Imidazoline receptor binding compounds
AssigneeThe University of North Carolina at Chapel Hill
InventorsRichard R. Tidwell, James E. Hall, Dorothy H. Wood
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Abstract
Pentamidine and analogs thereof have activity as imidazoline receptor binding compounds. A method of binding the imidazoline receptor, comprises contacting a bis-benzene to said imidazoline receptor in an amount effective to bind to said receptor, wherein said bis-benzene contains at least one amidine group (e.g., one or two). The contacting step may be carried out in vivo or in vitro. Contacting may be carried out with individual active compounds or with libraries of active compounds.
Claims8
A method of binding the imidazoline receptor, comprising:
- contacting a bis-benzene to said imidazoline receptor in an amount effective to bind to said receptor, wherein said bis-benzene contains at least one amidine group, wherein said contacting step is carried out in vivo by administering said compound to a subject afflicted with a disease state which is alleviable by treatment with a compound having high selectivity and affinity for the imidazoline receptor site.
A method according to claim wherein said bis-benzamidine has the formula (V):
- wherein:
- A and B are each independently selected from the group consisting of H, loweralkyl, oxyalkyl, nitro, amino, aminoalkyl, halo, hydroxy, carboxy, and compounds of formula (ii):
- subject to the proviso that at least one of A and B is a substituent of formula (ii);
- R1 and R2 are each independently selected from the group consisting of H, loweralkyl, aryl, alkylaryl, aminoaryl, halogen, oxyalkyl, oxyaryl, or oxyarylalkyl;
- R3 and R4 are each independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkylaryl, aryl, oxyaryl, aminoalkyl, aminoaryl, or halogen;
- and
- each R5 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl or two R5 groups together represent C2 to C10 alkyl, hydroxyalkyl, or alkylene;
- and
- R6 is H, hydroxy, loweralky, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylamino, alkylaminoalkyl, cycloalkyl, hydroxycycloalkyl, alkoxycycloalkyl, aryl, or alkylaryl;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.