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Claims for Patent: RE42152

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Claims for Patent: RE42152

Title:Aromatic-linked polyamine macrocyclic compounds with anti-HIV activity
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.
Inventor(s): Bridger; Gary J. (Bellingham, WA), Padmanbhan; Sreenivasan (Exton, PA), Skerlj; Renato (Newton, MA), Thornton; David M. (Reading, GB)
Assignee: Genzyme Corporation (Cambridge, MA)
Application Number:12/192,704
Patent Claims: 1. 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.]. .Iadd.4 .Iaddend.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 .Iadd.unsubstituted .Iaddend.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.Iadd., in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

2. A composition according to claim 1, wherein in the compound of formula I, each moiety Z and Y has 14 ring members and 4 amine nitrogens in the ring.

3. A .Iadd.pharmaceutical .Iaddend.composition .[.according to claim 1, wherein the.]. .Iadd.active against HIV comprising as an .Iaddend.active ingredient .[.is.]. 1,1'-[1,3-phenylenebis(methylene)]-bis-1,4,8,11-tetra-azacyclotetradecane in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

4. A .Iadd.pharmaceutical .Iaddend.composition .[.according to claim 1, wherein the.]. .Iadd.active against HIV comprising as an .Iaddend.active ingredient .[.is.]. 1,1'-[1,4-phenylenebis(methylene)]-bis-1,4,8,11-tetra-azacyclotetradecane in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

5. A .Iadd.pharmaceutical .Iaddend.composition .[.according to claim 1, wherein the.]. .Iadd.active against HIV comprising as an .Iaddend.active ingredient .[.is.]. a bis-zinc complex of 1,1'-[1,4-phenylene-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecan- e .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

6. A .Iadd.pharmaceutical .Iaddend.composition .[.according to claim 1, wherein the.]. .Iadd.active against HIV comprising as an .Iaddend.active ingredient .[.is.]. a bis-copper complex of 1,1'-[1,4-phenylene-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecan- e .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

7. A .Iadd.pharmaceutical .Iaddend.composition .[.according to claim 1, wherein the.]. .Iadd.active against HIV comprising as an .Iaddend.active ingredient .[.is.]. 1,1'-[3,3'-biphenylene-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetrade- cane in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

8. A .Iadd.pharmaceutical .Iaddend.composition .[.according to claim 1, wherein the.]. .Iadd.active against HIV comprising as an .Iaddend.active ingredient .[.is 11,11'-[1,4-phenylene-bis-(methylene)]-bis-1,4,7,11-tetraazacyclotetradec- ane.]. .Iadd.11,11'-[1,4-phenylene-bis-(methylene)]-bis-1,4,7,11-tetraazac- yclotetradecane .Iaddend.in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

9. A .Iadd.pharmaceutical .Iaddend.composition .[.according to claim 1, wherein the.]. .Iadd.active against HIV comprising as an .Iaddend.active ingredient .[.is.]. 1,11'-[1,4-phenylene-bis-(methylene)]-1,4,8,11-tetraazacyclotetradecane-1- ,4,7,11-tetraazacyclotetradecane in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

10. A .Iadd.pharmaceutical .Iaddend.composition .[.according to claim 1, wherein the.]. .Iadd.active against HIV comprising as an .Iaddend.active ingredient .[.is.]. 1,1'-[2,6-pyridine-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

11. A .Iadd.pharmaceutical .Iaddend.composition .[.according to claim 1, wherein the.]. .Iadd.active against HIV comprising as an .Iaddend.active ingredient .[.is.]. 1,1-[3,5-pyridine-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

12. A .Iadd.pharmaceutical .Iaddend.composition .[.according to claim 1, wherein the.]. .Iadd.active against HIV comprising as an .Iaddend.active ingredient .[.is.]. 1,1'-[2,5-thiophene-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecan- e in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

13. A .Iadd.pharmaceutical .Iaddend.composition .[.according to claim 1, wherein the.]. .Iadd.active against HIV comprising as an .Iaddend.active ingredient .[.is.]. 1,1'-[4,4'-(2,2'-bipyridine)-bis-(methylene)]-bis-1,4,8,11-tetraazacyclot- etradecane in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

