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1. 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。

2. 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。

3. 发明申请

US20120316169A1 2-ARYL-PROPIONAMIDE DERIVATIVES USEFUL AS BRADYKININ RECEPTOR ANTAGONISTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：作为BRADYKININ受体拮抗剂和含有它们的药物组合物有用的2-ARYL-PROPNAAMIDE衍生物
公开(公告)号：US20120316169A1
公开(公告)日：2012-12-13
申请号：US13504535
申请日：2010-10-28
申请人： Andrea Beccari , Andrea Aramini , Gianluca Bianchini , Alessio Moriconi
发明人： Andrea Beccari , Andrea Aramini , Gianluca Bianchini , Alessio Moriconi
IPC分类号： A61K31/255 , C07D231/12 , A61K31/415 , C07D213/74 , A61K31/4402 , C07D211/58 , A61K31/4468 , C07D239/42 , A61K31/505 , C07D413/12 , A61K31/5377 , C07D417/14 , A61P25/04 , A61P29/00 , A61P11/00 , A61P17/00 , A61P7/10 , A61P9/00 , A61P1/00 , A61P25/00 , A61P9/04 , A61P25/28 , A61P9/10 , A61P25/08 , A61P25/06 , A61P35/00 , A61P19/10 , A61P13/10 , A61P11/06 , A61P11/08 , A61P11/02 , A61P1/02 , A61P17/06 , A61P25/16 , C07C309/66
CPC分类号： C07C235/34 , C07C233/40 , C07C235/78 , C07C237/20 , C07C271/22 , C07C275/50 , C07C309/65 , C07C311/08 , C07C311/46 , C07C2601/14 , C07D207/04 , C07D211/58 , C07D213/40 , C07D213/89 , C07D231/12 , C07D231/38 , C07D239/42 , C07D263/48 , C07D277/42 , C07D277/46 , C07D295/125 , C07D307/52 , C07D333/22 , C07D409/12 , C07D413/12
摘要： (R,S) 2-aryl-propionamide derivatives, or their single enantiomers (R) and (S) are disclosed useful in the treatment or prevention of symptoms and disorders such as pain and inflammation associated with the bradykinin B1 pathway.
摘要翻译：（R，S）2-芳基 - 丙酰胺衍生物或其单一对映体（R）和（S）可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状和病症。

4. 发明授权

US08026367B2 (R)-arylalkylamino derivatives and pharmaceutical compositions containing them 有权
标题翻译：（R）芳基烷基氨基衍生物和含有它们的药物组合物
公开(公告)号：US08026367B2
公开(公告)日：2011-09-27
申请号：US12094837
申请日：2006-11-24
申请人： Marcello Allegretti , Alessio Moriconi , Andrea Aramini , Maria Candida Cesta , Andrea Beccari , Riccardo Bertini
发明人： Marcello Allegretti , Alessio Moriconi , Andrea Aramini , Maria Candida Cesta , Andrea Beccari , Riccardo Bertini
IPC分类号： C07D417/00 , A01N43/40
CPC分类号： C07C311/21 , C07C233/76 , C07C309/65 , C07C311/03 , C07D213/70 , C07D213/76 , C07D277/42 , C07D295/108 , C07D295/15 , C07D307/52 , C07D307/68 , C07D333/34
摘要： The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
摘要翻译：本发明涉及式（I）的选择的（R） - 芳基烷基氨基衍生物，其中R，R 1和Ar如权利要求中所定义。这些化合物显示出对C5a诱导的人类PMN趋化性的惊人的有效抑制作用。本发明化合物绝对缺乏CXCL8抑制活性。所述化合物可用于治疗病理学，这取决于由补体的级分C5a诱导的嗜中性粒细胞和单核细胞的趋化活化。特别地，本发明的化合物可用于治疗败血症，牛皮癣，类风湿性关节炎，溃疡性结肠炎，急性呼吸窘迫综合征，特发性纤维化，肾小球性肾炎，以及预防和治疗由缺血和再灌注引起的损伤。

