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1.发明授权
公开(公告)号：US5418234A
公开(公告)日：1995-05-23
申请号：US298494
申请日：1994-08-30
IPC分类号： A61K31/495 , C07D403/12 , A61K31/50
CPC分类号： C07D403/12 , A61K31/495 , Y10S514/816 , Y10S514/854 , Y10S514/93
摘要： A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.4 are independently selected from the group consisting of H and alkyl radicals having 1 to 4 carbon atoms; the R.sub.2 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R.sub.3 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the 2-imidazolin-2-ylamino group may be in any of the 5-, 6, 7- or 8-positions of the quinoxaline nucleus; and R.sub.5, R.sub.6 and R.sub.7 each is located in one of the remaining 5-, 6-, 7- or 8-positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals having 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain and reduction in or prevention of at least one effect of ischemia.
摘要翻译： 治疗哺乳动物的方法包括向哺乳动物施用有效量以在哺乳动物中提供所需治疗效果，所述化合物选自下列化合物：具有下式的那些化合物：其药学上可接受的酸加成盐及其混合物， 其中R 1和R 4独立地选自H和具有1至4个碳原子的烷基; R 2独立地选自H或具有1至4个碳原子的烷基，或者一起是氧代; R 3独立地选自H或具有1至4个碳原子的烷基，或者一起是氧代; 2-咪唑啉-2-基氨基可以在喹喔啉核的5-，6-或7-位中的任一个中; 并且R5，R6和R7各自位于喹喔啉核的剩余的5-，6-，7-或8-位中的一个，并且独立地选自Cl，Br，H和具有1至 3个碳原子。 当向哺乳动物施用时，这些化合物提供期望的治疗效果，例如减少外周疼痛和减少或预防至少一种局部缺血的作用。
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2.发明授权
公开(公告)号：US5373010A
公开(公告)日：1994-12-13
申请号：US195184
申请日：1994-02-10
IPC分类号： A61K31/495 , C07D403/12 , A61K31/50
CPC分类号： C07D403/12 , A61K31/495 , Y10S514/816 , Y10S514/854 , Y10S514/93
摘要： A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## , pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.4 are independently selected from the group consisting of H and alkyl radicals having 1 to 4 carbon atoms; the R.sub.2 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R.sub.3 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the 2-imidazolin-2-ylamino group may be in any of the 5-, 6, 7- or 8- positions of the quinoxaline nucleus; and R.sub.5, R.sub.6 and R.sub.7 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals having 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as constriction of one or more blood vessels and decongestion of one or more nasal passages.
摘要翻译： 治疗哺乳动物的方法包括向哺乳动物施用有效量以在哺乳动物中提供选自下列化合物的化合物所需的治疗效果：具有下式的那些化合物：其药学上可接受的酸加成盐及其混合物 其中R 1和R 4独立地选自H和具有1至4个碳原子的烷基; R 2独立地选自H或具有1至4个碳原子的烷基，或者一起是氧代; R 3独立地选自H或具有1至4个碳原子的烷基，或者一起是氧代; 2-咪唑啉-2-基氨基可以在喹喔啉核的5-,6,7或8-位中的任一个中; 并且R5，R6和R7各自位于喹喔啉核的剩余的5-，6-，7-或8-位中的一个中，并且独立地选自Cl，Br，H和具有1至 3个碳原子。 当向哺乳动物施用时，这些化合物提供所需的治疗效果，例如一个或多个血管的收缩和一个或多个鼻通道的减充血。
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3.发明授权
公开(公告)号：US5231096A
公开(公告)日：1993-07-27
申请号：US820329
申请日：1992-01-13
IPC分类号： C07D403/12 , A61K31/495 , A61P7/10 , A61P9/08 , A61P9/10 , A61P27/02
CPC分类号： C07D403/12 , A61K31/495 , Y10S514/816
摘要： A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## ,pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.4 are independently selected from the group consisting of H and alkyl radicals having 1 to 4 carbon atoms; the R.sub.2 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R.sub.3 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the 2-imidazolin-2-ylamino group may be in any of the 5-, 6, 7- or 8- positions of the quinoxaline nucleus; and R.sub.5, R.sub.6 and R.sub.7 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals having 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain, anesthetization of the central nervous system, constriction of one or more blood vessels, reduction in or prevention of at least one effect of ischemia, decongestion of one or more nasal passages, and reduction of at least one effect of an inflammatory disorder.
