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1. 发明授权

US07098233B2 5-halo-tryptamine derivatives used as ligands on the 5-HT6 and/or 5-HT7 serotonin receptors 失效
标题翻译：用作5-HT6和/或5-HT7血清素受体的配体的5-卤素 - 色胺衍生物
公开(公告)号：US07098233B2
公开(公告)日：2006-08-29
申请号：US10481433
申请日：2002-06-17
申请人： Maria Assunta Di Cesare , Patrizia Minetti , Giorgio Tarzia , Gilberto Spadoni
发明人： Maria Assunta Di Cesare , Patrizia Minetti , Giorgio Tarzia , Gilberto Spadoni
IPC分类号： A61K31/405 , C07D209/196
CPC分类号： C07D209/16 , A61K31/405
摘要： Compounds of Formula (I): (I); wherein: R1 and R2 either the same or different, are H or linear or branched C1–C6 alkyl; R3=linear or branched C1–C6 alkyl; R4=halogen, and pharmaceutically acceptable salts thereof are useful as active ingredients in the preparation of medicaments used as ligands of the 5-HT6 and/or 5-HT7 serotoninergic receptors.
摘要翻译：式（I）的化合物：（I）; 其中：R 1和R 2相同或不同，为H或直链或支链C 1 -C 6 - 烷基; R 3 =直链或支链C 1 -C 6烷基; R 4 =卤素及其药学上可接受的盐可用作制备用作5-HT 6和/或5-HT 6配体的药物的活性成分， 5-羟色胺能受体。

2. 发明授权

US08791163B2 Melatonin ligands having antidepressant activity as well as sleep inducing properties 有权
标题翻译：具有抗抑郁活性的褪黑激素配体以及睡眠诱导性质
公开(公告)号：US08791163B2
公开(公告)日：2014-07-29
申请号：US12160728
申请日：2007-01-12
申请人： Gabriella Gobbi , Marco Mor , Silvia Rivara , Franco Fraschini , Giorgio Tarzia , Annalida Bedini , Gilberto Spadoni , Valeria Lucini
发明人： Gabriella Gobbi , Marco Mor , Silvia Rivara , Franco Fraschini , Giorgio Tarzia , Annalida Bedini , Gilberto Spadoni , Valeria Lucini
IPC分类号： A61K31/16 , C07C233/00 , C07C233/35
CPC分类号： C07C233/43 , C07C233/36
摘要： Novel melatonin ligands of Formula I: or pharmaceutically acceptable salts thereof wherein: n is 1 or 2; m is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, 6, 7 or 8; v is 2 or 3; A is aryl or heteroaryl; Z is O, S or NR8; Y is selected from the group consisting of hydrogen, aryl, heteroaryl, C1-C6 alkyl, C3-C6 cycloalkyl, and R is selected from the group consisting of hydrogen, hydroxyl, —OCF3, CF3, C1-C8 alkyl, C1-C8 alkyloxy, C1-C8 alkylthio, halogen and —Z—(CH2)p-A; R1 is selected from the group consisting of C1-C4 alkyl, C3-C6 cycloalkyl, CF3, hydroxy-substituted C1-C4 alkyl, hydroxy-substituted C3-C8 cycloalkyl, and NHR5, wherein R5 is C1-C3 alkyl or C3-C6 cycloalkyl; R2 is selected from the group consisting of: hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R3 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R and R3 may be connected together to form an —O—(CH2)v bridge representing with the carbon atoms to which they are attached a 5- or 6-membered heterocyclic ring system; R4 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R6 is selected from the group consisting of hydrogen and C1-C6 alkyl; R7 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; and R8 is selected from the group consisting of hydrogen and C1-C4 alkyl.
摘要翻译：式I的新型褪黑素配体：或其药学上可接受的盐，其中：n为1或2; m为0,1或2; p为0,1,2,3,4,5,6,7或8; v为2或3; A是芳基或杂芳基; Z是O，S或NR8; Y选自氢，芳基，杂芳基，C 1 -C 6烷基，C 3 -C 6环烷基，R选自氢，羟基，-OCF 3，CF 3，C 1 -C 8烷基，C 1 -C 8 烷氧基，C1-C8烷硫基，卤素和-Z-（CH2）pA; R 1选自C 1 -C 4烷基，C 3 -C 6环烷基，CF 3，羟基取代的C 1 -C 4烷基，羟基取代的C 3 -C 8环烷基和NHR 5，其中R 5是C 1 -C 3烷基或C 3 -C 6 环烷基 R 2选自：氢，C 1 -C 4烷基，C 1 -C 4烷氧基，OCF 3，CF 3，羟基和卤素; R 3选自氢，C 1 -C 4烷基，C 1 -C 4烷氧基，OCF 3，CF 3，羟基和卤素; R和R 3可以连接在一起形成一个-O-（CH 2）v桥，代表它们连接有5或6元杂环系的碳原子; R 4选自氢，C 1 -C 4烷基，C 1 -C 4烷氧基，OCF 3，CF 3，羟基和卤素; R 6选自氢和C 1 -C 6烷基; R 7选自氢，C 1 -C 4烷基，C 1 -C 4烷氧基，OCF 3，CF 3，羟基和卤素; 并且R 8选自氢和C 1 -C 4烷基。