14. A .Iadd.pharmaceutical .Iaddend.composition .[.according to claim 1, wherein the.]. .Iadd.active against HIV comprising as an .Iaddend.active ingredient .[.is.]. 1,1'-[2,9-(1,10-phenanthroline)-bis-(methylene)]-bis-1,4,8,11-tetraazacyc- lotetradecane in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

15. A .Iadd.pharmaceutical .Iaddend.composition .[.according to claim 1, wherein the.]. .Iadd.active against HIV comprising as an .Iaddend.active ingredient .[.is.]. 1,1'-[1,3-phenylene-bis-(methylene)]-bis-1,4,7,10-tetraazacyclotetradecan- e in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

16. A .Iadd.pharmaceutical .Iaddend.composition .[.according to claim 1, wherein the.]. .Iadd.active against HIV comprising as an .Iaddend.active ingredient .[.is.]. 1,1'-[1,4-phenylene-bis-(methylene)]-bis-1,4,7,10-tetraazacyclotetradecan- e in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

17. .[.The compound of claim 1, which is.]. .Iadd.A pharmaceutical composition active against HIV comprising as an active ingredient .Iaddend.1,1'-[5-nitro-1,3-phenylenebis(methylene)]bis-1,4,8,11-tetraazac- yclotetradecane in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

18. .[.The compound of claim 1, which is 1'1'-[2,4,5,6-tetrachloro-1,3-phenyleneis(methylene)]bis-1,4,8,11-tetraaz- acyclotetradecane.]. .Iadd.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-tetraa- zacyclotetradecane .Iaddend.in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

19. .[.The compound of claim 1, which is.]. .Iadd.A pharmaceutical composition active against HIV comprising as an active ingredient .Iaddend.1,1'-[2,3,5,6-tetrafluoro-1,4-phenylenebis(methylene)]bis-1,4,8,- 11-tetraazacyclotetradecane in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

20. .[.The compound of claim 1, which is.]. .Iadd.A pharmaceutical composition active against HIV comprising as an active ingredient .Iaddend.1,1'-[1,4-naphthylene-bis-(methylene)]bis-1,4,8,11-tetraazacyclo- tetradecane in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

21. .[.The compound of claim 1, which is.]. .Iadd.A pharmaceutical composition active against HIV comprising as an active ingredient .Iaddend.1,1'-[1,3-phenylenebis-(methylene)]bis-1,5,9-triazacyclododecane in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

22. .[.The compound of claim 1, which is 1,1'-[1,4-phenylene-bis-(methylene)]-1,5,9-triazacyclododecane.]. .Iadd.A pharmaceutical composition active against HIV comprising as an active ingredient 1,1'-[1,4-phenylene-bis-(methylene)]-bis-1,5,9-triazacyclododecane .Iaddend.in acid addition salt form .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

.[.23. The compound of claim 1, which is a bis-zinc complex of 1,1'[1,4-phenylene-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane- ..].

.[.24. The compound of claim 1, which is 1,1'-[3,3'-biphenylene-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetrade- cane in acid addition salt form..].

.[.25. The compound of claim 1, which is 1,1'-[2,6-pyridine-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane in acid addition salt form..].

.[.26. The compound of claim 1, which is 1,1'-[3,5-pyridine-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane in acid addition salt form..].

.[.27. The compound of claim 1, which is 1,1'-[2,5-thiophene-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecan- e in acid addition salt form..].

.[.28. The compound of claim 1, which is 1,1'-[4,4'-(2,2'-bipyridine)-bis-(methylene)]-bis-1,4,8,11-tetraazacyclot- etradecane in acid addition salt form..].

.[.29. The compound of claim 1, which is 1,1'-[2,9-(1,10-phenanthroline)-bis-(methylene)]-bis-1,4,8,11-tetraazacyc- lotetradecane in acid addition salt form..].

.[.30. The compound of claim 1, which is 1,1'-[1,3-phenylene-bis-(methylene)]-bis-1,4,7,10-tetraazacyclotetradecan- e in acid addition salt form..].

