IP Library › Granted Patent US 7,666,865
Granted Patent B2
US 7,666,865 · App. 11/601,005 · Granted Feb 23, 2010

Calcium channel blockers

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Quick Facts
Patent No.
US 7,666,865
App. No.
11/601,005
Granted
Feb 23, 2010
Kind
B2
Abstract

Compounds of the formula wherein m is 0, 1 or 2; wherein when m is 0, Z is O, when m is 1, Z is N, and when m is 2, Z is C; Y is H, OH, NH 2 , or an organic moiety of 1-20C, optionally additionally containing 1-8 heteroatoms selected from the group consisting of N, P, O, S and halo; each l 1 and l 2 is independently 0-5; l 3 is 0 or 1; each of R 1 , R 2 and R 3 is independently alkyl (1-6C), aryl (6-10C) or arylalkyl (7-16C) optionally containing 1-4 heteroatoms selected from the group consisting of halo, N, P, O, and S or each of R 1 and R 2 may independently be halo, COOR, CONR 2 , CF 3 , CN or NO 2 , wherein R is H or lower alkyl (1-4C) or alkyl (1-6C); n is 0 or 1; X is a linker; with the proviso that Y is not a tropolone, a coumarin, or an antioxidant containing an aromatic group and with the further proviso that if l 3 is 0, and either l 1 and l 2 is 0 or 1 and if R 1 and/or R 2 represent F in the para position, Z cannot be C or N; and are useful to treat pain. Libraries of these compounds can also be used to identify antagonists for other targets.

Claims (20)

1. A method to treat pain in a subject which method comprises administering to a subject in need of such treatment a compound of the formula

wherein m is 0, 1 or 2;

wherein when m is 0, Z is O, when m is 1, Z is N, and when m is 2, Z is C;

Y is H, OH, NH 2 , or an organic moiety of 1-20C, optionally additionally containing 1-8 heteroatoms selected from the group consisting of N, P, O, S and halo;

each l 1 and l 2 is independently 0-5;

l 3 is 0 or 1;

each of R 1 , R 2 and R 3 is independently alkyl (1-6C), aryl (6-10C) or arylalkyl (7-16C) optionally containing 1-4 heteroatoms selected from the group consisting of halo, N, P, O, and S or each of R 1 and R 2 may independently be halo, COOR, CONR 2 , CF 3 , CN or NO 2 , wherein R is H or lower alkyl (1-4C) or alkyl (1-6C);

n is 0 or 1;

X is a linker;

with the proviso that Y is not a tropolone, a coumarin, or an antioxidant containing an aromatic group and with the further proviso that if l 3 is 0, and either l 1 and l 2 is 0 or 1 and if R 1 and/or R 2 represent F in the para position, Z cannot be N or C.

2. A pharmaceutical composition for use in treating pain which composition comprises, in admixture with a pharmaceutically acceptable excipient, a dosage amount of a compound of the formula

wherein m is 0, 1 or 2;

wherein when m is 0, Z is O, when m is 1, Z is N, and when m is 2, Z is C;

Y is H, OH, NH 2 , or an organic moiety of 1-20C, optionally additionally containing 1-8 heteroatoms selected from the group consisting of N, P, O, S and halo;

each l 1 and l 2 is independently 0-5;

l 3 is 0 or 1;

each of R 1 , R 2 and R 3 is independently alkyl (1-6C), aryl (6-10C) or arylalkyl (7-16C) optionally containing 1-4 heteroatoms selected from the group consisting of halo, N, P, O, and S or each of R 1 and R 2 may independently be halo, COOR, CONR 2 , CF 3 , CN or NO 2 , wherein R is H or lower alkyl (1-4C) or alkyl (1-6C);

n is 0 or 1;

X is a linker;

with the proviso that Y is not a tropolone, a coumarin, or an antioxidant containing an aromatic group and with the further proviso that if l 3 is 0, and either l 1 and l 2 is 0 or 1 and if R 1 and/or R 2 represent F in the para position, and Z cannot be N or C.