3. 发明申请

US20100267836A1 NOVEL MELATONIN LIGANDS HAVING ANTIDEPRESSANT ACTIVITY AS WELL AS SLEEP INDUCING PROPERTIES 有权
标题翻译：具有抗静电活性的新型胶原蛋白配体，如睡眠诱导性质
公开(公告)号：US20100267836A1
公开(公告)日：2010-10-21
申请号：US12160728
申请日：2007-01-12
申请人： Gabriella Gobbi , Marco Mor , Silvia Rivara , Franco Fraschini , Giorgio Tarzia , Annalida Bedini , Gilberto Spadoni , Valeria Lucini
发明人： Gabriella Gobbi , Marco Mor , Silvia Rivara , Franco Fraschini , Giorgio Tarzia , Annalida Bedini , Gilberto Spadoni , Valeria Lucini
IPC分类号： A61K31/165 , C07C233/05 , A61P25/22 , A61P25/24
CPC分类号： C07C233/43 , C07C233/36
摘要： Novel melatonin ligands of Formula I: or pharmaceutically acceptable salts thereof wherein: n is 1 or 2; m is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, 6, 7 or 8; v is 2 or 3; A is aryl or heteroaryl; Z is O, S or NR8; Y is selected from the group consisting of hydrogen, aryl, heteroaryl, C1-C6 alkyl, C3-C6 cycloalkyl, and R is selected from the group consisting of hydrogen, hydroxyl, —OCF3, CF3, C1-C8 alkyl, C1-C8 alkyloxy, C1-C8 alkylthio, halogen and —Z—(CH2)p-A; R1 is selected from the group consisting of C1-C4 alkyl, C3-C6 cycloalkyl, CF3, hydroxy-substituted C1-C4 alkyl, hydroxy-substituted C3-C8 cycloalkyl, and NHR5, wherein R5 is C1-C3 alkyl or C3-C6 cycloalkyl; R2 is selected from the group consisting of: hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R3 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R and R3 may be connected together to form an —O—(CH2)v bridge representing with the carbon atoms to which they are attached a 5- or 6-membered heterocyclic ring system; R4 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R6 is selected from the group consisting of hydrogen and C1-C6 alkyl; R7 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; and R8 is selected from the group consisting of hydrogen and C1-C4 alkyl.
摘要翻译：式I的新型褪黑素配体：或其药学上可接受的盐，其中：n为1或2; m为0,1或2; p为0,1,2,3,4,5,6,7或8; v为2或3; A是芳基或杂芳基; Z是O，S或NR8; Y选自氢，芳基，杂芳基，C 1 -C 6烷基，C 3 -C 6环烷基，R选自氢，羟基，-OCF 3，CF 3，C 1 -C 8烷基，C 1 -C 8 烷氧基，C1-C8烷硫基，卤素和-Z-（CH2）pA; R 1选自C 1 -C 4烷基，C 3 -C 6环烷基，CF 3，羟基取代的C 1 -C 4烷基，羟基取代的C 3 -C 8环烷基和NHR 5，其中R 5是C 1 -C 3烷基或C 3 -C 6 环烷基 R 2选自：氢，C 1 -C 4烷基，C 1 -C 4烷氧基，OCF 3，CF 3，羟基和卤素; R 3选自氢，C 1 -C 4烷基，C 1 -C 4烷氧基，OCF 3，CF 3，羟基和卤素; R和R 3可以连接在一起形成一个-O-（CH 2）v桥，代表它们连接有5或6元杂环系的碳原子; R 4选自氢，C 1 -C 4烷基，C 1 -C 4烷氧基，OCF 3，CF 3，羟基和卤素; R 6选自氢和C 1 -C 6烷基; R 7选自氢，C 1 -C 4烷基，C 1 -C 4烷氧基，OCF 3，CF 3，羟基和卤素; 并且R 8选自氢和C 1 -C 4烷基。