摘要翻译： 治疗哺乳动物的方法包括向哺乳动物施用有效量以在哺乳动物中提供选自下列化合物的化合物所需的治疗效果：具有下式的那些化合物：其药学上可接受的酸加成盐及其混合物 其中R 1和R 4独立地选自H和具有1至4个碳原子的烷基; R 2独立地选自H或具有1至4个碳原子的烷基，或者一起是氧代; R 3独立地选自H或具有1至4个碳原子的烷基，或者一起是氧代; 2-咪唑啉-2-基氨基可以在喹喔啉核的5-,6,7或8-位中的任一个中; 并且R5，R6和R7各自位于喹喔啉核的剩余的5-，6-，7-或8-位中的一个中，并且独立地选自Cl，Br，H和具有1至 3个碳原子。 当向哺乳动物施用时，这些化合物提供期望的治疗效果，例如减少周围疼痛，中枢神经系统麻醉，一个或多个血管的收缩，减少或预防至少一种缺血作用，减压 一个或多个鼻通道，以及减少至少一种炎症性疾病的作用。
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4.发明授权
公开(公告)号：US5326763A
公开(公告)日：1994-07-05
申请号：US10954
申请日：1993-01-29
IPC分类号： A61K31/495 , C07D403/12 , A61K31/50
CPC分类号： C07D403/12 , A61K31/495 , Y10S514/816 , Y10S514/854 , Y10S514/93
摘要： A method of treating a mammal comprises administering to a mammal an effective amount to provide a reduction inflammation in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.4 are independently selected from the group consisting of H and alkyl radicals having 1 to 4 carbon atoms; the R.sub.2 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R.sub.3 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the 2-imidazolin-2-ylamino group may be in any of the 5-, 6, 7- or 8- positions of the quinoxaline nucleus; and R.sub.5, R.sub.6 and R.sub.7 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals having 1 to 3 carbon atoms.
摘要翻译： 治疗哺乳动物的方法包括向哺乳动物施用有效量以在哺乳动物中提供选自下列化合物的化合物的还原性炎症：具有下式的那些化合物：其药学上可接受的酸加成盐及其混合物，其中 R 1和R 4独立地选自H和具有1至4个碳原子的烷基; R 2独立地选自H或具有1至4个碳原子的烷基，或者一起是氧代; R 3独立地选自H或具有1至4个碳原子的烷基，或者一起是氧代; 2-咪唑啉-2-基氨基可以在喹喔啉核的5-,6,7或8-位中的任一个中; 并且R5，R6和R7各自位于喹喔啉核的剩余的5-，6-，7-或8-位中的一个中，并且独立地选自Cl，Br，H和具有1至 3个碳原子。
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5.发明授权
公开(公告)号：US5756503A
公开(公告)日：1998-05-26
申请号：US636740
申请日：1996-04-19
IPC分类号： C07D401/12 , A61K31/495 , A61K31/498 , A61P1/12 , A61P1/14 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/02 , A61P13/02 , A61P13/12 , A61P15/00 , A61P23/00 , A61P23/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P27/16 , A61P29/00 , C07D403/12
CPC分类号： A61K31/498 , A61K31/495
摘要： A method of treating a mammal is disclosed comprising administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.2 each is selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8- positions of the quinoxaline nucleus, and R.sub.3, R.sub.4 and R.sub.5 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain.
