7-phenylpyrazolopyridine compounds
A compound represented by the formula: [wherein R 1 is methoxy, methylthio, ethyl, etc.; R 5 and R 6 are each independently cyclopropylmethyl, (4-tetrahydropyranyl)methyl, etc.; and two of R 40 , R 41 and R 42 are C 1-6 alkoxy while the remaining one is methoxymethyl, etc.], a salt thereof, or a hydrate of the foregoing. This compound has excellent antagonism against corticotropin-releasing factor receptor.
1. A compound represented by the formula:
wherein R 1 is a group represented by the formula -G 1z -R 1z wherein G 1z is a single bond, oxygen or sulfur, and R 1z is methyl or ethyl or methoxymethyl;
R 5 and R 6 are each independently hydrogen, t-butoxycarbonyl or a group represented by the formula -X 6b -X 7b wherein X 6b is methylene and X 7b is C 1-6 alkyl, C 3-8 cycloalkyl, tetrahydropyran-yl or tetrahydrofuran-yl; and wherein R 40 and R 42 are each independently C 1-6 alkoxy, and R 41 is a group represented by the formula:
(wherein R 44 and R 45 are each independently hydrogen, methyl or ethyl; and R 43 is C 1-6 alkyl optionally substituted with 1 to 3 substituents selected from Substituent Group B below,
wherein Substituent Group B is the group consisting of fluorine atom, chlorine atom, bromine atom, cyano, C 1-6 alkoxy, pyrrolidinyl, piperazinyl, piperidyl, morpholinyl, C 3-8 cycloalkyl, tetrahydropyran-yl and tetrahydrofuran-yl),
a salt thereof or a hydrate of the foregoing.
2. A compound represented by the formula:
wherein R 5t and R 6t are each independently cyclopropylmethyl, (4-tetrahydropyranyl)methyl, (3-tetrahydrofuranyl)methyl or (2-tetrahydrofuranyl)methyl;
R 1t is methoxy, methylthio, methyl, ethyl or methoxymethyl; and
R 43t is C 1-6 alkyl,
a salt thereof or a hydrate of the foregoing.
3. A compound according to claim 2 , a salt thereof or a hydrate of the foregoing, wherein R 43t is methyl.
4. A compound according to claim 2 , a salt thereof or a hydrate of the foregoing, wherein R 1t is methoxy, methylthio or ethyl.
5. A compound according to claim 2 , a salt thereof or a hydrate of the foregoing, wherein R 5t is cyclopropylmethyl or (4-tetrahydropyranyl)methyl.
6. A compound according to claim 2 , a salt thereof or a hydrate of the foregoing, wherein R 5t is (4-tetrahydropyranyl)methyl.
7. A compound according to claim 2 , a salt thereof or a hydrate of the foregoing, wherein R 5t is (4-tetrahydropyranyl)methyl, and R 6t is cyclopropylmethyl.
8. A compound according to claim 1 , a salt thereof or a hydrate of the foregoing, wherein the compound is N-cyclopropylmethyl-N-7-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-2-ethylpyrazolo[1,5-a]pyridin-3-yl-N-tetrahydro-2H-4-pyranylmethylamine, N-cyclopropylmethyl-N-7-[4-(ethoxymethyl)-2,6-dimethoxyphenyl]-2-ethylpyrazolo[1,5-a]pyridin-3-yl-N-tetrahydro-2H-4-pyranylmethylamine or N-cyclopropylmethyl-N-[7-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-2-(methylsulfanyl)pyrazolo[1,5-a]pyridin-3-yl]-N-tetrahydro-2H-4-pyranylmethylamine.
9. A compound according to claim 1 , a salt thereof or a hydrate of the foregoing, wherein the compound is N-cyclopropylmethyl-N-7-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-2-ethylpyrazolo[1,5-a]pyridin-3-yl-N-tetrahydro-2H-4-pyranylmethylamine.
10. A corticotropin-releasing factor (CRF) receptor antagonist comprising a compound according to claim 1 or a salt thereof and pharmaceuticcally acceptable carrier.
11. A therapeutic method for treating at least one disease selected from the group consisting of depression, general anxiety disorder and anxiety, comprising administration of an effective amount of a compound according to claim 1 or a salt thereof for treating said disease.