PYRAZOLOPYRIMIDINES AS CRF RECEPTOR ANTAGONISTS
This invention concerns compounds of formula 1 including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R 1 is NR 4 R 5 or OR 5 ; R 2 is C 1-6 alkyl, C 1-6 alkyloxy or C 1-6 alkylthio; R 3 is hydrogen, C 1-6 alkyl, C 1-6 alkylsulfonyl, C 1-6 alkylsulf...
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Format: | Patent |
Sprache: | eng |
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Zusammenfassung: | This invention concerns compounds of formula
1
including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R
1
is NR
4
R
5
or OR
5
; R
2
is C
1-6
alkyl, C
1-6
alkyloxy or C
1-6
alkylthio; R
3
is hydrogen, C
1-6
alkyl, C
1-6
alkylsulfonyl, C
1-6
alkylsulfoxy or C
1-6
alkylthio; R
4
is hydrogen, C
1-6
alkyl, mono- or di(C
3-6
cycloalkyl)methyl, C
3-6
cycloalkyl, C
3-6
alkenyl, hydroxyC
1-6
alkyl, C
1-6
alkylcarbonyloxyC
1-6
alkyl or C
1-6
alkyloxyC
1-6
alkyl; R
5
is C
1-8
alkyl, mono- or di(C
3-6
cycloalkyl)methyl, Ar
1
CH
2
, C
1-6
alkyloxyC
1-6
alkyl, hydroxyC
1-6
alkyl, C
3-6
alkenyl, thienylmethyl, furanylmethyl, C
1-6
alkylthioC
1-6
alkyl, morpholinyl, mono- or di(C
1-6
alkyl)aminoC
1-6
alkyl, di(C
1-6
alkyl)amino, C
1-6
alkylcarbonylC
1-6
alkyl, C
1-6
alkyl substituted with imidazolyl; or a radical of formula -Alk-O-CO-Ar
1
; or R
4
and R
5
taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I). |
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