Patent ID: 6303312
Filing Date: 2001-10-16
Classification: A61K,A61P,C07D,C07K,C12N

Abstract:
A method for inhibiting transcription of a gene in an organism, said method comprising:administering to said organism, one or more oligomers selected to provide specific binding either singly or in pairs to a target dsDNA in a minor groove target site of said dsDNA,wherein each of said oligomers comprises organic cyclic groups of from 5 to 6 annular members, where at least 60% of the groups are heterocycles having from 1 to 3 heteroatoms, where the heteroatoms are nitrogen, oxygen and sulfur, and wherein at least 60% of the heterocycles have at least one nitrogen atom, and said heterocycles are linked by chains of 2 atoms, wherein at least some of the chains have NH,wherein at least one of said oligomers has at least 7 of said nitrogen containing heterocycles, where at least one of said heterocycles is specific for A, G, C or T, and a pair of heterocycles refers to two heterocycles paired to a complementary pair of nucleotides in said dsDNA,each oligomer comprising at least two units of 2 consecutive heterocycles which form, at the target site, intramolecular pairs of heterocycles with itself or intermolecular pairs of heterocycles with another oligomer,where when an oligomer forms intramolecular pairs, said oligomer comprises an internal molecule which shifts the spacing of the heterocycles or forms a hairpin turn, andwhen two oligomers form intermolecular pairs, each oligomer comprises an internal aliphatic amino acid of from 2 to 6 carbon atoms, where said internal aliphatic amino acid is paired with an A or T; andeach of said oligomers comprising at least one terminus, an aliphatic amino acid of from 2 to 6 carbon atoms or an alkyl chain comprising a polar group 2 to 4 carbon atoms from the bond linking said alkyl chain to the remainder of each oligomer,where each oligomer has one or more hydrogen atoms away from the surface of said minor groove target site which may be substituted, wherein the total number of carbon atoms of substituents is not more than 100 carbon atoms; andwherein said target dsDNA is all or part of a target gene; andsaid 1 or more oligomers bind to said target site, inhibiting transcription of said gene in said organism.