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US 8,008,499 B2Granted
Anabaseine derivatives, pharmaceutical compositions and methods of use thereof
AssigneeCornerstone Therapeutics, Inc.
InventorsGregory J. Habgood, Daniel Elbaum
Life of this patent
Estimating the term…
Abstract
Disclosed are novel anabaseine derivatives that act as agonists of the α7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.
Claims1
The compound of Formula (II):
- or a pharmaceutically acceptable salt thereof, wherein:
- R12 is selected from the group consisting of:
- R13 is selected from the group consisting of 6 membered monocyclic aryl, 5 or 6 membered monocyclic heteroaryl comprising 1-3 heteroatoms, 8-12 membered bicyclic aryl, 8-12 membered bicyclic heteroaryl comprising 1-6 heteroatoms, 11-14 membered tricyclic aryl and 11-14 membered heteroaryl comprising 1-9 heteroatoms, wherein each of said heteroatoms is independently selected from the group consisting of O, N and S and wherein said aryl and heteroaryl are each optionally substituted with one or more R17;
- Each R14 is independently selected from the group consisting of H, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, C4-C10 cycloalkenyl, 3-10 membered heterocycloalkyl, 4-10 membered heterocycloalkenyl, aryl, heteroaryl and haloalkyl;
- Each R15 is independently selected from the group consisting of halo, haloalkyl, CF3, OCF3, OR14, SR14, C(O)R14, OC(O)R14, C(O)OR14, NR14R14, NO2, CN, OC(O)NR14R14, C(O)NR14R14, N(R14)C(O)R14, N(R14)(COOR14), S(O)tNR14R14, C3-C8 cycloalkyl, C4-C10 cycloalkenyl, 3-8 membered heterocycloalkyl, 4-10 membered heterocycloalkenyl, C5-C11 bicycloalkyl, C5-C11 bicycloalkenyl, 5-11 membered heterobicycloalkyl, 5-11 membered heterobicycloalkenyl, aryl and heteroaryl
- Each R16 is independently selected from the group consisting of R15, C1-C10 alkyl, C1-C10 alkyl substituted with one or more R15, C2-C10 alkenyl, C2-C10 alkenyl substituted with one or more R15, C2-C10 alkynyl and C2-C10 alkynyl substituted with one or more R15;
- Each R17 is independently selected from the group consisting of C1-C10 alkyl, C1-C10 alkyl substituted with one or more R15, C2-C10 alkenyl, C2-C10 alkenyl substituted with one or more R15, C2-C10 alkynyl, C2-C10 alkynyl substituted with one or more R16, C3-C10 cycloalkyl, C3-C10 cycloalkyl substituted with one or more R16, C4-C10 cycloalkenyl, C4-C10 cycloalkenyl substituted with one or more R16, 3-8 membered heterocycloalkyl, 3-8 membered heterocycloalkyl substituted with one or more R16, 4-10 membered heterocycloalkenyl, 4-10 membered heterocycloalkenyl substituted with one or more R16, C5-C11 bicycloalkyl, C5-C11 bicycloalkyl substituted with one or more R16, C5-C11 bicycloalkenyl, C5-C11 bicycloalkenyl substituted with one or more R16, 5-11 membered heterobicycloalkyl, 5-11 membered heterobicycloalkyl substituted with one or more R16, 5-11 membered heterobicycloalkenyl, 5-11 membered heterobicycloalkenyl substituted with one or more R16, halo, CF3, OCF3, OR14, SR14, NR14R14, C(O)OR14, NO2, CN, C(O)R14, C(O)C(O)R14, C(O)NR14R14, C(O)C(O)NR14R14, N(R14)C(O)R14, NR14S(O)tR14, N(R14)C(O)OR14, NR14C(O)R14, NR14C(O)NR14R14, NR14S(O)tNR14R14, NR14S(O)tR14, S(O)tR14, S(O)tNR14R14, OC(O)R14, optionally substituted aryl and optionally substituted heteroaryl;
- and
- t is 1 or 2.
6 more elements
Dependencies are inferred from the claim text.