Mch receptor antagonists
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Abstract
The present invention relates to novel compounds of the formula (I) which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of obesity, obesity related disorders, anxiety, or depression.
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Citations
20 Claims
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1. A compound of Formula I:
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 18, 19, 20)
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2. A compound according to claim 1, wherein Q is Formula II;
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R1 represents (i) C1-C10 alkyl, C1-C10 alkyl substituted by substituent(s) independently selected from halogen, oxo, C1-C3 alkoxy, C1-C3 alkoxy substituted by carbocyclic aryl, C1-C3 alkylcarbonyloxy, carbocyclyloxy, carbocyclic aryloxy, carbocyclic aryloxy substituted by substituent(s) independently selected from halogen, nitro, C1-C4 alkyl, C1-C4 alkyl substituted by substituent(s) independently selected from oxo, carbocyclic arylcarbonylamino, halogenated carbocyclic arylcarbonylamino, heterocyclyloxy, heterocyclyloxy substituted by C1-C3 alkyl, substituted heterocyclyl-ethylideneaminooxy, C1-C3 alkoxycarbonyl, C1-C3 alkoxycarbonyl substituted by carbocyclic aryl, mono- or di-C1-C3 alkylaminocarbonyl, mono- or di-carbocyclic arylamino, mono- or di-carbocyclic arylamino substituted by hydroxy, C1-C3 alkylcarbonylamino, C1-C3 alkylcarbonylamino substituted by substituent(s) independently selected from C1-C3 alkylcarbonylamino, carbocyclic arylcarbonylamino, heterocyclyl, C1-C4 alkoxycarbonylamino, heterocyclyl carbonylamino, carbocyclic arylsulfonylamino, carbocyclic arylsulfonylamino substituted by substituent(s) independently selected from nitro, C1-C3 alkyl, mono- or di-C1-C3 alkylamino, C1-C3 alkylthio, C1-C3 alkylthio substituted by substituent(s) independently selected from mono- or di-carbocyclic arylaminocarbonyl, halogenated mono- or di-carbocyclic arylaminocarbonyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, C1-C3 alkoxy, carbocyclic arylthio, carbocyclic arylthio substituted by substituent(s) independently selected from halogen, C1-C3 alkyl, carbocyclic arylsulfonyl, halogenated carbocyclic arylsulfonyl, heterocyclylthio, heterocyclylthio substituted by substituent(s) independently selected from nitro, C1-C3 alkyl, C3-C6 cycloalkyl, C3-C6 cycloalkyl substituted by C1-C3 alkyl, C3-C6 cycloalkenyl, carbocyclyl, carbocyclyl substituted by substituent(s) independently selected from halogen, C1-C3 alkyl, C1-C3 alkoxy, C2-C3 alkenyl, C2-C3 alkenyl substituted by carbocyclic aryl, C2-C3 alkenyl substituted by carbocyclic aryl substituted C1-C3 alkylsulfinyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, hydroxy, nitro, C1-C4 alkyl, C1-C4 alkyl substituted by substituent(s) independently selected from oxo, carbocyclic aryl, heterocyclyl, C1-C4 alkoxy, C1-C4 alkoxy substituted by substituent(s) independently selected from halogen, carbocyclic aryl, carbocyclic aryloxy, C1-C3 alkylcarbonyloxy, mono- or di-carbocyclic arylamino, halogenated mono- or di-carbocyclic arylamino, mono- or di-carbocyclic arylaminocarbonyl, mono- or di-carbocyclic arylaminocarbonyl substituted by substituent(s) independently selected from halogen, nitro, C1-C3 alkyl, C1-C3 alkoxy, halogenated C1-C3 alkoxy, mercapto, C1-C3 alkylthio, halogenated C1-C3 alkylthio, C1-C3 alkylsulfonyl, C3-C6 cycloalkyl, carbocyclic aryl, heterocyclyl, heterocyclyl, heterocyclyl substituted by substituent(s) independently selected from hydroxy, C1-C3 alkyl, C1-C3 alkyl substituted by carbocyclic aryl, C1-C3 alkoxy, C1-C3 alkoxy substituted by carbocyclic aryl, carbocyclic aryl, halogenated carbocyclic aryl, (ii) C2-C6 alkenyl, C2-C6 alkenyl substituted by substituent(s) independently selected from oxo, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, nitro, C1-C3 alkyl, halogenated C1-C3 alkyl, C1-C3 alkoxy, halogenated C1-C3 alkoxy, heterocyclyl, heterocyclyl substituted by substituent(s) independently selected from hydroxy, C1-C3 alkyl, C1-C3 alkoxy, (iii) C3-C6 cycloalkyl, C3-C6 cycloalkyl substituted by substituent(s) independently selected from C1-C3 alkyl, C1-C3 alkyl substituted by substituent(s) independently selected from oxo, carbocyclic aryl, carbocyclic arylcarbonylamino, carbocyclic aryl, (iv) carbocyclyl, carbocyclyl substituted by nitro, (v) carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, hydroxy, cyano, nitro, C1-C9 alkyl, C1-C9 alkyl substituted by substituent(s) independently selected from halogen, oxo, carbocyclic aryloxy, carbocyclylimino, carbocyclylimino substituted by carbocyclic aryl, mono- or di-carbocyclic arylaminocarbonyl, mono- or di-carbocyclic arylaminocarbonyl substituted by C1-C3 alkoxy, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, C1-C3 alkyl, halogenated C1-C3 alkyl, heterocyclyl, heterocyclyl substituted by C1-C3 alkyl, C1-C7 alkoxy, C1-C7 alkoxy substituted by substituent(s) independently selected from halogen, carbocyclic aryl, C1-C3 alkylcarbonyloxy, carbocyclic aryloxy, carbocyclic aryloxy substituted by C1-C3 alkoxy, C1-C3 alkoxycarbonyl, mono- or di-C1-C3 alkylaminocarbonyl, mono- or di-C1-C3 alkylaminocarbonyl substituted by carbocyclic aryl, mono- or di-carbocyclic arylaminocarbonyl, mono- or di-carbocyclic arylaminocarbonyl substituted