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US 6,440,969 B2Granted
Certain isoquinolinamine and phthalazinamine derivatives: corticotropin-releasing factor receptor CRF1 specific ligands
AssigneeNeurogen Corporation
InventorsJun Yuan, Taeyoung Yoon
Life of this patent
Estimating the term…
Abstract
Disclosed are compounds that are highly selective partial agonists or antagonists at human CRF1 receptors that 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. The compounds have the formula or the pharmaceutically acceptable salts thereof wherein Ar, R1, R2, R3, R4 and W are various organic and inorganic substituents.
Claims18
A pharmaceutical composition comprising a compound of the formula:
- or the pharmaceutically acceptable salts thereof wherein
- Ar is phenyl, 1- or 2- naphthyl, 2-, 3-, or 4-pyridinyl, 2- or 3- thienyl, or 4- or 5-pyrimidinyl, each of which is mono-, di-, or trisubstituted with halogen, hydroxy, C1-C6 alkyl, or C1-C6 alkoxy, with the proviso that at least one of the positions on Ar ortho to the point of attachment to the nitrogen-containing 8-membered aromatic ring is substituted;
- R1 and R2 are the same or different and represent hydrogen, C1-C6 alkyl, halogen, hydroxy, C1-C6 alkoxy, NH2, NH(C1-C6 alkyl), N(C1-C6 alkyl)2, NO2, cyano, trifluoromethyl;
- R3 and R4 are the same or different and represent
- C1-C6 alkyl optionally substituted with halogen, hydroxy, or C1-C6 alkoxy;
- or
- C1-C6 alkylaryl, where aryl is phenyl, 1-or 2-naphthyl, 2-, 3-, or 4-pyridinyl, 2- or 3- thienyl or 2-, 4-, or 5-pyrimidinyl, each of which is optionally mono- or disubstituted with halogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy;
- or C1-C6 alkyl-Y-R5, wherein Y is O, S NH, N(C1-C6 alkyl), and R5 is hydrogen or C1-C6 alkyl;
- together with a pharmaceutically acceptable carrier, adjuvant, or vehicle.
6 more elements
A pharmaceutical composition comprising a compound of the formula:
- or the pharmaceutically acceptable salts thereof wherein
- Ar is phenyl mono, di-, or trisubstituted with halogen, hydroxy, C1-C6 alkyl, or C1-C6 alkoxy, with the proviso that at least one of the positions on Ar ortho to the point of attachment to the phthalazinamine ring is substituted;
- and
- R3 and R4 are the same or different and represent
- C1-C6 alkyl optionally substituted with halogen, hydroxy, or C1-C6 alkoxy;
- or
- C1-C6 alkylaryl, where aryl is phenyl, 1- or 2-naphthyl, 2-, 3-, or 4-pyridinyl, 2- or 3-thienyl or 2-, 4-, or 5-pyrimidinyl, each of which is optionally mono- or disubstituted with halogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy;
- or C1-C6 alkyl-Y-R5, wherein Y is O, S NH, N(C1-C6 alkyl), and R5 is hydrogen or C1-C6 alkyl;
- together with a pharmaceutically acceptable carrier, adjuvant, or vehicle.
6 more elements
Dependencies are inferred from the claim text.