摘要翻译： 公开了一种治疗哺乳动物的方法，其包括向哺乳动物施用有效量以在哺乳动物中提供期望的治疗效果，所述化合物选自具有下式的那些化合物及其药学上可接受的酸加成盐，以及 其混合物，其中R 1和R 2各自选自含有1至4个碳原子的烷基和含有1至4个碳原子的烷氧基，2-咪唑啉-2-基氨基可以是5- 喹喔啉核的6-，7-或8-位，并且R3，R4和R5各自位于喹喔啉核的剩余的5-，6-，7-或8-位之一，并且独立地选自 由Cl，Br，H组成的组和含有1至3个碳原子的烷基。 当向哺乳动物施用时，这些化合物提供期望的治疗效果，例如减少外周疼痛。
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6.发明授权
公开(公告)号：US5561132A
公开(公告)日：1996-10-01
申请号：US390265
申请日：1995-02-15
IPC分类号： C07D401/12 , A61K31/495 , A61K31/498 , A61P1/12 , A61P1/14 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/02 , A61P13/02 , A61P13/12 , A61P15/00 , A61P23/00 , A61P23/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P27/16 , A61P29/00 , C07D403/12
CPC分类号： A61K31/498 , A61K31/495
摘要： A method of treating a mammal comprising administering an effective amount of a compound of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, is disclosed wherein R.sub.1 and R.sub.2 each is selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8- positions of the quinoxaline nucleus, and R.sub.3, R.sub.4 and R.sub.5 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms wherein the desired therapeutic effect is an alteration in the rate of fluid transport in the gastrointestinal tract.
摘要翻译： 公开了一种治疗哺乳动物的方法，其包括施用有效量的下式化合物及其药学上可接受的酸加成盐及其混合物，其中R 1和R 2各自选自含有1个 至4个碳原子和含有1至4个碳原子的烷氧基，2-咪唑啉-2-基氨基可以在喹喔啉核中的5-，6-，7-或8-位任何一个，R3，R4 并且R 5各自位于喹喔啉核的剩余的5-，6-，7-或8-位之一，并且独立地选自Cl，Br，H和含有1至3个碳原子的烷基，其中 期望的治疗效果是胃肠道中流体输送速率的改变。
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7.发明授权公开(公告)号：US06323204B1
公开(公告)日：2001-11-27
申请号：US09222844
申请日：1998-12-30
IPC分类号： A61K31495
CPC分类号： A61K31/495 , A61K31/498
摘要： A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R1 and R2 each is selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8-positions of the quinoxaline nucleus, and R3, R4 and R5 each is located in one of the remaining 5-, 6-, 7- or 8-positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide desired therapeutic effects, such as reduction in peripheral pain.
摘要翻译： 治疗哺乳动物的方法包括向哺乳动物施用有效量以在哺乳动物中提供所需治疗效果，所述化合物选自具有下式的那些化合物：及其药学上可接受的酸加成盐及其混合物，其中R 1 并且R 2各自选自含有1至4个碳原子的烷基和含有1至4个碳原子的烷氧基，2-咪唑啉-2-基氨基可以在5-，6-，7- - 或8-位的喹喔啉核，R3，R4和R5各自位于喹喔啉核的剩余的5-，6-，7-或8-位之一，并且独立地选自Cl ，Br，H和含有1至3个碳原子的烷基。 当向哺乳动物施用时，这些化合物提供期望的治疗效果，例如减少外周疼痛。
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8.发明授权
公开(公告)号：US5552403A
公开(公告)日：1996-09-03
申请号：US332029
申请日：1994-10-31
IPC分类号： C07D401/12 , A61K31/495 , A61K31/498 , A61P1/12 , A61P1/14 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/02 , A61P13/02 , A61P13/12 , A61P15/00 , A61P23/00 , A61P23/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P27/16 , A61P29/00 , C07D403/12
CPC分类号： A61K31/498 , A61K31/495
摘要： A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.2 each is independently selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8-positions of the quinoxaline nucleus, and R.sub.3, R.sub.4 and R.sub.5 each is located in one of the remaining 5-, 6-, 7- or 8-positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms. Such compounds, when administered to a mammal, provide treatment for ischemia.