by C1-C3 alkyl, amino, mono- or di-C1-C3 alkylamino, C1-C3 alkynylcarbonylamino, C1-C3 alkynylcarbonylamino substituted by carbocyclic aryl, carbocyclic arylsulfonylamino, carbocyclic arylsulfonylamino substituted by C1-C3 alkyl, (carbocyclic aryl)NHC(O)NH, (carbocyclic aryl)NHC(O)NH substituted by C1-C3 alkoxy, (carbocyclic aryl)NHC(O)NH substituted by haloganated C1-C3 alkoxy, C1-C3 alkylthio, halogenated C1-C3 alkylthio, carbocyclic arylthio, carbocyclic arylthio substituted by cyano, C1-C3 alkylsulfonyl, mono- or di-C1-C3 alkylaminosulfonyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from C1-C7 alkyl, halogenated C1-C7 alkyl, heterocyclyl, heterocyclyl substituted by substituent(s) independently selected from C1-C3 alkyl, carbocyclic aryl, halogenated carbocyclic aryl, (vi) heterocyclyl, or heterocyclyl substituted by substituent(s) independently selected from halogen, nitro, C1-C4 alkyl, C1-C4 alkyl substituted by substituent(s) independently selected from halogen, oxo, C1-C3 alkylthio, C1-C3 alkylthio substituted by carbocyclic aryl, C1-C3 alkylthio substituted by halogenated carbocyclic aryl, carbocyclic aryl, halogenated carbocyclic aryl, heterocyclyl, C1-C3 alkoxy, carbocyclic aryloxy, carbocyclic aryloxy substituted by substituent(s) independently selected from halogen, C1-C3 alkyl, C1-C3 alkylthio, C1-C3 alkenylthio, carbocyclic arylthio, C1-C3 alkylsulfonyl, carbocyclic arylsulfonyl, halogenated carbocyclic arylsulfonyl, carbocyclic arylsulfonyl substituted by C1-C4 alkyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, nitro, C1-C3 alkyl, C1-C3 alkoxy, heterocyclyl, heterocyclyl substituted by substituent(s) independently selected from C1-C3 alkyl, halogenated C1-C3 alkyl;
Y is —
C(O)—
;
wherein carbocyclic aryl is phenyl, naphthyl, anthranyl, or biphenyl;
carbocyclyl is 10,11-dihydro-5-oxo-dibenzo[a,d]cycloheptyl, 1-oxo-indanyl, 9H-fluorenyl, 9-oxo-fluorenyl, acenaphthyl, anthraquinonyl, C-fluoren-9-ylidene, indanyl, indenyl, 1,2,3,4-tetrahydro-naphthyl, or bicyclo[2.2.1]hepteny;
heterocyclyl is 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2-dihydro-3-oxo-pyrazolyl, 1,3-dioxo-isoindolyl, 1H-indolyl, 1H-pyrrolyl, 1-oxo-3H-isobenzofuranyl, 2,3-dihydro-benzo[1,4]dioxinyl, 2,3-dihydro-benzofuryl, 2,4-dihydro-3-oxo-pyrazolyl, 2H-benzopyranyl, 2-oxo-benzopyranyl, 2-oxo-pyrrolidinyl, 3,4-dihydro-2H-benzo[b][1,4]dioxepinyl, 4-oxo-1,5,6,7-tetrahydro-indolyl, 4-oxo-3,4-dihydro-phthalazinyl, 4-oxo-benzopyranyl, 9,10,10-trioxo-thioxanthenyl, 9H-xanthenyl, azetidinyl, benzimidazolyl, benzo[1,3]dioxolyl, benzo[2,1,3]oxadiazolyl, benzo[b]thienyl, cinnolyl, furyl, imidazolyl, isoxazolyl, morpholino, morpholinyl, oxazolyl, oxolanyl, piperidyl, piridyl, pyrazolyl, pyridyl, pyrimidyl, pyrrolidyl, quinolyl, quinoxalyl, thiazolidyl, thiazolyl, thienyl, thiolanyl, tetrahydro-thienyl, benzofuranyl, or benzothiazolyl;
halogen is fluoro, chloro, bromo, or iodo;
or a salt thereof.
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3. A compound according to claim 2, wherein
R1 represents (i) C1-C10 alkyl, C1-C10 alkyl substituted by substituent(s) independently selected from oxo, di-propylaminocarbonyl, methoxy substituted by carbocyclic aryl, methylcarbonyloxy, carbocyclic aryloxy, halogenated carbocyclic aryloxy, carbocyclic aryloxy substituted by nitro, heterocyclyloxy substituted by methyl, substituted heterocyclyl-ethylideneaminooxy, tert-butoxycarbonylamino, carbocyclic arylcarbonylamino, C1-C2 alkylthio, C1-C2 alkylthio substituted by substituent(s) independently selected from halogenated carbocyclic aryl, carbocyclic aryl substituted by methoxy, carbocyclic arylthio, hetrocyclylthio substituted by nitro, hetrocyclylthio substituted by methyl, C5-C6 cycloalkyl, C5-C6 cycloalkenyl, carbocyclyl substituted by substituent(s) independently selected from halogen, methyl, methoxy, ethenyl substituted by carbocyclic aryl substituted methylsulfinyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, hydroxy, nitro, C1-C4 alkyl, C1-C4 alkyl substituted by substituent(s) independently selected from oxo, carbocyclic aryl, heterocyclyl, C1-C4 alkoxy, halogenated C1-C4 alkoxy, C1-C4 alkoxy substituted by carbocyclic aryl, carbocyclic aryloxy, halogenated mono-carbocyclic arylaminocarbonyl, carbocyclic aryl, heterocyclyl, heterocyclyl, heterocyclyl substituted by substituent(s) independently selected from C1-C2 alkyl, C1-C2 substituted by carbocyclic aryl, methoxy, methoxy substituted by carbocyclic aryl, carbocyclic aryl, halogenated carbocyclic aryl, (ii) C2-C3 alkenyl substituted by substituent(s) independently selected from carbocyclic aryl, halogenated carbocyclic aryl, carbocyclic aryl substituted by nitro, (iii) C3-C6 cycloalkyl, C3-C6 cycloalkyl substituted by substituent(s) independently selected from methyl substituted by oxo, methyl substituted by carbocyclic aryl, carbocyclic aryl, (iv) carbocyclyl, (v) carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, hydroxy, cyano, nitro, C1-C9 alkyl, C1-C9 alkyl substituted by substituent(s) independently selected from halogen, oxo, carbocyclic aryl, carbocyclic aryl substituted by methyl, carbocyclic aryloxy, C1-C7 alkoxy, halogenated C1-C7 alkoxy, C1-C7 alkoxy substituted by carbocyclic aryl, methylcarbonyloxy, carbocyclic aryloxy, carbocyclic aryloxy substituted by methoxy, amino, di-methylamino, propargynylcarbonylamino substituted by carbocyclic