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1. 发明申请

US20140371276A1 TRPM8 ANTAGONISTS 有权
公开(公告)号：US20140371276A1
公开(公告)日：2014-12-18
申请号：US14366796
申请日：2012-12-19
申请人： Alessio Moriconi , Gianluca Bianchini , Sandro Colagioia , Laura Brandolini , Andrea Aramini , Chiara Liberati , Silvia Bovolenta
发明人： Alessio Moriconi , Gianluca Bianchini , Sandro Colagioia , Laura Brandolini , Andrea Aramini , Chiara Liberati , Silvia Bovolenta
IPC分类号： C07D417/10 , C07D277/56
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：本发明涉及作为瞬时受体电位阳离子通道亚族M成员8（TRPM8）的选择性拮抗剂的化合物，并且具有式（I）。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/或恶化呼吸障碍和泌尿系统疾病。

2. 发明授权

US08906946B2 TRPM8 receptor antagonists 有权
标题翻译： TRPM8受体拮抗剂
公开(公告)号：US08906946B2
公开(公告)日：2014-12-09
申请号：US13982235
申请日：2012-01-27
申请人： Alessio Moriconi , Gianluca Bianchini , Andrea Aramini , Laura Brandolini , Chiara Liberati , Silvia Bovolenta , Andrea Beccari , Simone Lorenzi
发明人： Alessio Moriconi , Gianluca Bianchini , Andrea Aramini , Laura Brandolini , Chiara Liberati , Silvia Bovolenta , Andrea Beccari , Simone Lorenzi
IPC分类号： C07D207/335 , C07D213/38 , C07D307/52 , C07D333/20 , A61K31/44 , C07D213/36 , C07D207/323 , C07D307/56 , C07D333/28
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, Br, CN, NO2, SO2NH2, SO2NHR′ and SO2NR′2, where R′ is selected from linear or branched C1-C4 alkyl; X is selected from: F, Cl, C1-C3 alkyl, NH2 and OH Y is selected from: O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C1-C4 alkyl; Z is selected from: NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: H and linear or branched C1-C4 alkyl R5 is a residue selected from: H and linear or branched C1-C4 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 furyl and a substituted or not substituted pyridinyl. Said compounds are useful in the prevention and treatment of pathologies depending on TRPM8 activity such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, inflammatory conditions and urological disorders.
摘要翻译：作为瞬时受体电位阳离子通道亚族M成员8（以下称为TRPM8）的选择性拮抗剂的化合物，其具有式：其中R选自：H，Br，CN，NO 2，SO 2 NH 2，SO 2 NHR'和SO 2 NR 2，其中 R'选自直链或支链C 1 -C 4烷基; X选自：F，Cl，C 1 -C 3烷基，NH 2和OH Y选自：O，CH 2，NH和SO 2 R 1和R 2彼此独立地选自H，F和直链或支链C1 -C 1-4烷基; R 3和R 4彼此独立地选自H和直链或支链C 1 -C 4烷基; Z选自：NR 6和R 6 R 7 N +，其中R 6和R 7彼此独立地选自：H和直链或支链C 1 -C 4烷基R 5是选自以下的残基：H和直链或支链C 1 -C 4烷基Het是取代或未取代的N-甲基吡咯基，取代或未取代的噻吩基，取代或未取代的呋喃基和取代或未取代的吡啶基的杂芳基。所述化合物可用于预防和治疗根据TRPM8活性如疼痛，炎症，局部缺血，神经变性，中风，精神疾病，炎症状况和泌尿系统疾病的病理学。

3. 发明申请

US20140031398A1 TRPM8 RECEPTOR ANTAGONISTS 有权
标题翻译： TRPM8受体拮抗剂
公开(公告)号：US20140031398A1
公开(公告)日：2014-01-30
申请号：US13982235
申请日：2012-01-27
申请人： Alessio Moriconi , Gianluca Bianchini , Andrea Aramini , Laura Brandolini , Chiara Liberati , Silvia Bovolenta , Andrea Beccari , Simone Lorenzi
发明人： Alessio Moriconi , Gianluca Bianchini , Andrea Aramini , Laura Brandolini , Chiara Liberati , Silvia Bovolenta , Andrea Beccari , Simone Lorenzi
IPC分类号： C07D333/20 , C07D213/38 , C07D207/335 , C07D307/52
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, Br, CN, NO2, SO2NH2, SO2NHR′ and SO2NR′2, where R′ is selected from linear or branched C1-C4 alkyl; X is selected from: F, Cl, C1-C3 alkyl, NH2 and OH Y is selected from: O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C1-C4 alkyl; Z is selected from: NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: H and linear or branched C1-C4 alkyl R5 is a residue selected from: H and linear or branched C1-C4 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 furyl and a substituted or not substituted pyridinyl. Said compounds are useful in the prevention and treatment of pathologies depending on TRPM8 activity such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, inflammatory conditions and urological disorders.
摘要翻译：作为瞬时受体电位阳离子通道亚族M成员8（以下称为TRPM8）的选择性拮抗剂的化合物，其具有式：其中R选自：H，Br，CN，NO 2，SO 2 NH 2，SO 2 NHR'和SO 2 NR 2，其中 R'选自直链或支链C 1 -C 4烷基; X选自：F，Cl，C 1 -C 3烷基，NH 2和OH Y选自：O，CH 2，NH和SO 2 R 1和R 2彼此独立地选自H，F和直链或支链C1 -C 1-4烷基; R 3和R 4彼此独立地选自H和直链或支链C 1 -C 4烷基; Z选自：NR 6和R 6 R 7 N +，其中R 6和R 7彼此独立地选自：H和直链或支链C 1 -C 4烷基R 5是选自以下的残基：H和直链或支链C 1 -C 4烷基Het是取代或未取代的N-甲基吡咯基，取代或未取代的噻吩基，取代或未取代的呋喃基和取代或未取代的吡啶基的杂芳基。所述化合物可用于预防和治疗根据TRPM8活性如疼痛，炎症，局部缺血，神经变性，中风，精神疾病，炎症状况和泌尿系统疾病的病理学。

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