Substituted N-heteroaryl spirolactam bipyrrolidines, preparation and therapeutic use thereof
AssigneeSanofi
InventorsZhongli Gao, Daniel Hall, David Stefany
Life of this patent
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Abstract
The present disclosure relates to a series of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I). Wherein R1, R2, Q1, Q2, Q3, Q4, X, m, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl spirolactam bipyrrolidines of formula (I) and intermediates therefor.
Claims8
A compound of formula (I):
- wherein:
- m, p=1;
- n, s=1;
- X is O, NR3 or CR4R5;
- Q1 to Q4 are independently CH or N provided that one of Q1 to Q4 is N;
- R1 is hydrogen, (C1-C4)alkyl, CF3 or (C1-C4)alkoxy;
- R2 is hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy or CF3;
- R3 is hydrogen or (C1-C6)alkyloxycarbonyl;
- R4 is hydrogen;
- and
- R5 is hydrogen or OH;
- or a salt thereof or an enantiomer or a diastereomer thereof.
A pharmaceutical composition comprising a compound of formula (I):
- wherein:
- m, p =1;
- n, s =1;
- X is O, NR3 or CR4R5;
- Q1 to Q4 are independently CH or N provided that one of Q1 to Q4 is N;
- R1 is hydrogen, (C1-C4)alkyl, CF3 or (C1-C4)alkoxy;
- R2 is hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy or CF3;
- R3 is hydrogen or (C1-C6)alkyloxycarbonyl;
- R4 is hydrogen;
- and
- R5 is hydrogen or OH;
- or
- a pharmaceutically acceptable salt thereof or an enantiomer or a diastereomer thereof in combination with at least one pharmaceutically acceptable excipient, diluent or a carrier.
Dependencies are inferred from the claim text.