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公开(公告)号：US08552060B2
公开(公告)日：2013-10-08
申请号：US11922128
申请日：2006-06-13
申请人： Joseph Palumbo , Jonathan Sporn , Thomas Steckler , Yong Choi , James S. Lee
发明人： Joseph Palumbo , Jonathan Sporn , Thomas Steckler , Yong Choi , James S. Lee
IPC分类号： A61K31/24
CPC分类号： A61K31/165
摘要： This invention is directed to a method of treating sexual dysfunction in a subject, comprising the step of administering a therapeutically effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, CI, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R1 and R2 can be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R1 and R2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, wherein the cyclic compound can comprise 1 to 2 nitrogen atoms and O to 1 oxygen atom, wherein the nitrogen atoms are not directly connected with each other or with the oxygen atom.
摘要翻译： 本发明涉及治疗受试者的性功能障碍的方法，其包括施用治疗有效量的式（I）化合物或其药学上可接受的盐或酯的步骤，其中Rx是选自下组的成员 由氢，1至8个碳原子的低级烷基，选自F，Cl，Br和I的卤素，含有1至3个碳原子的烷氧基，硝基，羟基，三氟甲基和含有1至3个碳原子的硫代烷氧基组成; x为1〜3的整数，条件是当x为2或3时R可以相同或不同; R 1和R 2可以相同或不同，并且独立地选自氢，1至8个碳原子的低级烷基，芳基，芳基烷基，3至7个碳原子的环烷基; R1和R2可以连接形成被选自氢，烷基和芳基的成员所取代的5至7元杂环，其中环状化合物可包含1至2个氮原子和0至1个氧原子 其中氮原子彼此不直接连接或与氧原子直接连接。
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公开(公告)号：US08440715B2
公开(公告)日：2013-05-14
申请号：US11921995
申请日：2006-06-07
CPC分类号： C07C271/12 , A61K9/0053 , A61K31/165 , A61K31/27
摘要： This invention is directed to a method of treating Excessive daytime Sleepiness (EDS) in a subject, comprising the step of administering a therapeutically effective amount of a compound of Formula (I): Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R1 and R2 can be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R1 and R2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, wherein the cyclic compound can comprise 1 to 2 nitrogen atoms and 0 to 1 oxygen atom, wherein the nitrogen atoms are not directly connected with each other or with the ox en atom.
摘要翻译： 本发明涉及一种治疗受试者过度白昼睡眠（EDS）的方法，包括施用治疗有效量的式（I）化合物：式（I）或其药学上可接受的盐或酯的步骤，其中 Rx是选自氢，1至8个碳原子的低级烷基，选自F，Cl，Br和I的卤素，含有1至3个碳原子的烷氧基，硝基，羟基，三氟甲基和含有1个 至3个碳原子; x为1〜3的整数，条件是当x为2或3时R可以相同或不同; R 1和R 2可以相同或不同，并且独立地选自氢，1至8个碳原子的低级烷基，芳基，芳基烷基，3至7个碳原子的环烷基; R1和R2可以连接形成被选自氢，烷基和芳基的成员取代的5至7元杂环，其中环状化合物可包含1至2个氮原子和0至1个氧原子 ，其中氮原子彼此不直接连接或与氧原子直接连接。
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公开(公告)号：US08729120B2
公开(公告)日：2014-05-20
申请号：US11666521
申请日：2005-10-26
申请人： Jonathan Sporn
发明人： Jonathan Sporn
IPC分类号： A61K31/27 , A61K31/135 , A61K31/55 , A61K31/335
CPC分类号： A61K31/27 , A61K33/00 , A61K45/06 , A61K2300/00
摘要： This invention is directed to a method of treating depression in a subject, comprising the step of administering a therapeutically effective amount of a conventional antidepressant and, in addition, administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member Rx selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R1 and R2 can be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R1 and R2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, wherein the cyclic compound can comprise 1 to 2 nitrogen atoms and 0 to 1 oxygen atom, wherein the nitrogen atoms are not directly connected with each other or with the oxygen atom.
