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US 2006/0235050 A1Published application
Diamine calcium channel blockers
AssigneeNueromed Technologies, Inc.
InventorsHassan Pajouhesh, Hossein Pajouhesh, Yanbing Ding, Terrance Snutch, Francesco Belardetti
Life of this patent
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Abstract
Aromatic derivatives of aliphatic diamines are effective in ameliorating conditions characterized by unwanted calcium ion channel activity, especially T-type and N-type channels. These conditions include, for example, stroke and pain.
Claims22
A compound of the formula
- (Ar1—X1)n—NR1—X3—NR2—X2—CR3(Ar2)2 (1)
- and the salts and conjugates thereof, wherein
- each Ar1 is independently a cyclic moiety which is aromatic or nonaromatic, carbocyclic or heterocyclic wherein heterocyclic forms of Ar1 contain 1-3 heteroatoms selected from O, S and N;
- X1 is a linker comprising a chain of 1-5 members;
- n is 1 or 2;
- R1 is absent when n is 2 and when n is 1, R1 is H, alkyl (1-8C), alkenyl (2-8C) or alkynyl (2-8C);
- X3 is alkylene, alkenylene or alkynylene (2-8C);
- R2 is H, alkyl (1-8C), alkenyl (2-8C) or alkynyl (2-8C);
- X2 is a linker comprising a chain of 2-9 members;
- R3 is H, OH or alkyl (1-4C);
- each Ar2 independently comprises a 6-membered aromatic ring optionally containing 1-3 nitrogen atoms
- wherein each Ar1 and Ar2 in formula (1) may be unsubstituted or substituted by one or more substituents selected from the group consisting of ═O (in nonaromatic cyclic moieties), alkyl (1-8C), alkenyl (2-8C), alkynyl (2-8C), aryl, alkylaryl, halo, CHF2, CF3, OCF3, OCHF2, CN, NO2, NR2, OR, SR, COR, COOR, CONR2, SOR, SO2R, SO3R, SONR2, SO2NR2, SO3NR2, NROCR, OOCR, NRSOR, NRSO2R, and NRSO3R, wherein R is H, alkyl (1-8C), alkenyl (2-8C), alkynyl (2-8C), aryl, or alkylaryl or heteroforms of any of the foregoing, each of which may optionally be substituted, and wherein two R on the same N may form a 5-7 membered ring, and wherein two substituents on adjacent atoms may form a 5-7 membered ring;
- and
- wherein the chain comprised in X1 and X2 may be substituted by ═O, alkyl (1-8C), alkenyl (2-8C), alkynyl (2-8C), halo, CHF2, CF3, OCF3, OCHF2, CN, NO2, NR2, OR, SR, COR, COOR, CONR2, SOR, SO2R, SO3R, SONR2, SO2NR2, SO3NR2, NROCR, OOCR, NRSOR, NRSO2R, and/or NRSO3R, wherein R is H or alkyl (1-8C), alkenyl (2-8C), alkynyl (2-8C), aryl, or alkylaryl or heteroforms of any of the foregoing, each of which may optionally be substituted wherein two R on the same N may form a 5-7 membered ring, and wherein two substituents on adjacent atoms may form a 5-7 membered ring.
11 more elements
Dependencies are inferred from the claim text.