摘要翻译： 治疗哺乳动物的方法包括向哺乳动物施用有效量以在哺乳动物中提供选自下列化合物的化合物所需的治疗效果：具有下式的那些化合物及其药学上可接受的酸加成盐及其混合物 其中R 1和R 2各自独立地选自含有1至4个碳原子的烷基和含有1至4个碳原子的烷氧基，2-咪唑啉-2-基氨基可以是5-， 喹喔啉核的6-，7-或8-位，且R 3，R 4和R 5各自位于喹喔啉核的剩余的5-，6-，7-或8-位之一，并独立地选自 由Cl，Br，H组成的基团和含有1至3个碳原子的烷基。 当向哺乳动物施用时，这些化合物提供缺血治疗。
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公开(公告)号：US06841684B2
公开(公告)日：2005-01-11
申请号：US09815362
申请日：2001-03-21
申请人： Ken Chow , Daniel W. Gil , James A. Burke , Dale A. Harcourt , Michael E. Garst , Larry A. Wheeler , Stephen A. Munk , Dario G. Gomez , Todd M. Heidelbaugh
发明人： Ken Chow , Daniel W. Gil , James A. Burke , Dale A. Harcourt , Michael E. Garst , Larry A. Wheeler , Stephen A. Munk , Dario G. Gomez , Todd M. Heidelbaugh
IPC分类号： C07D233/58 , A61K31/4164 , A61K31/4178 , A61K31/421 , A61K31/435 , A61K31/4709 , A61K31/4725 , A61K31/498 , A61K31/538 , A61P1/12 , A61P7/12 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P25/02 , A61P25/04 , A61P25/14 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/06 , A61P27/16 , A61P43/00 , C07D233/06 , C07D233/10 , C07D233/54 , C07D233/64 , C07D233/84 , C07D263/28 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/12 , C07D495/04
CPC分类号： C07D233/56 , C07D233/06 , C07D233/10 , C07D233/64 , C07D233/84 , C07D263/28 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/12 , C07D495/04
摘要： Methods and compounds for the treatment of conditions including pain, particularly chronic pain, glaucoma or elevated intraocular pressure with reduced cardiovascular or sedative side effects. Also included are methods of making and using such compounds.
摘要翻译： 用于治疗包括疼痛，特别是慢性疼痛，青光眼或升高的眼内压，降低心血管或镇静剂副作用的病症的方法和化合物。 还包括制备和使用这些化合物的方法。
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10.发明授权
公开(公告)号：US5773440A
公开(公告)日：1998-06-30
申请号：US880473
申请日：1997-06-23
IPC分类号： C07D401/12 , A61K31/495 , A61K31/498 , A61P1/12 , A61P1/14 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/02 , A61P13/02 , A61P13/12 , A61P15/00 , A61P23/00 , A61P23/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P27/16 , A61P29/00 , C07D403/12
CPC分类号： A61K31/498 , A61K31/495
摘要： A method of treating a mammal is disclosed comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## , and pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.2 each is selected from the group consisting of alkyl radicals containing 1 to 4 carbon atoms and alkoxy radicals containing 1 to 4 carbon atoms, the 2-imidazolin-2-ylamino group may be in any of the 5-, 6-, 7- or 8-positions of the quinoxaline nucleus, and R.sub.3, R.sub.4 and R.sub.5 each is located in one of the remaining 5-, 6-, 7- or 8-positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals containing 1 to 3 carbon atoms wherein said desired therapeutic effect is a reduction of at least one effect of an inflammatory disorder.
摘要翻译： 公开了治疗哺乳动物的方法包括向哺乳动物施用有效量以在哺乳动物中提供期望的治疗效果，所述化合物选自下列化合物：具有下式的那些化合物及其药学上可接受的酸加成盐 和其混合物，其中R 1和R 2各自选自含有1至4个碳原子的烷基和含有1至4个碳原子的烷氧基，2-咪唑啉-2-基氨基可以是5 喹喔啉核的6-，7-或8-位，并且R3，R4和R5各自位于喹喔啉核的剩余的5-，6-，7-或8-位之一中，并且独立选择 来自由Cl，Br，H组成的组和含有1至3个碳原子的烷基，其中所述期望的治疗效果是减少至少一种炎性病症的作用。
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