms;
- nitro, cyano, halo, (C2-C6)alkenyl, (C2-C6)alkynyl, hydroxy, amino, (C1-C6)alkylamino and ((C1-C6)alkyl)2amino, —CO2R4, —CONR5R6, —SO2NR7R8, —C(═O)R13 and —XC(═O)R13;
- wherein each R4, R5, R6, R7, R8 and R13 is selected, independently, from hydrogen and (C1-C6) alkyl, or R5 and R6, or R7 and R8 together with the nitrogen to which they are attached, form a pyrrolidine, piperidine, morpholine, azetidine, piperazine, —N—(C1-C6)alkylpiperazine or thiomorpholine ring, or a thiomorpholine ring wherein the ring sulfur is replaced with a sulfoxide or sulfone;
- and
- each X is, independently, (C1-C6)alkylene;
- or a pharmaceutically acceptable salt thereof.
5 more elements
A compound of the formula (I′)
- wherein
- R2 and R3, together with the carbons to which they are attached, form a four to seven membered monocyclic, or ten to fourteen membered bicyclic, carbocyclic ring that can be saturated or unsaturated, wherein from one to three of the nonfused carbon atoms of said monocyclic rings, and from one to five of the carbon atoms of said bicyclic rings that are not part of the benzo ring shown in formula I, may optionally and independently be replaced by a nitrogen, oxygen or sulfur, and wherein said monocyclic and bicyclic rings may optionally be substituted with one or more substituents that are selected, independently, from (C1-C6) alkyl optionally substituted with from one to seven fluorine atoms;
- (C1-C6)alkoxy optionally substituted with from one to seven fluorine atoms;
- nitro, cyano, halo, (C2-C6)alkenyl, (C2-C6)alkynyl, hydroxy, amino, (C1-C6)alkylamino and ((C1-C6)alkyl)2amino, —CO2R4, —CONR5R6, —SO2NR7R8, —C(═O)R13 and —XC(═O)R13;
- wherein each R4, R5, R6, R7, R8 and R13 is selected, independently, from hydrogen and (C1-C6) alkyl, or R5 and R6, or R7 and R8 together with the nitrogen to which they are attached, form a pyrrolidine, piperidine, morpholine, azetidine, piperazine, —N—(C1-C6)alkylpiperazine or thiomorpholine ring, or a thiomorpholine ring wherein the ring sulfur is replaced with a sulfoxide or sulfone;
- and
- each X is, independently, (C1-C6)alkylene;
- and P′ is COOR16 wherein R16 is allyl, 2,2,2-trichloroethyl or (C1-C6)alkyl;
- —C(═O)NR5R6 wherein R5 and R6 are selected, independently, from hydrogen and (C1-C6) alkyl, or R5 and R6 together with the nitrogen to which they are attached, form a pyrrolidine, piperidine, morpholine, azetidine, piperazine, —N—(C1-C6)alkylpiperazine or thiomorpholine ring, or a thiomorpholine ring wherein the ring sulfur is replaced with a sulfoxide or sulfone;
- —C(═O)H, —C(═O)(C1-C6)alkyl wherein the alkyl moiety may optionally be substituted with from 1 to 3 halo atoms;
- benzyl, or t-butoxycarbonyl (t-Boc).
8 more elements
Dependencies are inferred from the claim text.