aryl, carbocyclic arylsulfonylamino substituted by methyl, (carbocyclic aryl)NHC(O)NH substituted by halogenated methoxy, halogenated methylthio, carbocyclic arylthio substituted by cyano, di-propylamino sulfonyl, mono- or di-ethylaminocarbonyl substituted by carbocyclic aryl, carbocyclic aryl, heterocyclyl substituted by methyl, heterocyclyl substituted by halogenated carbocyclic aryl, (vi) heterocyclyl, or heterocyclyl substituted by substituent(s) independently selected from halogen, nitro, C1-C4 alkyl, C1-C4 alkyl substituted by substituent(s) independently selected from halogen, methylthio substituted by halogenated carbocyclic aryl, carbocyclic aryl, halogenated carbocyclic aryl, heterocyclyl, methoxy, carbocyclic aryloxy, carbocyclic aryloxy substituted by methyl, C1-C3 alkylthio, propenylthio, carbocyclic arylthio, C1-C3 alkylsulfonyl, carbocyclic arylsulfonyl substituted by C1-C4 alkyl, carbocyclic aryl, halogenated carbocyclic aryl, carbocyclic aryl substituted by methyl, carbocyclic aryl substituted by nitro, heterocyclyl; -
R2 is methylamino or dimethylamino;
L is selected from Formula Va, VIIIa, or IXa;
wherein R4 and R5 are independently selected from H or C1-C3 alkyl;
wherein carbocyclic aryl is phenyl, naphthyl, anthranyl, or biphenyl;
carbocyclyl is 1-oxo-indanyl, 9-oxo-fluorenyl, indenyl, anthraquinonyl, C-fluoren-9-ylidene, 1,2,3,4-tetrahydro-naphthyl, or bicyclo[2.2.1]heptenyl;
heterocyclyl is 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2-dihydro-3-oxo-pyrazolyl, 1,3-dioxo-isoindolyl, 1H-indolyl, 1H-pyrrolyl, 1-oxo-3H-isobenzofuranyl, 2,3-dihydro-benzo[1,4]dioxinyl, 2,4-dihydro-3-oxo-pyrazolyl, 2H-benzopyranyl, 2-oxo-benzopyranyl, 3,4-dihydro-2H-benzo[b][1,4]dioxepinyl, 4-oxo-3,4-dihydro-phthalazinyl, 4-oxo-benzopyranyl, 9,10,10-trioxo-thioxanthenyl, 9H-xanthenyl, azetidinyl, benzimidazolyl, benzo[1,3]dioxolyl, benzo[2,1,3]oxadiazolyl, benzo[b]thienyl, furyl, imidazolyl, isoxazolyl, morpholino, morpholinyl, oxolanyl, piperidyl, piridyl, pyrazolyl, pyridyl, quinolyl, quinoxalyl, thiazolidyl, thiazolyl, thienyl, thiolanyl, 2,3-dihydro-1-oxo-isoindolyl, 2,3-dihydro-benzofuryl, 2-oxo-pyrrolidinyl, 4-oxo-1,5,6,7-tetrahydro-indolyl, cinnolyl, pyrimidyl, pyrrolidyl, tetrahydro-thienyl, benzofuranyl, or benzothiazolyl;
halogen is fluoro, chloro, bromo, or iodo;
or a salt thereof.
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4. A compound according to claim 3, wherein
R1 represents (i) C1-C10 alkyl substituted by substituent(s) independently selected from oxo, di-propylaminocarbonyl, methoxy substituted by carbocyclic aryl, methylcarbonyloxy, carbocyclic aryloxy, halogenated carbocyclic aryloxy, carbocyclic aryloxy substituted by nitro, heterocyclyloxy substituted by methyl, substituted heterocyclyl-ethylideneaminooxy, tert-butoxycarbonylamino, carbocyclic arylcarbonylamino, C1-C2 alkylthio, C1-C2 alkylthio substituted by substituent(s) independently selected from halogenated carbocyclic aryl, carbocyclic aryl substituted by methoxy, carbocyclic arylthio, hetrocyclylthio substituted by nitro, hetrocyclylthio substituted by methyl, C5-C6 cycloalkenyl, carbocyclyl substituted by substituent(s) independently selected from halogen, methyl, methoxy, ethenyl substituted by carbocyclic aryl substituted methylsulfinyl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, hydroxy, nitro, C1-C4 alkyl, C1-C4 alkyl substituted by substituent(s) independently selected from carbocyclic aryl, heterocyclyl, C1-C4 alkoxy, halogenated C1-C4 alkoxy, C1-C4 alkoxy substituted by carbocyclic aryl, carbocyclic aryloxy, halogenated mono-carbocyclic arylaminocarbonyl, carbocyclic aryl, heterocyclyl, heterocyclyl substituted by substituent(s) independently selected from C1-C2 alkyl, C1-C2 substituted by carbocyclic aryl, methoxy, methoxy substituted by carbocyclic aryl, carbocyclic aryl, halogenated carbocyclic aryl, (ii) C2-C3 alkenyl substituted by substituent(s) independently selected from carbocyclic aryl, halogenated carbocyclic aryl, carbocyclic aryl substituted by nitro, (iii) C3-C6 cycloalkyl substituted by substituent(s) independently selected from methyl substituted by oxo, methyl substituted by carbocyclic aryl, carbocyclic aryl, (iv) carbocyclyl, (v) carbocyclic aryl substituted by substituent(s) independently selected from halogen, hydroxy, cyano, nitro, C1-C9 alkyl, C1-C9 alkyl substituted by substituent(s) independently selected from halogen, oxo, carbocyclic aryl, carbocyclic aryl substituted by methyl, carbocyclic aryloxy, C1-C7 alkoxy, halogenated C1-C7 alkoxy, C1-C7 alkoxy substituted by carbocyclic aryl, methylcarbonyloxy, carbocyclic aryloxy, carbocyclic aryloxy substituted by methoxy, amino, di-methylamino, propargynylcarbonylamino substituted by carbocyclic aryl, carbocyclic arylsulfonylamino substituted by methyl, (carbocyclic aryl)NHC(O)NH substituted by halogenated methoxy, halogenated methylthio, carbocyclic arylthio substituted by cyano, di-propylamino sulfonyl, mono- or di-ethylaminocarbonyl substituted by carbocyclic aryl, carbocyclic aryl, heterocyclyl substituted by methyl, heterocyclyl substituted by halogenated carbocyclic aryl, (vi) or heterocyclyl substituted by substituent(s) independently selected from halogen, nitro, C1-C4 alkyl, C1-C4 alkyl substituted by substituent(s) independently selected from halogen, methylthio substituted by halogenated carbocyclic aryl, carbocyclic aryl, halogenated carbocyclic aryl, heterocyclyl, methoxy, carbocyclic aryloxy, carbocyclic aryloxy substituted by methyl, C1-C3 alkylthio, propenylthio, carbocyclic arylthio, C1-C3 alkylsulfonyl, carbocyclic arylsulfonyl, carbocyclic arylsulfonyl substituted by C1-C4 alkyl, carbocyclic aryl, halogenated carbocyclic aryl, carbocyclic aryl substituted by methyl, carbocyclic aryl substituted by nitro, heterocyclyl; -
