Title:
TRPM8 receptor antagonist
Document Type and Number:
Japanese Patent JP6043298
Kind Code:
B2
Abstract:
Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula:
wherein R is selected from:
- H, CN, NO 2 , SO 2 NH 2 , SO 2 NHR' and SO 2 NR' 2 , where R' is selected from linear or branched C 1 -C 4 alkyl; X is selected from:
- F, Cl, CH 3 , NH 2 and OH Y is selected from:
- O, CH 2 , NH and SO 2 R1, R2, R3 and R4, indipendently one from the other, are selected from
- H and linear or branched C 1 -C 4 alkyl; Z is selected from:
- NR6 and R6R7N + , where R6 and R7 indipendently one from the other, are selected from:
€¢ H and linear or branched C 1 -C 4 alkyl R5 is a residue selected from:
- H and linear or branched C 1 -C 4 alkyl Het is a heteroaryl group selected from
- a substituted or not substituted pyrrolyl, a substituted or not substituted N-methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted or not substituted furanyl and a substituted or not substituted pyridinyl. Said compounds are useful in the treatment of pathologies depending on TRPM8 activity such as pain, cancer, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, inflammatory conditions, urological disorders.
Inventors:
Mauriconi, Alessio
Biantoni, Gianluca
Aramini, Andrea
Blaundani, Laura
Liberty, Chiara
Svolvia, Bovolenta
Beckali, Andrea
Lorenzi, Simone
Biantoni, Gianluca
Aramini, Andrea
Blaundani, Laura
Liberty, Chiara
Svolvia, Bovolenta
Beckali, Andrea
Lorenzi, Simone
Application Number:
JP2013550889A
Publication Date:
December 14, 2016
Filing Date:
January 27, 2012
Export Citation:
Assignee:
Dompe Farmacheutici Sochieta Per Azioni
International Classes:
C07D207/335; A61K31/341; A61K31/381; A61K31/40; A61K31/4402; A61P1/00; A61P9/10; A61P11/00; A61P13/00; A61P13/08; A61P13/10; A61P17/00; A61P19/02; A61P25/00; A61P25/06; A61P25/22; A61P25/24; A61P29/00; A61P43/00; C07D213/36; C07D307/52; C07D307/56; C07D333/20; C07D333/28
Domestic Patent References:
| JP2014503486A | ||||
| JP2015504874A |
Foreign References:
| US20100160289 | ||||
| WO2007017093A1 |
Other References:
REGISTRY(STN)[online],2008.09.17[検索日 2015.08.26]CAS登録番号 1049699-38-8
REGISTRY(STN)[online],2008.02.07[検索日 2015.08.26]CAS登録番号 1001867-62-4
REGISTRY(STN)[online],2008.02.07[検索日 2015.08.26]CAS登録番号 1001867-62-4
Attorney, Agent or Firm:
Shinjiro Ono
Yasushi Kobayashi
Shigeo Takeuchi
Osamu Yamamoto
Akiko Yamaguchi
Yasushi Kobayashi
Shigeo Takeuchi
Osamu Yamamoto
Akiko Yamaguchi