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US 2006/0135554 A1Published application
Novel compounds
AssigneeAstraZeneca AB
InventorsYun-Xing Cheng, Miroslaw Tomaszewski, Christopher Walpole, Hua Yang
Life of this patent
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Abstract
Compounds of general formula I are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.
Claims6
A compound of formula I or a pharmaceutically acceptable salt thereof;
- wherein
- R1 is selected from the group consisting of —(C1-C8)alkyl, —(C2-C8)alkenyl, R42N(C1-C6)alkyl-, R42NC(═O)(C1-C6)alkyl-, R4O(C1-C6)alkyl-, R4OC(═O)(C1-C6)alkyl-, R4C(═O)(C1-C6)alkyl-, R4C(═O)NR4(C1-C6)alkyl-, R42NSO2(C1-C6)alkyl-, R4CSO2NR4(C1-C6)alkyl-, R42NC(═O)NR4(C1-C6)alkyl-, R42NSO2NR4(C1-C6)alkyl-, aryl(C1-C6)alkyl, aroyl(C1-C6)alkyl, heteroaryl(C1-C6)alkyl, heteroaroyl(C1-C6)alkyl, (C3-C8)heterocycloalkyl(C1-C6)alkyl, bicyclic heteroaryl(C1-C6)alkyl and bicyclic heteroaroyl(C1-C6)alkyl;
- R1 moieties comprise unsubstituted —(C2-C8)alkenyl, and —(C1-C8)alkyl unsubstituted or substituted by one or more moieties independently selected from the group consisting of halogen, cyano, acetoxymethyl, and nitro;
- Ar is an optionally substituted aryl moiety;
- R2 is —(C1-C6)alkyl, unsubstituted or substituted on 1-6 carbons by one or more fluorine substituents, or (C3-C6)cycloalkyl;
- R3 is selected from the group consisting of:
- R4 is a moiety independently selected from the group consisting of —H, —(C1-C6)alkyl, —(C2-C6) alkenyl and —(C2-C6)alkynyl;
- R5 moieties are independently selected from the group consisting of —H, —(C1-C6)alkyl, —(C2-C6)alkenyl and heterocyclyl;
- R6 moieties are independently selected from the group consisting of:
- —H, —(C1-C6)alkyl, —(C2-C6)alkenyl and —(C1-C6)alkanoyl, heterocyclyl, heterocyclyl(C1-C3)alkyl, aryl, aryl(C1-C3)alkyl, heteroaryl, heteroaryl(C1-C3)alkyl, bicyclic heteroaryl, and bicyclic heteroaryl(C1-C3)alkyl;
- R5 and R6 may combine to form a 5-7 membered heterocycle;
- X is selected from the group consisting of —C(R5)2—, —NR5—, C(═O)—, —CH2—CH2—, —CH═CH—, —O—, —C(R)(R′)—, and —S(O)n— (where n=0, 1 or 2), where R and R′═(C1-C6)alkyl, OR″, or H, and R″═H or (C1-C6)alkyl;
- and
- Y is nitrogen,
- wherein if R1 represents R42N(C1-C6)alkyl-, wherein both occurrences of R4 represent —(C1-C6)alkyl, then R3 is not acetyl, —NH2, or acetamido.
12 more elements
Dependencies are inferred from the claim text.