L is selected from Formula XX-XXII;
wherein carbocyclic aryl is phenyl, naphthyl, or biphenyl;
carbocyclyl is 1-oxo-indanyl, 9-oxo-fluorenyl, indenyl, anthraquinonyl, C-fluoren-9-ylidene, 1,2,3,4-tetrahydro-naphthyl, or bicyclo[2.2.1]heptenyl;
heterocyclyl is 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2-dihydro-3-oxo-pyrazolyl, 1H-indolyl, 1H-pyrrolyl, 2,4-dihydro-3-oxo-pyrazolyl, 2H-benzopyranyl, 4-oxo-benzopyranyl, azetidinyl, benzo[b]thienyl, furyl, isoxazolyl, morpholinyl, piperidyl, piridyl, pyrazolyl, pyridyl, quinolyl, thiazolidyl, thiazolyl, thienyl, thiolanyl, 2,3-dihydro-1-oxo-isoindolyl, 2,3-dihydro-benzofuryl, 2-oxo-benzopyranyl, 2-oxo-pyrrolidinyl, 4-oxo-1,5,6,7-tetrahydro-indolyl, 9H-xanthenyl, cinnolyl, imidazolyl, morpholino, pyrimidyl, pyrrolidyl, tetrahydro-thienyl, benzofuranyl, or benzothiazolyl;
halogen is fluoro, chloro, bromo, or iodo;
or a salt thereof.
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5. A compound according to claim 4, wherein
R1 represents (i) C1-C5 alkyl substituted by substituent(s) independently selected from oxo, di-propylaminocarbonyl, methoxy substituted by carbocyclic aryl, methylcarbonyloxy, carbocyclic aryloxy, halogenated carbocyclic aryloxy, carbocyclic aryloxy substituted by nitro, heterocyclyloxy substituted by methyl, substituted heterocyclyl-ethylideneaminooxy, tert-butoxycarbonylamino, carbocyclic arylcarbonylamino, C1-C2 alkylthio, C1-C2 alkylthio substituted by substituent(s) independently selected from halogenated carbocyclic aryl, carbocyclic aryl substituted by methoxy, carbocyclic arylthio, hetrocyclylthio substituted by nitro, hetrocyclylthio substituted by methyl, cyclohexenyl, carbocyclyl substituted by substituent(s) independently selected from halogen, methyl, methoxy, ethenyl substituted by carbocyclic aryl substituted methylsulfinyl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, hydroxy, nitro, C1-C4 alkyl, C1-C4 alkyl substituted by substituent(s) independently selected from oxo, carbocyclic aryl, heterocyclyl, C1-C2 alkoxy, halogenated C1-C2 alkoxy, C1-C2 alkoxy substituted by carbocyclic aryl, carbocyclic aryloxy, halogenated mono-carbocyclic arylaminocarbonyl, carbocyclic aryl, heterocyclyl, heterocyclyl substituted by substituent(s) independently selected from C1-C2 alkyl, C1-C2 substituted by carbocyclic aryl, methoxy, methoxy substituted by carbocyclic aryl, carbocyclic aryl, halogenated carbocyclic aryl, (ii) C2-C3 alkenyl substituted by substituent(s) independently selected from carbocyclic aryl, halogenated carbocyclic aryl, carbocyclic aryl substituted by nitro, (iii) C3-C6 cycloalkyl substituted by substituent(s) independently selected from methyl substituted by oxo, methyl substituted by carbocyclic aryl, carbocyclic aryl, (iv) carbocyclyl, (v) carbocyclic aryl substituted by substituent(s) independently selected from halogen, hydroxy, cyano, nitro, C1-C4 alkyl, C1-C2 alkyl substituted by substituent(s) independently selected from halogen, oxo, carbocyclic aryl, carbocyclic aryl substituted by methyl, carbocyclic aryloxy, C1-C2 alkoxy, halogenated C1-C2 alkoxy, C1-C2 alkoxy substituted by carbocyclic aryl, methylcarbonyloxy, carbocyclic aryloxy, carbocyclic aryloxy substituted by methoxy, amino, di-methylamino, propargynylcarbonylamino substituted by carbocyclic aryl, carbocyclic arylsulfonylamino substituted by methyl, (carbocyclic aryl)NHC(O)NH substituted by halogenated methoxy, halogenated methylthio, carbocyclic arylthio substituted by cyano, di-propylamino sulfonyl, mono- or di-ethylaminocarbonyl substituted by carbocyclic aryl, carbocyclic aryl, heterocyclyl substituted by methyl, heterocyclyl substituted by halogenated carbocyclic aryl, (vi) or heterocyclyl substituted by substituent(s) independently selected from halogen, nitro, C1-C4 alkyl, C1-C4 alkyl substituted by substituent(s) independently selected from halogen, methylthio substituted by halogenated carbocyclic aryl, carbocyclic aryl, halogenated carbocyclic aryl, heterocyclyl, methoxy, carbocyclic aryloxy, carbocyclic aryloxy substituted by methyl, C1-C3 alkylthio, propenylthio, carbocyclic arylthio, C1-C3 alkylsulfonyl, carbocyclic arylsulfonyl, carbocyclic arylsulfonyl substituted by methyl, carbocyclic aryl, halogenated carbocyclic aryl, carbocyclic aryl substituted by methyl, carbocyclic aryl substituted by nitro, heterocyclyl; -
wherein carbocyclic aryl is phenyl, naphthyl, or biphenyl;
carbocyclyl is 1-oxo-indanyl, indenyl, 9-oxo-fluorenyl, 1,2,3,4-tetrahydro-naphthyl, or bicyclo[2.2.1]heptenyl;
heterocyclyl is 1H-indolyl, 2,4-dihydro-3-oxo-pyrazolyl, furyl, pyrazolyl, pyridyl, thienyl, 1,2,3-triazolyl, 1H-pyrrolyl, 2,3-dihydro-1-oxo-isoindolyl, 2,3-dihydro-benzofuryl, 2H-benzopyranyl, 2-oxo-benzopyranyl, 4-oxo-1,5,6,7-tetrahydro-indolyl, imidazolyl, isoxazolyl, morpholino, morpholinyl, pyrazolyl, pyrimidyl, quinolyl, thiazolyl, tetrahydro-thienyl, benzofuranyl, or benzothiazolyl;
halogen is fluoro, chloro, bromo, or iodo;
or a salt thereof.
