Aromatic-linked polyamine macrocyclic compounds with anti-HIV activity
AssigneeGenzyme Corporation
InventorsGary J. Bridger, Sreenivasan Padmanbhan, Renato Skerlj, David M. Thornton
Life of this patent
Estimating the term…
Abstract
Polyamine macrocyclic compounds, e.g. of 10 to 15 ring members and 3 to 6 ring amine nitrogens, linked through methylene groups to an aromatic moiety, show high selective activity against HIV.
Claims52
A pharmaceutical composition active against HIV comprising as an active ingredient a linked cyclic compound of formula I,
- Z-R-A-R′-Y (I)
- in which Z and Y are identical cyclic polyamine moieties having from 10 to 15 ring members and from 3 to 6 4 amine nitrogens in the ring spaced by 2 or more carbon atoms from each other, said amine nitrogens being the only ring heteroatoms,
- A is an unsubstituted aromatic or heteroaromatic moiety other than quinoline,
- R and R′ are each methylene linked to nitrogen atoms in Z and Y,
- the amine nitrogen atoms being otherwise unsubstituted, in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 1,1′-[1,3-phenylenebis(methylene)]-bis-1,4,8,11-tetra-azacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 1,1′-[1,4-phenylenebis(methylene)]-bis-1,4,8,11-tetra-azacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 1,1′-[3,3′-biphenylene-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 11,11′-[1,4-phenylene-bis-(methylene)]-bis-1,4,7,11-tetraazacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 1,1′-[2,6-pyridine-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 1,1-[3,5-pyridine-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 1,1′-[2,5-thiophene-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 1,1′-[4,4′-(2,2′-bipyridine)-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 1,1′-[2,9-(1,10-phenanthroline)-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 1,1′-[1,3-phenylene-bis-(methylene)]-bis-1,4,7,10-tetraazacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 1,1′-[1,4-phenylene-bis-(methylene)]-bis-1,4,7,10-tetraazacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 1,1′-[5-nitro-1,3-phenylenebis(methylene)]bis-1,4,8,11-tetraazacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 1′1′-[2,4,5,6-tetrachloro-1,3-phenylenebis(methylene)]bis-1,4,8,11-tetraazacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 1,1′-[2,3,5,6-tetra-fluoro-1,4-phenylenebis(methylene)]bis-1,4,8,11-tetraazacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 1,1′-[1,4-naphthylene-bis-(methylene)]bis-1,4,8,11-tetraazacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 1,1′-[1,3-phenylenebis-(methylene)]bis-1,5,9-triazacyclododecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
A pharmaceutical composition active against HIV comprising as an active ingredient 1,1′-[1,4-phenylene-bis-(methylene)]-bis-1,5,9-triazacyclododecane in admixture or association with a pharmaceutically acceptable diluent or carrier.
Dependencies are inferred from the claim text.