4. 发明申请

US20150045442A1 NOVEL MELATONIN LIGANDS HAVING ANTIDEPRESSANT ACTIVITY AS WELL AS SLEEP INDUCING PROPERTIES 审中-公开
标题翻译：具有抗静电活性的新型胶原蛋白配体，如睡眠诱导性质
公开(公告)号：US20150045442A1
公开(公告)日：2015-02-12
申请号：US14304473
申请日：2014-06-13
申请人： Gabriella GOBBI , Marco MOR , Silvia RIVARA , Franco FRASCHINI , Giorgio TARZIA , Annalida BEDINI , Gilberto SPADONI , Valeria LUCINI
发明人： Gabriella GOBBI , Marco MOR , Silvia RIVARA , Franco FRASCHINI , Giorgio TARZIA , Annalida BEDINI , Gilberto SPADONI , Valeria LUCINI
IPC分类号： C07C233/43
CPC分类号： C07C233/43 , C07C233/36
摘要： Novel melatonin ligands of Formula I: or pharmaceutically acceptable salts thereof wherein: n is 1 or 2; m is 0, 1 or 2; p is 0, 1, 2, 3, 4, 5, 6, 7 or 8; v is 2 or 3; A is aryl or heteroaryl; Z is O, S or NR8; Y is selected from the group consisting of hydrogen, aryl, heteroaryl, C1-C6 alkyl, C3-C6 cycloalkyl, and R is selected from the group consisting of hydrogen, hydroxyl, —OCF3, CF3, C1-C8 alkyl, C1-C8 alkyloxy, C1-C8 alkylthio, halogen and —Z—(CH2)p-A; R1 is selected from the group consisting of C1-C4 alkyl, C3-C6 cycloalkyl, CF3, hydroxy-substituted C1-C4 alkyl, hydroxy-substituted C3-C6 cycloalkyl, and NHR5, wherein R5 is C1-C3 alkyl or C3-C6 cycloalkyl; R2 is selected from the group consisting of: hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R3 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R and R3 may be connected together to form an —O—(CH2)v bridge representing with the carbon atoms to which they are attached a 5- or 6-membered heterocyclic ring system; R4 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; R6 is selected from the group consisting of hydrogen and C1-C6 alkyl; R7 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkyloxy, OCF3, CF3, hydroxyl, and halogen; and R8 is selected from the group consisting of hydrogen and C1-C4 alkyl.
摘要翻译：式I的新型褪黑素配体：或其药学上可接受的盐，其中：n为1或2; m为0,1或2; p为0,1,2,3,4,5,6,7或8; v为2或3; A是芳基或杂芳基; Z是O，S或NR8; Y选自氢，芳基，杂芳基，C 1 -C 6烷基，C 3 -C 6环烷基，R选自氢，羟基，-OCF 3，CF 3，C 1 -C 8烷基，C 1 -C 8 烷氧基，C1-C8烷硫基，卤素和-Z-（CH2）pA; R 1选自C 1 -C 4烷基，C 3 -C 6环烷基，CF 3，羟基取代的C 1 -C 4烷基，羟基取代的C 3 -C 6环烷基和NHR 5，其中R 5是C 1 -C 3烷基或C 3 -C 6 环烷基 R 2选自：氢，C 1 -C 4烷基，C 1 -C 4烷氧基，OCF 3，CF 3，羟基和卤素; R 3选自氢，C 1 -C 4烷基，C 1 -C 4烷氧基，OCF 3，CF 3，羟基和卤素; R和R 3可以连接在一起形成一个-O-（CH 2）v桥，代表它们连接有5或6元杂环系的碳原子; R 4选自氢，C 1 -C 4烷基，C 1 -C 4烷氧基，OCF 3，CF 3，羟基和卤素; R 6选自氢和C 1 -C 6烷基; R 7选自氢，C 1 -C 4烷基，C 1 -C 4烷氧基，OCF 3，CF 3，羟基和卤素; 并且R 8选自氢和C 1 -C 4烷基。

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