23-06-2016 дата публикации
Номер: US20160175315A1
Принадлежит:
Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1). 2. The pharmaceutical composition of wherein Ar is substituted phenyl.3. The pharmaceutical composition of wherein n is 0.4. The pharmaceutical composition of wherein the substituents on Ar are independently selected from fluoro claim 1 , bromo claim 1 , chloro claim 1 , trifluoromethyl claim 1 , methyl claim 1 , difluoromethoxy claim 1 , trifluoromethoxy claim 1 , methylsulfonyl claim 1 , t-butyl claim 1 , t-butyloxy claim 1 , methoxy claim 1 , phenoxy claim 1 , pyrrolidinyl claim 1 , pyridinyloxy morpholinomethyl claim 1 , hydroxy claim 1 , (CH)COC(O) or wherein two optional substituents together form a five membered heterocyclic ring with Ar wherein the two substituents together form —O—CH—O— claim 1 , —O—CF—O— or —O—CHCH—.5. The pharmaceutical composition of wherein B is NY.6. The pharmaceutical composition of wherein at least one Y is H or methyl.7. The pharmaceutical composition of wherein at least one Y is an alkyl or heteroalkyl.8. The pharmaceutical composition of wherein a carbonyl is immediately adjacent to the N in B.9. The pharmaceutical composition of wherein each R is H claim 1 , or two R on the same carbon atom together form ═O.11. The pharmaceutical composition of wherein one Y is H or methyl and one Y is an optionally substituted alkyl (1-6C) or SORwherein Ris an optionally substituted C1-C5 alkyl. This application is a continuation of U.S. patent application Ser. No. 13/601,357, filed Aug. 31, 2012, which is a continuation of U.S. patent application Ser. No. 12/420,793, filed Apr. 8, 2009, which claims benefit to U.S. Provisional Application No. 61/058,179, filed Jun. 2, 2008, each of which is hereby incorporated by reference in its entirety.The invention relates ...
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