Small molecule modulators of non-endogenous, constitutively activated human serotonin receptors
First Claim
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1. A compound structurally represented as follows:
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Abstract
Disclosed herein are non-endogenous, constitutively activated forms of the human 5-HT2A and human 5-HT2C receptors and uses of such receptors to screen candidate compounds. Further disclosed herein are candidate compounds identified by the screening method which act at the 5HT2A receptors. Yet further disclosed is a new class of compounds which act at the 5HT2A receptors.
133 Citations
12 Claims
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1. A compound structurally represented as follows:
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- View Dependent Claims (3)
- 2. A compound structurally represented as follows:
- 5. A compound structurally represented as follows:
- 6. A compound structurally represented as follows:
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9. A compound structurally represented as follows:
- wherein;
X is O or S; Z is H or CH3 ; R3 and R10 are each independently selected from H, C1-8 straight chain or branched alkyl, C3-8 cycloalkyl, C4-9 alkylcycloalkyl, and C2-8 alkenyl; R11 is H, F, Cl, Br, I, R7, CF3, CCl3, NR8 R9, NR10 COR7, NR10 SO2 R7, OR7, OCF3, OCOR7, OSO2 R7, SR7, SCF3, SCOR7, SO3 R7, SO2 NR8 R9, NO2, CN, COOR7, COSR7, or CONR8 R9, with the proviso that when a position adjacent to R11 is substituted, then R11 and said adjacent position can together be selected from SCH2 S, SCH2 CH2 S, OCH2 O, and OCH2 CH2 O to form a bi-cyclic structure; R7 is H, C1-8 straight chain or branched alkyl, C3-8 cycloalkyl, C4-9 alkylcycloalkyl, C2-8 alkenyl, aryl or alkylaryl; R8 and R9 are independently selected from H, C1-8 straight chain or branched alkyl, and C2-8 alkenyl or cycloalkyl, or alkylcycloalkyl, or aryl or CH2 aryl wherein each moiety within said C1-8 straight chain or branched alkyl, C2-8 alkenyl or cycloalkyl, or alkylcycloalkyl, or aryl or CH2 aryl may be optionally substituted by up to four substituents in any position, whereby each substituent is independently selected from;
F, Cl, Br, I, CF3, CCl3, CH3, C2 H5, C3 H7, C4 H9, NH2, NHCH3, N(CH3)2, NHC2 H5, N(C2 H5)2, NHC3 H7, N(C3 H7)2, NHC4 H9, N(C4 H9)2, NHCOH, NHCOCH3, NHCOC2 H5, NHCOC3 H7, NHCOC4 H9, NHSO2 CH3, NHSO2 C2 H5, NHSO2 C3 H7, NHSO2 C4 H9, OH, OCH3, OC2 H5, OC3 H7, OC4 H7, OC4 H9, OC5 H9, OC5 H11, OC6 H11, OC6 H13, OCF3, OCOCH3, OCOC2 H5, OCOC3 H7, OCOC4 H9, OSO2 CH3, OSO2 C2 H5, OSO2 C3 H7, OSO2 C4 H9, SH, SCH3, SC2 H5, SC3 H7, SC4 H7, SC4 H9, SC5 H9, SC5 H11, SC6 H11, SC6 H13,, SCF3, SCOCH3, SCOC2 H5, SCOC3 H7, SCOC4 H9, SO3 CH3, SO3 C2 H5, SO3 C3 H7, SO3 C4 H9, SO2 NH, SO2 NH2, SO2 NHCH3, SO2 N(CH3)2, SO2 NHC2 H5, SO2 N(C2 H5)2, SO2 NHC3 H7, SO2 N(C3 H7)2, SO2 NHC4 H9, SO2 N(C4 H9)2, NO2, CN, COOCH3, COOC2 H5, COOC3 H7, COOC4 H9, COSCH3, COSC2 H5, COSC3 H7, COSC4 H9, CONH2, CONHCH3, CON(CH3)2, CONHC2 H5, CON(C2 H5)2, CONHC3 H7, CON(C3 H7)2, CONHC4 H9, and CON(C4 H9)2, andwith the proviso that when either of R8 or R9 contain an aryl ring substituted at at least two adjacent positions on said aryl ring, then said two adjacent positions can together be selected from SCH2 S, SCH2 CH2 S, OCH2 O, or OCH2 CH2 O to form a bi-cyclic structure; R12, R13, R14, and R15 are each independently selected from;
F, Cl, Br, I, CF3, CCl3, CH3, C2 H5, C3 H7, C4 H9, NH2, NHCH3, N(CH3)2, NHC2 H5, N(C2 H5)2, NHC3 H7, N(C3 H7)2, NHC4 H9, N(C4 H9)2, NHCOH, NHCOCH3, NHCOC2 H5, NHCOC3 H7, NHCOC4 H9, NHSO2 CH3, NHSO2 C2 H5, NHSO2 C3 H7, NHSO2 C4 H9, OH, OCH3, OC2 H5, OC3 H7, OC4 H7, OC4 H9, OC5 H9, OC5 H11, OC6 H11, OC6 H13, OCF3, OCOCH3, OCOC2 H5, OCOC3 H7, OCOC4 H9, OSO2 CH3, OSO2 C2 H5, OSO2 C3 H7, OSO2 C4 H9, SH, SCH3, SC2 H5, SC3 H7, SC4 H7, SC4 H9, SC5 H9, SC5 H11, SC6 H11, SC6 H13,, SCF3, SCOCH3, SCOC2 H5, SCOC3 H7, SCOC4 H9, SO3 CH3, SO3 C2 H5, SO3 C3 H7, SO3 C4 H9, SO2 NH, SO2 NH2, SO2 NHCH3, SO2 N(CH3)2, SO2 NHC2 H5, SO2 N(C2 H5)2, SO2 NHC3 H7, SO2 N(C3 H7)2, SO2 NHC4 H9, SO2 N(C4 H9)2, NO2, CN, COOCH3, COOC2 H5, COOC3 H7, COOC4 H9, COSCH3, COSC2 H5, COSC3 H7, COSC4 H9, CONH2, CONHCH3, CON(CH3)2, CONHC2 H5, CON(C2 H5)2, CONHC3 H7, CON(C3 H7)2, CONHC4 H9, and CON(C4 H9)2, andwith the proviso that when any two adjacent positions of R12, R13, R14, and R15 are substituted, said two adjacent positions can together be further selected from SCH2 S, SCH2 CH2 S, OCH2 O, and OCH2 CH2 O to form a bi-cyclic structure; and with the proviso that at least two of R12, R13, R14, and R15 must be H. - View Dependent Claims (10, 11, 12)
- wherein;
Specification
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Current AssigneeArena Pharmaceuticals Incorporated
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Original AssigneeArena Pharmaceuticals Incorporated
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InventorsRusso, Joseph F., Liaw, Chen W., Chalmers, Derek T., Beeley, Nigel R. A., Menzaghi, Frederique, Liu, Qian, Thomsen, William J., Behan, Dominic P., Lawless, Michael S., Glen, Robert C., Smith, Julian R., Foster, Richard J.
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Primary Examiner(s)STOCKTON, LAURA LYNNE
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Application NumberUS09/418,721Time in Patent Office403 DaysField of Search548/375.1, 548/377.1, 514/406US Class Current514/406CPC Class CodesA61P 25/00 Drugs for disorders of the ...C07D 231/12 with only hydrogen atoms, h...C07D 231/16 Halogen atoms or nitro radi...C07D 409/12 linked by a chain containin...C07K 14/70571 for neuromediators, e.g. se...
