公开(公告)号：EP2793883A1

公开(公告)日：2014-10-29

申请号：EP12812229.8

申请日：2012-12-19

申请人： Dompe' S.p.A.

发明人： MORICONI, Alessio ,  BIANCHINI, Gianluca ,  COLAGIOIA, Sandro ,  BRANDOLINI, Laura ,  ARAMINI, Andrea ,  LIBERATI, Chiara ,  BOVOLENTA, Silvia

IPC分类号： A61K31/421 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  C07D263/40 ,  C07D263/48 ,  C07D277/34 ,  C07D277/42 ,  C07D277/56 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02 ,  A61P29/00

CPC分类号： C07D417/12 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/472 ,  C07D263/40 ,  C07D263/42 ,  C07D277/56 ,  C07D413/04 ,  C07D417/04 ,  C07D417/10

摘要： The invention relates to compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula (I). Said compounds are useful in the treatment of diseases associated with activity of TRPM8 such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, itch, irritable bowel diseases, cold induced and/or exhacerbated respiratory disorders and urological disorders.

摘要翻译： 所述化合物可用于治疗与TRPM8的活性相关的疾病，例如疼痛，炎症，局部缺血，神经变性，中风，精神疾病，瘙痒，肠易激综合征，冷诱导和/或恶化的呼吸系统疾病和泌尿系统疾病。

公开(公告)号：EP2668160A1

公开(公告)日：2013-12-04

申请号：EP12705078.9

申请日：2012-01-27

申请人： Dompe' S.p.A.

发明人： MORICONI, Alessio ,  BIANCHINI, Gianluca ,  BRANDOLINI, Laura ,  ARAMINI, Andrea ,  LIBERATI, Chiara ,  BOVOLENTA, Silvia ,  BECCARI, Andrea ,  LORENZI, Simone

IPC分类号： C07D213/36 ,  C07D307/52 ,  C07D307/56 ,  C07D333/20 ,  C07D333/28 ,  C07D207/323 ,  A61K31/341 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/4402 ,  A61P29/00

CPC分类号： C07D213/38 ,  C07D207/323 ,  C07D207/335 ,  C07D213/36 ,  C07D307/52 ,  C07D307/56 ,  C07D333/20 ,  C07D333/28

摘要： 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.