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6. A compound according to claim 5 of Formula I selected from the group consisting of
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7. A compound according to claim 3, wherein
R1 represents (i) C1-C10 alkyl, C1-C10 alkyl substituted by substituent(s) independently selected from C5-C6 cycloalkyl, carbocyclic aryl, heterocyclyl, (ii) C3-C6 cycloalkyl, (iii) carbocyclic aryl, (iv) or heterocyclyl; -
L is selected from Formula XX-XXII;
wherein carbocyclic aryl is phenyl, naphthyl, anthranyl, or biphenyl;
heterocyclyl is 1,3-dioxo-isoindolyl, 1H-indolyl, 1-oxo-3H-isobenzofuranyl, 2,3-dihydro-benzo[1,4]dioxinyl, 3,4-dihydro-2H-benzo[b] [1,4]dioxepinyl, 4-oxo-3,4-dihydro-phthalazinyl, 9,10,10-trioxo-thioxanthenyl, 9H-xanthenyl, benzimidazolyl, benzo[1,3]dioxolyl, benzo[2,1,3]oxadiazolyl, benzo[b]thienyl, furyl, imidazolyl, isoxazolyl, morpholino, oxolanyl, piperidyl, pyridyl, quinoxalyl, thienyl, quinolyl, or benzothiazolyl;
or a salt thereof.
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8. A compound according to claim 7, wherein
R1 represents (i) C1-C4 alkyl, C1-C4 alkyl substituted by substituent(s) independently selected from cyclopentyl, carbocyclic aryl, heterocyclyl, (ii) carbocyclic aryl, (iii) or heterocyclyl; -
wherein carbocyclic aryl is phenyl, naphthyl, anthranyl, or biphenyl;
heterocyclyl is 9H-xanthenyl, benzo[1,3]dioxolyl, benzo[2,1,3]oxadiazolyl, benzo[b]thienyl, thienyl, 1H-indolyl, quinoxalyl, quinolyl, or benzothiazolyl;
or a salt thereof.
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9. A compound according to claim 8 of Formula I thereof selected from the group consisting of
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10. A compound according to claim 1, wherein Q is Formula II;
-
R1 represents (i) C1-C10 alkyl, C1-C10 alkyl substituted by substituent(s) independently selected from halogen, hydroxy, oxo, C1-C3 alkoxy, C1-C3 alkoxy substituted by substituent(s) independently selected from carbocyclic aryl, heterocyclyl, heterocyclyl substituted by C1-C3 alkyl, carbocyclic aryloxy, carbocyclic aryloxy substituted by substituent(s) independently selected from halogen, nitro, carbocyclic aryl, carbocyclic aryl substituted by C1-C3 alkoxy, C1-C4 alkyl, C1-C4 alkyl substituted by substituent(s) independently selected from mono- or di-C1-C3 alkylamino, mono- or di-C1-C3 alkylamino substituted by carbocyclic aryl, mono- or di-C1-C3 alkylamino substituted by halogenated carbocyclic aryl, mono- or di-C1-C3 alkylamino, mono- or di-C1-C3 alkylamino substituted by substituent(s) independently selected from cyano, carbocyclic aryl, heterocyclyl, mono- or di-carbocyclic arylamino, mono- or di-carbocyclic arylamino substituted by C1-C3 alkyl, C1-C3 alkylcarbonylamino, C1-C4 alkoxycarbonylamino, carbocyclic arylsulfonylamino, carbocyclic arylsulfonylamino substituted by substituent(s) independently selected from nitro, C1-C3 alkyl, mono- or di-C1-C3 alkylamino, C1-C3 alkylthio, C1-C3 alkylthio substituted by substituent(s) independently selected from mono- or di-carbocyclic arylamino, halogenated mono- or di-carbocyclic arylamino, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, C1-C3 alkoxy, carbocyclic arylthio, carbocyclic arylthio substituted by substituent(s) independently selected from halogen, C1-C3 alkyl, carbocyclic arylsulfonyl, halogenated carbocyclic arylsulfonyl, heterocyclylthio, C3-C6 cycloalkyl, C3-C6 cycloalkyl substituted by C1-C3 alkyl, carbocyclyl, carbocyclyl substituted by substituent(s) independently selected from halogen, C1-C3 alkyl, C2-C3 alkenyl, C2-C3 alkenyl substituted by carbocyclic aryl, C2-C3 alkenyl substituted by carbocyclic aryl substituted C1-C3 alkylsulfinyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, hydroxy, nitro, C1-C4 alkyl, C1-C4 alkyl substituted by substituent(s) independently selected from halogen, hydroxy, carbocyclic aryl, mono- or di-carbocyclic arylamino, mono- or di-carbocyclic arylamino substituted by substituent(s) independently selected from
halogen,
nitro,
C1-C3 alkyl,
C1-C3 alkoxy,
halogenated C1-C3 alkoxy,C1-C3 alkoxy, C1-C3 alkoxy substituted by substituent(s) independently selected from halogen, carbocyclic aryl, carbocyclic aryloxy, C1-C3 alkoxycarbonyl, mono- or di-C1-C3 alkylamino, C1-C3 alkylthio, halogenated C1-C3 alkylthio, C1-C3 alkylsulfonyl, C3-C6 cycloalkyl, carbocyclic aryl, heterocyclyl, heterocyclyl, heterocyclyl substituted by substituent(s) independently selected from C1-C3 alkyl, C1-C3 alkoxy, C1-C3 alkoxy substituted by carbocyclic aryl, carbocyclic aryl, halogenated carbocyclic aryl, (ii) C2-C8 alkenyl, C2-C8 alkenyl substituted by substituent(s) independently selected from halogen, C1-C3 alkoxy, C1-C3 alkoxy substituted by carbocyclic aryl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, hydroxy, C1-C3 alkoxy, halogenated C1-C3 alkoxy, heterocyclyl, heterocyclyl substituted by nitro, (iii) C2-C4 alkynyl, C2-C4 alkynyl substituted by carbocyclic aryl, (iv) C3-C6 cycloalkyl, C3-C6 cycloalkyl substituted by substituent(s) independently selected from C1-C3 alkyl, C1-C3 alkyl substituted by substituent(s) independently selected