5. 发明申请

US20090124664A1 (R)-Arylalkylamino Derivatives and Pharmaceutical Compositions Containing Them 有权
标题翻译：（R） - 芳基烷基氨基衍生物和含有它们的药物组合物
公开(公告)号：US20090124664A1
公开(公告)日：2009-05-14
申请号：US12094837
申请日：2006-11-24
申请人： Marcello Allegretti , Alessio Moriconi , Andrea Aramini , Maria Candida Cesta , Andrea Beccari , Riccardo Bertini
发明人： Marcello Allegretti , Alessio Moriconi , Andrea Aramini , Maria Candida Cesta , Andrea Beccari , Riccardo Bertini
IPC分类号： A61K31/4453 , C07C309/64 , A61K31/185 , C07D213/71 , A61K31/44 , C07C311/00 , A61K31/18 , C07D333/34 , A61K31/426 , A61P7/00 , A61P11/00 , A61P9/10 , A61P19/02 , C07D277/42 , A61K31/381 , C07D207/04 , A61K31/40 , C07D307/64 , A61K31/341 , C07D211/32
CPC分类号： C07C311/21 , C07C233/76 , C07C309/65 , C07C311/03 , C07D213/70 , C07D213/76 , C07D277/42 , C07D295/108 , C07D295/15 , C07D307/52 , C07D307/68 , C07D333/34
摘要： The present invention relates to selected (R)-arylalkylamino derivatives of formula (I), in which R, R1 and Ar are as defined in the claims. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
摘要翻译：本发明涉及式（I）的选择的（R） - 芳基烷基氨基衍生物，其中R，R 1和Ar如权利要求中所定义。这些化合物显示出对C5a诱导的人类PMN趋化性的惊人的有效抑制作用。本发明化合物绝对缺乏CXCL8抑制活性。所述化合物可用于治疗病理学，这取决于由补体的级分C5a诱导的嗜中性粒细胞和单核细胞的趋化活化。特别地，本发明的化合物可用于治疗败血症，牛皮癣，类风湿性关节炎，溃疡性结肠炎，急性呼吸窘迫综合征，特发性纤维化，肾小球性肾炎，以及预防和治疗由缺血和再灌注引起的损伤。

6. 发明申请

US20080312293A1 2-Arylpropionic Acid Derivatives and Pharmaceutical Compositions Containing Them 有权
标题翻译： 2-芳基丙酸衍生物和含有它们的药物组合物
公开(公告)号：US20080312293A1
公开(公告)日：2008-12-18
申请号：US11721971
申请日：2005-12-13
申请人： Marcello Allegretti , Riccardo Bertini , Andrea Beccari , Alessio Moriconi , Andrea Aramini , Cinzia Bizzarri , Francesco Colotta
发明人： Marcello Allegretti , Riccardo Bertini , Andrea Beccari , Alessio Moriconi , Andrea Aramini , Cinzia Bizzarri , Francesco Colotta
IPC分类号： A61K31/341 , C07D277/56 , C07D213/72 , C07D307/40 , A61P19/02 , A61P1/00 , A61K31/426 , A61K31/44
CPC分类号： C07D307/46 , C07C233/66 , C07C235/34 , C07C235/78 , C07C237/20 , C07C237/22 , C07C311/51 , C07C317/44 , C07C2601/08 , C07D213/74 , C07D213/75 , C07D263/32 , C07D277/24 , C07D307/80
摘要： The present invention relates to selected (R)-2-phenyl-propionamides and (R)-2-phenyl-sulfonamides with a hydrogen bond acceptor atom/group in a well defined position in the chemical space. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
摘要翻译：本发明涉及选择的（R）-2-苯基 - 丙酰胺和（R）-2-苯基磺酰胺，其具有在化学空间中明确定义的位置的氢键受体原子/基团。这些化合物显示出对C5a诱导的人类PMN趋化性的惊人的有效抑制作用。本发明化合物绝对缺乏CXCL8抑制活性。所述化合物可用于治疗病理学，这取决于由补体的级分C5a诱导的嗜中性粒细胞和单核细胞的趋化活化。特别地，本发明的化合物可用于治疗败血症，牛皮癣，类风湿性关节炎，溃疡性结肠炎，急性呼吸窘迫综合征，特发性纤维化，肾小球性肾炎，以及预防和治疗由缺血和再灌注引起的损伤。

