3-aryl substituted pyrazolo[4,3-D]pyrimidine derivatives; corticotropin-releasing factor receptor (CRF1) specific ligands
AssigneeNeurogen Corporation
InventorJun Yuan
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Abstract
This invention encompasses compounds of the formula wherein Ar represents a mono-, di- or trisubstituted aryl group where at least one position on Ar ortho to the point of attachment to the pyrazole ring is substituted; and R1 represents lower alkyl; R2 is hydrogen or lower alkyl; and R3 and R4 independently represent organic and inorganic substituents, which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.
Claims16
A compound of the formula:
- or the pharmaceutically acceptable salts thereof wherein
- Ra, Rb, and Rc are all methyl;
- R1 and R2 independently represent lower alkyl;
- R3 and R4 are the same or different and represent hydrogen, C1-C4 alkyl, alkenyl, alkoxy lower alkyl, phenyl-lower alkyl where the phenyl is optionally substituted with lower alkyl, or
- R3 and R4 together represent —(CH2)n—A—(CH2)m— where
- n is 2 or 3 and m is 1, 2, or 3, and A is methylene,
- oxygen, or NR6 where R6 is lower alkyl, provided that not both R3 and R4 are hydrogen.
A compound of the formula:
- or the pharmaceutically acceptable salts thereof wherein
- Ra, Rb, and Rc are all methyl;
- R1 and R2 independently represent lower alkyl;
- R3 and R4 are the same or different and represent hydrogen, C1-C4 alkyl, alkenyl, alkoxy lower alkyl, phenyl-lower alkyl where the phenyl is optionally substituted with lower alkyl, or
- R3 and R4 together represent —(CH2)n—A—(CH2)m— where
- n is 2 or 3 and m is 1, 2, or 3, and A is methylene,
- oxygen, or NR6 where R6 is lower alkyl,
- provided that not both R3 and R4 are hydrogen.
Dependencies are inferred from the claim text.