from hydroxy, oxo, carbocyclic aryl, mono- or di-C1-C3 alkylamino, mono- or di-C1-C3 alkylamino substituted by carbocyclic aryl, carbocyclic aryl, (v) C3-C6 cycloalkenyl, C3-C6 cycloalkenyl substituted by C1-C3 alkyl, (vi) carbocyclyl, carbocyclyl substituted by substituent(s) independently selected from hydroxy, nitro, (vii) carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, hydroxy, cyano, nitro, C1-C9 alkyl, C1-C9 alkyl substituted by substituent(s) independently selected from halogen, hydroxy, oxo, C1-C3 alkoxy, carbocyclic aryloxy, mono- or di-C1-C3 alkylamino-N-oxy, mono- or di-C1-C3 alkylamino, mono- or di-C1-C3 alkylamino substituted by carbocyclic aryl, mono- or di-carbocyclic arylamino, mono- or di-carbocyclic arylamino substituted by C1-C3 alkoxy, carbocyclic aryl, halogenated carbocyclic aryl, heterocyclyl, heterocyclyl substituted by C1-C3 alkyl, C2-C3 alkenyl, C2-C3 alkenyl substituted by carbocyclic aryl, C1-C9 alkoxy, C1-C9 alkoxy substituted by substituent(s) independently selected from hydroxy, halogen, carboxy, mono- or di-C1-C3 alkylamino, carbocyclic aryl, halogenated carbocyclic aryl, heterocyclyl, heterocyclyl substituted by substituent(s) independently selected from heterocyclyl, heterocyclyl substituted by substituent(s) independently selected from
halogen,
C1-C3 alkyl,
halogenated C1-C3 alkyl,C2-C3 alkenyloxy, C1-C3 alkylcarbonyloxy, carbocyclic aryloxy, carbocyclic aryloxy substituted by substituent(s) independently selected from halogen, C1-C4 alkyl, halogenated C1-C4 alkyl, C1-C3 alkoxy, heterocyclyloxy, heterocyclyloxy substituted by substituent(s) independently selected from halogen, C1-C3 alkyl, halogenated C1-C3 alkyl, (carbocyclic aryl)S(O)2O, carboxy, C1-C3 alkoxycarbonyl, mono- or di-C1-C3 alkylaminocarbonyl, mono- or di-C1-C3 alkylaminocarbonyl substituted by carbocyclic aryl, amino, mono- or di-C1-C4 alkylamino, mono- or di-C1-C4 alkylamino substituted by cyano, mono- or di-carbocyclic arylamino, C1-C3 alkylcarbonylamino, carbocyclic arylsulfonylamino, carbocyclic arylsulfonylamino substituted by C1-C3 alkyl, (carbocyclic aryl)NHC(O)NH, (carbocyclic aryl)NHC(O)NH substituted by C1-C3 alkoxy, (carbocyclic aryl)NHC(O)NH substituted by haloganated C1-C3 alkoxy, C1-C3 alkylthio, halogenated C1-C3 alkylthio, carbocyclic arylthio, halogenated carbocyclic arylthio, carbocyclic arylthio substituted by C1-C3 alkyl, heterocyclylthio, C1-C3 alkylsulfonyl, mono- or di-C1-C3 alkylaminosulfonyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from C1-C7 alkyl, halogenated C1-C7 alkyl, heterocyclyl, heterocyclyl substituted by substituent(s) independently selected from C1-C3 alkyl, carbocyclic aryl, halogenated carbocyclic aryl, (viii) heterocyclyl, or heterocyclyl substituted by substituent(s) independently selected from halogen, hydroxy, cyano, nitro, C1-C4 alkyl, C1-C4 alkyl substituted by substituent(s) independently selected from halogen, hydroxy, oxo, C1-C3 alkylcarbonyloxy, C1-C3 alkoxycarbonyl, C1-C3 alkylthio, C1-C3 alkylthio substituted by carbocyclic aryl, C1-C3 alkylthio substituted by halogenated carbocyclic aryl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, nitro, heterocyclyl, C1-C3 alkoxy, C1-C3 alkoxy substituted by carbocyclic aryl, carbocyclic aryloxy, carbocyclic aryloxy substituted by C1-C3 alkyl, mono- or di-C1-C3 alkylamino, C1-C4 alkylcarbonylamino, C1-C3 alkylthio, carbocyclic arylthio, halogenated carbocyclic arylthio, carbocyclic arylthio substituted by C1-C3 alkoxycarbonyl, heterocyclylthio, heterocyclylthio substituted by C1-C3 alkyl, C1-C3 alkylsulfonyl, carbocyclic arylsulfonyl, carbocyclic arylsulfonyl substituted by C1-C4 alkyl, C1-C3 alkoxycarbonyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, nitro, C1-C3 alkyl, halogenated C1-C3 alkyl, C1-C3 alkoxy, halogenated C1-C3 alkoxy, heterocyclyl, heterocyclyl substituted by substituent(s) independently selected from C1-C3 alkyl, halogenated C1-C3 alkyl, C1-C3 alkoxy, C1-C3 alkoxycarbonyl;
Y is —
(CH2)m, m is 0 or 1;
wherein carbocyclic aryl is phenyl, naphthyl, biphenyl, or phenanthryl;
carbocyclyl is 9H-fluorenyl, 9-oxo-fluorenyl, acenaphthyl, anthraquinonyl, indanyl, or indenyl;
heterocyclyl is 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2-dihydro-3-oxo-pyrazolyl, 1,3,4-thiadiazolyl, 1,3-dioxo-isoindolyl, 1,3-dioxolanyl, 1H-indolyl, 1H-pyrrolo[2,3-c]pyridyl, 1H-pyrrolyl, 2,2′
,5′
,2″
-terthiophenyl, 2,2′
-bithiophenyl, 2,3-dihydro-1-oxo-isoindolyl, 2,3-dihydro-benzo[1,4]dioxinyl, 2,3-dihydro-benzofuryl, 2,4-dihydro-3-oxo-pyrazolyl, 2H-benzopyranyl, 2-oxo-pyrrolidinyl, 3,4-dihydro-2H-benzo[1,4]oxazinyl, 3,4-dihydro-2H-benzo[b] [1,4]dioxepinyl, 4H-benzo[1,3]dioxinyl, 4H-benzopyranyl, 4-oxo-1,5,6,7-tetrahydro-indolyl, 4-oxo-benzopyranyl, 9H-carbazolyl, 9H-xanthenyl, azetidinyl, benzimidazolyl, benzo[1,3]dioxolyl, benzo[b]thienyl, benzofuryl, benzothiazolyl, furyl, imidazo[2,1-b]thiazolyl, imidazolyl, isoxazolyl, morpholino, morpholinyl, oxolanyl, piperazyl, piperidyl, pyrazolo[5,1-b]thiazolyl, pyrazolyl, pyridyl, pyrimidyl, pyrrolidyl, quinolyl, quinoxalyl, thiazolidyl, thiazolyl, thienyl, or thiolanyl;
halogen is fluoro, chloro, bromo, or iodo;
or a salt thereof.
