Calcium channel blockers
AssigneeNeuroMed Technologies, Inc.
InventorsTerrance Preston Snutch, Gerald Werner Zamponi
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AssigneeNeuroMed Technologies, Inc.
InventorsTerrance Preston Snutch, Gerald Werner Zamponi
Estimating the term…
Compounds of the formula ##STR1## 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.sub.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 I.sup.1 and I.sup.2 is independently 0-5; I.sup.3 is 0 or 1; each of R.sup.1, R.sup.2 and R.sup.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.sup.1 and R.sup.2 may independently be halo, COOR, CONR.sub.2, CF.sub.3, CN or NO.sub.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 I.sup.3 is 0, and either I.sup.1 and I.sup.2 is 0 or 1 and if R.sup.1 and/or R.sup.2 represent F in the para position, Z cannot N or C; and are useful as calcium channel blockers. Libraries of these compounds can also be used to identify antagonists for other targets.
A method to treat conditions associated with calcium channel activity in a subject which method comprises administering to a subject in need of such treatment a compound of the formula ##STR4## wherein m is 0, 1 or 2;
A pharmaceutical composition for use in treating conditions characterized by calcium channel activity which composition comprises, in admixture with a pharmaceutically acceptable excipient, a dosage amount of a compound of the formula ##STR5## wherein m is 0, 1 or 2;
A library comprising at least ten different compounds of the formula ##STR6## wherein m is 0, 1 or 2;
Dependencies are inferred from the claim text.