Preferentially substituted calcium channel blockers
AssigneeNeuroMed Technologies, Inc.
InventorTerrance P. Snutch
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AssigneeNeuroMed Technologies, Inc.
InventorTerrance P. Snutch
Estimating the term…
Compounds of the formula and their salts, wherein Cy represents cyclohexyl; Y is CH═CHΦ, CHΦ2, Φ or Cy, X is trivalent straight-chain alkylene (3-10C) or trivalent straight-chain 1-alkenylene (3-10C) optionally substituted by oxo at the C adjacent N when n is 0 and Y is Φ2CH; and is otherwise trivalent straight-chain alkylene (5-10C) or trivalent straight-chain 1-alkenylene (5-10C) optionally substituted by oxo at the C adjacent N; Z is N, NCO, CHNCOR1 or CHNR1, wherein R1 is alkyl (1-6C); and n is 0-5; wherein each Φ and Cy independently may optionally be substituted by alkyl (1-6C) or by halo, CF3, OCF3, NO2, NR2, OR, SR, COR, COOR, CONR2, NROCR or OOCR where R is H or alkyl (1-4C), or two substituents may form a 5-7 membered ring with the proviso that the compounds of formula (1) contain at least one aromatic moiety, are useful as calcium channel blockers.
A method to identify a blocker of ion channel activity which method comprises contacting cells which display an ion channel of interest with a candidate compound under conditions wherein activation of said ion channel would occur in the absence of said compound;
A method to identify a compound which is a blocker of ion channel activity which method comprises contacting a cell which displays said ion channel on its surface with a labeled compound known to bind said ion channel, said contacting in the presence and absence of said candidate compound and
Dependencies are inferred from the claim text.