-
-
11. A compound according to claim 10, wherein
R1 represents (i) C1-C10 alkyl substituted by substituent(s) independently selected from methoxy, methoxy substituted by carbocyclic aryl, carbocyclic aryloxy, halogenated carbocyclic aryloxy, mono-C1-C2 alkylamino substituted by cyano, mono- or di-C1-C2 alkylamino substituted by carbocyclic aryl, mono-carbocyclic arylamino, mono-carbocyclic arylamino substituted by methyl, carbocyclic arylsulfonylamino substituted by methyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, nitro, C1-C4 alkyl, C1-C4 alkyl substituted by carbocyclic aryl, C1-C4 alkyl substituted by hydroxy, C1-C2 alkoxy, halogenated C1-C2 alkoxy, heterocyclyl substituted by carbocyclic aryl, (ii) C2-C8 alkenyl substituted by substituent(s) independently selected from methoxy substituted by carbocyclic aryl, carbocyclic aryl, carbocyclic aryl substituted by methoxy, (iii) C2-C4 alkynyl substituted by carbocyclic aryl, (iv) cyclohexyl substituted by carbocyclic arylmethyl, (v) carbocyclyl, (vi) carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, hydroxy, cyano, amino, C1-C9 alkyl, halogenated C1-C9 alkyl, C1-C9 alkoxy, C1-C9 alkoxy substituted by substituent(s) independently selected from halogen, halogenated carbocyclic aryl, propenyloxy, methylamino, di-C1-C2 alkylamino, di-C1-C2 alkylamino substituted by cyano, methylthio, halogenated methylthio, (vii) heterocyclyl, or heterocyclyl substituted by substituent(s) independently selected from halogen, C1-C4 alkyl, C1-C4 alkyl substituted by hydroxy, C1-C4 alkyl substituted by carbocyclic aryl, methoxy, C1-C2 alkoxycarbonyl, carbocyclic arylthio substituted by methoxycarbonyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, halogenated methyl, heterocyclyl; -
R2 is methylamino or dimethylamino;
L is selected from Formula Va, VIIIa, or IXa;
wherein carbocyclic aryl is phenyl, naphthyl, biphenyl, or phenanthryl;
carbocyclyl is 9H-fluorenyl, acenaphthyl, or anthraquinonyl;
heterocyclyl is 1,2,3-thiadiazolyl, 1,2,3-triazolyl, 1,2-dihydro-3-oxo-pyrazolyl, 1,3-dioxolanyl, 1H-indolyl, 1H-pyrrolyl, 2,2′
,5′
,2″
-terthiophenyl, 2,2′
-bithiophenyl, 2,3-dihydro-benzo[1,4]dioxinyl, 3,4-dihydro-2H-benzo[1,4]oxazinyl, 4-oxo-benzopyranyl, 9H-carbazolyl, 9H-xanthenyl, benzimidazolyl, benzo[1,3]dioxolyl, benzo[b]thienyl, benzofuryl, benzothiazolyl, furyl, imidazolyl, isoxazolyl, oxolanyl, pyrazolo[5,1-b]thiazolyl, pyrazolyl, pyridyl, pyrimidyl, quinolyl, quinoxalyl, thiazolidyl, thiazolyl, thienyl, 2H-benzopyranyl, 4H-benzo[1,3]dioxinyl, azetidinyl, imidazo[2,1-b]thiazolyl, morpholinyl, or 2,3-dihydro-benzofuryl;
halogen is fluoro, chloro, bromo, or iodo;
or a salt thereof.
