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US 2003/0119837 A1Published application
Pharmaceutical composition for the treatment of CNS and other disorders
AssigneePfizer Inc.
InventorsBrian Thomas O'Neill, Jotham Wadsworth Coe, Christopher J. O'Donnell
Life of this patent
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Abstract
The present invention relates to a method of treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal a CNS-penetrant α7 nicotinic receptor agonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant α7 nicotinic receptor agonist.
Claims13
A compound of the formula
- 6
- wherein
- n=1-2;
- m=1-2;
- o=1-2;
- A=O, S or NR1;
- B═N or CR2;
- Q=N or CR3;
- D=N or CR4;
- E=N or CR5;
- R1 is H, a straight chain or branched (C1-C8)alkyl, C(═O)OR6, CH2R6, C(═O)NR6R7, C(═O)R6, or SO2R6;
- each R2, R3, R4 and R5 is independently selected from F, Cl, Br, I, nitro, cyano, CF3, —NR6R7, —NR6C(═O)R7, —NR6C(═O)NR7R8, —NR6C(═O)OR7, —NR6S(═O)2R7, —NR6S(═O)2NR7R8, —OR6, —OC(═O)R6, —OC(═O)OR6, —OC(═O)NR6R7, —OC(═O)SR6, —C(═O)OR6, —C(═O)R6, —C(═O)NR6R7, —SR6, —S(═O)R6, —S(═O)2R6, —S(═O)2NR6R7, and R6;
- each R6, R7, and R8 is independently selected from H, straight chain or branched (C1-C8)alkyl, straight chain or branched (C2-C8)alkenyl, straight chain or branched (C2-C8)alkynyl, (C3-C8)cycloalkyl, (C4-C8)cycloalkenyl, 3-8 membered heterocycloalkyl, (C5-C11)bicycloalkyl, (C7-C11)bicycloalkenyl, 5-11 membered heterobicycloalkyl, 5-11 membered heterobicycloalkenyl, (C6-C11)aryl, and 5-12 membered heteroaryl;
- wherein each R6, R7, and R8 is optionally substituted with from one to six substituents, independently selected from F, Cl, Br, I, nitro, cyano, CF3, —NR9R10, —NR9C(═O)R10, —NR9C(═O)NR10R11, —NR9C(═O)OR10, —NR9S(═O)2R10, —NR9S(═O)2NR10R11, —OR9, —OC(═O)R9, —OC(═O)OR9, —OC(═O)NR9R10, —OC(═O)SR9, —C(═O)OR9, —C(═O)R9, —C(═O)NR9R10, —SR9, —S(═O)R9, —S(═O)2R9, —S(═O)2NR9R10 and R9;
- each R9, R10 and R11 is independently selected from H, straight chain or branched (C1-C8)alkyl, straight chain or branched (C2-C8)alkenyl, straight chain or branched (C2-C8)alkynyl, (C3-C8)cycloalkyl, (C4-C8)cycloalkenyl, 3-8 membered heterocycloalkyl, (C5-C11)bicycloalkyl, (C7-C11)bicycloalkenyl, 5-11 membered heterobicycloalkyl, (5-11 membered) heterobicycloalkenyl, (C6-C11)aryl or 5-12 membered heteroaryl;
- wherein each R9, R10 and R11 is optionally substituted with from one to six substituents independently selected from F, Cl, Br, I, nitro, cyano, CF3, —NR12R13, —NR12C(═O)R13, —NR12C(═O)NR13R14, —NR12C(═O)OR13, —NR12S(═O)2R13, —NR12S(═O)2NR13R14, —OR12, —OC(═O)R12, —OC(═O)OR12, —OC(═O)NR12R13, —OC(═O)SR12, —C(═O)OR12, —C(═O)R12, —C(═O)NR12R13, —SR12, S(═O)R12, —S(═O)2R12, —S(═O)2NR12R13 and R12;
- each R12, R13, and R14 is independently selected from H, straight chain or branched (C1-C8)alkyl, straight chain or branched (C2-C8)alkenyl, straight chain or branched (C2-C8)alkynyl, (C3-C8)cycloalkyl, (C4-C8)cycloalkenyl, 3-8 membered heterocycloalkyl, (C5-C11)bicycloalkyl, (C7-C11)bicycloalkenyl, 5-11 membered heterobicycloalkyl, 5-11 membered heterobicycloalkenyl, (C6-C11)aryl and (5-12 membered) heteroaryl;
- or R2 and R3, or R3 and R4, or R4 and R5, may form another 6-membered aromatic or heteroaromatic ring sharing B and Q, or Q and D, or D and E, respectively, and may be optionally substituted with from one to four substituents independently selected from the group of radicals set forth in the definition of R6, R7and R8 above;
- or an enantiomeric, diastereomeric, or tautomeric isomer thereof, or a pharmaceutically acceptable salt of such compound or isomer.
16 more elements
Dependencies are inferred from the claim text.