Back to results
US 2010/0075953 A1Published application
Substituted piperazines, (1,4) diazepines, and 2,5-diazabicyclo (2.2.1) heptanes as histamine h1 and/or h3 antagonists or histamine h3 reverse antagonists
AssigneeGlaxo Group Limited
InventorsRachael Ancliff, Colin David Eldred, Ashley Paul Hancock, Thomas Daniel Heightman, Heather Hobbs, Simon Teanby Hodgson, David Matthew Wilson
Life of this patent
Estimating the term…
Abstract
The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurodegenerative disorders including Alzheimer's disease.
Claims9
A compound of formula (I)
- wherein:
- R1 represents heteroaryl, optionally substituted by one or more:
- halogen;
- trifluoromethyl;
- —C1-6alkyl optionally substituted by COOR15;
- —C1-6alkoxy optionally substituted by COOR15;
- C1-6 alkenyl;
- NR15R16;
- or C1-6alkylthio groups, and in which
- R15 and R16 independently represent hydrogen, C1-6alkyl or C3-8cycloalkyl or together may be fused to form a 5- to 7-membered non-aromatic heterocyclic ring optionally interrupted by an O or S atom and optionally substituted by halogen, C1-6alkyl or —C1-6alkylC1-6alkoxy group;
- wherein R15 and R16 independently represent hydrogen, C1-6alkyl or C3-8cycloalkyl or together may be fused to form a 5- to 7-membered non-aromatic heterocyclic ring optionally interrupted by an O or S atom and optionally substituted by a halogen, C1-6alkyl or C1-6alkylC1-6alkoxy group;
- Z is a bond or CO;
- m is 0 or 2;
- p is 1;
- R3 represents —(CH2)q—NR11R12 in which q represents 3 and
- NR11R12 represents pyrrolidinyl, piperidinyl, azepanyl or azocanyl optionally substituted by one or more C1-6 alkyl groups;
- or a pharmaceutically acceptable salt thereof.
14 more elements
Dependencies are inferred from the claim text.