-
-
12. A compound according to claim 11, wherein
R1 represents (i) C1-C7 alkyl substituted by substituent(s) independently selected from methoxy, methoxy substituted by carbocyclic aryl, carbocyclic aryloxy, halogenated carbocyclic aryloxy, mono-ethylamino substituted by cyano, di-methylamino substituted by carbocyclic aryl, mono-carbocyclic arylamino, mono-carbocyclic arylamino substituted by methyl, carbocyclic arylsulfonylamino substituted by methyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, nitro, C1-C4 alkyl, C1-C4 alkyl substituted by carbocyclic aryl, C1-C4 alkyl substituted by hydroxy, metoxy, halogenated methoxy, heterocyclyl substituted by carbocyclic aryl, (ii) C2-C7 alkenyl substituted by substituent(s) independently selected from methoxy substituted by carbocyclic aryl, carbocyclic aryl, carbocyclic aryl substituted by methoxy, (iii) butynyl substituted by carbocyclic aryl, (iv) cyclohexyl substituted by carbocyclic arylmethyl, (v) carbocyclyl, (vi) carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, hydroxy, cyano, amino, C1-C2 alkyl, halogenated methyl, C1-C3 alkoxy, C1-C3 alkoxy substituted by substituent(s) independently selected from halogen, halogenated carbocyclic aryl, propenyloxy, di-C1-C2 alkylamino, di-C1-C2 alkylamino substituted by cyano, methylthio, halogenated methylthio, (vii) heterocyclyl, or heterocyclyl substituted by substituent(s) independently selected from halogen, C1-C3 alkyl, C1-C3 alkyl substituted by hydroxy, C1-C3 alkyl substituted by carbocyclic aryl, methoxy, ethoxycarbonyl, carbocyclic arylthio substituted by methoxycarbonyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, halogenated methyl, heterocyclyl; -
L is selected from Formula XX-XXII;
wherein carbocyclic aryl is phenyl, naphthyl, or biphenyl;
carbocyclyl is acenaphthyl;
heterocyclyl is 1H-indolyl, 1H-pyrrolyl, 2,3-dihydro-benzo[1,4]dioxinyl, 9H-carbazolyl, benzo[1,3]dioxolyl, furyl, pyrazolyl, thienyl, 4-oxo-benzopyranyl, azetidinyl, imidazo[2,1-b]thiazolyl, pyridyl, imidazolyl, 2,3-dihydro-benzofuryl, or benzo[b]thienyl;
halogen is fluoro, chloro, bromo, or iodo;
or a salt thereof.
-
-
13. A compound according to claim 12 of Formula I selected from the group consisting of
-
14. A compound according to claim 1, wherein Q is Formula II;
-
R1 represents (i) C1-C16 alkyl, C1-C16 alkyl substituted by substituent(s) independently selected from halogen, carbocyclyl, carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, nitro, C1-C3 alkyl, halogenated C1-C3 alkyl, C1-C3 alkoxy, halogenated C1-C3 alkoxy, (ii) C2-C3 alkenyl, C2-C3 alkenyl substituted by carbocyclic aryl, (iii) carbocyclic aryl, carbocyclic aryl substituted by substituent(s) independently selected from halogen, cyano, nitro, C1-C5 alkyl, C1-C5 alkyl substituted by substituent(s) independently selected from halogen, oxo, C2-C3 alkenyl, C1-C4 alkoxy, C1-C4 alkoxy substituted by substituent(s) independently selected from halogen, heterocyclyl, halogenated heterocyclyl, carbocyclic aryloxy, carbocyclic aryloxy substituted by substituent(s) independently selected from halogen, nitro, heterocyclyloxy, heterocyclyloxy substituted by substituent(s) independently selected from halogen, C1-C3 alkyl, halogenated C1-C3 alkyl, C1-C3 alkoxycarbonyl, mono- or di-C1-C4 alkylamino, C1-C3 alkylcarbonylamino, carbocyclic aryl diazo, carbocyclic aryl diazo substituted by mono- or di-C1-C3 alkylamino, C1-C3 alkylsulfonyl, carbocyclic aryl, (iv) heterocyclyl, or heterocyclyl substituted by substituent(s) independently selected from halogen, C1-C3 alkyl, C1-C3 alkyl substituted by substituent(s) independently selected from halogen, oxo, carbocyclic arylcarbonylamino, halogenated carbocyclic arylcarbonylamino, heterocyclyl, heterocyclyl substituted by substituent(s) independently selected from halogen, C1-C3 alkyl, halogenated C1-C3 alkyl, C1-C3 alkoxy, C1-C3 alkylcarbonylamino, carbocyclic arylsulfonyl, C1-C3 alkoxycarbonyl, carbocyclic aryl, halogenated carbocyclic aryl, heterocyclyl, heterocyclyl substituted by substituent(s) independently selected from halogen, C1-C3 alkyl, halogenated C1-C3 alkyl;
Y is —
S(O)2—
;
wherein carbocyclic aryl is phenyl, biphenyl, or naphthyl;
carbocyclyl is 7,7-dimethyl-2-oxo-bicyclo[2.2.1]heptyll;
heterocyclyl is 1,2,3,4-tetrahydro-isoquinolyl, 1,2,3-thiadiazolyl, 1H-pyrrolyl, benzo[2,1,3]oxadiazolyl, benzo[b]thienyl, furyl, imidazolyl, isoxazolyl, pyrazolyl, pyridyl, quinolyl, thiazolyl, or thienyl;
halogen is fluoro, chloro, bromo, or iodo;
or a salt thereof.
-
-
15. A compound according to claim 14 of Formula I selected from the group consisting of
-
16. A compound according to claim 1, wherein Q is Formula II;
-
R1 is selected from H, —
CO2tBu, or —
CO2Bn (Bn is a benzyl group);
R2 is methyl amino or dimethylamino;
L is selected from Formula XX-XXII;
Y is a single bond;
or a salt thereof.
-
-
18. A method for modulating the G-protein receptor, SLC-1, comprising the step of contacting said SLC-1 with a compound of any one of claims 1-16.
-
19. A method of prophylaxis or treatment of obesity, obesity related disorders, anxiety, or depression in mammals in need of such treatment comprising administering to the mammal a therapeutically effective amount of a compound having the composition of any one of claims 1-16.
-
20. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound, or a salt thereof, of any one of claims 1-16.
-
2. A compound according to claim 1, wherein Q is Formula II;
-
17. A method for modulating the G-protein receptor, SLC-1, comprising the step of contacting said SLC-1 with a MCH receptor antagonist.
Specification
- Resources
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Current AssigneeTaisho Pharmaceutical Company Limited (Taisho Pharmaceutical Holdings Company Limited)
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Original AssigneeTaisho Pharmaceutical Company Limited (Taisho Pharmaceutical Holdings Company Limited)
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InventorsTran, Thuy-Anh, Sekiguchi, Yoshinori, Kanuma, Kosuke, Omodera, Katsunori, Kramer, Bryan, Beeley, Nigel
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Granted Patent
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Time in Patent OfficeDays
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Field of Search
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US Class Current514/266.200
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CPC Class CodesA61P 25/22 AnxiolyticsA61P 25/24 AntidepressantsA61P 3/04 Anorexiants; Antiobesity ag...A61P 43/00 Drugs for specific purposes...C07D 239/95 with hetero atoms directly ...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 409/12 linked by a chain containin...C07D 413/12 linked by a chain containin...C07D 417/12 linked by a chain containin...