摘要翻译： 本发明涉及一种治疗受试者的抑郁症的方法，包括施用治疗有效量的常规抗抑郁药的步骤，此外，向受试者施用治疗有效量的式（I）化合物或 其药学上可接受的盐或酯，其中Rx是选自氢，1至8个碳原子的低级烷基，选自F，Cl，Br和I的卤素，含有1至3个碳原子的烷氧基，硝基， 羟基，三氟甲基和含有1至3个碳原子的硫代烷氧基; x为1〜3的整数，条件是当x为2或3时R可以相同或不同; R 1和R 2可以相同或不同，并且独立地选自氢，1至8个碳原子的低级烷基，芳基，芳基烷基，3至7个碳原子的环烷基; R1和R2可以连接形成被选自氢，烷基和芳基的成员取代的5至7元杂环，其中环状化合物可包含1至2个氮原子和0至1个氧原子 其中氮原子彼此不直接连接或与氧原子直接连接。
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公开(公告)号：US20080039529A1
公开(公告)日：2008-02-14
申请号：US11666521
申请日：2005-10-26
申请人： Jonathan Sporn
发明人： Jonathan Sporn
IPC分类号： A61K31/165 , A61P25/00
CPC分类号： A61K31/27 , A61K33/00 , A61K45/06 , A61K2300/00
摘要： This invention is directed to a method of treating depression in a subject, comprising the step of administering a therapeutically effective amount of a conventional antidepressant and, in addition, administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member Rx selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R1 and R2 can be the same or different each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R1 and R2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, wherein the cyclic compound can comprise 1 to 2 nitrogen atoms and 0 to 1 oxygen atom, wherein the nitrogen atoms are not directly connected with each other or with the oxygen atom.
摘要翻译： 本发明涉及一种治疗受试者的抑郁症的方法，包括施用治疗有效量的常规抗抑郁药的步骤，此外，向受试者施用治疗有效量的式（I）化合物或 其药学上可接受的盐或酯，其中Rx是选自氢，1至8个碳原子的低级烷基，选自F，Cl，Br和I的卤素，含有1至3个碳原子的烷氧基，硝基， 羟基，三氟甲基和含有1至3个碳原子的硫代烷氧基; x为1〜3的整数，条件是当x为2或3时R可以相同或不同; R 1和R 2可以彼此相同或不同，并且独立地选自氢，1至8个碳原子的低级烷基，芳基，芳烷基 3〜7个碳原子的环烷基; R 1和R 2可以连接形成被选自氢，烷基和芳基的成员所取代的5至7元杂环，其中 环状化合物可以包含1至2个氮原子和0至1个氧原子，其中氮原子彼此不连接或与氧原子直接相连。
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公开(公告)号：US20090312416A1
公开(公告)日：2009-12-17
申请号：US11921995
申请日：2006-06-07
CPC分类号： C07C271/12 , A61K9/0053 , A61K31/165 , A61K31/27
摘要： This invention is directed to a method of treating Excessive daytime Sleepiness (EDS) in a subject, comprising the step of administering a therapeutically effective amount of a compound of Formula (I): Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R1 and R2 can be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R1 and R2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, wherein the cyclic compound can comprise 1 to 2 nitrogen atoms and 0 to 1 oxygen atom, wherein the nitrogen atoms are not directly connected with each other or with the ox en atom.
摘要翻译： 本发明涉及一种治疗受试者过度白昼睡眠（EDS）的方法，包括施用治疗有效量的式（I）化合物：式（I）或其药学上可接受的盐或酯的步骤，其中 Rx是选自氢，1至8个碳原子的低级烷基，选自F，Cl，Br和I的卤素，含有1至3个碳原子的烷氧基，硝基，羟基，三氟甲基和含有1个 至3个碳原子; x为1〜3的整数，条件是当x为2或3时R可以相同或不同; R 1和R 2可以相同或不同，并且独立地选自氢，1至8个碳原子的低级烷基，芳基，芳基烷基，3至7个碳原子的环烷基; R1和R2可以连接形成被选自氢，烷基和芳基的成员取代的5至7元杂环，其中环状化合物可包含1至2个氮原子和0至1个氧原子 ，其中氮原子彼此不直接连接或与氧原子直接连接。
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公开(公告)号：US20090221553A1
公开(公告)日：2009-09-03
申请号：US11922128
申请日：2006-06-13
IPC分类号： A61K31/553 , A61K31/27 , A61K31/55 , A61P15/00
CPC分类号： A61K31/165
摘要： This invention is directed to a method of treating sexual dysfunction in a subject, comprising the step of administering a therapeutically effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, CI, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R1 and R2 can be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R1 and R2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, wherein the cyclic compound can comprise 1 to 2 nitrogen atoms and O to 1 oxygen atom, wherein the nitrogen atoms are not directly connected with each other or with the oxygen atom.
摘要翻译： 本发明涉及治疗受试者的性功能障碍的方法，其包括施用治疗有效量的式（I）化合物或其药学上可接受的盐或酯的步骤，其中Rx是选自下组的成员 由氢，1至8个碳原子的低级烷基，选自F，Cl，Br和I的卤素，含有1至3个碳原子的烷氧基，硝基，羟基，三氟甲基和含有1至3个碳原子的硫代烷氧基组成; x为1〜3的整数，条件是当x为2或3时R可以相同或不同; R 1和R 2可以相同或不同，并且独立地选自氢，1至8个碳原子的低级烷基，芳基，芳基烷基，3至7个碳原子的环烷基; R1和R2可以连接形成被选自氢，烷基和芳基的成员所取代的5至7元杂环，其中环状化合物可包含1至2个氮原子和0至1个氧原子 其中氮原子彼此不直接连接或与氧原子直接连接。
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