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US 6,310,059 B1Granted
Fused ring calcium channel blockers
AssigneeNeuroMed Technologies, Inc.
InventorTerrance P. Snutch
Life of this patent
Estimating the term…
Abstract
Compounds of the formula or salts thereof, wherein the variable are as defined herein are useful as calcium channel blockers.
Claims27
A method to treat conditions associated with undesired calcium channel activity in a subject which method comprises administering to a subject in need of such treatment a compound of the formula
- or the salts thereof,
- wherein Z is N or CH;
- wherein n is 0 or 1;
- X1 and X2 are linkers;
- Ar represents one or two substituted or unsubstituted aromatic or heteroaromatic rings, and
- Cy represents one or two substituted or unsubstituted aliphatic cyclic or heterocyclic moietics, or consists of one substituted or unsubstituted aliphatic cyclic or heterocyclic moiety and one substituted or unsubstituted aromatic or heteroaromatic moiety,
- Y is O, S, NR or CR2 where R is H or alkyl (1-6C);
- each l1 and l2 is independently 0-4;
- l3 is 0 or 1;
- each of R1, R2 and R3 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 may independently be halo, OR, SR, NR2, OOCR, NROCR, COR, COOR, CONR2, CF3, CN or NO2, wherein R is H or alkyl (1-6C), and
- wherein the dotted lines represent optional π-bonds, or
- compounds of formulas (1a) or (1b) where (X2)nAr or (X2)nCy is replaced by alkyl (1-6C).
9 more elements
A pharmaceutical composition for use in treating conditions characterized by undesired calcium channel activity which composition comprises, in admixture with a pharmaceutically acceptable excipient, a dosage amount of at least one compound of the formula
- or salts thereof,
- wherein Z is N or CH;
- wherein n is 0 or 1;
- X1 and X2 are linkers;
- Ar represents one or two substituted or unsubstituted aromatic or heteroaromatic rings, and
- Cy represents one or two substituted or unsubstituted aliphatic cyclic or heterocyclic moieties, or consists of one substituted or unsubstituted aliphatic cyclic or heterocyclic moiety and one substituted or unsubstituted aromatic or heteroaromatic moiety,
- Y is O, S, NR or CR2 where R is H or alkyl (1-6C);
- each l1 and l2 is independently 0-4;
- l3is 0 or 1;
- each of R1, R2 and R3 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 may independently be halo, OR, SR, NR2, OOCR, NROCR, COR, COOR, CONR2, CF3, CN or NO2, wherein R is H or alkyl (1-6C), and
- wherein the dotted lines represent optional π-bonds, or
- compounds of formulas (1a) or (1b) where (X2)nAr or (X2)nCy is replaced by alkyl (1-6C).
9 more elements
A library comprising at least ten different compounds of the formula
- or salts thereof,
- wherein Z is N or CH;
- wherein n is 0 or 1;
- X1 and X2 are linkers;
- Ar represents one or two substituted or unsubstituted aromatic or heteroaromatic rings, and
- Cy represents one or two substituted or unsubstituted aliphatic cyclic or heterocyclic moieties, or consists of one substituted or unsubstituted aliphatic cyclic or heterocyclic moiety and one substituted or unsubstituted aromatic or heteroaromatic moiety,
- Y is O, S, NR or CR2 where R is H or alkyl (1-6C);
- each l1 and l2 is independently 0-4;
- l3 is 0 or 1;
- each of R1, R2 and R3 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 may independently be halo, OR, SR, NR2, OOCR, NROCR, COR, COOR, CONR2, CF3, CN or NO2, wherein R is H or alkyl (1-6C), and
- wherein the dotted lines represent optional π-bonds, or
- compounds of formulas (1a) or (1b) where (X2)nAr or (X2)nCy is replaced by alkyl (1-6C).
9 more elements
Dependencies are inferred from the claim text.