7. 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。

8. 发明授权

US07939521B2 2-arylpropionic acid derivatives and pharmaceutical compositions containing them 有权
标题翻译： 2-芳基丙酸衍生物和含有它们的药物组合物
公开(公告)号：US07939521B2
公开(公告)日：2011-05-10
申请号：US11721971
申请日：2005-12-13
申请人： Marcello Allegretti , Riccardo Bertini , Andrea Beccari , Alessio Moriconi , Andrea Aramini , Cinzia Bizzarri , Francesco Colotta
发明人： Marcello Allegretti , Riccardo Bertini , Andrea Beccari , Alessio Moriconi , Andrea Aramini , Cinzia Bizzarri , Francesco Colotta
IPC分类号： A61K31/55 , C07D487/00
CPC分类号： C07D307/46 , C07C233/66 , C07C235/34 , C07C235/78 , C07C237/20 , C07C237/22 , C07C311/51 , C07C317/44 , C07C2601/08 , C07D213/74 , C07D213/75 , C07D263/32 , C07D277/24 , C07D307/80
摘要： The present invention relates to selected (R)-2-phenyl-propionamides and (R)-2-phenyl-sulfonamides with a hydrogen bond acceptor atom/group in a well defined position in the chemical space. These compounds show a surprising potent inhibitory effect on C5a induced human PMN chemotaxis. The compounds of the invention absolutely lack of CXCL8 inhibitory activity. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of sepsis, psoriasis, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
摘要翻译：本发明涉及选择的（R）-2-苯基 - 丙酰胺和（R）-2-苯基磺酰胺，其具有在化学空间中明确定义的位置的氢键受体原子/基团。这些化合物显示出对C5a诱导的人类PMN趋化性的惊人的有效抑制作用。本发明化合物绝对缺乏CXCL8抑制活性。所述化合物可用于治疗病理学，这取决于由补体的级分C5a诱导的嗜中性粒细胞和单核细胞的趋化活化。特别地，本发明的化合物可用于治疗败血症，牛皮癣，类风湿性关节炎，溃疡性结肠炎，急性呼吸窘迫综合征，特发性纤维化，肾小球性肾炎，以及预防和治疗由缺血和再灌注引起的损伤。

9. 发明授权

US08133911B2 (R)-4-(heteroaryl) phenylethyl derivatives and pharmaceutical compositions containing them 有权
标题翻译：（R）-4-（杂芳基）苯基乙基衍生物和含有它们的药物组合物
公开(公告)号：US08133911B2
公开(公告)日：2012-03-13
申请号：US12681841
申请日：2008-10-17
申请人： Alessio Moriconi , Andrea Aramini
发明人： Alessio Moriconi , Andrea Aramini
IPC分类号： A61K31/4174 , A61K31/422 , A61K31/427 , C07D233/88 , C07D263/48 , C07D277/38
CPC分类号： C07D417/12 , C07D413/12
摘要： The present invention relates to a novel class of (R)-4-(heteroaryl)phenylpropionic derivatives of formula (I), useful in the inhibition of the chemotactic activation induced by the fraction C5a of complement. Said compounds are useful in the treatment of pathologies depending on the chemotactic activation of neutrophils and monocytes induced by the fraction C5a of the complement. In particular, the compounds of the invention are useful in the treatment of autoimmune hemolytic anemia (AIHA), psoriasis, bullous pemphigoid, rheumatoid arthritis, ulcerative colitis, acute respiratory distress syndrome, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of injury caused by ischemia and reperfusion.
摘要翻译：本发明涉及一类新颖的式（I）的（R）-4-（杂芳基）苯基丙酸衍生物，其可用于抑制补体级分C5a诱导的趋化活化。所述化合物可用于治疗病理学，这取决于由补体的级分C5a诱导的嗜中性粒细胞和单核细胞的趋化活化。特别地，本发明的化合物可用于治疗自身免疫性溶血性贫血（AIHA），牛皮癣，大疱性类天疱疮，类风湿性关节炎，溃疡性结肠炎，急性呼吸窘迫综合征，特发性纤维化，肾小球性肾炎，以及预防和治疗造成的损伤通过缺血和再灌注。

10. 发明授权

US07652169B2 (2R)-2-[(4-sulfonyl) aminophenyl] propanamides and pharmaceutical compositions containing them 有权
公开(公告)号：US07652169B2
公开(公告)日：2010-01-26
申请号：US12227519
申请日：2007-05-17
申请人： Marcello Allegretti , Riccardo Bertini , Cinzia Bizzarri , Maria Candida Cesta , Andrea Aramini , Alessio Moriconi
发明人： Marcello Allegretti , Riccardo Bertini , Cinzia Bizzarri , Maria Candida Cesta , Andrea Aramini , Alessio Moriconi
IPC分类号： C07C303/00 , A01N41/06
CPC分类号： C07C311/08 , C07B2200/07 , C07C311/09 , C07C311/13 , C07C311/14 , C07C311/21 , C07C311/29 , C07C2601/02 , C07C2601/08 , C07D277/46 , C07D333/34
摘要： The present invention relates to novel (2R)-2-phenylpropanamides bearing a 4-sulfonylamino substituent on the 4 position of the phenyl group and to pharmaceutical compositions containing them, which are used as inhibitors of the chemotaxis of polymorphonucleate and mononucleate cells, and which are useful in the treatment of various ELR+CXC chemokine-mediated disorders. In particular, the compounds of the invention are useful in the treatment and control of specific CXCR2 dependent pathologies such as BOS, COPD, angiogenesis and melanoma.

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