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US 7,803,825 B2Granted
Aminoalkylazole derivatives as histamine-3 antagonists
AssigneeWyeth
InventorsJonathan Laird Gross, Albert Jean Robichaud, Marla Jean Williams, Alessandro Mazzacani
Life of this patent
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Abstract
The present invention provides a compound of formula Ia: and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
Claims26
A compound of formula (Ia)
- wherein
- X is (CH2)0;
- m is 1, 2 or 3;
- n is 0, 1, 2 or 3;
- R is H, halogen or an optionally substituted C1-C6 alkyl group;
- R1 and R2 are each independently H or an optionally substituted C1-C6 alkyl group or R1 and R2 may be taken together with the atom to which they are attached to form an optionally substituted 4- to 7-membered cycloheteroalkyl;
- R3, R4, R7 and R8 are each independently H, or a C1-C6 alkyl, C3-C10 cycloalkyl, or C6-C10 aryl group each optionally substituted;
- R5 and R6 are each independently H, halogen, OR10 or C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl;
- R10 is H or an optionally substituted C1-C6 alkyl group;
- and
- R11 and R12 are taken together with the atom to which they are attached to form an optionally substituted fused bicyclic 9- to 11-membered ring system optionally containing one to three additional heteroatoms selected from N, O or S;
- or
- a stereoisomer or a pharmaceutically acceptable salt thereof;
- wherein the optionally substituted groups are selected from the group consisting of C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo, nitro, cyano, hydroxy, C6-C10 aryl, a 3-10 membered heterocyclyl ring, a 5-10 membered heteroaryl ring, —N(Ra)2, —C(O)Rb, —ORc and —S(O)pRd;
- wherein each Ra is independently H, C1-C4 alkyl, —CHO, —C(O)(C1-C4 alkyl), or —C(O)—O—(C1-C4 alkyl);
- each Rb is independently H, —OH, O(C1-C4alkyl), C1-C4 alkyl, —NH2, —NH(C1-C4 alkyl), or —N(C1-C4 alkyl)2;
- each Rc is independently H, C1-C4 alkyl optionally substituted with halo, —CHO or —C(O)(C1-C4 alkyl);
- each Rd is independently C1-C4 alkyl, or —OH;
- and p is 0, 1 or 2.
16 more elements
Dependencies are inferred from the claim text.