.[.31. The compound of claim 1, which is 1,1'-[1,4-phenylene-bis-(methylene)]-bis-1,4,7,10-tetraazacyclotetradecan- e in acid addition salt form..].

32. .[.The compound of claim 1, which is.]. .Iadd.A pharmaceutical composition active against HIV comprising as an active ingredient .Iaddend.1,1'-[2,5-dimethyl-1,4-phenylenebis-(methylene)]-bis-1,4,8,11-te- traazacyclotetradecane .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

33. .[.The compound of claim 1, which is.]. .Iadd.A pharmaceutical composition active against HIV comprising as an active ingredient .Iaddend.1,1'-[2,5-dichloro-1,4-phenylenebis-(methylene)]-bis-1,4,8,11-te- traazacyclotetradecane .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

34. .[.The compound of claim 1, which is.]. .Iadd.A pharmaceutical composition active against HIV comprising as an active ingredient .Iaddend.1,1'-[2-bromo-1,4-phenylenebis-(methylene)]-bis-1,4,8,11-tetraaz- acyclotetradecane .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

35. .[.The compound of claim 1, which is.]. .Iadd.A pharmaceutical composition active against HIV comprising as an active ingredient .Iaddend.1,1'-[6-phenyl-2,4-pyridinebis-(methylene)]-bis-1,4,8,11-tetraaz- acyclotetradecane .Iadd.in admixture or association with a pharmaceutically acceptable diluent or carrier.Iaddend..

.Iadd.36. 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..Iaddend.

.Iadd.37. 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..Iaddend.

.Iadd.38. A pharmaceutical composition active against HIV comprising as an active ingredient 1,1'-[3,3'-biphenylene-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetrade- cane in admixture or association with a pharmaceutically acceptable diluent or carrier..Iaddend.

.Iadd.39. A pharmaceutical composition active against HIV comprising as an active ingredient 11,11'-[1,4-phenylene-bis-(methylene)]-bis-1,4,7,11-tetraazacyclotetradec- ane in admixture or association with a pharmaceutically acceptable diluent or carrier..Iaddend.

.Iadd.40. 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..Iaddend.

.Iadd.41. 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..Iaddend.

.Iadd.42. A pharmaceutical composition active against HIV comprising as an active ingredient 1,1'-[2,5-thiophene-bis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecan- e in admixture or association with a pharmaceutically acceptable diluent or carrier..Iaddend.

.Iadd.43. 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-tetraazacyclot- etradecane in admixture or association with a pharmaceutically acceptable diluent or carrier..Iaddend.

.Iadd.44. 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-tetraazacyc- lotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier..Iaddend.

.Iadd.45. A pharmaceutical composition active against HIV comprising as an active ingredient 1,1'-[1,3-phenylene-bis-(methylene)]-bis-1,4,7,10-tetraazacyclotetradecan- e in admixture or association with a pharmaceutically acceptable diluent or carrier..Iaddend.

.Iadd.46. A pharmaceutical composition active against HIV comprising as an active ingredient 1,1'-[1,4-phenylene-bis-(methylene)]-bis-1,4,7,10-tetraazacyclotetradecan- e in admixture or association with a pharmaceutically acceptable diluent or carrier..Iaddend.

.Iadd.47. A pharmaceutical composition active against HIV comprising as an active ingredient 1,1'-[5-nitro-1,3-phenylenebis(methylene)]bis-1,4,8,11-tetraazacyclotetra- decane in admixture or association with a pharmaceutically acceptable diluent or carrier..Iaddend.

.Iadd.48. 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-tetraa- zacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier..Iaddend.

.Iadd.49. 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-tetra- azacyclotetradecane in admixture or association with a pharmaceutically acceptable diluent or carrier..Iaddend.

.Iadd.50. A pharmaceutical composition active against HIV comprising as an active ingredient 1,1'-[1,4-naphthylene-bis-(methylene)]bis-1,4,8,11-tetraazacyclotetradeca- ne in admixture or association with a pharmaceutically acceptable diluent or carrier..Iaddend.

.Iadd.51. 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..Iaddend.

.Iadd.52. 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..Iaddend.
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